34 results about "Lafutidine" patented technology

The invention relates to a lafutidine gastric-retention controlled-release composite belonging to the field of pharmaceutic preparations. The lafutidine gastric-retention controlled-release composite is characterized by comprising the following components in percentage by weight: 5%-20% of the lafutidine, 10%-40% of framework materials, 10%-30% of assistant bleaching agents, 5%-15% of foaming agents, 5%-15% of filling agents and 0.5%-10% of lubricating agents. The composite has reasonability and simple preparation process; compared with same pharmaceuticals, the lafutidine gastric-retention controlled-release composite has little dose, good tolerance, little side effect, and the like; and in addition, compared with the conventional tablets, the lafutidine gastric-retention controlled-release composite enhances the solubility of lafutidine, prolongs the action time (prolonged from 2-3 hours to 5-6 hours) on the upper parts of a stomach and a small intestine, promotes the absorption, enhances the bioavailability, reduces the pharmaceutical usage times, achieves the maximum treatment effect through minimum doses, reduces the concentration change of peaks and valleys and has good patient compliance.

The invention relates to a method for preparing lafutidine by virtue of aminolysis. The method comprises the following steps: reacting a compound shown in a formula 2 or a pharmaceutically acceptable salt thereof with amine RNH2 so as to generate a compound shown in a formula 5, wherein R represents hydrogen, linear-chain or branched C1-4 alkyl, phenyl or C1-4 alkyl substituted phenyl; reacting the compound shown in the formula 5 with the amine RNH2 so as to obtain a compound shown in a formula 3, wherein R represents hydrogen, linear-chain or branched C1-4 alkyl, phenyl or C1-4 alkyl substituted phenyl; condensing the compound shown in the formula 3 and a compound shown in a formula 4 so as to obtain the lafutidine; and optionally, converting the obtained lafutidine into a pharmaceutically acceptable salt of the lafutidine.

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 present invention is Lafutidine injection for intravenous injection and intramuscular injection. The recipe of the Lafutidine injection includes Lafutidine, organic solvent, surfactant, antioxidant, osmotic pressure regulator and water for injection. Compared with Lafutidine tablet, the Lafutidine injection has fast effect, short peak reaching time in the blood high medicine concentration andhigh treating effect; and compared with Famotidine or Ranitidine injection, the Lafutidine injection has less dosage and higher curative effect in treating gastric ulcer.

The invention relates to a synthesis method of 2-chloro-4-(piperidylmethyl)pyridine, belonging to the field of medicine synthesis. The method comprises the following steps: dropwisely adding a nitrite water solution into acid and 2-amino-4-methylpyridine to react, thereby obtaining a white solid product; adding POCl3 into the white solid to obtain a compound 2-chloro-4-methylpyridine; dropwisely adding SO2Cl2 into the compound 2-chloro-4-methylpyridine while adding a free-radical initiator batch by batch, and distilling under reduced pressure to obtain a compound 2-chloro-4-chloromethylpyridine; and condensing the 2-chloro-4-chloromethylpyridine and piperidine to obtain the 2-chloro-4-(piperidylmethyl)pyridine. Compared with the traditional synthesis method of 2-chloro-4-(piperidylmethyl)pyridine, the synthesis method provided by the invention has the advantages of simpler steps (only three steps) and lower cost of raw materials, and the total yield is higher than 32%. Generally, the invention can greatly lower the synthesis cost of lafutidine.

The invention relates to a reducing preparation method for lafutidine, which comprises the following steps: reducing a compound shown in formula 2 or a pharmaceutically acceptable salt thereof with a reducing agent to obtain a compound shown in formula 5; heating to decompose the compound shown in formula 5 to obtain a compound shown in formula 3; carrying out condensation reaction on the compound shown in formula 3 and a compound shown in formula 4 to obtain lafutidine; and optionally converting the obtained lafutidine into a pharmaceutically acceptable salt thereof.

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 discloses a method for detecting ranitidine hydrochloride, cimetidine, famotidine, nizatidine and lafutidine. The method comprises the following steps: (1) selecting chromatographic conditions; (2) selecting mass spectrometric conditions; (3) preparing a standard solution; (4), preparing samples; (5), detecting and calculating. Tests prove that the method is rapid and high in specificity; the method is suitable for detecting the illegally added ranitidine hydrochloride, famotidine, lafutidine, nizatidine, cimetidine and other chemical medicines in Chinese patent medicines and health-care foods which have the effects of invigorating the stomach, improving the gastrointestinal function (having an auxiliary protection effect on gastric mucosal injury) and having an auxiliary protection effect on gastric mucosal injury or in other foods illegally claimed to have said functions.

The invention belongs to the technical field of a medicine, and particularly relates to a lafutidine crystal compound shown in a formula (I). An X-ray powder diffraction spectrum obtained by using a Cu-K alpha ray is shown in a figure 1. The lafutidine crystal compound provided by the invention is a novel lafutidine crystal compound different from that in the prior art, the novel lafutidine crystal compound has improved solubility in water while the preparation prepared by adopting the novel lafutidine crystal compound disclosed by the invention has good bioavailability in comparison with the prior art.

