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Solid Dispersion: A Mechanistic and Realistic Approach on Antihypertensive Drug as a Drug Carrier System
ASSAY and Drug Development Technologies ( IF 1.6 ) Pub Date : 2021-07-12 , DOI: 10.1089/adt.2020.1055
Pallavi Swarup 1 , Gopal Prasad Agrawal 2
Affiliation  

A major percentage of the new chemical entities are reported to have poor aqueous solubility. Several antihypertensive drugs used clinically have either low solubility or high hepatic metabolism, thereby presenting low bioavailability (BA) and high pharmacokinetic variability. Improving the aqueous solubility of drug molecules would assist in overcoming the variability, and several approaches for improving solubility have been reported. Solid dispersion (SD) is known as a potential technique to conquer the problem of poor aqueous solubility and low BA. Drug solubility is improved by increasing the wetting property of drugs. This review is focused on discussing various approaches to improve solubility, classification, and different approaches used for formulation of SDs, along with special emphasis on the application of the SD approach for improving solubility and eventually enhancing dissolution and increasing the BA of antihypertensive drugs. The review leads to the conclusion that the use of more than one polymeric carrier for formulating SDs might help in overcoming storage and stability issues and in increasing the commercial viability and success of SDs.

中文翻译:

固体分散体:抗高血压药物作为药物载体系统的一种机制和现实方法

据报道,大部分新化学实体的水溶性较差。临床上使用的几种抗高血压药物具有低溶解度或高肝脏代谢,因此呈现出低生物利用度(BA)和高药代动力学变异性。提高药物分子的水溶性将有助于克服可变性,并且已经报道了几种提高溶解度的方法。固体分散体(SD)被认为是克服水溶性差和低BA问题的潜在技术。通过增加药物的润湿性来提高药物溶解度。这篇综述的重点是讨论提高溶解度、分类的各种方法,以及用于配制 SD 的不同方法,同时特别强调应用 SD 方法来提高溶解度并最终提高溶出度并增加抗高血压药物的 BA。审查得出的结论是,使用一种以上的聚合物载体来配制 SD 可能有助于克服储存和稳定性问题,并提高 SD 的商业可行性和成功率。
更新日期:2021-07-14
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