含替硝唑和醋酸地塞米松口腔溃疡双层膜的质量控制

Quality control of bilayer adhesive patch containing tinidazole and dexamethasone acetate for aphthous ulcer

目的对本院自制的含替硝唑和醋酸地塞米松口腔溃疡双层膜进行质量控制。方法建立HPLC法测定药物含量，并对膜剂的体内外黏附时间、溶出等指标进行测定和评价。结果替硝唑在2～180mg·L^-1、醋酸地塞米松在0．25-22．5mg·L^-1时线性关系良好，平均提取回收率分别为101．59％（n=5，RSD=0．89％）和99．18％（n=5，RSD=1．35％）。膜剂在溶菌酶生理盐水中的平均溶解时间为25min；体内外平均黏附时间分别为29．87和27．25min；在37℃人工唾液中药物呈一级释放，替硝唑和醋酸地塞米松最大溶出度为80％和70％；在口腔黏膜处药物呈一级释放，30min时释药率100％。结论本实验建立的膜剂药物HPLC测定方法及其他相应指标的测定方法简便合理，可很好控制该双层膜的质量。

AIM To control the quality of a bilayer adhesive patch containing tinidazole and dexamethasone acetate for aphthous ulcer. METUODS A drug content assay method by HPLC was established to determine and evaluate other markers such as adhesive time, dissolution, etc. of the preparation. RESULTS Tinidazole showed good linear correlation over a concentration range of 2 - 180 mg· L^- 1, while dexamethasone acetate showed good linear correlation over 0.25- 22.5 mg· L^-1. The mean extraction recoveries of these two ingredients were 101.59% （n = 5, RSD = 0.89% ）and 99.18%（ n = 5, RSD = 1.35% ）, respectively. The mean dissolution time of the patch in lysozyme saline solution was 25 min, and the in vitro mean adhesive times were 29.87 min and 27.25 min, respectively. The preparation showed a first-order release in artificial saliva at 37℃. The maximum degree of dissolution of tinidazole was 80%, while that of dexamethasone acetate was 70%. Moreover, the preparation showed a first-order release at oral mucosa, and the percent drug release was 100% at 30 min. CONCLUSION The assay methods for adhesive preparations by HPLC and detennination of other markers are simple and appropriate, and hence can be used to control the quality of the bilayer adhesive patch promisingly.