Solubility and Permeability Improvement of Allopurinol by Cocrystallization
Posted on 2020-06-25 - 18:05
Allopurinol is a
xanthine oxidase inhibitor with poor solubility
and permeability, which severely limit its drug absorption following
the administration of some dosage forms, such as tablets and rectal
suppositories. To improve the physicochemical properties, three cocrystals
of allopurinol with isonicotinamide (ALP-INA), piperazine
(ALP-PIP), and 2,4-dihydroxybenzoic acid (ALP-24DHBZA) were successfully prepared by a slurry or liquid-assisted grinding
method. The obtained cocrystal materials were characterized by single-crystal
X-ray diffraction, powder X-ray diffraction, infrared spectroscopy,
differential scanning calorimetry, and thermogravimetric analyses
and were subjected to dynamic vapor sorption, dissolution, and membrane
permeability studies. ALP-INA showed solubility and diffusion/membrane
permeability similar to those of the parent drug. In contrast, ALP-PIP exhibited improved diffusion/membrane permeability,
and ALP-24DHBZA exhibited improved dissolution behavior,
respectively. These results suggest that ALP-PIP and ALP-24DHBZA have the potential to be developed as new, more
efficient formulations of allopurinol.
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Dai, Xia-Lin; Yao, Jia; Wu, Chao; Deng, Jun-Hui; Mo, Yong-Hui; Lu, Tong-Bu; et al. (2020). Solubility and Permeability Improvement of Allopurinol by Cocrystallization. ACS Publications. Collection. https://doi.org/10.1021/acs.cgd.0c00326