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Molecular dynamics and physical stability of amorphous nimesulide drug and its binary drug-polymer systems
Knapik, J. Wojnarowska, Z. Grzybowska, K. Tajber, L. Mesallati, H. Paluch, Krzysztof J. Paluch, M.
Knapik, J.
Wojnarowska, Z.
Grzybowska, K.
Tajber, L.
Mesallati, H.
Paluch, Krzysztof J.
Paluch, M.
Publication Date
2016
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© 2016 ACS. This document is the Accepted Manuscript version of a Published Work that appeared in final form in Molecular Pharmaceutics, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/acs.molpharmaceut.6b00115
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2016-05-05
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Abstract
In this paper we study the effectiveness of three well known polymers: inulin, Soluplus and PVP in stabilizing amorphous form of nimesulide (NMS) drug. The re-crystallization tendency of pure drug as well as measured drug-polymer systems were examined at isothermal conditions by using broadband dielectric spectroscopy (BDS), and at non-isothermal conditions by differential scanning calorimetry (DSC). Our investigation has shown that the crystallization half-life time of pure NMS at 328 K is equal to 33 minutes. We found that this time can be prolonged to 40 years after adding to NMS 20% of PVP polymer. This polymer proved to be the best NMS’s stabilizer, while the worst stabilization effect was found after adding the inulin to NMS. Additionally, our DSC, BDS and FTIR studies indicate that for suppression of NMS’s re-crystallization in NMS-PVP system, the two mechanisms are responsible: the polymeric steric hindrances as well as the antiplastization effect excerted by the excipient.
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Accepted manuscript
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Knapik J, Wojnarowska Z, Grzybowska K, Tajber L, Mesallati H, Paluch KJ and Paluch M (2016) Molecular dynamics and physical stability of amorphous nimesulide drug and its binary drug-polymer systems. Molecular Pharmaceutics. 13(6): 1937–1946.
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Article