Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science

Drug Solubulity and Delivery Systems

Works Count: 49919

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Description

This cluster of papers focuses on the advances in drug delivery systems, including the use of cyclodextrins, solid dispersions, nanosuspensions, and lipid-based formulations to improve drug solubility and enhance oral delivery. It also explores the application of the Biopharmaceutics Classification System and the development of amorphous pharmaceuticals for improved drug absorption. The research covers a wide range of topics related to pharmaceutical materials and gastrointestinal drug absorption.

Keywords

Cyclodextrins; Solid Dispersions; Nanosuspensions; Lipid-Based Formulations; Drug Solubility; Oral Delivery; Biopharmaceutics Classification System; Amorphous Pharmaceuticals; Polymeric Materials; Gastrointestinal Drug Absorption

Insoluble drug delivery strategies: review of recent advances and business prospects

2015-08-25

Sandeep Kalepu , Vijaykumar Nekkanti

The emerging trends in the combinatorial chemistry and drug design have led to the development of drug candidates with greater lipophilicity, high molecular weight and poor water solubility. Majority of … The emerging trends in the combinatorial chemistry and drug design have led to the development of drug candidates with greater lipophilicity, high molecular weight and poor water solubility. Majority of the failures in new drug development have been attributed to poor water solubility of the drug. Issues associated with poor solubility can lead to low bioavailability resulting in suboptimal drug delivery. About 40% of drugs with market approval and nearly 90% of molecules in the discovery pipeline are poorly water-soluble. With the advent of various insoluble drug delivery technologies, the challenge to formulate poorly water soluble drugs could be achieved. Numerous drugs associated with poor solubility and low bioavailabilities have been formulated into successful drug products. Several marketed drugs were reformulated to improve efficacy, safety and patient compliance. In order to gain marketing exclusivity and patent protection for such products, revitalization of poorly soluble drugs using insoluble drug delivery technologies have been successfully adopted by many pharmaceutical companies. This review covers the recent advances in the field of insoluble drug delivery and business prospects.

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A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability.

1995-01-01

Gordon L. Amidon , Hans Lennernäs , Vinod P. Shah +1 more

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Encyclopedia of Pharmaceutical Technology

2013-07-01

James Swarbrick

Presenting authoritative and engaging articles on all aspects of drug development, dosage, manufacturing, and regulation, this Third Edition enables the pharmaceutical specialist and novice alike to keep abreast of developments … Presenting authoritative and engaging articles on all aspects of drug development, dosage, manufacturing, and regulation, this Third Edition enables the pharmaceutical specialist and novice alike to keep abreast of developments in this rapidly evolving and highly competitive field. A dependable reference tool and constant companion for years to com

Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms.

1998-01-01

Jennifer Dressman , Gordon L. Amidon , Christos Reppas +1 more

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Pharmaceutics : the science of dosage form design

2002-01-01

Michael E. Aulton

What is the true solubility advantage for amorphous pharmaceuticals?

2000-01-01

Bruno C. Hancock , Michael Parks

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

1999-10-01

Abu T.M. Serajuddin

Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention

2000-02-03

Baljinder Singh

Pharmaceutical Quality by Design: Product and Process Development, Understanding, and Control

2008-01-09

Lawrence X. Yu

Nanosizing: a formulation approach for poorly-water-soluble compounds

2003-02-01

Elaine Merisko‐Liversidge , Gary G. Liversidge , Eugene R. Cooper

Amorphous pharmaceutical solids: preparation, characterization and stabilization

2001-05-01

Lian Yu

Cyclodextrin Drug Carrier Systems

1998-06-09

Kaneto Uekama , Fumitoshi Hirayama , Tetsumi Irie

ADVERTISEMENT RETURN TO ISSUEPREVArticleCyclodextrin Drug Carrier SystemsKaneto Uekama, Fumitoshi Hirayama, and Tetsumi IrieView Author Information Faculty of Pharmaceutical Sciences, Kumamoto University, 5-1, Oe-honmachi, Kumamoto 862-0973, Japan Cite this: Chem. Rev. … ADVERTISEMENT RETURN TO ISSUEPREVArticleCyclodextrin Drug Carrier SystemsKaneto Uekama, Fumitoshi Hirayama, and Tetsumi IrieView Author Information Faculty of Pharmaceutical Sciences, Kumamoto University, 5-1, Oe-honmachi, Kumamoto 862-0973, Japan Cite this: Chem. Rev. 1998, 98, 5, 2045–2076Publication Date (Web):June 9, 1998Publication History Received16 October 1997Revised5 January 1998Published online9 June 1998Published inissue 30 July 1998https://doi.org/10.1021/cr970025pCopyright © 1998 American Chemical SocietyRIGHTS & PERMISSIONSArticle Views13329Altmetric-Citations1726LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InReddit Read OnlinePDF (324 KB) Get e-AlertsSUBJECTS:Absorption,Macrocyclic compounds,Oligosaccharides,Peptides and proteins,Pharmaceuticals Get e-Alerts

Determination of Tablet Strength by the Diametral-Compression Test

1970-05-01

John T. Fell , John Newton

Understanding Pharmaceutical Quality by Design

2014-05-22

Lawrence X. Yu , Gregory E. Amidon , Mansoor A. Khan +4 more

Mathematical modeling of drug delivery

2008-09-12

Juergen Siepmann , F. Siepmann

Cyclodextrins and their pharmaceutical applications

2006-11-10

Þorsteinn Loftsson , Dominique Duchêne

Nanosizing — Oral formulation development and biopharmaceutical evaluation

2007-05-26

Filippos Kesisoglou , Santipharp Panmai , Yunhui Wu

Drug nanocrystals of poorly soluble drugs produced by high pressure homogenisation

2005-08-30

Cornelia M. Keck , Robert Müller

Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals

1995-07-01

Tugrul T. Kararli

Abstract In addition to metabolic differences, the anatomical, physiological, and biochemical differences in the gastrointestinal (G.I.) tract of the human and common laboratory animals can cause significant variation in drug … Abstract In addition to metabolic differences, the anatomical, physiological, and biochemical differences in the gastrointestinal (G.I.) tract of the human and common laboratory animals can cause significant variation in drug absorption from the oral route. Among the physiological factors, pH, bile, pancreatic juice, and mucus and fluid volume and content can modify dissolution rates, solubility, transit times, and membrane transport of drug molecules. The microbial content of the G.I. tract can significantly affect the reductive metabolism and enterohepatic circulation of drugs and colonic delivery of formulations. The transit time of dosage forms can be significantly different between species due to different dimensions and propulsive activities of the G.I. tract. The lipid/protein composition of the enterocyte membrane along the G.I. tract can alter binding and passive, active, and carrier‐mediated transport of drugs. The location and number of Peyer's patches can also be important in the absorption of large molecules and particulate matter. While small animals, rats, mice, guinea pigs, and rabbits, are most suitable for determining the mechanism of drug absorption and bioavailability values from powder or solution formulations, larger animals, dogs, pigs, and monkeys, are used to assess absorption from formulations. The understanding of physiological, anatomical, and biochemical differences between the G.I. tracts of different animal species can lead to the selection of the correct animal model to mimic the bioavailability of compounds in the human. This article reviews the anatomical, physiological, and biochemical differences between the G.I. tracts of humans and commonly used laboratory animals.

