冰片对丹参脂溶性药效成分促吸收作用研究

Absorption-Promoting Effect of Borneol on Fat-Soluble Medicinal Ingredients of Salvia Miltiorrhiza

目的探讨冰片对丹参脂溶性药效成分二氢丹参酮Ⅰ、隐丹参酮、丹参酮Ⅰ和丹参酮ⅡA的促吸收作用,以及4种药效成分在大鼠血浆、脑和心脏组织中分布的影响。方法取SD大鼠20只,随机分为冰片组和未加冰片组,各10只,两组灌胃丹参醇提物后,冰片组立即灌胃冰片,测定给药30 min后4种药效成分的血药浓度,以及脑和心脏组织中的药物浓度。色谱柱采用Waters Symmetry C_(18)柱(250 mm×4. 6 mm,5μm),丙酸睾酮为内标,流动相为水-甲醇(22∶78),检测波长二氢丹参酮Ⅰ、丹参酮Ⅰ和丙酸睾酮为244 nm,隐丹参酮和丹参酮Ⅱ_A为266 nm。结果冰片组血浆样品可明显检测到隐丹参酮,而未加冰片组血浆样品中没有检测到隐丹参酮;冰片组心脏组织样品中隐丹参酮的峰高明显高于未加冰片组。两组的脑组织样品中均未检测到隐丹参酮,所有生物样品里均未检测到二氢丹参酮Ⅰ、丹参酮Ⅰ和丹参酮Ⅱ_A。结论丹参脂溶性药效成分的口服生物利用度很低,冰片能促进大鼠对隐丹参酮的吸收,能提高隐丹参酮在大鼠血液和心脏组织中的药物浓度。

Objective To investigate the absorption-promoting effect of borneol on the fat-soluble medicinal ingredients(such as dihydrotanshinoneⅠ,cryptotanshinone,tanshinoneⅠand tanshinoneⅡA)of Salvia miltiorrhiza,and to investigate the distribution of four medicinal ingredients in plasma,brain and heart of rats.Methods Totally20rats were randomly divided into borneol group and non-borneol group,and all the rats were given intragastric administration of ethanol extract of Salvia miltiorrhiza,then the rats in borneol group were given borneol immediately.After30min of administration,the concentration of four medicinal ingredients in blood,brain and heart tissues were detected,and the difference of drug concentration between the two groups was analyzed.Waters Symmetry C18column(250mm×4.6mm,5μm)was used as the chromatographic column,testosterone propionate was used as the internal standard,the mobile phase was water-methanol(22∶78),the detection wavelength of dihydrotanshinoneⅠ,tanshinoneⅠand testosterone propionate was244nm,the detection wavelength of cryptotanshinone and tanshinoneⅡA was266nm.Results Cryptotanshinone was detected in plasma samples of borneol group,but not in plasma samples of non-borneol group.The peak of cryptotanshinone in heart tissue samples of borneol group was higher than that of non-borneol group.Cryptotanshinone was not detected in brain tissue samples of the two groups,and dihydrotanshinoneⅠ,tanshinoneⅠand tanshinoneⅡA were not detected in all biological samples.Conclusion The oral bioavailability of fat-soluble medicinal ingredients of Salvia miltiorrhiza is very low.Borneol can promote the absorption of cryptotanshinone in rats and increase the concentration of cryptotanshinone in blood and heart tissues of rats.