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Drug Solubility: Importance and Enhancement Techniques
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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. 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.
Yu, and Di Doris Zhang. Cannon, Yi Shi, and Pramod Gupta. Cannon and Michelle A.
Sensible Use of Technologies to Increase Solubility and Bioavailability in Formulation Development
Laird Forrest, Glen S. Cannon, and Sophia Y. Neau, Nikhil C. Loka, and Kalyan K.
Lee, James McShane, J. Michael Shaw, Ray W. Wood, and Dinesh B. Myrdal, Stephen J. Finally these formulations were subjected for dissolution studies in discriminating medium. Darunavir Ethanolate exhibits pH dependant solubility, and shows increasing solubility at lower pH and vice versa. Phosphate buffer pH 6.
- Introduction | Water-Insoluble Drug Formulation | Taylor & Francis Group!
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Formulations were filled in hard gelatin capsules and dissolution was performed using parameters as follows in Table 1. Solid dispersion: Solubility studies: Solubility studies were aimed at identifying the suitable polymer which can exhibit maximum solubility and is able to dissolve quickly to release drug from the polymeric formulation. Soluplus aqueous solution exhibited maximum solubility for DRVE and Poloxamer exhibited quick dissolving property.
Results are depicted in Table 2. Solid dispersions comprising of Darunavir Ethanolate corresponding to mg of Darunavir were prepared. Prepared solid dispersions were compared for dissolution rate studies in discriminating medium and release obtained are depicted in Table 3 and Fig. A dsorption using spray drying: The spray dried product was evaluated for percent drug content. Percent drug content in the spray dried formulation was found to be Release obtained by this method is depicted in Table 4 and Fig.
Dissolution rate in discriminating medium was obtained and it is depicted as in Table 5 and Fig. Formulations prepared using various approaches were screened on the basis of their dissolution performance in discriminating medium. Solid dispersions were prepared which exhibited slightly fair release with Poloxamer formulation containing drug: Poloxamer ratio showed Adsorption of drug on an inert carrier like Aeroperl can be used to increase its effective surface area for dissolution leading to increase rate of dissolution. However, It showed merely The study shown increased dissolution rate than the API, hence solubility of Darunavir Ethanolate was increased.
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The methods used are simple and easy to scale up. Among formulation methods attempted Darunavir Ethanolate-Poloxamer solid dispersion shown promising results hence this formulation is most convenient, easy and cost-effective dosage form that can be prepared. Here methods attempted are simple, industrially feasible and easy to scale up. Int J Pharm Sci Res ; 7 1 : Download: Cited By: 0. Authors: S. Sawarkar and P. Authors Address: Department of Pharmaceutics, S. Vile Parle W , Mumbai. DOI: Ravikumar Department of Pharmaceutics, S. Solid dispersion: Solid dispersion is one of the widely used method for enhancing solubility of poorly soluble drugs.
Adsorption on a carrier: Adsorption of drug on mesoporous and inert substance like silica has been studied widely. Optimization of formulae: Darunavir Ethanolate exhibits pH dependant solubility, and shows increasing solubility at lower pH and vice versa.
Water-Insoluble Drug Formulation, Second Edition book download - Mon premier blog
Solution 0. Time min Percent cumulative release pH 6. Time min. Percent cumulative release pH 6. Drug-like properties: concepts, structure design and methods: from ADME to toxicity optimization. Academic Press Serajuddin, A. Salt formation to improve drug solubility. Advanced drug delivery reviews, 59 Talegaonkar, S. Microemulsions: a novel approach to enhanced drug delivery. Lipinski, C. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings.
Advanced drug delivery reviews, 64 Hauss, D. Pharmaceutical research, 24 PMID: Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug discovery today, 12 Leuner, C. European journal of pharmaceutics and biopharmaceutics, 50 International journal of pharmaceutics, Physicochemical principles of pharmacy.
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Nair A. Poster presentation. Sinko, P. Babu, N. Journal of pharmaceutical sciences 98 Caldwell, G. ADME optimization and toxicity assessment in early-and late-phase drug discovery.
Current topics in medicinal chemistry, 9 Drug delivery system, 25 Nature Reviews Drug Discovery, 3 DOI