Studies on the in Vitro Dissolution of Insoluble Volatile Drug from Su-Anxin Nasal Inhalant and Its Correlation on the Nose Steady Self-Controllable Expiration and Inspiration at Night

In the paper, the in vitro dissolution of borneol in 12 hours from 6 batches of optimized inhalant samples were investigated. As a new dosage form, the in vitro release apparatus of nasal inhalant was invented and a pushing bump was used according to the simulation of the nose expiration and inspiration. Based on the data of r2 in the profile and similar factor f2 from 6 linear release tendencies, a good controlled release and a zero order tendency were observed. It can be suggested that there is a good correlation between the in vitro controlled release and the nose steady self-controllable expiration and inspiration, which will contribute to the trend of insoluble volatile drug controlled release and the effect of quick absorption in nasal pulmonary delivery to cure severe or acute cardiovascular or lung diseases at patients' sleeping, such as angina or breathing obstruction. Also, it was concluded that the prescription composed of insoluble volatile drugs can be prepared to be nasal inhalant from which drugs can be absorbed through nose steady self-controllable inspiration to the lung then into the blood and have a great effectiveness improvement of bioavailability at night timing drug delivery system.

苏安心鼻吸剂在家兔体内外药物成分的分析

目的分析苏安心鼻吸剂家兔体内外的药物化学成分,判断药物在家兔体内可能存在的代谢产物,为中药吸入制剂的开发奠定基础。方法采用气相-质谱联用(GC-MS)的技术,对苏安心鼻吸剂中苏合香、冰片等药物的化学成分进行了鉴别,同时,分析家兔经鼻吸入上述药物后血液中可能存在的药物成分,测定不同时间段冰片在家兔体内的血药浓度。结果体外方面,苏安心鼻吸剂中含有肉桂酸苄酯、苯甲酸苄酯、冰片、18-去松香烷等药物成分;家兔体内,冰片分别在第30分钟和第4小时出现血药峰浓度,同时观察到2-羟基苯甲酸甲酯的存在,而体外其它成分在家兔体内未观察到。结论体外的肉桂酸苄酯、苯甲酸苄酯、冰片等成分和方中苏合香、冰片的成分一致。冰片在家兔体内以原型成分吸收入血、分布、代谢和排泄,而苯甲酸苄酯和肉桂酸苄酯的代谢产物为2-羟基苯甲酸甲酯。从冰片的两个血药峰浓度现象可知冰片具有吸收快、消除快的特点,说明该制剂具有良好的速效、长效作用。