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Hydroxypropylcellulose-flurbiprofen conjugates: design, characterization, anti-inflammatory activity and enhanced bioavailability.
Saudi Pharmaceutical Journal ( IF 4.1 ) Pub Date : 2020-06-23 , DOI: 10.1016/j.jsps.2020.06.009
Muhammad Ajaz Hussain 1 , Iqra Shad 1 , Iram Malik 1 , Fasiha Amjad 1 , Tehreem Kausar 2 , Kamran 2 , Muhammad Sher 1 , Muhammad Nawaz Tahir 3 , Nisar Ullah 3 , Muhammad Ashraf 3 , Syed Nasir Abbas Bukhari 4
Affiliation  

Herein, we report novel macromolecular prodrugs (MPDs) of flurbiprofen (FLB) onto a cellulose ether, hydroxypropylcellulose (HPC). The FLB was activated with a powerful acylation reagent carbonyldiimadazole (CDI) in N,N′ dimethylacetamide (DMAc) solvent at room temperature. Imidazolide of FLB generated in situ reacts at 80 °C for 24 h with pre-dissolved HPC to prepare HPC-FLB conjugates. The resultant MPDs of FLB showed moderate to high degree of substitution (DS: 0.35–1.3) with good yield (70–82%). Structures were thoroughly characterized using FTIR, UV and NMR spectroscopic analyses. The pharmacokinetic studies showed that the t1/2 and tmax values of FLB from HPC-FLB conjugate were increased substantially as compare to standard FLB indicates enhanced bioavailability of drug after conjugate formation. Remarked anti-inflammatory activity of the HPC-FLB conjugate was also observed.



中文翻译:

羟丙基纤维素-氟比洛芬偶联物:设计,表征,抗炎活性和增强的生物利用度。

在本文中,我们报告了氟比洛芬(FLB)的新型大分子前药(MPD)到纤维素醚羟丙基纤维素(HPC)上。室温下N,N '二甲基乙酰胺(DMAc)溶剂中,用功能强大的酰化试剂羰基二咪唑(CDI)激活FLB 。生成FLB的咪唑就地在80℃下进行反应24小时,用预先溶解HPC以制备HPC-FLB缀合物。所产生的FLB MPD显示出中等至高度的取代度(DS:0.35–1.3),且产率高(70–82%)。使用FTIR,UV和NMR光谱分析对结构进行了全面表征。药代动力学研究表明,t 1/2和t max与标准FLB相比,HPC-FLB共轭物的FLB值显着增加,表明共轭物形成后药物的生物利用度提高。还观察到HPC-FLB缀合物的显着抗炎活性。

更新日期:2020-06-23
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