133 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 present invention relates to a multiparticulate tablet with improved gastro-protection comprising at least a pharmaceutically active substance in the form of enteric coated particles, and a mixture of tableting excipients, wherein the said mixture of excipients comprising xylitol and / or maltitol, each in a directly compressible form, a disintegrating agent, a lubricant and at least one other diluent and the ratio of a) the xylitol and / or the maltitol to b) the other diluent(s) is less than 5 / 95 (weight / weight) and the result of the “test of integrity of the film” is greater than 95%, preferably greater than 97% and more preferably still greater than 99% and the result of the “release test” is greater than 90%, preferably greater than 95%. According to one embodiment of the invention, the active substance is omeprazole or esomeprazole. According to another embodiment the tablet is a disintegratable tablet, which disintegrate in the mouth with or without chewing. The invention also comprises a process for preparing the claim tablet and its use in medicine.

The invention provides esomeprazole and a preparation method of magnesium trihydrate of the esomeprazole. The preparation method includes the following steps of subjecting racemization omeprazole and inorganic base to acid-base neutralization reaction in an alcoholic solution to obtain racemization omeprazole sodium salt; dissolving omeprazole sodium salt, organic metal coordination agents, chelating agents and organic base in an organic solvent for complex reaction to obtain esomeprazole complex; subjecting S-mandelic acid and the esomeprazole complex to condensation reaction to obtain an esomeprazole mandelate compound; dissolving the esomeprazole mandelate compound in an acetone solution, and performing filtering to obtain S-omeprazole-S-mandelate compound; and suspending the S-omeprazole-S-mandelate compound in a first solvent to obtain a suspension solution, and adjusting potential of hydrogen (pH) of the suspension solution to be 8-10 to obtain the esomeprazole, wherein the first solvent includes 30-32v / v% of an alkaline aqueous solution and 68-70v / v% of an organic solvent. By means of the preparation method, the technical problem that the yield and the purity of the esomeprazole in prior art are low is solved.

Aspects of the invention relate to pharmaceutical formulations comprising an NSAID and acid reducer drug for therapeutic purposes, and methods of preparing the same. Further aspects of the invention relate to fixed dose pharmaceutical formulations comprising naproxen, or pharmaceutically acceptable salts thereof, and esomeprazole, or pharmaceutically acceptable salts thereof.

A stabilized pharmaceutical composition of benzimidazole compounds preferably amorphous form of esomeprazole and a process for preparing the same. The pharmaceutical compositions formulated into solid dosage forms preferably multiple unit tablet dosage forms and capsules and a method for preparing the same.

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.

The present invention relates to a process for stereoselective synthesis of substituted sulfoxides either as a single enantiomer or in an enantiomerically enriched form. Thus, 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]thio]-1H-benzimidazole is reacted with (R)-camphorsulfonyl chloride to form a mixture of 1-(R)-camphorsulfonyl-5- (and 6-)methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methylthio]-1H-benzimidazole, oxidized to obtain a diastereomeric excess of 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole over 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(R)-sulfinyl]-1H-benzimidazole, the diastereomers are separated by fractional crystallization and the separated 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole is deprotected to give esomeprazole.

A method and composition for the transdermal administration of proton pump inhibitors such as substituted pyridyl methylsulfinyl benzimidazoles, and in particular, omeprazole, lansoprazole, esomeprazole, pantoprazole and raberprazole. The method and composition include the use of a hydroxide-releasing agent as a permeation enhancer to increase the flux of the protein pump inhibitor through a patient's skin or mucosal tissues and optionally also include the use of a carrier such as 1,3-butanediol, dipropylene glycol, and hexylene glycol.

The invention discloses a method for preparing an esomeprazole impurity. 5-methoxy-2-[(S)-[(4-chloro-3,5-dimethyl-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole (II) is obtained through demethylation, halogenation, condensation and asymmetric oxidation by taking 2-chloromethyl-4-methoxy-3,5-dimethylpyridine hydrochloride as a starting raw material. According to the method disclosed by the invention,a synthesis route is simple and short, the starting raw material is easy to obtain, the reaction conditions are gentle, the operation is simple and convenient, and the impurity can be obtained withoutcolumn chromatography; the purity of the prepared impurity can be up to 99 percent or above, the ee (Enantiomeric Excess) value can be up to 99 percent or above, and the impurity can be used as reference substance in quality research.

The invention relates to a purification method of esomeprazole. According to the purification method, esomeprazole or salt thereof to be purified is transformed into potassium esomeprazole and then separated by crystallization, and if necessary, the crystallization product is transformed into esomeprazole or salt thereof. Compared with the conventional recrystallization method, the purification method can purify esomeprazole with high efficiency to obtain high-purity esomeprazole or salt thereof. The purification method is particularly suitable for purification of drug compounds with extremely strict requirements on the purity.

The present invention relates to esomeprazole free base or its alkali salt-containing composition which stability is improved and is easy to manufacture.