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Formation of inclusion complex of enrofloxacin with 2-hydroxypropyl-β-cyclodextrin.
Drug Delivery ( IF 6 ) Pub Date : 2020-02-24 , DOI: 10.1080/10717544.2020.1724210
Yili Ding 1 , Yuchang Pang 1 , Chamakura V N S Vara Prasad 2 , Bingyun Wang 1
Affiliation  

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-β-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.

中文翻译:

恩诺沙星与2-羟丙基-β-环糊精的包合物形成。

恩诺沙星(Enrofloxacin)是第三代氟喹诺酮,是一种针对许多兽医细菌疾病的广谱抗菌药物。然而,恩诺沙星的杀菌活性是浓度依赖性的,其不良的水溶性和苦味限制了其开发和应用。同时,广泛使用的环糊精类似物2-羟丙基-β-环糊精(HP-β-CD)是安全有效的药物载体。它与其药物底物形成包合物,并改善其理化和药代动力学特性。还发现恩诺沙星与HP-β-CD形成稳定的包合物,不同的研究小组显示对恩诺沙星的溶解度提高了32.5%,9.25和165倍。与以前的研究相比,我们在这个方向上的努力导致其溶解度得到了许多提高(916倍)。
更新日期:2020-04-20
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