The purpose of this work was to develop optimized press-coated tablets of salbutamol sulfate using polyethylene glycol 6000 (PEG 6000)-Eudragit S100 dispersion blends in the outer shell. To facilitate the direct application of the Eudragit S100 and PEG 6000 onto the inner core, solid Eudragit S100 powder was mixed with PEG 6000 by fusion method. The optimized, pulverized dispersions of polymer blends were evaluated by various methods of characterization, including differential scanning calorimetry, X-ray diffraction and spectroscopy. The press-coated tablets containing salbutamol sulfate in the inner core were prepared by compression-coating with (PEG 6000)-Eudragit S100 dispersion blends as the outer layer in different ratios. The amount of outer layer on the delayed drug release was investigated. The press-coated tablets release were evaluated in 0.1 M HCl for the first 2 h and then in pH 6.8 phosphate buffer for 7 h. The mechanism of delayed drug release is based on erosion of the out layer blends. The results showed the 0.15 g of PEG 6000/ Eudragit S100 (2:1) in the outer shell achieving delayed release of drug in vitro as well as in the plasma of beagle dogs.

目的:采用山榆酸甘油酯作为基本骨架材料,制备了日服一次的盐酸氨溴索缓释片.方法:通过单因素实验考察药物释放的影响因素,确立处方组成;采用中心复合设计试验对处方进行优化.结果:山榆酸甘油酯和乳糖的量为药物释放的主要影响因素,以综合评分值为考察指标拟合所得多元二次方程为Y=105.9390-1.1116X1-0.2686X2+0.0081X12-0.0049X1X2+0.0021X22,复相关系数r=0.8387.结论:中心复合设计优化处方预测性良好,制得盐酸氨溴索缓释片符合实验设计要求.

OBJECTIVE To optimize the preparation of fluorouracil-loaded gelatin microspheres (5-FuMS) for chemo-embolization therapy of hepatocellular carcinoma using central composite design. METHODS 5-FuMS was prepared by an emulsion-chemical-crosslinking method. The effects of gelation concentration X1 , amount of emulsifier X2 and stirring speed X3 on a number of response variables were system-ically investigated. The response variables were drug loading, loading efficiency and geometric mean diameter,respectively. A desirability function that combines these three response variables was constructed. A second-order polynomial equation was fitted to the data, and the resulting equation was used to predict the responses in the optimal region. RESULTS All the investigated response variables were found to be highly dependent on the formulation variables. CONCLUSION The central composite design was successfully used to optimize the preparation of 5-FuMS.

OBJECTIVE To prepare bilayer tablet, which consists of a metoclopramide rapid release layer and a naproxen sodium sustained release layer. METHODS Orthogonal experiment design and central composite design were adopted to optimize the formulation of metoclopramide rapid release layer and naproxen sodium sustained release layer, respectively. The behaviors of compound naproxen sodium sustained release tablets were evaluated by release test in vitro. RESULTS The cumulative release of the bilayer tablet was up to criteria, when the amount of CMS-Na was 30% in metoclopramide rapid release layer, Eudragit~ RLPO and HPMC K4M were 20% and 15% in naproxen sodium sustained release layer. CONCLUSION Orthogonal experiment design and central composite design were successful in optimizing the preparation of tablets with accurate and reliable results.