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分散有机溶剂酸催化水解在开发新的微胶囊化工艺技术中的应用。

Application of acid-catalyzed hydrolysis of dispersed organic solvent in developing new microencapsulation process technology.

机构信息

College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-gu, Seoul 120-750, Korea.

出版信息

J Microencapsul. 2012;29(4):380-7. doi: 10.3109/02652048.2011.651502. Epub 2012 Feb 3.

Abstract

The aim of this study was to evaluate a new microencapsulation technology employing an acid-catalyzed solvent extraction method in conjunction to an emulsion-based microencapsulation process. Its process consisted of emulsifying a dispersed phase of poly(D,L-lactide-co-glycolide) and isopropyl formate in an aqueous phase. This step was followed by adding hydrochloric acid to the resulting oil-in-water emulsion, in order to initiate the hydrolysis of isopropyl formate dissolved in the aqueous phase. Its hydrolysis caused the liberation of water-soluble species, that is, isopropanol and formic acid. This event triggered continual solvent leaching out of emulsion droplets, thereby initiating microsphere solidification. This new processing worked well for encapsulation of progesterone and ketoprofen that were chosen as a nonionizable model drug and a weakly acidic one, respectively. Furthermore, the structural integrity of poly(D,L-lactide-co-glycolide) was retained during microencapsulation. The new microencapsulation technology, being conceptually different from previous approaches, might be useful in preparing various polymeric particles.

摘要

本研究旨在评估一种新的微胶囊化技术,该技术采用酸催化溶剂萃取法结合乳液基微胶囊化工艺。其工艺包括将聚(D,L-丙交酯-共-乙交酯)和异丙基甲酸酯的分散相乳化在水相中。然后,向所得的油包水乳液中加入盐酸,以引发溶解在水相中的异丙基甲酸酯的水解。其水解导致水溶性物质,即异丙醇和甲酸的释放。这一事件引发了乳液液滴的持续溶剂浸出,从而引发微球的固化。这种新的处理方法适用于分别选择为非离子化模型药物和弱酸性药物的孕酮和酮洛芬的包封。此外,聚(D,L-丙交酯-共-乙交酯)的结构完整性在微胶囊化过程中得以保留。这种新的微胶囊化技术在概念上不同于以前的方法,可能对制备各种聚合物颗粒有用。

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