247 results about "Telmisartan" patented technology

The present invention relates to a bilayer pharmaceutical tablet comprising a first layer formulated for immediate release of the angiotensin II receptor antagonist telmisartan from a dissolving tablet matrix which contains telmisartan in substantially amorphous form, and a second layer formulated for immediate release of a diuretic like hydrochlorothiazide from a fast disintegrating tablet matrix. A method of producing the bilayer tablet is also disclosed.

A pharmaceutical composition comprising about 80 mg of telmisartan or a salt thereof and about 25 mg of hydrochlorothiazide or about 160 mg of telmisartan or a salt thereof and about 50 mg of hydrochlorothiazide, and methods of treating hypertension in patients with such combination.

A pharmaceutical composition comprising a solid unit dosage form comprising: one or more of pharmaceutically active ingredients selected from valacyclovir, olanzapine, voriconazole, topotecan, artesunate, amodiaquine, guggulosterone, ramipril, telmisartan, tibolone, atorvastatin, simvastatin, amlodipine, ezetimibe, fenofibrate, tacrolimus, valgancyclovir, valsartan, clopidrogel, estradiol, trenbolone, efavirenz, metformin, pseudoephedrine, verapamil, felodipine, valproic acid / sodium valproate, mesalamine, hydrochlorothiazide, levosulpiride, nelfinavir, cefixime and cefpodoxime proxetil in combination with a water insoluble polymer and / or a water soluble polymer. Methods for making the pharmaceutical composition are also disclosed.

The present invention relates to a method for the prophylaxis of vascular headaches which do not originate from hypertension, especially migraine, the method comprising administration of telmisartan to a subject in need of such a treatment. The present invention relates also to a method for the prophylaxis of vascular headaches, comprising the co-administration of telmisartan in combination with other drugs suitable for migraine prophylaxis and / or acute treatment of migraine.

Pharmaceutical tablets comprising a first layer formulated for immediate release of telmisartan from a dissolving matrix and a second layer formulated for immediate release of hydrochlorothiazide from a dissolving matrix, methods for producing tablets and methods of use for treating hypertension.

The invention supplies an intermediate to make intermediate of Telmisartan that has the structure of 4'-((4- methyl-6-(2- methylamino) carbanilino)-2-propyl-1H- benzimidazole-1-radicle) methyl) biphenyl-2-carboxylic acid. It has the advantages of high yield, save operation, low environment pollution, etc.

The invention discloses a key intermediate of telmisartan. A chemical name of the key intermediate is 4'-[(4'-methyl-2'propyl[2,6'-bi-1H-benzimidazole]-1'-yl) methyl], and the key intermediate has a structural formula (6) shown below. The invention also discloses a synthetic method for the key intermediate of the telmisartan and a method for synthesizing the telmisartan by the intermediate. A newprocess for synthesizing the telmisartan by the intermediate thereof has the advantages of low-cost and readily available materials, mild reaction condition, low production cost, high yield and quality and the like.

The invention belongs to the technical field of medicinal preparation, and in particular relates to a telmisartan tablet composition. The telmisartan tablet composition is characterized by being prepared from 80 parts of telmisartan, 6.72 parts of sodium hydroxide, 24 parts of meglumine, 250 to 280 parts of sorbierite, 58 to 88 parts of calcium hydrophosphate, 20 parts of polyvidone and 10 parts of magnesium stearate. By selecting and using the combination of sorbierite and calcium hydrophosphate as filler, the composition can obviously improve the stability of the preparation and is favorable for production and application of the preparation.

The invention discloses a preparation method for telmisartan, and belongs to the technical field of pharmaceutical synthesis. The key points of the technical scheme lie in that in the preparation method for the telmisartan takes ionic liquid as a reaction medium, and 3-methyl-4-nitryl-benzoic acid as a raw material, 2-n-propyl-4-methyl-6- carboxyl benzimidazole is obtained successively through an esterification reaction, a reduction reaction, an acylation reaction, a nitratlon reaction, a reduction reaction and a cyclization reaction, then under the action of a polyphosphoric acid, the 2-n-propyl-4-methyl-6-carboxyl benzimidazole and N-methyl-o-phenlenediamine dihydrochloride are condensed to obtain 2-n-propyl-4-methyl-6-[1-methylbenzimidazole-2-yl] benzimidazole, 2-n-propyl-4-methyl-6-[1-methylbenzimidazole-2-yl] benzimidazole is condensed with 4,-bromine biphenyl-2-carboxylic acid methyl ester, and hydrolysis is carried out to obtain the telmisartan. According to the method, the ionic liquid is used for replacing methanol with larger toxicity in an original technology to be used as the reaction medium, raw materials are easy to obtain, the operation is simple and convenient, the yield is high, the purity of products is high, the residual quantity of an organic solvent is small, and the method is environmentally-friendly and is suitable for industrialized production.

