罗红霉素胶囊人体药物动力学及生物等效性研究  

Study of pharmacokinetics and relative bioavalability of roxithromycin

作　　者：严方[1] 杨劲[2] 赵陆华[1] 吴孟华[1] 谭喜莹[1] 潘娟[1] 

机构地区：[1]中国药科大学分析中心,南京210009 [2]中国药科大学药物代谢动力学研究中心,南京210009

出　　处：《中国现代应用药学》2006年第5期374-377,共4页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的建立人血浆中罗红霉素的HPLC-MS方法，测定其片剂的药物动力学参数及相对生物利用度。方法20名健康受试者随机交叉口服罗红霉素胶囊。血样用乙腈沉淀、离心后进入LC-MS分析系统，色谱柱：Hypersil C18ODS（5μm，25em×4．6mm）：流动相：10mmol／L醋酸铵缓冲液（pH3．5）-甲醇（15：85）；质谱条件：气动辅助电喷雾离子化，正离子检测，选择性离子检测（SIM），检测离子：罗红霉素m／z837．5[M＋H]^＋，克拉霉素m／z748．3[M＋H]^＋。结果在0．025～50μg／mL范围内峰比值（罗红霉素峰峰面积As和内标克拉霉素面积Ai的比值）与浓度线性关系良好（r=0．9999），最低定量限为3ng／mL。绝对回收率为85．87％～95．03％。罗红霉素片剂的相对生物利用度为（102．2±26．0）％。结论建立的分析方法灵敏、准确、简便，符合血浆样品的测定要求。受试制剂和参比制剂后，统计学结果表明：两种制剂生物等效。OBJECTIVE An HPLC-MS method was developed for determination of roxithromyein in human plasma to study the pharmacokinetie parameters in capsule and relative bioavailability. METHODS The plasma was added acetonitrile, vortexed and centrifuged. And the supernate was analyzed by LC-MS. A RP-eolumn （Hypersil ODS, 5μm, 25cm×4.6mm） was used with a mobile phase of methanol-acetate buffer solution （pH 3.5） （85：15）. LC-ESI MS was used in the selected ion monitoring （SIM） mode with target ions at m/z 837.5 for roxithromycin and m/z 748.3 for clarithromycin. RESULTS The standard curve was linear in the range of 0.025～50μg/mL. The limited concentration was 3ng/mL and the recovery was 85.87%～95.03%. The relative bioavilability of roxithromycin capsule was （102.2±26.0）%. CONCLUSION The assay was proved to be sensitive, accurate and suitable for pharmacokinetic study of roxithromycin. The results of pharmacokinetics study after oral administration roxithromycin capsules showed that the two formulations were bio-equivalent.

关 键 词：罗红霉素 HPLC/MS 药物动力学 相对生物利用度 

分 类 号：R961.1[医药卫生—药理学]