摘要
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 micelles consisting of lecithin and isopropyl myristate （IPM） were prepared and the critical reverse micelle concentration （CRMC） values determined by both spectrometric iodine method and water solubilization method were （2.37±0.15）% and （1.78±0.34）%. The solubilities of fat-soluble salicylic acid in IPM or reverse micellar system containing 0.04 or 0.15 g/ml lecithin were 35.86, 47.66 and 65.17 mg/ml, respectively. The transdermal performance of reverse micellar system loaded with fat-soluble salicylic acid or water-soluble sodium salicylate was investigated with excised mouse skin as a barrier. The results showed that with the increasing of salicylic acid content （2, 4 and 8 mg/ml） in reverse micellar system, the cumulative permeation amount and penetration rate of salicylic acid were both increased in a dose-dependent manner. In reverse micellar systems containing different concentrations of lecithin （5%—30%）, the penetration coefficients of sodium salicylate were all significantly higher than that of sodium salicylate saturated solution. The penetration coefficients of sodium salicylate exhibited first increase then decrease with an increasing of lecithin, and the maximum value was observed when the concentration of lecithin was 15% in IPM. Compared with the penetration coefficient of saturated solution group （5.58×10^（-5） cm/h）, the maximum value reached 5.99×10^（-3） cm/h. It indicated that reverse micellar system had a good role in promoting the transdermal transport for fat-soluble salicylic acid and water-soluble sodium salicylate.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2016年第10期1275-1279,共5页
Chinese Journal of Pharmaceuticals
基金
"十二五"国家科技重大专项重大新药创制(2014ZX09507001007)
河北省自然科学基金资助项目(H2015206458)
河北省卫生和计划生育委员会重点科技研究计划(20130455)
关键词
卵磷脂
反胶束
临界反胶束浓度
透皮
水溶性药物
脂溶性药物
水杨酸
水杨酸钠
lecithin
reverse micelle
critical reverse micelle concentration （CRMC）
transdermal
water-soluble drug
fat-soluble drug
salicylic acid
sodium salicylate
