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基于固体分散技术的阿托伐他汀钙聚合物辅助制剂的制备、表征及评价。

Preparation, characterization, and evaluation of polymer-assisting formulation of atorvastatin calcium based on solid dispersion technique.

作者信息

Dong Wenxiang, Su Xitong, Xu Meng, Hu Mingming, Sun Yinghua, Zhang Peng

机构信息

Shenyang Pharmaceutical University, Shenyang 110016, China.

出版信息

Asian J Pharm Sci. 2018 Nov;13(6):546-554. doi: 10.1016/j.ajps.2018.08.010. Epub 2018 Oct 12.

Abstract

Due to low solubility and bioavailability, atorvastatin calcium is confronted with challenge in conceiving appropriate formulation. Solid dispersion of atorvastatin calcium was prepared through the solvent evaporation method, with Poloxamer 188 as hydrophilic carriers. This formulation was then characterized by scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction and fourier transform infrared spectroscopy. Moreover, all these studies suggested the conversion of crystalline atorvastatin calcium. In addition, the drug solubility studies as well as dissolution rates compared with bulk drug and market tablets Lipitor were also examined. Furthermore, the study investigated the pharmacokinetics after oral administration of Lipitor and solid dispersion. And the   and increased after taking ATC-P188 solid dispersion orally compared with that of Lipitor. All these could be demonstrated that ATC-P188 solid dispersions would be prospective means for enhancing higher oral bioavailability of ATC.

摘要

由于阿托伐他汀钙的低溶解度和生物利用度,在设计合适的制剂方面面临挑战。采用溶剂蒸发法,以泊洛沙姆188作为亲水性载体,制备了阿托伐他汀钙固体分散体。然后通过扫描电子显微镜、差示扫描量热法、粉末X射线衍射和傅里叶变换红外光谱对该制剂进行表征。此外,所有这些研究均表明结晶态阿托伐他汀钙发生了转变。另外,还考察了药物溶解度研究以及与原料药和市售片剂立普妥相比的溶出速率。此外,该研究还调查了口服立普妥和固体分散体后的药代动力学。与立普妥相比,口服ATC-P188固体分散体后 和 增加。所有这些都表明,ATC-P188固体分散体有望成为提高阿托伐他汀钙口服生物利用度的手段。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bba9/7081932/8e4df831c7eb/fx1.jpg

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