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丹参酮 IIA 固体分散体的制备及理化性质研究。

Preparation and physicochemical characterizations of tanshinone IIA solid dispersion.

机构信息

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.

出版信息

Arch Pharm Res. 2011 Jun;34(6):949-59. doi: 10.1007/s12272-011-0612-3. Epub 2011 Jul 2.

DOI:10.1007/s12272-011-0612-3
PMID:21725816
Abstract

This investigation describes a novel approach to prepare solid dispersions of tanshinone IIA using a laboratory-scale planetary ball mill. Poloxamer 188 was employed as the surfactant carrier to improve the solubility and dissolution of the poorly soluble drug, tanshinone IIA. Solubility and dissolution were evaluated compared to the corresponding physical mixtures and pure drug. Furthermore, the physicochemical properties of the solid dispersions were investigated using scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, Fourier transform infrared spectroscopy and ultraviolet spectrophotometry. The solid dispersion significantly enhanced drug solubility and dissolution compared with pure drug and the physical mixtures. Scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared spectroscopy analyses of tanshinone IIA/poloxamer 188 system confirmed that there were intermolecular interactions between tanshinone IIA and poloxamer 188 and no conversion to crystalline material. Tanshinone IIA existed in a microcrystalline form in the system. These results suggested that improvement of the dissolution rate could be correlated to the formation of a eutectic mixture between the drug and the carrier. After 60 days the solid dispersion samples were chemically and physically stable. The present studies indicated that the planetary ball mill technique could be considered as a novel and efficient method to prepare solid dispersion formulations.

摘要

本研究描述了一种使用实验室行星式球磨机制备丹参酮 IIA 固体分散体的新方法。泊洛沙姆 188 用作表面活性剂载体以提高难溶性药物丹参酮 IIA 的溶解度和溶解速率。与相应的物理混合物和纯药物相比,评估了溶解度和溶解速率。此外,使用扫描电子显微镜、粉末 X 射线衍射、差示扫描量热法、傅里叶变换红外光谱和紫外分光光度法研究了固体分散体的物理化学性质。与纯药物和物理混合物相比,固体分散体显著提高了药物的溶解度和溶解速率。丹参酮 IIA/泊洛沙姆 188 体系的扫描电子显微镜、粉末 X 射线衍射、差示扫描量热法和傅里叶变换红外光谱分析证实了丹参酮 IIA 与泊洛沙姆 188 之间存在分子间相互作用,且没有转化为晶态物质。丹参酮 IIA 以微晶形式存在于该体系中。这些结果表明,溶解速率的提高可能与药物和载体之间形成共晶混合物有关。60 天后,固体分散体样品在化学和物理上均稳定。本研究表明,行星球磨机技术可被视为制备固体分散体配方的一种新颖且有效的方法。

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