伊曲康唑纳米混悬膜剂的制备

Itraconazole Nanosuspension Films Preparation

〔目的〕通过单因素考察法筛选最适处方并制备伊曲康唑纳米混悬膜剂。〔方法〕以空白膜剂的外观和手感为指标,考察空白膜剂处方中各组分用量,筛选最佳用量;以平均粒径、多分散指数及Zeta电位值为指标,筛选伊曲康唑纳米混悬剂的稳定剂种类和用量,并确定最优配比;将纳米混悬剂与空白膜剂基质充分混匀,制备伊曲康唑纳米混悬膜剂。〔结果〕空白膜剂处方中各组分最佳用量为聚乙烯吡咯烷酮5.0%,十二烷基硫酸钠1.5%,甘油7.5%,羧甲基纤维素钠2.0%;伊曲康唑纳米混悬剂的稳定剂最优配比为泊洛沙姆、卡波姆和胆酸钠比例为10∶9∶1;制得的纳米混悬膜剂溶质分散均匀,无明显颗粒,色泽均一,黏性好,流动性好以及成膜时间较短,并测得其平均粒径为230.98 nm,PDI为0.224,电位值为29.85。〔结论〕我们通过单因素考察法筛选出了较为适合的伊曲康唑纳米混悬膜剂处方,并且能够制备出符合膜剂基本要求的伊曲康唑纳米混悬膜剂,为伊曲康唑纳米混悬膜剂的进一步开发奠定了基础。

〔Objective〕To screen the optimal formulation of itraconazole nanosuspension films by single-factor method and prepare it. 〔Methods〕The amount of each component was optimized through single-factor experiment, apparance and feel of the blank films were used for result evaluation; the sort, amount and best ratio of itraconazole nanosuspension stabilizer were determined by average particle size, dispersion index and zate potential value. The films could obtain by nanosuspension and base material of blank films fully mixed. 〔Results〕In the optimized formulation of blank films, PVP accounted for 5. 0%, the dosage of the sodium dodecyl sulfate for 1. 5%, glycerin accounted for 7. 5%, CMC-Na accounted for 5. 0%. The ratio of Poloxamer to carbomer to sodium cholate was 10∶ 9 ∶ 1 in this itraconazole nanosuspension. Solute was unifor m Ly dispersed in itraconazole nanosuspension films, the prepared films had suitable film formation time, good flowability and nice viscosified property, clear and even in color and size. And films size was 230. 98 nm, PDI 0. 224 and zeta potential was 29. 85. 〔Conclusion 〕The formulation of itraconazole nanosuspension films was optimized through single-factor experiment and successfully perpared it. It was laid the foundations for itraconazole nanosuspension films further development.