The invention provides a compound preparation of telmisartan and amlodipine and a preparation method thereof. The compound preparation consists of first mini-pills containing the telmisartan and second mini-pills containing the amlodipine. The preparation has high stability and convenient production. The invention also relates to a preparation method for the compound preparation of telmisartan and amlodipine.

Amorphous telmisartan and combinations of amorphous telmisartan with one or more pharmaceutical carriers.

The invention provides an improved process for preparing a telmisartan raw material medicament. The improved process comprises the following step: preparing an intermediate 2-n-propyl-4-methyl-benzimidazole-6-carboxylic acid by using methyl 4-butylacetamino-3-methylbenzoate as a raw material through four steps, namely nitration, reduction, cyclization and hydrolysis. According to the process, crude products in nitrification, reduction and cyclization reactions are not subjected to purification and separation, and a target product can be separated by regulating the pH of a reaction liquid obtained in a hydrolysis reaction to be between 6 and 7, so that the problems of complicated operation and yield loss caused by separation of nitrified and reduced products by recrystallization and chromatographic separation of a cyclized product by a column are solved. Therefore, the purity of the prepared telmisartan crude product is over 99 percent after recrystallization. The improved process is simple to operate, high in yield and low in cost, and is advantageous to industrial production.

The invention provides a solid oral preparation without a surfactant. The solid oral preparation comprises the following components in percentage by weight: 5-25% of telmisartan, an alkaline reagent and the balance of pharmaceutically acceptable vectors, wherein the weight of the alkaline reagent is equal to 7-20% of that of telmisartan. The invention also provides a method for preparing the solid oral preparation. The preparation prepared by the method can be quickly and sufficiently released in the psychophysical pH range of gastrointestinal tracts; and compared with the prior art, the preparation method has the advantages that the process is simpler, the quality of the soli oral preparation is more stable, the cost is greatly saved, and the efficiency is improved.

Methods and compositions are disclosed to treat neuropsychiatric disorders post-traumatic stress disorder (PTSD). In particular, described herein are angiotensin receptor blockers (ARBs), and in particular the combination of one or more ARB (such as telmisartan) and an agent that enhances the delivery of the ARB across the blood-brain barrier (such as minocycline). PTSD may be treated using a combination of telmisartan and minocycline at levels of each that are, by themselves, infective to treat PTSD. Also described herein are methods for treating PTSD by first identifying patents for whom the use of an ARB treatment would be effective, by determining that patient has a dysfunction in their angiotensin converting enzyme and / or other genes in the autonomic arousal axis.

The invention relates to the fields of pharmaceutical chemistry and pharmaceutical therapeutics, and more particularly to an optically active ring-opening butylphthalide-telmisartan heterocomplex or a pharmaceutically acceptable salt or ester thereof, preparation methods thereof, pharmaceutical compositions containing the compounds, and pharmaceutical application of the pharmaceutical compositions, particularly application in prevention and treatment of neuroinflammation-related diseases, including ischemic stroke, alzheimer's disease, brain trauma, Parkinson's disease, multiple sclerosis and depression.

The invention provides a pharmaceutical composition which comprises calcium channel blockers of a medicinal dose, angiotensin II receptor antagonists of a medicinal dose, one or more of B vitamins of a medicinal dose and pharmaceutically acceptable carriers, wherein the calcium channel blockers are selected from amlodipine, felodipine, israbipine, nicardipine, nifedipine, nisoldipine, nitrendipine, lacidipine, diltiazem or verapamil; the angiotensin II receptor antagonists are selected from candesartan, telmisartan, losartan, valsartan, irbesartan, eprosartan, tasosartan or olmesartan; and the B vitamins are selected from one or more of vitamin B6, vitamin B12, folic acid and calcium leucovorin. The pharmaceutical composition of the invention can improve the curative effect of the hypotensor, enhance the target organ protecting action of the hypotensor, and reduce the morbidity of complications of angina, myocardial infarction and the like.

