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。

Analysis of in vitro and in vivo Drug Components from Su-anxin Nasal Inhalant in Rabbit

Objective To identify in vitro and in vivo drug components from Su-anxin nasal inhalant and obtain the possible metabolites in rabbits,which may found a good base for the development of nasal inhalant of tradition Chinese medicine. Methods Rabbits were selected as the models and the method of gas chromatography and mass spectrum （GC-MS） was used to identify in vitro and in vivo chemical components of volatile drugs borneol and styrax in nasal inhalant. And the blood concentrations of borneol in rabbits in interval time were determined. Results The in vitro drug components included benzyl benzoate,benzyl cinnamate,18-norabietane and borneol etc. However,only borneol and 2-hydroxy methyl benzoate were found in vivo,and the former having two peak blood concentrations at 30 minutes and 4 hours after administration,respectively. Conclusion The in vitro drug components benzyl benzoate,benzyl cinnamate,and borneol are in accordance with the components from styrax and borneol. The analysis of the in vivo chemical components showed that original borneol and metabolite 2-hydroxy methyl benzoate from benzyl benzoate and benzyl cinnamate entere into the rabbit blood to get an effectiveness,and other components in vitro were not found in vivo. The two peak concentrations of borneol in blood suggests that borneol has a characteristic of quick absorption and quick excretion and Su-anxin nasal inhalant has a quick and prolonged effectiveness to cure cardiovascular diseases.