[关键词]
[摘要]
目的 优化舒肺原位凝胶的制备工艺,研究舒肺不同剂型离体皮肤渗透过程及机制。方法 以冷溶法制备舒肺原位凝胶,以泊洛沙姆188(P188)和泊洛沙姆407(P407)为凝胶基质,以胶凝温度为指标,采用单因素实验和星点设计-效应面法确定凝胶基质P188和P407的用量范围,最终确定舒肺原位凝胶的最优处方。采用Franz透皮扩散池,研究舒肺原位凝胶的经皮渗透过程,探索舒肺原位凝胶的经皮渗透机制。结果 确定舒肺原位凝胶的处方:凝胶基质-药物为1∶3,舒肺原位凝胶的最优处方P188用量为4%,P407用量为22.5%,相转变温度在32~36℃形成凝胶。舒肺原位凝胶中芥子碱硫氰酸盐、芫花素的释放均符合Higuchi释放模型。结论 舒肺原位凝胶的制剂工艺稳定可行,产品质量可靠,有良好的应用前景,适于工业生产与临床应用。
[Key word]
[Abstract]
objective To optimize the preparation technology of sulfuric in situ gel and study the infiltration experiment of different dosage forms. Methods Shufei in situ gel was prepared by cold cut method with poloxamer 188 (P188) and poloxamer 407 (P407) as gel base. Using gelling temperature index, the dosage range of gel matrix P407 and P188 in Shufei in situ gel was determinated by the single factor and star design-response surface methods to get the best prescription of Shufei in situ gel. The transdermal diffusion process of Shufei in situ gel was carried out in Franz diffusion cells to explore the permeation mechanism. Results The optimized prescription of Shufei in situ gel was as follow:The ratio of gel matrix to drug at 1:3, P188 dosage of 4%, P407 dosage of 22.5%, and the phase transition temperature within 32-36℃ to form gel. The releases of sinapine thiocyanate and genkwanin in Shufei in situ gel were all in line with the Higuchi release model. Conclusion The preparation process of Shufei in situ gel is stable and feasible with reliable product quality and good application prospect, which is suitable for industrial production and clinical application.
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[基金项目]
河南省科技攻关计划项目(092102310112);呼吸疾病诊疗与新药研发河南省协同创新中心基金项目(20130012)