新型经皮渗透促进剂的合成及其促渗特性的研究  

SYNTHESIS OF NEW PENETRATION ENHANCER AND IN VITRO TEST FOR THE TRANSDERMAL ABSORPTION OF DRUGS

作　　者：成志毅[1] 陈浩凡 鲁向阳 刘宁[1] 蔡丽玲[1] 

机构地区：[1]中山医科大学化学教研室,广东广州510089 [2]广东深圳市公安边防中心医院

出　　处：《药学学报》2000年第5期381-384,共4页Acta Pharmaceutica Sinica

摘　　要：目的　开发新型经皮渗透促进剂并研究其促渗特性。方法　合成了N 月桂基 α 羟基丙酰胺 (DHPA)和N 甲基焦谷氨酸月桂酯 (MDPG)。在改良的Franz扩散池上 ,用离体无毛小鼠皮作生物膜 ,分别用亲水和亲脂性药物进行经皮渗透促进活性试验。结果　 12h的累积透过量显示对双氯芬酸钠、咖啡因在其饱和水溶液中的透皮扩散 ,与无促透剂对照组相比较 ,DHPA的增大率 (enhancementratios ,ER)分别为 9 9和 8 7,MDPG的ER分别为 7 9和 5 3,月桂氮　酮的ER分别为 8 7和 4 6。对维生素E在其乙醇—水 (80∶2 0 )饱和溶液中的透皮扩散 ,DHPA ,MDPG和月桂氮　酮相应的ER分别为 3 6 ,2 3和 2 2。结论　这两个化合物对药物的透皮吸收有很好的促进作用 ,其促透活性超过或接近月桂氮　酮在相同条件下的促透效果。AIM To research for new skin penetration enhancers. METHODS N Dodecyl α hydroxyl propanamide (DHPA) and N methyl dodecyl pyroglutamate (MDPG) were synthesized. The penetration enhancing ability of the compounds were evaluated in vitro using excised hairless mouse skins as bio membrane in modified Franz type diffusion cells. RESULTS Data ( n =6, P <0.05) showed that the enhancement ratio (ER) of DHPA and MDPG for the permeability of diclofenac sodium, caffeine in saturated aqueous solution was 9 9, 8 7 and 7 9, 5 3 respectively compared with the control group (no enhancer present); and that of laurocapram was 8 7 and 4 6. ER of the three enhancers for vitamin E in saturated ethanol — H 2O (80∶20) solution was 3 6, 2 3 and 2 2 respectively.CONCLUSION DHPA and MDPG can enhance the transdermal effect of diclofenac sodium, and the effect surpasses or approaches that of laurocapram at the same condition.

关 键 词：经皮给药系统 渗透促进剂 TDS DHPA MDPG 

分 类 号：R944.9[医药卫生—药剂学] R452[医药卫生—药学]