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Research articles

ScienceAsia 45 (2019): 28-35 |doi: 10.2306/scienceasia1513-1874.2019.45.028

Characterization of donepezil prepared by cogrinding with salicylic acid and p-aminobenzoic acid

Weenawan Somphon*, Sirimol Makatan

ABSTRACT:     Two systems for the formation of cocrystals of donepezil were investigated using donepezil hydrochloride and donepezil solvate with salicylic acid and p-aminobenzoic acid. The donepezil solvate was prepared through an acidbase reaction between a hydrochloride salt and a base in methanol. Donepezil HCl (DH) and the solvate with salicylic acid and p-aminobenzoic acid (PABA) at 1:1 molar ratios were prepared using the cogrinding method. Cocrystals were characterized using attenuated total reflection-FTIR spectroscopy (ATR-FTIR), nuclear magnetic resonance spectroscopy (13C and 1H NMR), Powder X-ray diffraction, and differential scanning calorimetry. These results indicate that the cogrinding process could induce cocrystal formation in donepezil systems through a simple process that allows for rapid screening of cocrystals of donepezil.

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a Department of Chemistry, Faculty of Liberal Arts and Science, Kasetsart University, Kamphaeng Saen Campus, Nakhon Pathom 73140 Thailand

* Corresponding author, E-mail: faaswnw@ku.ac.th

Received 18 Jan 2018, Accepted 16 Feb 2019