Dissolution rate enhancement, in vitro evaluation and investigation of drug release kinetics of chloramphenicol and sulphamethoxazole solid dispersions

Formulation of solid dispersions is one of the effective methods to increase the rate of solubilization and dissolution of poorly soluble drugs. Solid dispersions of chloramphenicol (CP) and sulphamethoxazole (SX) as model drugs were prepared by melt fusion method using polyethylene glycol 8000 (PEG...

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Veröffentlicht in:Drug development and industrial pharmacy 2013-05, Vol.39 (5), p.704-715
Hauptverfasser: Khan, Sheraz, Batchelor, Hannah, Hanson, Peter, Saleem, Imran Y., Perrie, Yvonne, Mohammed, Afzal R.
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container_end_page 715
container_issue 5
container_start_page 704
container_title Drug development and industrial pharmacy
container_volume 39
creator Khan, Sheraz
Batchelor, Hannah
Hanson, Peter
Saleem, Imran Y.
Perrie, Yvonne
Mohammed, Afzal R.
description Formulation of solid dispersions is one of the effective methods to increase the rate of solubilization and dissolution of poorly soluble drugs. Solid dispersions of chloramphenicol (CP) and sulphamethoxazole (SX) as model drugs were prepared by melt fusion method using polyethylene glycol 8000 (PEG 8000) as an inert carrier. The dissolution rate of CP and SX were rapid from solid dispersions with low drug and high polymer content. Characterization was performed using fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). FTIR analysis for the solid dispersions of CP and SX showed that there was no interaction between PEG 8000 and the drugs. Hyper-DSC studies revealed that CP and SX were converted into an amorphous form when formulated as solid dispersion in PEG 8000. Mathematical analysis of the release kinetics demonstrated that drug release from the various formulations followed different mechanisms. Permeability studies demonstrated that both CP and SX when formulated as solid dispersions showed enhanced permeability across Caco-2 cells and CP can be classified as well-absorbed compound when formulated as solid dispersions.
doi_str_mv 10.3109/03639045.2012.689763
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Solid dispersions of chloramphenicol (CP) and sulphamethoxazole (SX) as model drugs were prepared by melt fusion method using polyethylene glycol 8000 (PEG 8000) as an inert carrier. The dissolution rate of CP and SX were rapid from solid dispersions with low drug and high polymer content. Characterization was performed using fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). FTIR analysis for the solid dispersions of CP and SX showed that there was no interaction between PEG 8000 and the drugs. Hyper-DSC studies revealed that CP and SX were converted into an amorphous form when formulated as solid dispersion in PEG 8000. Mathematical analysis of the release kinetics demonstrated that drug release from the various formulations followed different mechanisms. 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subjects Anti-Infective Agents - chemistry
Anti-Infective Agents - pharmacokinetics
BCS
Caco-2 cell lines
Caco-2 Cells - drug effects
Calorimetry, Differential Scanning
chloramphenicol
Chloramphenicol - chemistry
Chloramphenicol - pharmacokinetics
Dissolution rate
Drug Delivery Systems
Humans
Microscopy, Electron, Scanning
Models, Theoretical
PEG 8000
Polyethylene Glycols - chemistry
release kinetics
solid dispersions
Solubility
Sulfamethoxazole - chemistry
Sulfamethoxazole - pharmacokinetics
sulphamethoxazole
Surface-Active Agents - chemistry
title Dissolution rate enhancement, in vitro evaluation and investigation of drug release kinetics of chloramphenicol and sulphamethoxazole solid dispersions
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