Ueda M, Nakamura Y, Makita H, Kawashima Y
Pharmaceutical Research Laboratories, Dainippon Pharmaceutical Co. Ltd, Osaka, Japan.
J Microencapsul. 1993 Jan-Mar;10(1):25-34. doi: 10.3109/02652049309015309.
A novel microencapsulation method was developed by using the wet spherical agglomeration (WSA) technique. Spherical agglomerates containing enoxacin (ENX) or lactose were prepared in the acetone-n-hexane-ammonia water (or distilled water) solvent system, and were microencapsulated continuously with the aminoalkylmethacrylate copolymer (Eudragit RS). Microencapsulation was performed with a modified organic phase separation by the non-solvent addition method. By selecting proper composition ratio of acetone and n-hexane, the WSA solvent system turned to a non-solvent for a wall material, i.e. Eudragit RS. Dichloromethane was used as a good solvent because it did not affect the characteristics of spherical agglomerates prepared in the WSA system. With this technique the Eudragit RS coacervate droplets were firstly generated in the solvent composed of a higher acetone volume ratio in the acetone/n-hexane mixture, and continuously the coacervate droplets were deposited efficiently onto the agglomerates by adding additional n-hexane into the system. Spherical microcapsules with the size ranged between 100 and 1000 microns, were successfully produced owing to the spherical shape of agglomerates containing ENX or lactose.
通过使用湿式球形团聚（WSA）技术开发了一种新型微囊化方法。在丙酮-正己烷-氨水（或蒸馏水）溶剂体系中制备了含有依诺沙星（ENX）或乳糖的球形团聚物，并用甲基丙烯酸氨基烷基酯共聚物（Eudragit RS）对其进行连续微囊化。微囊化通过非溶剂添加法采用改良的有机相分离进行。通过选择丙酮和正己烷的适当组成比例，WSA溶剂体系转变为壁材即Eudragit RS的非溶剂。二氯甲烷用作良溶剂，因为它不影响在WSA体系中制备的球形团聚物的特性。利用该技术，首先在丙酮/正己烷混合物中丙酮体积比更高的溶剂中产生Eudragit RS凝聚层液滴，然后通过向体系中添加额外的正己烷，将凝聚层液滴有效地沉积在团聚物上。由于含有ENX或乳糖的团聚物呈球形，成功制备出了尺寸在100至1000微米之间的球形微胶囊。
