依诺沙星在前列腺中相对生物利用度

Relative bioavailability of enoxacin in prostate

本文报道了豚鼠口服５０ｍｇ／ｋｇ依诺沙星后，血和前列腺组织中药物动力学及相对生物利用度的结果。采用微生物法测定生物样品的药物浓度，用３Ｐ８７实用药代动力学程序处理药物浓度，并自动算出各项动力学参数和Ｃ－Ｔ曲线图，主要参数ｔ＿（１／２ｋｅ），ｔ＿ｐ，Ｃ＿（ｍａｘ），ＡＵＣ，Ｃｌ和Ｖｄ在血液中分别为３．０２ｈ，１．４５５ｈ，３．３３μｇ／ｍｌ，１９．８８９μｇ·ｈ／ｍｌ，２．５１４Ｌ／ｋｇ·ｈ，１０．９５１Ｌ／ｋｇ和前列腺组织中分别为１．８６８ｈ，２．４９ｈ，５．７０１μｇ／ｍｌ，３３．１４μｇ·ｈ／ｍｌ，１．５０９Ｌ／ｋｇ·ｈ和４．０６６Ｌ／ｋｇ，前列腺组织药物浓度曲线下面积相对血液中生物利用度为１６６．６％，结果表明药物在前列腺组织中达峰时间为２．４９ｈ，峰浓度高，清除较慢，前列腺组织中浓度明显高于血液浓度。

The relative bioavilability and pharmacokinetics of enosacin in blood and prostate of guinea-pig after single oral adminis-tration was relported. The concentrations in biological samples were detected by microbiological assay. The concentration- timedata were fitted by a practical pharmacokinetic program(3p87).The pharmacokinetic parameters were as follows : The t_(1/2)Ke,t_(peak), Cmax, AUC, Cl and Vd in blood were 3.02h,1.455h,3.33μg/ml, 19.889μg.h/ml,2.514L/kg/h,10.95IL/kg; The t_(1/2)Ke,t_(peak), Cmax, AUC, Cl and Vd in prostate were 1.868h,2.49h,5.70lμg/ml,33.14μg·h/ml,1.509L/kg· h and 4.066L/kg , relative bioavailability in prostate was 166.6%. The result of elimination kinetics in prostate showedt_(peal) was 2.49h, Cmax was higher and ke was lower. The concentration in prostate was more than that in blood.