34 results about "Lafutidine" patented technology

The invention relates to lafutidine freeze-dried injection, which can treat gastric ulcer, duodenal ulcer and ulcer on the anastomosed part. The lafutidine freeze-dried injection is composed of lafutidine and mannitol, wherein, the mass ratio of the lafutidine and the mannitol is 1 : 10 to 100; the preferable mass ratio is 1 : 20 to 50; and one or the mixture of sodium chloride and citrate can be added into the lafutidine freeze-dried injection so as to prevent the medicine bottle from exploding in the process of freeze-drying the lafutidine freeze-dried injection. The preparation processes are as following: the lafutidine is taken to be placed inside the aseptic container, and then the water for injection is added to be heated until the temperature reaches 70 DEG C so that the lafutidine can be dissolved in the water for injection; and then the mannitol is added to be mixed so that the mannitol can be dissolved and is mixed evenly; the content of the intermediate is measured; after the content of the intermediate is qualified, in the aseptic condition, the solution is filtered until to be clear by microporous membrane of 0.22 microns; the filtrate is filled inside the aseptic silin bottle; and part of the silin bottle is plugged by butyl rubber closure, with the posterior steps of tray filling, freeze-drying in the freeze dryer, tamponing, unpacking, mouth rolling, quality inspecting and packaging.

The invention belongs to the technical field of chemistry and in particular relates to a synthetic method of Lafutidine oxide impurities, namely -2-[(2- furyl methyl) sulfonyl]-N-[4-[4-(1-piperidyl methyl)-2-pyridyl]oxygen-(Z)-2-butenyl] acetamide (formula I). The synthetic method mainly comprises the following steps: 2-(2-furfuryl sulfydryl)acetic acid-(4-nitrophenol) ester, namely the compound II is oxidized and then docked and refined with 4-[4-(N-piperidine methyl) pyridine-2-oxygen] cis-2-butene-1-amine, namely the compound IV to obtain oxide impurities of which the purity is more than 99.5%. The synthesized high-purity Lafutidine oxide impurities are taken as impurity standards for product inspection, thereby being beneficial to strengthening location and qualitativeness of the impurities so as to improve the quality control of Lafutidine active pharmaceutical ingredients.

The invention relates to a novel chemical synthetic method for lafutidine, and in particular relates to a method for preparing the lafutidine from hydroxylamine hydrochloride serving as aminolysis reagent. The method comprises the following steps of: (1) reacting a compound in a formula 4 with the hydroxylamine hydrochloride and sodium hydroxide so as to obtain a compound in a formula 2; (2) carrying out condensation on the compound in the formula 2 and a compound in a formula 3 so as to obtain the lafutidine in a formula 1. The whole preparation process is as shown in the specification. When in preparation of the key intermediate the compound in the formula 2, the hydroxylamine hydrochloride is chosen for substituting other reagents for aminolysis reaction, and the prepared lafutidine product has higher purity and can reach 99.88%; compared with the condition that the aminolysis reagent is removed from the intermediate, the hydroxylamine is easier to remove; and furthermore, the hydroxylamine hydrochloride is a solid reagent, has high purity and high stability, and industrial production is more easily realized.

The invention relates to an anti-peptic ulcer drug lafutidine composition and a preparation method thereof. The lafutidine composition is prepared from the following components in the following weight percentages: lafutidine: 5-20%; filler: 70-95%; disintegrant: 0-15%; lubricant: 0-15% 5%; surfactant: 0‑5%; appropriate amount of binder; coating material: 1‑10%. The preparation method is wet granulation and tabletting. The lafutidine composition prepared by the invention has reliable quality, stable properties, simple production process, meets the requirements of large-scale production of preparations and is low in cost.