Recent trends in solubility and bioavailability enhancement for poorly water-soluble drugs

Recent trends in solubility and bioavailability enhancement for poorly water-soluble drugs

Author: 최한곤

Publisher: 한양대학교 출판부

Published: 2019-12-17

Total Pages: 700

ISBN-13: 8972186481

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난용상 약물의 용해도 및 생체[이용율 증진에 대한 최근 연구동향을 모아 발간하고자 함 1. Silymarin-loaded solid nanoparticles with excellent hepatic protection: physicochemical characterization and in vivo evaluation. 2. The Influence of Bile Salt on the Chemotherapeutic Response of Docetaxel-loaded Thermosensitive Nanomicelles. 3. Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: Physicochemical characterization and in vivo investigation. 4. Tumor-targeting. pH-sensitive nanoparticles for docetaxel delivery to drug-resistant cancer cells. 5. Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe. 6. Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate. 7. Receptor-targeted. drug-loaded. functionalized graphene oxides for chemotherapy and photothermal therapy. 8. Progressive slowdown/prevention of cellular senescence by CD9-targeted delivery of rapamycin using lactose-wrapped calcium carbonate nanoparticles. 9. Optimization and physicochemical characterization of a cationic lipid-phosphatidylcholine mixed emulsion formulated as a highly efficient vehicle that facilitates adenoviral gene transfer. 10. Combination of NIR therapy and regulatory T cell modulation using layer-by-layer hybrid nanoparticles for effective cancer photoimmunotherapy. 11. Cyclic RGD-conjugated Pluronic® blending system for active. targeted drug delivery. 12. Transferrin-Conjugated Polymeric Nanoparticle for Receptor-Mediated Delivery of Doxorubicin in Doxorubicin-Resistant Breast Cancer Cells. 13. Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate. 14. Comparison of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol-loaded self-emulsifying granule and solid self-nanoemulsifying drug delivery system: powder property. dissolution and oral bioavailability. 15. Liposomal Formulations for Nose-to-Brain Delivery: Recent Advances and Future Perspectives. 16. Development of folate-functionalized zein nanoparticles for ligand-directed delivery of paclitaxel.


Drug Delivery Strategies for Poorly Water-Soluble Drugs

Drug Delivery Strategies for Poorly Water-Soluble Drugs

Author: Dionysios Douroumis

Publisher: John Wiley & Sons

Published: 2012-12-19

Total Pages: 543

ISBN-13: 1118444671

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Many newly proposed drugs suffer from poor water solubility, thus presenting major hurdles in the design of suitable formulations for administration to patients. Consequently, the development of techniques and materials to overcome these hurdles is a major area of research in pharmaceutical companies. Drug Delivery Strategies for Poorly Water-Soluble Drugs provides a comprehensive overview of currently used formulation strategies for hydrophobic drugs, including liposome formulation, cyclodextrin drug carriers, solid lipid nanoparticles, polymeric drug encapsulation delivery systems, self–microemulsifying drug delivery systems, nanocrystals, hydrosol colloidal dispersions, microemulsions, solid dispersions, cosolvent use, dendrimers, polymer- drug conjugates, polymeric micelles, and mesoporous silica nanoparticles. For each approach the book discusses the main instrumentation, operation principles and theoretical background, with a focus on critical formulation features and clinical studies. Finally, the book includes some recent and novel applications, scale-up considerations and regulatory issues. Drug Delivery Strategies for Poorly Water-Soluble Drugs is an essential multidisciplinary guide to this important area of drug formulation for researchers in industry and academia working in drug delivery, polymers and biomaterials.


