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氨基酸衍生前药:提高临床批准药物生物利用度的一种方法。

Amino Acid Derived Prodrugs: An Approach to Improve the Bioavailability of Clinically Approved Drugs.

机构信息

Department of Pharmaceutical Sciences and Natural Products (DPSNP), Central University of Punjab, Bathinda-151401, Punjab, India.

出版信息

Curr Top Med Chem. 2021;21(24):2170-2183. doi: 10.2174/1568026621666210602154438.

Abstract

Amino acids derived prodrugs emerged as an attractive approach to improve oral delivery of drugs with low solubility and permeability. Conjugation of amino acids with parent drug molecules resulted in several-fold increases in water solubility. Acceptability of the amino acids derived prodrug approach increases day by day to fulfill the different characteristics needed to get the desired pharmacological or therapeutic activity. Due to the significant structural diversity of amino acids, various amino acids can be employed as a carrier to provide desirable Pharmacokinetic-Pharmacodynamic (PK-PD) characteristics. The present review focused on using amino acids as a carrier moiety to improve approved drugs' bioavailability. Attempts have been made to cover amino acid conjugated clinically available drugs.

摘要

氨基酸衍生前药作为一种有吸引力的方法,已经被用于提高具有低溶解度和通透性的药物的口服递送。将氨基酸与母体药物分子连接,可使水溶解度提高数倍。氨基酸衍生前药方法的可接受性日益提高,以满足获得所需药理或治疗活性所需的不同特性。由于氨基酸具有显著的结构多样性,因此可以使用各种氨基酸作为载体,提供理想的药代动力学-药效学(PK-PD)特征。本综述重点介绍了使用氨基酸作为载体部分来提高已批准药物的生物利用度。已经尝试涵盖了与氨基酸相连的临床可用药物。

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