41 results about "Prulifloxacin" patented technology

This invention relates to preparation method of a compound as formulae(1). The chart is the structure of R.

The invention provides a preparation method of prulifloxacin using [(3,4-difluorophenyl)amido](ethylthio) methylene malonic ester as starting material, xylene or ion liquid as reaction medium, Lewis acid as catalyst to synthesize 6,7-difluoro-4-hydroxy-2-(ethylthio) quinoline-3-ethyl formate of formula (IV), synthesizing compound of formula (II) by reacting compound of formula (IV) with acetic anhydride, chlorosulfonic acid, sodium carbonate by way of multi-charging 'one-pot'; performing displacement reaction of the compound of formula (II) and piperazine of formula (V) in ion liquid to generate the corresponding compound of formula (VI); obtaining the compound of formula (VII) by hydrolyzing the compound of formula (VI), reacting the compound of formula (VII) with the compound of formula(IX) to obtain prulifloxacin of formula (I). The preparation method has features of high yield, high product purity, and simple technique, suitable for industrialization.

The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing prulifloxacin, and a preparation method thereof. The pharmaceutical composition is characterized by containing prulifloxacin and a pharmaceutically acceptable carrier, wherein the pharmaceutically acceptable carrier at least comprises phosphate, and the weight ratio of the prulifloxacin to the phosphate is (1:2)-(2:1). Shown by stability tests, the impurity content of the pharmaceutical composition provided by the invention is obviously lower than that of a common preparation.

The invention relates to a synthetic method of prulifloxacin, comprising the steps of: stirring DMDO-Cl and sodium iodide in an organic solvent, carrying out a one-pot reaction of the unseparated reaction liquid, a compound 2 and alkali substances to obtain the prulifloxacin. The synthetic method of the invention is advantaged in that the raw material DMDO-Cl used in the invention is cheap, easily available, and easily stored and transported, the prulifloxacin synthesized by the method has high yield, increased purity, and the operation is convenient.

The invention discloses a prulifloxacin oral solid composition and a preparation method thereof. The prulifloxacin oral solid composition is prepared from 130 to 135 parts by weight of prulifloxacin, 10 to 30 parts by weight of starch, 30 to 50 parts by weight of microcrystalline cellulose, 20 to 40 parts by weight of lactose, 0.05 to 10 parts by weight of one or more binders, 2 to 15 parts by weight of one or more disintegrants and 0.5 to 10 parts by weight of one or more lubricants. The one or more binders are selected from polyvinylpyrrolidone, lauryl sodium sulfate and polyethylene glycol mixed aqueous solutions or alcoholic solutions. The one or more disintegrants are selected from carboxymethyl starch sodium, polyvinylpolypyrrolidone and hydroxy propyl cellulose. The one or more lubricants are selected from magnesium stearate, calcium stearate and aerosil. The prulifloxacin oral solid composition can be processed into tablets, capsules or granules, has good stability, can effectively improve a dissolution rate, solves the problem that the existing prulifloxacin oral solid preparation has a slow dissolution speed, and improves bioavailability.

The invention discloses an industrialization production method for Prulifloxacin. By carrying out chlorination on N-Chlorosuccinimide and BF3 to generate an intermediate ethyl 6,7-difuoro-1-methyl-4-oxo-4H-[1,3]thiazete[3,2-a]quinoline-3-carboxylate, the invention not only greatly improves yield, but also avoids utilization of poisonous and volatile chlorosulfonic acid or sulfonyl chloride, and is suitable for the industrialization production.

Prulifloxacin has low bioavailability due to poor water solubility. The invention relates to a novel prulifloxacin mesylate and a preparation thereof, a kit comprising an antibiotic preparation of the novel prulifloxacin mesylate, and application of the novel prulifloxacin mesylate in preparing an anti-bacterial infection medicine. Specifically, the invention particularly relates to a novel preparation for injection of a medicine, with a chemical name of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxole-4-yl)-methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-mesylate, which can be stably stored. Prulifloxacin is directly injected for administration in the form of thiabutyldine quinoline mesylate, so that the solubility, bioavailability and curative effect of prulifloxacin are improved.

The invention provides a dispersible tablet preparation containing antiseptic Prulifloxacin, wherein the constituents of the preparation include Prulifloxacin, lactose, crystalline cellulose, sodium carboxymethylstarch, polyvidone and talcum powder.

The invention provides a dispersible tablet containing an antibacterial agent prulifloxacin and a preparation method thereof. The preparation is composed of: prulifloxacin, microcrystalline cellulose-101, low-substituted hydroxypropyl cellulose, aspartame, Magnesium stearate, PVPk30; Its weight ratio is: prulifloxacin 120-160 parts, microcrystalline cellulose-101 260-320 parts, low-substituted hyprolose 24-40 parts, aspartame 24- 30 parts, PVPk3013-22 parts, magnesium stearate 5-6 parts. The dispersible tablet prepared by the invention greatly improves the dissolution rate after taking, improves the bioavailability, improves the compliance of patients, and is especially suitable for patients who have difficulty in swallowing solids.