63 results about "Losartan Potassium" patented technology

The invention discloses a liposome solid preparation of a losartan potassium hydrochlorothiazide pharmaceutical composition and a preparation method thereof. In the invention, active components of losartan potassium and hydrochlorothiazide and specific combined hydrogenated yolk lecithin, cholesterol and poloxamer 188 are prepared into a liposome which is then mixed with other pharmaceutical accessories to prepare the solid preparation, thereby greatly improving the pharmaceutical stability and bioavailability and having stable and lasting effect, small side effect and obvious curative effect.

The invention discloses preparation methods of losartan potassium and a preparation thereof. The losartan potassium is prepared by the steps of: by taking 2-butyl-5(4)-formoxyl-4(5)-trichlorophenidin (II) and N-(triphenylmethyl)-5-[(4'-brooethyl)-xenyl-2-]tetrazole (III) as raw materials and adopting tetrabutyl ammonium bromide as a phase-transfer catalyst for N-alkylating, performing condensation, reduction and deprotection to synthesize losartan; and salifying the obtained losartan with potassium hydroxide to synthesize raw material losartan potassium. The raw material losartan potassium is mixed with proper auxiliaries to prepare a medicinal preparation. The preparation methods in the invention have the characteristics of mild requirements on production conditions, simplicity in operation and high yield, and are suitable for industrial production.

A dripping pill of losartan potassium and hydrochrothiazide for treating hypertension and heart failure is prepared from losartan potassium, hydrochrothiazide and matrix. Its preparing process is also disclosed.

The invention relates to a compound preparation containing losartan potassium and hydrochlorothiazide and a preparation method for the compound preparation. The compound preparation containing the losartan potassium and the hydrochlorothiazide comprises a tablet core and a film coating, wherein the tablet core comprises active pharmaceutical ingredients of the losartan potassium and the hydrochlorothiazide, and minor pharmaceutical ingredients such as microcrystalline cellulose, lactose, low substituted hydroxyprepyl cellulose and magnesium stearate. The prepared compound preparation has high dissolubility, is simple in preparation process and can be easily produced in large scale; and moreover, the degradation speed and degree of the hydrochlorothiazide can be remarkably lowered, and impurities 4-amino-6-chloro-1,3-benzenedisulfonamide (DSA) and chlorothiazide can be prevented from increasing.

The invention relates to a stable oral solid preparation containing losartan potassium and hydrochlorothiazide, comprising 100 parts by weight of hydrochlorothiazide, 400 parts by weight of losartan potassium and 0.5-160 parts by weight of pharmacologically-allowable acid substance, wherein the pharmacologically-allowable acid substance is selected from organic acid, acidic amino acid or a combination of the organic acid and the acidic amino acid. A certain amount of pharmacologically-allowable acid substance is added in the oral solid preparation containing losartan potassium and hydrochlorothiazide to prepare a composition which can remarkably reduce the speed and the degree of degrading the hydrochlorothiazide and prevent an impurity of 4-amino-6-chloro-1,3-benzene disulfonamide (DSA) from raising. Therefore, the composition has better clinical treatment function and clinical medication safety.

The invention relates to an amlodipine and losartan potassium medicinal composition, which comprises the following components calculated according to weight part: 2.5-10 parts of amlodipine, 20-100 parts of losartan potassium, 5-20 parts of pregelatinized starch, 20-60 parts of microcrystalline cellulose, 15-40 parts of low substitution hydroxypropyl cellulose, 1-8 parts of carboxymethyl starch sodium and 1-3 parts of magnesium stearate. The amlodipine is an amlodipine maleate hydrate crystal with a molecular formula of C24H29ClN2O9.1.5H2O. The amlodipine maleate in the medicinal composition can be used for stably releasing the medicinal effect within 24 hours and stably and quickly taking effect. The medicinal composition has strong synergism, accumulation and complementary action and high bioavailability.

This invention relates to novel amorphous losartan potassium, novel losartan potassium in a crystalline form that is a hydrate, novel crystalline losartan potassium Form IV and solvates thereof, novel crystalline losartan potassium Form V and solvates thereof, to processes for their preparation, to compositions containing them and to their use in medicine. This invention further relates to a novel process for preparing crystalline losartan potassium Form I and Form II.

