Development of meloxicam formulations utilizing ternary complexation for solubility enhancement

Meloxicam [an oxicam derivative], a relatively new cyclo-oxygenase inhibitor, is a member of enolic acid group of non-steroidal anti-inflammatory drugs. It is generally used in the treatment of rheumatoid arthritis, osteoarthritis and other joint pains. Meloxicam is practically insoluble in water [8 microg/ml], which directly influences the C[max], T[max], as well as the bioavailability of the drug. In the present study, an attempt has been made to improve the dissolution of Meloxicam by preparation of its solid dispersion using p-cyclodextrin blended with various water soluble polymer carriers i.e., HPMC [methocel IH], methylcellulose [400cps], PVP K30, HPMC [K[4]M], HPMC [50cps]. It is reported that when small amount of water soluble polymer is added to beta-cyclodextrin, its nature of solubilization significantly increases due to increase in the apparent complex stability constant. Phase solubility studies were carried out to evaluate the solubilizing power of beta-cyclodextrin along with various water soluble polymers. The solid dispersion was prepared and formulated into tablets and suspension, which were evaluated on the basis of various official tests. All the studies suggest that formulations of Meloxicam utilizing solid dispersion technique significantly enhances solubility [90 microg/ml] of the drug and results in superior formulations of the drug by using beta-cyclodextrin blended with 0.12% w/w HPMC [Methocel IH]. Ternary complexation is a valuable tool for solubility enhancement of drugs

Bioequivalence studies of two brands of meloxicam tablets in healthy Pakistani volunteers

The pharmacokinetic parameters of two oral formulations of meloxicam tablets were compared in a randomized, single oral dose; two treatments cross over design in 12 healthy male volunteers belonging to Pakistan under fasting conditions. After an overnight fast, the volunteers received 30 mg meloxicam and the blood samples were collected up to 96 hours and drug concentrations were determined by a validated HPLC method. Various pharmacokinetic parameters were determined from the plasma concentration-time curves of both formulations. The 90% confidence intervals obtained by analysis of variance were 87-94% for Cmax and 88-97% for AUC0-t, that fell well within the acceptance range of 80-125%. Also, no significant difference [beta = 0.05, Wilcoxon Signed rank test] were detected between Tmax of both formulations. The two formulations were well tolerated and no adverse effect was reported during the study

Factors affecting the diffusion of meloxicam from different bases

The value of meloxicam as a non-steroidal anti-inflammatory drug is well established. This study was carried out to formulate a stable and effective meloxicam topical preparation. The in vitro release of meloxicam from different semisolid bases, which are: o/w, w/o emulsions, sodium carboxy methylcellulose gel and carbomer gel base was established. The study also involved the diffusion of meloxicam through excised mouse skin with different concentrations using carbomer gel in addition to the effect of different enhancing agents such as PG [Propylene Glycol], methyl salicylate, urea, oleic acid, DMSO [Dimethyl Sulfoxide], xanthan gum and PEG 1000 [Poly Ethylene Glycol] and the last one gave the highest diffusion. The results showed that the selected formula of meloxicam was not irritant and this result was supported by histological examination. In addition, the results showed that the use of disodium EDTA [stabilizer] gave more stable formula where the expiration date was 2 years compared to 0.8 year when using both dl- alpha tocopherol and blank formula. The results showed that the temperature and the storage period led to decrease both the diffusion rate and viscosity of meloxicam 1% gel but with little change in pH. On the other hand preliminary clinical study was carried out for 26 patients and the results indicated that 84.6% of patients got positive responses