盐酸地尔硫卓缓释片的制备及释药因素考察

目的制备日服1次的盐酸地尔硫卓缓释片并对释药因素进行考察。方法分别单独采用羟丙基甲基纤维素(HPMC)、联合应用HPMC与羧甲基纤维素钠(CMC-Na)作为基本骨架材料制备盐酸地尔硫卓缓释片,并对影响释药的因素进行考察。结果HPMC规格、压片压力对药物的释放几乎无影响;HPMC用量、稀释剂用量对药物的释放产生一定的影响;CMC-Na用量对药物的释放有较大影响。结论HPMC和CMC-Na联合应用可以有效地解决水易溶性药物盐酸地尔硫卓释药快的问题,加入一定比例的微晶纤维素(MCC)能促进药物中后期释放,以制备日服1次的盐酸地尔硫卓缓释片。

Preparation of diltiazem hydrochloride sustained-release tablets and the factors influencing drug release from matrix tablets

Objective To prepare diltiazem hydrochloride sustaind-release tablets(DTZ-SRTs) for administration once a day and examine the factors affecting the drug release.Methods DTZ-SRTs were prepared by emploging HPMC,the mixture of HPMC and CMC-Na as basic matrix materials,respectively.The factors affecting drug release were investigated.Results The viscosity of HPMC and tableting pressure had few effects on drug release.The amount of HPMC and diluents influenced the release of drug to some degree.The significant effect was observed when the amount of CMC-Na was changed.Conclusions The application of HPMC together with CMC-Na can effectively solve the problem of rapid release of the water soluble drug diltiazem hydrochloride.Addition of certain ratio of MCC can promote the later release of the drug so as to prepare diltiazem hydrochloride sustaind-release tablets for administration once daily.