涂布法制备三明治式的曲安奈德口腔膜剂及其体外释放行为的研究

Preparation of Sandwich Triamcinolone Acetonide Oral Film by Tape Casting Process and Its Release Behavior in Vitro

目的制备一种由背衬层、缓释层和黏附层组成的载曲安奈德的“三明治”式口腔膜剂用于治疗口腔溃疡。方法以乙基纤维素、羟丙基甲基纤维素和聚丙烯酸为载体,采用涂布法制备曲安奈德口腔膜剂。以膜剂外观、厚度、均匀度和黏附性、机械强度等为指标,通过单因素法优化背衬层、缓释层和黏附层处方。以市售制剂Taisho®为对照,对该膜剂的理化性质和体外药物释放进行评估。结果制得曲安奈德三层口腔膜剂载药量为96.0%,该膜剂具有较好的均一性、机械强度和黏附性,与市售制剂Taisho®的释放行为对比,两者的相似因子f2为54.25。结论采用涂布法制备的曲安奈德口腔膜剂与Taisho®有较好的质量一致性。该膜剂的制备工艺简单可行,具有一定的产业化优势。

OBJECTIVE To prepare a“sandwich”oral film(composed ofthe backing layer,sustained release layer,and adhesion layer)containing triamcinolone acetonide for the treatment of oral ulcers.METHODS Triamcinolone acetonide oral film was prepared by a tape casting process using ethyl cellulose(EC),hydroxypropyl methylcellulose(HPMC),and polyacrylic acid(PAA)as carrier materials.Taking the appearance,thickness,uniformity,adhesion,and mechanical strength of the film as indicators,the formulation of the backing layer,sustained release layer,and adhesion layer was optimized by a single factor study.The film's physicochemical properties and drug release in vitro were compared with the commercially available formulation Taisho®.RESULTS The drug loading of the resulting triamcinolone acetonide three-layer oral film was 96.0%,and the film had good uniformity,mechanical strength,and adhesion.The designed oral film had a release curve similarity factor f2 of 54.25 when compared to the commercially available formulation of Taisho®.CONCLUSION The quality of triamcinolone acetonide oral film prepared by the tape casting process is consistent with that of Taisho®.Moreover,the technology of this film is simple and feasible,with the potential for industrial conversion.