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Cocrystal Screening of Ibuprofen with Oxalic Acid and Citric Acid via Grinding Method

机译:通过研磨方法将布洛芬与草酸和柠檬酸的Cocrystal筛选

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Ibuprofen is a Class II Biological Safety Class(BSC)drugs used for relief of arthritis,as an analgesic and possesses the effect of antiplatelet.The major problem involves in ibuprofen is it has a low solubility and high permeability thus causes an unsatisfactory therapeutic effect to humans.Thus,in this work,alteration of ibuprofen’s physicochemical properties is conducted by means of cocrystallization technique.Co-crystallizations of ibuprofen were prepared with selected coformers using dry grinding and liquid assisted grinding(LAG)techniques in different molar ratios while ethanol and propanol were used as a solvent.The new crystalline forms were identified and characterized by differential scanning,calorimetry(DSC),powder X-ray diffraction(PXRD)and fourier transform infrared spectroscopy(FTIR).Analysis for Ibuprofen-Citric acid(IBP-CA)system,co-crystal was successfully formed in 1:2,1:3,2:1 and 3:1 molar ratios for neat grinding method although the co-crystal produced is unstable.Meanwhile,for Ibuprofen-Oxalic acid(IBP-OA)system,the co-crystal formation was identified only in 1:1,1:2 and 1:3 molar ratios for the neat grinding method.LAG method shows that co-crystal formation was unsuccessful in both solvents for IBP-CA,while IBP-OA co-crystal was formed in the molar ratio 1:1,2:1 and 3:1 in ethanol,and 2:1 and 3:1 in propanol.
机译:布洛芬是一种II类生物安全等级(BSC)的药物用于关节炎的救济,作为止痛剂和具有antiplatelet.The重大问题的影响涉及布洛芬是它具有低的溶解度并因此高渗透性会导致不令人满意的治疗效果humans.Thus,在这项工作中,布洛芬的物理化学性质的改变是通过布洛芬的共结晶technique.Co-结晶的方式进行的用使用干研磨和液体选择的助形成物制备辅助磨削在不同摩尔比(LAG)技术,同时乙醇和丙醇被用作一个solvent.The新结晶形式被鉴定和表征通过差示扫描,量热法(DSC),粉末X射线衍射(PXRD)和傅里叶变换红外光谱(FTIR)。分析布洛芬 - 柠檬酸(IBP-CA )系统中,成功地形成共晶体在1:2,1:3,2:1和3:1分的摩尔比为整洁研磨方法虽然所产生的共晶体是unstable.Me anwhile,对于布洛芬草酸(IBP-OA)的系统,所述共晶体的形成仅鉴定在1:1,1:2和1:纯磨削method.LAG方法示出了3个摩尔比该共晶体形成在两种溶剂为IBP-CA不成功,而在摩尔比1形成IBP-OA共晶体:1,2:1和3:在乙醇中1和2:1和3:1的丙醇。

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