吡罗昔康凝胶的兔透皮吸收及药物动力学

Study on the percutaneous absorption andpharmacokinetics of piroxicam gel in rahhits

作者采用高效液相色谱法研究了吡罗昔康（Ｐｉｒ）凝胶剂２０、３０ｍｇ／ｋｇ在１０只家兔的透皮吸收过程及药物动力学。药－时曲线符合一房室模型特征，两组的吸收和消除参数无明显差异（Ｐ＞０．０５），平均值（ｎ＝１０）Ｋａ为０．４３５ｈ￣（－１），Ｋｅ为０．１０９ｈ￣（－１），Ｔ＿（１／２）Ｋａ为２．０５ｈ，Ｔ＿（１／２）Ｋｅ为６．７４ｈ，Ｔ＿（ｍａｘ）为５．５７ｈ。Ｃ＿（ｍａｘ）和ＡＵＣ随给药剂量增加呈比例增高。两组的Ｃ＿（ｍａｘ）分别为５．４２和８．９５μｇ／ｍｌ，ＡＵＣ为８３．７５和１３４．４０（μｇ·ｈ）／ｍｌ，表明该Ｈｒ凝胶剂透皮性能较好。

he percutaneous absorption and pharmacokinetics of piroxicam (Piri gel in 10 rabbits were studied usingHPLC. The concentrationtime curve was fit to onecompartment model after skin administration of Pir gel at dosesof 20 and 30 mg/kg,respectively. No significant difference (P>0. 05 ) was found in the absorbing and elimina-tingparameters between the two groups. Mean of Ka was 0. 435/h ,Ke 0. 109/h ,Ti.x.2. 05 h ,T.sx.6. 74 h,and Tmax5. 57h. C,ax and AUC increased in Proportion to increasing dose. Means of Cmax for each group were 5. 42 and 8. 95 μg/ml ,AUC 83. 75 and 134. 40 Pg . h/ml,respectively. Pir gtl could be absorbted through rabbit skin with good char-acterictics of percutaneous.