复方苯佐卡因膜剂的制备及处方优化.pdfVIP

复方苯佐卡因膜剂的制备及处方优化 ＊ 陶明涛 ，李人宇（连云港师范高等专科学校化学化工系，江苏连云港 222000） 中图分类号 R943 文献标志码 A 文章编号 1001-0408（2015）19-2720-03 DOI 10.6039/j.issn. 1001-0408.2015.19.40 摘 要 目的：制备复方苯佐卡因膜剂并优化其处方。方法：以聚乙烯醇1788（PVA ）、羧甲基纤维素钠（CMC-Na ）为基质，制备复 方苯佐卡因膜剂。以基质PVA 、CMC-Na 和附加剂甘油、聚山梨酯80的用量为因素，以主药苯佐卡因（BZ ）和醋酸地塞米松（DA ） 累积释放度（0.25、2h ）的平均值为指标，采用正交试验优选处方，并对最优处方进行验证。采用高效液相色谱法测定制剂中BZ 和 DA 的含量，计算累积释放度。结果：最优处方为PVA 1.2g ，CMC-Na 1.2g ，甘油 1.6g ，聚山梨酯801.5ml 。所制单片药膜中BZ 、 DA 的含量分别为21.607mg （RSD ＝0.71％，n ＝6）、4.375mg （RSD ＝0.55％，n ＝6），0.25、2h 的平均累积释放度分别为32.7％ （RSD ＝2.01％）、69.25％（RSD ＝1.43％）。结论：该膜剂制备方法简单、含量均匀。 关键词 复方苯佐卡因；膜剂；制备；处方优化 Preparation and Formulation Optimization of Compound Benzocaine Film TAO Ming-tao ，LI Ren-yu （Dept. of Chemistry and Chemical Engineering ，Lianyungang Normal College ，Jiang- su Lianyungang 222000，China ） ABSTRACT OBJECTIVE ：To prepare Compound benzocaine film and optimize the formulation. METHODS ：Compound benzo- caine film was prepared with the base materials of polyving akohol-1788 （PVA ）and sodium carboxymethyl cellulose （CMC-Na ）. With the factors of amounts of the base materials PVA and CMC-Na and the additives glycerol and polysorbate 80，and the indexes of the average of the cumulative release rates （0.25 h and 2 h ）of the main drugs benzocaine （BZ ）and dexamethasone acetate （DA ），the orthogonal experiment was conducted to optimize the formulation ，and then the optimal formulation was verified. HPLC was adopted to determine the contents of BZ and DA in the preparation for the calculation of cumulative release rates. RESULTS ： The optimal formulation was as follows as PVA of 1.2g ，CMC-Na of 1.2g ，glycerol of 1.6 g ，polysorbate 80 of 1.5ml. The con- tents of BZ and DA in the single film prepared respectively were 21.607mg （RSD ＝0.71％，n ＝6）and 4.375mg （RSD ＝0.55％， n ＝6）；the average cumulative release rates were respectively 32.7％ （RSD ＝2.01％）and 69