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与 Gelucire 50/13 形成固体分散体提高卡维地洛的溶解度和理化特性。

Solubility enhancement and physicochemical characterization of carvedilol solid dispersion with Gelucire 50/13.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, St. Peter's Institute of Pharmaceutical Sciences, Vidyanagar, Warangal, AP, India.

出版信息

Arch Pharm Res. 2011 Jan;34(1):51-7. doi: 10.1007/s12272-011-0106-3. Epub 2011 Apr 6.

Abstract

The objective of the study was enhancement of dissolution of poorly soluble carvedilol by solid dispersions (SDs) with Gelucire 50/13 using solvent evaporation method. The solubility of carvedilol showed linear increase with increasing concentrations of Gelucire indicating A(L) type solubility diagrams. SDs characterized for physicochemical characteristics using differential scanning calorimetry and X-ray diffractometry revealed transformation of crystalline form of drug to amorphous form which was confirmed by scanning electron micrographs. Further fourier transform infrared spectroscopy results suggested there is no drug carrier interaction. From the dissolution parameters such as mean dissolution time, dissolution efficiency and drug release rate, improved dissolution characteristics for SDs were observed compared with physical mixture and pure drug. Thus SDs of carvedilol in Gelucire 50/13 showed enhanced solubility and dissolution rate compared to pure drug.

摘要

本研究的目的是通过溶剂蒸发法,利用 Gelucire 50/13 制备固体分散体(SD)来提高难溶性卡维地洛的溶解性能。卡维地洛的溶解度随 Gelucire 浓度的增加呈线性增加,表明属于 A(L)型溶解度图。使用差示扫描量热法和 X 射线衍射法对 SDs 的物理化学特性进行了表征,结果表明药物的晶型发生了向无定形的转变,这一点通过扫描电子显微镜得到了证实。进一步的傅里叶变换红外光谱结果表明药物载体之间没有相互作用。从平均溶出时间、溶出效率和药物释放率等溶出参数来看,与物理混合物和纯药物相比,SDs 的溶解特性得到了改善。因此,与纯药物相比,Gelucire 50/13 中的卡维地洛 SD 具有更高的溶解度和溶解速率。

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