223 results about "Pantoprazole" patented technology

An oral pharmaceutical composition comprises an acid-labile irreversible proton pump inhibitor in pellet or tablet form, wherein the irreversible proton pump inhibitor is at least partly in slow-release form. On combined administration with an anti-microbially-active ingredient, the composition is distinguished by imparting an enhanced action of rapid onset against disorders caused by Helicobacter.

The invention relates to the dihydrate of the magnesium salt of pantoprazole.

Pantoprazole sodium multiparticulates are described which avoid sticking to nasogastric and gastronomy tubes. The pantoprazole multiparticulates have a spheroid core of pantoprazole or an enantiomer thereof, or a salt thereof, a surfactant, and a distintegrant; a sub coat which is comprised of hydroxypropyl methylcellulose (hypromellose) and water, an enteric coat on the sub-coat, and a final seal coat over the enteric coat, which is composed of hydroxypropyl methylcellulose (hypromellose) and water.

The invention aims at providing a pantoprazole sodium freeze-dried powder injection and comprises pantoprazole sodium and mannitol with the weight ratio of 1: 2 to 5. The invention is simple in formula and little in side effect; products prepared by the method are plump in appearance, good in complex solubility and excellent in quality with the adoption of an advanced freezing and drying process.

The invention relates to a method for preparing batoracosodium freeze dried, whose pH value is 9.5-11.5. And the invention comprises 1 deal of batoracosodium, 0.5-1 deals of supporting agent, 0-0.06 deals of weak-acid strong-alkali salt, and some inorganic alkali. And the preparation comprises that 1, preparing materials; 2, dissolving the supporting agent and weak-acid strong-alkali salt via injection water, using inorganic salt to adjust the pH value to 9.5-11.5, adding batoracosodium, dissolving and using inorganic salt to adjust the pH value to 9.5-11.5; 3, filtering; 4, freezing and drying to obtain the final product. The invention can be used treat peptic ulcer, ulcer bleed, or the like.

A freeze-dried powder injection of pantorazole sodium is proportionally prepared from pantorazole sodium, excipient, weak-acdic strong-alkaline salt, edathamil disodiumk, and inorganic alkali.

The invention provides a novel method for preparing optically pure substituted [(pyridyl methylene) sulfinyl]-1H-benzimidazole sulphoxide compound by enantioselective synthesis. The method requiring protection is to directly and asymmetrically oxidize prochiral thioether into a corresponding optically pure sulphoxide compound or a sulphoxide compound rich in single enantiomer by a mild and cheap oxidizing agent in the presence of a complex compound catalyst formed by an accessible and stable (+)- or (-)- tartaric acid diamide ligand shown in a general formula and titanium. Therefore, optically pure omeprazole, lansoprazole and pantoprazole can be obtained, wherein R8, R9, R10 and R11 are the same or different, and are selected from hydrogen, alkyl, aralkyl, aryl, organic polymers or a silica loading body.

Dosage forms for the oral administration of the magnesium salt of (S)-pantoprazole are described.

The invention relates to a pantoprazole sodium enteric-coated tablet and a preparation method thereof. The enteric-coated tablet is prepared by a pantoprazole sodium plain tablet which is coated with an insulating layer and an enteric coating layer, and the pantoprazole sodium plain tablet contains 0.5 to 5 percent of silicon dioxide and 0.5 to 5 percent of talcum powder. The method solves the tablet pressing problem of extremely easy sticking during the pressing of the pantoprazole sodium plain tablet.

The invention discloses a pantoprazole sodium enteric-coated pellet which contains the following components in percentage by weight from inside to outside: 20-60 percent of blank core pellet, 4-38 percent of medicinal layer containing pantoprazole sodium and one or more medicinal excipients, 2-15 percent of isolated layer and 15-26 percent of enteric-coated layer. The invention also discloses a preparation method and an application of the enteric-coated pantoprazole sodium pellet. The pantoprazole sodium enteric-coated capsule has the advantages of better stability, uniform absorption, smaller difference of bioavailability among individuals, and the like.

