The use of spray-drying to enhance celecoxib solubility

Abstract

The present research investigates the enhancement of the dissolution rate of celecoxib by using spray-drying to prepare a solid dispersion with various polymers, namely Kollicoat IR® (Kollicoat), polyvinyl alcohol (PVA) 22000, or polyethylene glycol 6000 (PEG). The investigated drug-to-polymer mass ratios were 1:1, 1:2, and 1:4 by weight. Hydroalcoholic or methylene chloride solvent systems were used. The obtained yields ranged from 65% to 78%, whereas the entrapment efficiencies were between 68% and 82%. The results revealed an increase in the dissolution rate of the prepared particles up to 200% within 20 min. The prepared particles were investigated using differential scanning calorimetry, scanning electron microscopy, X-ray diffraction, and Fourier transform infrared spectroscopy. The increased dissolution rate was attributed to hydrogen bond formation between celecoxib and each polymer together with the reduced size of the formed particles offering a greater overall surface area. It was concluded that spray-drying may be considered a successful one-step technique to improve the dissolution rate of celecoxib when using Kollicoat, PVA, or PEG as the carrier polymer.

In-line monitoring of compaction properties on a rotary tablet press during tablet manufacturing of hot-melt extruded amorphous solid dispersions

“…The sharp doublet at 3333 cm -1 and 3227 cm -1 is attributed to the N-H stretching vibration of the -SO 2 NH 2 group of CEL. This doublet was clearly diminished and broadened after HME, suggesting that the sulphonamide group of CEL acted as H-donor and engaged in interactions with -C=O carbonyl groups (H-acceptors) of the polymer (Fouad et al, 2011;Gupta et al, 2005). Similar spectra were obtained for the solid dispersions with VA 64 and EPO (data not shown), which were in line with earlier findings linking this spectra to the formation of an amorphous drug form and possible molecular interactions between CEL and the carriers (Albers et al, 2009), favouring stability of the formulation.…”

Agglomeration of Celecoxib by Quasi Emulsion Solvent Diffusion Method: Effect of Stabilizer

“…The sink conditions was maintained by adding 0.25% (w/v) SDS in 1000 ml distilled water. 8,9 Each vessel was introduced the amount of sample equivalent to 40 mg celecoxib. At pre-determined time intervals, samples were withdrawn from the vessels through a 5 µm membrane filter (Millipore) followed by their spectrophotometric analysis employing a UV detector (UV-160A, Shimadzu, Japan) at 253 nm.…”

Hot-melt extrusion of polyvinyl alcohol for oral immediate release applications

“…9) showed characteristic peaks of CEL at 3331.4 and 3225.8 cm -1 , which corresponded to N-H stretching in the SO 2 NH 2 group. While those bands were clearly visible in the physical mixture (PM), they broadened after extrusion (EX), likely due to hydrogen bonding between the acidic hydrogen of N-H as hydrogen donor from CEL and O-H as hydrogen acceptor of PVOH (Fouad et al, 2011). This resulted in a fast release of CEL from the PVOH mixtures (Fig.…”