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Papers of the Week

Papers: 30 Jul 2022 - 5 Aug 2022

Pharmacology/Drug Development

2022 Jul 26

Int J Pharm

A novel soluble lornoxicam-sodium chelate monohydrate with improved plasticity and tabletability.


Chen H, Zhang J, Qiao Q, Hu E, Wei Y, Pang Z, Gao Y, Qian S, Zhang J, Heng W
Int J Pharm. 2022 Jul 26:122060.
PMID: 35905932.


Lornoxicam (LOR), a BCS Ⅱ nonsteroidal anti-inflammatory drug, has been clinically utilized for moderate to severe acute pain management. However, it has poor water solubility and insufficient tabletability, leading to erratic absorption and challenge in tablet processability. This study reported a novel solid state of LOR (i.e., LOR sodium chelate monohydrate, LOR-Na·HO) with significantly improved solubility, dissolution rate and tabletability. The prepared chelate (CCDC No.: 2125157) contains LOR, Na, and HO in a molar ratio of 1:1:1, where Na ions bridged with O(5) of amide group, and N(2) of pyridine group on LOR, as well as O(4) on HO through coordination bonds. LOR-Na·HO displayed a superior dissolution rate (5∼465 folds) than commercial LOR due to its increased wettability (contact angle: 74.5° vs 85.6°) and lower solvation free energy (∼2-fold). In addition, the significant improvement in tabletability was caused by high plasticity and deformability, which was attributed to its special interlayer gliding with weak bonding interactions across layers but strong coordination bonding interactions within layers. The novel LOR-Na·HO with significantly enhanced pharmaceutical performance offers a promising strategy for further product development.