The invention provides a method for preparing (L)-pantoprazole sodium, which comprises the following steps of: oxidizing 5-difluoromethoxy-2-{[(3,4-dimethoxy-2-pyridinyl)methyl]thio}-1H-benzimidazole by using 3,5-diisopropylbenzene hydroperoxide under the catalysis of a tetraisopropyl titanate, D-(-)-diethyl tartrate and N,N-diisopropylethylamine system to obtain S-(-)-5-difluoromethoxy-2-{[(3,4-dimethoxy-2-pyridinyl)methyl]sulfinyl}-1H-benzimidazole, namely (L)-pantoprazole, refining the (L)-pantoprazole, and preparing a salt to obtain the (L)-pantoprazole sodium.

Dosage forms for the oral administration of the magnesium salt of pantoprazole are described.

The invention relates to a pantoprazole sodium freeze-drying medicinal composition for injection and a preparation method thereof. The pantoprazole sodium freeze-drying medicinal composition for injection comprises the following components in part by weight: 1 part of pantoprazole sodium, 0.01 to 0.1 part of mannitol, 0.02 to 0.03 part of natrium adetate, 0.07 to 0.10 part of sodium sulfite and 0 to 0.1 part of sodium citrate. In the method, the stability of the solution of the pantoprazole sodium is improved, related matters of the solution of the pantoprazole sodium in the process of preparation, packaging or freeze-drying during preparation are not increased obviously, the content of the related matters is not reduced obviously; the prepared pantoprazole sodium freeze-drying powder injection is good in stability in the process of transportation and storage; solution mixed with the injection during clinical use can be placed for a long time, so that the clinical use is more convenient; and simultaneously, hidden troubles of the medication safety of patients due to the increase of impurities (related matters) and the problem of the curative effect on the patients due to content reduction are reduced greatly.

Novel crystalline forms of pantoprazole sodium salt solvate with ketone solvents, a process for the preparation thereof, the use of the forms for the purification of pantoprazol, pharmaceutical compositions therefrom and the use thereof in therapy.

The invention provides a preparation method of pantoprazole sodium. The method comprises the following steps of: 1) generating 2-chloromethyl-3,4-dimethoxypyridine hydrochloride (III) by taking 2-hydroxymethyl-3,4-dimethoxypyridine (II) as the start raw material in the presence of chloride; 2) condensing the obtained compound (III) with 5-difluoromethoxy-2-sulfydryl-1H-benzimidazole in alkaline conditions in the presence of inorganic base to generate 5-difluoromethoxy-2-[(3,4-dimethoxy-2-pyridyl)methyl]thioxo-1H-benzimidazole (IV); and 3) salifying the obtained compound (IV) with sodium hydroxide, and oxidizing with an oxidizing agent to generate 5-difluoromethoxy-2-[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl-1H-benzimidazole sodium, namely pantoprazole sodium (I). According to the invention, the operation is simple and efficient, the reaction conditions are mild, the safety is high, the control is easy, the yield is relatively high, and the method is suitable for industrial production.

The present invention provides a process comprising admixing a thioether with about 1.05 to about 1.6 molar equivalents of an active chlorine-containing oxidant, preferably sodium hypochlorite, and about 2.5 to about 5.0 molar equivalents of an alkali metal base; and recovering a sulfoxide that is preferably pantoprazole, lansoprazole, omeprazole, or rabeprazole. The process may further comprise contacting the sulfoxide with a source of sodium ions, preferably sodium hydroxide, to produce the sodium salt of the sulfoxide. The invention also relates to novel chlorinated derivatives of pantoprazole including 5(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chloromethyl]sulfinyl]-1H- benzimidazole and 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)chlorohydroxymethyl] sulfinyl]-1H-benzimidazole and processes for making them. The invention also relates to processes of quantifying and identifying a compound other than pantoprazole in a mixture of pantoprazole and at least one other compound.

