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

发布时间：2018-08-06 21:12

【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 000V负极性驻极体和-2 000V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)0.25g 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 000V驻极体和-2 000V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(P0.05)。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。
[Abstract]:Objective to study the optimum formulation of 5-fluorouraciline (5-FU) patch and the effect of negative electret electrostatic field on the release of 5-FU in vitro. Methods the negative electrets of 10000V and 2.000V were prepared by normal temperature corona charging technique. The negative electret 5-FU patches were prepared by using pressure sensitive adhesive Eudragit E100 as matrix, tributyl citrate as plasticizer and water-soluble azone as chemical permeation enhancer. The effects of pressure sensitive adhesive Eudragit E100, plasticizer, water-soluble azone and negative electret on the parameters of 5-FU patch were investigated by single factor. The optimum formulation of 5-FU patch was selected by orthogonal design. The effect of negative electret electrostatic field on the release of 5-FU in vitro was studied by improved Franz diffusion cell and high performance liquid chromatography (HPLC). Results (1) 0.25g Eudragit E100, the mass ratio of plasticizer to Eudragit E100 was 55: 100, the optimum formulation of 5-FU patch was obtained when the mass fraction of water-soluble azone was 3%. (2) both 1 000V electret and 2 000V electret promoted the release of 5-FU in vitro. The higher the voltage, the stronger the effect. (3) compared with the single use of 3% water-soluble azone, the negative electret combined with 3% mass fraction of water-soluble azone further increased the amount of 5-FU released in vitro (P0.05). Conclusion both negative electret and water-soluble azone can decrease the adhesion of 5-FU patch and promote the release of 5-FU in vitro.
【作者单位】：第二军医大学基础部数理学教研室;第二军医大学药学院无机化学教研室;
【基金】：国家自然科学基金(51477175) 第二军医大学校级军事课题(2013JSD2)~~
【分类号】：R943

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