Molecular Dynamics and Physical Stability of Amorphous Nimesulide Drug and Its Binary Drug-Polymer Systems

作者：Knapik J; Wojnarowska Z; Grzybowska K; Tajber L; Mesallati H; Paluch K J; Paluch M

来源：Molecular Pharmaceutics, 2016, 13(6): 1937-1946.

DOI：10.1021/acs.molpharmaceut.6b00115

• amorphous drug
• physical stability
• molecular dynamics
• nimesulide
• drug-polymer system
• PVP
• Soluplus
• inulin

In this article we study the effectiveness of three well-known polymers: inulin, Soluplus, and PVP in stabilizing the amorphous form of nimesulide (NMS) drug. The recrystallization tendency of pure drug as well as measured drug-polymer systems were examined at isothermal conditions by broadband dielectric spectroscopy (BDS) and at nonisothermal 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 min. We found that this time can be prolonged to 40 years after adding 20% w/w PVP to NMS. This polymer proved to be the best NMS stabilizer, while the worst stabilization effect was exhibited by inulin. Additionally, our DSC, BDS, and FTIR studies indicate that for suppression of NMS recrystallization in the NMS-PVP system, the two mechanisms are responsible: the polymeric steric hindrances and the antiplastization effect exerted by the excipient.

• 出版日期2016-6