The invention relates to a losartan potassium gastric floating capsule, which comprises losartan potassium, PEG6000 (polyethyleneglycol), stearic acid, octodecyl alcohol, pre-gelatinized starch and mannite, wherein the losartan potassium is a powdery substance which is sieved with a 100-mesh sieve. A preparation method of the capsule comprises the following steps of: S1, mixing the PEG6000, the stearic acid and the octodecyl alcohol according to a certain proportion, heating to 64-66 DEG C, and smelting into a liquid; S2, heating the liquid mixture to 69-72 DEG C, and preserving heat for 9-11 minutes; S3, adding a proportional amount of losartan potassium into the mixture obtained in the step S2, keeping the temperature at 69-72 DEG C, and stirring uniformly; S4, adding a proportional amount of the pre-gelatinized starch and the mannite, and stirring uniformly; and S5, after the uniformity is qualified, filling in a hot state, covering a capsule cap, and cooling to the room temperature. The losartan potassium gastric floating capsule has the advantages that the medicament releasing time is long, the medicine taking times of a patient are reduced, the treatment compliance of the patient is enhanced, and the quality in a storage life is stable.

The invention belongs to the technical field of medicaments and relates to a losartan potassium troche and a preparation method thereof. In components of the troche, 10-30% of losartan potassium is used as a primary medicine in percentage by weight; magnesium stearate is used as a lubricant, wherein the ratio of the magnesium stearate to the losartan potassium is 1:10-1:25 in percentage by weight. A wet granulation technology and a tabletting technology with the primary medicine externally used are adopted in the preparation process. The invention aims at providing the troche with stable quality and simple and feasible process.

The invention provides a pharmaceutic preparation of iosartan potassium, comprising losartan potassium, lactose, microcrystalline cellulose, calcium hydrophosphate and lauryl sodium sulfate, and prepared by the wet granulation technology. The pharmaceutic preparation has the advantage that high hydroscopicity of iosartan potassium can be improved, and the mixed materials have good flowability. Besides, the pharmaceutic preparation has high dissolution rate and good stability.

The invention relates to a preparation method for a losartan potassium-hydrochlorothiazide tablet. The losartan potassium-hydrochlorothiazide tablet is characterized in that: after losartan potassium and starch are mixed, 10% of starch slurry is used to prepare particles with a suitable hardness; hydrochlorothiazide, cross linked sodium carboxymethyl cellulose and lactose are mixed, and particles with a proper hardness are prepared from an obtained mixture by using 5% of a polyvinylpyrrolidone K30 solution; the two kinds of particles and magnesium stearate are uniformly mixed and then are subjected to tabletting. According to the invention, a low dissolution rate caused by interaction among drugs in primary granulation is avoided, and an in vitro dissolution rate can be improved greatly, thereby enhancing bioavailability.

The invention belongs to the technical field of pharmacy, and in particular relates to a hydrochlorothiazide solid dispersion and hydroxypropyl-beta-cyclodextrin inclusion compound, and a preparation comprising losartan potassium and hydrochlorothiazide. The hydrochlorothiazide solid dispersion is prepared from hydrochlorothiazide and dispersion medium urea or povidone, and the hydrochlorothiazide hydroxypropyl-beta-cyclodextrin inclusion compound is prepared from hydrochlorothiazide and hydroxypropyl-beta-cyclodextrin inclusion. The preparation is an osmotic pump controlled release tablet comprising hydrochlorothiazide solid dispersion and inclusion compound and losartan potassium, consists of a tablet core and a coating for coating the tablet core, and a drug release hole with diameter of between 0.3 and 0.9mm is formed in the center of one side of the coating. The hydrochlorothiazide is compressed in the tablet core in a solid dispersion or inclusion compound mode together with losartan potassium, and is produced into a final product by utilizing an osmotic pump controlled release technology, so that the dissolubility of hydrochlorothiazide is improved, and the losartan potassium and the hydrochlorothiazide can be released at controlled speed in 0 to 24 hours in vitro. Therefore, the osmotic pump controlled release tablet has extremely high application value.

