【作者】 姚琳；

【导师】 逄秀娟；

【作者基本信息】 沈阳药科大学 ， 药剂学， 2004， 硕士

【摘要】 环维黄杨星D系从黄杨科植物小叶黄杨(Buxus microphlla Sieb．Et Zucc．Var．Sinica Rehd．Et Wils．)及其同属植物中提取精制所得，具有降低心肌耗氧量，增强心肌收缩力，改善心脏泵功能，对心肌具有一定保护的药理作用。在治疗冠心病、心绞痛的药物中，环维黄杨星D组成的单味药制剂黄杨宁以其中药标本兼治，副作用小特点受到关注。由于目前国内主要是环维黄杨星D的速释制剂，每天服用3～4次，血药浓度波动较大，为此本文以减少给药次数，降低血药浓度波动，提高患者用药顺从性为目的，制备了环维黄杨星D缓释微丸。 建立了分光光度法对环维黄杨星D缓释微丸进行含量测定，经方法学考察适用于本品的体外质量控制。在处方前研究中测定了环维黄杨星D在不同介质中的溶解度，不同pH值下油／水分配系数。 使用万能粉体处理装置，以可压性淀粉为稀释剂，PVP乙醇溶液为粘合剂，制备了环维黄杨星D缓释微丸，测定了微丸的粉体学性质，粒径20～30目的微丸收率约为90％，外观圆整，有较强的机械强度。 用流化床悬浮包衣法对微丸进行缓释包衣。分别采用乙基纤维素(EC)和Surelease水分散体进行缓释包衣。乙基纤维素包衣的最佳工艺条件为：投料量为10g，包衣温度为30～35℃，喷雾压力为中压，喷液速度为1.0ml／min。最佳处方为：3g EC(N100)、1.5g滑石粉、0.9g DEP、1.05g PVP-K30加95％的乙醇至100ml。 Surelease水分散体缓释包衣的最佳工艺条件为：投料量为10g，包衣温度为38～40℃，喷雾压力为中压，喷液速度为1.0ml／min。最佳处方为：Surelease水分散体加水稀释至15％。结果表明：两种包衣材料均具有明显更多还原

【Abstract】 Nowdays CVB-D is taken 3～4 times daily and shows bigger fluctuation in the drug concention.The aim of this work was designed to develop a kind of CVB-D sustained-release pellets,which would reduce the dosing frequency,narrow the blood concention fluctuation and be more convenient for patients to use.Spectrophotometry method was developed to determine the CVB-D content in sustained-release pellets.In the preformulation researches,the physicochemical propertied of CVB-D were investigated,which benefit phaemaceutical design.CVB-D pellets were prepared in the MECHANOMILL NEW ,using compressible starch as the dilute afent and PVP solution as the adhesive agent.The powder propertied of the pellets were determined and the yield of objective pellets (20～30 mesh) was about 90%.A fluid-bed spray processor was adopted for coating the pellets.The sustained -release pellets were coated with EC and Surelease respectively. The influence factors on the release of CVB-D sustained-release pellets coated by EC or Surelease respectively were investigated.The formulation and technology of two kind of CVB-D sustained-release pellets were optimized.For EC,they were 30～35℃ coating temperature,middle pressure of atomization air and 1.0ml/min spray rate.The更多还原