This invention is related to pharmacology, medicine, veterinary science and pharmaceutical industry. It particularly concerns a process for producing original composite antimicrobial preparations for parenteral administration, which possess a higher therapeutic efficiency in case of severe infections and inflammatory diseases.The proposed pharmaceutical compositions contain as active agents betalactam antibiotics and finely dispersed nanostructured silica dioxide in a weight ratio of from 10:1 to 75:1 respectively.The silica dioxide particles present in the composition are agents for delivering antibiotic molecules into the phagocytes which allows to increase the concentration of antimicrobial preparations at inflammation areas and considerably decrease the antibiotic resistance of microorganisms.The proposed process for preparing the pharmaceutical composition includes mixing betalactam antibiotic with finely dispersed nanostructured silica dioxide and is characterized in that the mixture of the above-mentioned substances in a weight ratio of from 10:1 to 75:1 respectively is exposed to mechanical treatment by impact and abrasive actions until the fine powder fraction weight proportion increases (< 5 micron) until it becomes not less than 25%.The obtained mixture is used for preparing injectable solutions.