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用于提高难溶性药物溶解度的各种聚合物及基于聚合物的技术的应用:综述

APPLICATION OF VARIOUS POLYMERS AND POLYMERS BASED TECHNIQUES USED TO IMPROVE SOLUBILITY OF POORLY WATER SOLUBLE DRUGS: A REVIEW.

作者信息

Muhammad Sarfraz Rai, Bashir Sajid, Mahmood Asif, Ahsan Haseeb, Riaz Humayun, Raza Hina, Rashid Zermina, Atif Raza Syed, Asad Abrar Muhammad, Abbas Khawar, Yasmeen Tahira

出版信息

Acta Pol Pharm. 2017 Mar;74(2):347-356.

Abstract

Solubility is concerned with solute and solvent to form a homogenous mixture. If solubility of a drug is low, then usually it is difficult to achieve desired therapeutic level of drug. Most of the newly developed entities have solubility problems and encounter difficulty in dissolution. Basic aim of solubility enhancement is to achieve desired therapeutic'level of drug to produce required pharmacological response. Different techniques are being used to enhance the solubility of water insoluble drugs. These techniques include particle size reduction, spray drying, kneading method, solvent evaporation method, salt formation, microemulsions, co-solven- cy, hydrosols, prodrug approach, supercritical fluid process, hydrogel micro particles etc. Selection of solubility improving method depends on drug properties, site of absorption, and required dosage form characteristics. Variety of polymers are also used to enhance solubility of these drugs like polyethylene glycol 300, polyvinyl pyrrolidone, chitosan, β-cyclodextrins etc.

摘要

溶解度涉及溶质和溶剂形成均匀混合物的过程。如果一种药物的溶解度较低,那么通常很难达到所需的药物治疗水平。大多数新开发的药物实体都存在溶解度问题,并且在溶解方面遇到困难。提高溶解度的基本目的是达到所需的药物治疗水平,以产生所需的药理反应。人们正在使用不同的技术来提高水不溶性药物的溶解度。这些技术包括减小粒径、喷雾干燥、捏合法、溶剂蒸发法、盐形成、微乳、助溶、水溶胶、前药方法、超临界流体工艺、水凝胶微粒等。溶解度提高方法的选择取决于药物性质、吸收部位和所需剂型特征。多种聚合物也被用于提高这些药物的溶解度,如聚乙二醇300、聚乙烯吡咯烷酮、壳聚糖、β-环糊精等。

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