Effect of Drug Particle Size on Complexation, Physicochemical Properties and Dissolution of Cyclodextrin Inclusion Complexes
Effect of Drug Particle Size on Complexation, Physicochemical Properties and Dissolution of Cyclodextrin Inclusion Complexes
复制标题
DOI：
10.4172/pharmaceutical-science.1000209
复制
发表时间：
2017-01-01
影响因子：
0.5
通讯作者：
Ma, Y.
中科院分区：
文献类型：
--
作者：
Ai, F.;Wang, J.;Ma, Y.
本研究的主要目的是研究药物粒径对β-环糊精包合物的包合、理化性质和溶出度的影响。在这项工作中，采用3 μ m和45 μ m大小的布洛芬（布洛芬3和布洛芬45）作为水溶性差的药物模型。采用包合动力学和包合效率研究了布洛芬与β-环糊精在水中的包合反应。采用捏合法制备了环糊精固体包合物，并用红外光谱、差示扫描量热法、X射线粉末衍射法、光学显微镜和溶出度等方法对包合物进行了表征。在包合动力学研究中，粒径较小的环糊精与β-环糊精的包合速率较高。通过比较复合物的表观稳定常数、K-c和包合效率，还表明较小的药物颗粒比较大的颗粒更有效地与β-环糊精相互作用。相溶解度图属于Bs型，表明配合物具有有限的溶解度.傅立叶变换红外光谱、差示扫描量热法、X射线粉末衍射法和光学显微镜分析证实了布洛芬3或布洛芬45与β-环糊精形成包合物。在溶出度研究中，包合物的溶出速度比物理混合物和纯药物快。小粒径布洛芬包合物的溶出度比大粒径布洛芬包合物的溶出度高。
The main purpose of this study was to investigate the role of drug particle size on the complexation, physicochemical properties and dissolution of beta-cyclodextrin inclusion complexes. In this work, ibuprofen in size of 3 mu m and 45 mu m (ibuprofen 3 and ibuprofen 45) were employed as the poorly water-soluble drug model. Complexation kinetics and complexation efficiency studies were conducted to investigate the complexation of ibuprofen with beta-cyclodextrin in water. The solid cyclodextrins inclusion complexes were prepared with kneading method and characterized by Fourier transform-infrared spectroscopy, differential scanning calorimetry, X-ray powder difractometry, optical microscopy analyses and dissolution test. Ibuprofen with smaller particle size showed higher complexation rate with beta-cyclodextrin in complexation kinetics study. By comparing the apparent stability constant, K-c and complexation efficiency of complexes, it also indicated that smaller drug particles are more efficient to interact with beta-cyclodextrin than larger particles. The phase solubility diagram could be classified as Bs type, which denotes complexes with limited solubility. The Fourier transform-infrared spectroscopy, differential scanning calorimetry, X-ray powder difractometry and optical microscopy analyses confirmed the formation of beta-cyclodextrin inclusion complexes with ibuprofen 3 or ibuprofen 45. In the dissolution study, the inclusion complexes presented faster dissolution rate on contrast with the physical mixtures and pure drugs. What is more, the inclusion complexes prepared with ibuprofen in small particle size showed improving dissolution rate than in large particle size.