The invention relates to pantoprazole sodium and a preparation method thereof and in particular relates to a method for preparing the pantoprazole sodium. The preparation method comprises the following steps of: (1) with 2-hydroxymethyl-3,4-dimethoxyl pyridine (II) as a starting material, generating 2-chloromethyl-3,4-dimethoxyl pyridine hydrochloride (III) under the action of chlorides; (2) carrying out condensation on the obtained compound (III) and 5-difluoromethoxyl-2-sulfydryl-1H-benzimidazole in the presence of inorganic base to generate 5-difluoromethoxyl-2-[(3,4-dimethoxyl-2-pyridyl) methyl] sulfenyl-1H-benzimidazole (IV); (3) oxidizing the obtained compound (IV) by using an oxidant to generate 5-difluoromethoxyl-2-[(3,4-dimethoxyl-2-pyridyl) methyl] sulfinyl-1H-benzimidazole; (4) enabling the 5-difluoromethoxyl-2-[(3,4-dimethoxyl-2-pyridyl) methyl] sulfinyl-1H-benzimidazole to react with sodium hydroxide to generate a salt, namely the pantoprazole sodium (I); and optionally (5) refining the prepared pantoprazole sodium. According to the preparation method, the prepared pantoprazole sodium product has high purity.

The invention provides a pantoprazole sodium drug composition and a preparation method thereof. The pantoprazole sodium drug composition is characterized by comprising the raw materials in parts by weight as follows: 1 part of pantoprazole sodium, 0.3-0.6 parts of sucrose, 0.005-0.05 parts of metal ion complexing agent and a proper amount of inorganic base. Meanwhile, the invention further provides a preparation method of a pantoprazole sodium freeze-dried powder injection.

The invention relates to a pantoprazole sodium freeze-dried preparation for injection and a preparation method thereof. The freeze-dried preparation is formed by preparing components containing the following parts by weight into liquor for freeze drying after dissolving into water for injection: 60 to 80 parts of pantoprazole sodium, 100 to 300 parts of glycocoll, 50 to 100 parts of glucose and aright amount of sodium hydroxide. According to the pantoprazole sodium freeze-dried preparation for the injection, which is disclosed by the invention, the problem of stability of a preparation is solved; and moreover, an adverse reaction existing in a traditional product is lowered.

The invention discloses pantoprazole and the sodium salt enteric sustained-release micropill preparation thereof. The preparation comprises pantoprazole-containing micropills, an isolation layer, a sustained-release layer, another isolation layer and an enteric layer from inside to outside in sequence; the weight of the first isolation layer is 0.5% to 40% of that of the pantoprazole-containing micropills, the weight of the sustained-release layer is 5% to 100% of that of the pantoprazole-containing micropills, the weight of the second isolation layer is 0.5% to 40% of that of the pantoprazole-containing micropills, and the weight of the enteric layer is 20% to 200% of that of the pantoprazole-containing micropills. The pantoprazole enteric sustained-release micropills can stably release the drug.

The invention discloses a freeze-dried preparation of pantoprazole sodium liposomes, wherein pantoprazole sodium is encapsulated in antioxidant-containing liposomes made of soybean lecithin and cholesterol. The freeze-dried preparation is administered intravenously with stable quality, less toxicity and high effectiveness.

The invention provides a pantoprazole sodium enteric-coated tablet and a preparation method thereof. The pantoprazole sodium enteric-coated tablet comprises a pantoprazole sodium tablet, an isolated layer and an enteric-coated layer, wherein the pantoprazole sodium tablet comprises main drug pantoprazole sodium and auxiliaries; and the auxiliaries include a filler, a disintegrant, a lubricating agent, an adhesive, a pH regulating agent, and the like. The pantoprazole sodium enteric-coated tablet accelerates the disintegration time of the pantoprazole sodium enteric-coated tablet and solves the problem of drug instability during a storage period.

