酮洛芬异丙酯在皮肤细胞中的代谢

Metabolism of ketoprofen isopropyl ester in skin cells

目的 :研究酮洛芬异丙酯在皮肤细胞中的代谢作用 ,为进一步研究利用酯类前体药物方法改善药物的经皮吸收特性提供实验依据。方法 :将人包皮的第 3代角质形成细胞或成纤维细胞超声破碎制成匀浆 ,加入不同量的酮洛芬异丙酯进行37℃温孵实验 ,通过高效液相色谱法分别在不同时间测定细胞匀浆中酮洛芬异丙酯及酮洛芬的浓度。结果 :酮洛芬异丙酯在表皮角质形成细胞和真皮成纤维细胞的匀浆中存在代谢现象 ,且前者的代谢能力明显大于后者。结论

OBJECTIVE To study the metabolism of ketoprofen isopropyl ester in skin cells. METHODS Human keratinocytes and dermal fibroblasts were fractured in PBS by ultrasound, the homogenates with different concentrations of ketoprofen isopropyl ester were incubated at 37℃, the concentration of samples was measured by HPLC.RESULTS Ketoprofen isopropyl ester was hydrolyzed in human keratinocytes or dermal fibroblasts homogenate, the metabolism capability of Human keratinocytes was bigger than that of dermal fibroblasts. CONCLUSIONS Skin cells can hydrolyze ester prodrug.