液固技术在提高瑞舒伐他汀溶解度和溶出度方面的应用。
Application of liquisolid technology for enhancing solubility and dissolution of rosuvastatin.
作者信息
Kamble Pavan Ram, Shaikh Karimunnisa Sameer, Chaudhari Pravin Digambar
机构信息
Department of Pharmaceutics, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, India-411044.
出版信息
Adv Pharm Bull. 2014;4(2):197-204. doi: 10.5681/apb.2014.029. Epub 2013 Dec 24.
PURPOSE
Rosuvastatin is a poorly water soluble drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Hence it is necessary to increase the solubility of the Rosuvastatin.
METHODS
Several liquisolid tablets formulations containing various drug concentrations in liquid medication (ranging from 15% to 25% w/w) were prepared. The ratio of Avicel PH 102 (carrier) to Aerosil 200 (coating powder material) was kept 10, 20, 30. The prepared liquisolid systems were evaluated for their flow properties and possible drug-excipient interactions by Infrared spectra (IR) analysis, differential scanning calorimetry (DSC) and X- ray powder diffraction (XRPD).
RESULTS
The liquisolid system showed acceptable flow properties. The IR and DSC studies demonstrated that there is no significant interaction between the drug and excipients. The XRPD analysis confirmed formation of a solid solution inside the compact matrix. The tabletting properties of the liquisolid compacts were within the acceptable limits. Liquisolid compacts demonstrated significantly higher drug release rates than those of conventional and marketed tablet due to increasing wetting properties and surface area of the drug.
CONCLUSION
This study shows that liquisolid technique is a promising alternative for improvement of the dissolution rate of water insoluble drug.
目的
瑞舒伐他汀是一种水溶性较差的药物，其口服吸收速率通常受胃肠道中溶解速率的控制。因此，有必要提高瑞舒伐他汀的溶解度。
方法
制备了几种液固分散体片剂制剂，其中液体药物中的药物浓度各不相同（范围为15%至25% w/w）。微晶纤维素PH 102（载体）与气相二氧化硅200（包衣粉末材料）的比例保持为10、20、30。通过红外光谱（IR）分析、差示扫描量热法（DSC）和X射线粉末衍射（XRPD）对制备的液固分散体系统的流动性和可能的药物-辅料相互作用进行评估。
结果
液固分散体系统表现出可接受的流动性。IR和DSC研究表明药物与辅料之间没有显著相互作用。XRPD分析证实了在致密基质内部形成了固溶体。液固分散体压片的压片性能在可接受范围内。由于药物的润湿性和表面积增加，液固分散体压片的药物释放速率明显高于传统片剂和市售片剂。
结论
本研究表明液固分散体技术是提高水不溶性药物溶解速率的一种有前景的替代方法。
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