Betulin(BE)can be obtained from many plants,such as those belonging Betulaceae family,and pharmacological investigations showed its notable biological properties and good potential for food and pharmaceutical developm...Betulin(BE)can be obtained from many plants,such as those belonging Betulaceae family,and pharmacological investigations showed its notable biological properties and good potential for food and pharmaceutical development.We investigated the homogeneity,stability,purity,and uncertainty of a newly certified reference material(CRM)of BE.The certified purity value for the CRM of BE was 99.56%with an extended uncertainty of 0.07%(k=2,P=0.95),as determined by differential scanning calorimetry(DSC).In this study,DSC was used for the first time for purity determination of BE.Given its high accuracy,precision,and reproducibility,DSC can be used as an alternative technique for purity determination of CRMs in the pharmaceutical and food industry.展开更多
Voriconazole(VZL)is a second-generation and broad-spectrum triazole against fungal infections.Being a BCS(biopharmaceutics classification system)class II compound,the poor aqueous solubility has limited its bioavailab...Voriconazole(VZL)is a second-generation and broad-spectrum triazole against fungal infections.Being a BCS(biopharmaceutics classification system)class II compound,the poor aqueous solubility has limited its bioavailability and clinical efficacy.Aims to overcome this disadvantage,a cocrystallization strategy based on crystal engineering principles has resulted in five new multi-component crystals of VZL with maleic acid,L-tartaric,protocatechuic,gallic,and 3,5-dinitrobenzoic acids.Structure analysis revealed that the hydroxyl/carboxylic acid···triazole N_(3)hydrogen bonding interaction appears as a main supramolecular heterosynthon in the VZL multi-component crystals with organic acids.And VZL molecule has a flexible conformation in each of the five multi-component structures.The newly synthesized multi-component crystals showed impressive solubility improvement compared to that of the raw material of VZL.Molecular electrostatic potential surfaces(MEPS)analysis based on density functional(DFT)calculations revealed that hydrogen bond interactions in cocrystals mainly involved pairwise interactions in the global maxima and minima sites,but this rule is not always followed.This study indicates the potential of cocrystals to improve the solubility and dissolution rate of VZL.展开更多
Pharmaceutical salt formation is the most preferred and effective method to enhance the physicochemical properties of APIs. The aim of the study was to design and synthesize a series of new salts to improve the solubi...Pharmaceutical salt formation is the most preferred and effective method to enhance the physicochemical properties of APIs. The aim of the study was to design and synthesize a series of new salts to improve the solubility of Imatinib(IM). Two stable salts with malonic acid(S1) and citric acid(S5), one metastable salt with fumaric acid(S2), two unstable salts with citric acid(S3, S4) were obtained for the first time.Single crystal and powder X-ray diffraction, Fourier transform infrared, differential scanning calorimetry,and thermogravimetric analysis were used to characterize the novel salts. The solubility and stability of the solid were also evaluated, and three salts(S1, S2, S5) had a more than 20 folds of solubility and a faster dissolution rate improved as compared to the pure drug in water and p H 6.8 buffer, respectively.展开更多
HPLC fingerprinting and determination methods were applied to evaluate 88 batches of Rhizoma Coptidis from 27 different areas. The results showed that HPLC fingerprint of Rhizoma Coptidis was established with good sep...HPLC fingerprinting and determination methods were applied to evaluate 88 batches of Rhizoma Coptidis from 27 different areas. The results showed that HPLC fingerprint of Rhizoma Coptidis was established with good separation and repeatability, which could be used for quality assessment of Rhizoma Coptidis. Twelve common peaks were defined in characteristic fingerprints, and similarity evaluation system was applied to evaluate the fingerprints of 88 batches of Rhizoma Coptidis, the contents of six alkaloids have been determined. The method of assessing Rhizoma Coptidis and evaluation of its quality has been established.展开更多
基金supported by National Key R&D Program of China(Grant No.2016YFC1000900)National Science and Technology Major Project of China(Grant Nos.2017ZX09101001003,2018ZX09711001-003-022,2018ZX09711001-010)+1 种基金National Natural Science Foundation of China(NSFC)(Grant No.81703473)CAMS Innovation Fund for Medical Sciences(Grant No.2017-I2M-3-010).
