星点设计-效应面优化法优化三七总皂苷鼻腔用粉雾剂

目的:确定三七总皂苷鼻腔用粉雾剂的较优处方.方法:以人参皂苷Rb1 1 h、12 h和人参皂苷Rg1 1 h、12 h的累积释放度、制剂的生物粘附强度及蟾蜍上腭黏膜纤毛毒性为指标,采用星点设计-效应面优化法,确定较优处方.结果:当三七总皂苷、微晶纤维素和中等粘度羟丙基纤维素的比例分别为31%、60%和9%时,Rb1 1 h、12 h和Rg1 1 h、12 h的累积释放度分别为6.82%、53.25%和83.47%、95.09%,生物粘附强度为78 min,蟾蜍上腭黏膜纤毛持续运动时间为为生理盐水组的94.84%,几乎没有纤毛毒性.结论:应用星点设计-效应面优化法能够快速方便地得到三七总皂苷鼻腔用粉雾剂的较优处方.

Optimization of the intranasal powders of Panax Notoginseng Saponins by the central composite design-response surface methodology

AIM: To determine the optimized intranasal powders formulation of Panax Notoginseng Saponins(PNS). METHODS: According to the indexes of the in vitro release rate in 1h and 12h of Rb1 and Rg1, bioadhesive intensity and the ciliary toxicity in situtoad palatal mucosa of the preparations, the optimized formulation was determined by the central composite design-response surface methodology. RESULTS: When the correspondent percentage of PNS, microcrystalline cellulose (MCC) and moderate viscosity hydroxypropyl cellulose (H-HPC) was 31%, 60% and 9%, respectively, the release rate in 1h and 12h of Rb1 and Rg1 was 6.82%, 53.25% and 83.4%, 95.09%, respectively. The adhesive time was 78min, and the lasting time of ciliary movement after the rinsing of the PNS powders was 94.84% to the physiological saline group which suggested the powder was almost no toxicity. CONCLUSIONS: The optimized formulation of the PNS intranasal powder was obtained quickly and conveniently by the central composite design-response surface methodology.