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本文报道18例健康志愿者口服依诺沙星后的药代动力学参数和制剂的生物利用度。用高效液相色谱仪测定服药后15小时内的血浆药浓,结果表明:该药吸收迅速、分布相短暂,体内过程符合线性动力学。口服原粉(553mg)后主要药代动力学参数为:t_(max)=1.10±0.49h;C_(max)=4.37±0.82mg/L;K_α=2.89±1.10h~(-1);tlag=0.18±0.08h;AUC_(-noit)=31.71±6.84h·mg/L;其中13例为二室模型:K_(12)=0.51±0.36h~(-1);K_(21)=0.46±0.12h_(-1);t_(1/2)α=0.72±0.27h;t_(1/2)β=6.77±1.12h;另5例为一室模型:t_(1/2)Ke=4.98±0.55h。随机交叉口服片剂(600mg)和胶囊剂(1200mg),未发现血药浓度消除呈现剂量依赖性。供试3种片剂和1种胶囊剂与原粉比较,均具有较高的相对生物利用度,其范围为98.3％～101. 6％。
This article reports pharmacokinetic parameters and bioavailability of enoxacin in 18 healthy volunteers. The plasma drug concentration within 15 hours after taking the drug was measured by HPLC. The results showed that the drug absorbed rapidly and the distribution was short, and the in vivo process was in accordance with the linear kinetics. The main pharmacokinetic parameters of oral powder (553 mg) were as follows: t max = 1.10 ± 0.49 h; C max = 4.37 ± 0.82 mg / L; Kα = 2.89 ± 1.10 h -1; tlag = 0.18 ± 0.08h; AUC_ (- noit) = 31.71 ± 6.84h · mg / L, of which 13 were two-compartment model: K 12 = 0.51 ± 0.36h -1; K 21 = (1/2) α = 0.72 ± 0.27h; t 1/2 (1/2) β = 6.77 ± 1.12h; and the other 5 cases were single chamber model: t 1/2 (1/2) 4.98 ± 0.55h. Randomized crossover oral tablets (600 mg) and capsules (1200 mg) did not show a dose-dependent decrease in plasma concentrations. 6%. The three test tablets and one capsule compared with the original powder, have a relatively high bioavailability, the range of 98.3% ~ 101.6%.