Formulações sólidas de lactase: estudos de estabilidade acelerada, liberação e sua quantificação por espectroscopia no infravermelho

Abstract

Lactose intolerance is characterized by the absence of the enzyme lactase (β-galactosidase) and affects almost 50% of the population. The treatment is based on a restrictive diet of dairy products which can result in nutritional loss and is associated with decreased bone mineral density and fractures. Our aim was to evaluate a lactase gastro formulation to ensure increased activity in the action site of the enzyme (lumen of the small intestine). Simultaneously, we also evaluated the stability and enzyme activity of the american commercial product (tablets of Lactaid® 9000 U). And lastly, we developed an analytical method for measuring the lactase content in solid formulations by spectroscopy in the infrared region. In carrying out the stability test to note that the primary packaging is critical in maintaining the enzymatic activity of lactase. At the end of the stability study, the tablets that were in the primary package had a decrease in their activity by approximately 7.5%, while the tablets were stored outside of its original container had a loss of approximately 35%. When carrying out dissolution test also the american commercial product it is noted that the existing formulation is not able to protect the enzyme from the degrading action of gastric environment of the stomach, with the end of the test a loss of 65% of enzyme activity. Compared with the gastroresistant pharmaceutical form there was no loss of activity during the acid step and the end of the dissolution test the activity was found 93%. As regards the measurement method by IR, it was found that the best multivariate calibration model (PLS) features 7 LV, RMSECV 4.3%, RMSEP of 1.2% and the data obtained with MIR is very similar to the data obtained by the USP reference method.