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以肉豆蔻酸异丙酯(IPM)为溶剂,卵磷脂为表面活性剂,制备反胶束体系,并利用碘光谱法和水增溶量法测定了反胶束体系的临界反胶束浓度(CRMC)。两种方法测得的CRMC值为(2.37±0.15)%和(1.78±0.34)%。测得脂溶性药物水杨酸在IPM和含0.04和0.15 g/ml卵磷脂的反胶束体系中的溶解度分别为35.86、47.66和65.17 mg/ml。以离体小鼠皮肤为屏障,考察了载水杨酸以及水溶性药物水杨酸钠的反胶束体系的透皮性能。结果显示,随反胶束体系中水杨酸含量(2、4和8 mg/ml)的增加,药物累积渗透量和渗透速度均呈现出剂量依赖性增加。在含不同浓度(5%~30%)卵磷脂的反胶束体系组中,水杨酸钠的渗透系数均显著高于饱和溶液组;水杨酸钠的渗透系数随反胶束体系中卵磷脂浓度的增加出现先增后减的情况,其中卵磷脂浓度为15%时渗透系数最高,为5.99×10~(-3) cm/h,饱和溶液组仅5.58×10~(-5) cm/h。结果提示,反胶束体系对脂溶性的水杨酸和水溶性的水杨酸钠均有良好的促进透皮转运作用。
The reverse micellar system of reverse micellar system was determined by iodine spectroscopy and water solubilization method using isopropyl myristate (IPM) as solvent and lecithin as surfactant. CRMC). The CRMC values measured by both methods were (2.37 ± 0.15)% and (1.78 ± 0.34)%. The solubility of the lipophilic drug salicylic acid in IPM and the reverse micellar system containing 0.04 and 0.15 g / ml lecithin was 35.86, 47.66 and 65.17 mg / ml, respectively. In vitro mouse skin as a barrier, investigated salicylic acid and water-soluble sodium salicylate reverse micellar system transdermal properties. The results showed that with the increase of the content of salicylic acid (2, 4 and 8 mg / ml) in the reverse micellar system, the drug cumulative infiltration rate and infiltration rate showed a dose-dependent increase. In the reverse micellar system containing different concentrations of lecithin (5% ~ 30%), the osmotic coefficients of sodium salicylate were significantly higher than those of the saturated solution; the osmotic coefficient of sodium salicylate was When the lecithin concentration was 15%, the highest permeability coefficient was 5.99 × 10 ~ (-3) cm / h, while the saturated solution group was only 5.58 × 10 ~ (-5) cm / h. The results suggest that the reverse micelles system has good transdermal transport to fat-soluble salicylic acid and water-soluble sodium salicylate.