| 临床常用尼群地平片在大鼠体内药代动力学比较研究 |
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| 引用本文： | 孙加琳,宋俊科,邢程,吕扬,杜冠华. 临床常用尼群地平片在大鼠体内药代动力学比较研究[J]. 中国临床药理学与治疗学, 2012, 17(7): 755-760 |
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| 作者姓名： | 孙加琳 宋俊科 邢程 吕扬 杜冠华 |
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| 作者单位： | 中国医学科学院北京协和医学院药物研究所,“药物靶点研究与新药筛选”北京市重点实验室,北京100050 |
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| 基金项目： | 中国药典委员会国家药品标准提同研究项目“药典品种晶型检测分析方法的建立(1680);卫生部公益性行业科研专项(200802041,200902008) |
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| 摘 要： | 目的:研究大鼠灌胃不同厂家尼群地平片后体内药代动力学的一致性.方法:固体灌胃给予SD雄性大鼠尼群地平50 mg/kg,用液质联用的方法测定不同时间的血药浓度,用DAS 3.0数据处理系统对测得的血药浓度数据进行药代动力学参数的计算.结果:三个原料药生产厂家的测定结果显示,晶Ⅳ型尼群地平原料药较常用晶型即晶Ⅰ型有着更好的药物吸收和相对生物利用度,为优势药物晶型;随机抽取的临床常用的16个不同厂家尼群地平产品的大鼠体内药代动力学参数结果呈现差异性,Cmax、tmax、t1-2、AUC(0-t)四个主要参数的最大差异分别可以达到2.5、24.4、4.5和1.6倍之多.结论:不同厂家的尼群地平片在大鼠体内的药代动力学过程存在显著差异,化合物的晶型状态是导致差异的一个重要因素.
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| 关 键 词： | 尼群地平 LC-MS 晶型 药代动力学 生物利用度 |
Pharmacokinetics of different nitrendipine tablets in rats |
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| SUN Jia lin , SONG Jun-ke , XING Cheng , LV Yang , DU Guan-hua. Pharmacokinetics of different nitrendipine tablets in rats[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2012, 17(7): 755-760 |
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| Authors: | SUN Jia lin SONG Jun-ke XING Cheng LV Yang DU Guan-hua |
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| Affiliation: | Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing Key Laboratory of Drug Targets Identification and Drug Screening,Beijing 100050,China |
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| Abstract: | AIM: To study the pharmacokinetics of different nitrendipine tablets in rats.METHODS: An LC-MS method was established for the detection of nitrendipine in plasma after a single oral dose of 50 mg/kg nitrendipine tablets.Pharmacokinetics parameters were calculated by DAS 3.0 data-processing system.RESULTS:Determination results of the three bulk drug manufactures indicated that nitrendipine form Ⅳ had a higher absorption and bioavailability than nitrendipine form Ⅰ which was commonly used.Pharmacokinetic parameters of the 16 products selected randomly from different industries were different after a single dose of 50 mg/kg.Maximum differences of Cmax,tmax,t1/2,AUC(0-t) came up to 2.5,24.4,4.5 and 1.6 times.CONCLUSION: There are differences among the pharmacokinetics of different nitrendipine tablets in rats.Crystal form is a principal element leading to the discrepancies. |
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| Keywords: | Nitrendipine LC-MS Crystal form Pharmacokinetics Bioavailability |
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