Correlations between in vitro dissolution, in vivo bioavailability and hypoglycaemic effect of oral glibenclamide

Chalk, J.B., Patterson, M., Smith, M.T. and Eadie, M.J. (1986) Correlations between in vitro dissolution, in vivo bioavailability and hypoglycaemic effect of oral glibenclamide. European Journal of Clinical Pharmacology, 31 2: 177-182. doi:10.1007/BF00606655


Author Chalk, J.B.
Patterson, M.
Smith, M.T.
Eadie, M.J.
Title Correlations between in vitro dissolution, in vivo bioavailability and hypoglycaemic effect of oral glibenclamide
Journal name European Journal of Clinical Pharmacology   Check publisher's open access policy
ISSN 0031-6970
1432-1041
Publication date 1986-03
Sub-type Article (original research)
DOI 10.1007/BF00606655
Open Access Status Not Open Access
Volume 31
Issue 2
Start page 177
End page 182
Total pages 6
Publisher Springer-Verlag
Language eng
Formatted abstract
A study has been carried out investigating four different marketed oral preparations of glibenclamide, correlating the effectiveness of the drug in these preparations in lowering plasma glucose concentrations with (i) the in vitro dissolution of the drug, measured by the British Pharmacopoeal and Desaga methods, and (ii) the in vivo bioavailability, assessed in 12 healthy human volunteers. The two dissolution methods yielded different rank orders of ease of dissolution of the drug from the various preparations; the findings of neither dissolution method correlated adequately with the results of the in vivo bioavailability studies, which correctly predicted the abilities of the preparations to reduce plasma glucose concentrations. Relative to an oral glibenclamide solution the bioavailabilities of the drug from three tablet preparations were 0.69, 0.49 and 0.24. The mean elimination half-life of the drug was 1.5 h and assuming complete bioavailability of the drug from oral solution the mean systemic clearance was 0.095 l kg-1h-1, and the mean apparent volume of distribution was 0.20 l kg-1. It is concluded that it may be unsafe to use in vitro dissolution data as a basis for assessing the bioequivalences of different glibenclamide preparations intended for oral use
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Pharmacy Publications
 
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