132 results about "Esomeprazole" patented technology

The present invention relates to an oral pharmaceutical preparation for use in the prevention and/or reduction of gastrointestinal complications associated with the use of acetyl salicylic acid. The present preparation comprises a fixed oral dosage form comprising a proton pump inhibitor in combination with acetyl salicylic acid. Furthermore, the present invention refers to a method for the manufacture thereof and the use thereof in medicine. The present invention also relates to a specific combination comprising esomeprazole, or an alkaline salt thereof or a hydrated form of any one of them, and acetyl salicylic acid for use as a medicament for the prevention of thromboembolic vascular events, such as myocardial infarction or stroke, and for the prevention and/or reduction of gastrointestinal complications associated with the use of acetyl salicylic acid.

The invention discloses a method for synthesizing and refining salt of esomeprazole. According to the method, 2-sulfydryl-5-methoxyl-1H-benzimidazole is used as an initiative raw material for reaction, and a reaction condition is optimized, so that reaction is performed under a mild condition, and the content of impurities in the product is reduced effectively. After the synthesized product is refined further, the purity and enantiomer excess of the product are over 99 percent, so that the effect and safety of administration are improved.

The present disclosure is directed to drug dosage forms that release an agent that raises the pH of a patient's gastrointestinal tract, followed by a non-steroidal anti-inflammatory drug. The dosage form is designed so that the NSAID is not released until the intragastric pH has been raised to a safe level. The disclosure also encompasses methods of treating patients by administering this coordinated release, gastroprotective, antiarthritic/analgesic combination unit dosage form to achieve pain and symptom relief with a reduced risk of developing gastrointestinal damage such as ulcers, erosions and hemorrhages.

This invention relates to an oral dosage form of a pharmaceutically active ingredient comprising: (a) an outer capsule and (b) non-uniform pellets, having a non-uniform shape and/or size, contained within the capsule, wherein the pellets comprise a compressed powder comprising a pharmaceutically active ingredient. In one embodiment the active ingredient is selected from the group consisting of doxycycline, omeprazole, esomeprazole, and propafenone. Pharmaceutical formulations of the active ingredients as well as methods and tools for making the oral dosage form are also described.

The invention provides application of a cyclohexanone monooxygenase characterized by high catalytic activity, high reaction yield, and environmental friendliness to asymmetric oxidation reaction to synthesize single-configuration prazole drugs. The invention also provides a gene of the cyclohexanone monooxygenase, a recombinant expression vector containing the gene, a recombinant expression transformant and an efficient preparation method of the cyclohexanone monooxygenase, and application of the cyclohexanone monooxygenase in catalysis of a prochiral thioether compound into single-configuration sulfoxide.

The present invention relates to a process for preparing substituted sulfoxides either as a single enantiomer or in an enantiomerically enriched form. Thus, racemic omeprazole is reacted with (S)-camphorsulfonyl chloride to form a diastereomeric mixture and the diastereomers are separated by fractional crystallization, followed by deprotection to give esomeprazole.

A stick of gum is provided containing therapeutic benefits of non-steroid anti-inflammatory drugs for inflammation in conditions such as arthritis, and also alleviates subsequent side effects of NSAID administration, as well as antacid effects from compounds such as an H2 antagonist (ranitidine, cimetidine, famotidine) and/or a proton pump inhibitor (such as lansoprazole, pantoprazole, omeprazole, esomeprazole or rabeprazole) and/or an acid pump antagonist selected from the group of soraprazan, AZD0865, YH1885 and CS-526.

The invention discloses cyclohexanone monooxygenase and an application thereof, in particular cyclohexanone monooxygenase obtained by site-specific mutagenesis and an application thereof. Compared with a SEQ ID NO: 1, the amino acid sequence of the cyclohexanone monooxygenase has gene mutation in at least one site as follows: serine Ser at the 386th site is mutated to asparagines Asn, and serine Ser at the 435th is mutated to threonine Thr. Experiments show that the cyclohexanone monooxygenase disclosed by the invention can catalytically convert a high concentration omeprazole thioether primerinto esomeprazole.

