36 results about "Fidaxomicin" patented technology

A bacterial strain of Actinoplanes sp. and an application thereof. The bacterial strain is named Actinoplanes sp. HS-16-20, whose preservation number is CGMCC No.7294. The bacterial strain can generate Fidaxomicin, and Fidaxomicin has an inhibitory effect on various gram positive bacteria pathogens, and in particular, on Clostridium difficile.

The present invention relates to pharmaceutical compositions for rectal administration comprising fidaxomicin and to a process for preparing the pharmaceutical compositions for rectal administration. The invention also relates to an aerosol canister comprising a foamable pharmaceutical composition comprising fidaxomicin for rectal administration and to the treatment or maintenance of remission of infections such as diarrhoea caused by Clostridium difficile..

The invention discloses a fidaxomicin crystal form II and a preparation method thereof. An X-ray powder diffraction spectrum of the crystal formula has X-ray powder diffraction peaks at 2theta, namely 7.04 degrees, 15.87 degrees, 19.14 degrees, 20.46 degrees and 22.95 + / -0.2 degrees. The crystal form obtained by the method is stable, simple in preparation method, strong in maneuverability and applicable to industrial production.

The invention is a method for separating and purifying fidaxomicin, which solves the problems of many separation steps, high production cost and low recovery rate in the existing method for separating and purifying fidaxomicin. The method of the present invention comprises the following steps: (1) the crude product containing fidaxomicin is dissolved in an organic solvent, washed with an alkaline solution, and the organic phase is dried with a desiccant, then concentrated under reduced pressure to obtain a concentrate; (2) step ( 1) The obtained concentrate is passed through a polyamide column for gradient elution, and the eluate containing Fidaxomycin is collected, concentrated under reduced pressure and crystallized to obtain pure Fidaxomicin in the form of a white powder. The purity of Fidaxomicin obtained is More than 97%, the total yield reaches more than 75%. The method of the invention can obtain high-purity fidaxomicin, has few steps, simple and easy process, high yield, and is environmentally friendly, and is very suitable for commercial production.

The invention discloses a Fidaxomicin crystal and a preparation method of the crystal. The characteristic peaks of the X-ray powder diffraction spectrum of the crystal are located at 3.324, 7.745, 9.989, 10.607, 13.954, 14.475, 15.355, 15.855, 18.800, 19.999, 20.321, 22.245, 23.104, 24.028, 24.446 in 2θ. The preparation steps of the method are as follows: adding fidaxomicin to an aqueous solution of ethanol to dissolve, performing crystallization, suction filtration and drying to obtain fidaxomicin crystals. The invention has the advantages of stable process, simple and quick operation, easy recovery of solvent, environmental protection and suitability for industrialized production. The obtained fidaxomicin crystal form is stable and the particles are uniform, which is convenient for packaging and storage.

The invention discloses a fidaxomicin enteric-coated preparation, which contains 40-400 mg of fidaxomicin; the fidaxomicin enteric-coated preparation includes a drug inner core, an isolation coat layer and an enteric coat layer; the isolation coat layer includes A copolymer of polyvinyl alcohol and polyethylene glycol, the weight of which is 0.3wt% to 2.5wt% of the drug inner core; the enteric coating layer includes enteric materials dissolved at pH 4.5 to 6.8, whose weight is 0.3% to 2.5wt% of the drug inner core 5wt% ~ 25wt%. The enteric-coated preparation of the present invention remains intact in the gastric juice, does not leak the drug, and effectively avoids the degradation and consumption of fidaxomicin under the action of gastric acid; and when the enteric-coated preparation leaves the stomach and enters the pylorus, the enteric coating and isolation coat can quickly Disintegration and rapid release of Fidaxomycin, Fidaxomicin in the enteric-coated preparation reaches the therapeutic concentration in a short time after reaching the intestinal tract, there is no time lag effect, prolonging the residence time of the drug in the human body, making The bactericidal effect is maximized, thereby effectively improving the bioavailability and bactericidal efficacy of the drug.

The invention discloses a fidaxomicin crystal form I and a preparation method thereof. An X-ray powder diffraction spectrum of the crystal form has X-ray powder diffraction peaks at 2theta of 4.22 degrees, 7.60 degrees, 8.17 degrees, 9.51 degrees, 10.07 degrees, 11.07 degrees, 11.51 degrees, 12.85 degrees, 13.28 degrees, 15.47 degrees, 16.24 degrees, 18.55 degrees, 19.78 degrees, 20.15 degrees, 20.80 degrees and 21.47 degrees. The crystal form provided by the invention is stable, simple in preparation method, strong in maneuverability, and applicable to industrial production.