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探讨和比较了吡罗昔康以口服和透皮两种途径给药后的血药浓度与局部浓度。将小鼠随机分组，分别给予口服混悬剂０．０７２ｍｇ·ｍｌ－１或透皮凝胶剂１ｍｇ·ｇ－１（或２ｍｇ·ｇ－１）。以ＨＰＬＣ法测定小鼠的血药浓度（Ｃｓ）和局部浓度（Ｃ１）。结果表明，透皮给药以血药浓度计算凝胶剂的相对生物利用度仅为口服混悬剂的１０％。但是透皮给药的Ｃ１／Ｃｓ＝０．１３，远远大于口服给药的Ｃ１／Ｃｓ（０．０１）。透皮给药后，局部药物浓度—时间曲线下面积为１５．８５μｇ·ｈ－１·ｍｌ－１，远远高于口服给药相应值（１．９３μｇ·ｈ－１·ｍｌ－１）。揭示单纯以血药浓度作为局部作用透皮制剂的生物利用度评价标准是不全面的，应同时考察作用部位的药物浓度。
The plasma concentrations and local concentrations of piroxicam after oral administration and transdermal administration were investigated and compared. The mice were randomized to receive oral injections of 0.072 mg ml-1 or 1 mg g-1 (or 2 mg g-1) of transdermal gel, respectively. The plasma concentration (Cs) and the local concentration (C1) of mice were determined by HPLC. The results showed that the relative bioavailability of the gels calculated by transdermal administration at plasma concentrations was only 10% of the oral suspension. However, transdermal administration of C1 / Cs = 0.13, far greater than the oral administration of C1 / Cs (0.01). After transdermal administration, the area under the local drug concentration-time curve was 15.85μg · h-1 · ml-1, much higher than that of oral administration (1.93μg · h-1 · ml-1). It is not comprehensive to reveal the bioavailability evaluation criteria of the transdermal drug with the local blood concentration alone. Therefore, the drug concentration of the active site should be examined at the same time.