Pharmaceutical
cocrystals offer a promising strategy to increase
the solubility and dissolution rate of poorly soluble drugs. However,
their manufacturing process requires a large quantity of solvents.
The present study aimed to produce cocrystals by a solvent-free hot
melt extrusion (HME) method to improve their solubility and dissolution
rate. Aripiprazole (ARP) and adipic acid (ADP) were used as a weakly
basic drug and acidic coformer, respectively. The processability of
a plain ARP-ADP physical mixture (PM) compared with a PM with 5% Soluplus
polymeric matrix (SOL) was investigated. Incorporating 5% SOL into
the ARP-ADP blend reduced the processing torque and improved processability.
The effects of temperature and screw speed on the formation of cocrystals
were studied, and cocrystals were characterized by differential scanning
calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy,
nuclear magnetic resonance (NMR) spectroscopy, powder X-ray diffraction
(PXRD), scanning electron microscopy (SEM), and hot-stage microscopy.
FTIR spectra revealed non-covalent interaction between ARP and ADP,
which was confirmed by NMR spectra. Similarly, PXRD data exhibited
characteristic peaks confirming the formation of new crystalline material.
Further, the results indicated that cocrystals demonstrated higher
dissolution rates and improved compressibility, as well as enhanced
flow characteristics compared with pure ARP, suggesting their suitability
in the development of solid dosage forms.
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