伊曲康唑凝胶的制备及体外透皮性考察

Preparation of Itraconazole Gel Formulation and Its in Vitro Transdermal Performance

目的探索伊曲康唑凝胶的制备方法,并考察其体外透皮给药性能与特点。方法以卡波姆940为基质,以外观性状、涂展性、稳定性、耐热耐寒实验为综合观察指标,采用正交设计法优化处方,制备伊曲康唑凝胶。采用改良Franz扩散池,高效液相色谱(HPLC)法测定伊曲康唑含量,评价伊曲康唑凝胶体外透皮性能与特点。结果伊曲康唑凝胶最优处方为伊曲康唑含量1%,卡波姆含量1%,聚乙二醇-400(PEG-400)含量15%,甘油含量10%。制得的伊曲康唑凝胶均匀细腻、稳定性好,在常温时保持胶状。体外释放实验表明,伊曲康唑凝胶体外释放符合Higuchi方程,随着时间延长其累积释放量也逐步增加,具有缓释效果。结论伊曲康唑凝胶处方设计合理,性质稳定,具有缓释效果,可提高患者依从性。

Objective To study the preparation method of the itraconazole gel formulation,and investigate its drug performance and characteristics in topical transdermal drug delivery. Methods Itraconazole gel was prepared with carbomer940 as matrix,of which optimal formulation parameters were screened according to the appearance quality test,spreading property,stability and cold-heat resistance by orthogonal experiments. And the drug performance and characteristics of the transdermal delivery of the itraconazole gel formulation were evaluated by a modified Franz diffusion cell technique and HPLC.Results The best formulation parameters were as follows,1% itraconazole,1% carbomer,15% PEG-400 and 10% glycerin. As the in vitro transdermal experiments shown,the time-release curve of itraconazole gel fit well with Higuchi formulation,which indicated that it has a sustained release effect. Conclusion The characteristics of the optimal itraconazole gel is stable with sustained release effect,which may improve the patient compliance.