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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(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。
OBJECTIVE To study the formulation optimization of 5-fluorouracil (5-FU) patch and the effect of negative electret electrostatic field on in vitro release of 5-FU. Methods The -1000V negative-polarity electret and -2000V negative-polarity electret were prepared by normal-temperature corona charging. The pressure-sensitive adhesive Eudragit E100 was used as matrix and tributyl citrate as plasticizer. The water-soluble Azone was Preparation of negative electret 5-FU patch by chemical penetration enhancers. The influence of pressure-sensitive adhesive Eudragit E100, plasticizer, water-soluble azone and negative electret on the parameters of 5-FU patch was investigated by single factor. The optimum formulation of 5-FU patch was screened by orthogonal design. The modified Franz diffusion cell and HPLC were used to study the effect of negative electret electrostatic field on the release of 5-FU in vitro. Results (1) 0.25g Eudragit E100, plasticizer and Eudragit E100 mass ratio of 55:100, water-soluble azone content of 3% of the combination of 5-FU patch for the optimal prescription. (2) -1000V electret and -2000V electret both promoted the release of 5-FU in vitro, and the higher the voltage, the stronger the promotion. (3) Compared with 3% water-soluble azone alone, the negative electret combined with 3% water-soluble azone further enhanced the in vitro release of 5-FU (P <0.05). Conclusion Both the negative electret and the water-soluble Azone can reduce the holding capacity of 5-FU patch and promote the release of 5-FU in vitro.