The invention relates to a losartan potassium membrane controlled-release pellet capsule. The controlled-release film of the pellet adopts Eurdragit NE 30D as a film forming material, the core of the controlled-release pellet contains high-expansibility low-substituted hydroxypropylcellulose and a pharmaceutically-acceptable excipient commonly used for controlled-release pellets, and optimally, the excipient is microcrystalline cellulose, wherein the weight percentage of the low-substituted hydroxypropylcellulose in the core of the controlled-release pellet is 10-40%. The controlled-release film of the controlled-release pellet includes the Eurdragit NE 30D and an anti-adherent talcum powder, the optimal ratio of the Eurdragit NE 30D to the talcum powder is 30:6, and the optimal coating weight gain is 19-36%. The core will obviously expand after absorbing water because of the containment of the low-substituted hydroxypropylcellulose highly expanding after contacting with water, so the controlled-release film is stretched, the thickness of the film is thinned, the apertures of water-pervious micro-pores are increased, the permeability is good, and the permeability decrease caused by film ageing is compensated, thereby the middle and later stage release speed is basically constant, the last stage residue is small, and a stable release performance is always maintained prior to the expiration date.

A process for the synthesis of Losartan Potassium by reacting Trityl Losartan in a primary alcohol with potassium tertiary alkoxide.

The invention discloses a losartan potassium liposome solid preparation and a preparation method thereof. Excellent quality of losartan potassium liposome is prepared by selecting specific weight proportions of losartan potassium, phosphatidylinositol, dimyristoyl lecithin and cholesterol, and then the losartan potassium liposome is prepared into a solid preparation by a general preparation method. Compared with the existing preparation, the liposome solid preparation provided by the invention has a high encapsulating rate and a uniform grain size, the medicine is maintained in blood circulation for a long time, apparently the stability and the bioavailability of the preparation product are improved, the quality of the preparation product is improved, and toxic and side effects are reduced.

The invention discloses a preparation method of an amlodipine and losartan potassium compound composition. The preparation method comprises the following steps of mixing losartan potassium and hydroxypropyl methylcellulose, adding microcrystalline cellulose and pregelatinized starch, mixing, adding a proper amount of ethanol water solution, granulating, drying to obtain losartan potassium dry particles, and mixing amlodipine besylate and sodium carboxymethyl starch to obtain the amlodipine and losartan potassium compound composition; crushing losartan potassium, adding microcrystalline cellulose and pregelatinized starch, mixing to obtain amlodipine mixed powder, mixing losartan potassium dry particles, amlodipine mixed powder, silicon dioxide and magnesium stearate, tabletting, and coating so that the tablet obtained by the method is stable, and the dissolution rate of the tablet is close to or consistent with that of an original product on the market.

The invention relates to a brand new medicinal composition containing levamlodipine and losartan potassium and a preparation method thereof. The composition comprises the levamlodipine and the losartan potassium serving as active ingredients and pharmaceutically acceptable auxiliary materials, wherein the levamlodipine refers to a levamlodipine besylate crystal; and the characteristic peaks of the crystal in an X-ray powder diffraction pattern obtained by measuring through Cu-K alpha rays are displayed when 2 theta is 8.0 degrees, 12.1 degrees, 15.4 degrees, 17.0 degrees, 19.8 degrees, 21.6 degrees, 23.0 degrees, 24.3 degrees, 25.7 degrees, 27.4 degrees, 30.7 degrees and 33.5 degrees. Since the composition contains the crystal which can improve the solubility of levamlodipine besylate, synchronous release of the levamlodipine besylate and the losartan potassium can be realized, and the synergic action of the levamlodipine besylate and the losartan potassium is brought into fuller play. In the method, a direct powder tableting process is adopted; and the method has a simple process, a short production period and low production cost.

The invention relates to a composition with losartan potassium and gliclazide and a preparation method thereof. The composition is prepared from the following components in parts by weight: 40-60 parts of losartan potassium, 60-100 parts of gliclazide, 40-60 parts of microcrystalline cellulose, 20-40 parts of anhydrous calcium hydrogen phosphate, 60-80 parts of pregelatinized starch, 4-8 parts ofsilicon dioxide and 2-4 parts of magnesium stearate. The preparation method comprises the following steps: taking part of pregelatinized starch, adding water into the part of pregelatinized starch toprepare a pregelatinized starch slurry with the concentration of 8-12%, taking the pregelatinized starch slurry as an adhesive, adding the adhesive into a mixture composed of losartan potassium, microcrystalline cellulose and the part of the pregelatinized starch to prepare a soft material, preparing the soft material into particles through a 20-30-mesh sieve, drying the particles at 40-70 DEG C till the water content of the particles is 1-3%, then neatening the particles through a 20-mesh sieve, then uniformly mixing the particles with gliclazide, anhydrous calcium hydrogen phosphate, silicondioxide and magnesium stearate, then directly tabletting to obtain tablets of the composition with losartan potassium and gliclazide. The composition is capable of exerting the beneficial effect of losartan potassium on treatment of hypertension with diabetes; losartan potassium and gliclazide are capable of synergistically exerting the effect of reducing blood pressure and blood glucose.