Review: A History of Cyclodextrins

2014-09-23

Grégorio Crini

ADVERTISEMENT RETURN TO ISSUEPREVReviewNEXTReview: A History of CyclodextrinsGrégorio Crini*View Author Information Faculté Sciences & Techniques, UMR Chrono-environnement 6249, Université de Franche-Comté, 16 Route de Gray, 25030, Besançon Cedex, France*E-mail: [email … ADVERTISEMENT RETURN TO ISSUEPREVReviewNEXTReview: A History of CyclodextrinsGrégorio Crini*View Author Information Faculté Sciences & Techniques, UMR Chrono-environnement 6249, Université de Franche-Comté, 16 Route de Gray, 25030, Besançon Cedex, France*E-mail: [email protected]Cite this: Chem. Rev. 2014, 114, 21, 10940–10975Publication Date (Web):September 23, 2014Publication History Received10 February 2014Published online23 September 2014Published inissue 12 November 2014https://pubs.acs.org/doi/10.1021/cr500081phttps://doi.org/10.1021/cr500081preview-articleACS PublicationsCopyright © 2014 American Chemical SocietyRequest reuse permissionsArticle Views23298Altmetric-Citations1382LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose SUBJECTS:Cadmium sulfide,Carbohydrates,Macrocyclic compounds,Molecules,Oligosaccharides Get e-Alerts

Pharmaceutical Applications of Solid Dispersion Systems

1971-09-01

Win L. Chiou , Sidney Riegelman

Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and ‘self-microemulsifying’ drug delivery systems

2000-10-01

Colin W. Pouton

Improving drug solubility for oral delivery using solid dispersions

2000-07-03

C Leuner

Cyclodextrin-based pharmaceutics: past, present and future

2004-12-01

Mark E. Davis , Marcus E. Brewster

Pharmaceutical Applications of Cyclodextrins. III. Toxicological Issues and Safety Evaluation

1997-02-01

Tetsumi Irie , Kaneto Uekama

Nanosuspensions in drug delivery

2004-09-01

Barrett Rabinow

Formulation of poorly water-soluble drugs for oral administration: Physicochemical and physiological issues and the lipid formulation classification system

2006-05-19

Colin W. Pouton

Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC)

2001-06-11

Juergen Siepmann , Nicholas A. Peppas

Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs

2004-03-14

R. Neslihan Gürsoy , Simon Benita

Cyclodextrins in drug delivery: An updated review

2005-06-01

Rajeswari Challa , Alka Ahuja , Javed Ali +1 more

Cyclodextrins as pharmaceutical solubilizers

2007-05-30

Marcus E. Brewster , Þorsteinn Loftsson

Characteristics and Significance of the Amorphous State in Pharmaceutical Systems

1997-01-01

Bruno C. Hancock , George Zografi

On the importance and mechanisms of burst release in matrix-controlled drug delivery systems

2001-06-01

Xiao Huang , Christopher S. Brazel

Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs

2007-12-01

Teófilo Vasconcelos , Bruno Sarmento , Paulo Costa

Caco-2 monolayers in experimental and theoretical predictions of drug transport1PII of original article: S0169-409X(96)00415-2. The article was originally published in Advanced Drug Delivery Reviews 22 (1996) 67–84.1

2001-03-01

Per Artursson , Katrin Palm , Kristina Luthman

Mechanism of sustained‐action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices

1963-12-01

Tsunehiko Higuchi

Modeling and comparison of dissolution profiles

2001-05-01

Paulo Costa , José Manuel Sousa Lobo

Cyclodextrins and their uses: a review

2003-10-11

Eva M. Martín del Valle

Strategies to Address Low Drug Solubility in Discovery and Development

2013-01-01

Hywel D. Williams , Natalie L. Trevaskis , Susan A. Charman +4 more

Drugs with low water solubility are predisposed to low and variable oral bioavailability and, therefore, to variability in clinical response. Despite significant efforts to "design in" acceptable developability properties (including … Drugs with low water solubility are predisposed to low and variable oral bioavailability and, therefore, to variability in clinical response. Despite significant efforts to "design in" acceptable developability properties (including aqueous solubility) during lead optimization, approximately 40% of currently marketed compounds and most current drug development candidates remain poorly water-soluble. The fact that so many drug candidates of this type are advanced into development and clinical assessment is testament to an increasingly sophisticated understanding of the approaches that can be taken to promote apparent solubility in the gastrointestinal tract and to support drug exposure after oral administration. Here we provide a detailed commentary on the major challenges to the progression of a poorly water-soluble lead or development candidate and review the approaches and strategies that can be taken to facilitate compound progression. In particular, we address the fundamental principles that underpin the use of strategies, including pH adjustment and salt-form selection, polymorphs, cocrystals, cosolvents, surfactants, cyclodextrins, particle size reduction, amorphous solid dispersions, and lipid-based formulations. In each case, the theoretical basis for utility is described along with a detailed review of recent advances in the field. The article provides an integrated and contemporary discussion of current approaches to solubility and dissolution enhancement but has been deliberately structured as a series of stand-alone sections to allow also directed access to a specific technology (e.g., solid dispersions, lipid-based formulations, or salt forms) where required.

Pharmaceutical particle technologies: An approach to improve drug solubility, dissolution and bioavailability

2014-06-13

Prakash Khadka , Jieun Ro , Hyeongmin Kim +6 more

Pharmaceutical particle technology is employed to improve poor aqueous solubility of drug compounds that limits in vivo bioavailability owing to their low dissolution rate in the gastrointestinal fluids following oral … Pharmaceutical particle technology is employed to improve poor aqueous solubility of drug compounds that limits in vivo bioavailability owing to their low dissolution rate in the gastrointestinal fluids following oral administration. The particle technology involves several approaches from the conventional size reduction processes to the newer, novel particle technologies that modify the solubility properties of the drugs and produce solid, powdered form of the drugs that are readily soluble in water and can be easily formulated into various dosage forms. This review highlights the solid particle technologies available for improving solubility, dissolution and bioavailability of drugs with poor aqueous solubility.

Solubilizing Excipients in Oral and Injectable Formulations

2004-02-01

Robert G. Strickley

The mechanisms of drug release from solid dispersions in water-soluble polymers

2002-01-01

Duncan Q.M. Craig

Drug Solubility: Importance and Enhancement Techniques

2012-07-05

Ketan T. Savjani , Anuradha K. Gajjar , Jignasa Savjani

Solubility, the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the important parameters to achieve desired concentration of drug in systemic circulation for … Solubility, the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the important parameters to achieve desired concentration of drug in systemic circulation for desired (anticipated) pharmacological response. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. More than 40% NCEs (new chemical entities) developed in pharmaceutical industry are practically insoluble in water. Solubility is a major challenge for formulation scientist. Any drug to be absorbed must be present in the form of solution at the site of absorption. Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation, and so forth. Selection of solubility improving method depends on drug property, site of absorption, and required dosage form characteristics.

