Life Science Department, Foshan University, Foshan, P. R. China.
Das Pharma, Kakinada, India.
Drug Deliv. 2020 Dec;27(1):334-343. doi: 10.1080/10717544.2020.1724210.
Enrofloxacin, a third-generation fluoroquinolone, is a broad-spectrum antimicrobial drug against a lot of veterinary bacterial diseases. However, bactericidal activity of enrofloxacin is concentration-dependent and its poor aqueous solubility and bitter taste limit its development and application. Meanwhile, 2-hydroxypropyl--cyclodextrin (HP-β-CD), a widely used cyclodextrin analog, is a safe and an effective drug carrier. It forms inclusion complexes with its drug substrates and improves their physiochemical and pharmacokinetic properties. Enrofloxacin was also found to form a stable inclusion complex with HP-β-CD and different research groups have shown improved solubility for enrofloxacin by 32.5%, 9.25 and 165-fold. Our own efforts in this direction resulted in manifold improvement (916-fold) in its solubility compared to the previous studies. It was further shown that pharmaceutical properties, absorption and bioavailability, of enrofloxacin have also been significantly improved by complexation with HP-β-CD.
恩诺沙星，第三代氟喹诺酮类药物，是一种广谱抗菌药物，可用于治疗多种兽医细菌病。然而，恩诺沙星的杀菌活性与浓度有关，其较差的水溶性和苦味限制了它的发展和应用。同时，2-羟丙基-β-环糊精（HP-β-CD）作为一种广泛使用的环糊精类似物，是一种安全有效的药物载体。它与药物底物形成包合物，提高了它们的理化和药代动力学性质。恩诺沙星也被发现与 HP-β-CD 形成稳定的包合物，不同的研究小组已经表明，恩诺沙星的溶解度提高了 32.5%、9.25 倍和 165 倍。我们在这方面的努力使它的溶解度比以前的研究提高了 916 倍。进一步表明，恩诺沙星与 HP-β-CD 形成复合物后，其药物性质、吸收和生物利用度也得到了显著改善。
