Zakeri-Milani Parvin, Hallaj Nezhadi Somayeh, Barzegar-Jalali Mohammad, Mohammadi Leila, Nokhodchi Ali, Valizadeh Hadi
Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran ; Liver and Gastrointestinal Diseases Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Adv Pharm Bull. 2011;1(1):48-53. doi: 10.5681/apb.2011.007. Epub 2011 Jul 20.
Prednisolone is a class II substance according to the Biopharmaceutics Classification System. It is a poorly water soluble agent. The aim of the present study was to improve dissolution rate of a poorly water-soluble drug, prednisolone, by a solid dispersion technique.
Solid dispersion of prednisolone was prepared with PEG 6000 or different carbohydrates such as lactose and dextrin with various ratios of the drug to carrier i.e., 1:10, 1:20 and 1:40. Solid dispersions were prepared by coevaporation method. The evaluation of the properties of the dispersions was performed using dissolution studies, Fourier-transform infrared spectroscopy and x-ray powder diffractometery.
The results indicated that lactose is suitable carriers to enhance the in vitro dissolution rate of prednisolone. The data from the x-ray diffraction showed that the drug was still detectable in its solid state in all solid dispersions except solid dispersions prepared by dextrin as carrier. The results from infrared spectroscopy showed no well-defined drug-carrier interactions for coevaporates.
Solid dispersion of a poorly water-soluble drug, prednisolone may alleviate the problems of delayed and inconsistent rate of dissolution of the drug.
根据生物药剂学分类系统，泼尼松龙属于II类物质。它是一种水溶性较差的药物。本研究的目的是通过固体分散技术提高水溶性差的药物泼尼松龙的溶出速率。
用聚乙二醇6000或不同的碳水化合物如乳糖和糊精以药物与载体1:10、1:20和1:40的不同比例制备泼尼松龙的固体分散体。通过共蒸发法制备固体分散体。使用溶出度研究、傅里叶变换红外光谱和X射线粉末衍射对分散体的性质进行评估。
结果表明乳糖是提高泼尼松龙体外溶出速率的合适载体。X射线衍射数据表明，除了以糊精为载体制备的固体分散体外，在所有固体分散体中仍能检测到药物的固态形式。红外光谱结果表明共蒸发物没有明确的药物-载体相互作用。
水溶性差的药物泼尼松龙的固体分散体可能缓解药物溶出延迟和速率不一致的问题。
