Crystal engineering of multiple-component organic solids to improve the solubility:Pharmaceutical co

来源 :2013年中国药物制剂大会——中国药学会药剂专业委员会2013年学术年会暨国际控释协会中国分会2013年学术年会 | 被引量 : 0次 | 上传用户:xybcn960
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
  Objectives The objectives of this study were to prepare and characterize the novel myricetin cocrystals and to demonstrate the enhanced solubility and dissolution.Methods The experiments based on the solution method yielded four cocrystals, with nicotinamide (NIC), isonicotinamide (INM), caffeine (CAF), 4-cyanopyridine (CYA) and reaction crystallization experiments were carried out to scale-up the hits.Solid-state characterization was carried out by PXRD, DSC, IR spectroscopy and liquid-state NMR analysis.Solubility and dissolution studies were performed by comparison with its pure components in different pH buffers.Phase transition was showed through the creation of a ternary phase diagram.Key findings Four new solid myricetin cocrystals with unique melting point, DSC, FTIR and PXRD data was obtained.The molar ratio of four cocrystals was different: MYR-CAF (1∶1),MYR-CYA (1∶3), MYR-NIC (1∶2), MYR-INM (1∶2).The cocrystals had a pH-independent dissolution profile and showed a nearly ten-fold increase in the dissolution efficiency in different pH buffers.The crystal structures of four cocrystals were solved by single-crystal X-ray diffraction and were analyzed in terms of their supramolecular synthons.
其他文献
会议
会议
To enhance targeting ability and reduce non-specific uptake of drug delivery system for cancer therapy, a smart anti-tumor liposomal carrier with concealed RGD (cyclic Arginine-Glycine-Aspartic acid-D
Modernization of Chinese medicine is the only way to the world for the Chinese medicine.The development of new preparation technology has brought a new direction and methods for the traditional Chines
会议
Aim: To determine the best way of adding bomeol and the content of bomeol in Sanjie Zhitong cataplasm.Methods: The determination methodology of bomeol by Gas Chromatography was established.The four ki
In order to obtain a lower-toxicity and higher-efficiency drug delivery system, we have focused on a multifunctional envelope-type nano device (MEND) for efficient delivery.For antitumor drug delivery
会议