| 引用本文: | 付伟,任秀华,陈倩,雷永芳,张冬林,杜光.多剂量口服马来酸曲美布汀缓释片的药动学及生物等效性研究[J].中国现代应用药学,2016,33(4):461-466. |
| FU Wei,REN Xiuhua,CHEN Qian,LEI Yongfang,ZHANG Donglin,DU Guang.Pharmacokinetics and Bioequivalence of Trimebutine Maleate Sustained-release Tablets with Multiple Dose Administration[J].Chin J Mod Appl Pharm(中国现代应用药学),2016,33(4):461-466. |
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| 摘要: |
| 目的 研究多剂量口服马来酸曲美布汀缓释片在中国健康人体内的药动学特征和生物等效性。方法 26名健康男性志愿者随机交叉多剂量早晚口服马来酸曲美布汀缓释片受试制剂或参比制剂300 mg，每日2次，连续6 d。采用HPLC-MS/MS测定血浆中曲美布汀和N-去甲基曲美布汀浓度，用DAS2.1药动学程序计算药动学参数，并进行生物等效性评价。结果 多剂量口服马来酸曲美布汀受试和参比制剂后，血浆曲美布汀Cmax分别为(35.668±22.196)，(33.022±16.077)ng·mL-1，tmax分别为(3.154±1.875)，(0.365±9.946)h，t1/2分别为(20.793±13.305)，(16.989±4.707)h，AUCss分别为(252.075±150.358)，(224.106±95.405)ng·h·mL-1；血浆N-去甲基曲美布汀Cmax分别为(1 571.809±823.169)，(1 623.535±536.813)ng·mL-1，tmax分别为(-0.250±11.259)，(2.481±1.237)h，t1/2分别为(9.796±2.450)，(9.220±2.009)h，AUCss分别为(11 254.863±5 746.620)，(10 911.059±4 111.751)ng·h·mL-1。受试制剂和参比制剂主要药动学参数均无显著性差异。结论 马来酸曲美布汀受试制剂与参比制剂具有生物等效性。 |
| 关键词: 曲美布汀 药动学 生物等效性 液-质联用 |
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| 基金项目:科技部重大专项“泌尿生殖系统肿瘤的国际化新药临床评价研究技术平台建设”；华中科技大学同济医学院附属同济医院新技术新业务项目“治疗药物与毒物监测及临床试验生物样本分析技术平台建设” |
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| Pharmacokinetics and Bioequivalence of Trimebutine Maleate Sustained-release Tablets with Multiple Dose Administration |
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FU Wei, REN Xiuhua, CHEN Qian, LEI Yongfang, ZHANG Donglin, DU Guang
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Department of Pharmacy, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China
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| Abstract: |
| OBJECTIVE To explore the pharmacokinetics and bioequivalence of trimebutine maleate sustained-release tablets with multiple dose administration in healthy Chinese volunteers. METHODS A multiple oral dose (300 mg of test or reference preparation twice a day for 6 days) were given to 26 male healthy volunteers in a randomized crossover study. The concentration of trimebutine and N-demethyl trimebutine in plasma were determined by HPLC-MS/MS. The pharmacokinetic parameters were calculated and the bioequivalence of 2 formulations were evaluated by DAS program. RESULTS After multiple dose, the pharmacokinetic parameters of the test and reference trimebutine were as follows: Cmax were (35.668±22.196), (33.022±16.077)ng·mL-1, tmax were (3.154±1.875), (0.365±9.946)h, t1/2 were (20.793±13.305)h and (16.989±4.707)h, AUCss were (252.075±150.358), (224.106±95.405)ng·h·mL-1, respectively. Meanwhile, the pharmacokinetic parameters of N-demethyl trimebutine were as follows: Cmax were (1 571.809±823.169), (1 623.535±536.813)ng·mL-1, tmax were (-0.250±11.259), (2.481±1.237)h, t1/2 were (9.796±2.450), (9.220±2.009)h, AUCss were (11 254.863±5 746.620), (10 911.059±4 111.751)ng·h·mL-1, respectively. CONCLUSION The test and reference preparation of trimebutine are bioequivalent. |
| Key words: trimebutine pharmacokinetics bioequivalence HPLC-MS/MS |
