伊曲康唑纳米混悬凝胶剂的制备

The preparation of itraconazole nanoparticle suspension gel

〔目的〕制备伊曲康唑纳米混悬凝胶剂。〔方法〕以凝胶剂的外观形态为考查指标,筛选空白凝胶的处方;运用高压匀质法,以粒径、多分散指数(PDI)及zeta电位值为指标,考察并筛选出伊曲康唑纳米混悬剂的制备工艺及稳定剂的种类和比例。〔结果〕空白凝胶的处方为卡波姆0.50 g,硒化卡拉胶0.15 g,尼泊金乙酯0.05 g,甘油12.5 g,三乙醇胺0.35 g,加蒸馏水至100 g;制备伊曲康唑纳米混悬剂的稳定剂为泊洛沙姆、卡波姆、胆酸钠,比例为10∶9∶1;纳米混悬剂最佳制备工艺为500 bar/循环9次;1 000 bar/循环20次。〔结论〕采用我们的方法可以制得黏度适宜、稳定性好的乳白色伊曲康唑纳米混悬凝胶剂。

〔Objective〕To prepare traconazole nanoparticle suspension gel. 〔Methods〕To screen the formulation of blank gel, the appearance of gel was used as index. Itraconazole nanosuspension was prepared by high pressure homogenization and then manufactured into drug-loading gel by mixed with blank gel. Taking the particle size, PDI and Zeta potential as index, preparation procedures of itraconazole nanosuspension and type and proportion of stabilizer were exa mined. 〔Results〕The amount of blank gel prescription was 0. 50 g, 0. 15 g, 0. 05 g, 12. 5 g, 0. 35 g for control, and carbomer, selenide carrageenan, nipagin, glycerol,triethanola mine, respectively. And added distilled water to 100g; the best ratio of itraconazole nanosuspension stabilizer was poloxamer to carbomer to sodium cholate at 10∶ 9∶ 1. The best preparation process was 500 bar /9 cycles; 1 000 bar /20 cycles.〔Conclusion〕The sui Table. viscosity and s Table. milky itraconazole nanosuspension gel could obtain by this method.