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Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: Basic approaches and practical applications

2011-08-31

Yohei Kawabata , Koichi Wada , Manabu Nakatani +2 more

Cyclodextrins and their inclusion complexes

1982-01-01

Eva Smolková-Keulemansová

Handbook of Pharmaceutical Excipients

1987-08-01

Flynn W. Warren

Journal Article Handbook of Pharmaceutical Excipients Get access Handbook of Pharmaceutical Excipients Published by the American Pharmaceutical Association, 2215 Constitution Ave., N.W., Washington, DC 20037, and The Pharmaceutical Society of … Journal Article Handbook of Pharmaceutical Excipients Get access Handbook of Pharmaceutical Excipients Published by the American Pharmaceutical Association, 2215 Constitution Ave., N.W., Washington, DC 20037, and The Pharmaceutical Society of Great Britain, 1 Lambeth High St., London SE1 7JN, England, 1986. xi + 375 p. Price $110. Flynn Warren, M.S. Flynn Warren, M.S. College of Pharmacy, The University of Georgia, Athens, GA 30602 Search for other works by this author on: Oxford Academic Google Scholar American Journal of Hospital Pharmacy, Volume 44, Issue 8, 1 August 1987, Pages 1946–1948, https://doi.org/10.1093/ajhp/44.8.1946 Published: 01 August 1987

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Salt formation to improve drug solubility

2007-05-30

Abu T.M. Serajuddin

Kinetic modeling on drug release from controlled drug delivery systems.

2010-06-09

Suvakanta Dash , P. N. Murthy , Lilakanta Nath +1 more

In this paper we review the mathematical models used to determine the kinetics of drug release from drug delivery systems. The quantitative analysis of the values obtained in dissolution/release rates … In this paper we review the mathematical models used to determine the kinetics of drug release from drug delivery systems. The quantitative analysis of the values obtained in dissolution/release rates is easier when mathematical formulae are used to describe the process. The mathematical modeling can ultimately help to optimize the design of a therapeutic device to yield information on the efficacy of various release models.

Cyclodextrins and their inclusion complexes

1982-01-01

József Szejtli

Formulation and Characterization of Methyldopa Floating Tablets Using Polymeric Excipients: A Study on Gastroretentive Drug Delivery System

2025-06-25

Amaresh Prusty , Chinmaya Keshari Sahoo , Snigdha Senapati +2 more | Jordan Journal of Pharmaceutical Sciences

This research aims to develop a novel gastro retentive drug delivery system (GRDDS) that can prolong the drug release of methyldopa. In the present research tablets are prepared by direct … This research aims to develop a novel gastro retentive drug delivery system (GRDDS) that can prolong the drug release of methyldopa. In the present research tablets are prepared by direct compression method using carbapol 934 and HPMC K100M polymer, by the use effervescent (for Formulations F1, F2, F3, and F4) and non-effervescent (F5) technology. One of the medications used to treat hypertension is methyldopa, a sympatholytic drug that acts centrally having short half-life of 2 h. Sedation, nausea, and vomiting are some of the drug's side effects that occur as a result of its frequency of its administration (250 mg two to three times day). Therefore, it would be far more effective to prepare GRDDS of methyldopa to release drug in the gastric environment for an extended duration. F3 is the most effective formulation batch because the combination of polymers HPMC K 100M and carbopol 934 in methyldopa effervescent tablets significantly prolongs the drug release in 0.1N HCl for more than 12 hours with a floating lag time of 60 seconds. The drug release mechanism reveals a new approach to treat hypertension with methyldopa floating tablets by utilising a mixture of HPMC K 100 M and carbopol 934 polymers.

Comparative analyses of Weibull model and conventional kinetics models of drug release of formulated multi-component tablets

2025-06-24

Maha Al-Ali | Al-Qadisiyah Journal for Engineering Sciences

The Kinetics study of drug release is an essential requirement to examine the capability of the drug formulation to modulate with the typical drug release profile. In the present work, … The Kinetics study of drug release is an essential requirement to examine the capability of the drug formulation to modulate with the typical drug release profile. In the present work, hence, Weibull model and other traditional drug release models are selected to investigate the release of tablets prepared using different drying techniques in a simulated abdominal solution. These tablets are prepared using electromagnetic microwave irradiation tablet (MVT), convective drying (CVT), freeze drying (FRT), vacuum drying (VAT), and that without drying process (NDT). This study aims to compare the Weibull models with other conventional drug release models in inspecting the kinetics of the drug release of all tablets. These models are the Zero-Order, Higuchi, First-Order, Hixson-Crowell, and Korsmeyer-Peppas. This work delves into the best kinetic model that defined the tablets' release mechanisms including the new multi-component tablets (MVT), to ensure their releases are on appropriate behavior. The results show that the Weibull model is the best model to present the release profile of all tablets except for MVT and VAT tablets, while Higuchi gets the optimal model. Among the conventional models, Higuchi, Korsmeyer-Peppas, and Hixon-Crowell are the best conventional models that fit all types of tablets. Based on the Weibull model factor, non-Fickian diffusion is the dominant release mechanism for NDT and VAT. Though Fick diffusion controls the drug release mechanism of FTR, CVT, and MVT tablets. Additionally, three modified models were created and found to be more convenient to denote the release of the formulated tablets with very high accuracy.

Thermodynamic Perspectives on the Impact of a Second Drug on Amorphous Drug Solubility

2025-06-23

Shun Kaneko , Keisuke Ueda , Rei Hakata +4 more | Molecular Pharmaceutics

Drug amorphous solubility can be changed in the presence of other compounds, making it essential to elucidate the underlying mechanisms for designing supersaturated formulations. In this study, we experimentally determined … Drug amorphous solubility can be changed in the presence of other compounds, making it essential to elucidate the underlying mechanisms for designing supersaturated formulations. In this study, we experimentally determined how a second drug affects the amorphous solubility of ritonavir (RTV) and analyzed these effects from a thermodynamic perspective. Lopinavir (LPV), cilnidipine (CND), and probucol (PBC) were used as second drugs. The coexistence of each second drug in an aqueous solution reduced the amorphous solubility of RTV. In the presence of LPV and CND, the experimentally determined RTV amorphous solubility was close to the value predicted under the assumption of ideal mixing of RTV and second drugs. In contrast, in the presence of PBC, the experimentally determined RTV amorphous solubility exceeded the predicted value. Dynamic vapor sorption (DVS) measurements revealed that the RTV/LPV coamorphous absorbed water similarly to amorphous RTV. Conversely, water absorption in the RTV/CND and RTV/PBC coamorphous decreased compared with amorphous RTV. Using the experimentally determined amorphous solubilities and water absorption data, the interaction parameters between RTV and each second drug within the water-saturated drug-rich phase were calculated. The absolute value of the interaction parameter in the RTV/LPV system is relatively small, suggesting that incorporating LPV into the RTV-rich phase had minimal impact on water absorption and drug-drug interaction strength in the RTV-rich phase, resulting in experimentally determined solubility values that align closely with those predicted by ideal mixing of RTV and LPV. Meanwhile, the interaction parameters of the RTV/CND and RTV/PBC systems were negative, indicating relatively strong drug-drug interactions that can further reduce RTV amorphous solubility. However, for these two systems, the mixing of second drugs also decreased the water content in the RTV-rich phase, which would mitigate the extent of the solubility reduction. In the RTV/CND system, the strong drug-drug interaction and reduced water content largely offset each other. This results in an experimentally determined RTV amorphous solubility similar to the value predicted by the ideal mixing of RTV and CND. In contrast, in the RTV/PBC system, the water content of the RTV-rich phase was more substantially decreased, leading to a higher experimentally determined value of RTV amorphous solubility than that predicted by ideal mixing of RTV and PBC. Overall, this study elucidates the impact of a second drug on the amorphous solubility of a primary drug and provides valuable insights for the design of supersaturated formulations containing multiple drugs.

