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A cikk állandó MOB linkje:
http://mob.gyemszi.hu/detailsperm.jsp?PERMID=151697
MOB:2021/2
Szerzők:Kiss Tamás; Katona Gábor; Ambrus Rita
Tárgyszavak:PARKINSON-KÓR; LEVODOPA; KRISTÁLYOSODÁS
Folyóirat:Acta Pharmaceutica Hungarica - 2021. 91. évf. 2. sz.
[https://www.aph-hsps.hu/acta/index.php/aph/issue/archive]


  Crystallization and physicochemical investigation of melevodopa hydrochloride, a commercially available antiparkinsonian active substance / Tamás Kiss, Gábor Katona, Rita Ambrus
  Bibliogr.: p. 52. - Abstr. eng. - DOI: https://doi.org/10.33892/aph.2021.91.45-52
  In: Acta Pharmaceutica Hungarica. - ISSN 0001-6659. - 2021. 91. évf. 2. sz., p. 45-52. : ill.


Abstract: In this work, the levodopa methyl ester was crystallized from different solvents and its physicochemical proper ties were explored. This active pharmaceutical ingredient (API) is commercially available as an effervescent tablet in Italy. The crystallization methods were solvent evaporation from different solvents (water, ethanol, methanol) and crystalliza tion by adding an antisolvent. These methods led to the same product which had the same different X­ray powder diffrac togram that was different from the diffractogram of LDME­I. According to the hot­stage microscopy and differential scan ning calorimetry (DSC), the melting point was remarkably decreased, however, above the melting point, the melt tended to recrystallize to the LDME­I which was shown by an exothermic peak on the DSC curve. This was verified by an additional test during which the API was heated to 145 °C, thereafter the diffractogram matched perfectly with the LDME­I. These results indicate the presumable formation of a new polymorph. During the crystallization, the LDME did not degrade ac cording to the high-performance liquid chromatography. Besides the recrystallization kinetics of the amorphous form was also followed, the activation energy of recrystallization was 85.3 kJ/mol, the diffractogram of recrystallization was the same as in the case of the crystallized products.  Kulcsszavak: melevodopa hydrochloride, crystallization, potential polymorph, melting point, X-ray powder diffractometry