普伐他汀钠片和胶囊的人体生物等效性

Study on the bioequivalent evaluation of pravastatin sodium tablets and capsules

目的:评价健康受试者单剂量口服受试普伐他汀钠片剂、胶囊剂及参比普伐他汀钠片剂在人体内的生物等效性。方法:采用3周期的二重3×3拉丁方交叉试验设计,24名健康男性受试者随机交叉口服40mg的3种普伐他汀钠制剂。用HPLC法测定受试者体内普伐他汀钠的血药浓度变化,并进行生物等效性评价。结果:普伐他汀钠片剂、胶囊剂与参比制剂普伐他汀钠片的AUC0→∞分别为(234.3±45.0),(229.7±50.3),(243.0±40.9)μg·h·L-1;AUC0→T分别为(205.4±38.3),(202.8±40.1),(211.4±36.7)μg·h·L-1;tmax分别为(1.4±0.4),(1.4±0.3),(1.5±0.3)h;Cmax分别为(48.3±9.7),(49.0±12.5),(49.2±11.3)μg·L-1。普伐他汀钠片与胶囊的相对生物利用度分别为(97.5±10.7)%和(96.2±10.2)%。结论:经统计学分析,2种受试制剂均与参比制剂生物等效。

OBJECTIVE To evaluate the bioequivalence of pravastatin sodium tablets and capsules. METHODS Concentration of pravastatin sodium in plasma were determined by HPLC after 24 healthy male volunteers received a single dose of pravastatin sodium tablets, capsules and reference tablets in three-treatment,three-period, duplex 3 × 3 Latin square crossover design. RESULTS The main pharmacokinetic parameters of pravastatin sodium tablets, capsules and reference tablets were as followings： AUC0→∞ were （234. 3 ± 45.0）, （229. 7 ± 50. 3）, （243. 0 ±40. 9）μg·h·L^-1 , AUC0→T were （205. 4 ± 38. 3）, （202. 8 ± 40. 1）,（211.4± 36. 7）μg·h·L^-1 ; tmax were （1.4 ± 0. 4）, （1.4 ± 0. 3）, （1.5 ± 0. 3）h; Cmax were （48.3 ± 9. 7）, （49. 0 ± 12. 5）, （49. 2 ± 11, 3）μ· g· L^-1, respectively. CONCLUSION The results of statistic anlysis show that three preparations of Pravastatin Sodium are bioequivalent.