醋酸曲安奈德温敏凝胶的制备与体外释放度

Preparation of Triamcinolone Acetonide Acetate Thermosensitive Hydrogel and Its In Vitro Release

目的制备关节腔注射用醋酸曲安奈德(TAA)温敏凝胶,并考察其体外释放度。方法以聚乳酸-羟基乙酸共聚物(PLGA)-聚乙二醇(PEG)-PLGA为凝胶基质,以黄原胶为助悬剂、氯化钠(Na Cl)为絮凝剂,制备TAA混悬温敏凝胶,通过其含量测定方法的建立和体外释放度考察,对制剂进行初步评价。结果最佳处方:凝胶基质PLGA-PEGPLGA含量25%,助悬剂黄原胶含量0.05%,絮凝剂Na Cl含量0.9%,主药TAA含量4 mg·m L-1,胶凝温度为35.3℃,平均回收率(98.98±0.31)%。采用无膜释放方法,16 d内体外累积释药达83.31%,药物释放遵循Ritger-Peppas数学模型。结论 TAA温敏凝胶具有温敏特性和明显的缓释作用,有望成为新的关节腔给药传递系统。

Objective To prepare triamcinolone acetonide acetate（TAA）thermosensitive hydrogel for intra-articular injection,and to investigate its release in vitro. Methods TAA suspending thermosensitive hydrogel was prepared by using poly lactic-co-glycolic acid（PLGA）-polyethylene glycol（PEG）-PLGA as gel matrices,xanthan gum as suspending agent and NaCl as flocculant. It was evaluated preliminarily by determining its contents and its in vitro release. Results The best compositions for preparation of TAA suspending thermosensitive hydrogel were 25% PLGA-PEG-PLGA,0.05% xanthan gum, 0.9% NaCl and 4 mg·mL^-1 TAA.The gelation temperature was 35.3 ℃ .The average recovery was（98.98±0.31）%. By the method of membraneless dissolution,the accumulative drug release was up to 83. 31% at 16 days. The drug release followed Ritger-Peppas methematical model. Conclusion The TAA thermosensitive hydrogel with obviously sustained release is expected to become a new drug delivery system for intra-articular injection.