The Chemical Stability Characterization and Kinetics of Statins in Aqueous Cyclodextrin Ocular Preparations: A Formulation Perspective

2025-06-23

Ismael Abo Horan , Þorsteinn Loftsson , Hákon Hrafn Sigurðsson | Pharmaceutics

Background: Topical statin therapy holds promise for ocular diseases, such as age-related macular degeneration, but the effective delivery to the posterior segment is limited by poor aqueous solubility, chemical instability, … Background: Topical statin therapy holds promise for ocular diseases, such as age-related macular degeneration, but the effective delivery to the posterior segment is limited by poor aqueous solubility, chemical instability, and ocular barriers. Cyclodextrins (CDs) can enhance statin solubility and stability; however, the behavior of CD–statin complexes in aqueous eye drops—particularly their influence on the equilibrium between the inactive lactone (ring closed) and active hydroxyacid forms (ring open)—remains unclear. This study aimed to (i) investigate how 5% and 10% (w/v) concentrations of selected CDs affect the lactone/acid equilibrium of simvastatin and atorvastatin and (ii) define formulation parameters (statin form, CD type and concentration, and pH range) for stable eye drop development. Methods: Simvastatin or atorvastatin was added to buffered solutions (pH 2.0 to pH 9.5) of RMβCD, HPβCD, γ-CD, or SBEβCD at 0%, 5%, and 10% (w/v), incubated at 23 ± 1 °C, and sampled over time for UPLC quantification of lactone and hydroxyacid forms, and rate constants for the forward and reverse reaction were calculated. Phase solubility studies were also conducted to further characterize equilibrium behavior in aqueous CD systems. Results: The lactone form was most stable at a pH of 4.5, while the hydroxyacid form prevailed at a pH ≥ 7. γ-CD and HPβCD accelerated lactone hydrolysis for both statins, whereas RMβCD exerted a stabilizing effect. Increasing the CD concentration from 5% to 10% provided minimal additional stabilization. Conclusions: These findings highlight that the precise control of the pH, an appropriate cyclodextrin choice, and the selection of the statin form are critical to developing chemically stable eye drops.

Comparative Bioavailability Study of Jaspine B: Impact of Nanoliposomal Drug Delivery System on Pharmacokinetics

2025-06-22

Biwash Ghimire , P.G. Shankar Giri , Sameena Mateen +2 more | Pharmaceutics

Background/Objectives: Jaspine B, a synthetic analog of anhydrophytosphingosine, demonstrates significant anticancer activity; however, its clinical application is hindered by its poor oral bioavailability, resulting in suboptimal systemic exposure. This study … Background/Objectives: Jaspine B, a synthetic analog of anhydrophytosphingosine, demonstrates significant anticancer activity; however, its clinical application is hindered by its poor oral bioavailability, resulting in suboptimal systemic exposure. This study aimed to enhance the pharmacokinetic properties of Jaspine B by developing a liposomal delivery system. Methods: Jaspine B-loaded liposomes were formulated using a microfluidic approach and characterized by transmission electron microscopy (TEM) to assess particle morphology and size distribution. A sensitive and selective LC-MS/MS assay was developed and fully validated to quantify Jaspine B in rat plasma. The assay revealed excellent linearity across a broad concentration range and high intra- and inter-day precision. A pharmacokinetic study was conducted in Sprague Dawley rats to evaluate the influence of liposomal encapsulation on the pharmacokinetic profile of Jaspine B. Results: The liposomal formulation accelerated the absorption of Jaspine B, reaching the maximum concentration (Tmax) at 2 h as opposed to 6 h in plain Jaspine B. The half-life (t1/2) increased significantly from 7.9 ± 2.3 h to 26.7 ± 7.3 h. The area under the curve (AUC0–∞) increased over two-fold from 56.8 ± 12.3 ng.h/mL to 139.7 ± 27.2 ng.h/mL, suggesting increased systemic drug exposure. Similarly, the drug molecule’s mean residence time (MRT) increased over three-fold. Conclusions: These results indicate that liposomal formulation enhances the pharmacokinetics of Jaspine B, prolonging its body circulation and exposure, which explains the improved therapeutic outcomes we observed in our previous pharmacodynamic study.

Pharmaceutical Solid Form Screening and Selection: Which Form Emerges?

2025-06-22

Praveen Chappa , Ramesh Naidu Jenjeti , Jakob Kljun +3 more | Crystal Growth & Design

Evaluation of Vibratory Ball Mill Mixing as an Alternative to Wet Granulation in the Manufacturing of Sodium Naproxen Tablets with Dolomite-Based Formulations

2025-06-20

Mateusz Przywara , Klaudia Jękot , Wiktoria Jednacz | Applied Sciences

The development of robust and scalable tablet manufacturing methods remains a key objective in pharmaceutical technology, especially when dealing with active pharmaceutical ingredients (APIs) and excipients that exhibit suboptimal processing … The development of robust and scalable tablet manufacturing methods remains a key objective in pharmaceutical technology, especially when dealing with active pharmaceutical ingredients (APIs) and excipients that exhibit suboptimal processing properties. This study evaluated two alternative manufacturing strategies for tablets containing sodium naproxen (20%, API), dolomite (65%, sustainable mineral filler), cellulose (7%), polyvinylpyrrolidone (5%, binder), and magnesium stearate (3%, lubricant). The direct compression method used a vibrating ball mill (SPEX SamplePrep 8000M), while the indirect method employed wet granulation using a pan granulator at different inclination angles. Physical properties of raw materials and granules were assessed, and final tablets were evaluated for mass, thickness, mechanical resistance, abrasiveness, and API content uniformity. Direct compression using vibratory mixing for 5–10 min (DT2, DT3) resulted in average tablet masses close to the target (0.260 g) and improved reproducibility compared to a reference V-type blender. Wet granulation produced tablets with the lowest abrasiveness (<1.0%) and minimal variability in dimensions and API content. The best uniformity (SD < 0.5%) was observed in batch IT2. Overall, vibratory mixing proved capable of achieving tablet quality comparable to that of wet granulation, while requiring fewer processing steps. This highlights its potential as an efficient and scalable alternative in solid dosage manufacturing.

