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Fast dissolving cyclodextrin complex of piroxicam in solid dispersion part I: influence of β-CD and HPβ-CD on the dissolution rate of piroxicam.
Int J Pharm. 2015 Jan 30; 478(2):625-32.IJ

Abstract

Sublingual drug delivery is an interesting route for drug having significant hepatic first-pass metabolism or requiring rapid pharmacological effect as for patients suffering from swallowing difficulties, nausea or vomiting. Sublingual absorption could however be limited by the kinetic of drug dissolution. This study evaluated influences of cyclodextrins (β-CD or HP-β-CD) and their different inclusion process (spray-drying or freeze-drying) on the drug dissolution kinetic of solid dispersions in poly(ethylene glycol) (PEG, Mw 6000Da) of piroxicam, used as poor hydrosoluble drug model. A secondary objective was to determine influences of drug dispersion process in PEG (evaporation or melting methods) on the drug dissolution kinetic of piroxicam. Piroxicam solid dispersions containing or not cyclodextrins were characterized by different scanning calorimetry (DSC), Thermogravometry analyser (TGA) and Fourier transform-infrared spectroscopy (FT-IR) spectroscopy. In vitro drug dissolution study of these solid dispersions was then performed. The results demonstrated the high potential and interest of solid dispersions of drug previously included in cyclodextrins for sublingual delivery of hydrophobic drugs. This study also showed the advantages of evaporation method on the melting ones during drug dispersion in PEG. Indeed, drug complexation with cyclodextrins as dispersion by melting prevented the presence in solid dispersions of drug in crystalline form which can represent up to 63%. Moreover, dispersion in PEG by evaporation method gave more porous drug delivery system than with melting methods. This allowed complete (limited at most at 80-90% with melting methods) and quick drug dissolution without rebound effect like with melting ones.

Authors+Show Affiliations

Galenic Pharmaceutical Laboratory, UFR Medecine and Pharmacy, Rouen University, 22 Bd Gambetta, F-76183 Rouen, France; Pharmaceutical Laboratory, Department of Engineering Processes, Faculty of Technology, Abderrahmane-Mira University, Route de Targua Ouzemmour, DZ-06000 Bejaia, Algeria.Galenic Pharmaceutical Laboratory, UFR Medecine and Pharmacy, Rouen University, 22 Bd Gambetta, F-76183 Rouen, France. Electronic address: mohamed.skiba@univ-rouen.fr.Galenic Pharmaceutical Laboratory, Medecine Faculty, Badji Mokhtar University, DZ-23000 Annaba, Algeria.Galenic Pharmaceutical Laboratory, UFR Medecine and Pharmacy, Rouen University, 22 Bd Gambetta, F-76183 Rouen, France.Pharmaceutical Laboratory, Department of Engineering Processes, Faculty of Technology, Abderrahmane-Mira University, Route de Targua Ouzemmour, DZ-06000 Bejaia, Algeria.Galenic Pharmaceutical Laboratory, UFR Medecine and Pharmacy, Rouen University, 22 Bd Gambetta, F-76183 Rouen, France.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

25522828

Citation

Bouchal, F, et al. "Fast Dissolving Cyclodextrin Complex of Piroxicam in Solid Dispersion Part I: Influence of β-CD and HPβ-CD On the Dissolution Rate of Piroxicam." International Journal of Pharmaceutics, vol. 478, no. 2, 2015, pp. 625-32.
Bouchal F, Skiba M, Chaffai N, et al. Fast dissolving cyclodextrin complex of piroxicam in solid dispersion part I: influence of β-CD and HPβ-CD on the dissolution rate of piroxicam. Int J Pharm. 2015;478(2):625-32.
Bouchal, F., Skiba, M., Chaffai, N., Hallouard, F., Fatmi, S., & Lahiani-Skiba, M. (2015). Fast dissolving cyclodextrin complex of piroxicam in solid dispersion part I: influence of β-CD and HPβ-CD on the dissolution rate of piroxicam. International Journal of Pharmaceutics, 478(2), 625-32. https://doi.org/10.1016/j.ijpharm.2014.12.019
Bouchal F, et al. Fast Dissolving Cyclodextrin Complex of Piroxicam in Solid Dispersion Part I: Influence of β-CD and HPβ-CD On the Dissolution Rate of Piroxicam. Int J Pharm. 2015 Jan 30;478(2):625-32. PubMed PMID: 25522828.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fast dissolving cyclodextrin complex of piroxicam in solid dispersion part I: influence of β-CD and HPβ-CD on the dissolution rate of piroxicam. AU - Bouchal,F, AU - Skiba,M, AU - Chaffai,N, AU - Hallouard,F, AU - Fatmi,S, AU - Lahiani-Skiba,M, Y1 - 2014/12/15/ PY - 2014/11/04/received PY - 2014/12/09/revised PY - 2014/12/11/accepted PY - 2014/12/20/entrez PY - 2014/12/20/pubmed PY - 2015/9/29/medline KW - Hydroxypropyl-β-cyclodextrin KW - PEG6000 KW - Piroxicam KW - Piroxicam (PubChem CID: 54676228) KW - Sublingual administration KW - Ternary complex KW - β-Cyclodextrin SP - 625 EP - 32 JF - International journal of pharmaceutics JO - Int J Pharm VL - 478 IS - 2 N2 - Sublingual drug delivery is an interesting route for drug having significant hepatic first-pass metabolism or requiring rapid pharmacological effect as for patients suffering from swallowing difficulties, nausea or vomiting. Sublingual absorption could however be limited by the kinetic of drug dissolution. This study evaluated influences of cyclodextrins (β-CD or HP-β-CD) and their different inclusion process (spray-drying or freeze-drying) on the drug dissolution kinetic of solid dispersions in poly(ethylene glycol) (PEG, Mw 6000Da) of piroxicam, used as poor hydrosoluble drug model. A secondary objective was to determine influences of drug dispersion process in PEG (evaporation or melting methods) on the drug dissolution kinetic of piroxicam. Piroxicam solid dispersions containing or not cyclodextrins were characterized by different scanning calorimetry (DSC), Thermogravometry analyser (TGA) and Fourier transform-infrared spectroscopy (FT-IR) spectroscopy. In vitro drug dissolution study of these solid dispersions was then performed. The results demonstrated the high potential and interest of solid dispersions of drug previously included in cyclodextrins for sublingual delivery of hydrophobic drugs. This study also showed the advantages of evaporation method on the melting ones during drug dispersion in PEG. Indeed, drug complexation with cyclodextrins as dispersion by melting prevented the presence in solid dispersions of drug in crystalline form which can represent up to 63%. Moreover, dispersion in PEG by evaporation method gave more porous drug delivery system than with melting methods. This allowed complete (limited at most at 80-90% with melting methods) and quick drug dissolution without rebound effect like with melting ones. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/25522828/Fast_dissolving_cyclodextrin_complex_of_piroxicam_in_solid_dispersion_part_I:_influence_of_β_CD_and_HPβ_CD_on_the_dissolution_rate_of_piroxicam_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(14)00916-8 DB - PRIME DP - Unbound Medicine ER -