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目的:评价利培酮分散片与参比制剂维思通片的生物等效性。方法:采用开放、随机、双交叉试验,选择22名健康男性分别服用2 mg的受试制剂和参比制剂液质联用(LC-MS/MS)法检测受试者血浆中利培酮和9-羟基利培酮的浓度。结果:21名健康受试者口服受试制剂和参比制剂后,利培酮的主要药动学参数:AUC0-τ为(79.94±57.64)h·ng·ml-1和(79.13±58.15)h·ng·ml-1,AUC0-τ为(82.74±60.63)h·ng·ml-1和(81.69±60.65)h·ng·ml-1,Cmax为(14.74±7.64)ng·ml-1和(15.51±7.39)ng·ml-1,tmax为(1.2±0.8)h和(1.1±0.4)h,t1/2为(3.73±1.51)h和(3.68±1.33)h;相对生物利用度为(106.8±26.0)%。9-羟基利培酮的主要药动学参数:AUC0-τ为(327.29±87.98)h·ng·ml-1和(307.41±77.35)h·ng·ml-1,AUC0-τ为(348.02±96.58)h·ng·ml-1和(321.88±82.74)h·ng·m L-1,Cmax为(12.80±3.55)ng·ml-1和(11.89±3.54)ng·ml-1,tmax为(5.1±3.7)h和(4.6±3.1)h,t1/2为(23.58±6.04)h和(20.92±4.51)h;相对生物利用度为(107.6±18.1)%。结论:利培酮分散片与利培酮普通片生物等效。
OBJECTIVE: To evaluate the bioequivalence of risperidone dispersible tablet and reference formulation VST. Methods: Open-label, randomized, double-crossover trials were conducted in 22 healthy volunteers to test the plasma concentrations of risperidone and LC-MS / MS. 9-Hydroxy risperidone concentration. RESULTS: The main pharmacokinetic parameters of risperidone in 21 healthy volunteers were as follows: AUC0-τ (79.94 ± 57.64) h · ng · ml-1 and (79.13 ± 58.15) The mean AUC0-τ was (82.74 ± 60.63) h · ng · ml-1 and (81.69 ± 60.65) h · ng · ml-1, and the Cmax was (14.74 ± 7.64) ng · ml- And (15.51 ± 7.39) ng · ml-1, respectively. The tmax was (1.2 ± 0.8) h and (1.1 ± 0.4) h respectively, and the t 1/2 was (3.73 ± 1.51) h and (3.68 ± 1.33) h respectively. The relative bioavailability (106.8 ± 26.0)%. The main pharmacokinetic parameters of 9-hydroxy risperidone were AUC0-τ of 327.29 ± 87.98 h · ng · ml-1 and 307.41 ± 77.35 h · ng · ml-1, and the AUC0-τ of (348.02 ± 96.58, ng · ml-1 and (321.88 ± 82.74) h · ng · m L-1, respectively, with Cmax of (12.80 ± 3.55) ng · ml-1 and (11.89 ± 3.54) ng · ml- (5.1 ± 3.7) h and (4.6 ± 3.1) h, respectively, and t1 / 2 was (23.58 ± 6.04) h and (20.92 ± 4.51) h respectively. The relative bioavailability was (107.6 ± 18.1)%. Conclusions: Risperidone dispersible tablets are bioequivalent to Risperidone tablets.