桂利嗪自微乳化软胶囊的制备和溶出度的考察

 目的研制桂利嗪自微乳化软胶囊,并考察其溶出度,以降低药物溶出量受pH的影响。方法通过溶解度实验,三相图的绘制,体外乳化和稳定性实验确定最佳处方;以市售硬胶囊为参比制剂测定自微乳化软胶囊(SMESC)的溶出度。结果该自微乳化软胶囊中的乳化剂为聚山梨酯-80,助乳化剂为二甲基异山梨酯,油相为油酸;其最佳比例为4:2:1。SMESC在水,pH6.8缓冲液和0.1mol·L^-1HCl中,45min的溶出度分别为77.9%,87.4%和89.3%,而市售硬胶囊分别为2.4%,3.1%和101.5%。结论桂利嗪自微乳化软胶囊与市售硬胶囊相比,其在水和人工肠液中的溶出度有了显著的提高,且溶出量受pH值的影响较小。

Preparation of self-microemulsifying soft capsule and investigation of dissolution for cinnarizine in soft capsule

OBJECTIVE In order to decrease the influence of pH on the dissolution of cinnarizine, the self-microemulsifying soft capsule (SMESC) of cinnarizine was prepared and its dissolution property was investigated. METHODS Through solubility experiment, self-microemulsification in vitro, drawing phase diagram and investigating the stability of solution, the optimum formulation was determined for cinnarizine. The dissolutions of SMESC was measured, taking the commercoal capsule as reference. RESULTS In the optimum formulation, Tween80, Dimethyl isosorbide and oleate were. screened as emulsifier, co-emulsifier and oil phase, respectively. The optimized proportion was 4: 2:1. The dissolution of SMESC in distilled water, pH 6.8 phosphate buffer and 0.1 mol L~(-1) HCI were 77.9 %, 87.4 % and 89.3 %, while those of the commercial capsule were 2.4%, 3.1% and 101.5%, respectively. CONCLUSION In comparison with the commercial hard capsule, the dissolution of cinnarizine is sufficiently improved and is dissolved is slightly influenced by pH in the SMESC.