Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications |
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Authors: | Kawabata Yohei Wada Koichi Nakatani Manabu Yamada Shizuo Onoue Satomi |
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Institution: | a Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan b Department of Chemistry, Manufacturing and Control, Kobe Pharma Research Institute, Nippon Boehringer Ingelheim Co., Ltd., 6-7-5, Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo, 650-0047, Japan |
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Abstract: | The poor oral bioavailability arising from poor aqueous solubility should make drug research and development more difficult. Various approaches have been developed with a focus on enhancement of the solubility, dissolution rate, and oral bioavailability of poorly water-soluble drugs. To complete development works within a limited amount of time, the establishment of a suitable formulation strategy should be a key consideration for the pharmaceutical development of poorly water-soluble drugs. In this article, viable formulation options are reviewed on the basis of the biopharmaceutics classification system of drug substances. The article describes the basic approaches for poorly water-soluble drugs, such as crystal modification, micronization, amorphization, self-emulsification, cyclodextrin complexation, and pH modification. Literature-based examples of the formulation options for poorly water-soluble compounds and their practical application to marketed products are also provided. Classification of drug candidates based on their biopharmaceutical properties can provide an indication of the difficulty of drug development works. A better understanding of the physicochemical and biopharmaceutical properties of drug substances and the limitations of each delivery option should lead to efficient formulation development for poorly water-soluble drugs. |
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Keywords: | API active pharmaceutical ingredient ASD amorphous solid dispersion AUC area under the curve BA bioavailability BCS biopharmaceutics classification system CSD crystalline solid dispersion EMEA European Medicines Agency FDA U S Food and Drug Administration IR immediate-release JP theJapanese Pharmacopoeia SEDDS self-emulsifying drug delivery systems SMEDDS self-microemulsifying drug delivery systems SNEDDS self-nanoemulsifying drug delivery systems WHO World Health Organization |
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