The invention provides a telmisartan medicinal composition, telmisartan medicinal composition tablets and a preparation method for the telmisartan medicinal composition tablets. The composition consists of the following components: telmisartan sodium salt, sorbitol, polacrilin potassium, anhydrous calcium phosphate, lactose, microcrystalline cellulose and magnesium stearate. The invention provides a preparation method for the telmisartan sodium salt, reaction conditions are mild, few side reactions are performed, and the generated sodium salt has higher water solubility; meanwhile, the sorbitol in the medicine has a diuresis effect, and has a synergistic antihypertensive effect with telmisartan in human bodies, so that the therapeutic effect of the product is strengthened; and after the telmisartan is taken, the urinary albumin excretion rate (UAER) of patients with early diabetic nephropathy is remarkably reduced, so the telmisartan has a kidney protection effect.

The invention relates to a preparation technology of a telmisartan active pharmaceutical ingredient, which comprises the technological routes: taking 3-methyl-4-nitryl-benzoic acid as an initial raw material; preparing 4-amino-3-methyl benzoic acid methyl ester through esterification and reduction; preparing 4-methyl-2-propyl-benzimidazole-6-carboxylic acid through acylation, nitration of fuming nitric acid, reduction, cyclization and hydrolysis; producing 4-methyl-2-propyl-6-(1-benzimidazole-methylbenzimidazole-2-yl)-benzimidazo through the condensation with N-methy-o-phenylenediamine; and condensing with 4'-brooethyl biphenyl-2-carboxylic methyl ester in the presence of potassium tert-butoxide and preparing a telmisartan crude product through the hydrolysis of a sodium hydroxide solution-methanol system. The technological routes are simple and mature. The total molar yield can finally reach 23.2% through improving the traditional technological routes; and reaction operation is more easier, the process is simpler, serious three-waste pollution is not generated and the preparation technology is convenient for industrial production.

The invention discloses a compound tablet containing telmisartan and hydrochlorothiazide. The tablet is prepared by uniformly mixing telmisartan particles and hydrochlorothiazide particles, and tabletting the mixture. According to the weight of the hydrochlorothiazide particles, the hydrochlorothiazide particles contain 6 to 50 percent of disintegrant. The compound tablet is a single-layer tablet. The telmisartan / hydrochlorothiazide tablet is quickly dissolved and is stable in quality. The invention also provides a preparation method for the compound tablet, which is simple in process, low in cost and suitable for industrial mass production.

The invention relates to a new process for preparing telmisartan, which uses 2-n-propyl-4-methyl-6-(1'-methylbenzimidazol-2'-yl)-benzimidazole and 4' -Bromomethyl-biphenyl-2-carboxylate alkyl ester or 4'-bromomethyl-biphenyl-2-carbonitrile undergoes a one-step reaction to complete the two-step synthesis reaction of condensation and hydrolysis to directly obtain Telmisartan. Compared with other processes, it has the advantages of solving the technical difficulties of industrial production, simple operation, green synthesis, high purity of telmisartan, high yield and low cost, and has been successfully applied in industrial production.

The invention relates to the technical field of medicines, in particular to a telmisartan solid dispersion as a specific angiotensin II receptor antagonist (ATI type) and a preparation method thereof. The telmisartan solid dispersion comprises medicine telmisartan, a carrier and an alkali matter, and also comprises a surfactant, wherein the carrier is a hydrophilic polymeric carrier, and the mass ratio of the medicine telmisartan to the hydrophilic polymeric carrier to the alkali matter to the surfactant is 1:(1-9):(0.1-0.5):(0.1-0.5). The telmisartan solid dispersion has better dissolution rate during the use, and is convenient for gastrointestinal tract absorption, thereby improving bioavailability.

The invention provides a medicine composition, which comprises 100 weight portions of telmisartan, 25 to 45 weight portions of alkaline reagents, 15 to 40 weight portions of polyvinylpyrrolidone, and pharmacologically acceptable carriers. The invention also provides a preparation method for the medicine composition.

The present invention provides an intermediate and a process for preparing Telmisartan, which overcomes the drawbacks of conventional methods and produces Telmisartan in high purity and yield.

