Biopharmaceutical evaluations glibenclamidum

Authors: Alina Mihaela Mihu, Ion Mircioiu, Raluca Maria Sbora

Abstract: Glibenclamidum is an antidiabetic sulphamide, classified in the second class of the

biopharmaceutical classification system, because it has low solubility and high permeability.
The results of the in vitro dissolution test are limited but they can be estimated in vivo and
correlations can be established.
The objectives of this study were to perform the comparative assessment of in vitro
dissolution for four glibenclamide formulations in the 5 mg tablet formulation.
In this case, the conditions for the dissolution test are: pharmaceutical form - tablets,
concentration 5 mg, apparatus number 2, dissolution medium 1% sodium lauryl sulphate, 500
ml volume, agitation 75 rpm. Samples will be prelevated at 0, 15, 30, 45 and 60 minutes. The
absorbance of the samples will be read on the UV spectrophotometer at a 230nm wavelength.
The first dissolution study was followed by two drugs: Reference I-Tested I. The results for
F1 = 15,56 and F2 = 42,35 noted that the two values do not fall within the reference ranges
for the two values, so RI and TI are not similar.
The second experiment follows a tested drug: RII-TII. The following values were obtained:
F1 = 37.1 and F2 = 29.2. As in the first experiment, the two drugs are not similar. Based on
the data obtained, a comparative evaluation of the four formulations was performed,
comparing the dissolution profiles obtained in the two experiments. The four products became
bioequivalent following the pharmacokinetic data analysis. However, the dissolution tests
provided data on their dissimilarity and it can be concluded that the dissolution test was more
discriminatory in this case and therefore the test parameters can be adjusted or correlated to a
lower F2 value for which we obtain identical bioavailability of the pharmaceutical forms.