Free website traffic

This entry was posted in Analytical Discussion and tagged biorelevant, class 2, Dissolution media, glibenclamide, glyburide.

The purpose of this studywas to predict the oral absorption of glyburide. Biorelevant dissolution

methods, combined with permeability measurements and computational simulations,

were used to predict the oral absorption of glyburide. The objectivewas to establish in vitro/in

vivo correlations (IVIVCs) based on the biopharmaceutics drug classification system. The solubility

of the glyburide powder was measured in different media. The dissolution behavior

of two commercial tablet formulations was tested in different media. Two chemical grades

of sodium taurocholate: low quality (LQ) = crude and high quality (HQ) = 97% purity, and egglecithin:

LQ = 60% and HQ= 99.1% purity were used to prepare fasted state small intestinal

fluid (FaSSIF). Simulated intestinal fluid (SIF) and blank FaSSIF without lecithin and taurocholate

(BL-FaSSIF) were used as controls. The dissolution tests were performed under

constant pH and dynamic pH conditions. The dynamic pH range from 5.0 to 7.5 simulated

the biological pH range of gastrointestinal (GI) tract in the fasted state. The drug permeability

was studied using Caco-2 cell line. The predictions of the fraction dose absorbed were

performed using GastroPlusTM. The results of the simulations were compared with actual

clinical data taken from a bioequivalence study. The solubility of glyburide was highest in

LQ-FaSSIF. The two tablet formulations had significantly different dissolution behaviors in

LQ-FaSSIF. The in vitro data was used as the input function into a simulation software. The

dynamic LQ-FaSSIF dissolution data achieved the best prediction of the average AUC and

Cmax of the clinically observed data. The present study shows that BCS based parameters

combined with software simulations can be used to establish an IVIVC for glyburide. In

vitro/in silico tools can potentially be used as surrogate for bioequivalence studies.

© Interactive Pharm 2022

Reach Out

We're not around right now. But you can send us an email and we'll get back to you, asap.


Log in with your credentials


Forgot your details?


Create Account