醋氯芬酸缓释微丸在犬体内的药动学及相对生物利用度

Pharmacokinetics and relative bioavailability of aceclofenac sustained-release pellets in dogs

目的:评价自制醋氯芬酸缓释微丸在犬体内的药动学和相对生物利用度。方法:3只犬分别单剂量服用自制醋氯芬酸缓释胶囊和市售醋氯芬酸普通胶囊,剂量均为200 mg。1周后两组交叉用药。采用HPLC法,以乙萘酚为内标测定犬给药后不同时间的血药浓度,用3P87软件估算药动学参数和相对生物利用度。结果:参比制剂和测试制剂的Tmax分别为(3．33±0．58)和(7．33±0．58)h,Cmax分别为(17．12±0．48)和(12．26±0．27)μg·mL-1, AUC0～24h分别为(96．26±21．70)和(133．22±24．50)μg·h·mL-1。统计分析显示,各主要药动学参数均有显著性差异。醋氯芬酸缓释微丸相对于普通胶囊的平均生物利用度为142．6％。结论:醋氯芬酸缓释微丸具有明显的缓释特征,其生物利用度优于醋氯芬酸普通胶囊。

Objective： To assess the relative bioavailability and bioequivalence of aceclofenac sustained release pellets in dogs. Methods： Three dogs were orally supplemented with a single dose of aeeelofenae sustained-release pellets （test） or aeeelofenae capsules （reference）, 200 mg each. The crossover dosing was taken in one week after the first single dose. The blood samples of the dogs were collected to measure the blood-drug concentration curve by HPLC with aethyl-naphthol as internal standard. The pharmaeokinetic parameters and relative bioavailability were determined using a 3P87 program. Resuits： The pharmacokinetic parameters of the reference and test samples were as follow： Tmax （3.33 ± 0.58） vs. （7.33 ±0.58）h,C max（17.12 ±0.48）vs. （12.26 ±0.27）μg·mL^-1 and AUC0-24 （96. 26 ± 21.70） vs. （133.22 ±24.50）μg·h·mL^-1; the P values of these parameters showed a statistical difference. The relative bioavailability of the test samples was 142.6%. Conclusion： The aceclofenac sustained release pellets feature a sustained release profile, and had superior bioavailability to the aceclofenac capsules