【摘要】 将雄性Ｗｉｓｔａｒ大鼠１６只随机分为两组，分别口服自制和进口环孢素Ａ（ＣｙＡ）微乳浓缩液，采用高效液相色谱法测定血药浓度，对其药代动力学和相对生物利用度进行了研究。试验结果表明两种制剂中ＣｙＡ的药动学过程均符合口服吸收二室模型。自制和进口环孢素Ａ微乳浓缩液的全血药物浓度达峰时间分别为１．５７±０．５５和１．６８±０．４３ｈ；Ｃｍ ａｘ 分别为１７５５．６±２２６．０和１８３２．２±５９８．８ｎｇ／ｍｌ；Ｔ１／２ 分别为１９．９３±６．４４和１９．７９±６．９８ｈ；ＡＵＣ分别为３０６３７．９±７５５２．４和３０３１６．６±６５７８．９ｎｇ·ｈ／ｍ ｌ；自制环孢素Ａ微乳浓缩液的相对生物利用度为１０１．１％ 。经统计分析，两种制剂的药代动力学参数均无显著性差异（Ｐ＞ ０．０５），两种制剂具有生物等效性。更多还原

【Abstract】 Sixteen male Wistar rats were paired by body weight following on overnight fast. Micro emulsion preconcentrate solution containing CyA (CyA MEPC sol) were diluted in water at a concentretion of 1mg/ml and given by gavage to the animal pairs at a dosage of 10mg/kg. The whole blood CyA concentrations were determined by HPLC method. The bioavailability of the CyA MEPC sol was studied with Sandimmun Neoral R solution (Neoral, a commercially available CyA MEPC sol product) as control preparation. The concentration time course of the two preparations fit well to two compartment open model with first order absorption. T max of the CyA MEPC sol and Neoral were 1.57±0.55 and 1.68±0.43h; C max were 1755.6±226.0 and 1832.2±598.8ng/ml; T 1/2 were 19.93±6.44 and 19.79±6.98h; AUC were 30637.9±7552.4 and 30316.6±6578.9 ng·h/ml, respectively. The relative bioavailability of the CyA MEPC sol was 101.1%. Statistical analysis showed the two preparations were bioequivalence.更多还原