扎来普隆片人体生物等效性

Bioequivalence of zaleplon tablets in healthy volunteers

目的 :评价国产扎来普隆片和胶囊的人体生物等效性。方法 :采用高效液相色谱荧光检测法 ,测定 2 0名健康男性志愿者单次交叉口服 1 5mg扎来普隆供试片和参比胶囊后血浆中不同时间点药物浓度 ,用 3P97程序 ,计算其药动学参数和相对生物利用度 ,评价两制剂的生物等效性。结果 :扎来普隆供试片和参比胶囊的药 时曲线均符合一房室模型 ,其AUC0 - 8分别为 (1 2 3 .6± 2 5 .6) μg·L- 1 ·h与 (1 2 8.6± 2 9.0 ) μg·L- 1 ·h ;Cmax分别为 (55 .9± 1 6 .2 ) μg·L- 1 与 (6 1 .6± 1 6 .7) μg·L- 1 ;Tpeak分别为 (1 .0± 0 .3)h与 (0 .99± 0 .2 2 )h ;T1 /2ke分别为 (1 .0 0± 0 .2 9)h与 (0 .93± 0 .1 3)h。经配对t检验 ,各药动学参数均无统计学差异 (P >0 .0 5)。结论 :供试片相对于参比胶囊的人体生物利用度为 (97.7± 1 4 .5) % 。

OBJECTIVE To evaluate the bioequivalence of zaleplon tablets in healthy volunteers.METHODS The drug concentrations in plasma were determined by high performance liquid chromatography RP(HPLC RP) method following a single oral dose of 15 mg of tested zaleplon tablets and reference zaleplon capsules given respectively to 20 healthy male volunteers in an open randomized crossover design. The pharmacokinetic parameters and relative bioavailability were calculated on the basis of compartment models by using 3p97 program to evaluate the bioequivalence of the two dosage forms.RESULTS The concentration time curves of the two dosage forms were fitted to one compartment model with oral absorption. AUC 0-8 of the tested drug and reference drug were ( 123.6 ± 25.6 ) μg·L -1 ·h and( 128.6 ± 29.0 ) μg·L -1 ·h, C max were ( 55.9 ± 16.2 ) μg·L -1 and ( 61.6 ± 16.7 ) μg·L -1 , T peak were ( 1.0 ± 0.3 ) h and ( 0.99 ± 0.22 ) h, T 1/2ke were ( 1.00 ± 0.29 ) h and ( 0.93 ± 0.13 ) h, respectively.These main pharmacokinetic parameters obtained showed no statistically significant difference between two products ( P > 0.05 ). CONCLUSIONS Both preparations are bioequivalent.The relative bioavailability of the tested tablet to reference capsule is ( 97.7 ± 14.5 )%.