伊曲康唑温敏微乳凝胶的研制

Formulation of thermoreversible microemulsion-based gel containing itraconazole

目的:研究伊曲康唑温敏型水包油微乳凝胶的处方工艺。方法:通过伊曲康唑溶解性的考察、伪三元相图的绘制筛选微乳油相、乳化剂、助乳化剂和Km值,通过凝胶温度以及黏附力的测定筛选凝胶基质,采用星点设计-效应面法,确定最佳处方。并对微乳凝胶的外观,粒径,物理性质以及溶出度进行考察。结果:微乳凝胶最终处方为,苯甲醇∶中链油∶Cremophor EL-35∶Transcutol P∶P407∶P188∶纯化水=3∶1∶4.5∶1.5∶3.44∶4.56∶22。体外释放试验表明,伊曲康唑微乳凝胶可以改善药物的释放。结论:伊曲康唑微乳凝胶工艺简单,具有良好的温敏性和黏附性,并能促进药物释放。

Objective： To develop the formulation of thermoreversible mieroemulsion-based gel containing itraconazole （ITZ-MBG） using an O/W microemulsion-based gel system. Methods： Through solubility experiment and pseudo-tertiary phase diagrams, the compatible combination of oils, surfactants, cosurfactants and Km were screened. Solution-gel transition temperature and adhesive force were determined to optimize the formulation by central composite design-response surface methodology. The appearance, particle size and distribution, physical properties and dissolution rate of the optimal formulation were tested. Results ： The best formulation was as follows, benzyl alcohol： MCT： eremophor EL-35： transeutol P： poloxamer 407： poloxamer 188 was 3： 1：4.5： 1.5： 3.44： 4.56： 22. The in vitro release rate of ITZ was improved from MBG. Conclusion ： The solubility of ITZ can be improved in microemulsion system. ITZ-MBG is easy to prepare and shows good temperature-sensltive adhesion and liquidity.