| 摘要 |
The present invention is related to medicine and pharmaceutics, specifically, to means for the treatment of tuberculosis, more particularly, to the suitable for oral administration pharmaceutical composition for the treatment of tuberculosis, based on the hybrid lipid-polymer nanoparticles containing as the active agent an antibiotic, selected from rifabutin and rifampicin, and lipid-polymer matrix, which comprises a composition consisting of a biodegradable polymer and lipid at a certain quantitative ratio (antibiotic: lipid: biodegradable polymer), where the biodegradable polymer is a copolymer of lactic acid and glycolic acid, having a molecular weight from 2 to 500 kDa, and glycolic acid content in these copolymers is from 0 to 50 mol. %, and the lipid is selected from transesterified ethoxylated vegetable oil and lipoic acid. According to the present invention the pharmaceutical composition is a lyophilizate, which after reconstitution in water or saline forms a stable suspension with the particle size not exceeding 0.8 μm. Furthermore, the present invention relates to the method of producing the said pharmaceutical composition, the method for treating tuberculosis, comprising administration of the said pharmaceutical composition according to a specific treatment schedule (with longer time intervals between the doses, and in lower doses), and to the lipid-polymer matrix for the manufacture of the nanoparticulate pharmaceutical compositions. The pharmaceutical composition of the present invention provides a significantly more pronounced antibacterial effect in comparison with the known, non-particulate dosage forms of these antibiotics, which allows usage of these preparations in considerably lower doses and with lower frequency of administration. |
