Crystallization of progesterone polymorphs using polymer-induced heteronucleation (PIHn) method |
| |
Authors: | Andrea Mariela Araya-Sibaja Valdir Soldi Carlos Eduardo Maduro Campos Simone Gonçalves Cardoso |
| |
Affiliation: | 1. Programa de Pós-Gradua??o em Farmácia, Universidade Federal de Santa Catarina, Florianópolis, Brasil,;2. Escuela de Química, Universidad de Costa Rica, San José, Costa Rica,;3. Grupo de estudo em materiais poliméricos (POLIMAT), Departamento de Química, Universidade Federal de Santa Catarina, Florianópolis, Brasil,;4. Programa de Pós-Gradua??o em Física, Universidade Federal de Santa Catarina, Florianópolis, Brasil, and;5. Programa de Pós-Gradua??o em Farmácia, Universidade Federal de Santa Catarina, Florianópolis, Brasil, |
| |
Abstract: | Progesterone is a natural hormone steroid used in humans for several treatments and in livestock for artificial insemination, which exhibits two polymorphic forms at ambient conditions: form 1 and form 2. Form 2 is metastable and more soluble than form 1; however, it is not suitable to use as powder raw material because it transforms into form 1 by the effects of grinding. A polymorphic screening of progesterone based on polymer-induced heteronucleation method was performed as an alternative to prepare the metastable form. Polyvinyl alcohol, hydroxypropyl methylcellulose (HPMC), dextran, gelatin, polyisoprene (PI) and acrylonitrile-butadiene (NBR) copolymer were used. Crystals were prepared from 0.5, 10 and 40?mg/mL solutions in acetone at room temperature by solvent evaporation. The samples were characterized by X-ray powder diffraction, differential scanning calorimetry (DSC), scanning electron microcopy and attenuated total reflectance infrared Fourier transform spectroscopy. Form 1 was nucleated from 40?mg/mL solutions on the six polymers and from 10?mg/mL solutions on PI and NBR. The mixture of form 1 and form 2 was obtained from 10?mg/mL solution on HPMC, dextran and gelatin and from 0.5?mg/mL solution crystallizations. Therefore, the polymeric devices, which crystallized the metastable and more soluble polymorph (2) of progesterone, would be a promissory alternative for the pharmaceutical applications. |
| |
Keywords: | Growth from solutions polymer-induced heteronucleation polymer templating polymorph screening preferred orientation progesterone |
|
|