Pharmaceutical Co-crystal Study Based On The Active Ingredients Of Traditional Chinese Medicines In Guangxi Province

Objective: Most effective components extracted from traditional Chinese medicine have superior pharmacological activity in the treatment of relevant disease,but numerous of active ingredients shows low bioavailability due to its poor water solubility.Thus,it is this reason that influence the clinical efficacy,become the bottleneck of limited application of Traditional Chinese medicine preparations and internationalization.To solve these problem,we utilizing co-crystallization technology,take active ingredients(API)of native Traditional Chinese medicine in Guangxi production as the research object,match various biologically acceptable components(CCF)such as amino acids and carboxylic acids to design and preparation of drug cocrystal.Based on the cocrystal compounds related physicochemical properties(such as melting point,stability and solubility)and drug properties were systematically characterized,on cocrystal system of active pharmaceutical ingredients and eutectic component interactions,and then improve the solubility of active ingredients,improve the bioavailability,provide the theoretical foundation and experimental material in the field of development of new dosage forms of traditional Chinese medicine and property modulation.Methods: This topic focuses on the active components of traditional Chinese medicines,such as rhein,apigenin,quercetin,mangiferin,and theophylline,aims at preparation of eutectic drugs by means of slow solventevaporation method,incorporation method and incorporation combining solvent evaporation method.Furthermore,the resulting crystal was characterized by single crystal X-ray diffraction,powder X-ray diffraction,infrared spectroscopy,differential scanning calorimetry and melting point values.The solubility of pharmaceutical co-crystal was measured by high performance liquid chromatography.Results: Rhein-L-Arginine,rhein-L-Lysine,rhein-4,4'-Bipyridine,apigenin-4,4'-Bipyridine,apigenin-D-glutamine,quercetin-4,4'-Bipyridyl,Mangiferin-Nicotinamide and theophylline-nicotinamide were obtained successfully during the experiment,and all the pharmaceutical cocrystals was characterized by a series of analytical instrument.The experimental results show that,the combination of API and CCF is mainly through hydrogen bonding and ?-? stacking.After the cocrystals were formed,the melting points were lower than that of the crude drugs and their solubility have been improved to varying degrees.different.A great improvement in degree.Conclusion: Through the preparation of eutectic of rhein,apigenin,mangiferin,quercetin and theophylline,systematically studying the physicochemical properties such as melting point,stability and solubility of eutectic compounds,and researching the interaction between API and CCF,the result provide important theoretical and practical support for the modernization of traditional Chinese medicine in Guangxi and development the Traditional Chinese medicine products with independent intellectual property rights.