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首页> 外文期刊>Crystal growth & design >Tracing the Architecture of Caffeic Acid Phenethyl Ester Cocrystals: Studies on Crystal Structure, Solubility, and Bioavailability Implications
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Tracing the Architecture of Caffeic Acid Phenethyl Ester Cocrystals: Studies on Crystal Structure, Solubility, and Bioavailability Implications

机译：跟踪咖啡酸苯乙基酯共晶体的体系结构：晶体结构，溶解度和生物利用度含义的研究。

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摘要

Caffeic acid phenethyl ester (CAPE) is a polyphenolic active compound present in popular apiproduct, "propolis", obtained from beehives, Though it has broad therapeutic capability, the bioavailability of CAPE is limited due to poor solubility. In this study, we report novel cocrystals of CAPE engineered using coformers such as caffeine (CAP), isonicotinamide (INIC), and nicotinamide (NIC) with enhanced solubility and bioavailability of CAPE. The cocrystals were prepared by microwave-assisted cocrystallization and characterized using PXRD, DSC, and Raman spectroscopy. PXRD and DSC confirm the successful formation and phase purity of CAPE-CAF, CAPE-INIC, and CAPE-NIC cocrystals. Raman spectra of CAPE cocrystals complement these results in confirming the formation of novel crystalline phases. CAPE-NIC cocrystal was further subjected X-ray crystallography to understand its molecular arrangement and hydrogen bonding in the crystal structure. The CAPE-NIC cocrystal structure is found to be stabilized by a rare 1,2-benzenediol-amide heterosynthon. Cocrystallization of CAPE with NIC improved its aqueous solubility and pharmacokinetic profile, thereby demonstrating a 2.76-fold escalation in bioavailability.
机译：咖啡酸苯乙酯（CAPE）是存在于流行的蜂产品“蜂胶”中的一种多酚活性化合物，得自蜂箱，尽管具有广泛的治疗能力，但由于溶解性差，CAPE的生物利用度受到限制。在这项研究中，我们报告了使用诸如咖啡因（CAP），异烟酰胺（INIC）和烟酰胺（NIC）等共形成物工程改造的CAPE的新型共结晶，具有提高的CAPE溶解度和生物利用度。通过微波辅助共结晶制备共晶体，并使用PXRD，DSC和拉曼光谱进行表征。 PXRD和DSC证实了CAPE-CAF，CAPE-INIC和CAPE-NIC共晶体的成功形成和相纯度。 CAPE共晶体的拉曼光谱补充了这些结果，从而证实了新型晶相的形成。对CAPE-NIC共晶体进一步进行X射线晶体学分析，以了解其分子排列和晶体结构中的氢键。发现CAPE-NIC共晶结构被稀有的1,2-苯二醇-酰胺杂合子稳定。 CAPE与NIC的共结晶改善了其水溶性和药代动力学特征，从而证明其生物利用度提高了2.76倍。

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