萘普生缓释片处方工艺因素对体外溶出的影响(英文)

Prescription of naproxen sustained release tablets influences their dissolution in vitro

背景:药物以缓释片剂形式存在,可减少用药次数,延长释药时间,有利于其治疗效应的发挥。目的:制备萘普生缓释片,考察其处方工艺因素对体外溶出的影响。设计、时间及地点:以重复测量设计在2005-09于顺德职业技术学院实验室完成实验。材料:萘普生、Ⅱ号丙烯酸树脂、羟丙基甲基纤维素(Hydroxypropyl Methyl Cellulose,HPMC)和硬脂酸由广州市新港化工有限公司提供,乙醇为分析纯。方法:经单因素考察,采用正交试验设计,筛选萘普生缓释片处方(萘普生250g,HPMC(K4M)12.5g,乙醇适量,硬脂酸镁1.2g)。以不同材料(硬脂酸、HPMC、20%丙烯酸树脂Ⅱ、聚维酮K30),不同黏度规格的HPMC(K4M,K15M,K100M),不同硬度的HPMC(2,4,6kg),在相同粒度和相同压力下压片。主要观察指标:不同材料、不同黏度规格的HPMC、不同硬度对释放度的影响。测定并比较萘普生缓释片的释药速度及释放效果。结果:①材料为HPMC的缓释片较符合缓释片标准。用黏度规格为K4M所制缓释片8h释放度符合缓释片标准。硬度为2,4,6kg,压力越大,释放越慢。②所制备的萘普生缓释片在12h内呈现良好的零级释放特征。结论:该处方制出的萘普生缓释片具有理想的缓释效果。

BACKGROUND： The pattern of sustained release tablets can reduce medication frequency and prolong release time, which are both beneficial for a better therapeutic effect. OBJECTIVE： To prepare naproxen sustained release tablets and investigate the influence of their prescription on the dissolution in vitro. DESIGN, TIME AND SETTING： A repeated measurement was carried out in the laboratory of Shunde Polytechnic in September 2005. MATERIALS： Naproxen, acrylic resin II, hydroxypropyl methyl cellulose （HPMC） and octadecanoic acid were all offered by Guangzhou Xingang Chemical Industry Co., Ltd. Alcohol was analytical pure. METHODS： With the orthogonal design, the prescription of naproxen sustained release tablets was screened out by simple factor analysis, consisting of 250 g naproxen, 12.5 g HPMC （K4M）, alcohol, and 1.2 g magnesium stearate. Drug tabletting was performed with different materials （octadecanoic acid, HPMC, 20% acrylic resin II and polyvidone K30）, different viscosities of HPMC （K4M, K15M and K100M）, and different rigidities of HPMC （2, 4 and 6 kg） at the same granularity and same pressure. MAIN OUTCOME MEASURES： The influences of different materials, different viscosities of HPMC and different rigidities of HPMC on the release were observed. The release rate and release effect of naproxen sustained release tablets were determined. RESULTS： In accordance with the standard of sustained release tablets, the release for 8 hours of the materials prepared with HPMC at K4M viscosity were satisfied. At the rigidity of 2, 4 and 6 kg, the higher pressure indicated the slower release. The naproxen sustained release tablets showed a good zero order release within 12 hours after the preparation. CONCLUSION： The prepared naproxen sustained release tablets have achieved the satisfactory release outcome.