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ZHOU Shengyan, ZHANG Bowen, WEI Yuanfeng, QIAN Shuai, ZHANG Jianjun, GAO Yuan. Enhanced dissolution and oral bioavailability of baicalein by cocrystallization[J]. Journal of China Pharmaceutical University, 2018, 49(6): 682-688. DOI: 10.11665/j.issn.1000-5048.20180607
Citation: ZHOU Shengyan, ZHANG Bowen, WEI Yuanfeng, QIAN Shuai, ZHANG Jianjun, GAO Yuan. Enhanced dissolution and oral bioavailability of baicalein by cocrystallization[J]. Journal of China Pharmaceutical University, 2018, 49(6): 682-688. DOI: 10.11665/j.issn.1000-5048.20180607
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Enhanced dissolution and oral bioavailability of baicalein by cocrystallization

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  • Baicalein(BE), a natural flavonoid mainly extracted from Radix Scutellaria, has comprehensive pharmacological actions such as anti-inflammation, anti-virus and anti-cancer activities. It belongs to BCS class II compound with relatively low oral bioavailability. The current study aims to improve its aqueous solubility and dissolution and hence to enhance its oral absorption by cocrystallization technique. Slurry crystallization method was employed to prepare baicalein cocrystal with co-former caffeine(CA), followed by physicochemical characterizations with DSC, XRPD and FTIR. Compared to BE and physical mixture of BE and CA, BE-CA cocrystal had a significantly higher dissolution of BE. In addition, in comparison to BE, this cocrystal achieved reduced time to peak(tmax)as well as significantly higher peak plasma concentrations(cmax)and area under the curve(AUCs)for both BE and its active metabolite baicalin(BI)in rats, suggesting enhanced the oral bioavailability of BE.
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  • [1]
    Gao Y,Zu H,Zhang JJ.Pharmaceutical Cocrystals[J].Prog Chem(化学进展),2010,22(5):829-836.
    [2]
    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.
    [3]
    Gao Y,Gao J,Liu Z,et al.Coformer selection based on degradation pathway of drugs:a case study of adefovir dipivoxil-saccharin and adefovir dipivoxil-nicotinamide cocrystals[J].Int J Pharm,2012,438(1/2):327-335.
    [4]
    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.
    [5]
    Yu B,Ding JW,Wang XA.Progress of EntrestoTM in the treatment of heart failure[J].Hainan Med J(海南医学),2018,29(10):1420-1422.
    [6]
    Zhang JJ,Zhang L,Qian S,et al.Preparation method of ibuprofen-nicotinamide eutectic through solvent:CN,106632024A[P].2017-05-10[2018-08-01] .
    [7]
    Zhang JJ,Xia DR,Xu JJ,et al.Naringenin isonicotinamide co-crystal:CN,104817526A[P].2015-04-10[2018-08-01] .
    [8]
    Li-Weber M.New therapeutic aspects of flavones:the anticancer properties of Scutellaria and its main active constituents wogonin,baicalein and baicalin[J].Cancer Treat Rev,2009,35(1):57-68.
    [9]
    Wang Q,Wang YT,Pu SP,et al.Zinc coupling potentiates anti-HIV-1 activity of baicalin[J].Biochem Biophys Res Commun,2004,324(2):605-610.
    [10]
    Kubo M,Kimura Y,Odani T,et al.Studies on Scutellariae radix.Part II:the antibacterial substance[J].Planta Med,1981,43(2):194-201.
    [11]
    Lee H,Bae S,Kim K,et al.Beta-catenin mediates the anti-adipogenic effect of baicalin[J].Biochem Biophys Res Commun,2010,398(4):741-746.
    [12]
    Shao ZH,Vanden Hoek TL,Qin YM,et al.Baicalein attenuates oxidant stress in cardiomyocytes[J].Am J Physiol Heart C,2002,282(3):H999-H1006.
    [13]
    Evers DL,Chao CF,Wang X,et al.Human cytomegalovirus-inhibitory flavonoids:studies on antiviral activity and mechanism of action[J].Antiviral Res,2005,68(3):124-134.
    [14]
    Fan YJ,Song YT,Zhang YQ,et al.Effect of solvents on the formation thermodynamics of baicalein-nicotinamide cocrystals[J].J China Pharm Univ(中国药科大学学报),2016,47(4):437-441.
    [15]
    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.
    [16]
    Lagarde D,Batejat D,Sicard B,et al.Slow-release caffeine:a new response to the effects of a limited sleep deprivation[J].Sleep,2000,23(5):651-661.
    [17]
    Xu JJ,Wei YF,Qian S,et al.Preparation of myricetin-caffeine cocrystal and its single crystal analysis[J].J Chin Pharm Univ(中国药科大学学报),2016,47(3):324-328.
    [18]
    Zhang J,Liu D,Huang Y,et al.Biopharmaceutics classification and intestinal absorption study of apigenin[J].Int J Pharm,2012,436(1/2):311-317.
    [19]
    Karan M,Chadha K,Chadha R,et al.Cocrystal of caffeine with propionic acid:preliminary characterization and stability evaluation[J].J Pharm Res,2012,5(4):2022-2026.
    [20]
    Markovic ZS,Dimitric-Markovic JM,Milenkovic D,et al.Structural and electronic features of baicalein and its radicals[J].Monatsh Chem,2011,142(2):145-152.
    [21]
    Gunasekaran S,Sankari G,Ponnusamy S.Vibrational spectral investigation on xanthine and its derivatives-theophylline,caffeine and theobromine[J].Spectrochim Acta A,2005,61(1/2):117-127.
    [22]
    He X,Pei L,Tong HH,et al.Comparison of spray freeze drying and the solvent evaporation method for preparing solid dispersions of baicalein with Pluronic F68 to improve dissolution and oral bioavailability[J].AAPS PharmSciTech,2011,12(1):104-113.
    [23]
    Kesimli B,Topacli A,Topacli C.An interaction of caffeine and sulfamethoxazole:studied by IR spectroscopy and PM3 method[J].J Mol Struct,2003,645(2/3):199-204.
    [24]
    Zhang JJ,Lv HX,Jiang K,et al.Enhanced bioavailability after oral and pulmonary administration of baicalein nanocrystal[J].Int J Pharm,2011,420(1):180-188.
    [25]
    FDA.Guidance for Industry:Dissolution Testing of Immediate Release Solid Oral Dosage Forms[S].1997:1-11.
    [26]
    Khan KA.The concept of dissolution efficiency[J].J Pharm Pharmacol,1975,27(1):48-49.
    [27]
    Gong MT,Yu LF,Chen QH,et al.Pharmacokinetic studies of baicalein and baicalin after oral administration of baicalein to rats[J].Chin Trand Herb Drugs(中草药),2009,40(3):392-394.
    [28]
    Guo XY,Yang L,Chen Y,et al.Comparison of pharmacokinetics of baicalein and baicalin in rats[J].Chin Pharm J(中国药学杂志),2008,43(7):524-526.
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