305 results about "Lansoprazole" patented technology

A method of treating gastric acid disorders by administering to a patient a pharmaceutical composition comprising a proton pump inhibitor (PPI) in a pharmaceutically acceptable carrier.

The present invention provides an oral solution/suspension comprising a proton pump inhibitor and at least one buffering agent. The PPI can be any substituted benzimidazole compound having H⁺,K⁺-ATPase inhibiting activity and being unstable to acid. Omeprazole and lansoprazole are the preferred PPIs for use in oral suspensions in concentrations of at least greater than 1.2 mg/ml and 0.3 mg, respectively. The liquid oral compositions can be further comprised of parietal cell activators, anti-foaming agents and/or flavoring agents. The inventive compositions can alternatively be formulated as a powder, tablet, suspension tablet, chewable tablet, capsule, effervescent powder, effervescent tablet, pellets and granules. Such dosage forms are advantageously devoid of any enteric coating or delayed or sustained-release delivery mechanisms, and comprise a PPI and at least one buffering agent to protect the PPI against acid degradation. Similar to the liquid dosage form, the dry forms can further include anti-foaming agents, parietal cell activators and flavoring agents. Kits utilizing the inventive dry dosage forms are also disclosed herein to provide for the easy preparation of a liquid composition from the dry forms. In accordance with the present invention, there is further provided a method of treating gastric acid disorders by administering to a patient a pharmaceutical composition comprising a proton pump inhibitor in a pharmaceutically acceptable carrier and at least one buffering agent wherein the administering step comprises providing a patient with a single dose of the composition without requiring further administering of the buffering agent. Additionally, the present invention relates to a method for enhancing the pharmacological activity of an intravenously administered proton pump inhibitor in which at least one parietal cell activator is orally administered to the patient before, during or after the intravenous administration of the proton pump inhibitor.

The present invention relates to a production method of a crystal of (R)-lansoprazole or (S)-lansoprazole, which includes crystallization at a temperature of about 0° C. to about 35° C. from a C1-4 alkyl acetate solution containing (R)-lansoprazole or (S)-lansoprazole at a concentration of about 0.1 g/mL to about 0.5 g/mL and the like. According to the production method of the present invention, a crystal of (R)-lansoprazole or (S)-lansoprazole superior in preservation stability can be produced efficiently on an industrial large scale.

The invention provides orally disintegrating tablets that readily disintegrates in the mouth, releasing enteric coated drug sub-tablets.

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.

The present invention relates to a lansoprazole freeze-dried powder injection and its preparation method. Said lansoprazole freeze-dried powder injection contains ethylene diamine tetraacetic acid (EDTA) and/or its salt, and is made up by using active component lansoprazole, ethylene diamine tetraacetic acid and/or its salt, stabilizing agent, excipient, pH regulator and injection water through a certain preparation process. Besides, said invention also provides the concrete steps of said preparation process.

The invention relates to a lansoprazole crystalline compound. An X-ray powder diffraction pattern represented by a diffraction angle of 2 theta +/- 0.2 DEG displays feature diffraction peaks at the positions of 5.8 DEG, 7.5 DEG, 9.1 DEG, 11.8 DEG, 12.1 DEG, 12.8 DEG, 13.3 DEG, 15.6 DEG, 16.7 DEG, 18.3 DEG, 20.4 DEG, 25.7 DEG, 26.8 DEG and 31.5 DEG. The invention also relates to a lansoprazole enteric capsule containing the lansoprazole crystalline compound. The lansoprazole enteric capsule comprises 20 to 60 parts of l crystalline compound, 90 to 140 parts of microcrystalline cellulose, 1.5 to 3.5 parts of disodium hydrogen phosphate, 2 to 5 parts of anhydrous sodium sulphite, 1 to 10 parts of crospovidone, 0.8 to 4.2 parts of lauryl sodium sulfate, 2 to 8 parts of povidone K30 and 1 to 3 parts of magnesium stearate.