The invention adopts 2-chloromethyl-4-nitryl-3, 5-dimethyl pyridine hydrochloride and 5-methoxyl-2-mercapto benzimidazole as starting materials to prepare esomeprazole salt by condensation, asymmetric oxidation and methoxidation. A preparation method has the advantages that the repeatability is good, the operation is simple, and the industrial production is easy; and the preparation conditions are moderate, the generation of impurities such as nitric oxide and sulphone is reduced in the preparation process, and the yield and the purity of the esomeprazole salt are increased.

A combination preparation for remedying the gastroesophageal reflux disease (GERD) and the functional dyspepsia is characterized in that the prescription of the combination preparation consists of a proton pump depressor and a gastrointestinal power drug of itopride; the proton pump depressor is selected from one of a Pantoprazole, a Omeprazole, a Esomeprazole, a Lansoprazole, a Rabeprazole, a Tenatoprazole and a Leminorazole, wherein the Pantoprazole is preferential, and at the same time the neutral form of the basic salt of the proton pump depressor is also included, such as Na^plus, Mg^2plus, Ca^2plus, K^plus or Li ^plus salt and a pure optical stereoisomer of the proton pump depressor or an active metabolite of the proton pump depressor; the gastrointestinal power drug is the itopride and a ramification of the itopride or one of the medicinal salts of the itopride; in the combination preparation, the weight ratio of the Pantoprazole and the itopride is 2 to 5 to 2 to 7. The invention has important affect for remedying the gastroesophageal reflux disease and the functional dyspepsia, and the preparation method of the invention is simple and convenient; the cost is low; the invention is fit for being orally taken by the patient; the invention has good conformance performance, high curative effect, low recrudescence rate and little adverse reaction.

The invention discloses a method for preparing esomeprazole, belonging to the technical field of medicine. According to the invention, 2-chloromethyl-4-methoxy-3,5-dimethylpyridine hydrochloride and 2-mercapto-5-methoxybenzimidazole are used as starting materials and are subjected to condensation and oxidation so as to prepare an esomeprazole salt. The method has good reproducibility, and is simple to operate, easy for realizing industrial production and mild in preparation conditions; and the production of impurity nitrogen oxide and sulfone (peroxide) during the preparation is reduced, and the yield and purity of the esomeprazole salt are improved.

The present invention relates to new salts of omeprazole and esomeprazole respectively, i.e. salts of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole and the (S)-enantiomer thereof. More specifically, the present invention relates to alkylammonium salt of the compounds, formed by a reaction of omeprazole and esomeprazole respectively and an alkylamine with formula NR?1#191R?2#191R?3#191 wherein R?1#191 is a linear, branched or cyclic C?1#191-C?12#191-alkyl group, R?2#191 and R?3#191 are hydrogen. The present invention also relates to a process for preparing crystalline salts, a pharmaceutical preparation and a method for treatment of gastric related disorders by administering the compound of the invention.

The invention discloses an esomeprazole medicated pellet and a preparing method of the esomeprazole medicated pellet. The esomeprazole medicated pellet is mainly prepared from 25-50% of esomeprazole raw material and ramification of the esomeprazole raw material, 20-50% of mannitol and 5-30% of polyvinylpolypyrrolidone according to weight percentage; and in addition, pharmaceutic adjuvant acceptable pharmaceutically is also contained. The ingredients of the esomeprazole medicated pellet are proportioned, and the esomeprazole medicated pellet product can be prepared by virtue of an extruding-rolling preparing method. Compared with the prior art, the technical scheme provided by the invention has the advantages that the efficiency is greatly improved, and waste of a large amount of time, manpower and material resources are avoided; and the method is simple, and the midbody of the obtained product preparation has the advantages of stable medicine, high reproducibility and the like.

The invention relates to a preparation method for esomeprazole enteric pellet tablets. The method comprises the following steps of: preparing esomeprazole enteric pellets, and preparing mixed tablets of the pellets and excipient; the esomeprazole enteric pellets contain active pharmaceutical pellet cores, isolation layers and enteric coatings; the esomeprazole enteric pellets prepared by the method have certain elasticity and are pressureproof; the esomeprazole enteric pellets and the excipient are pressed to form tablets, so that the pellets can be isolated from air, and are more stable than pellet capsules; the validity period can reach over three years; and the esomeprazole enteric pellet tablets have the advantages of small size, dividable dose and the like, and the compliance of a patient is improved.

