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目的探讨水溶性药物纳洛酮微乳的制备以及作为载体促进药物的透皮吸收。方法以肉豆蔻酸异丙酯(IPM)-水-卵磷脂-正丙醇作为微乳的组成部分,制备纳洛酮-卵磷脂油包水型微乳。采用效应面优化法,对微乳处方进行星点设计,筛选出最佳处方。采用Franz扩散池,SD雄性大鼠离体皮肤作为透皮模型,HPLC测定药物含量。结果最佳处方条件为卵磷脂:29%,正丙醇:25%,IPM:35%。按此最优条件制备的纳洛酮微乳稳态渗透速率为4.33μg·h-1·cm-2,大大高于水溶液稳态渗透速率(0.20μg·h-1·cm-2)。结论微乳对纳洛酮的经皮渗透具有促进作用。
Objective To investigate the preparation of water-soluble drug naloxone microemulsion and to promote transdermal absorption of the drug as a carrier. Methods Naloxone-lecithin water-in-oil microemulsion was prepared with isopropyl myristate (IPM) -water-lecithin-n-propanol as a component of microemulsion. The effect surface optimization method was used to design the star point of the microemulsion prescription, and the best prescription was screened out. Franz diffusion cells were used in vitro. SD male rats were used as transdermal skin samples and the drug content was determined by HPLC. Results The best prescription conditions were lecithin: 29%, n-propanol: 25%, IPM: 35%. The steady state permeation rate of naloxone microemulsion was 4.33μg · h-1 · cm-2, which was much higher than that of aqueous solution (0.20μg · h-1 · cm-2). Conclusion Microemulsion can promote the transdermal penetration of naloxone.