Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
Vol. 16, No. 2, 2017, pp. 297-303
Bioline Code: pr17039
Full paper language: English
Document type: Research Article
Document available free of charge
Tropical Journal of Pharmaceutical Research, Vol. 16, No. 2, 2017, pp. 297-303
© Copyright 2017 - Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria.
Simvastatin-nicotinamide co-crystal: design, preparation and preliminary characterization|
Sopyan, Iyan; Fudholi, Achmad; Muchtaridi, Muchtaridi & Sari, Ika Puspita
Purpose: To improve the solubility of simvastatin (SV) by co-crystallization using nicotinamide (Nic) as
co-crystal agent (co-former).
Methods: In silico molecular modeling of Nic counter to SV were investigated using Auto Dock 4.2. Co-crystal
of Nic-SV was obtained by solvent evaporation (SE) using an equimolar ratio of Nic and SV. Co-crystal
of SV-Nic was evaluated by scanning electron microscopy (SEM), saturated solubility, intrinsic
dissolution, x-ray powder diffraction (XRPD), differential scanning calorimetric (DSC), infrared
spectrophotometry (FT-IR), binary phase diagram, and for stability at 40 oC and relative humidity (RH)
75% in one month.
Results: In silico results showed that the interaction of Nic with SV took place through hydrogen
bonding as the synthon agent. The solubility and intrinsic dissolution properties of the co-crystal
improved significantly compared to pure SV. Characterization of the co-crystal SV: Nic (1: 1) by SEM,
XRPD, DSC, FT-IR, and binary phase diagram indicate the formation of a new solid phase that was
different from either SV or Nic. Furthermore, the cocrystal of SV: Nic remained stable for one month.
Conclusion: Co-crystallization using Nic has the potential to enhance drug solubility, intrinsic
dissolution, and the stability of solution.
Simvastatin; Co-crystal; Nicotinamide; Solubility; Dissolution
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