Formulation and evaluation of stiripentol oral suspension

2025-06-20

Ujjwala Kandekar , Dinesh Bitale , Limbaji Chounde +1 more | Ars Pharmaceutica (Internet)

Introducción: El trabajo de investigación se llevó a cabo para desarrollar una suspensión estable y eficaz de estiripentol para el tratamiento de la epilepsia. Método: Se utilizó el estudio FT-IR … Introducción: El trabajo de investigación se llevó a cabo para desarrollar una suspensión estable y eficaz de estiripentol para el tratamiento de la epilepsia. Método: Se utilizó el estudio FT-IR para evaluar la compatibilidad entre el fármaco y el excipiente y también se examinó la apariencia física de la mezcla del fármaco y el excipiente después de un mes de estudio de estabilidad. La suspensión se preparó mediante un agitador mecánico y se evaluó la viscosidad, el pH, el volumen de sedimentación, el potencial zeta y los estudios de liberación de fármaco in vitro. La formulación optimizada se evaluó adicionalmente para determinar el potencial zeta y el índice de polidispersidad. Resultados: Los resultados de FT-IR confirmaron la compatibilidad del fármaco y los excipientes. La apariencia física de la mezcla no se alteró durante las condiciones de almacenamiento aceleradas. La viscosidad, el pH y el volumen de sedimentación de la formulación oscilaron entre 22,92 ±1,2 cPs y 54,8 ± 2,1 cPs; 5,32 ± 0,04 y 6,01 ± 0,1 y 83,19 ± 0,9 % y 98,87 ± 1,2 % respectivamente. El potencial zeta y el índice de polidispersidad de la formulación optimizada fueron -52,1 mV y 0,198 respectivamente. Estos resultados fueron indicativos de una suspensión monodispersa estable. La formulación optimizada fue estable a temperaturas y humedad más altas y en presencia de luz, lo que indica una buena vida útil. Conclusiones: El estudio demostró que la suspensión oral de estiripentol puede formularse como una forma farmacéutica estable y eficaz para el tratamiento de la epilepsia.

Statistical Formulation Optimization of Naproxen Microsponges with Eudragit RS100 for Sustained Drug Release

2025-06-19

Sonia Gupta , Himanshu Chopra , Prabhjot Singh Bajwa +1 more | Journal of Pharmaceutical Innovation

Impact of Permeation Enhancers on the Release of Insulin from Tablets in Biorelevant Media

2025-06-17

Andrew Fagan , Lorraine M. Bateman , Abina M. Crean +2 more | Molecular Pharmaceutics

The use of chemical permeation enhancers (PEs) to improve the permeation of peptides across gastric and intestinal epithelia has proven an effective strategy in the development of oral dosage forms … The use of chemical permeation enhancers (PEs) to improve the permeation of peptides across gastric and intestinal epithelia has proven an effective strategy in the development of oral dosage forms of peptides. However, there remains a poor understanding of how the presence of PEs impacts the dissolution characteristics of oral formulations containing peptides, nor is it known how the complex composition of biological media can influence their behavior in vivo. This investigation sought to examine the effect of two widely studied PEs, sodium caprate (C10) and salcaprozate sodium (SNAC), on the release behavior of a model peptide, insulin, from minitablets in a variety of biorelevant media. First, the equilibrium solubilities of insulin, C10, and SNAC were determined in simulated gastric and intestinal media. Insulin, C10, and SNAC all displayed pH-dependent solubility across a physiologically relevant range of pH conditions. Moreover, at high concentrations, C10 was found to overwhelm the buffer capacity of the simulated media, increasing the pH of fasted state simulated intestinal fluid (FaSSIF) from 6.5 to 9.0, fed state simulated intestinal fluid (FeSSIF) from pH 5.0 to 8.8 and fasted state simulated gastric fluid (FaSSGF) from pH 1.6 to 9.2. Similarly, SNAC caused an increase in the pH of FaSSIF from 6.5 to 7.9, FeSSIF from pH 5.0 to 7.7, and FaSSGF from pH 1.6 to 7.6. Relative to in simulated intestinal media, the solubility of insulin was found to increase significantly in media at pH representative of saturated C10 and SNAC solutions, increasing from 0.1 mg/mL in blank FaSSIF to 14.0 mg/mL in phosphate buffer at pH 7.6 and to 23.7 mg/mL in phosphate buffer at pH 9.2, suggesting that the presence of C10 and SNAC at high concentrations could have a considerable favorable impact on insulin solubility. Furthermore, the release profiles of insulin from minitablets containing C10 and SNAC were investigated in each of the biorelevant media and compared with the release profiles of insulin from blank minitablets in the absence of PEs. Insulin release from the blank minitablets was found to be media dependent, following an apparent solubility trend. Complete release of insulin was observed in simulated gastric media; however, only between 67 and 82% release was observed in the simulated intestinal media. On the other hand, on the addition of C10 and SNAC to the formulation, greater than 90% release was observed across all media investigated. This difference in release behavior was determined to be caused by an increase in pH at the surface of the minitablets due to the presence of high local concentrations of C10 and SNAC, respectively, as confirmed by a change in color of a universal indicator solution. These findings offer a key insight into the influence that C10 and SNAC have on the dissolution characteristics of insulin from an oral dosage form in a variety of simulated gastric and intestinal media.

Formulation and Evaluation of Buoyant tablets loaded with Nanosponges containing entrapped Cefditoren pivoxil

2025-06-17

Naga Raju Kandukoori , Gundegani Saikumar , B Deepika +1 more | Research Square (Research Square)

<title>Abstract</title> Background The main objective of this research was to develop a novel gastroretentive formulation for Cefditoren pivoxil, an insoluble and poorly permeable drug. Floating and drug release characteristics of … <title>Abstract</title> Background The main objective of this research was to develop a novel gastroretentive formulation for Cefditoren pivoxil, an insoluble and poorly permeable drug. Floating and drug release characteristics of tablets formulated with pure Cefditoren pivoxil were compared with the same of formulations loaded with nanosponges (NS) form of drug. Results Test results related to physicochemical properties of all prepared tablets were observed to be in compliance with standards. More floating lag time and less log time have been resulted from the formulations with pure form of drug (F1 to F4), whereas, vice-versa was found with NS based dosage forms (F5 to F8). An evaluation test for in-vitro drug release was performed for all the dosage units and more controlled release pattern with diffusion mechanism was seen from tablets loaded with NS. F7 with a combination of NS form of drug and Guar gum in 1:1 ratio has shown best buoyancy and more controlled drug release among all 8 tablet compositions. Conclusions The importance and need for entrapment of an insoluble, less permeable drug to obtain the fruitful buoyant and drug release properties from Gastroretentive tablet dosage forms has been witnessed by all the observed results.

