目的 用高效液相色谱-质谱联用法(LC-MS/MS)测定受试者口服多潘立酮制剂后的血药浓度,估算受试制剂和参比制剂的药代动力学参数,评价2种制剂的生物等效性和相对生物利用度.方法 采用随机二交叉设计试验,24例男性健康志愿受试者,单剂量口服受试制剂和参比制剂多潘立酮片.以LC-MS/MS测定血浆中多潘立酮的浓度.采用BAPP3.0软件处理计算主要药动学参数.结果 受试制剂和参比制剂血浆中多潘立酮的半衰期(t1/2)分别为(10.2±1.9)和(10.2±2.2)h;达峰浓度(Cmax)分别为(26±11)和(25±12)μg/L,达峰时间(tmax)分别为(0.7±0.5)和(0.6±0.3)h;药-时曲线下面积(AUC0～36 h)分别为(75±24)和(70±27)μg·h-1·L-1;AUC0-∞分别为(80±26)和(74±28)μg·h-1·L-1;人体相对生物利用度为(114±30)%.结论 2种制剂在健康人体内具有生物等效性.%Objective To evaluate the re]ative bioequivalence of two domperidone preparations in healthy Chinese volunteers by estimated pharmacokinetics based on plasma concentrations of the drugs detected by LC-MS/ MS. Methods A single oral dose of two preparations was given to 24 healthy male volunteers according to a randomized crossover design. Plasma drug concentrations were determined by LC-MS/MS. The pharmacokinetic parameters were calculated by BAPP3.0. Results The major pharmacokinetic parameters of domperidone in test and reference preparations were as follows: t1/2( 10.2±l.9)and (10.2±2.2)h, Cmax (26±11 )and (25 ±12) μg/L, tmax(0.7±0.5 )and (0.6±0.3)h, AUC0～36 h (75±24)and (70±27) μg· h-1· L-1, AUC0-∞(80±26 )and (74±28) μg· h 1· L 1, respectively. The relative bioavailability of test preparation was (114±30)％. Conclusion The two preparations were bioeqnivalent in human body.
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