甲磺酸培氟沙星正常人药代动力学研究

PHARMACOKINETICS OF PEFLOXACIN IN NORMAL VOLUNTEERS

甲磺酸培氟沙星(pefloxacin)简称甲氟沙星,是一个新的喹诺酮类抗菌药物。八名男性正常志愿者分别单次口服400mg片剂和水溶液进行交叉试验,同时用微生物法和高效液相色谱法(HPLC)测定给药后48小时内各时间血浆和96小时内各次尿标本药物浓制,以研究其药代动力学特性。两次试验间隔10天。药代动力学用3P87程序处理。

Single-dose pharmacokinetics of pefloxacin was studied in 8 normal male volunteers given crossly 400mg pefloxacin in tablet and in solution.Plasma and urine levels of pefloxacin were measured by both bioassay andhigh performance liquid chromatography. Pefloxacin in both formulationswas rapidly absorbed from the gastrointestinal tract wiht a short lag time,but its absorption in solution was faster than in tablet. The maximumplasma concentrations (Cmax ) after administration of tablets were 5.78(±0.39) mg/l at 1.37 (±0.24) h and 6.03 (±0.80) mg/l at 1.40 (±0.20)h from bioassay and HPLC, respectively. The Cmax after administrationof Solution was similar to that of tablet, but the peak time was signific-antly shorter than that of tablet. Pefloxacin tablet was completely abso-rbed after oral administration. The level-time curves of the both formula-tions fitted a two-compartment model. Pefloxacin elimination after admin-istration of tablet was slow. The t1/2β were 16.09 (±1 .27) and 14.73(±1. 61 ) from bioassay and HPLC, respectively. Similar results were obtained after administration of solution. Attention to pefloxacin cumulationin the body should be paid when patients repeatedly take it for a longperiod. The recoveries of unchanged pefloxacin in the both formulationswere 23.48 (±7.02) and 18.53 (±3.20) % of the dose, respectively, andrenal clearance of it were low (1. 10± 0. 48 and 0. 98± 0. 32 1/h, respectively),indicating that non-renal clearance represents the major route of elimination of this quinolone.