Ege University, Faculty of Pharmacy, Department of Biopharmaceutics and Pharmacokinetics, Izmir, Turkey.
Drug Dev Ind Pharm. 2012 Jun;38(6):689-96. doi: 10.3109/03639045.2011.621434. Epub 2011 Oct 19.
This study aims to prove the complexation of cefpodoxime proxetil (CP) by hydroxypropyl-β-cyclodextrin (HP-β-CD) in the presence of sodium carboxymethyl cellulose (Na CMC), and makes a comparison of commercial tablets by dissolution and antimicrobial activity studies. The CP--HP-β-CD complex was prepared by kneading method and characterized by SEM, FTIR and DSC. The solubility method was used to investigate the effect of HP-β-CD and Na CMC on the solubility of CP. The complex tablets were prepared using direct compression method. Dissolution studies were performed with complex tablets and commercial tablets in pH 1.2, 4.5, 6.8 and 7.4 buffer solutions. It was observed that complexation occurred in all formulations, and HP-β-CD is able to increase CP solubility and dissolution rate of CP was improved from complex tablets, when compared with commercial tablets. Furthermore, the antimicrobial activity studies revealed that the CP--HP-β-CD complex and complex tablets were shown to have more effective antimicrobial activity than commercial tablets. It is evident from the results that complexation with HP-β-CD in the presence of Na CMC is feasible way to prepare a more efficient tablet formulation with improved dissolution and antimicrobial activity.
本研究旨在证明头孢泊肟酯（CP）在羧甲基纤维素钠（NaCMC）存在下与羟丙基-β-环糊精（HP-β-CD）的络合，并通过溶出度和抗菌活性研究对市售片剂进行比较。CP-HP-β-CD 配合物通过捏合法制备，并通过 SEM、FTIR 和 DSC 进行表征。采用溶解度法考察 HP-β-CD 和 NaCMC 对 CP 溶解度的影响。采用直接压片法制备配合物片剂。在 pH 值为 1.2、4.5、6.8 和 7.4 的缓冲溶液中对复合片剂和市售片剂进行溶出度研究。结果表明，所有配方均发生络合，HP-β-CD 能够提高 CP 的溶解度，且与市售片剂相比，CP 的溶出度得到改善。此外，抗菌活性研究表明 CP-HP-β-CD 配合物和复合片剂的抗菌活性均优于市售片剂。结果表明，在 NaCMC 存在下与 HP-β-CD 络合是一种可行的方法，可以制备具有改善的溶出度和抗菌活性的更有效的片剂制剂。
