<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml"><p>The purpose of this study was to obtain an amorphous system with minimum unit operations that will prevent recrystallization of amorphous drugs since preparation, during processing (compression) and further storage. Amorphous celecoxib, solid dispersion (SD) of celecoxib with polyvinyl pyrrollidone (PVP) and co-precipitate with PVP and carrageenan (CAR) in different ratios were prepared by the spray drying technique and compressed into tablets. Saturation solubility and dissolution studies were performed to differentiate performance after processing. Differential scanning calorimetry and X-ray powder difraction revealed the amorphous form of celecoxib, whereas infrared spectroscopy revealed hydrogen bonding between celecoxib and PVP. The dissolution profile of the solid dispersion and co-precipitate improved compared to celecoxib and amorphous celecoxib. Amorphous celecoxib was not stable on storage whereas the solid dispersion and co-precipitate powders were stable for 3 months. Tablets of the solid dispersion of celecoxib with PVP and physical mixture with PVP and carrageenan showed better resistance to recrystallization than amorphous celecoxib during compression but recrystallized on storage. However, tablets of co-precipitate with PVP and carageenan showed no evidence of crystallinity during stability studies with comparable dissolution profiles. This extraordinary stability of spray-dried co-precipitate tablets may be attributed to the cushioning action provided by the viscoelastic polymer CAR and hydrogen bonding interaction between celecoxib and PVP. The present study demonstrates the synergistic effect of combining two types of stabilizers, PVP and CAR, on the stability of amorphous drug during compression and storage as compared to their effect when used alone.</p></abstract>

The purpose of this study was to obtain an amorphous system with minimum unit operations that will prevent recrystallization of amorphous drugs since preparation, during processing (compression) and further storage. Amorphous celecoxib, solid dispersion (SD) of celecoxib with polyvinyl pyrrollidone (PVP) and co-precipitate with PVP and carrageenan (CAR) in different ratios were prepared by the spray drying technique and compressed into tablets. Saturation solubility and dissolution studies were performed to differentiate performance after processing. Differential scanning calorimetry and X-ray powder difraction revealed the amorphous form of celecoxib, whereas infrared spectroscopy revealed hydrogen bonding between celecoxib and PVP. The dissolution profile of the solid dispersion and co-precipitate improved compared to celecoxib and amorphous celecoxib. Amorphous celecoxib was not stable on storage whereas the solid dispersion and co-precipitate powders were stable for 3 months. Tablets of the solid dispersion of celecoxib with PVP and physical mixture with PVP and carrageenan showed better resistance to recrystallization than amorphous celecoxib during compression but recrystallized on storage. However, tablets of co-precipitate with PVP and carageenan showed no evidence of crystallinity during stability studies with comparable dissolution profiles. This extraordinary stability of spray-dried co-precipitate tablets may be attributed to the cushioning action provided by the viscoelastic polymer CAR and hydrogen bonding interaction between celecoxib and PVP. The present study demonstrates the synergistic effect of combining two types of stabilizers, PVP and CAR, on the stability of amorphous drug during compression and storage as compared to their effect when used alone.

Development of spray-dried co-precipitate of amorphous celecoxib containing storage and compression stabilizers

Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy and Research Centre, Erandawane, Pune-411038 Maharashtra, India

Acta Pharmaceutica

The purpose of this study was to obtain an amorphous system with minimum unit operations that will prevent recrystallization of amorphous drugs since...

Development of spray-dried co-precipitate of amorphous celecoxib containing storage and compression stabilizers

Publié en ligne: 18 sept. 2007

Pages: 287 - 300

DOI: https://doi.org/10.2478/v10007-007-0023-7

Mots clés
celekoksib, amorfna tvar, čvrsta disperzija, koprecipitat, PVP, karagenan, kompresija, stabilnost, tabletiranje

This content is open access.

Development of spray-dried co-precipitate of amorphous celecoxib containing storage and compression stabilizers

Publié en ligne: 18 sept. 2007

Pages: 287 - 300

DOI: https://doi.org/10.2478/v10007-007-0023-7

Mots cléscelekoksib, amorfna tvar, čvrsta disperzija, koprecipitat, PVP, karagenan, kompresija, stabilnost, tabletiranje

This content is open access.

Mots clés
celekoksib, amorfna tvar, čvrsta disperzija, koprecipitat, PVP, karagenan, kompresija, stabilnost, tabletiranje