芳冰鼻吸剂的处方工艺优选

Optimization of Formulation for Fangbing Nasal Inhalants

目的:优选芳冰鼻吸剂的处方工艺。方法:以大鼠睡眠持续时间和入睡潜伏期的综合评分为评价指标,采用L9(34)正交试验考察薄荷脑、芳樟醇、冰片用量对芳冰鼻吸剂处方工艺的影响。以冰片、薄荷脑的溶解性及鼻吸剂气味为指标,通过单因素试验考察乙醇不同体积对该制剂释药速率的影响;以薄荷脑、芳樟醇、冰片的体外释放度为指标,结合睡眠剥夺药效验证,确定芳冰鼻吸剂的最佳处方。结果:最佳处方为冰片0.15 g,芳樟醇0.4 mL,薄荷脑0.070 9 g,90%药用乙醇0.1mL;潜伏期(13.26±1.51)min,睡眠持续时间(43.58±1.94)min。结论:芳冰鼻吸剂处方设计合理,药味芳香宜人,为中药肺部给药制剂的开发提供启发。

Objective： To optimize formulation of Fangbing nasal inhalants. Method： With sleep duration and sleep latency of rats as comprehensive evaluation indexes, L9 （3^4） orthogonal test was performed to optimize prescription by taking amounts of menthol, linalool and borneol as factors. Considering and measuring solubility of menthol and borneol, odor of nasal inhalants, single factor test was adopted to investigate effect of ethanol concentration on release of Fangbing nasal inhalants; taking in vitro release of menthol, linalool and borneol as indexes, combined with efficacy test of sleep deprivation to determine optimum formulation of this preparation. Result： Optimum formulation was as following： borneol 0. 15 g, linalool 0.4 mL, menthol 0. 070 9 g, 90% ethanol 0. 1 mL; under these conditions, incubation period and sleep duration were （ 13.26 ± 1.51 ） , （43.58 ± 1.94 ） min. Conclusion： This optimized formulation was reasonable with flavor of aromatic and pleasing, it could provide a references for development of pulmonary drug delivery of traditional Chinese medicine.