PHARMACEUTICAL FORMULATIONS CONTAINING 3-(4-CINNAMYL-L-PIPERAZINYL) AMINO DERIVATIVES OF 3-FORMYLRIFAMYCIN SV AND 3-FORMYLRIFAMYCIN S AND A PROCESS OF THEIR PREPARATION

摘要

The present invention related to a process of preparation of pharmaceutically acceptable formulations containing as active substance 3-(4-cinnamyl-1-piperazinyl)-amino derivatives of 3-formylrifamycine SV and 3-formylrifamycine S, which possess high activity against Gram-positive and Gram-negative microorganisms, as well as against tuberculous micobacteria (including atypical and rifamycin resistant), and to a method for the preparation of 3-(4-cinnamyl-1-piperazinyl)-amino derivatives of 3-formylrifamycine SV and 3-formylrifamycine S. The method for the preparation of pharmaceutical compositions is readily feasible, and does not require special equipment for its implementation. The process for preparing the compounds is characterized by high yield and purity, using an environmental clean solvent-ethanol and water in the preparation and isolation of substances, and the absence of residual organic solvents in the final product.

主权项

1. Pharmaceutical formulations comprising a mixture of the active substance of a compound from the group 3-(4-cinnamyl-1-piperazinyl)-amino derivatives of 3-formylrifamycin SV, and S 3-formylrifamycin and excipients, characterized by the fact that the amount of active ingredient per dosage unit is from 100 to 600 mg, and the excipients are present in an amount from 1 to 25% based on the total weight of the mixture.