磷脂化合物促进盐酸丁卡因经皮渗透的研究

Study on the promotive effects of phospholipids upon the transdermal absorption of tetracaine hydrochloride

目的 比较磷脂酰甘油、磷脂酰丝氨酸、磷脂酰胆碱、鞘磷脂等 4种磷脂化合物对盐酸丁卡因促透作用的影响。方法 以小鼠普通皮肤 ,去角质层皮肤和经磷脂化合物预处理皮肤为渗透屏障 ,分别以 1%和 3%的磷脂化合物作为渗透促进剂 ,采用改进Franz扩散池进行离体皮肤渗透实验 ,用高效液相色谱法测定接收液中盐酸丁卡因的含量。结果 4种磷脂化合物对盐酸丁卡因的促透作用顺序为 :磷脂酰甘油 >磷脂酰丝氨酸 >磷脂酰胆碱 >空白组 >鞘磷脂 ;对于不同渗透屏障 ,盐酸丁卡因的经皮吸收顺序为 :去角质层皮肤 >经磷脂化合物预处理皮肤 >普通皮肤。结论 磷脂化合物作为一种低毒、无刺激性的渗透促进剂 ,能够提高药物的经皮渗透效果 ,具有开发应用前景。

OBJECTIVE: To study the enhancing effects of phospholipids on the percutaneous penetration of tetracaine hydrochloride in vitro. Phosphatidylcholine(PC), phosphatidylserine(PS), phosphatidylglycerol (PG) and sphingomyelin (SM) were used as phospholipids. METHODS: Common skin, the skin without stratum corneum and the skin saturated by phospholipids were used as the barriers of percutaneous penetration. 1% phospholipids and 3% phospholipids were used as the percutaneous absorption enhancers respectively. The rat skin permeation test in vitro was performed in modified Franz diffusion pool. The concentration of tetracaine hydrochloride in receptor fluid was determined by HPLC. RESULTS: The enhancing effects of the four phospholipids on the percutaneous penetration of tetracaine hydrochloride were in the following order: PG>PS>PC>Control>SM. With different barriers of percutaneous penetration, the percutaneous penetration effects of tetracaine hydrochloride were in the following order: the skin without stratum corneum>the skin saturated by phospholipids>common skin. CONCLUSION: Phospholipids are a series of percutaneous absorption enhancers with low toxicity and non-irritation, and may have wide prospect in transdermal drug delivery system.