434 results about "Omeprazole" patented technology

The invention relates to an omeprazole enteric micropill capsule and a process for preparing the same. The content of the capsule is omeprazole enteric micropill including a blank pill core; an activity medicine layer having an alkaline component; a separator containing magnesia and titanium pigment; and an enteric coat layer. According to synergistic reaction, stability of the medicine is distinctly improved. The omeprazole enteric micropill capsule of the invention has period of validity of the preparation to three years or more.

PCT No. PCT/SE98/00922 Sec. 371 Date Jun. 8, 1998 Sec. 102(e) Date Jun. 8, 1998 PCT Filed May 18, 1998 PCT Pub. No. WO98/53803 PCT Pub. Date Dec. 3, 1998An enteric coated oral pharmaceutical formulation comprising as active ingredient a compound selected from the group of omeprazole, an alkaline salt of omeprazole, the (-)-enantiomer of omeprazole and an alkaline salt of the (-)-enantiomer of omeprazole, wherein the formulation comprises a core material of the active ingredient and optionally an alkaline reacting compound, the active ingredient is in admixture with a pharmaceutically acceptable excipient, such as for instance a binding agent, and on said core material a separating layer and an enteric coating layer. A hydroxypropyl methylcellulose (HPMC) of low viscosity with a specific cloud point is used in the manufacture of pharmaceutical formulations. Furthermore, the application describes the processes for their preparation and the use of the claimed formualtions in medicine.

The present invention relates to a novel form of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole, known under the generic name omeprazole. More specifically, it relates to a novel crystalline form of the potassium salt of the (S)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole. The present invention also relates to processes for preparing such a form of the potassium salt of (S)-omeprazole and pharmaceutical compositions containing it.

A stable pharmaceutical composition of omeprazole for oral administration which consists essentially of: (a) a core of Omeprazole or a pharmaceutically equivalent salt, a filler and an alkaline material selected from the group consisting of lysing and arginine; and (b) a single layer of coating on said core which comprises a layer of an enteric coating agent which is applied from an organic solvent based system.

An improved process of synthesis of 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl-1H-benzimidazole (omeprazole) by oxidation of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole with 3-chloroperoxy-benzoic acid in ethyl acetate wherein omeprazole is poorly soluble, at a temperature between -10° C. and 5° C. is disclosed. The second step is a purification of the crude product by dissolution and reprecipitation of the final product.

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.

An enteric or slowly-released composition of omeprazole is prepared from omeprazole, the buffer substance for neutralizing gastric acid and improving the stability of omeprazole, and the pharmacologically acceptable assistant.

The present invention is directed to methods, kits, combinations, and compositions for treating, preventing or reducing the risk of developing a gastrointestinal disorder or disease, or the symptoms associated with, or related to a gastrointestinal disorder or disease in a subject in need thereof. In one aspect, the present invention provides a pharmaceutical composition comprising a proton pump inhibiting agent and a buffering agent for oral administration and ingestion by a subject. Upon administration, the composition contacts the gastric fluid of the stomach and increases the gastric fluid pH of the stomach to a pH that substantially prevents or inhibits acid degradation of the proton pump inhibiting agent in the gastric fluid and allows a measurable serum concentration of the proton pump inhibiting agent to be absorbed into the blood serum of the subject.

The invention relates to an industrial method for refining esomeprazole sodium salt. The method is mainly characterized by comprising the following steps of: suspending the esomeprazole sodium salt in a hot poor solvent in an amount which is 1 to 10 times weight of the esomeprazole sodium salt, slowly adding a good solvent such as methanol and ethanol in an amount which is 0.5 to 1.5 times weightof the mixture, filtering while heat to obtain a clarified solution, cooling to room temperature, separating out a solid, filtering, washing and performing vacuum drying. The method is easy and convenient to implement, and inorganic impurities and organic impurities contained in the crude product of esomeprazole sodium salt, including a peroxide sulphone impurity and an R-esomeprazole impurity can be effectively removed. The esomeprazole sodium salt refined by the method has the content of over 99.5 percent, and has the single impurity content of less than 0.1 percent.

