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晶体工程提高难溶性药物的溶解度和生物利用度。

Crystal Engineering for Enhanced Solubility and Bioavailability of Poorly Soluble Drugs.

机构信息

Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran.

出版信息

Curr Pharm Des. 2018;24(21):2473-2496. doi: 10.2174/1381612824666180712104447.

Abstract

BACKGROUND

Crystal engineering is dealing with the creation of new structures and new properties in drug molecules through inter-molecular interactions. Researchers of pharmaceutical sciences have used this knowledge to alter the structure of crystalline medications in order to remedy the problems of more than 40% of the new designed drugs which suffer from low solubility and consequently, low bioavailability which have limited their clinical application.

METHODS

This review covers a broad spectrum of aspects of the application of crystal engineering in pharmaceutics and includes a comprehensive wide range of different techniques used in crystal engineering of active pharmaceutical ingredients (API) to compensate the low water solubility and bioavailability of drugs related specially to class II of biopharmaceutical classification system (BCS).

RESULTS

These techniques include; crystalline habit modification, polymorphism, solvates and hydrates, cocrystals, surface modification, crystallization, spherical agglomeration, liquisolid crystals and solid dispersions which are introduced and discussed in this review article.

CONCLUSION

Each of these techniques has advantages and limitations which are emphasized on them.

摘要

背景

晶体工程通过分子间相互作用来研究药物分子中新结构和新性质的创造。药物科学的研究人员利用这一知识改变结晶药物的结构,以解决超过 40%的新设计药物的溶解度低的问题,从而导致生物利用度低,限制了它们的临床应用。

方法

本综述涵盖了晶体工程在药剂学中的应用的广泛方面,包括在活性药物成分(API)的晶体工程中使用的各种技术的全面概述,以补偿与生物制药分类系统(BCS)第二类相关的药物的低水溶性和生物利用度。

结果

这些技术包括:晶体形态修饰、多晶型、溶剂化物和水合物、共晶、表面修饰、结晶、球形团聚、液固晶体和固体分散体,本文对这些技术进行了介绍和讨论。

结论

这些技术中的每一种都有其优缺点,都有其强调的地方。

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