布地奈德缓释干粉吸入剂的制备及乳糖用量的影响

Preparation of budesonide sustained-release dry powder for inhalation and influence of lactose content

采用高压匀质联合喷雾干燥法制备载有布地奈德的壳聚糖微粒并考察其体外释放行为,用涡旋混合器使之与乳糖混合,以药物回收率和含量均匀度为指标考察混合速度与混合时间的影响,以药物回收率、含量均匀度、粉末流动性和体外沉积分布为指标考察乳糖用量的影响。制得微粒具有一定的体外缓释效果,可吸入组分百分比为46.0%,但流动性较差,加入10倍乳糖进行混合后,药物回收率高达96.5%,药物含量的相对标准偏差为2.5%,流动性较好,可吸入组分百分比提高至59.6%。结果表明,采用涡旋混合器可制备回收率及含量均匀度均较高的布地奈德缓释干粉吸入剂,处方具有较好的流动性,适于肺部吸入。

Using high pressure homogenization method combined with spray-drying, budesonide-loaded chitosan microparticles were prepared and the in vitro release profile was investigated. The microparticles were then blended with lactose using a vortex mixer, influence of mixing speed, mixing time on drug recovery rate and content homogeneity were investigated. Meanwhile, influence of lactose content on drug recovery rate, content homogeneity, powder flowability and in vitro deposition were studied. It turned out that budesonide was released from the microparicles in a sustained manner, with fine particle fraction as high as 46.0%, but the powder flowability was poor. After blending with 10 times of lactose, the drug recovery rate was 96.5%, with relative standard deviation of drug content 2.5%, and fine particle fraction of the formulation increased to 59.6% with good flowability. It＇s demonstrated that using a vortex mixer, budesonide sustained-release dry powder for inhalation with good recovery and content homogeneity could be prepared, the formulation had good flowability and was suitable for pulmonary inhaling.