Abstract
In this study, we attempted to prepare carbamazepine (CBZ) cocrystal through the solution method in ethanol-water solvent mixture (volume ratio 1:1) and polyvinyl pyrrolidone (PVP) solution. Nicotinamide (NIC) and saccharin (SAC) were selected as cocrystal coformers. Cocrystal screening products were characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Powder X-ray Diffraction (PXRD) techniques. Characterization results show that in ethanol-water solvent mixture, pure CBZ-NIC cocrystal can be prepared, while CBZ-SAC cocrystal cannot be obtained. The addition of PVP can inhibit CBZ-NIC cocrystal formation and facilitate CBZ-SAC cocrystal formation.
Highlights
Pharmaceutical cocrystal is a crystalline material with two components present in definite stoichimetric amounts [1]
active pharmaceutical ingredient (API) and cocrystal coformer (CCF) are combined to form cocrystal through intermolecular interactions such as hydrogen bond (H-bond), π-π stacking force, van der Waals contact forces [2,3,4]
In order to study the effect of polyvinyl pyrrolidone (PVP) on cocrystal formation, we attempted to prepare CBZ-NIC
Summary
Pharmaceutical cocrystal is a crystalline material with two components present in definite stoichimetric amounts [1]. Among all the physicochemical properties, solubility and dissolution behavior are important properties which take great role in bioavailability of drugs [7]. A pharmaceutical cocrystal can be prepared with the intention to improve solubility behavior of an API without affecting its intrinsic molecular structure. For biopharmaceutics classification system class II (BCS II) drugs, which have high permeability and low solubility, pharmaceutical cocrystal has becoming a popular method to improve its solubility [8]. Two main methods for cocrystal preparation are the grinding method and the solution method. It is difficult to obtain cocrystal product with high purity and good quality using the grinding method [15,16,17]. The solution method has been applied in many cases to prepare cocrystal [18,19]. The ideal solvent for the solution cocrystallization process is one in which API and CCF
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