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| 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 |
| 徐立丽1,苑旺1,梁媛媛1,郭鑫1,黄平1,崔黎丽2*,江键1* |
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(1. 第二军医大学基础部数理学教研室, 上海 200433;
2. 第二军医大学药学院无机化学教研室, 上海 200433
*通信作者) |
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| 摘要: |
| 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。 |
| 关键词: 驻极体 5-氟尿嘧啶 压敏胶贴剂 水溶性氮酮 静电场 |
| DOI：10.16781/j.0258-879x.2017.03.0294 |
| 投稿时间：2016-09-15修订日期：2016-12-14 |
| 基金项目:国家自然科学基金（51477175），第二军医大学校级军事课题（2013JSD2）. |
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| Effect of electrostatic field of negative polarity electret on in vitro release behavior of 5-fluorouracil patch |
| XU Li-li1,YUAN Wang1,LIANG Yuan-yuan1,GUO Xin1,HUANG Ping1,CUI Li-li2*,JIANG Jian1* |
(1. Department of Physics and Mathematics, College of Basic Medical Sciences, Second Military Medial University, Shanghai 200433, China;
2. Department of Inorganic Chemistry, School of Pharmacy, Second Military Medial University, Shanghai 200433, China
*Corresponding authors) |
| Abstract: |
| 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. |
| Key words: electret 5-fluorouracil pressure-sensitive adhesive patch water-soluble azone electrostatic field |
