Dai, Xia-Lin published the artcileSolubility and Permeability Improvement of Allopurinol by Cocrystallization, Category: amides-buliding-blocks, the publication is Crystal Growth & Design (2020), 20(8), 5160-5168, database is CAplus.
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 physicochem. 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, IR 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, resp. These results suggest that ALP-PIP and ALP-24DHBZA have the potential to be developed as new, more efficient formulations of allopurinol. Three cocrystals of allopurinol (ALP) with isonicotinamide (ALP-INA), piperazine (ALP-PIP), and 2,4-dihydroxybenzoic acid (ALP-24DHBZA) were synthesized, and ALP-PIP and ALP-24DHBZA resp. showed significant improvement in membrane permeability and dissolution behaviors in comparison to the original ALP.
Crystal Growth & Design published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Category: amides-buliding-blocks.
Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics