Preparation and physicochemical characterization of meloxicam orally fast disintegration tablet using its solid dispersion

Abstract

Meloxicam (MLX) is a non-steroidal, anti-inflammatory drug that is prescribed in the treatment of rheumatoid arthritis and osteoarthritis. MLX is practically insoluble in water and exhibits a slow onset of action. In this study, MLX solid dispersions (MLX SDs) were prepared to improve the water solubility of this poorly water-soluble drug. Then orally disintegrating tablets (ODT) of MLX were developed using MLX SD to decrease the onset of action of this drug. MLX, poloxamer 188, and crospovidone of different ratios were melted in molten poloxamer 188 as a hydrophilic carrier. The optimum SD with the highest saturation solubility in water (13.09±0.34 microgram/mL) consisting of MLX: poloxamer 188: crospovidone in the ratio of 1:2:0 was used for the preparation of MLX ODTs. MLX ODTs were prepared by the direct compression method and optimized by the 2 3 factorial design. The effect of the superdisintegrant concentration, the mannitol-avicel ratio, and the level of compression force on the disintegration time, hardness, and percent of dissolved MLX from MLX ODTs after 30 min was evaluated. DSC and XRD analysis approved an amorphous form of MLX in SDs. The optimized ODT formulation containing 10% of superdisintegrant, and mannitol and avicel in the ratio of 4:1 respectively was compressed using a high level of compression force. The optimized ODT showed hardness (34.37±2.1 N) and friability (1.26±0.04%). This formulation showed a rapid disintegration in 12.66±2.5 seconds, which 82.66±5.1% of the MLX released within 30 min. MLX ODTs, prepared from MLX SD, could be introduced as a suitable dosage form of MLX with improved solubility and the onset of action.

Solubility, correlation, dissolution thermodynamics and preferential solvation of meloxicam in aqueous mixtures of 2-propanol

“…Finally, in mixtures of δ 1+2 < 30.0 MPa 4) exhibits an endothermic peak corresponding to the meloxicam melting as original sample with on-set temperature of 524.0 K and peak temperature of 535.4 K. This last value is similar regarding some other values reported in the literature, i.e. 535.0 K, 38 535.2 K, 39 535.7 K, 40 536.1 K, 41 and 536.7 K. 29 However, some significant differences are observed regarding the values reported by Sathesh-Babu et al (530.0 K), 32 44 which also differ significantly regarding our peak value. X-ray diffraction spectra for meloxicam as original sample and after saturation in neat water, neat 2-propanol and the aqueous mixture of x 1 = 0.50 are shown in Figure 5.…”

Preparation, Characterization and Dissolution Enhancement of Dihydroartemisinin Microparticles

“…DSC study of pure drug (Figure 3) showed sharp exothermic peak at 162.17°C corresponding to melting point of drug indicating crystalline nature. As per result stated by author Zahra Shoormeij et al 25 in his research work, Poloxamer 188 showed sharp endothermic peak at 60.6°C, indicating its melting. Spray dried microparticles D4 in ratio 1:4 w/w ( Figure 4) prepared using Poloxamer 188 does not showed melting peak of Poloxamer 188 suggesting uniform distribution of polymer.…”

“…X-ray diffraction of pure drug DHA ( Figure 5) showed sharp peaks with diffraction angles (2θ) at 25.43 0 , 25.45 0 , 25.47 0 and 25.49 0 with peak intensity of 2138, 2109, 2005 and 1958 respectively signifying substantial crystallinity of drug. Poloxamer 188 showed characteristic peak at 18.83 0 and 22.86 0 with peak intensity 2504 and 2857 indicating crystallinity 25 . Spray dried microparticles ( Figure 6) showed peaks at 25.43 0 , 25.45 0 , 25.47 0 and 25.49 0 with peak intensity of 670, 670, 668 and 646 respectively.…”

Studying the Complex Formation of Sulfonatocalix[4]naphthalene and Meloxicam towards Enhancing Its Solubility and Dissolution Performance

“…However, the poorly aqueous solubility and wettability of ME resulted in a slower dissolution rate of the drug, and hence, a lower oral bioavailability concomitant with slowing its onset of action [ 33 , 34 ]. Enhancing the aqueous solubility of ME could facilitate its oral absorption and bioavailability and reduce its onset of action for the treatment of different types of acute pain [ 34 , 35 ].…”