The invention belongs to the technical field of traditional Chinese medicine preparation method, and provides a preparation method of a traditional Chinese medicine used for treating gastritis caused by insufficiency of spleen-yang. According to prior arts, gastritis caused by insufficiency of spleen-yang is commonly treated by using omeprazole, which causes adverse reactions. The technical scheme of the invention is that: traditional Chinese medicines of ginseng, human milk, common jujube, common yam rhizome, wheat, different leaves pseudostellaria root tuber, balck-bone silky fowl, wild cabbage, dried longan pulp, largehead atractylodes rhizome, radix paeoniae alba, American ginseng, ligusticum, lotus seed, pilose asiabell root, sharpleaf galangal fruit, mongolian milkvetch root, Siberian solomonseal rhizome, nonglutinous rice, edible bird nest, dried ginger, bayberry, garden radish seed, carica papaya, roof iris rhizome, carrot, buckwheat, medicated leaven, cydonia oblonga mill, cerealose, honey, and licorice are soaked in water, and are decocted by using a mild fire; the obtained solution is filtered, a slag is removed, and the obtained medicine liquid is the traditional Chinese medicine used for treating gastritis caused by insufficiency of spleen-yang. The method is advantaged in that: the preparation method is simple; toxic and side-effects of the traditional Chinese medicine liquid are low; a treatment course is short; and a recovery rate is high. According to the invention, a good effect can be obtained with the cooperation of monarch and minister medicines. A traditional Chinese medicine preparation is adopted, such that adverse reactions, allergic reactions and toxic reactions caused by western medicines are avoided.

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 discloses a kind of enteric omeprazole micropill preparation and its preparation process. The enteric omeprazole micropill preparation has core of omeprazole or its single antimer subsalt as the active component and excipient and middle isolating coating and enteric protecting layer to coat the core. The enteric omeprazole micropill preparation is prepared directly with the main medicine component and supplementary materials including magnesia as the stabilizer, hydroxypropylmethyl cellulose and talcum powder.

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 present invention relates to a delayed release drug delivery system containing omeprazole capable of site-specific delivery and pulsatile (bolus) kinetics for once-a-day dosage comprised of an alkaline core structure sequentially layered with suspensions of omeprazole; a separation barrier; and an enteric barrier. The separation barrier is coated with a pH-dependent enteric membrane, which is relatively insoluble in gastric fluid but rapidly to immediately soluble in intestinal fluid, whereby the drug is released in a pulsatile manner in the proximal segment of the gastrointestinal tract.

The invention provides a method for preparing S-Omeprazole and salt thereof by the resolution of racemic modification Omeprazole by an inclusion resolution method, the resolution regent of the inclusion resolution method is (S)-(-)-1, 1'-binaphthyl-2, 2'-diphenol, by adding S-Omeprazole and S-1, 1'-binaphthyl-2, 2'-diphenol inclusion complex seed grains at the temperature of 60 to 70 DEG C, the inclusion complex is obtained, then the inclusion complex is processed by the hydroxid aqueous solution of alkali metals to obtain the S-Omeprazole with high ee value, the S-Omeprazole and salt thereof obtained by the method have high ee value which is more than 99.2 percent, and the obtained S-Omeprazole has the color of kind of white, high yield and small pollution to the environment, and is suitable for industrial production.

The present invention discloses the chromatographic separation process of omeprazole antimer in simulated mobile bed. In a simulated mobile bed chromatographic system with chiral fixed phase of cellulose triphenyl carbomate and flow phase of the mixture of ethanol, n-hexane and diethylamine, mixture of R-(+)-omeprazole and S-(-)-omeprazole is separated to obtain high purity S-(-)-omeprazole. Said separation process is a continuous process, so that the present invention has high automation, high production efficiency, low solvent consumption and no toxic solvent.

The invention provides an omeprazole enteric coated tablet and a preparation method thereof. The enteric coated tablet is formed by an inner tablet core and an outer enteric coating, wherein the inner tablet core takes omeprazole as active constituent. No protective isolating layer is arranged between the tablet core and the enteric coating. The inner tablet core is made of omeprazole cyclodextrin inclusion compound and other pharmaceutically acceptable auxiliary materials. The enteric coating contains no plasticizer and the dosage of the enteric coating accounts for 5 percent to 15 percent of the weight of the tablet. The invention has the advantages that the stability and the dissolution of omeprazole are improved, the dosage of basic materials and the dosage of all kinds of inert auxiliary materials are greatly reduced, omeprazole can be stably and rapidly released in the intestinal tract and the bioavailability is improved.

