Takenaka H, Kawashima Y, Lin S Y
J Pharm Sci. 1980 May;69(5):513-6. doi: 10.1002/jps.2600690509.
Micronized sulfamethoxazole particles were microencapsulated using the gelatin-acacia complex conacervation method. The effects of the coacervation pH and the amount of formaldehyde used on the micromeritic parameters of the microcapsules were investigated. The particle-size and the wall thickness distributions were log-normal forms. As the pH was increased, the particle size decreased (8.5-28.5 micrometers). The porosity of various pH-adjusted microcapsules was between 0.158 and 0.277. The particle size of formalized microcapsules was larger than that of the unformalized microcapsules because formalization prevents shrinking of microcapsules during the dehydration and drying process. A smooth surface appeared on the unformalized microcapsule, but a net-like wrinkled structure was observed upon scanning the formalized one. Moreover, folding and invaginating structures were found on the spray-dried microcapsules. The optimum coacervation pH value was 3.5, at which the highest core content was obtained (77.5% w/w). Approximately 6.73 microgram of formaldehyde remained in 1 g of the microcapsules formalized with 50 ml of formaldehyde. The crystalline sulfamethoxazole in the microcapsules prepared by spray drying the coacervate slurries was changed into the amorphous form, while the microcapsules dried in the conventional manner showed the same sulfamethoxazole form as the starting substance.
采用明胶 - 阿拉伯胶复合凝聚法对微粉化的磺胺甲恶唑颗粒进行微囊化。研究了凝聚pH值和甲醛用量对微囊微观特性参数的影响。粒径和壁厚分布呈对数正态形式。随着pH值升高,粒径减小(8.5 - 28.5微米)。不同pH值调节的微囊孔隙率在0.158至0.277之间。甲醛化微囊的粒径大于未甲醛化微囊,因为甲醛化可防止微囊在脱水和干燥过程中收缩。未甲醛化微囊表面光滑,但扫描甲醛化微囊时观察到网状褶皱结构。此外,在喷雾干燥的微囊上发现了折叠和内陷结构。最佳凝聚pH值为3.5,此时可获得最高的核心含量(77.5% w/w)。用50 ml甲醛甲醛化的1 g微囊中残留约6.73微克甲醛。通过喷雾干燥凝聚物浆液制备的微囊中,结晶磺胺甲恶唑转变为无定形形式,而以传统方式干燥的微囊显示出与起始物质相同的磺胺甲恶唑形式。