Abstract:
:Crystallization of polymorphs still has a touch of art, as even prior observations of polymorphs do not guarantee their crystallization. However, once crystals of various polymorphs have been obtained, their relative stabilities can be established with a straightforward thermodynamic approach even if the conclusion will depend on the quality of the experimental data. Rotigotine is an active pharmaceutical ingredient, which has suffered the same setback as Ritonavir: a sudden appearance of a more stable crystalline polymorph than the one used for the formulation. Although the cause of the defect in the formulation was quickly established, the interpretation of the phase behavior of rotigotine has been lacking in clarity. In the present paper, data published in the patents resulting from the discovery of the new polymorph have been used to establish the pressure-temperature phase diagram of the two known solid forms of rotigotine. The analysis clearly demonstrates that form II is the stable solid phase and form I is metastable in the entire pressure-temperature domain: form I is overall monotropic in relation to form II. Thus, it was a sensible decision of European Medicines Agency to ask for a reformulation, as the first formulation was metastable even if crystallization appeared to be very slow.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Rietveld IB,Céolin Rdoi
10.1002/jps.24626subject
Has Abstractpub_date
2015-12-01 00:00:00pages
4117-4122issue
12eissn
0022-3549issn
1520-6017pii
S0022-3549(15)00058-1journal_volume
104pub_type
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