肉桂超微粉体外溶出度及主要药效学量效关系研究

目的 研究超微粉碎对肉桂中桂皮醛体外溶出度的影响；进行肉桂超微粉主要药效学的量效关系研究.方法 采用转篮法进行体外溶出实验,用HPLC法测定肉桂中桂皮醛的体外溶出量；用扭体法及热板法研究其镇痛作用；用炭末法研究其小鼠肠推进作用.结果 溶出度实验显示,肉桂超微粉中桂皮醛的相对累积溶出率高于普通粉.扭体法显示,肉桂能够明显降低醋酸所致小鼠扭体反应次数,超微粉在低剂量到中剂量间呈现出量效关系.热板法显示,除了超微粉大剂量组可明显提高小鼠的痛阈值,其他各组均无作用.小鼠肠推进实验显示,肉桂能显著促进小鼠的肠运动,超微粉在低剂量到大剂量间呈现出量效关系.结论 超微粉碎能促进肉桂中桂皮醛的体外溶出,增强药效,并呈现一定的量效关系.超微粉碎应用于肉桂药材具有一定的意义.

External Dissolution Rate and Dose -effect Relationship for Principal Pharmacodynamics of Superfine Powder of Cortex Cinnamomi Cassiae

Objective To study the effect of ultramicro smash technology on external dissolution rate of cinnamic aldehyde from Cortex Cinnamomi Cassiae.To study the dose-effect relationship for principal pharmacodynamics of the superfine powder. Methods Blasket stirring method and HPLC were used to study the external dissolution rate of cinnamic aldehyde.Methods of mice writhing response and hot plate were used to study analgesic activity.Charcoal powder propelling test of intestine was used to observe the effects on intestinal motility in mice. Results The external dissolution rate study showed the relative accumulated dissolution rate of cinnamic aldehyde in superfine powder was higher than ordinary powder.The method of mice writhing response showed Cortex Cinnamomi Cassiae could obviously decrease writhing times in mice as compared with ordinary.There was a dose-effect relationship in inhibiting intestinal motility from low dose to medium dose of superfine powder.Hot plate method showed there was no analgesic activity except for large dose group of superfine powder.Intestinal motility method in mice showed Cortex Cinnamomi Cassiae could obviously increase intestinal motility.There was a dose-effect relationship in inhibiting intestinal motility from low dose to large dose of superfine powder. Conclusion Micronization is helpful for the dissolution of the active components in Cortex Cinnamomi Cassiae and for increasing the potency.There is dose-effect relationship in principal pharmacodynamics of superfine powder.The application of super-crash in Cortex Cinnamomi Cassiae is significant.