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建立了液相色谱-串联质谱法测定健康志愿者口服瑞巴派特分散片(受试制剂)和普通片(参比制剂,膜固思达~(?))后的血药浓度,估算两制剂的药动学参数并评价生物等效性。采用随机、开放、双周期交叉试验设计,22名男性健康志愿者单剂量口服受试或参比制剂0.1 g后,血样经乙腈直接沉淀蛋白后进行LC-MS/MS分析,利用DAS2.1.1软件计算药动学参数,并进行生物等效性评价。受试和参比制剂在人血浆中瑞巴派特的c_(max)为(236.9±l 03.4)和(233.9±105.1)ng/ml,t_(max)为(2.7±1.1)和(2.9±1.4)h,t_(1/2)为(2.0±0.8)和(2.3±1.5)h,AUC_(0→12h)为(929.0±291.9)和(970.5±353.2)ngh·ml~(-1)。受试制剂的相对生物利用度为(102.6±29.8)%。
A liquid chromatography-tandem mass spectrometry (LC-MS / MS) method was developed for the determination of plasma concentrations of oral rebamipide dispersible tablets (test preparations) and normal tablets (reference preparations, Pharmacokinetic parameters of the formulation and evaluation of bioequivalence. Using a randomized, open and double-cycle crossover design, blood samples were directly precipitated by acetonitrile and analyzed by LC-MS / MS after a single oral dose of 0.1 g or 0.1 g of oral test drug or reference formulation in 22 healthy volunteers. Pharmacokinetic parameters were calculated and bioequivalence was evaluated. The c max values of the tested and reference preparations in human plasma were (236.9 ± 103.4) and (233.9 ± 105.1) ng / ml and the t max was (2.7 ± 1.1) and (2.9 ± (929.0 ± 291.9) and (970.5 ± 353.2) ngh · ml ~ (-1) for AUC_ (0 → 12h), t 1/2 for 2.0 ± 0.8 and 2.3 ± 1.5 h, . The relative bioavailability of the test preparation was (102.6 ± 29.8)%.