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

Congreso; 6ta Reunión Internacional de Ciencias Farmacéuticas (RICiFa 2020+1); 2021

Clarithromycin (CLM), is a semi-synthetic macrolide with very poor solubility. The drugswith low solubility but high permeability (class II of the Biopharmaceutical Classification System)lead to low oral bioavailability and erratic absorption . Therefore, one of the aim of this work was toimprove the solubility of the drug in order to enhance its bioavailability and microbiological activitythrough the formation and evaluation of CLM binary systems. CLM solubility assays were carried outthrough phase solubility analysis, which required validating an analytical method by HPLC, using thefollowing amino acids as the second component (SC): Arg, Gly, Cys, Val, Pro, and ascorbic acid(AA). The minimum inhibitory concentration (MIC) of CLM and the SC that increased the solubilitywas determined using the broth dilution method according to the norms of the Clinical LaboratoryStandards Institute. Finally, to evaluate the combination of ATM with SC against methicillin resistantStaphylococcus aureus (MRSA), the checkerboard method was used. Cys and AA were the SC thatproduced the greatest increase in the solubility of CLM. Although these compounds alone did notshow an inhibitory effect against MRSA combineds with CLM, a decrease in the MIC of ATM wasobserved.