Amorphous Solid Dispersions

Amorphous Solid Dispersions

Author: Navnit Shah

Publisher: Springer

Published: 2014-11-21

Total Pages: 702

ISBN-13: 1493915983

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This volume offers a comprehensive guide on the theory and practice of amorphous solid dispersions (ASD) for handling challenges associated with poorly soluble drugs. In twenty-three inclusive chapters, the book examines thermodynamics and kinetics of the amorphous state and amorphous solid dispersions, ASD technologies, excipients for stabilizing amorphous solid dispersions such as polymers, and ASD manufacturing technologies, including spray drying, hot melt extrusion, fluid bed layering and solvent-controlled micro-precipitation technology (MBP). Each technology is illustrated by specific case studies. In addition, dedicated sections cover analytical tools and technologies for characterization of amorphous solid dispersions, the prediction of long-term stability, and the development of suitable dissolution methods and regulatory aspects. The book also highlights future technologies on the horizon, such as supercritical fluid processing, mesoporous silica, KinetiSol®, and the use of non-salt-forming organic acids and amino acids for the stabilization of amorphous systems. Amorphous Solid Dispersions: Theory and Practice is a valuable reference to pharmaceutical scientists interested in developing bioavailable and therapeutically effective formulations of poorly soluble molecules in order to advance these technologies and develop better medicines for the future.


Melt Extrusion

Melt Extrusion

Author: Michael A. Repka

Publisher: Springer Science & Business Media

Published: 2013-10-11

Total Pages: 472

ISBN-13: 1461484324

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This volume provides readers with the basic principles and fundamentals of extrusion technology and a detailed description of the practical applications of a variety of extrusion processes, including various pharma grade extruders. In addition, the downstream production of films, pellets and tablets, for example, for oral and other delivery routes, are presented and discussed utilizing melt extrusion. This book is the first of its kind that discusses extensively the well-developed science of extrusion technology as applied to pharmaceutical drug product development and manufacturing. By covering a wide range of relevant topics, the text brings together all technical information necessary to develop and market pharmaceutical dosage forms that meet current quality and regulatory requirements. As extrusion technology continues to be refined further, usage of extruder systems and the array of applications will continue to expand, but the core technologies will remain the same.


Innovative Dosage Forms

Innovative Dosage Forms

Author: Yogeshwar Bachhav

Publisher: John Wiley & Sons

Published: 2019-12-04

Total Pages: 470

ISBN-13: 3527343962

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Teaches future and current drug developers the latest innovations in drug formulation design and optimization This highly accessible, practice-oriented book examines current approaches in the development of drug formulations for preclinical and clinical studies, including the use of functional excipients to enhance solubility and stability. It covers oral, intravenous, topical, and parenteral administration routes. The book also discusses safety aspects of drugs and excipients, as well as regulatory issues relevant to formulation. Innovative Dosage Forms: Design and Development at Early Stage starts with a look at the impact of the polymorphic form of drugs on the preformulation and formulation development. It then offers readers reliable strategies for the formulation development of poorly soluble drugs. The book also studies the role of reactive impurities from the excipients on the formulation shelf life; preclinical formulation assessment of new chemical entities; and regulatory aspects for formulation design. Other chapters cover innovative formulations for special indications, including oncology injectables, delayed release and depot formulations; accessing pharmacokinetics of various dosage forms; physical characterization techniques to assess amorphous nature; novel formulations for protein oral dosage; and more. -Provides information that is essential for the drug development effort -Presents the latest advances in the field and describes in detail innovative formulations, such as nanosuspensions, micelles, and cocrystals -Describes current approaches in early pre-formulation to achieve the best in vivo results -Addresses regulatory and safety aspects, which are key considerations for pharmaceutical companies -Includes case studies from recent drug development programs to illustrate the practical challenges of preformulation design Innovative Dosage Forms: Design and Development at Early Stage provides valuable benefits to interdisciplinary drug discovery teams working in industry and academia and will appeal to medicinal chemists, pharmaceutical chemists, and pharmacologists.


