Medical

Water-Insoluble Drug Formulation, Third Edition

Author: Ron Liu

Publisher: CRC Press

ISBN:

Category: Medical

Page: 736

View: 865

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.
Medical

Water-Insoluble Drug Formulation, Second Edition

Author: Ron Liu

Publisher: CRC Press

ISBN:

Category: Medical

Page: 688

View: 955

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 much-needed reformulation of currently marketed products can be significantly affected by these challenges. Water Insolubility is the Primary Culprit in over 40% of New Drug Development Failures The most comprehensive resource on the topic, this second 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 solubility properties and their impact on formulation, from theory to industrial practice. With detailed discussion on how these properties contribute to solubilization and dissolution, the text also features six brand new chapters on water-insoluble drugs, exploring regulatory aspects, pharmacokinetic behavior, early phase formulation strategies, lipid based systems for oral delivery, modified release of insoluble drugs, and scalable manufacturing aspects. The book includes more than 15 water-insoluble drug delivery systems or technologies, illustrated with case studies 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.
Medical

Water-Insoluble Drug Formulation

Author: Ron Liu

Publisher: CRC Press

ISBN:

Category: Medical

Page: 688

View: 183

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 much-needed reformulation of currently marketed products can be significantly affected by these challenges. Water Insolubility is the Primary Culprit in over 40% of New Drug Development Failures The most comprehensive resource on the topic, this second 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 solubility properties and their impact on formulation, from theory to industrial practice. With detailed discussion on how these properties contribute to solubilization and dissolution, the text also features six brand new chapters on water-insoluble drugs, exploring regulatory aspects, pharmacokinetic behavior, early phase formulation strategies, lipid based systems for oral delivery, modified release of insoluble drugs, and scalable manufacturing aspects. The book includes more than 15 water-insoluble drug delivery systems or technologies, illustrated with case studies 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.
Medical

Formulating Poorly Water Soluble Drugs

Author: Robert O. Williams III

Publisher: Springer

ISBN:

Category: Medical

Page: 648

View: 870

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.
Science

Role of Lipid Excipients in Modifying Oral and Parenteral Drug Delivery

Author: Kishor M. Wasan

Publisher: John Wiley & Sons

ISBN:

Category: Science

Page: 240

View: 795

This comprehensive resource covers the fundamentals, formulation, and biopharmaceutical issues of lipid-based drug delivery. It presents the principles of lipid absorption and covers formulation issues, such as dissolution testing and stability testing, and physiological and biopharmaceutical issues, including the role of specific enzymes, the evaluation of transport systems in the body, and the mechanisms governing the transport of water-insoluble drugs.

Liquisolid Technique

Author: Sandip Vajir

Publisher: LAP Lambert Academic Publishing

ISBN:

Category:

Page: 92

View: 426

This technique is a new technique that can approve in industry nowa days new liquisolid technique is populer in world. This is big achivements of any medicine faculty to form liquisolid tablet. Liquisolid technique is a new and promising method that can change the dissolution rate of drugs. It has been used to enhance dissolution rate of poorly water-soluble drugs. This technique was successfully applied for low dose water-insoluble drugs. However, formulation of the high dose insoluble-drugs as liquisolid tablets is one of the limitations of the liquisolid technique.
Science

Oral Controlled Release Formulation Design and Drug Delivery

Author: Hong Wen

Publisher: John Wiley & Sons

ISBN:

Category: Science

Page: 376

View: 951

This book describes the theories, applications, and challenges for different oral controlled release formulations. This book differs from most in its focus on oral controlled release formulation design and process development. It also covers the related areas like preformulation, biopharmaceutics, in vitro-in vivo correlations (IVIVC), quality by design (QbD), and regulatory issues.
Antineoplastic agents

Design of Macromolecular Anti-cancer Drug Delivery Systems Using Molecular Dynamics Simulation

Author: Negin Razavilar

Publisher:

ISBN:

