Aggarwal Amit Kumar, Singh Samarpreet
Rayat Institute of Pharmacy, Railmajra, Distt. Ropar, Punjab, India.
PDA J Pharm Sci Technol. 2012 May-Jun;66(3):201-13. doi: 10.5731/pdajpst.2012.00857.
The purpose of the present study was to enhance the solubility and dissolution of diacerein by preparing their fatty acid-based, self-emulsifying solid dispersions (SDs) containing polyethylene glycol 6000 (PEG 6000), surfactant, and self-emulsifying excipient with high drug content. Ternary and self-emulsifying SDs containing high drug content were prepared and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, solubility studies, and dissolution studies. When hydrophilic and lipophilic excipients were combined and incorporated into PEG 6000-based SDs, a remarkable enhancement of the dissolution rate was observed, even in SDs with high drug content. The presence of surfactant and self-emulsifying excipient did not affect the solid state characterization of the drug. The decrease in the intensity of the numerous distinctive peaks of the drug in the PXRD spectra and absence of drug melting peak in DSC spectra demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix. The utilization of self-emulsifying excipient and surfactant in PEG 6000-based SDs could be a useful tool to enhance the dissolution and bioavailability of diacerein by forming solubilizing and microemulsifying systems with high drug content.
The purpose of the present study was to enhance the solubility and dissolution of diacerein by preparing their fatty acid-based, self-emulsifying solid dispersions with high drug content. These solid dispersions were prepared and characterized by powder X-ray diffraction, differential scanning calorimetry, Fourier transform infrared spectroscopy, solubility studies, and dissolution studies. When hydrophilic and lipophilic excipients were combined and incorporated into PEG 6000-based solid dispersions, a remarkable enhancement of the dissolution rate was observed, even in solid dispersions with high drug content. Moreover, the presence of surfactant and self-emulsifying excipient did not affect the solid state characterization of the drug. The decrease in the intensity of the numerous distinctive peaks of the drug in the powder X-ray diffraction spectra and absence of drug melting peak in the spectra obtained by differential scanning calorimetry demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix.
本研究的目的是通过制备含聚乙二醇6000（PEG 6000）、表面活性剂和具有高药物含量的自乳化辅料的脂肪酸基自乳化固体分散体（SDs）来提高双醋瑞因的溶解度和溶出度。制备了含高药物含量的三元和自乳化SDs，并通过粉末X射线衍射（PXRD）、差示扫描量热法（DSC）、傅里叶变换红外光谱、溶解度研究和溶出度研究对其进行了表征。当将亲水性和亲脂性辅料组合并掺入基于PEG 6000的SDs中时，即使在高药物含量的SDs中也观察到溶出速率显著提高。表面活性剂和自乳化辅料的存在不影响药物的固态表征。PXRD光谱中药物众多特征峰强度的降低以及DSC光谱中药物熔融峰的缺失表明高浓度的药物分子溶解在固态载体基质中。在基于PEG 6000的SDs中使用自乳化辅料和表面活性剂可能是通过形成具有高药物含量的增溶和微乳化系统来提高双醋瑞因的溶出度和生物利用度的有用工具。
本研究的目的是通过制备具有高药物含量的脂肪酸基自乳化固体分散体来提高双醋瑞因的溶解度和溶出度。这些固体分散体通过粉末X射线衍射、差示扫描量热法、傅里叶变换红外光谱、溶解度研究和溶出度研究进行制备和表征。当将亲水性和亲脂性辅料组合并掺入基于PEG 6000的固体分散体中时，即使在高药物含量的固体分散体中也观察到溶出速率显著提高。此外，表面活性剂和自乳化辅料的存在不影响药物的固态表征。粉末X射线衍射光谱中药物众多特征峰强度的降低以及差示扫描量热法获得的光谱中药物熔融峰的缺失表明高浓度的药物分子溶解在固态载体基质中。
