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Formulation Strategies to Improve the Bioavailability of Poorly Absorbed Drugs with Special Emphasis on Self-Emulsifying Systems

机译:尤其重视自乳化系统的提高不良吸收药物生物利用度的制定策略

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摘要

Poorly water-soluble drug candidates are becoming more prevalent. It has been estimated that approximately 60–70% of the drug molecules are insufficiently soluble in aqueous media and/or have very low permeability to allow for their adequate and reproducible absorption from the gastrointestinal tract (GIT) following oral administration. Formulation scientists have to adopt various strategies to enhance their absorption. Lipidic formulations are found to be a promising approach to combat the challenges. In this review article, potential advantages and drawbacks of various conventional techniques and the newer approaches specifically the self-emulsifying systems are discussed. Various components of the self-emulsifying systems and their selection criteria are critically reviewed. The attempts of various scientists to transform the liquid self-emulsifying drug delivery systems (SEDDS) to solid-SEDDS by adsorption, spray drying, lyophilization, melt granulation, extrusion, and so forth to formulate various dosage forms like self emulsifying capsules, tablets, controlled release pellets, beads, microspheres, nanoparticles, suppositories, implants, and so forth have also been included. Formulation of SEDDS is a potential strategy to deliver new drug molecules with enhanced bioavailability mostly exhibiting poor aqueous solubility. The self-emulsifying system offers various advantages over other drug delivery systems having potential to solve various problems associated with drugs of all the classes of biopharmaceutical classification system (BCS).
机译:水溶性差的候选药物正变得越来越普遍。据估计,大约60-70%的药物分子在水性介质中溶解度不足和/或渗透性非常低,以使其在口服后无法从胃肠道(GIT)充分吸收且可重复吸收。配方科学家必须采取各种策略来增加其吸收。发现脂质制剂是应对挑战的有前途的方法。在这篇综述文章中,讨论了各种常规技术以及更新的方法(特别是自乳化系统)的潜在优缺点。严格审查了自乳化系统的各个组成部分及其选择标准。各种科学家尝试通过吸附,喷雾干燥,冻干,熔融制粒,挤出等方法将液体自乳化药物递送系统(SEDDS)转变为固体SEDDS,以配制各种剂型,例如自乳化胶囊,片剂,控释药丸,珠子,微球,纳米颗粒,栓剂,植入物等也已包括在内。 SEDDS的配制是一种潜在的策略,可提供具有增强的生物利用度的新药物分子,这些分子大多表现出较差的水溶性。自乳化系统提供了优于其他药物输送系统的各种优势,而其他药物输送系统具有解决与所有类别生物药物分类系统(BCS)药物相关的各种问题的潜力。

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