The invention relates to a pharmaceutical composition containing a calcium channel blocker (CCB) or the mixture thereof, an angiotonin 3II receptor blocker (ARB) or the mixture thereof, statins or the mixture thereof and a pharmaceutically acceptable carrier, wherein the CCB is selected from l-amlodipine, amlodipine, lacidipine, nitrendipine or the mixture thereof; the angiotonin II receptor blocker is selected from telmisartan, losartan, irbesartan, candesartan or the mixture thereof; and the statins are selected from atorvastatin, simvastatin, ruishufatadine, fluvastatin or the mixture thereof. The pharmaceutical composition is used for treating various high blood pressures and preventing or treating cardiovascular and cerebrovascular diseases relevant to the hypertension, reduces the disease rate and / or mortality rate of the cardiovascular and cerebrovascular diseases and also improves the adaptability for a sufferer taking medicine.

The invention relates to a preparation method of telmisartan tablets. The preparation method comprises the following steps: dissolving telmisartan, sodium hydroxide and povidone in purified water forpulping, pelleting with mannitol in a fluidized bed to obtained dried particles, and adding lactose, meglumine and magnesium stearate tablets by adopting an addition method. Equipment conditions adopted according to the invention are as follows: the inlet temperature is 90-95 DEG C (the temperature does not exceed 105 DEG C), the fluidization air volume is 50m<3> / h, the atomizing air pressure is 45psi, and the flow rate of an adhesive is 3r / min.

The invention discloses a telmisartan tablet preparation and a preparation method thereof. The tablet preparation is prepared through uniformly mixing drug-containing granules with a pharmaceutically acceptable excipient and then tabletting, wherein the drug-containing granules are prepared through uniformly mixing telmisartan and sodium dodecyl sulfate, micronizing the mixture, uniformly mixing the mixture with micronized lactose and then carrying out wet granulation. The preparation disclosed by the invention does not contain alkaline materials, is rapid in drug dissolution and is simple in preparation process, thereby being suitable for being produced in a large scale.

The invention discloses a telmisartan tablet and a preparation method thereof. The preparation method comprises the following steps: 1) in the presence of a solvent, mixing telmisartan with an acid and alkaline regulator to prepare a telmisartan sodium salt; 2) adding a binding agent into the telmisartan sodium salt to prepare slurry, adding a part of a filling agent into the slurry, drying and pelletizing, thereby preparing particulate matters; and 3) adding the rest of the filling agent and a lubricating agent into the particulate matters to tablet, thereby preparing the telmisartan tablet,wherein the acid and alkaline regulator comprises at least sodium hydroxide. The preparation method is used for firstly mixing the telmisartan with the acid and alkaline regulator in the existence ofthe solvent, adding the binding agent, then adding one part of the filling agent, drying and pelletizing to prepare the particulate matters, and further, adding the rest of the filling agent and all the lubricating agent into the particulate matters to mix and tablet, so that the telmisartan in the telmisartan tablet prepared through the steps is uniformly mixed without an obvious clustering phenomenon, and therefore, the material yield is relatively high.

The invention discloses a levamlodipine and telmisartan compound preparation and an optimal compound formulation. In the invention, the combination of the levamlodipine and the telmisartan is used for treating hypertension, good synergic antihypertension effect is obtained between the levamlodipine and the telmisartan, the doses of the levamlodipine and the telmisartan can be reduced while the equivalent and even better antihypertension effect is achieved, and the adverse effect caused by high dose of single drug is reduced. Besides, the telmisartan can obviously improve the tolerance of the levamlodipine, can inhibit heart rate increase caused by the levamlodipine and can reduce the incidence of peripheral edema.

The invention discloses a synthesis method for a telmisartan intermediate, N-Methyl-o-phenylenediamine (salt), and isomeride thereof. According to the synthesis method, o (m or p)-nitroaniline is subjected to methylation under the action of a methylation reagent and a catalyst so as to obtain N-Methyl-o (m or p)-nitroaniline; and then under the action of a reducing agent, the N-Methyl-o (m or p)-nitroaniline is used to prepare the N-Methyl-o (m or p)-phenylenediamine. According to the synthesis method, the o (m or p)-nitroaniline is adopted as an initial material and is cheap and easy to get, the selectivity of actions of the methylation reagent is strong, and by-product of N, N-dimethyl is avoided. The reaction in the two steps are all subjected to conventional unit operation, the reaction is simple and convenient, and the yield and quality are high, so that the synthesis method is applicable to mass industrial production.

The invention discloses a benzimidazole compound and a preparation method thereof, and applications of the benzimidazole compound in preparation of telmisartan. According to the present invention, the prepared benzimidazole compound can be used for preparing telmisartan, and the preparation method has advantages of low raw material cost, simple operation, safety, controllability, high product purity and high total yield, and is suitable for industrial production.