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目的建立Beagle犬血浆中米拉贝隆浓度测定的液相色谱串联质谱(LC-MS/MS)分析方法,研究米拉贝隆缓释片在犬体内的药动学特征。方法选取8只Beagle犬,雌雄各半,分成两组,每组4只,双交叉试验设计进行单剂量给药,分别给予50 mg受试制剂与参比制剂,采集不同时间血浆样品,采用LC-MS/MS分析方法测定Beagle犬体内的血药浓度并计算主要药动学参数。结果与米拉贝隆缓释片市售品(商品名:Myrbetriq)相比,米拉贝隆缓释片自制品的Cmax值为市售品相应参数的132.29%(几何均值为112.67%),相对生物利用度为106.37%(几何均值为100.45%)。结论米拉贝隆缓释片自制品与市售品的药代动力学参数之间比较差异未见统计学意义,提示自制品与市售品的药代动力学行为无显著差异。
Objective To establish a liquid chromatography-tandem mass spectrometry (LC-MS / MS) method for the determination of mirabelone concentration in plasma of Beagle dogs and study the pharmacokinetics of milabelon sustained-release tablets in dogs. Methods Eight Beagle dogs were randomly divided into two groups with 4 in each. Double-crossover trial was designed for single-dose administration of 50 mg of test and reference preparations respectively. Plasma samples from different time periods were collected and analyzed by LC The MS / MS method was used to determine the blood concentration in Beagle dogs and to calculate the main pharmacokinetic parameters. Results Compared with the commercial product of Mirabendan sustained-release tablets (trade name: Myrbetriq), the Cmax of the self-manufactured products of the Mirabendan sustained-release tablets was 132.29% (geometric mean 112.67%) of the corresponding parameters of the commercial products, The relative bioavailability was 106.37% (geometric mean 100.45%). Conclusion There was no significant difference between the pharmacokinetic parameters of the mirabeieron sustained-release tablets and the commercial products, which suggested that there was no significant difference between the pharmacokinetics of the self-manufactured and the commercial products.