新型疏水化羟丙甲基纤维素硬脂氧醚乳剂型凝胶的处方设计与优化

发布时间：2018-12-17 15:42

【摘要】：目的研究利用新型疏水化纤维素醚-羟丙甲基纤维素硬脂氧醚(hydroxypropylmethylcellulose stearoxy ether,Sangelose湟,SGL)制备乳剂型凝胶的处方及优化。方法以Sangelose 90 L、Span60、十八醇、液体石蜡用量作为影响因素,以乳剂型凝胶的手感、粒度大小、离心分层比作为响应指标,采用正交设计法进行处方优化;并以难溶性药物醋酸曲安奈德(triamcinolone acetonide acetate,TAA)及水溶性药物盐酸利多卡因(lidocaine hydrochloride,LH)作为模型药,采用改良的Franz扩散池进行体外释放试验,考察此乳剂型凝胶的释药特征,并通过模型拟合阐明其释药机制。结果优选处方为(w):0.6%Sangelose 90 L、0.5%Span 60、0.5%十八醇和8%液体石蜡。优选处方中TAA与LH在24 h的累积释放量分别为25.1%、71.8%。模型拟合结果显示,TAA的释放模型符合一级动力学,释药机制以骨架溶蚀为主;LH释放符合Higuchi方程,释药机制为药物扩散和骨架溶蚀协同作用。结论在Sangelose乳剂型凝胶中难溶性药物释放机制以骨架溶蚀作用为主,水溶性药物释放机制为扩散和骨架溶蚀的协同作用。
[Abstract]:Objective to study the preparation and optimization of emulsion gel by (hydroxypropylmethylcellulose stearoxy ether,Sangelose Huang, SGL), a new hydrophobic cellulose ether-hydroxypropyl methyl cellulose stearin ether. Methods using Sangelose 90L Span60ol, octadecanol, the amount of liquid paraffin as the influencing factors, the handle, particle size and centrifugal stratification ratio of emulsion gel as the response index, orthogonal design method was used to optimize the formulation. Using triamcinolone acetonide acetate (triamcinolone acetonide acetate,TAA) and water-soluble lidocaine hydrochloride (lidocaine hydrochloride,LH) as model drugs, the release characteristics of the emulsion gel were investigated by using an improved Franz diffusion cell in vitro. The mechanism of drug release was explained by model fitting. Results the optimal prescription was (w): 0.6%Sangelose 90 L, 0.5% Span 600.5% octadecanol and 8% liquid paraffin. The cumulative release of TAA and LH at 24 h were 25.1and 71.8, respectively. The results of model fitting showed that the release model of TAA was in accordance with first-order kinetics, the drug release mechanism was skeleton dissolution, the release of LH was consistent with Higuchi equation, and the drug release mechanism was the synergistic effect of drug diffusion and cytoskeleton dissolution. Conclusion the release mechanism of insoluble drugs in Sangelose emulsion gels is mainly the dissolution of skeleton, and the mechanism of release of water-soluble drugs is the synergism of diffusion and dissolution.
【作者单位】：沈阳药科大学中药学院;沈阳药科大学药学院;
【分类号】：R943

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