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Particle engineering/different film approaches for earlier absorption of meloxicam.

Authors :
Farid M
El-Setouhy DA
El-Nabarawi MA
El-Bayomi T
Source :
Drug delivery [Drug Deliv] 2016 Sep; Vol. 23 (7), pp. 2309-2317. Date of Electronic Publication: 2014 Nov 28.
Publication Year :
2016

Abstract

Meloxicam (Mel) is a non-steroidal potent anti-inflammatory drug with effective analgesic effect for various situations; e.g. postoperative pain. The early systemic exposure to Mel and hence the rapid onset of pharmacological action is limited by its poor water solubility; a situation which may be more pronounced during acute pain episode because of reduced gastric motility that affects disintegration and dissolution of solid dosage forms. To overcome delayed absorption of Mel, improvement in the dissolution behavior of Mel is essential. Firstly, Mel spherical crystalline agglomerates (SCA) were prepared. Secondly, selected Mel SCA were integrated into intraoral fast disintegrating (OF) and edible (EF) films, they possess larger surface area that leads to rapid disintegration and release of the drug into the oral cavity within seconds and hence a rapid onset of action could be achieved. Stability study of formulations resulting in faster and higher extent of dissolution and suitable mechanical properties (G3 and G12) revealed their physical and chemical stability after three months of storage under different conditions. Both G3 and G12 successfully offered rapid absorption rate and accordingly an earlier systemic exposure to Mel compared to Mobic tablets as revealed by significantly earlier T <subscript>max</subscript> and higher AUC <subscript>0-0.5h</subscript> and AUC <subscript>0-4h</subscript> . T <subscript>max</subscript> following G3 fast disintegrating film administration was comparable to that reported following Mel parenteral administration but avoiding patient inconvenience. Both films may be suitable alternative to conventional oral and intramuscular Mel especially when earlier onset of action is required (in acute conditions).

Details

Language :
English
ISSN :
1521-0464
Volume :
23
Issue :
7
Database :
MEDLINE
Journal :
Drug delivery
Publication Type :
Academic Journal
Accession number :
25431841
Full Text :
https://doi.org/10.3109/10717544.2014.982262