正极性聚丙烯驻极体外静电场对5-氟尿嘧啶贴剂中药物释放的影响  

Effect of External Electrostatic Field of Positive Polypropylene Electrets on Release of 5-fluorouracil from Adhesive Patch

作　　者：徐立丽[1] 黄平[1] 苑旺[1] 梁合鹃 崔黎丽[2] 江键[1] 

机构地区：[1]第二军医大学基础部数理教研室,上海200433 [2]第二军医大学药学院无机教研室,上海200433

出　　处：《高电压技术》2017年第6期1925-1929,共5页High Voltage Engineering

基　　金：国家自然科学基金(51477175)~~

摘　　要：为研究正极性聚丙烯驻极体对5-氟尿嘧啶(5-FU)压敏胶贴剂和含化学促渗剂(质量分数3%氮酮)5-FU压敏胶贴剂中药物体外释放的影响,采用常温电晕充电技术制备1 000 V和2 000 V驻极体,以压敏胶Eudragit E100为基质,柠檬酸三丁酯为增塑剂,水溶性氮酮为化学促渗剂,制备驻极体5-FU贴剂。借助于Franz扩散池和高效液相色谱仪检测贴剂的体外累积释放量。结果表明:1)正极性聚丙烯驻极体表面电位越高,外静电场越强,对5-FU压敏胶贴剂中药物释放的提高越多。2)1 000 V和2 000 V聚丙烯驻极体分别作用于含3%氮酮的5-FU贴剂36 h,贴剂的药物释放量分别较5-FU贴剂提高2.53倍和3.10倍。3)正极性聚丙烯驻极体通过改变5-FU贴剂的介电特性和降低贴剂黏滞力增加药物的释放。正极性聚丙烯驻极体与3%氮酮联用可进一步增加5-FU贴剂的药物释放量,从而给增生性瘢痕的治疗提供新剂型和新方法。To study the effects of positive polypropylene（PP） electrets on cumulative release amounts of 5-fluorouracil （5-FU） from 5-FU patch and chemical enhancer （3% azone） containing 5-FU patch, the ambient temperature corona charging technology was applied for preparation of 1 kV and 2 kV electret. For the preparation of 5-FU patch with electret, pressure-sensitive adhesive Eudragit E100 was used as matrix, tributyl citrate esters as plasticizer, and water-soluble azone as chemical permeation enhancer. The Franz diffusion pool and high performance liquid chromatograph were used to investigate the release rule of positive polarity electret electrostatic field to 5-FU in vitro. Results show that higher external electrostatic field of positive PP electrets with higher surface potential results in more drug release from 5-FU patches. The cumulative release amount of 5-FU from the 3% azone containing 5-FU patches at 36 h under the action of 1 kV and 2 kV PP electrets are 2.53 and 3.10 times as compared with that of the 5-FU patch, respectively. Positive PP electrets can increase the drug release from the patch by changing the dielectric property and viscose force of the patch. The combination of electrets and 3% azone can remarkably increase the release of 5-FU from its patches, which provides a new formulation and new strategy for treatment of hypertrophic scar.

关 键 词：驻极体 5-氟尿嘧啶 压敏胶贴剂 氮酮 静电场 透皮给药 

分 类 号：TQ460.1[化学工程—制药化工]