%0 Journal Article %T 负极性驻极体静电场对5-氟尿嘧啶贴剂体外释放规律的影响 %A 徐立丽 %A 苑旺 %A 梁媛媛 %A 郭鑫 %A 黄平 %A 崔黎丽 %A 江键 %J 第二军医大学学报 %D 2017 %R 10.16781/j.0258-879x.2017.03.0294 %X 目的 研究5-氟尿嘧啶（5-fluorouracil，5-FU）贴剂的处方优化工艺及负极性驻极体静电场对5-FU体外释放规律的影响。方法 采用常温电晕充电技术制备－1 000 V负极性驻极体和－2 000 V负极性驻极体，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负极性驻极体5-FU贴剂。单因素考察压敏胶Eudragit E100、增塑剂、水溶性氮酮和负极性驻极体对5-FU贴剂相关参数的影响，通过正交设计试验筛选5-FU贴剂的最优处方。利用改良的Franz扩散池和高效液相色谱仪研究负极性驻极体静电场对5-FU体外释放规律的影响。结果 （1）0.25 g Eudragit E100、增塑剂和Eudragit E100的质量比为55：100、水溶性氮酮的质量分数为3%组合时为5-FU贴剂的最优处方。（2）－1 000 V驻极体和－2 000 V 驻极体均促进了5-FU的体外释放，且电压越高促进作用越强。（3）与单用3%水溶性氮酮相比，负极性驻极体联合质量分数为3%的水溶性氮酮进一步提高了5-FU的体外释放量（P<0.05）。结论 负极性驻极体与水溶性氮酮均能降低5-FU贴剂的持黏力，促进5-FU的体外释放，两者联合使用时促进作用更为显著。</br>Objective To explore the effects of prescription optimization of 5-fluorouracil (5-FU) patch and electrostatic field of the negative polarity electret on the in vitro release behavior of 5-FU from the 5-FU patch. Methods The corona charging technology at ambient temperature was applied for preparation of －1 000 V and －2 000 V negative polarity electrets. The negative polarity electret 5-FU patch was prepared by using Eudragit E100 as pressure-sensitive adhesive (PSA), tributyl citrate as plasticizer, and water-soluble azone as chemical permeation enhancer. We used the single factor method to investigate the influences of PSA, plasticizer, water-soluble azone and negative polarity electret on the relevant parameters of the 5-FU patch. The optimal prescription was screened by orthogonal design test. We also studied the influence of negative polarity electret on the in vitro release behavior of 5-FU from the 5-FU patch by using modified Franz diffusion cell and high-performance liquid chromatography. Results (1) The optimal prescription was fitting when the mass of Eudragit E100 was 0.25 g, the mass ratio of plasticizer to Eudragit E100 was 55:100 and the mass fraction of water-soluble azone was 3%. (2) Both the －1 000 V and －2 000 V negative polarity electrets used in this study promoted the in vitro release of 5-FU from the 5-FU patch; and the promoting effect was proportional to the surface potential of the electret. (3) Compared with the single use of 3% water-soluble azone, negative polarity electret combined with 3% water-soluble azone significantly increased the in vitro release of 5-FU from the 5-FU patch (P<0.05). Conclusion Negative polarity electret and water-soluble azone can reduce the holding capacity of the 5-FU patch and promote the in vitro release of 5-FU from the 5-FU patch, and the promoting effect is more significant in the combination of them %K 驻极体 5-氟尿嘧啶 压敏胶贴剂 水溶性氮酮 静电场< %K /br> %K electret 5-fluorouracil pressure-sensitive adhesive patch water-soluble azone electrostatic field %U http://www.ajsmmu.cn/ajsmmu/ch/reader/view_abstract.aspx?file_no=20160327&flag=1