Anti-inflammatory, antinociceptive and ulcerogenic properties of indomethacin tablets based on solidified reverse micellar solution (SRMS)

Abstract

The aim of the present study was to evaluate in vivo the anti-inflammatory, antinociceptive and ulcerogenic properties of indomethacin tablets based on solidified reverse micellar solution (SRMS). SRMS consisting of mixtures of phospholipid (Phospholipon® 90H) and triglyceride (Softisan® 154) were prepared in the ratios of 1:1, 2:1 and 1:2, respectively. SRMS based tablets containing 75 mg of indomethacin each were prepared using validated plastic mould. The physicochemical properties of the tablet formulations were studied using both official and unofficial tests. Anti-inflammatory, analgesic/antinociceptive and ulcerogenic properties of indomethacin tablets based on SRMS were studied. The results showed that the physicochemical properties of the tablet formulations were significantly affected by the composition/ratio of the lipid matrix used. The softening time in SIF ranged from 53.7 ± 0.5 to 102.6 ± 0.5 min. Results of analgesic/antinociceptive properties showed that indomethacin tablets formulated with the SRMS 1:1 had an increase in pain reaction time at 7 h significantly (p < 0.05) different from the results exhibited by tablets formulated with the lipid matrices, SRMS 1:2 and 2:1 and the reference, which showed a decrease in pain reaction time at 7 h. Indomethacin tablets based on SRMS had good anti-inflammatory properties and also inhibited the ulcerogenicity of indomethacin by 70 to 80%. Therefore, indomethacin tablets based on SRMS could be used for improved oral bioavailability of indomethacin and to enhance patient’s compliance due to inhibition of gastric irritation effect of this drug. Key words: Non steroidal anti-inflammatory drugs (NSAIDS), solidified reverse micellar solutions (SRMS), tablets, ulcerogenicity, antinociception, lipids.