Background: Lactose intolerance is characterized by the absence of the enzyme lactase
(beta-galactosidase) and affects two thirds of the world adult population. Our aim was to evaluate a
lactase gastro-resistant formulation to ensure increased activity in the action site of the enzyme (lumen
of the small intestine). Simultaneously, we also evaluated the commercial product stability and enzyme
activity, because the product containing beta-galactosidase is classified as food supplement according
to the Food and Drug Administration (FDA), so it is free to pass quality testing, efficacy and stability.
So, it is possible that contain some irregularities as to the content and enzymatic activity.
Methods: The dissolution assay was performed using a dissolution test system and commercial product
and the gastro-resistant formulation were evaluated according to a method adapted to the conditions
recommended by United States Pharmacopeia (US Pharmacopeia) for gastro-resistant formulations.
For the assessment of enzymatic activity throughout the dissolution test was employed the official
method of lactase assay described in US Pharmacopoeia. This method is based on a colorimetric reaction
which the substrate reacts with the enzyme generate a colored product further analyzed by UVVisible
Results: When carrying out dissolution test in commercial product it is noted that the existing formulation
is not able to protect the enzyme from degrading action of gastric environment (a loss of 86.0 ± 0.8% of
lactase activity was observed). Our proposed gastro-resistant pharmaceutical form there was no loss of
activity during the acid step and the end of the dissolution test the found activity was 95 ± 1.3%.
Conclusion: The formulations proposed in this work using hypromellose capsules ensure the enzymatic
activity of lactase, preventing its contact with the acid medium. For the other side, the results of
commercial tablets for lactase release indicate a significant loss of enzyme activity due to the immediate
release of the enzyme in the simulated gastric fluids.