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为全面了解萘哌地尔（Ｎａｆ）在大鼠体内的代谢过程，用反相ＨＰＬＣＵＶ法，给大鼠ｉｇ１０，２０，３０ｍｇ·ｋｇ－１Ｎａｆ后，测定在不同时间各组织和体液中Ｎａｆ的含量。结果表明，Ｎａｆ在大鼠体内药代动力学为二室模型，Ｔ１／２α为０４７～１０１ｈ，Ｔ１／２β为４７８～７０８ｈ，达峰时间Ｔ（ｐｅａｋ）为０４２～０９０ｈ，Ｃｍａｘ，ＡＵＣ随剂量升高而增大。给药后１５ｍｉｎ，肠壁组织浓度最高，其次为肝、肺；２ｈ以后，除睾丸、卵巢和子宫外，其余组织药物浓度逐渐降低。尿、粪及胆汁中原形药总排出量不足给药量的１％，提示Ｎａｆ在大鼠体内有首过效应及代谢物生成。在１００～５００ｍｇ·ｍｌ－１浓度范围内，Ｎａｆ血浆蛋白结合率为８２％～９７％。
In order to fully understand the metabolic process of naftopidil (Naf) in rats, using reversed-phase HPLC-UV method, rats were given ig10, 20 and 30 mg · kg-1 of Naf. The levels of Naf Content. The results showed that pharmacokinetics of Naf in rats was a two-compartment model with T1 / 2α of 047 ~ 101h, T1 / 2β of 478 ~ 708h and peak time of 0 (peak) 42 ~ 090h, Cmax, AUC increased with dose. 15min after administration, the highest concentration of intestinal tissue, followed by the liver and lung; 2h later, in addition to testicular, ovarian and uterine, the other tissue drug concentrations gradually decreased. Urine, feces and bile in the prototype drug less than 1% of the total discharge, suggesting that Naf in rats with first-pass effect and metabolite formation. In the concentration range of 100 ~ 500mg · ml-1, Naf plasma protein binding rate of 82% to 97%.