正交试验优化尼索地平口腔黏附片处方

目的:优化尼索地平口腔黏附片制备处方。方法:采用正交试验设计,以含药层及保护层中卡波普与壳聚糖用量比例、乳糖含量、压片硬度为因素优化处方,并测定优化处方的生物黏附力和体外释放度。结果:优化的处方组成是含药层与保护层中卡波普与壳聚糖用量比例分别为22.5∶22.5、33.3∶16.7mg,乳糖为10mg,压片硬度为5kg;3批优化处方所制制剂平均生物黏附力为79.5g·cm-2,12h时平均体外累积释放度大于95%。结论:按照优化处方制备的尼索地平口腔黏附片具有理想的生物黏附力和缓释性。

Optimization of Nisoldipine Buccal Adhesive Tablets Formulation by Orthogoral Design

OBJECTIVE： To optimize the formulation of nisoldipine buccal adhesive tablets. METHODS： The formulation was optimized by orthogonal design with the dosage ratio of carhopol to chitosan in drug - containing layer and protection layer, the content of lactose and the tabletting hardness as factors. The bioadhesiveness and in vitro drug release rate of the tablets was measured as well. RESULTS： The optimal formulation was as follows： the ratio of carbopol to chitosan in drug - containing layer and protection layer were 22.5 ： 22.5 and 33.3 ： 16.7 mg, respectively; the dosage of lactose was 10 mg, and tabletting hardness was 5 kg. The averge bioadhesiveness of 3 bactbes of optimized preparations was 79.5 g·cm^2, and the average in vitro drug release rate of the tablets in 12 h was more than 95%. CONCLUSIONS： The optimized nisoldipine buceal adhesive tablets enjoy ideal bioadhesiveness and slow release character.