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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 :酯类前体药物可在皮肤细胞中被代谢为活性母体药物本身
OBJECTIVE: To study the metabolism of ketoprofen isopropyl in skin cells and to provide experimental basis for further study on the use of ester prodrugs to improve the percutaneous absorption characteristics of drugs. Methods: The third generation keratinocytes of human foreskin or fibroblasts were sonicated and homogenized. Different concentrations of ketoprofen isopropyl ester were added to incubate at 37 ℃. High performance liquid chromatography (HPLC) The concentrations of ketoprofen isopropyl and ketoprofen in the cell homogenates were determined. Results: Ketoprofen is metabolized in the homogenate of epidermal keratinocytes and dermal fibroblasts, and the metabolic capacity of the former is greater than the latter. Conclusion: Ester prodrugs can be metabolized in the skin cells as the active parent drug itself