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Investigation into Alternative Sugars as Potential Carriers for Dry Powder Formulation of Budesonide

机译:研究替代糖作为布地奈德干粉配方的潜在载体

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Introduction Dry powder inhaler (DPI) formulations are so far being used for pulmonary drug delivery, mainly for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Currently most of DPI formulations rely on lactose as a carrier in the drug powder blend. However, due to reducing sugar function of lactose which makes it incompatible with some drugs such as budesonide, it is realistic to investigate for alternative sugars that would overcome the concerned drawback but still have the positive aspects of lactose. Methods The study was conducted by characterizing carriers for their physico-chemical properties and preparing drug/carrier blends with concentration of 5% and 10% drug with the carrier. The mixing uniformity (homogeneity) of Budesonide in the blends was analyzed using spectrophotometer. The blend was then filled into NB7/2 Airmax inhaler device and the deposition profiles of the drug were determined using multi stage liquid impinger (MSLI) after aerosolization at 4 kPa via the inhaler. The morphology of the carriers conducted using the scanning electron microscope. Results The results determined that the mean fine particle fraction (FPF) of 5% and 10% blends of mannitol was 61%, possibly due to fine elongated particles. Dextrose exhibited excellent flowability. Scanning electron microscope illustrated mannitol with fine elongated particles and dextrose presenting larger and coarse particles. It was found out that type of carriers, particle size distribution, and morphology would influence the FPF of budesonide. Conclusion It may be concluded that mannitol could be suitable as a carrier on the basis of its pharmaceutical performance and successful achievement of FPF whereas the more hygroscopic sugars such as sorbitol or xylitol showed poor dispersibility leading to lower FPF.
机译:简介迄今为止,干粉吸入器(DPI)制剂已用于肺部药物输送,主要用于治疗哮喘和慢性阻塞性肺疾病(COPD)。当前,大多数DPI制剂在药物粉末混合物中依赖乳糖作为载体。但是,由于降低了乳糖的糖功能,使其与某些药物(如布地奈德)不相容,因此研究替代糖可以克服相关缺点,但仍具有乳糖的积极意义,这是现实的。方法通过表征载体的理化特性并制备浓度为5%和10%的药物与载体的药物/载体混合物来进行研究。使用分光光度计分析布地奈德在混合物中的混合均匀性(均质性)。然后将共混物填充到NB7 / 2 Airmax吸入器设备中,并通过吸入器在4 kPa雾化后,使用多级液体冲击器(MSLI)确定药物的沉积曲线。使用扫描电子显微镜进行的载体的形态。结果结果确定,甘露醇的5%和10%共混物的平均细颗粒分数(FPF)为61%,这可能是由于细的细长颗粒造成的。葡萄糖表现出优异的流动性。扫描电子显微镜显示甘露醇具有细长的细颗粒和右旋糖,呈现出较大的粗颗粒。发现载体的类型,粒径分布和形态会影响布地奈德的FPF。结论根据其药理性能和成功的FPF可以得出甘露醇可以作为载体的结论,而吸湿性较高的糖(如山梨糖醇或木糖醇)的分散性差,导致FPF较低。

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