去氧氟尿苷胶囊的人体药物动力学及相对生物利用度

Pharmacokinetics and relative bioavailability of 5'-deoxy-5-fluo-rouridine capsule in Chinese healthy volunteers

目的:了解国产去氧氟尿苷胶囊在人体的药物动力学及相对生物利用度.方法:采用随机交叉试验设计,10例男性健康志愿者单剂量po试验品与参比品去氧氟尿苷胶囊400mg,以HPLC法测定血药浓度.结果:试验品与参比胶囊各项动力学参数为T_1/2:(19.35±3.69)与(17.50±3.06)min,t_(max):(38.5±14.7)与(33.5±8.5)min.c_(max):(3.35±0.93)与(3.42±0.98)μg/ml;AUC(o-T):(157.58±41.90)与(154.20±45.36)(μg·min)/ml .经交叉试验方差分析,上述药物动力学参数无统计学显著差异(P>0.05).结论:试验品与参比胶囊生物等效,试验品的相对生物利用度为(104.05±13.97)%.

AIM: To study the pharmacokinetics and relative bioavailability of 5'-deoxy -5-fluorouridine capsule in Chinese healthy volunteers. METHODS: Ten male Chinese healthy volunteers received po 400 mg 5'-deoxy-5-fluorouridine capsule in a random crossover design. Drug concentrations in serum were determined by high performance liquid chromatography. RESULTS: The pharmacokinetic parameters of tested and reference cap-sules were as follows: T_(1/2): (19. 35 ± 3.69) vs (17. 50 ± 3. 06)min, t_(max): (38. 5 ± 14. 7) vs (33. 5 ± 8. 5)min, c_(max): (3. 35 ± 0. 93) vs (3. 42 ± 0. 98)μg/ml, AUC_(0-T): (157. 58 ± 41. 90) vs (154. 20 ± 45. 36) (μg · min)/ml, respectively. There were no significant differences in the pharmacokinetic parameters above between the 2 capsules(P>0. 05). CONCLUSION: The relative bioavailability of 5'-deoxy-5-fluorouridine capsule is (104. 05 ± 13. 97) %. The re-sults suggest the 2 preparations have bioequivalence.