【摘要】 目的制备一种高载药量、高渗透率的吲哚美辛纳米乳透皮制剂。方法利用冰片和薄荷醇低共熔物可增溶的特点,结合假三元相图和正交设计法,优化处方制备吲哚美辛纳米乳透皮制剂。通过考察离体大鼠皮肤的渗透特性,对比含低共熔物纳米乳、普通纳米乳剂和混悬液,评价透皮能力。结果处方为Lauroglycol FCC-薄荷/冰片(1∶1)-Cremophor ELP/Tran-scutol P(3∶2)(10∶50∶25);载药量为3.2%;低共熔物纳米乳、普通纳米乳和混悬液稳态渗透速率分别为40.46、14.85、2.0μg.cm-2.h-1,低共熔物纳米乳的累积渗透量明显高于其他两种剂型,且随时间增加,两者的差值变大。结论含有低共熔物的纳米乳剂能明显促进吲哚美辛的渗透与吸收。更多还原

【Abstract】 OBJECTIVE To prepare the eutectic-nanoemulsion formulation containing indomethacin with high drug loading and permeability.METHODS The nanoemulsion was prepared with the system of eutectic containing borneol and menthol.The false ternary phase diagram and orthogonal design was used to optimize the preparation.The permeability characteristics of indomethacin were compared among eutectic-nanoemulsion,nanoemulsion and suspension in vitro using diffusion cell with the skin of SD male rats.The concentration of indomethacin was measured by HPLC.RESULTS The optimal formulation contained Lauroglycol FCC(12%),menthol-borneol(1:1)(59%) and Cremophor ELP-Transcutol P(3:2)(29%).The drug loading was 3.2%.The steady permeation rate of eutectic-nanoemulsion was 40.46 μg·cm-2·h-1,which is much higher than that of other two containing nanoemulsion(14.85 μg·cm-2·h-1)and suspension(2.0 μg·cm-2·h-1).CONCLUSION The eutectic-nanoemulsion can enhance the permeation of indomethacin across the skin of SD male rats.更多还原