OPTIMIZATION OF ACECLOFENAC ONCE DAILY MATRIX TABLETS: IN-VITRO AND IN-VIVO STUDIES

Abstract

Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) indicated for
symptomatic treatment of pain and inflammation. The short biological half-life (4
h) and dosing frequency make aceclofenac a suitable candidate for sustained
release formulations. Sustained release matrix tablets of aceclofenac with
Eudragit® RSPO and Eudragit® RLPO were prepared using three techniques;
direct compression, wet granulation and solid dispersion. The most optimum
matrix formula was manipulated by addition of an immediate release layer for
prompt release of the drug. All tablets were evaluated regarding their physical
properties and in-vitro release over 24 hours. All the tablets were found within
the permissible limits for various physical parameters. In-vitro release studies
revealed that Eudragit RSPO retarded the release more than Eudragit RLPO and
solid dispersion was the most suitable preparation technique. Formulation F5
was selected for further optimization by addition of fast release layer. The double
layer tablet (F19) was successful in prolonging drug release up to 24 hours.
Pharmacokinetic studies in albino rabbits were conducted for the optimized
formula (Registration No. PI-260). The results of pharmacokinetic studies showed
that F19 exhibited longer MRT when compared to the commercial brand of
aceclofenac immediate release tablet (Bristaflam®), demonstrating the sustained
release properties of F19.