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Acta Pharmaceutica Sinica ; (12): 570-576, 2021.
Article in Chinese | WPRIM | ID: wpr-873779


Four salts of ticagrelor, ticagrelor-3,5-dinitrobenzoic acid, ticagrelor-pyrazinamide, ticagrelor-D-proline and ticagrelor-L-proline were prepared by solvent suspension and liquid-assisted grinding to improve the solubility of ticagrelor. The compounds were characterized by powder X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry, nuclear magnetic resonance spectroscopy, elemental analysis, and the intermolecular salt-bonding forces were analyzed. The equilibrium solubility of salts and pure drug in hydrochloride buffer pH 1.2 and phosphate buffer pH 6.8 were measured by high-performance liquid chromatography. Ticagrelor was salted with 3,5-dinitrobenzoic acid, pyrazinamide, D-proline, L-proline all in a stoichiometric ratio of 1∶1; with the exception of ticagrelor-D-proline, the solubility of the other three salts provided significantly improved solubility in hydrochloride buffer pH 1.2, and the equilibrium solubility of ticagrelor-3,5-dinitrobenzoic acid was increased by approximately 1.7 folds as compared to pure drug. Salt-forming technology is convenient and can improve the solubility of ticagrelor.

Acta Pharmaceutica Sinica ; (12): 673-676, 2010.
Article in Chinese | WPRIM | ID: wpr-354572


The powder X-ray diffraction Fourier fingerprint pattern technique was used to develop a new quantitation method for the analysis of andrographolide and dehydroandrographolide. And the high performance liquid chromatography method was used to evaluate the quantity of andrographolide and dehydroandrographolide. The relationship of diffraction peak intensity and content of andrographolide and dehydroandrographolide was investigated. The powder X-ray diffraction Fourier fingerprint pattern analysis technique can be used to evaluate the quantity of andrographolide and dehydroandrographolide in the herb simultaneously.

Andrographis , Chemistry , Chromatography, High Pressure Liquid , Diterpenes , Drugs, Chinese Herbal , Fourier Analysis , Plant Components, Aerial , Chemistry , Plants, Medicinal , Chemistry , Powders , X-Ray Diffraction , Methods
Article in Chinese | WPRIM | ID: wpr-266777


<p><b>OBJECTIVE</b>To study the selective isolation of a single chemical component from volatile oil of Fructus foeniculi by inclucion method.</p><p><b>METHOD</b>The host molecule was selected and a single chemical component isolated from volatile oil by the host-guest recognition.</p><p><b>RESULT</b>X-ray single crystal analysis showed that 1,1,6,6-tetraphenylhexa-2, 4-diyne-1, 6-diol could successfully include 4-[1-propenyl] benzaldehyde from volatile oil of Fructus foeniculi.</p><p><b>CONCLUSION</b>The host-guest inclusion technology can be used to isolate a single component selectively from mixture.</p>

Crystallization , Crystallography, X-Ray , Methods , Foeniculum , Chemistry , Molecular Conformation , Oils, Volatile , Chemistry , Plants, Medicinal , Chemistry , Seeds , Chemistry
Article in Chinese | WPRIM | ID: wpr-274984


<p><b>OBJECTIVE</b>To demonstrate the chemical constituents of Alyxia sinensis.</p><p><b>METHOD</b>The constituents were isolated by column chromatography and identified by advanced physical and spectral analysis.</p><p><b>RESULT</b>Eight compounds have been isolated and elucidated as bauereny acetate(18), scopletin(19), liriodendrin(20), pinoresinol-di-O-beta-D-glucopyranoside(21), daucosterol(22), flaxetin(23), esculin(24), aseculin(25).</p><p><b>CONCLUSION</b>These compounds were found from the plant for the first time, and compound 20,21,23-25 were found from Alyxiae genis for the first time, and compound 18 is firstly been isolated from natural source.</p>

Apocynaceae , Chemistry , Esculin , Chemistry , Furans , Chemistry , Glucosides , Chemistry , Molecular Structure , Plants, Medicinal , Chemistry , Triterpenes , Chemistry