The invention relates to a novel method for preparing esomeprazole and sodium salts, magnesium salts, lithium salts, potassium salts, calcium salts and ammonium salts thereof. The esomeprazole is prepared by oxidizing omeprazole sulfide; and an oxidant is a chiral camphorsulfonyloxaziridine compound. The method comprises the following steps of: dissolving the omeprazole sulfide into a solvent, adding an alkaline reagent, stirring for 30 to 90 minutes at room temperature, adjusting the temperature to -30 to 200 DEG C, adding the oxidant, namely the chiral camphorsulfonyloxaziridine compound, and stirring and reacting for 0.5 to 20 hours to obtain the esomeprazole. In the method, a chiral ligand and a metal compound are not required to be added, the introduction of heavy metals is avoided in the reaction, and the chiral camphorsulfonyloxaziridine compound which participates in the oxidation reaction can be recycled, so that the utilization rate of the oxidant is remarkably improved and the production cost is remarkably reduced; and the prepared esomeprazole in high in purity and yield.

The invention relates to a new method for synthesizing esomeprazole through asymmetrically catalytic oxidation. The method is characterized in that (S,S)-6,6'-dyhydroxy-2,2'-biphenyl dicarboxylate is used as a chiral ligand inducer, compounds containing molybdenum are used as catalyst, isopropyl hydrogen peroxide is used as oxidant, high-content and high-optical-purity esomeprazole which is a single enantiomer of omeprazole is obtained through room-temperature catalytic oxidation of prochiral thioether compounds, and corresponding alkali metal salts of esomeprazole can be further obtained through reaction with alkali inorganic salts. After the esomeprazole and the alkali metal salts thereof obtained by adopting the method are purified, the purity can reach more than 99 percent, the optical purity can reach more than 99.5 percent and the yield can reach more than 75 percent. The method can realize high utilization ratio of raw materials, is simple, convenient and feasible and is suitable for industrial mass production.

The invention belongs to the field of pharmacy and relates to a production method of high-optical-purity esomeprazole salt. The method takes m-chloro peroxy-sodium benzoate as an oxidizing agent and takes an organic solvent which is dissolved into water as a reaction solvent, so that the problem that the acidity of the m-chloro peroxy-sodium benzoate cannot be applied to preparing the esomeprazole is solved. The method is simple to operate and has a low cost; and the optical purify of the prepared product is high and the impurity content is low.

The invention discloses an enzymatic preparation method of esomeprazole. The enzymatic preparation method comprises: carrying out a reaction on omeprazole thioether as a substrate and an oxidizing agent in a solvent under the actions of monooxygenase, an auxiliary component and a phase transfer catalyst to generate esomeprazole. According to the present invention, with the enzymatic preparation method, esomeprazole is efficiently prepared; and by using the phase transfer catalyst, the efficiency of the enzyme catalytic reaction is improved, the reaction time is substantially reduced, the concentration of the reaction substrate is increased, the conversion rate can be up to 99.8%, the production cost is reduced, the single-batch yield is substantially improved, and the excellent industrialapplication value is provided.

The invention belongs to the field of drug preparation, provides a proton pump inhibitor and a preparation method thereof, and especially relates to an application of a water system of amine compound alkalizer in the preparation of stabilizer of esomeprazole free alkali. Besides, the invention provides a stable water system of esomeprazole free alkali, and the system is composed of amine compound alkalizer, esomeprazole free alkali and water medium. On the basis of the water system, an oral instant preparation of esomeprazole is prepared. The preparation has the advantages of stable quality, good taste, rapid absorption, quick effect and user-friendliness, can improve the compliance of the patients, and is especially suitable for the patients when the disease attacks with no water available. The preparation effectively solves the problem that esomeprazole is decomposed by acid, relieves the stimulation to the digestive tract, and increases the stability of the esomeprazole preparation and the safety of clinical application.