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机构地区:[1]杭州市第一人民医院消化内科,杭州310006 [2]河北省消化病研究所河北医科大学第二医院消化内科,石家庄050000
出 处:《药物分析杂志》2006年第11期1626-1630,共5页Chinese Journal of Pharmaceutical Analysis
摘 要:目的:探讨丹参有效成分原儿茶醛经机体代谢前后、以及经不同状态机体代谢后含量的变化,及其与临床疗效的相关性,以及本法用于临床药效评估的可行性。方法:40% CCl_4,sc 9周制备 SD 大鼠肝纤维化模型。提取大鼠正常、病理丹参药物血清。原儿茶醛测定采用 HPLC 法,Alltima C_(18)色谱柱(250 mm×4.6 mm,5 μm),乙腈-4%冰醋酸水溶液为流动相,梯度洗脱,紫外检测波长为281 nm。结果:丹参生药及其药物血清内均可检出原儿茶醛。样本在6 d 内保持稳定。原儿茶醛测定平均回收率:生药110.5%,正常药物血清102%,病理药物血清105.2%;RSD(n=6)分别为0.37%,1.96%,1.51%。原儿茶醛含量:丹参生药0.22%,正常药物血清0.15%,病理药物血清0.19%(P<0.05);RSD(n=6)分别为0.33%,0.75%,1.24%。结论:本法可用于检测机体代谢对于药物(尤其中药)有效成分含量的影响及临床药效的评价。病理药物血清内原儿茶醛含量高于正常药物血清,与临床不同用药对象的不同用药效果一致,可能与体内口服药物的首过效应及分解代谢有关。Objectives :To detect the contents of protocatechuic aldehyde in Salvia miltiorrhiza Bge. , and the corresponding drug sera( normal and fibrotic drug sera) by HPLC. To compare the protocatechuic aldehyde in Salvia miltiorrhiza Bge. before it was taken in vitro and after being metabolized under different conditions ( normal and fibrosis) in vivo. To study the relationship of different levels of protocatechuic aldehyde to curative effects in clinic. To evaluate the possibility of using the method clinically to predict the effects of treatment. Methods:Inducing liver fibrosis in rats by 40% CCl4 ,sc, for 9 weeks. Extracting normal and fibrotic drug sera from rats. The separation of protocatechuic aldehyde by HPLC was performed in a Alltima C18 column(250 mm ×4.6 mm,5 μm) with a mobile phase of acetonitrile-4% glacial acetic acid solution by gradient elution. The detection wavelength being 281 nm. Results :The average recovery( n = 6) was 110.5% (Salvia miltiorrhiza Bge. ), 102% (normal drug sera) and 105. 2% (fibrotic drug sera)with RSD 0.37%, 1.96% and 1.51%, respectively (n = 6). The content of protocatechuic aldehyde was respectively 0.22% ,0.15% and 0.19% ( n =6 ,P 〈0.05) with RSD 0.33% ,0.75% and 1.24% ( n = 6) for raw Salvia miltiorrhiza Bge. , normal drug sera and fibrotic drug sera. Conclusion: HPLC is a quick and sensitive method, and is suitable for the determination of bioactive components in drugs ( especially Traditional Chinese Medicine) in vitro and after metabolized in vivo under different conditions. The results show that protocatechuic aldehyde could be found in both raw Salvia miltiorrhiza Bge. and its corresponding drug sera. The samples are stable in 6 days. The levels of protocatechuic aldehyde in drug sera are lower than that in raw medicine. Protocatechuic Aldehyde in fibrotic drug sera is more than that in normal sera,which may be caused by different "first pass effect" under different liver conditions and the analytic metabolism of
分 类 号:R917[医药卫生—药物分析学]
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