摘要
目的通过对比分析在偏头痛模型下,制备物及其纯成分的不同药物形式在大鼠体内红景天苷、酪醇成分药物动力学特性表征及其相互作用性(PK-DI),以得到最佳药物体系及其组成形式。方法采用UPLC-PDA同时测定模型大鼠体内红景天苷、酪醇血药浓度分析法,获得各药物体内药代动力学表征数据,采用PK-DI关联分析法对比分析4种药物形式的特性表征。结果制备物组、纯配制组,经偏头痛大鼠口服给药后体内可同时检出相应红景天苷与酪醇2种成分,而纯红景天苷、纯酪醇高剂量组口服给药后体内只有相应单一成分可检出,但纯酪醇低剂量组在相同于制备物剂量下未检出。药代动力学表征为各组红景天苷基本相同,而酪醇在与红景天苷成分共存状态下发生明显改变。红景天苷体内生物利用度在制备物组、纯配制组、纯红景天苷组3组间无明显差异;酪醇体内生物利用度排序为:制备物组>纯配制组>纯酪醇高剂量组。结论在偏头痛模型下,红景天苷主要以原型类药形式存在,而酪醇在与红景天苷共存药物状态下,最大血药浓度大幅增加,且药代动力学表征发生了改变,使酪醇与红景天苷表征出协同吸收,从而构成抗偏头痛最佳药物体系。这为红景天苷制备物药物的研制提供了研究思路,同时亦为相关药物创新提供研究支撑。
objective To obtain the optimum medicinal system and its composition form, by the way of comparation of pharmacokinetic characteristics of different medicinal forms of salidroside and tyrosol in the rat model of migraine. Methods The plasma concentrations of salidroside and tyrosol after oral administration in rat model were measured by UPLC-PDA, by which the data of pharmacokinetic characteristics were obtained. Then the characteristics of different forms of salidrosides and tyrosol were compared by correlation analysis （PK-DI）. Results Both salidroside and tyrosol were detected in preparations group and mixed group （pure salidroside mixed with pure tyrosol ）. Only salidroside or tyrosol was detected in pure salidroside group and high-dose pure tyrosol group respectively. While nothing was found in low-dose pure tyrosol group whose concentration was equivalent to preparations of salidroside. There was no difference in bioavailability of salidroside showed in preparation group, mixed group and pure salidroside group, on the contrary, those of tyrosol showed significant difference in preparation group, mixed group, low-dose tyrosol in ascending order. Conclusion Salidroside was retained unchanged in migraine model rat after oral administration, however, for tyrosol, a substantial increase of maximum plasma concentration and changed pharmacokinetics parameters showed under the condition of salidroside coexisted. The best medicinal system in treating migraine was found and supported by synergistic effects of salidroside and tyrosol, by which provide techniques for medicinal research and development.
出处
《北京中医药大学学报》
CAS
CSCD
北大核心
2014年第10期696-700,共5页
Journal of Beijing University of Traditional Chinese Medicine
基金
十二五国家科技支撑计划项目(No.2012BAI29B06)
北京中医药大学创新团队项目(No.2011-CXTD-12)
北京中医药大学重点学科开放课题(No.2013-2DXKKF-23)