Category: Antineoplastic agents

Page: 185

View: 792

In recent years, the application of self-associating block copolymer based drug delivery systems has attracted increasing attention as nano-sized carriers for the encapsulation and the controlled delivery of water insoluble drugs. Most of the drug formulations are based on the "trial and error" method with no specific library of polymer and drug combination. This is simply because in the context of drug formulation and drug delivery from polymeric micelles, many factors are necessary to study such as drug-polymer intermolecular interactions, release kinetics, polymer compatibility with human cells, etc. Computer simulation that can help design such polymeric drug delivery systems will enable researchers to make educated decisions on choosing a particular polymeric carrier for a given drug, avoiding time consuming and expensive trial and error based formulation experiments. In the present thesis, we reported the use of molecular dynamics (MD) simulation to calculate the self-diffusion coefficients of a hydrophobic drug molecule in a series of micelle-forming PEO-b-PCL block copolymers with different structures and PCL block lengths in the presence of water molecules. MD analysis techniques like velocity auto-correlation functions, and squared displacement values along x, y and z axis provided useful atomistic details to understand the molecular origin of the diffusivity observed for drug molecules. Based on the evidence of reported work, intermolecular specific interactions between drug and different blocks of block copolymers all play important roles in the self-diffusion of drug molecule (CuB) in block copolymers. Additionally, water concentration, polymer swelling and wriggling motion of polymer chains affect the diffusivity of water molecules. The computed radius of gyration (Rg) of the PCL block confirmed that the PCL block tends to exhibit a higher degree of swelling than the PEO block. The understanding of relative contributions of the inter molecular interactions between drug and polymer can help us to customize the performance of drug carriers by engineering the structure of block copolymers to achieve a desired drug self-diffusion.

Poorly Soluble Drugs

Author: Lino Messana

Publisher:

ISBN:

Category:

Page: 300

View: 948

Solubility is the property of a solid, liquid, or gaseous chemical substance called solute to dissolve in a solid, liquid, or gaseous solvent to form a homogeneous solution of the solute in the solvent. The solubility of a substance fundamentally depends on the solvent used as well as on temperature and pressure. The extent of solubility of a substance in a specific solvent is measured as the saturation concentration where adding more solute does not increase its concentration in the solution. Solubility also plays a major role for other dosage forms like parenteral formulations as well. 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. This book provides a comprehensive overview of currently used formulation strategies for hydrophobic drugs discusses the main instrumentation, operation principles and theoretical background, with a focus on critical formulation features and clinical studies. It provides a comprehensive assessment of the application of fundamental principles of dissolution and drug release testing to poorly soluble compounds and formulations. Over 40% of new chemical entities developed in pharmaceutical industry are practically insoluble in water. These poorly water soluble drugs having slow drug absorption leads to inadequate and variable bioavailability and gastrointestinal mucosal toxicity. For orally administered drugs solubility is the most important one rate limiting parameter to achieve their desired concentration in systemic circulation for pharmacological response. Problem of solubility is a major challenge for formulation scientist. The improvement of drug solubility thereby its oral bioavailability remains one of the most challenging aspects of drug development process especially for oral-drug delivery system.

Self Emulsifying Drug Delivery Systems

Author: Jyoti Wadhwa

Publisher: LAP Lambert Academic Publishing

ISBN:

Category:

Page: 108

View: 540

Self emulsifying drug delivery systems, which are by no means a recent technological innovation, have not only proven their utility for mitigating the poor and variable gastrointestinal absorption of lipophilic drugs, but in many cases have shown the ability to reduce or eliminate the influence of food on the absorption of these drugs. A cursory review of literature will clearly underscore not only scientific interest in Self-Emulsifying formulations, but will reinforce the promise and versatility that this technology holds for addressing the constant and growing problems surrounding the oral delivery of many poorly soluble drug candidates. This book seeks to provide a comprehensive summary of both the theoretical and practical aspects of oral self-emulsifying formulations to formulators wishing to employ the technology as well as scientific and marketing executives who wish to gain a greater understanding of developing technology that is expected to assume increasing prominence in the years to come. It is the author's hope that the concepts and techniques described in this book will lead to the development of improved dosage forms for water-insoluble drugs.
Medicine

