Injection composition containing fab i inhibitor, and preparation method therefor
AssigneeCrystalGenomics, Inc.
InventorsJae Pyoung CHO, Joong Myung CHO
Life of this patent
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Abstract
The present invention relates to a pharmaceutical composition for intravenous administration, containing a Fab I inhibitor, and a preparation method therefor. The present invention can be effectively applied to an infection caused by antibiotic-resistant bacteria. Specifically, the present invention enables treatment effects to be more rapidly initiated by improving solubility and dissolution rate, and enables bioavailability to be improved. In addition, by controlling the size of particles, mixing and content uniformity of a preparation can be improved.
Claims13
A composition for injection comprising:
- 1-(3-amino-2-methylbenzyl)-4-(2-thiophen-2-yl-ethoxy)-1H-pyridin-2-one or a salt thereof;
- and
- a polymer compound, a solubilizing agent, or a mixture thereof.
A method of preparing a composition for injection comprising 1-(3-amino-2-methylbenzyl)-4-(2-thiophen-2-yl-ethoxy)-1H-pyridin-2-one or a salt thereof, the method comprising:
- adding 4-benzyloxy-1H-pyridone, 2-methyl-3-nitro-benzylchloride and potassium tert-butoxide to dimethylformamide and mixing and reacting them under heating;
- reacting the mixture, adding purified water and drying under heating;
- dissolving the dried product in an organic solvent and adding purified water for layer separation;
- recovering the organic layer, filtering and concentrating to prepare a concentrate;
- reconcentrating the concentrate and adding hexane to prepare an intermediate precipitate;
- dissolving the obtained precipitate, cooling, filtering and drying to obtain a dried product;
- and
- dissolving the obtained dried product in an organic solvent and then adding and reacting iron chloride hexahydrate, activated carbon and hydrazine monohydrate, cooling and filtering to obtain a final precipitate, and drying and pulverizing the obtained final precipitate to prepare the compound.
Dependencies are inferred from the claim text.