Formulation and evaluation of microspheres-loaded capsule of duloxetine HCL by extrusion-spheronization techniques

2025-06-16

Swamini Dumbare , Aakanksha Gadhave , Urmila Gaikwad +1 more | International Journal of Science and Research Archive

The present Investigation focuses on the formulation; optimization and evaluation of a microsphere-loaded capsule containing Duloxetine HCl; aimed at enhancing its oral bioavailability and therapeutic efficacy. Duloxetine HCl; a selective … The present Investigation focuses on the formulation; optimization and evaluation of a microsphere-loaded capsule containing Duloxetine HCl; aimed at enhancing its oral bioavailability and therapeutic efficacy. Duloxetine HCl; a selective serotonin and norepinephrine reuptake inhibitor (SNRI); exhibits limited water solubility and is unstable in acidic pH; leading to reduced absorption and erratic bioavailability. The goal was to develop a controlled-release multiparticulate dosage form to improve therapeutic efficacy and patient compliance. A series of formulations were prepared by varying the polymer type and drug-to-polymer ratios; and the process parameters were optimized with a particular focus on spheronization speed (fixed at 1200 rpm) and spheronization time. Optimization was guided by evaluating key parameters such as micromeritic properties (bulk density; tapped density; Carr’s index); particle size distribution; percentage yield; drug entrapment efficiency; and drug release. In vitro drug release studies were conducted over 12 hours to assess sustained-release behavior. Among the prepared batches; the formulation using Sodium Alginate in a 1:2 drug-to-polymer ratio demonstrated optimal performance; exhibiting high entrapment efficiency (above 85%); favorable spherical morphology; and sustained drug release following Higuchi diffusion kinetics. Surface morphology observed under Scanning Electron Microscopy (SEM) confirmed well-formed; discrete; and spherical microspheres. Among the various formulations; batch F6 demonstrated superior performance with excellent flow properties; high entrapment efficiency (85.4 %); and sustained drug release of 83.82% over 12 hours; indicating controlled release behavior.

Formulation and evaluation of controlled porosity osmotic pump tablets of verapamil hydrochloride

2025-06-15

Na An , Hung Pham Van , Xuan Dam Thanh +2 more | Ministry of Science and Technology Vietnam

Nanotechnology-Driven Colorectal Cancer Treatment: Coencapsulation of Irinotecan and Cyclosporine A in SNEDDS for Superior Outcomes

2025-06-15

Rati Yadav , Padakanti Sandeep Chary , Harshada Anil Bhalerao +5 more | ACS Applied Bio Materials

Irinotecan (IRN), a camptothecin derivative, has limited and inadequate oral absorption due to efflux pump activity by intestinal P-glycoprotein receptors. To complete these challenges, we designed and fabricated irinotecan and … Irinotecan (IRN), a camptothecin derivative, has limited and inadequate oral absorption due to efflux pump activity by intestinal P-glycoprotein receptors. To complete these challenges, we designed and fabricated irinotecan and cyclosporine. A coloaded self-nanoemulsifying drug delivery system (CO-IR-CP-SNs) can effectively prevent P-gp efflux and P450 enzyme metabolization, increasing oral bioavailability. To date, this combination has not been reported, which gives uniqueness to our formulation. The CO-IR-CP-SNs were fabricated by using the Box-Behnken design tool with Capryol 90, Cremophor EL, and PEG-400 as the oil, surfactant, and co-surfactant, respectively. The optimized CO-IR-CP-SNs had an average globule size of 16.36 ± 1.09 nm and a polydispersity index of 0.250 ± 0.01. The combination index value supports the existence of synergy in human colorectal cancer cell lines (HCT-116). The combination index shows a value of 0.78, which is <1, indicating synergism. Coloaded SNEDDS (CO-IR-CP-SNs) showed greater cellular uptake, reactive oxygen species generation, and apoptosis. In vivo pharmacokinetic studies demonstrated a 14-fold and 6.08-fold increase in Cmax and increased bioavailability compared with pure drug suspensions of IRN and CSP, respectively. Systemic toxicity signifies the nontoxic nature of CO-IR-CP-SNs in comparison to pure drug solutions of irinotecan and cyclosporine, individual and in combination. Hence, CO-IR-CP-SNs show promising results and improved oral bioavailability, which is beneficial in anticancer therapy with minimal side effects associated with the drug.

Formulation and Evaluation of Sustained release tablet of Trazodone hydrochloride by using Synthetic Polymer RS100 and RL 100

2025-06-15

Ashish R. Panchal , Supriya V. Mudgulkar | Journal of Drug Delivery and Therapeutics

Sustained release tablet was prepared by wet granulation method using synthetic polymer RS 100 and RL 100. The prepared tablet was also evaluated for their diameter, thickness, drug content, Hardness, … Sustained release tablet was prepared by wet granulation method using synthetic polymer RS 100 and RL 100. The prepared tablet was also evaluated for their diameter, thickness, drug content, Hardness, friability, weight variation. The thickness and diameter of tablet ranges from 5.43 ±0.288 to 5.76 ±0.05 and 09.68±0.577 to 10.04 ±0.04 respectively. Drug content was studied and its ranges from 92.03 to 98.60 %. Hardness was studied its ranges 5.5 to 6.5 kg/cm2, Friability ranges 0.71 to 0.95%, Weight variation ranges between 434±1.49 to 460±1.23. FTIR and DSC analysis does not show any interaction of drug with Excipients. Formulation was optimized on the basis of acceptable pre and post compressional parameters. The results of dissolution studies indicated that Batch F4 exhibited drug release of 88.06% at the end of 12 hr. to provide sufficient concentration for achieving satisfactory therapeutic value for extended period of time. The drug release from Batch F4 formulation was sustained 12hr. Fitting in-vitro drug release data from optimized matrix formulation to zero order followed by Higuchi model indicated that diffusion could be mechanism of drug release. The n value indicates a non – fiction or anomalous diffusion pattern. This means that both the diffusion and erosion mechanism were prevalent. Keywords: Trazodone hydrochloride, Wet granulation, RS100, RL100, sustained release.

Interaction of hydroxyapatite and chitosan with gentamicin and their antimicrobial activities: DFT and molecular docking approach

2025-06-15

Nassima Bou-ydia , Ben-issa El miraoui , Latifa Lâallam +1 more | Journal of the Nigerian Society of Physical Sciences

Motivated by the potential use of hydroxyapatite and chitosan as drug delivery systems for the antibiotic gentamicin in the coating of metal implants, a theoretical study was conducted to investigate … Motivated by the potential use of hydroxyapatite and chitosan as drug delivery systems for the antibiotic gentamicin in the coating of metal implants, a theoretical study was conducted to investigate the interaction mechanisms among these three compounds, assess the stability of the resulting coating, and evaluate the inhibitory potential of chitosan and gentamicin against Protein A from Staphylococcus aureus. The results of this study demonstrate that hydroxyapatite, chitosan, and gentamicin exhibit a low HOMO-LUMO energy gap, indicating that electron transfer between their molecular orbitals can occur readily due to the molecules’ structural flexibility. Additionally, chitosan shows a stronger binding affinity for gentamicin than hydroxyapatite, and both chitosan and gentamicin display a significant inhibitory effect against Protein A. Two theoretical approaches were employed: density functional theory using the B3LYP functional (Becke’s three-parameter hybrid functional combined with the LYP correlation functional) and the 3-21G basis set, as well as a molecular docking study using the MOE software (version 2015). The docking simulations generated 30 binding poses, which were evaluated using the London dG scoring function and refined twice using the Triangle Matcher placement method.

