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不同剂型琥珀酸美托洛尔在大鼠体内的药代动力学对比研究
温慧敏,尹小娟,杨沙,杨昭武,刘森,张忠,庞超平
0
(四川省骨科医院;四川志禾药业集团有限公司)
摘要:
【摘要】 目的 研究琥珀酸美托洛尔普通颗粒与自制缓释微丸的药代动力学行为,并验证缓释微丸的缓释特性,为后期开展缓释制剂研究打下基础。方法 将大鼠随机分为普通组、缓释组各6只,每组雌雄各3只,普通组大鼠单次口服琥珀酸美托洛尔普通颗粒,缓释组大鼠单次口服等剂量的琥珀酸美托洛尔缓释微丸。采用LCMS/MS法测定血药浓度,采用DAS 2.1.1版药代动力学软件计算药代动力学参数,采用SPSS130统计学软件进行统计学分析。结果 结果表明,两种剂型的AUC(0t) 、AUC(0∞) 、Cmax以及MRT(0t)、MRT(0∞)、t1/2z、Tmax差异显著,具有统计学意义。结论 琥珀酸美托洛尔自制缓释微丸具有显著的缓释特性。可为新剂型的研制、开发提供资料参考。
关键词:  琥珀酸美托洛尔  普通颗粒  缓释微丸  药代动力学
DOI:
基金项目:四川省中医药管理局中医药科学技术研究专项中青年课题(2014K125)
Different dosage form succinate metoprolol in rats in vivo pharmacokinetic research
WEN Huimin,YIN Xiaojuan,YANG Sha,YANG Zhaowu,LIU Seng,ZHANG Zhong,PANG Chaowping
(Sichuan Orthopeadic Hospital;Sichuan Zhihe Pharmaceutical Group Co., Ltd)
Abstract:
【Abstract】 Objective To study the succinic acid metoprolol ordinary particles with homemade slowrelease the pharmacokinetic behavior of micro pill, verify that slow release characteristics of slow release micro pill and lay the foundation for later research on sustainedrelease preparations. Methods Rats were randomly divided into normal group, lowdose group, each group of male and female 3 only. The normal group was tresated with single oral metoprolol succinic acid in rats of ordinary particles. The slowrelease group was treated with a single oral dose of succinic acid such as metoprolol sustainedrelease micro pill. The LC MS/MS method was used to detect the blood drug concentration. Results Statistical results shown that the two formulations of AUC (0 t), AUC (0 up), Cmax and the MRT (0 t) and the MRT (0 up), t1/2 z, Tmax were significantly different. Conclusion Homemade succinate metoprolol sustainedrelease micro pill has significant sustained release characteristics.
Key words:  Succinic acid metoprolol  Ordinary particles  Slow release micro pill  Pharmacokinetic

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