Ultrasound-compacted indomethacin/polyvinylpyrrolidone systems: effect of compaction process on particle morphology and dissolution behavior.
Indomethacin (IMC)/polyvinylpyrrolidone systems were prepared under different technological conditions, using co-evaporation, kneading, traditional, and ultrasound (US) compaction. The materials thus obtained were milled and sieved and the powders were analyzed by using scanning electron microscopy to evaluate the morphology of the final particles and the fractal dimension of the particle contour. In the case of US-treated particles, scanning electron micrographs suggest that IMC could have partially covered the excipient granule surface, which appears lustrous and smooth, whereas after co-evaporation, the particles display a stratified structure. The external color of the granules, the hot stage microscopy examination, and the absence of the melting peak of the drug in thermograms supports the idea that IMC converts into an amorphous form under US discharge. Each technological treatment performed on the binary mixtures increases the dissolution rate of the drug, with respect to the pure drug and the physical mixture, but to a lesser extent than US compaction. US compaction and co-evaporation produce comparable results in improving the release of the drug. Polyvinylpyrrolidone offers better results than beta-cyclodextrin in promoting the dissolution of IMC, when both systems are compacted under US.
Departamento de Farmacia y Tecnologia Farmaceutica, Universidad de Sevilla, Spain. fini@biocfarm.unibo.it
Adamo
A
Fini
Maria Angeles
MA
Holgado
Lorenzo
L
Rodriguez
Cristina
C
Cavallari
D004055:Differential Thermal Analysis; D004339:Drug Compounding; D017709:Fractals; D007213:Indomethacin / Q000008:administration & dosage / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D010592:Pharmaceutic Aids / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry*; D011208:Powders; D012995:Solubility; D014465:Ultrasonics
D010592:Pharmaceutic Aids; D011208:Powders; D011205:Povidone; D007213:Indomethacin