摘要
目的 研究托吡酯片剂在健康人体内的药代动力学过程,并比较2种托 吡酯片剂的生物等效性。方法 用随机交叉给药方案,18名健康男性受试者 分别单剂量口服试验和参比托吡酯片剂100 mg,用毛细管气相色谱-氮磷检测 法(GC-NPD)测定血浆中托吡酯浓度,并评价2种制剂的生物等效性。结果 口服试验和参比托吡酯片剂后的Cmax分别为(2．05±0．45)和(1．97±0．43) μg·mL-1;tmax分别为(1．14±0．68)和(1．28±0．60)h;t1／2分别为(30．19± 5．01)和(31．07±4．67)h;AUC0-t分别为(52．00±8．84)和(52．88±9．84)μg· h·mL-1;AUC0-∞分别为(65．74±14．34)和(67．62±14．22)μg·h·mL-1,口 服试验和参比托吡酯片剂后的相对生物利用度F0-t为(99．12±10．50)％,F0-∞ 为(97．65±10．96)％。结论 试验和参比托吡酯片剂具有生物等效性。
Objective To study the pharmacokinetic characteristics of topiramate tablets in healthy volunteers, compare the bioequivalence of two topiramate tablets. Methods A single oral dose 100 mg of tested and referenced topiramate tablets were given to 18 healthy volunteers in a randomized cross- over. The gas chromatography with nitrogen phosphorus detection method was used to assay the concentration of topiramate in plasma. The pharmacokinetic parameters and bioequivalence were measured. Results The main pharmacokinetic parameters of topiramate by oral administration were as follow ： Cmax were （ 2. 05 ± 0. 45 ） and （ 1.97 ± 0. 43 ） μg·mL^-1, tmax were （ 1.14 ± 0.68 ） and （ 1.28 ± 0.60 ） h, t1/2 were （30. 19 ± 5.01 ） and （31.07 ±4. 67） h, AUC0-t, were（52.00 ±8.84） and（52. 88 ±9. 84）μg·h·mL^-1, AUC0-∞ were（65.74 ± 14. 34） and（67.62 ± 14.22） μg·h·mL^-1 for test and reference topiramate tablets, respectively. The relative bioavailability F0-t and F0-∞ were （99. 12 ± 10.50）% and （97.65 ± 10. 96）%, respectively. Conclusion The test and reference topiramate tablets are bioequivalence.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2005年第6期441-444,共4页
The Chinese Journal of Clinical Pharmacology
关键词
托吡酯片
毛细管气相色谱-氮磷检测法
药代动力学
生物等效性
topiramate tablet
gas chromatography with nitrogen phosphorus detection
pharmacokinetics
bioequivalence
