• 中国精品科技期刊
  • 中国高校百佳科技期刊
  • 中国中文核心期刊
  • 中国科学引文数据库核心期刊
Advanced Search
FAN Yujie, SONG Yiting, ZHANG Yaqi, QIAN Shuai, WEI Yuanfeng, ZHANG Jianjun. Effect of solvents on the formation thermodynamics of baicalein-nicotinamide cocrystals[J]. Journal of China Pharmaceutical University, 2016, 47(4): 437-441. DOI: 10.11665/j.issn.1000-5048.20160408
Citation: FAN Yujie, SONG Yiting, ZHANG Yaqi, QIAN Shuai, WEI Yuanfeng, ZHANG Jianjun. Effect of solvents on the formation thermodynamics of baicalein-nicotinamide cocrystals[J]. Journal of China Pharmaceutical University, 2016, 47(4): 437-441. DOI: 10.11665/j.issn.1000-5048.20160408

Effect of solvents on the formation thermodynamics of baicalein-nicotinamide cocrystals

More Information
  • The purpose of this study was to investigate the formation thermodynamics of baicalein(BE)-nicotinamide(NCT)cocrystals in three solvents including ethyl acetate, acetone and trichloromethane. The solubilities of BE, NCT and BE-NCT in the above solvents at 25 °C were measured. Ternary phase diagrams(TPDs)of the BE-NCT-solvent systems were established. The non-linear fitting equation according to 1 ∶1 complexation mechanism of BE-NCT cocrystals demonstrated a good correlation between calculated and experiment data. ΔG0< 0 suggested that BE-NCT cocrystal formation was a spontaneous process. Among the organic solvents studied, the absolute value of ΔG0 in trichloromethane was significantly lower than that in the other two solvents. In addition, the cocrystallization zone in trichloromethane was far away from stoichiometric line. This study provides a theoretical foundation for solvent selection and preparation-condition optimization of BE-NCT cocrystals.
  • [1]
    Gao Y,Zu H,Zhang JJ.Pharmaceutical cocrystals[J].Prog Chem(化学进展),2010,22(5):829-836.
    [2]
    Shan N,Zaworotko MJ.The role of cocrystals in pharmaceutical science[J].Drug Discov Today,2008,13(9):440-446.
    [3]
    Gao Y, Zu H, Zhang JJ. Enhanced dissolution and stability of adefovir dipivoxil by cocrystal formation[J].J Pharm Pharmacol,2011,63(4):483-490.
    [4]
    Bolton O,Matzger AJ.Improved stability and smart-material functionality realized in an energetic cocrystal[J].Angew Chem Int Ed Engl,2011,50(38):8960-8963.
    [5]
    Huang YT, Zhang BW, Gao Y, et al. Baicalein-nicotinamide cocrystal with enhanced solubility,dissolution,and oral bioavailability[J].J Pharm Sci,2014,103(8):2330-2337.
    [6]
    Zhang YQ,Huang YT,Gao Y,et al.Thermodynamics of baicalein-nicotinamide co-crystallization process [J].J China Pharm Univ(中国药科大学学报),2015,46(5):568-574.
    [7]
    Kumar D,Shastri NR.Designed isomorphism of nifedipine:ajoint experimental and molecular simulation study with screened solvents and antisolvents[J].Cryst Growth Des,2013,14(1):326-338.
    [8]
    Sreekanth BR,Vishweshwar P,Vyas K.Supramolecular synthon polymorphism in 2∶1 cocrystal of 4-hydroxybenzoic acid and 2,3,5,6-tetramethylpyrazine[J].Chem Commun,2007,23(23):2375-2377.
    [9]
    Keraliya RA,Soni TG,Thakkar VT,et al.Effect of solvent on crystal habit and dissolution behavior of tolbutamide by initial solvent screening[J].Dissolut Technol,2010,17(1):16-21.
    [10]
    Ma K, Zhang Y, Kan HL, et al. Thermodynamic and kinetic investigation on the crucial factors affecting adefovir dipivoxil-saccharin cocrystallization[J].Pharm Res,2014,31(7):1766-1778.
    [11]
    Nehm SJ,Rodríguez-Spong B,Rodríguez-Hornedo N.Phase solubility diagrams of cocrystals are explained by solubility product and solution complexation[J].Cryst Growth Des,2005,6(2):592-600.
    [12]
    Schartman R.On the thermodynamics of cocrystal formation[J].Int J Pharm,2009,365(1/2):77-80.
  • Related Articles

    [1]LI Zhenming, HUO Meirong, DENG Qidan, CHEN Dengjun, SUN Hongzhang. In vitro evaluation of saxagliptin and metformin hydrochloride sustained-release tablets[J]. Journal of China Pharmaceutical University, 2021, 52(5): 541-546. DOI: 10.11665/j.issn.1000-5048.20210505
    [2]ZHANG Jinlin, YUAN Yaozuo, ZHANG Ya, ZHAO Shuqiang, ZHAO Xun, ZHANG Mei. Consistency evaluation of domestic generic rifampicin capsules and reference drug in vitro[J]. Journal of China Pharmaceutical University, 2018, 49(5): 603-609. DOI: 10.11665/j.issn.1000-5048.20180513
    [3]Study on Optimize the Preparation and Formulation of Nimodipine-Containing Nanoliposome[J]. Journal of China Pharmaceutical University, 2003, (1): 27-30.
    [4]Distribution of Nimodipine Microemulsion in Mice In vivo and Evaluation on Its Targeting Performance[J]. Journal of China Pharmaceutical University, 2002, (4): 31-34.
    [5]Study on Transdermal Therapeutic System for Nimodipine[J]. Journal of China Pharmaceutical University, 2000, (5): 28-31.
    [6]Development of Nimodipine Sustained Release Capsules[J]. Journal of China Pharmaceutical University, 1999, (5): 346-349.
    [7]The Factors Influencing Nimodipine Release from Hydroxypropyl Methylcellulose Matrix Tablet[J]. Journal of China Pharmaceutical University, 1998, (6): 418-421.
    [8]Improved Process of Nimodipine[J]. Journal of China Pharmaceutical University, 1998, (3): 82-83.
    [9]Study on Penetration Enhancers for Nimodipine[J]. Journal of China Pharmaceutical University, 1994, (3): 149-152.
    [10]CORRELATION BETWEEN THE ABSORPTION IN VIVO AND THE RELEASE IN VITRO OF TWO CONTROLLED-RELEASE TABLETS OF AMINOPHYLLINE[J]. Journal of China Pharmaceutical University, 1986, (1): 18-23.

Catalog

    Article views (1115) PDF downloads (1654) Cited by()

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return