Sustained-Release Tablets Prepared by Compression Coating Technology Achieve Similar Drug Release to Osmotic Pump Tablets: Process Parameters and In Vitro-In Vivo Evaluation

2025-06-14

Zhitao Cai , Bei Liu , Han Zeng +6 more | Journal of Drug Delivery Science and Technology

Microinjectors for Controlled Cross-Barrier Drug Delivery in the Gastrointestinal Tract

2025-06-13

Joshua A. Levy , Michael A. Straker , Justin M. Stine +2 more | ACS Applied Materials & Interfaces

The gastrointestinal tract is a desirable target for drug delivery because it acts as a gateway to the body through intestinal uptake mechanisms and because it is preferred by patients … The gastrointestinal tract is a desirable target for drug delivery because it acts as a gateway to the body through intestinal uptake mechanisms and because it is preferred by patients leading to better outcomes. While ingestible devices have been developed to enable delivery of drugs at specific locations in the intestinal tract using various methods, one undeveloped area of gastrointestinal drug delivery is controlled release from devices operating in the intestinal tract. In this work, a versatile combination of semiresident injection technologies has been developed to allow tunable drug delivery of >5 μL with half-lives between 4 s and 118 days. The injectors rely on a previously developed ingestible actuation technology to deploy into the intestinal tissue and prompt dosing across the mucosal barrier. The injectors are composed of a hybrid 3D-printed reservoir and microneedle structure with variable material and geometric properties to enable tailored dosing. The demonstrated technology provides a framework for higher-level control over drug delivery using advanced fabrication techniques to achieve versatile and advantageous structural properties.

Slurry Conversion: A General Method for Formulating Amorphous Solid Dispersions and Fully Integrating Drug and Polymer Components

2025-06-13

Amy Lan Neusaenger , Caroline Fatina , Yichun Shen +2 more | Molecular Pharmaceutics

A solvent-sparing method, called "slurry conversion", has been tested as a general approach to preparing amorphous solid dispersions (ASDs). In this method, a solid mixture of a drug and a … A solvent-sparing method, called "slurry conversion", has been tested as a general approach to preparing amorphous solid dispersions (ASDs). In this method, a solid mixture of a drug and a polymer is stirred in the presence of a small quantity of a solvent, which is subsequently removed. In previous work, the method enabled more complete salt formation between lumefantrine (LMF), a basic antimalarial, with acidic polymers, than the common methods of hot melt extrusion and spray drying, leading to improved physical stability and release. Here, we apply this method to 18 poorly soluble drugs formulated as binary and ternary ASDs. For a rigorous test, the drugs were formulated with a single polymer, poly(acrylic acid) (PAA), under the same condition: room temperature stirring in 1:1 ethanol-dichloromethane at 4:1 solvent/solid ratio. ASDs were prepared for 16 of the 18 drugs at 25% drug loading and 11 at 50% drug loading. The drugs that were not fully amorphized did not dissolve in the default solvent or crystallized during drying. For most drugs, an abrupt "clearing" of the slurry occurred during stirring, indicating complete dissolution and amorphization before drying. While clearing did not occur for some drugs (e.g., clofazimine), the product was still fully amorphous, through solvent-mediated conversion. For a basic drug, the degree of protonation by PAA increases smoothly with PAA concentration and is ordered by its basic strength, supporting the conclusion that the method allows the system to reach thermodynamic equilibrium. In addition to binary ASDs, ternary ASDs containing two drugs (LMF and artemether or LMF and artesunate) were successfully prepared to support applications in combination therapies. In these ternary formulations, the protonation of LMF follows the trend established for binary systems. We find that slurry conversion can be scaled up 60-fold from the typical batch size without any difficulties or adverse effect on the structure and properties of the product. Overall, our results demonstrate that slurry conversion is a general, low-cost, and green alternative to conventional methods for manufacturing ASDs where the components are fully integrated.

Design, Molecular Docking, In Vitro and In Vivo Evaluation of Dimenhydrinate-Cyclodextrin Complex for Fast-Disintegrating Tablet

2025-06-13

Raed Samara , Rana M.F. Sammour , Véronique Seidel +1 more | Current Pharmaceutical Design

Introduction: This study aimed to formulate and evaluate dimenhydrinate (DMH) as fastdisintegrating tablets (FDTs) complexed with β-cyclodextrin (β-CD) to enhance its solubility, dissolution profile, and pharmacological performance. Methods: A DMH:β-CD … Introduction: This study aimed to formulate and evaluate dimenhydrinate (DMH) as fastdisintegrating tablets (FDTs) complexed with β-cyclodextrin (β-CD) to enhance its solubility, dissolution profile, and pharmacological performance. Methods: A DMH:β-CD inclusion complex was prepared at a 1:1 molar ratio using the kneading method. Characterization was performed through phase solubility studies, FTIR analysis, molecular docking, and in vitro dissolution testing. FDTs were developed using various superdisintegrants and assessed for quality attributes of a tablet, including hardness, friability, wetting time, water absorption ratio, and drug content. Results: Phase solubility and FTIR analyses confirmed the formation of a stable DMH:β-CD complex. Molecular docking indicated a binding affinity of -4.2 kcal/mol between β-CD and diphenhydramine. Among the FDT formulations, CP3 containing 9% crospovidone showed the best performance, with a disintegration time of 4.3 seconds and the highest drug release rate. In vivo pharmacological tests demonstrated enhanced sedative and antiemetic activities of the optimized FDTs compared to conventional DMH formulations. Discussion: The findings suggest that cyclodextrin-based complexation combined with orodispersible tablet technology can significantly enhance DMH's pharmacological efficacy and patient compliance. However, additional investigations on long-term stability, pharmacokinetics, and clinical scalability are warranted. Conclusion: The DMH:β-CD FDTs developed in this study offer promising improvements in solubility, dissolution, and therapeutic performance, indicating their potential for better clinical outcomes and patient acceptability.

