Abstract
Linezolid is a second line antituberculosis which is currently available in the form of oral and parenteral dosage form. Compared to oral and parenteral dosage forms, the direct delivery of antituberculosis drugs to the lungs has proven to be better in maintaining the desire drug concentration. The present investigation was aimed to prepare the slow dissolving salts of linezolid using with long chained fatty acids – lauric acid(LA), palmitic acid (PA) and stearic acid (SA) as counterions for direct pulmonary delivery. The rotary vacuum evaporator and lyophilizer were used sequentially to evaporate the solvent in which the drug and counterions were dissolved. The results of DSC (differential scanning calorimetry) study, microscopic analysis and PXRD (powder X-ray diffraction) study proved the formation of novel crystalline material due to reaction between drug and counterions. The results of FTIR (Fourier transform infrared spectroscopy) and 1H NMR (Nuclear magnetic resonance) confirmed the transfer of hydrogen ion from the carboxylic acid group (–COOH–) of the counterions to the amide (–CONH–) group of the drug and thus the salt formation. The in-vitro dissolution study performed in the simulated lung fluid (SLG), the prepared salts exhibited significantly slower dissolution compared to pure drug and physical mixture. MMAD (Median mass aerodynamic diameter) for all the prepared salt was found to be less than 5 μm which proved ability of the prepared salt particles to reach deep affected area. MIC (Minimum inhibitory concetration) study indicated no significant difference in the MIC value of the pure drug and the prepared salts.
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