Aleem Omair, Kuchekar Bhanudas, Pore Yogesh, Late Sameer
Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra 415124, India.
J Pharm Biomed Anal. 2008 Jul 15;47(3):535-40. doi: 10.1016/j.jpba.2008.02.006. Epub 2008 Feb 15.
The solid-state properties, dissolution profile and antimicrobial activity of inclusion complexes of cefdinir (CEF) with beta-cyclodextrin (betaCD) and hydroxypropyl beta-cyclodextrin (HPbetaCD) were investigated. The phase solubility profiles of cefdinir with betaCD and HPbetaCD were classified as A(L)-type, which indicates the formation of 1:1 stoichiometry inclusion complexes. Stability constants with 1:1 molar ratio obtained from the phase solubility diagrams were 120.38+/-1.07 and 58.60+/-1.20 M(-1) for betaCD and HPbetaCD, respectively. Binary systems of CEF with betaCD and HPbetaCD prepared by kneading method were characterized by Fourier transformation-infrared spectroscopy (FTIR) and X-ray powder diffractometry (XRD). The aqueous solubility of CEF was enhanced by 101% for betaCD and 23.4% for HPbetaCD, respectively. The dissolution profiles of inclusion complexes were determined and compared with those of CEF alone and their physical mixtures. The dissolution rate of CEF was increased by betaCD and HPbetaCD inclusion complexation moderately. However, the antimicrobial activity of CEF was increased significantly (p<0.001) by betaCD and HPbetaCD inclusion complexation against S. aureus and E. coli. In all these studies, HPbetaCD had superior antimicrobial activity than that of betaCD while betaCD had greater effect on solubility enhancement of CEF.
研究了头孢地尼（CEF）与β-环糊精（βCD）和羟丙基-β-环糊精（HPβCD）包合物的固态性质、溶出曲线和抗菌活性。头孢地尼与βCD和HPβCD的相溶解度曲线属于A（L）型，这表明形成了化学计量比为1:1的包合物。从相溶解度图获得的1:1摩尔比的稳定常数，βCD和HPβCD分别为120.38±1.07和58.60±1.20 M⁻¹。通过捏合法制备的CEF与βCD和HPβCD的二元体系用傅里叶变换红外光谱（FTIR）和X射线粉末衍射（XRD）进行了表征。CEF的水溶性分别提高了101%（βCD）和23.4%（HPβCD）。测定了包合物的溶出曲线，并与单独的CEF及其物理混合物的溶出曲线进行了比较。βCD和HPβCD包合作用适度提高了CEF的溶出速率。然而，βCD和HPβCD包合作用对金黄色葡萄球菌和大肠杆菌的抗菌活性显著提高（p<0.001）。在所有这些研究中，HPβCD的抗菌活性优于βCD，而βCD对CEF的溶解度增强作用更大。
