Ding Yili, Yu Bo, Zhang Jianzhou, Ding Charles, Zhang Zhiyuan, Xu Shufeng, Li Lu, Yu Hui
College of Science and Technology, Wenzhou-Kean University, Wenzhou, Zhejiang 325000, PR China.
Life Science Department, Foshan University, Foshan, Guangdong 528000, PR China.
Eur J Pharm Biopharm. 2022 Dec;181:104-112. doi: 10.1016/j.ejpb.2022.10.024. Epub 2022 Nov 11.
Tilmicosin, as an effective broad-spectrum antibacterial drug, has incomplete absorption and low bioavailability due to its low water solubility, which limits its veterinary clinical applications. As a non-polymeric drug carrier, γ-cyclodextrin was complexed with tilmicosin through supercritical carbon dioxide assistance for the first time, and confirmed by FTIR, X-ray diffraction, proton NMR and scanning electron microscopy. The water solubility of tilmicosin was increased 57-fold through complexation with γ-cyclodextrin, and the release and bioavailability of tilmicosin in the complex were significantly improved. The tilmicosin in complex showed better anti-Streptococcus agalactiae activity than that of tilmicosin alone in MIC, MBC and drug susceptibility studies.
替米考星作为一种有效的广谱抗菌药物，由于其水溶性低，吸收不完全且生物利用度低，这限制了它在兽医临床中的应用。作为一种非聚合药物载体，首次通过超临界二氧化碳辅助使γ-环糊精与替米考星络合，并通过傅里叶变换红外光谱（FTIR）、X射线衍射、质子核磁共振（NMR）和扫描电子显微镜进行了确证。通过与γ-环糊精络合，替米考星的水溶性提高了57倍，且络合物中替米考星的释放和生物利用度显著提高。在最低抑菌浓度（MIC）、最低杀菌浓度（MBC）和药敏试验研究中，络合物中的替米考星比单独的替米考星表现出更好的抗无乳链球菌活性。
