Objective: The present study was aimed at designing of solid dispersion based pellets of curcumin (Cu) for improving its solubility.
Methods: Solid dispersion (SD) of Cu was prepared by the melt method using Poloxamer 407 (Pol 407) at a different weight ratio of Cu-Pol 407 (1:2, 1:3, 1:5, 1:7, 1:10). The solid dispersion was characterised by FTIR, SEM, DSC, XRD and evaluated for saturation solubility in water, drug content and in vitro dissolution. The pellets of Cu solid dispersion were prepared by extrusion spheronization technique and optimization was performed by 32full factorial design. The pellets were evaluated for size distribution, flow properties, hardness, disintegration and in vitro drug dissolution.
Results: From the phase solubility analysis, Pol 407 was selected as a Solid dispersion carrier. The formation of Cu-SD by melt method using Pol 407, was confirmed from FTIR and DSC studies. XRD studies indicated a change of Cu from crystalline to amorphous form. There was a significant increase of Cu when formulated as SD compared to plain Cu. The optimization of extrusion spheronization process revealed the significant effect of Cu-Pol 407 ratio (p<0.0001) on in vitro dissolution of pellets. Higher Cu dissolution was obtained with Cu-SD pellets compared to plain Cu pellets.
Conclusion: The present study demonstrated the potential of Cu-SD pellets in improving the solubility of poorly soluble Cu.
Objective: The rationale of the current work is to design, develop and optimize of mouth dissolving tablet of ambrisentan to treat hypertension.
Methods: Sodium starch glycolate and crospovidone were used as the super disintegrants in the direct compression method to create nine ambrisentan mouth-dissolving tablet formulations. Wetting time, drug content, in vitro disintegration time, dispersion time, and dissolution time were all assessed for the produced formulations.
Results: Based on the results obtained, formulation F6 containing 30 mg of crospovidone exhibited good wetting time, dispersion time, disintegration time and drug release. The hardness of formulations AS1 to AS9 was found to be in the range of 2.5 to 3.11 Kg/cm2. The friability of formulations AS1 to AS9 was found to be less than 1%. A water absorption ratio was performed for ensuring the moisture sorption and water uptake properties of super disintegrants. The in vitro drug release of formulation AS6 containing a concentration of Crospovidone 30 mg, shows 91.30% drug release respectively at the end of 12 min.
Conclusion: The mouth-dissolving tablets of ambrisentan were successfully designed, developed, and fabricated. It can be reasonably concluded that the AS6 batch of mouth-dissolving tablets of ambrisentan with 30 mg of crospovidone exhibited maximum cumulative drug release in 12 min.
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