Lipid-Based Nano-Delivery for Oral Administration of Poorly Water Soluble Drugs (PWSDs): Design, Optimization and in Vitro Assessment

Author: Mohsin Kazi

Publisher:

ISBN:

Category: Medicine

Page:

View: 652

Currently, more than 90% of compounds identified are water insoluble and or poorly water soluble, which is a bottle neck in the development of many new drug candidates. These poorly soluble drug molecules are difficult to formulate using conventional approaches and are associated with numerous formulation-related performance issues. Formulating these compounds using lipid-based systems is one of the rapidly growing interests and suitable drug delivery strategies. Lipid formulations such as self-emulsifying/microemulsifying/nanoemulsifying drug delivery systems (SEDDS/SMEDDS/SNEDDS) have been attempted in many researches to improve the bioavailability and dissolution rate for their better dispersion properties. One of the greatest advantages of incorporating the poorly soluble drug into such formulation products is their spontaneous emulsion and or microemulsion/nanoemulsion formation in aqueous media. The performance and ongoing advances in manufacturing technologies have rapidly introduced lipid-based drug formulations as commercial products into the marketplace with several others in clinical development. The current chapter aims to present the characteristics feature, development and utilization of oral lipid-based nanoformulations within the drug delivery regime. The content of the chapter also provides an insight into the in vitro evaluation of lipid-based nanosystems and their limitations.
Man - Nervous system - Therapy

Therapy for Neurologic Disorders

Author: Wigbert C. Wiederholt

Publisher: John Wiley & Sons

ISBN:

Category: Man - Nervous system - Therapy

Page: 437

View: 371

Formulation And Evaluation Of

Author: Shashidher Burra

Publisher: LAP Lambert Academic Publishing

ISBN:

Category:

Page: 80

View: 130

The present study enlightens to enhance the dissolution profile, absorption efficiency and bioavailability of water insoluble drugs like carvedilol. A novel "Powder Solution Technology" involves absorption and adsorption efficiency, which makes use of liquid medications admixed with suitable carriers and coating materials and formulated into a free flowing, dry looking, non adherent and compressible powder forms. Based upon a new mathematical model expression improved flow characteristics and hardness of the formulation has been achieved by changing the proportion of carrier and coating material ratio from 20:1 to 5:1. Di calcium phosphate, Avicel (r) PH 200 were showing acceptable flow properties compared with Avicel (r)PH 101 and Lactose. Higher dissolution rates (98.4%) were observed in Poly ethylene glycol 400 and Avicel (r)PH 200 containing liquisolid formulations (F5) compared with marketed product (CARCA(r) 12.5 mg tablets) 81% drug release. Poly ethylene glycol 400 was showing highest solubility compared with poly ethylene glycol 200, propylene glycol and glycerin. The crystalline state of carvedilol drug state is changed to amorphous state due to liquisolid formation and

Enhancement of the Rate of Solution of Relatively Insoluble Drugs from Solid-solid Systems Prepared by Supercritical Fluid Technology

Author: Carmen H. Ramirez

Publisher:

ISBN:

Category:

Page: 239

View: 334

Supercritical fluid technology, specifically the method of rapid expansion of supercritical solutions (RESS), has been used to prepare small particles consisting of solid solutions of a relatively insoluble drug and a water-soluble excipient. With an increasing number of relatively insoluble compounds being discovered, a general process for enhancing drug dissolution rates would assist formulation of these compounds for therapeutic use. Solid solutions could serve as a means for enhancing drug dissolution rates, since the drug is dispersed in a solid solvent in its smallest form, i.e., a molecule, prior to entering into solution. Therefore, solid solutions consisting of the relatively insoluble model drugs lidocaine or probucol and a water-soluble surfactant, poloxamers 407, 188, or 403 were prepared by RESS processing. Dissolution studies of these systems were performed and evaluated for their ability to enhance drug release rates. Furthermore, the mechanism by which solid solutions form in these systems was determined using differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy. Scanning electron microscopy (SEM) was also used to study the surface characteristics of these particulate systems.