Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

Abstract

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem. Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

Novel Advancements in Mouth Dissolving Film Technology

“…Saliva quickly hydrates the film and causes it to stick to the application location. It dissolves and disintegrates quickly, releasing the medication for mucosal absorption or-with some modifications-allowing for oral gastrointestinal absorption with fast-acting dissolve ability [23].…”

Formulation of Orally Disintegrating Films as an Amorphous Solid Solution of a Poorly Water-Soluble Drug

“…The phenytoin solubility increases with the decrease in the polarity of mixed solvents due to the effect of like-dissolve-like. PEG 400 is a cosolvent that is less polar than ethanol and has both a polar oxygen atom and a non-polar (CH 2 ) 2 group, in which the polar part is responsible for miscibility with water and the non-polar part is responsible for interacting with hydrophobic drug molecules, decreasing the hydrogen bond density of water and reducing the ability of the mixed-solvent system to squeeze out the non-polar drug [24,25]. Thus, adding PEG 400 as a cosolvent to water creates a less polar environment for the mixed solvent, resulting in more drug being able to solubilize in that mixture.…”

Using a Laser Monitoring Technique for Dissolution and Thermodynamic Study of Celecoxib in 2-Propanol and Propylene Glycol Mixtures

“…In different stages of drug discovery and development, equilibrium solubility is an important property and represents critical knowledge in pre-formulation, preparation of liquid pharmaceutical dosage forms, purification, and/or extraction (4). Different formulation techniques were used for the solubilization of CXB including solid dispersions, mesoporous formulations, cyclodextrin inclusion complex, microencapsulation, micellar formulation, nanoemulsion formulation, polymeric nanoparticles, co-crystal, hydrotropy, and cosolvency (5)(6)(7)(8)(9)(10)(11)(12)(13). Cosolvency is a feasible and reliable technique for solubilization of a drug compound exhibiting low aqueous solubility.…”