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 provides a pantoprazole sodium composition for injection. The composition contains pantoprazole sodium and disodium ethylene diamine tetraacetate that are in a proportion of 1:0.02-0.1 by weight. And the composition is prepared by the steps of: 1) liquid medicine preparation: placing pantoprazole sodium and disodium ethylene diamine tetraacetate in a preparation pot, adding water for injection and stirring to make the above agents dissolved and mixed well with the water, adjusting the pH value of the mixture to 10.5-12.5; 2) rubber stopper treatment; 3) aseptic filtration and separate packing; 4) vacuum freeze drying, thus obtaining the composition. For pantoprazole sodium medicaments extremely easy to react with exudates from a rubber stopper, the pantoprazole sodium composition for injection in the invention can simultaneously guarantee the visible foreign matters and insoluble particles in products meeting the requirement of an injection. According to the invention, quality level of the composition product is improved, and the hidden trouble that unqualified visible foreign matters and insoluble particles threat patient clinical medication safety can be avoided. Additionally, the composition of the invention has better curative effects and less clinical side effects.

The invention provides a pantoprazole sodium enteric-coated tablet. The pantoprazole sodium enteric-coated tablet is prepared by coating a pantoprazole sodium tablet with an isolation layer and an enteric-coated layer, wherein the pantoprazole sodium tablet comprises the following components in percentage by weight: 35-45% of pantoprazole sodium, 30-59% of a filling agent, 0.2-3% of a binder, 8.1-18% of a disintegrant, 5-15% of a stabilizer and 0.2-1.5% of a lubricant. According to the pantoprazole sodium enteric-coated tablet and the preparation method thereof provided by the invention, a dissolution curve of the pantoprazole sodium enteric-coated tablet in each of four dissolution media is consistent with that of an originally developed preparation, thereby being in line with the requirements of consistency evaluation; and furthermore, the stability of the pantoprazole sodium enteric-coated tablet is better than that of the originally developed preparation.

The invention provides a sub-micro emulsion frozen preparation of pantoprazole sodium and a preparation method thereof. The sub-micro emulsion frozen preparation of pantoprazole sodium is prepared mainly with the following components according to portions by weight: 1-10 portions of pantoprazole sodium, 5-50 portions of biodegradable polymer, 1-20 portions of emulsifying agent, 5-40 portions of skeleton supporting agent and 1-20 portions of stabilizing agent.

The invention discloses pantoprazole sodium enteric pellets which comprise cores containing pantoprazole sodium and enteric coating containing cellulose substances. The invention also discloses the process for preparing the cores. The invention realize higher preparation stability and facilitated mass production.

The present invention provides a process comprising admixing a thioether with about 1.05 to about 1.6 molar equivalents of an active chlorine-containing oxidant, preferably sodium hypochlorite, and about 2.5 to about 5.0 molar equivalents of an alkali metal base; and recovering a sulfoxide that is preferably pantoprazole, lansoprazole, omeprazole, or rabeprazole. The process may further comprise contacting the sulfoxide with a source of sodium ions, preferably sodium hydroxide, to produce the sodium salt of the sulfoxide. The invention also relates to novel chlorinated derivatives of pantoprazole including 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chloromethyl]sulfinyl]-1H-benzimidazole and 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chlorohydroxymethyl]sulfinyl]-1H-benzimidazole and processes for making them. The invention also relates to processes of quantifying and identifying a compound other than pantoprazole in a mixture of pantoprazole and at least one other compound.

The invention relates to the field of medicinal chemistry, in particular to a method for preparing (S)-pantoprazole in a high-enantioselectivity way. The method is characterized in that any organic alkali is not added under the condition of chiral reagent existence, and oxidants are used for directly oxidizing 5-difluoromethoxy-2-[[(3,4-dimethoxy-2-pyridyl)-methyl]-sulfenyl]-1H-benzimidazole. The ee value of the (S)-pantoprazole obtained by using the method provided by the invention can reach 100 percent.

The invention provides a preparation method of a chiral sulfoxide medicament though catalysis of asymmetric oxidation of sulfides compounds. A chiral complex formed by quadridentate nitrogen organic ligand and metal manganese compound as a catalyst and hydrogen peroxide as an oxidant are used for asymmetric catalytic oxidation of prochiral thioether compound, so as to obtain the corresponding chiral sulfoxide medicament compounds including S-omeprazole, S-lansoprazole, S-pantoprazole, S-rabeprazole, R-Modafinil and R-sulindac. The reaction has the advantages of cleaness, mild reaction conditions, high conversion rate and antipodal selectivity, and shows industrial prospects.