A pharmaceutical composition comprising microtablets, wherein said microtablets comprise lansoprazole, a lubricant, optionally one or more excipients, and an enteric coating, wherein the weight ratio of lansoprazole to lubricant is from about 1:4 to about 8:1, wherein said microtablets have a tablet size of about 1 mm to about 4 mm, and a tablet weight of 1 to 50 mg, and said microtablets are free of a separating or intermediate layer between the lansoprazole and enteric coating.

Lansoprazole of formula (I) can be produced economically in a high yield using a simple, two-step method comprising reacting hydroxymethylpyridine and benzimidazole starting materials in the presence of a phosphine compound and a dialkyl azodicaboxlate and oxidizing the product of the first step in the presence of an organic radical catalyst:

A orally disintegrating tablet is obtained by tableting fine granules showing controlled release of lansoprazole and an additive, which is capable of suppressing breakage of the fine granules during tableting, and can control the release of lansoprazole for a long time, and can maintain a therapeutically effective concentration for a prolonged time, and shows superior disintegration property in the oral cavity.

The present invention relates to new stable enteric coated pharmaceutical dosage forms for oral use containing Omeprazole or Lansoprazole, to a formulation and a method for the manufacture of such a dosage forms, and to a method of gastric acid pump inhibition and providing gastrointestinal cytoprotective benefit by using them.

The invention provides an r-lansoprazole for injection and a preparation method thereof. The medicament comprises active components of r-lansoprazole, or r-lansoprazole salt or r-lansoprazole water crystal as well as an excipient, a pH regulator and an antioxidizer. The preparation method comprises the following steps of: dissolving raw and auxiliary materials in water; adjusting the pH value; adding active carbon to decolor; filtering with a filter membrane; sub-packaging; freezing and drying to obtain the r-lansoprazole. The medicament is clinically used for treating gastric ulcer, duodenal ulcer, erosive gastro-esophageal reflux disease, helicobacter pylori, zollinger-ellison syndrome, and the like, can prevent the orally taken r-lansoprazole from being damaged in gastric acid and reach the aims of fast onset and improving the bioavailability.

The invention provides a lansoprazole-contained freeze-dried powder injection and a preparation method thereof, wherein the freeze-dried powder injection comprises 1 part of lansoprazole, 0.05-50 parts of excipient and 0.1-10 parts of polyethylene glycol; the preparation method of the freeze-dried powder injection comprises the following steps of: weighing the lansoprazole, adding into water for injection, adding a pH regulator for regulating the pH value of a solution to be 10-12.5, stirring until the lansoprazole in the solution is completely dissolved, adding the polyethylene glycol and the excipient, adding the water for injection until reaching the whole volume, quantitatively filling into a cillin bottle, and carrying out freeze-drying; and the freeze-dried powder injection can simultaneously solve the problem of stability and solubility puzzling the preparation and has good redissolution property.

The invention relates to a refining method for a lansoprazole crude drug, which is characterized in that the lansoprazole sample is dissolved in anhydrous alcohol and stirred to complete dissolution, and activated carbon is added to be stirred, pumped and filtered; then the solution which is placed in a freezing chamber to freeze and crystallize is pumped and filtered to be dry, the filter cake is washed to be dry by the anhydrous alcohol, and white solid can be obtained; finally, the obtained white solid is dried in an oven, and the solid is turned over discontinuously during the drying until reaching constant weight. The preparation method for the lansoprazole crude drug is simple and convenient, high in refining yield, low in the total impurities of the refined lansoprazole and good in clarity after being prepared into injections.

Lansoprazole is a second generation proton pump inhibitor developed by Takeda in Japan, and is clinically and widely applied for treatment of acid related diseases and helicobacter pylori eradiation. The invention provides a preparation method of a Lansoprazole lyophilized powder injection preparation, creatively screens and tests the composition and dosage as well as the technology of the Lansoprazole lyophilized powder injection, obtains the optimal experiment condition, and gains good effect. The weight ratio of all the components of the Lansoprazole lyophilized powder injection satisfies the relation that Lansoprazole: meglumine: mannitol: sodium hydroxide equals to 30:10:60:4-4.1, the optimal weight ratio of all the components meets the relation that Lansoprazole: meglumine: mannitol: sodium hydroxide equals to 30:10:60:4.

