双氯芬酸钠缓释胶囊的人体药动学及生物等效性

Pharmacokinetics and Bioequivalence of Diclofenac Sodium Sustained-Release Capsules

18名男性健康志愿者单剂量和多剂量交叉口服两种双氯芬酸钠缓释胶囊,用HPLC法测定血浆中的药物浓度。单剂量口服受试胶囊和参比胶囊100mg后的tmax为(3.4±0.9)和(3.3±0.9)h,cmax为(416.0±183.5)和(466.3±238.2)ng/ml,AUC0-∞为(1986.3±713.1)和(2137.1±871.0)ng·h·ml-1。受试胶囊的相对生物利用度为(95.6±19.9)%。多剂量试验(100mg/d,连续6d)表明,受试和参比胶囊tmax为(3.7±0.9)和(3.6±1.0)h,cmax为(322.4±93.5)和(337.8±104.9)ng/ml,AUCss为(1618.6±424.4)和(1728.1±454.3)ng·h·ml-1。受试胶囊的相对生物利用度为(94.3±8.1)%。双单侧t检验结果表明,两种胶囊具有生物等效性。

Two brands of diclofenac sodium sustained-release capsules were orally given to 18 healthy male volunteers to investigate the bioequivalence with single-dose and multiple-dose randomized cross-over designs. The drug concentration in plasma was determined by HPLC. The results showed that tmax, Cmax, and AUC0-∞ of the test （T） and reference （R） capsules after single oral administration of 100mg were （3.4±0.9） and （3.3±0.9）h, （416.04±183.5） and （466.34±238.2） ng/ml, （ 1986.3±713.1 ） and （2137.1±871.0） ng·h·ml^-1, respectively. The tmax cmax and AUCss in the multipledose test （100mg/d for 6d） were （3.7±0.9） and （3.6±1.0）h, （322.4±93.5）and （337.8±104.9）ng/ml, （1618.6±424.4） and （1728.1±454.3） ng·h·ml^-1, respectively. The relative bioavailability of T capsules in single-dose and multiple-dose tests were （95.6±19.9） % and （94.3±8.1） %. Two capsules were bioequivalent by two one-side t test.