A reliable crystallization process for the preparation of agomelatine form I

XU Yinrong; SHENG Xiaoxia

doi:10.11665/j.issn.1000-5048.20160208

Journal of China Pharmaceutical University > 2016 > 47(2): 171-175. > DOI: 10.11665/j.issn.1000-5048.20160208

XU Yinrong, SHENG Xiaoxia. A reliable crystallization process for the preparation of agomelatine form I[J]. Journal of China Pharmaceutical University, 2016, 47(2): 171-175. DOI: 10.11665/j.issn.1000-5048.20160208

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A reliable crystallization process for the preparation of agomelatine form I

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A reliable crystallization process was developed for the preparation of stable agomelatine form I. This antisolvent crystallization was explored in ethanol-n-heptane by adding PVP and ethanol-water system by adding HPMC, respectively. Factors such as solvent, polymer, concentration of polymer, and solvent ratio were subjected to detailed examination. Accelerated and long-term stability observations indicates that the presence of polymeric additives in the crystallization process enhances the stability of agomelatine form I.
- agomelatine form I,
- polymer,
- stability,
- preparation,
- PVP,
- HPMC

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[1]	Song L,Wang M,Wen SD,et al.Determination of agomelatine in human plasma by LC-MS/MS:application to a pharmacokinetic study in Chinese volunteers[J].J China Pharm Univ(中国药科大学学报),2014,45(6):698-702.
[2]	Zhu JQ,Wei WT,Dai Y,et al.Study on the polymorphs of agomelatine[J].Chin J Med Chem(中国药物化学杂志),2012,22(6):495-498.
[3]	Sun LL,Zhou QG,Zhang ZJ.Study on the polymorphism of agomelatine[J].West China J Pharm Sci(华西药学杂志),2012,27(5):533-536.
[4]	Qin LH,Yu H.Effect of water-soluble polymers on the inhibition of osthole crystallization[J].Acta Pharm Sin(药学学报),2010,45(12):1559-1564.
[5]	Konno H1,Handa T,Alonzo DE,et al.Effect of polymer type on the dissolution profile of amorphous solid dispersion scontaining felodipine[J].Eur J Pharm Biopharm,2008,70(2):493-499.
[6]	Schram CJ,Beaudoin SP,Taylor LS.Impact of polymer conformation on the crystal growth inhibition of a poorly water-soluble drug in aqueous solution[J].Langmuir,2015,31(1):171-179.
[7]	Raina SA,Alonzo DE,Zhang GG,et al.Impact of polymers on the crystallization and phase transition kinetics of amorphous nifedipine during dissolution in aqueous media[J].Mol Pharm,2014,11(10):3565-3576.
[8]	Sarode AL,Wang P,Obara S,et al.Supersaturation,nucleation,and crystal growth during single-andbiphasic dissolution of amorphous solid dispersions:polymer effectsand implications for oral bioavailability enhancement of poorly water soluble drugs[J].Eur J Pharm Biopharm,2014,86(3):351-360.
[9]	Ratiopharm Gmbh.Solid agomelatine in non-crystalline form:WO,2012130837A1[P].2012-03-27[2015-04-23] .
[10]	Zhejiang Huahai Pharm Co.,LTD.Preparation of agomelatine solid preparations:CN,201210381283.X[P].2012-09-28[2015-04-23] .

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A reliable crystallization process for the preparation of agomelatine form I

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