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脂质——改善生物利用度差的药物口服递送的新兴平台。

Lipid--an emerging platform for oral delivery of drugs with poor bioavailability.

机构信息

Department of Pharmaceutics, Banaras Hindu University, Varanasi, India.

出版信息

Eur J Pharm Biopharm. 2009 Sep;73(1):1-15. doi: 10.1016/j.ejpb.2009.06.001. Epub 2009 Jun 6.

Abstract

The sole objective of pharmaceutical science is to design successful dosage forms which fulfill the therapeutic needs of the patients effectively. Development of new drug entities is posing real challenge to formulators, particularly due to their poor aqueous solubility which in turn is also a major factor responsible for their poor oral bioavailability. Lipids as carriers, in their various forms, have the potential of providing endless opportunities in the area of drug delivery due to their ability to enhance gastrointestinal solubilization and absorption via selective lymphatic uptake of poorly bioavailable drugs. These properties can be harvested to improve the therapeutic efficacy of the drugs with low bioavailability, as well as to reduce their effective dose requirement. The present communication embodies an in-depth discussion on the role of lipids (both endogenous and exogenous) in bioavailability enhancement of poorly soluble drugs, mechanisms involved therein, approaches in the design of lipid-based oral drug delivery systems with particular emphasis on solid dosage forms, understanding of morphological characteristics of lipids upon digestion, in vitro lipid digestion models, in vivo studies and in vitro-in vivo correlation.

摘要

制药科学的唯一目标是设计成功的剂型,有效地满足患者的治疗需求。新药物实体的开发给制剂师带来了真正的挑战,特别是由于它们的水溶性差,这也是导致其口服生物利用度差的主要因素。各种形式的脂质作为载体,由于能够通过选择性淋巴摄取生物利用度差的药物来增强胃肠道的溶解和吸收,因此具有在药物传递领域提供无尽机会的潜力。这些特性可用于提高生物利用度低的药物的治疗效果,并降低其有效剂量需求。本通讯深入讨论了脂质(内源性和外源性)在提高难溶性药物生物利用度方面的作用、相关机制、设计基于脂质的口服药物传递系统的方法,特别强调了固体剂型,理解脂质在消化过程中的形态特征、体外脂质消化模型、体内研究和体外-体内相关性。

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