The invention provides a lafutidine composition freeze-dried powder injection for injection and relates to the field of medicines and medicine manufacturing technique. The lafutidine composition freeze-dried powder injection includes the following raw materials: by weight, 8.34-9.21 parts of lafutidine, 3.75-5.56 parts of chitosan nanoparticles and 87.23-88.13 parts of water for injection. The invention has the following advantages: 1) the composition composed of lafutidine and chitosan nanoparticles according to the ratio of 1:0.5 can raise water solubility of lafutidine and shorten dissolution time of lafutidine, has good stability, has few insoluble particles, and is beneficial to be used in clinic; 2) the composition can promote reproduction of beneficial bacteria in the intestine, inhibit growth of harmful bacteria and achieve the effect of absorbing nutrients, has antiacid and anti-ulcer activities, can prevent medicinal stimulation of the stomach, has better anti-Hp performance, promotes ulcer healing, minimizes recurrence, has high healing rate of mice, and can be used to reduce dosage of lafutidine in clinic and decrease adverse reaction of lafutidine; and 3) the chitosan nanoparticles can replace mannitol to be used as a freeze-drying skeleton agent of the freeze-dried powder injection so as to eliminate the active effect of mannitol on human body.

The present invention discloses a lafutidine chewing tablet and a preparation method thereof, the lafutidine chewing tablet is prepared from lafutidine, a filler, a flavoring agent, a binder, a coating agent and a lubricant; the lafutidine chewing tablet is a highly-efficient long-acting H2 receptor antagonist, has obvious inhibitory effect on gastric acid secretion, can inhibit gastric acid secretion caused by histamine, pentagastrin, food and the like, has gastric mucosal protective effect, has dose-dependent inhibition effect on the formation of a variety of experimental animal ulcer models, promotes ulcer healing, relieves symptoms and prevents ulcer recurrence. The lafutidine chewing tablet is easy to take, can promote drug dissolution and absorption in the body, even in a water deficiency state, can ensure medication on time, is especially suitable for the elderly, children, stroke patients, and patients with poor gastrointestinal functions and swallowing difficulties, and may reduce gastrointestinal tract drug burdens.

The invention relates to the field of medicine preparation, in particular to a lafutidine tablet and a preparation method thereof. The preparation method of the lafutidine tablet comprises the following steps: enabling lafutidine raw materials subjected to pretreatment to be mixed with a binding agent, an internal disintegrant and a filling agent and then carrying out fluidized drying; and then mixing with an external disintegrant and a lubricant to carry out tabletting and coating. The particle size range D10 of the lafutidine raw materials subjected to the pretreatment is 1.015-2.16 mu m, D50 is 2.684-7.367 mu m, and D90 is 4.325-52.8 mu m. By the preparation method, the prepared lafutidine tablet can be guaranteed to have good stability, the dissolution curve is similar to that researched originally, and the preparation process is low in energy consumption and pollution, and is green and environmentally friendly.

The invention relates to a compound containing Lafutidine and a preparation containing Lafutidine. The compound comprises Lafutidine, lactose, tween-80, hydroxypropyl cellulose and talcum powder. Compared with the prior art, the compound is evidently faster in capsule dissolution rate and low in impurity content. In addition, the results of various detection of the compound meet the specification.

The invention relates to a preparation method for lafutidine, and the technology comprises the following steps: preparing 4-[4-(piperidine-1-group-methylene)pyridine-2-group-oxygen]-2(Z)-butylene-1-amine and preparing 2-(2-furans methyl sulfoxide group)acetate, then dissolving 2-(2-furans methyl sulfoxide group)acetate into methylene chloride at the room temperature, and then adding a methylene chloride solution possessing 4-[4-(piperidine-1-group-methylene)pyridine-2-group-oxygen]-2(Z)-butylene-1-amine at the room temperature, stirring and separating to obtain lafutidine. The preparation method of lafutidine of the invention modifies the original route, wherein the reaction is milder and easy to operate without using sodium hydride, the intermediate fragment employs a nontoxic and innocuous molybdenum tungsten metal for catalyzing, the reaction condition is milder, the environmental pollution can be reduced and the reaction cost can be decreased.

The invention relates to the technical field of oral solid preparation analysis, and provides a method for detecting the content of lafutidine tablets, which adopts a high performance liquid chromatography to detect the content of each component in the lafutidine tablets. Chromatographic conditions of the high performance liquid chromatography are as follows: a mobile phase is a mixed solution of acetonitrile and a phosphate buffer solution added with sodium pentanesulfonate in a volume ratio of (10: 90)-(20: 80); the column temperature is 35-45 DEG C; the detection wavelength is 250nm to 300nm, and the preparation range of detectable sample concentration is 50mu g/ml to 150mu g/ml. According to the method for detecting the content of the lafutidine tablets, the content of each substance in the lafutidine tablets is measured through a high performance liquid chromatography external standard method, chromatographic conditions are optimized, efficient detection of the content of each substance in the lafutidine tablets is achieved, the method is good in reproducibility, easy to operate, high in accuracy and low in requirement for a chromatographic column, and the method is suitable for industrial production. The separation degree, the durability and the reproducibility are good.

The present invention relates to an anti-peptic ulcer drug lafutidine composition and a preparation method thereof. The composition is prepared from the following components, by weight: 5-20% of lafutidine, 70-95% of a filler, 0-15% of a disintegrating agent, 0-5% of a lubricant, 0-5% of a surfactant, an appropriate amount of a binder, and 1-10% of a coating material. The preparation method is a wet granulation tableting method. The prepared lafutidine composition has characteristics of reliable quality, stable property, simple production process, meeting of requirements of large-scale preparation production, and low cost.