Improving the solubility and bioavailability of anti-hepatitis B drug PEC via PEC–fumaric acid cocrystal

Abstract

A cocrystal of PEC with fumaric acid (FUA) (PEC–FUA, 1 : 1) was successfully obtained and characterized. The mean AUC0–24 h of the cocrystal is about 4.2 times that of free PEC.

Mechanosynthesis of Stable Salt Hydrates of Allopurinol with Enhanced Dissolution, Diffusion, and Pharmacokinetics

“…Solubility and dissolution play a vital role in determining the absorption and bioavailability of a drug. ,− ALO exhibits poor aqueous solubility. The dense packing of ALO molecules in its crystal structure, strong hydrogen-bonded dimer/hexamer involving pyrimidine/pyrazole ring “N” atoms, and exceptionally high melting point are the probable reason for its poor solubility.…”

Novel pharmaceutical salts of cephalexin with organic counterions: structural analysis and properties

“…The poor physicochemical properties of APIs which prohibit their utilization in formulation development are nonnegligible disadvantages in the pharmaceutical industry. [1][2][3][4][5][6] In recent years, crystal engineering facilitating the design and synthesis of novel solid forms of APIs with optimized physicochemical properties has emerged into the elds of the pharmaceutical industry with paramount importance in the process of drug development. [7][8][9][10][11][12] Such various solid forms of APIs including amorphous, polymorphs, hydrates, solvates, cocrystals and salts formulation can enable the improvement of solubility, dissolution, stability and bioavailability, without affecting the pharmacological activities of APIs.…”