生物利用度
泊洛沙姆
溶解度
化学
三元运算
溶解
泊洛沙姆407
核化学
色谱法
体内
环糊精
药理学
有机化学
医学
聚合物
共聚物
程序设计语言
生物技术
生物
计算机科学
作者
Md. Khalid Anwer,Muzaffar Iqbal,Mohammad Muqtader Ahmed,Mohammed F. Aldawsari,Mohd Nazam Ansari,Essam Ezzeldin,Nasr Y. Khalil,Raisuddin Ali
出处
期刊:Pharmaceuticals
[Multidisciplinary Digital Publishing Institute]
日期:2021-04-26
卷期号:14 (5): 411-411
被引量:16
摘要
In the current study, the effect of poloxamer 188 on the complexation efficiency and dissolution of arbidol hydrochloride (ADL), a broad-spectrum antiviral agent, with β-cyclodextrin (β-CD) was investigated. Phase solubility studies confirmed a stoichiometry of a 1:1 ratio for both ADL:β-CD and ADL/β-CD with a 1% poloxamer 188 system with an AL type of phase solubility curve. The stability constants (K1:1) calculated from the AL type diagram were 550 M-1 and 2134 M-1 for AD:β-CD and ADL/β-CD with 1% poloxamer 188, respectively. The binary ADL/β-CD and ternary ADL/β-CD with 1% poloxamer 188 complexes were prepared by kneading and a solvent evaporation method and were characterized by aqueous solubility, FTIR, PXRD, DSC and SEM in vitro studies. The solubility (13.1 fold) and release of ADL were markedly improved in kneaded ternary ADL/β-CD with 1% poloxamer 188 (KDB). The binding affinity of ADL and β-CD was confirmed by 1H NMR and 2D ROSEY studies. The ternary complex (KDB) was further subjected for in vivo pharmacokinetic studies in rats and a significant improvement in the bioavailability (2.17 fold) was observed in comparison with pure ADL. Therefore, it can be concluded that the solubilization and bioavailability of ADL can be remarkably increased by ADL/β-CD complexation in the presence of a third component, poloxamer 188.
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