Water-Insoluble Drug Formulation

Water-Insoluble Drug Formulation

Author: Ron Liu

Publisher: CRC Press

Published: 2018-03-12

Total Pages: 781

ISBN-13: 1351646826

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Properties and Formulation: From Theory to Real-World Application Scientists have attributed more than 40 percent of the failures in new drug development to poor biopharmaceutical properties, particularly water insolubility. Issues surrounding water insolubility can postpone or completely derail important new drug development. Even the much-needed reformulation of currently marketed products can be significantly affected by these challenges. More recently it was reported that the percentage increased to 90% for the candidates of new chemical entities in the discovery stage and 75% for compounds under development. In the most comprehensive resource on the topic, this third edition of Water-Insoluble Drug Formulation brings together a distinguished team of experts to provide the scientific background and step-by-step guidance needed to deal with solubility issues in drug development. Twenty-three chapters systematically describe the detailed discussion on solubility theories, solubility prediction models, the aspects of preformulation, biopharmaceutics, pharmacokinetics, regulatory, and discovery support of water-insoluble drugs to various techniques used in developing delivery systems for water-insoluble drugs. This book includes more than 15 water-insoluble drug delivery systems or technologies, illustrated with case studies and featuring oral and parenteral applications. Highlighting the most current information and data available, this seminal volume reflects the significant progress that has been made in nearly all aspects of this field. The aim of this book is to provide a handy reference for pharmaceutical scientists in the handling of formulation issues related to water-insoluble drugs. In addition, this book may be useful to pharmacy and chemistry undergraduate students and pharmaceutical and biopharmaceutical graduate students to enhance their knowledge in the techniques of drug solubilization and dissolution enhancement.


Oral Drug Absorption

Oral Drug Absorption

Author: Jennifer B. Dressman

Publisher: CRC Press

Published: 2016-04-19

Total Pages: 432

ISBN-13: 1420077341

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Oral Drug Absorption, Second Edition thoroughly examines the special equipment and methods used to test whether drugs are released adequately when administered orally. The contributors discuss methods for accurately establishing and validating in vitro/in vivo correlations for both MR and IR formulations, as well as alternative approaches for MR an


Formulating Poorly Water Soluble Drugs

Formulating Poorly Water Soluble Drugs

Author: Robert O. Williams III

Publisher: Springer Science & Business Media

Published: 2011-12-04

Total Pages: 656

ISBN-13: 1461411440

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This volume is intended to provide the reader with a breadth of understanding regarding the many challenges faced with the formulation of poorly water-soluble drugs as well as in-depth knowledge in the critical areas of development with these compounds. Further, this book is designed to provide practical guidance for overcoming formulation challenges toward the end goal of improving drug therapies with poorly water-soluble drugs. Enhancing solubility via formulation intervention is a unique opportunity in which formulation scientists can enable drug therapies by creating viable medicines from seemingly undeliverable molecules. With the ever increasing number of poorly water-soluble compounds entering development, the role of the formulation scientist is growing in importance. Also, knowledge of the advanced analytical, formulation, and process technologies as well as specific regulatory considerations related to the formulation of these compounds is increasing in value. Ideally, this book will serve as a useful tool in the education of current and future generations of scientists, and in this context contribute toward providing patients with new and better medicines.


Supercritical Fluids

Supercritical Fluids

Author: E. Kiran

Publisher: Springer Science & Business Media

Published: 2012-12-06

Total Pages: 602

ISBN-13: 9401139296

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Supercritical fluids are neither gas nor liquid, but can be compressed gradually from low to high density and they are therefore interesting and important as tunable solvents and reaction media in the chemical process industry. By adjusting the density the properties of these fluids can be customised and manipulated for a given process - physical or chemical transformation. Separation and processing using supercritical solvents such as CO2 are currently on-line commercially in the food, essential oils and polymer industries. Many agencies and industries are considering the use of supercritical water for waste remediation. Supercritical fluid chromatography represents another, major analytical application. Significant advances have recently been made in materials processing, ranging from particle formation to the creation of porous materials. The chapters in this book provide tutorial accounts of topical areas centred around: (1) phase equilibria, thermodynamics and equations of state; (2) critical behaviour, crossover effects; (3) transport and interfacial properties; (4) molecular modelling, computer simulation; (5) reactions, spectroscopy; (6) phase separation kinetics; (7) extractions; (8) applications to polymers, pharmaceuticals, natural materials and chromatography; (9) process scale-up.