川陈皮素微乳离子敏感型凝胶剂的研制及体外释放考察

Research on the Preparation and in-vitro Release of Nobiletin Microemulsion Ion-Sensitive Gel

目的:制备川陈皮素微乳离子敏感型凝胶剂,并考察其理化性质及体外释药行为。方法:通过溶解度考察和绘制伪三元相图,进行微乳处方筛选与优化;通过粘度测定筛选凝胶基质的用量;对微乳凝胶的微观形态、粒径、p H值、含量及体外释放进行评价。结果:微乳凝胶的最优处方为:0.9%川陈皮素、0.8%中碳链三甘酯、31.5%聚氧乙烯-35-蓖麻油、10.5%聚乙二醇-400、0.3%去乙酰结冷胶,其微乳及微乳凝胶粒径均小于50 nm,p H值6.64±0.20,药物含量为8.665 mg/m L,微乳凝胶剂12 h的积累释药率为84%,且符合Higuchi方程。结论:所制备的川陈皮素微乳凝胶剂可提高其药物溶解度并具有一定的缓释特性,可作为鼻腔给药载体。

Objective： To prepare nobiletin microemulsion ion-sensitive gel,and to study its physicochemical properties and drug release behavior in vitro. Methods： The microemulsion formulation was screened and optimized by solubility test,and the pseudo-ternary phase diagrams were drawn up. The quantity of gel matrix was selected through viscosity measurement; and the micro-morphology,particle size,p H,drug content and in-vitro release were evaluated. Results： The best formulation of microemulsion-based gel was 0. 9% nobiletin,0. 8% MCT,31. 5% cremophor EL-35,10. 5% PEG-400,0. 3% deacetylated gellan gum,the particle size of microemulsion and microemulsion-based gel were below 50 nm,the p H value was 6. 64 ± 0. 20,the content of drug was 8. 665 mg / m L,the cumulative release rate in 12 h of microemulsion-based gel was 84%,and conform to the Higuchi equation. Conclusion： Nobiletin microemulsionbased gel could improve the solubility of nobiletin and show a sustained release behavior,which can be used as carrier for nasal delivery system.