Tirkkonen S, Turakka L, Paronen P
Department of Pharmaceutical Technology, University of Kuopio, Finland.
J Microencapsul. 1994 Nov-Dec;11(6):615-26. doi: 10.3109/02652049409051111.
Gelatin-acacia microcapsules containing indomethacin were prepared by a complex coacervation method. To improve the wetting of hydrophobic core material different surfactants, cationic benzalkonium chloride, anionic sodium lauryl sulphate (SLS) or non-ionic polysorbate 20, were used. The effects of surfactants on microencapsulation were investigated at concentrations below, at and above their critical micelle concentration (CMC) using three different stirring speeds (200, 310 and 420 rpm). A considerable fraction of the core was leached out during the dehydration of microcapsules with isopropanol when the capsules were prepared without surfactant, and especially with SLS. SLS was noted to be an unsuitable surfactant for this process of microencapsulation, and this was considered to be due to ionic complexes, solubilization of gelatin and too-effective spreading of small coacervate droplets. Benzalkonium chloride enhanced encapsulation at concentrations below and at CMC, but above CMC the encapsulation was slightly decreased due to too-effective spreading of coacervate. Polysorbate 20 enhanced encapsulation with all the concentrations allowing for the formation of intact-walled microcapsules. All the microcapsules reduced in size with increasing stirring speed. The two lowest concentrations of benzalkonium chloride and all the concentrations of polysorbate 20 increased microcapsule size due to a greater amount of the colloids being available in formation of thicker walled microcapsules. The dissolution of unencapsulated indomethacin was very slow, but the drug was released quickly from all the microcapsules whether or not any type of surfactant was used. A hydrophilic wall of gelatin-acacia microcapsules in itself ensured quick wetting of hydrophobic indomethacin.
采用复凝聚法制备了含吲哚美辛的明胶-阿拉伯胶微胶囊。为改善疏水性核心材料的润湿性,使用了不同的表面活性剂,即阳离子型苯扎氯铵、阴离子型十二烷基硫酸钠(SLS)或非离子型聚山梨酯20。在低于、等于和高于其临界胶束浓度(CMC)的浓度下,使用三种不同的搅拌速度(200、310和420转/分钟)研究了表面活性剂对微囊化的影响。当在不使用表面活性剂,尤其是不使用SLS的情况下制备微胶囊时,在使用异丙醇对微胶囊进行脱水过程中,相当一部分核心物质会被浸出。SLS被认为是这种微囊化过程不合适的表面活性剂,这被认为是由于离子复合物、明胶的增溶作用以及小凝聚液滴的过度有效铺展。苯扎氯铵在低于和等于CMC的浓度下增强了包封效果,但在高于CMC时,由于凝聚层的过度有效铺展,包封率略有下降。聚山梨酯20在所有浓度下都增强了包封效果,从而形成了完整壁的微胶囊。随着搅拌速度的增加,所有微胶囊的尺寸都减小了。苯扎氯铵的两个最低浓度以及聚山梨酯20的所有浓度都增加了微胶囊的尺寸,这是因为在形成壁厚更大的微胶囊时,有更多的胶体可用。未包封的吲哚美辛的溶解非常缓慢,但无论是否使用任何类型的表面活性剂,药物都能从所有微胶囊中快速释放。明胶-阿拉伯胶微胶囊的亲水性壁本身确保了疏水性吲哚美辛的快速润湿。