The aim of this study was to evaluate the influence of three chemically diverse polymers of Hydroxypropylemthylcellulose acetate succinate (HPMCAS), Polyvinylpyrrolidone (PVP) and PolyEthylene Glycol (PEG) on the phase transformation of three carbamazepine (CBZ) cocrystals of carbamazepine-nicotinamide (CBZ-NIC), carbamazepine-saccharin (CBZ-SAC) and carbamazepine-cinnamic acid (CBZ-CIN) in solution and tablet based formulations. Ba sed on the solubility and powder dissolution studies, it demonstrates that cocrystals can be easily formulated through a simple solution formulation or powder formulation to generate supersaturated concentrations and faster dissolution rates to overcome th ose drugs with solubility and/or dissolution limited bioavailability. However, a polymer based CBZ cocrystal tablet formulation has not shown any advantage of an improved CBZ release rate compared with the formulation of CBZ III or physical mixtures of CBZ III and coformers. This is contradictive to the solution behaviours of CBZ cocrystals in the solubility and powder dissolution tests because crystallization of the stable solid form of CBZ dihydrate (CBZ DH) within the tablet has taken place, leading to a reduced drug release rate and incomplete release. The mechanism of a polymer inhibition effect on the drug precipitation in solution has been elucidated through investigating the molecular interactions among CBZ, coformers and polymers in solution using infrared spectroscopy. Finally the formulation strategy has been proposed to capture the significant advantage of cocrystals.
The aim of the study was to investigate the effects of the loading factors, i.e., the initial drug loading concentration and the ratio of the drug to carriers, on the in vitro pharmaceutical performance of drug-loaded mesoporous systems. Ibuprofen (IBU) was used as a model drug, and two non-ordered mesoporous materials of commercial silica Syloid® 244FP (S244FP) and Neusilin® US2 (NS2) were selected in the study. The IBU-loaded mesoporous samples were prepared by a solvent immersion method with a rotary evaporation drying technique and characterized by polarized light microscopy (PLM), Fourier transform infrared (FTIR) spectroscopy, X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). Dissolution experiments were performed in simulated gastric media at 37 °C under non-sink conditions. The concentration of IBU in solution was determined by HPLC. The study showed that the dissolution rate of IBU can be improved significantly using the mesoporous S224FP carriers due to the conversion of crystalline IBU into the amorphous form. Both of the loading factors affected the IBU dissolution kinetics. Due to the molecular interaction between the IBU and NS2 carriers, the loading factors had little effects on the drug release kinetics with incomplete drug desorption recovery and insignificant dissolution enhancement. Care and extensive evaluation must therefore be taken when mesoporous materials are chosen as carrier delivery systems.
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