正常人一次口服国产环丙沙星药代动力学研究

PHARMACOKINETIC OF CIPROFLOXACIN AFTER A SINGLE ORAL DOSE IN NORMAL VOLUNTEERS

8名男性健康志愿者交叉口服环丙沙星片剂和胶囊各600mg,进行药代动力学研究,血浆标本采用HPLC荧光检测法测定。口服二种剂型的药时曲线均符合二室开放模型。片剂和胶囊的峰浓度(C_(max))分别为6.99±1.39mg/l和7.05±1.31mg/l,达峰时间(t_(max))分别为1.15±0.31h和1.09±0.45h。片剂和胶囊的Vd值分别为96.14±14.98l和106.89±23.17l,总消除速率常数β分别为0.1656±0.007h^(-1)和0.1661±0.013h^(-1),消除半衰期(t_(1/2)β)分别为4.19±0.18 h和4.19±0.36 h,与国外文献报告的一致,血浆总的消除率(Cl)分别为15.86±1.98 l/h和17.31±5.01 l/h,AUC分别36.57±7.83mg/l·h和38.35±4.52mg/l·h。胶囊对片剂的相对生物利用度为104.9±15.8%。片剂和胶囊两组之间的上述参数均无显著性差别。

Pharmacokinetics of ciprofloxacin was studied in 8 normal volunteers after a single oraldose of 600 mg in tablet or in capsule. Plasma levels of ciprofloxacin were assayed by high performance liquidchromatography. Ciprofloxacin in both preparations were rapidly absorbed from the gastrointestinal tract witha short lag time,The Cmax in tablet and capsule were 7.05(±1.31)mg/l and 6.99(±1.39)mg/l respective-ly. The lag time and peak time of casuple were slight shorter than that of tablet. The concentration-timecurves of the both preparations were fitted to open two-compartment model. The apparent volume of distribu-tion of ciprofloxacin in tablet and in capsule were 96.14(±14.98)l and 106.89(±23.17)l and t1/2β were 4.19(±0.18)h and 4/.19(±0.36)h respectively. The results were corresponding with the previous reports. Thetotal serum clearance of ciprofloxacin in healthy volunteers were 15.86(±1.98) l/h and 17.31 (±5.01 ) l/hand AUC values were 36.57(±7.83)mg/l·h and 38.35 (±4.52)mg/l·h respectively. There was no signifi-cant difference in all these parameters between preparations of tablet and capsule.