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以甲氨蝶呤与磷脂的复合率为评价指标,采用单因素试验和正交设计优化复合物制备工艺。结果表明,优化的制备工艺为复合温度40℃,甲氨蝶呤浓度为30 mg/ml,药物:磷脂摩尔比1:2。以离体乳猪皮肤作渗透屏障,采用改良直立式Franz扩散池法进行体外透皮研究。结果表明,甲氨蝶呤磷脂复合物24 h累积渗透量低于游离药物,在表皮及真皮层的滞留量则分别是游离药物组的2.1和2.3倍。提示甲氩蝶呤磷脂复合物可增加药物皮肤滞留量,并减小经皮透过量。
The composite rate of methotrexate and phospholipid was taken as the evaluation index, the single factor experiment and the orthogonal design were used to optimize the preparation process of the complex. The results showed that the optimum preparation conditions were as follows: the compound temperature was 40 ℃, the concentration of methotrexate was 30 mg / ml and the molar ratio of drug to phospholipid was 1: 2. In vitro pig skin permeability barrier, improved vertical Franz diffusion cell method in vitro transdermal study. The results showed that the cumulative permeation amount of methotrexate phospholipid complex in 24 h was lower than that of free drug and the retention in the epidermis and dermis was 2.1 and 2.3 times that of the free drug group respectively. Suggest that methotrexate phospholipid complexes can increase drug retention in the skin and reduce transdermal penetration.