A new strategy for nanosuspension stabilizer screening based on computer-aided drug design and molecular self-assembly

2025-06-13

Xiaoyang Zhang , Yao Zhang , Chaoliang Jia +2 more | International Journal of Pharmaceutics

Innovative Formulation and Evaluation of Sumatriptan Fast Dissolving Tablets through 3² Factorial Design

2025-06-12

Anusha Ravulapati , A. Suneetha , Ravi Shankar Kunderu +2 more | Current Trends in Biotechnology and Pharmacy

DESIGN-BASED DEVELOPMENT OF CANAGLIFLOZIN ORODISPERSIBLE TABLETS: FORMULATION AND CHARACTERIZATION STUDIES

2025-06-07

NAGA PHANI PJVV , RATNAMALA KV , Ramana Murthy Kv | Asian Journal of Pharmaceutical and Clinical Research

Objectives: The study aimed to convert liquid self-microemulsifying drug delivery systems (SMEDDS) of canagliflozin into solid SMEDDS to enhance stability and develop an orally disintegrating tablet (ODT) formulation. The key … Objectives: The study aimed to convert liquid self-microemulsifying drug delivery systems (SMEDDS) of canagliflozin into solid SMEDDS to enhance stability and develop an orally disintegrating tablet (ODT) formulation. The key goal was to improve disintegration time and in vitro drug release. Methods: Solidification of SMEDDS was achieved using two approaches: Adsorption onto carriers and lyophilization with mannitol. An I-optimal design was used to optimize the tablet formulation. Key variables included concentrations of super-disintegrants and adsorbents, while responses evaluated were disintegration time (R1) and in vitro drug release (R2). Aerosil 200 was used as the primary adsorbent, and croscarmellose as the super-disintegrant. Pre-compression parameters, such as flow properties, were analyzed based on different ratios of lactose and Aerosil 200. In addition, lyophilized formulations (L1-L4) were prepared and compared to adsorbed SMEDDS. Results: Disintegration time was significantly influenced by the concentration of the super-disintegrant, with croscarmellose promoting faster disintegration. Among the formulations, S6 demonstrated optimal characteristics, including a rapid disintegration time of 40 s and a high dissolution rate of 97.3%. Lyophilized formulation L4 showed the highest drug release (at 25 min), though adsorption onto Avicel proved superior in enhancing overall dissolution. Pre-compression evaluations confirmed improved flow properties with optimized ratios. Conclusion: Adsorption of SMEDDS onto solid carriers, particularly using Avicel, was more effective than lyophilization in improving dissolution and tablet performance. The optimized formulation (S6) exhibited robust characteristics suitable for long-term storage and use, demonstrating the potential of this approach for enhancing the bioavailability of poorly water-soluble drugs such as canagliflozin

BIO ANALYTICAL METHOD FOR QUANTITATIVE ESTIMATION, PHARMACOKINETIC AND BIOEQUIVALENCE STUDY OF NIZATIDINE NOVEL RAFT GASTRO RETENTIVE FORMULATION USING RP-HPLC

2025-06-07

SHANTI SAGAR , NERELLA MOUNIKA , Ramgopal Appani +1 more | Asian Journal of Pharmaceutical and Clinical Research

Objective: This study presents for the development and validation of RP-HPLC method for the determination of nizatidine in rabbit plasma. Methods: The method was used to perform a pharmacokinetics and … Objective: This study presents for the development and validation of RP-HPLC method for the determination of nizatidine in rabbit plasma. Methods: The method was used to perform a pharmacokinetics and bio-equity study to compare a raft gastro-retentive formulation of nizatidine with a marketed formulation. Nizatidine is a competitive H2 receptor antagonist that prescribed for the treatment of different disorders connected with gastric acid production, mainly for nocturnal acid secretion. Twelve New Zealand white rabbits were divided into two groups: one of them receive the new raft formulation that is made up from novel ingredients and the second one receive the marketed raft formulation. Results: The results indicated that the novel raft formulation significantly enhanced the bioavailability of nizatidine, with higher Cmax (230.28±0.61 ng/ml) and AUC0-∞ (1826.17±2.38 ng•h/ml) compared to the marketed formulation (Cmax: 210.Mean Cmax values for esomeprazole were 8±4.5 ng/ml, and Cmax for the metabolite were 6.5±1.9 ng/ml AUC0-∞ was 619.1±21,14 ng•h/ml. Conclusion: Also, the physical characterization demonstrated that, for the raft formulation, the mean resident time (MRT) was higher (7.22 ± 0.014 h) than that of the marketed product (3.17 ± 0.07 h) and suggested a sustained release product. A strong in vitro-in vivo correlation (IVIVC) R² = 0.9162 was confirmed to the predictability of the raft formulations performance

Impact of medication swallowing lubricants on the in vitro dissolution of crushed and whole metformin tablets: dissolution kinetics study

2025-06-05

Vivek B. Nooney , Thilini Thrimawithana , Barbora de Courten +5 more | Pharmaceutical Development and Technology

Metformin is the most common drug used in patients with type 2 diabetes. Our aim is to assess if the in vitro dissolution of Metformin IR 500 mg tablets and … Metformin is the most common drug used in patients with type 2 diabetes. Our aim is to assess if the in vitro dissolution of Metformin IR 500 mg tablets and its kinetics is altered in the presence of various medication swallowing lubricants used in vivo and to evaluate their rheological properties of tablet lubricant. The dissolution profile of metformin tablets (crushed and whole) mixed with selected medication swallowing lubricants was studied in a Distek® Dissolution apparatus at 6 different time points (n = 5). Samples were diluted and analysed using a UV-visible Spectrometer at a wavelength of 232 nm using a calibrated absorbance-concentration curve. Dissolution data will be modelled to understand the effect on its dissolution kinetics. Rheology studies were completed using an AR G2 System Rheometer. Gloup® Forte delayed the in vitro dissolution of metformin from crushed or whole tablets and produced lower peak concentrations, irrespective of the pH of the dissolution media (reduction up to 35% reduction in concentration in pH = 6.8). Gloup® Forte has changed the release to almost erosion-controlled in different media when mixed with crushed metformin tablets. Further studies evaluating the effects of commonly used thickened fluids on medication may be required to better inform clinical practice.

Assessing Impact of Food on Oral Drug Bioequivalence Supporting ICH M13 A with the Advancements of Physiologically Based Pharmacokinetic Modeling

2025-06-04

Arindom Pal , Khondoker Alam , Ethan Stier +7 more | Pharmaceutical Research

Untangling “dissolved” drug species from various formulations of a poorly soluble drug: Sampling methods, mechanistic insights, and IVIVC

2025-06-01

Jakob Tobias Lynnerup , Tim Lillotte , Maximilian Feldmüller +5 more | Journal of Pharmaceutical Sciences

The impact of ionic excipients on stabilization of enalapril tablets by the formation of alkaline salt “in situ”

2025-06-01

Aleš Franc , Bořek Žaludek , Petr Sova +2 more | European Journal of Pharmaceutics and Biopharmaceutics

An integrated material-sparing method for determining dilution potential of direct compression tablet fillers

2025-06-01

Weeraya Tharanon , Yiwang Guo , Jomjai Peerapattana +1 more | Journal of Pharmaceutical Sciences

Characterization and Pharmacokinetic Analysis of Rosuvastatin calcium-2-Hydroxypropyl-β-cyclodextrin Inclusion Complexes for Enhanced Oral Bioavailability

2025-06-01

K Rahul , Sarath Chandran C , Alexis Diomedi P +7 more | Next research.