Complexes of antitubercular antibiotics with cellulose sulfate acetate

Abstract

Water-insoluble complexes of antituberculosis antibiotics (AB) kanamycin (CNMC), amikacin (AMCC) and capreomycin (CPRMC), traditionally used parenterally, with cellulose acetate sulphate in the form of sodium salt (Na-SAC) were obtained. The possibility of their immobilization on the activated carbon (AC) to create a tablet form of AB was demonstrated. The composition of the complexes was determined depending on the medium pH and the order of solutions components mixing. It was shown that with decreasing pH from 6 to 1 due to an increase in the number of protonated amine groups in AB molecules, the number of contacts with polymer macromolecules increases and the amount of cellobiosic units in the complex’s composition increases as well: in the case of CNMC and AMCC from one to three and to four in the case of CPRMC. The electrostatic nature of the complexation is confirmed by the corresponding bands’ shifts in the IR spectra: Na-SAC sulfate groups and the antibiotic amino groups. It was established in vitro that the Na-SAC–CNMC complexes and their compositions with activated carbon are not only equivalent, but also have the double activity of the standard (injectable) form of CNMC in the relation to tuberculosis mycobacterium. The resulting compositions can be recommended for in vivo testing as a new form of aminoglycoside antibiotics for oral administration.