The invention discloses a lansoprazole enteric liquid capsule which has a simple manufacturing process, avoids water from being led in during the manufacturing process, and has good storage stability and a manufacturing method. The lansoprazole enteric liquid capsule consists of lansoprazole, dispersant, edible vegetable oil, magnesium oxide or magnesium carbonate, an emulsifier, poloxamer, animal and vegetable glue, and sodium citrate. After being mixed uniformly, raw materials enter into a colloid mill, and then the raw materials are infused into a hollow capsule, and polyacrylic resin ethanol solution is used as the sealing material to sleeve and seal the infused capsule. The invention suspends the lansoprazole into hydrophobic excipient oil, forms a protective film around the lansoprazole powder, does not lead in water during the manufacturing process, avoids the degradation of the lansoprazole, does not need to wrap an isolation layer and an enteric coating, and has short production cycle, simple production process, low cost, and good product quality and stability.

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 belongs to the technical field of medicines and in particular relates to a lansoprazole compound. The lansoprazole compound has a chemical structural formula and is measured by a powder X-ray diffraction measurement method, and an X-ray diffraction pattern represented by a diffraction angle of 2theta 0.2 degrees is as shown in a figure 1. The lansoprazole compound provided by the invention is a novel lansoprazole crystal form different from that in the prior art, and the crystal form is lower in moisture absorptivity and better in solubility.

Ulcer is a serious oxidative stress induced disease with complex pathologic events including upregulation of H⁺K⁺ ATPase of parietal cell (PC) membrane, damage of mucin layer around PC, PC-DNA damage etc. The polysaccharide (GRPP) fraction and antioxidant extract (GRAOX) of ginger was examined for their ability to inhibit H⁺ K⁺ ATPase. Results indicated that the inhibition of H⁺ K⁺ ATPase activity which causes acidity in the lumen of the stomach, also exhibited better H⁺K⁺ ATPase inhibition (PPI) at the IC50 of 27.2 μg (GRPP) and 16.5 μg GAE (AOX) respectively than the known antiulcer proton pump blocker Lansoprazole (19.3 μg). Further the antioxidant activity in antioxidant extract (GRAOX) by various assay systems was examined such as Reducing power, Free radical scavenging (FRS), DNA and cytoprotection systems etc. GRAOX exhibited concentration dependent reducing power ability at 5-25 g equivalent of phenol. FRS activity with IC₅₀ of 6.8 μg equivalent of phenol etc. At 0.3 μg level GRAOX offered >80% protection to DNA and against FeSO₄-Asc'orbate induced oxidation. The major active phenolic components were identified as Gallic acid/Tannic acid (46%), and Cinnamic acid (51%).

The invention relates to lansoprazole composition freeze-dried powder for injection. The lansoprazole composition freeze-dried powder is characterized by comprising lansoprazole used as a main material, meglumine, mannitol, sodium hydrogensulfite and ethylene diamine tetraacetic acid, wherein the proportion of the components is 3:(0.1-1):(1-20):(0.01-0.5):(0.01-0.5); preferably, the proportion is 3:(0.5-1):(10-20):(0.1-0.3):(0.05-0.3); and more preferably, the proportion is 3:1:20:0.2:0.2. The preparation method comprises the following steps of: dissolving the raw material and the auxiliary materials by adding water; regulating the pH value; adding active carbon for decolorizing; filtering for decarburizing; fine filtering by using a filter membrane; sub-packaging; cooling to -50 to -46 DEG C according to a speed of 1-1.2 DEG C/minute; preserving heat and freezing for 3 hours; vacuumizing to 15Pa; uniformly heating up to -22 to -18 DEG C within 7-9 hours and then preserving heat for 1-2 hours; uniformly heating up to 3-7 DEG C within 4-6 hours and then heating up to 40 DEG C within 4 hours; preserving heat and drying for 3 hours; and packaging and storing after inspection.

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.

A liposome of lansoprazole is prepared from lansoprazole, phosphatide, cholesterol and the supporting agent chosen from sorbitol, mannitol, cane sugar, sodium chloride, water-soluble starch, etc. It is used for treating gastric ulcer, duodenal ulcer, reflux esophagitis, etc. Its preparing process is also disclosed.