Interchangeability and Comparative Effectiveness between Micronized and Non-micronized Products of Glibenclamide Tablets

Abstract

Background: During the last few years there was wide debate about the interchangeability and effectiveness between circulated products containing Glibenclamide in the market.
Objectives: This study aimed to compare the effectiveness of this product “non-micronized” to the originator’s product of Glibenclamide tablets “of micronized” sulfonylurea.
Methods: 12 volunteers received a dose of 5mg of Glibenclamide (from test and standard products) under fasting conditions in two separate sessions using randomized crossover design. Blood glucose level for the volunteers was monitored to avoid the development of hypoglycemia. Plasma samples were collected over 24 hours and analyzed using HPLC.
Results: The maximum concentration Cmax for the test and reference products were 2.508 ± 0.104 and 3.526 ± 0.118 (ìg/ml) respectively and the area under the curve AUC0-[ were 3.511 ± 0.153 4.572 ± 0.202 (ìg.h/ml) for these products respectively, with a difference of about 24% between the test and reference products in its AUC.
Conclusions: The results indicate that the test product is not bioequivalent to reference product. The difference in formulation between micronized product and non-micronized product of Glibenclamide tablets has impact on clinical outcomes.

Key words:sulfonylurea,Blood glucose,hypoglycemia.