In vitro evaluation and in vivo performance of lyophilized gliclazide

Abstract Enhancement of the dissolution rate of the poorly water-soluble hypoglycemic agent, gliclazide, by the aid of lyophilization was investigated. Mannitol, sodium lauryl sulfate (SLS) and polyvinyl pyrrolidone (PVP-k-30) were employed in different weight ratios (43%, 56% and 64% w/w, respectiv...

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Bibliographic Details
Published in:Drug development and industrial pharmacy 2015-04, Vol.41 (4), p.650-657
Main Authors: Mansour, Heba F., F. Aly, Usama
Format: Article
Language:English
Subjects:
Animals
Biological Availability
Blood Glucose - analysis
Calorimetry, Differential Scanning
Chemical Phenomena
Dissolution
Drug Compounding
Drug Liberation
Drug Stability
Excipients - chemistry
Freeze Drying
Gastrointestinal Absorption
gliclazide
Gliclazide - blood
Gliclazide - chemistry
Gliclazide - pharmacokinetics
Gliclazide - pharmacology
Hypoglycemic Agents - blood
Hypoglycemic Agents - chemistry
Hypoglycemic Agents - pharmacokinetics
Hypoglycemic Agents - pharmacology
hypoglycemic effect
lyophilization
Male
Mannitol - chemistry
Povidone - chemistry
Powder Diffraction
Rabbits
Sodium Dodecyl Sulfate - chemistry
Spectroscopy, Fourier Transform Infrared
Suspensions
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Summary:Abstract Enhancement of the dissolution rate of the poorly water-soluble hypoglycemic agent, gliclazide, by the aid of lyophilization was investigated. Mannitol, sodium lauryl sulfate (SLS) and polyvinyl pyrrolidone (PVP-k-30) were employed in different weight ratios (43%, 56% and 64% w/w, respectively) as water-soluble excipients in the formulation. Lyophilized systems were found to exhibit extremely higher in vitro dissolution rate compared to the unprocessed drug powder. Solid state characterization of the lyophilized systems using X-ray powder diffraction, Fourier transform infrared spectroscopy and differential scanning calorimetry techniques revealed that dissolution enhancement was attributable to transformation of gliclazide from the crystalline to an amorphous state in the solid dispersion formed during the lyophilization process. The gastrointestinal absorption and hypoglycemic effect of the lyophilized gliclazide/SLS system were investigated following oral administration to Albino rabbits. Cmax and area under the plasma concentration-time curve of gliclazide (AUC0-12) after administration of the lyophilized formulations were significantly higher than those obtained after administration of the unprocessed gliclazide.
ISSN:0363-9045
1520-5762
DOI:10.3109/03639045.2014.891131