国产依贝沙坦片剂人体药动学及生物等效性评价

Studies on the pharmacokinetics and bioequivalence of domestic irbesartan tablet in healthy volunteers

目的 评价国产和进口依贝沙坦片剂在人体生物等效性。方法 采用高效液相色谱荧光检测法测定 2 4名健康受试者po 30 0mg依贝沙坦后 ,血浆中依贝沙坦的浓度。 结果 国产依贝沙坦片剂和进口片剂的tmax分别为 (1.90± 0 .6 3)和 (2 .0 0±0 .6 3)h ,cmax为 (40 5 8.16± 12 39.4 5 )和 (40 12 .5 4± 14 4 9.71) μg·L-1,AUC0～ 48为 (194 18.91± 3991.0 )和 (1976 0 .38±4 12 7.12 ) μg·h·L-1,t1/ 2ke为 (10 .2 3± 1.6 3)和 (10 .4 1± 2 .4 8)h。国产依贝沙坦片剂的相对生物利用度为 (98.9± 10 .8) %。结论 经统计学分析 。

OBJECTIVE: To observe the bioavailability of domestic irbesartan tablet and imported tablet. METHODS: A single oral dose of 300 mg domestic or imported irbesartan tablet was given to 24 healthy volunteers in a randomized crossover study. Irbesartan concentrations in plasma were determined by HPLC methods. RESULTS The main pharmacokinetics of the two products were as follow: tmax were (1.90 ± 0.63) h and (2.00 ± 0.63) h, cmax were (4058.16 ± 1 239.45) μg &middot L-1 and (4012.54 ± 1449.71) μg &middot L-1, AUC0∼48 were (19 418.91 ± 3 991.0) μ &middot h &middot L-1 and (19 760.38 ± 4 127.12) μ &middot h &middot L-1, t1/2kc were (10.23 ± 1.63) h and (10.41 ± 2.48) h respectively. The relative bioavailability of domestic to imported tablets was (98.9 ± 10.8) %. CONCLUSION: There were no significant difference between the two parameters (P > 0.05). The results demonstrated that the two preparations were bioquivalent.