Hu Liandong, Song Weihua, Niu Feng, Jiao Kuiliang, Jia Zheng
College of Pharmaceutical Sciences, Hebei University, Baoding, China.
Pak J Pharm Sci. 2013 May;26(3):629-36.
Solid dispersion technique has been developed many years for improving solubility of water-insoluble drugs, aiming to achieve a better oral bioavailability. However, this technique exhibits many inconveniences when used for large-scale tableting procedures. The objective of current research work was to develop cilnidipine solid dispersions (SDs) to improve the dissolution behaviors of this water-insoluble drug. Moreover, an innovative granulation method was designed to simplify the traditional tableting technology used in solid dispersion technique. Three different kinds of polymers, polyethylene glycol (PEG), polyvinylpyrrolidone (PVP) and poloxamer, were used as carriers to prepare solid dispersions. The interactions in the solid state were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and FT-IR spectroscopy. The designed granulation method was employed to prepare solid dispersion tablets and the formulation was optimized through investigating the dissolution behaviors. The results indicated PEG solid dispersion showed the best effect both on physical characterizations and dissolution studies. Furthermore, all type of solid dispersions significantly improved the dissolution rates when compared to pure drug and its corresponding physical mixture (PM). The solid dispersion tablets prepared in simplified tableting method exhibited better operability, stability and dissolution behavior than the tablets prepared in traditional ways, which brought more opportunities to solid dispersion technique for industrial production.
多年来一直在开发固体分散技术以提高水不溶性药物的溶解度，旨在实现更好的口服生物利用度。然而，该技术在用于大规模压片过程时存在许多不便之处。当前研究工作的目的是开发西尼地平固体分散体（SDs）以改善这种水不溶性药物的溶出行为。此外，设计了一种创新的制粒方法以简化固体分散技术中使用的传统压片工艺。使用三种不同的聚合物，聚乙二醇（PEG）、聚乙烯吡咯烷酮（PVP）和泊洛沙姆作为载体来制备固体分散体。通过差示扫描量热法（DSC）、粉末X射线衍射（PXRD）和傅里叶变换红外光谱（FT-IR）对固态中的相互作用进行了表征。采用设计的制粒方法制备固体分散体片剂，并通过研究溶出行为对配方进行优化。结果表明，PEG固体分散体在物理表征和溶出研究方面均显示出最佳效果。此外，与纯药物及其相应的物理混合物（PM）相比，所有类型的固体分散体均显著提高了溶出速率。采用简化压片方法制备的固体分散体片剂比传统方法制备的片剂表现出更好的可操作性、稳定性和溶出行为，这为固体分散技术的工业化生产带来了更多机会。