The invention discloses a compound omeprazole capsule, and a preparation method and a detection method thereof. The capsule is prepared by: in parts by weight, 20 parts of omeprazole, 1100 parts of sodium bicarbonate, 30 parts of cross linked sodium carboxymethyl cellulose and proper amount of magnesium stearate; or the capsule is prepared by 40 parts of omeprazole, 1100 parts of sodium bicarbonate, 30 parts of cross linked sodium carboxymethyl cellulose and proper amount of magnesium stearate. Aiming at the deficiency of the prior art The formulation, the preparation technology and the detection method of the conventional compound omeprazole capsule are optimized, the compound omeprazole capsule of the invention exhibits more substantial curative effect for diseases comprising peptic ulcer, gastroesophageal reflux disease and the like caused by gastric hyperacidity; a systematic, integrated and effective component discrimination and content determination method is established, thereby the medicine quality is effectively controlled, and thus the clinic curative effect is guaranteed.

The present relates to a stable pharmaceutical composition comprising as an active component thereof one or more known 2-[(2-pyridyl)]-methylsulphinyl]benzimidazole derivatives

The invention discloses a preparation method for esomeprazole magnesium trihydrate, and the preparation method comprises the following steps: 1) taking omeprazole sulfide, then adding a chiral ligand, a catalyst and an organic solvent, heating and mixing for reaction, so as to form a chiral omeprazole sulfide compound; 2) adding an inorganic oxidant for oxidation reaction, and oxidizing omeprazole sulfide into esomeprazole; 3) adding inorganic base aqueous solution, extracting so as to enable the esomeprazole, obtained in the step 2), to form an esomeprazole inorganic salt, and dissolving the esomeprazole inorganic salt into the inorganic base aqueous solution layer; 4) adding inorganic magnesium salt into the inorganic base aqueous solution layer, stirring for reaction, and then carrying out centrifugation and drying, thus obtaining the esomeprazole magnesium trihydrate. The preparation method has the advantages of being high in product purity, high in yield, simple in technique, high-efficiency, environment-friendly, low in cost and the like.

The invention relates to an omeprazole enteric micro-pellet, a capsule and a preparation method of the omeprazole enteric micro-pellet. The omeprazole enteric micro-pellet specifically comprises a pill core, an isolating layer coating and an enteric coating, wherein the pill core is prepared from the following components in percentage by weight: 10 to 13 percent of omeprazole, 82 to 87 percent offiller, 2 to 5 percent of an adhesive, 0.4 to 0.8 percent of a surfactant and 0.4 to 0.8 percent of an alkaline stabilizer; the isolating layer coating is prepared from hydroxypropyl methylcellulose and talcum powder of which the weight ratio is 4 to 1, and the coating weight gain rate is 5 to 10 percent; the enteric layer coating is prepared from eudragit L30D-55, triethyl citrate and talcum powder of which the weight ratio is 1 to 0.1 to 0.1, and the coating weight gain rate is 25 to 30 percent.

The invention relates to the field of pharmaceutical preparations, in particular to a method for preparing an omeprazole enteric fast-release tablet, which is characterized in that in the preparing process with a conventional method, omeprazole is dispersed in binding agent suspension solution, the mixture is granulated by a fluidized bed through top spraying, and the grain size is between 80 and 120 meshes. Besides, a sealing coat of the omeprazole enteric fast-release tablet comprises a first sealing coat and a second sealing coat, wherein the first sealing coat contains hydroxypropyl methylcellulose and a basifier, and the second sealing coat contains the hydroxypropyl methylcellulose, smoothers and titanium dioxide. An in vitro dissolution experiment shows that the omeprazole enteric fast-release preparation prepared by the method is dissolved for 100 percent at the 15th minute; and an acid resistance test shows that a coating tablet has no obvious change in two hours in an environment of which the pH is 1.2.