提高吸收不良药物生物利用度的配方策略,特别强调自乳化系统。

Shweta Gupta, Rajesh Kesarla, Abdelwahab Omri
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引用次数: 285

摘要

水溶性差的候选药物正变得越来越普遍。据估计,大约60-70%的药物分子在水介质中不能充分溶解和/或渗透性很低,因此口服给药后无法从胃肠道(GIT)充分和可重复吸收。配方科学家必须采取各种策略来提高它们的吸收。脂质制剂被认为是对抗这些挑战的一种很有前途的方法。本文综述了各种传统技术和新技术的优缺点,特别是自乳化系统。对自乳化系统的各种组成部分及其选择标准进行了严格的审查。各种科学家通过吸附、喷雾干燥、冻干、熔融造粒、挤压等方法将液体自乳化给药系统(SEDDS)转化为固体自乳化给药系统,以配制各种剂型,如自乳化胶囊、片剂、控释颗粒、微珠、微球、纳米颗粒、栓剂、植入物等。SEDDS的配方是一种潜在的策略,以提供具有提高生物利用度的新药物分子,主要表现为水溶性差。自乳化系统与其他药物传递系统相比具有各种优点,具有解决与生物制药分类系统(BCS)所有类别的药物相关的各种问题的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Formulation strategies to improve the bioavailability of poorly absorbed drugs with special emphasis on self-emulsifying systems.

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).

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