Binary systems of clarithromycin: An alternative to enhancement its solubility and antimicrobial activity

ANTONELA BARTOLILLA; ARIANA ZOPPI; MARCELA R. LONGHI; VIRGINIA AIASSA

Congreso; 6ta Reunión Internacional de Ciencias Farmacéuticas; 2021

RICiFa

Clarithromycin (CLM), is a semi-synthetic macrolide with very poor solubility.The drugs with low solubility but high permeability (class II of the Biopharmaceutical Classification System). Therefore, one of the aim of this work was improve the drug solubility and antimicrobial activity of them through the formation and evaluation of binary systems. CLM solubility assays were carried out through phase solubility analysis, using different amino acids and ascorbic acid (AA) as the second component (SC). The minimum inhibitory concentration (MIC) of CLM and the SC that increased the solubility was determined using the broth dilution method. Finally, to evaluate the combination of ATM with SC against methicillin resistant Staphylococcus aureus (MRSA), the checkerboard method was used. Cys and AA were the SC that produced the greatest increase in the solubility of CLM of 1.4 at 5.8 and 84.8 mM respectively. Although these compounds alone did not show an inhibitory effect against MRSA combineds with CLM, a decrease in the MIC of ATM was observed of 0.25 until 0.06 µg/ml. Given that this combinations showed greater solubility and an increase in antimicrobial activity, it can be concluded that could be potentially useful for application in a future pharmaceutical formulation.