Investigation Of Meloxicam Gel

Meloxicam is a cyclooxygenase-2 selective inhibitor when tested in vitro, Then meloxicam transdermal emulgel was prepared in order to reduce the adverse effects after oral administration, and promote drug therapeutic effect and patient compliance.In present study, we synthesized six complexes of meloxicam(ML) with adding ethanolamine (EA), diethanolamine(DEA), triethanolamine(TEA) and N-(2-hydroxyethyl)-piperidine (D-HEPP), diethylamine (DETA), triethylamine (TETA),and the complex formation was proved by DSC and NMR studies. These results suggest that the degree of enhancement possibly depends on the structure and hydrophilicity of the counter-ions, which indicates these complexes should be more suitable for percutaneous absorption than meloxicam.The mono-factor method was adopted to optimize the emulgel formulation, and optimal formulation was acpuired with 0.5%Carbomer as mitrix,4% IPM as oil phase and 3%menthol as penetrated enhancer. Our emulgel represented a higher permeability. The experiments was also performed to investigate the quality of emulgel, and our emulgel was testified to be a formulation with a suitable value of pH, good-tolerated properties of centrifugalization,heat and cold, and a steady drug concentration.A simple reversed-phase HPLC method has been developed for determination of meloxicam in rat plasma, excised skin and muscles samples. As compared to oral administration without dose normalization, the C max values of transdermal administration were significantly decreased (3.28μg/ml). On the contrary, the [AUC] 0-48h values were significantly increased (74.01μg·h/ml). The transdermal incorporating meloxicam would provide a useful strategy for prevention and treatment of inflammation, suggesting that the possible side effects from meloxicam may be attenuated due to the lowered peak concentrations, and pharmacological effects can be enhanced and extended.The pharmacological experiment indicated that meloxicam emulgel(p<0.001) and diclofenac diethylamine emulgel (Votalin) (p< 0.01) significantly relieved the pain of rats induced by acetic acid aqueous solution, the former was a more efficient one (p< 0.05) compared with the latter, and its pain inhibition ratio was 61.07% and 37.40%, respectively.All the properties of meloxicam indicated that it’s suitable for transdermal administration, which can be facilitated by organic bases and chemical enhancers. The dosage of emulgel is able to enhanced by enhancers, too. The transdermal incorporating meloxicam would provide a useful strategy for prevention and treatment of inflammation, suggesting that the possible side effects from meloxicam may be attenuated due to the lowered peak concentrations, and pharmacological effects can be enhanced and extended.