Cocrystallization process involved the understanding of interaction at molecular level between two molecules in context to their crystal packing and designing of new solids having improved physicochemical as well as pharmaceutical properties. In the present research, an attempt to increase the aqueous solubility and dissolution rate of a poorly aqueous soluble drug fenofibrate (FB) by formulation and evaluation of its cocrystals with benzoic acid (BZ) as a coformer was carried out. The drug and coformer were cocrystallized by using the solvent drop grinding method. For prediction of cocrystals formation, CSD (Cambridge Structure Database) software was utilized. Fourier transformation infrared spectroscopy (FTIR), X-ray diffraction (XRD) and differential scanning calorimetry (DSC) techniques were used for analysis of cocrystals. Albino rats were procured from institution as per IAEC guidelines for in vivo anti-hyperlipidaemic studies. The in vitro dissolution profile of cocrystals, pure drug, their physical mixture and marketed formulation was found to be 89%, 39%, 47% and 61%, respectively. An enhanced anti-hyperlipidaemic activity of cocrystals was found compared to pure drug. The FB: BZ cocrystals also compared to the pure drug showed better dissolution profile and improved in vivo anti-hyperlipidaemic activity in rats. The study proved that cocrystals can promise to improve in vitro dissolution rate of poorly aqueous soluble drugs, which in turn can lead to better in vivo activities.

中文翻译：

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非诺贝特的制备、表征和评价：具有增强药物特性的苯甲酸共晶

共结晶过程涉及理解两个分子之间在分子水平上的相互作用，以及它们的晶体堆积和具有改进的物理化学和药物特性的新固体的设计。在目前的研究中，尝试通过以苯甲酸 (BZ) 作为共形成剂的共晶进行配方和评估来提高水溶性差的药物非诺贝特 (FB) 的水溶性和溶出速率。使用溶剂滴磨法使药物和共形成物共结晶。为了预测共晶形成，使用了 CSD（剑桥结构数据库）软件。傅里叶变换红外光谱 (FTIR)、X 射线衍射 (XRD) 和差示扫描量热法 (DSC) 技术用于分析共晶。白化大鼠是根据 IAEC 体内抗高脂血症研究指南从机构采购的。共晶、纯药物、它们的物理混合物和市售制剂的体外溶出度分别为 89%、39%、47% 和 61%。与纯药物相比，发现共晶具有增强的抗高血脂活性。与纯药物相比，FB: BZ 共晶也显示出更好的溶出曲线和改善的大鼠体内抗高血脂活性。该研究证明，共晶有望提高难溶性药物的体外溶出度，从而提高体内活性。发现它们的物理混合物和市售配方分别为 89%、39%、47% 和 61%。与纯药物相比，发现共晶具有增强的抗高血脂活性。与纯药物相比，FB: BZ 共晶也显示出更好的溶出曲线和改善的大鼠体内抗高血脂活性。该研究证明，共晶有望提高难溶性药物的体外溶出度，从而提高体内活性。发现它们的物理混合物和市售配方分别为 89%、39%、47% 和 61%。与纯药物相比，发现共晶具有增强的抗高血脂活性。与纯药物相比，FB: BZ 共晶也显示出更好的溶出曲线和改善的大鼠体内抗高血脂活性。该研究证明，共晶有望提高难溶性药物的体外溶出度，从而提高体内活性。