文摘Betulin(BE)can be obtained from many plants,such as those belonging Betulaceae family,and pharmacological investigations showed its notable biological properties and good potential for food and pharmaceutical development.We investigated the homogeneity,stability,purity,and uncertainty of a newly certified reference material(CRM)of BE.The certified purity value for the CRM of BE was 99.56%with an extended uncertainty of 0.07%(k=2,P=0.95),as determined by differential scanning calorimetry(DSC).In this study,DSC was used for the first time for purity determination of BE.Given its high accuracy,precision,and reproducibility,DSC can be used as an alternative technique for purity determination of CRMs in the pharmaceutical and food industry.
基金supported by Beijing Natural Science Foundation(No.7222261)Key R&D Program of Shan Dong Province(No.2021ZDSYS26)+2 种基金the Fundamental Research Funds for the Central Universities(No.2021-RW350-001)the Xinjiang Uygur Autonomous Region Innovation Environment Construction Special FundTechnology Innovation Base Construction Key Laboratory Open Project(No.2022D04016)。
文摘Voriconazole(VZL)is a second-generation and broad-spectrum triazole against fungal infections.Being a BCS(biopharmaceutics classification system)class II compound,the poor aqueous solubility has limited its bioavailability and clinical efficacy.Aims to overcome this disadvantage,a cocrystallization strategy based on crystal engineering principles has resulted in five new multi-component crystals of VZL with maleic acid,L-tartaric,protocatechuic,gallic,and 3,5-dinitrobenzoic acids.Structure analysis revealed that the hydroxyl/carboxylic acid···triazole N_(3)hydrogen bonding interaction appears as a main supramolecular heterosynthon in the VZL multi-component crystals with organic acids.And VZL molecule has a flexible conformation in each of the five multi-component structures.The newly synthesized multi-component crystals showed impressive solubility improvement compared to that of the raw material of VZL.Molecular electrostatic potential surfaces(MEPS)analysis based on density functional(DFT)calculations revealed that hydrogen bond interactions in cocrystals mainly involved pairwise interactions in the global maxima and minima sites,but this rule is not always followed.This study indicates the potential of cocrystals to improve the solubility and dissolution rate of VZL.
基金CAMS Innovation Fund for Medical Sciences(Nos. 2017-I2M-1–010, 2020-I2M-1–003)Key National Research and Development Program (No. 2016YFC1000901)+1 种基金Construction and Application of Technology Integration System for Efficient Identification of Natural/Effective Active Small Molecules (No.2018ZX09711001–001)National Science and Technology Major Project:Resource Library of Traditional Chinese Medicine Component (No. 2019ZX09735002) for the financial support。
文摘Pharmaceutical salt formation is the most preferred and effective method to enhance the physicochemical properties of APIs. The aim of the study was to design and synthesize a series of new salts to improve the solubility of Imatinib(IM). Two stable salts with malonic acid(S1) and citric acid(S5), one metastable salt with fumaric acid(S2), two unstable salts with citric acid(S3, S4) were obtained for the first time.Single crystal and powder X-ray diffraction, Fourier transform infrared, differential scanning calorimetry,and thermogravimetric analysis were used to characterize the novel salts. The solubility and stability of the solid were also evaluated, and three salts(S1, S2, S5) had a more than 20 folds of solubility and a faster dissolution rate improved as compared to the pure drug in water and p H 6.8 buffer, respectively.
基金Special Scientific Research of Chinese Medicine Industry(Grant No 200707014)
文摘HPLC fingerprinting and determination methods were applied to evaluate 88 batches of Rhizoma Coptidis from 27 different areas. The results showed that HPLC fingerprint of Rhizoma Coptidis was established with good separation and repeatability, which could be used for quality assessment of Rhizoma Coptidis. Twelve common peaks were defined in characteristic fingerprints, and similarity evaluation system was applied to evaluate the fingerprints of 88 batches of Rhizoma Coptidis, the contents of six alkaloids have been determined. The method of assessing Rhizoma Coptidis and evaluation of its quality has been established.
