CONICET | Buscador de Institutos y Recursos Humanos

Introduction: Acetazolamide (ACZ) is a potent inhibitor of carbonic anhydrase that acts by reducing the rate of fluid formation, which makes it useful in the treatment of glaucoma. However, ACZ has low aqueous solubility, low permeability and often causes damage to the intestinal mucosa when administered orally. Have developed numerous experimental models to determine the potential amount of drug absorbed in the intestinal lumen and its absorption mechanism. The Simple Pass Intestinal Permeation (SPIP) is the in situ technique most frequently used because it provides the closest conditions to which a drug is after oral administration. Using specific permeability markers enables a simple screening test for classifying a drug by its permeability. Objectives: To determine the values of Peff of ACZ using as standards of reference atenolol (ATE), a low permeability marker, propranolol (PRO) and verapamil (VER), a high permeability markers. Methodology: Studies SPIP developed in Wistar male rats. The rats were anesthetized. Once the animals reached the plane of anesthesia was performed an incision in the abdomen and intestinal segment of approximately 10 cm was isolated and canalized at both ends. The first sample was taken 15 min after the start of infusion of a solution containing the test compound at a rate of 0.2 ml / min. The outlet solutions of the intestinal segments, were collected each 7 min into Eppendorf tubes and stored until analysis by HPLC. Results: Peff values obtained were: 4.4 ± 1.4; 7.7 ± 1.9; 7.6 ± 5.3 and 27.9 ± 1.5 x10-5 cm/seg for ATE, PRO, VER and ACZ respectively. Conclusions: From the results obtained it was concluded that ACZ permeability is higher than the obtained for PRO and VER and also higher than that obtained for ATE. Therefore, these results indicate that ACZ is a high permeability drug according to the SCB.