Improved processes using primary, secondary and tertiary alcohols and with safer mode of introduction of the reagent and reaction conditions are described. Further, the process of manufacture of Losartan potassium by use of alkali metal salt such as Potassium carbonate is disclosed. A process for preparation of the polymorphic Form I of Losartan potassium is also disclosed herein.

The invention discloses a medicine composition containing losartan potassium and hydrochlorothiazide and a preparation method thereof. The composition also contains auxiliary materials, namely sodium alginate and lactose. The medicine composition can be prepared into capsules, tablets, granules and so on after being added with other proper pharmaceutic adjuvant.

The invention belongs to the field of medicines, and particularly relates to an application of a losartan potassium and dacarbazine combined medicine to preparation of a medicine for treating intestinal cancer. The application of the losartan potassium and dacarbazine combined medicine to preparation of the medicine for treating intestinal cancer is proposed for the first time, losartan potassiumand the dacarbazine have an obvious synergistic effect, the curative effect is effectively improved, compared with a single component, for the losartan potassium and dacarbazine combined medicine, thecurative effect is more remarkable, and the lethality to tumor cells is improved. The dosage is effectively reduced, so that the toxic and side effects are reduced. The losartan potassium and dacarbazine combined medicine can also save cost, reduce economic burden of patients, provide a new approach for prevention and treatment of intestinal cancer, and have broad application prospects in the field of medicine and pharmacology.

The invention discloses a liposome solid preparation of a losartan potassium hydrochlorothiazide pharmaceutical composition and a preparation method thereof. In the invention, active components of losartan potassium and hydrochlorothiazide and specific combined hydrogenated yolk lecithin, cholesterol and poloxamer 188 are prepared into a liposome which is then mixed with other pharmaceutical accessories to prepare the solid preparation, thereby greatly improving the pharmaceutical stability and bioavailability and having stable and lasting effect, small side effect and obvious curative effect.

The invention discloses a brand new oral solid medicinal composition and its preparation method, the medicinal composition is an oral preparation prepared by hydrochlorothiazide, levamlodipine, losartan potassium and pharmaceutically-accepted auxiliary materials, the oral preparation is including but not limited to tablets or capsules. The composition comprises the following raw materials by weight part: 5-25 parts of hydrochlorothiazide, 2.5-5 parts of levamlodipine, 20-120 parts of losartan potassium, 30-90 parts of lactose, 20-60 parts of microcrystalline cellulose, 20-60 parts of pregelatinized starch, 2-5 parts of hydroxypropylcellulose, 1-3 parts of silica and 1-2 parts of magnesium stearate. The medicinal composition has the advantages of scientific and reasonable prescription, lowauxiliary materials content and high biological availability, and is a preferred medicine for treating hypertension.

Losartan is prepared by acid catalyzed cleavage of a triarylmethyl group from a triarylmethyl-substituted losartan derivative in a diluent comprising liquid ketone. The reaction mixture is basified and liquid ketone is evaporated from the mixture leaving a residue from which a triarylmethyl alcohol and losartan are each obtained in high yield and high purity. In addition, losartan potassium is prepared by a process that is more convenient that those previously known in the art in which losartan is contacted with potassium ions in substantially pure liquid alcohol and losartan potassium is precipitated from the alcohol.

The invention relates to a preparation method for a losartan potassium-hydrochlorothiazide tablet. The losartan potassium-hydrochlorothiazide tablet is characterized in that: after losartan potassium and starch are mixed, 10% of starch slurry is used to prepare particles with a suitable hardness; hydrochlorothiazide, cross linked sodium carboxymethyl cellulose and lactose are mixed, and particles with a proper hardness are prepared from an obtained mixture by using 5% of a polyvinylpyrrolidone K30 solution; the two kinds of particles and magnesium stearate are uniformly mixed and then are subjected to tabletting. According to the invention, a low dissolution rate caused by interaction among drugs in primary granulation is avoided, and an in vitro dissolution rate can be improved greatly, thereby enhancing bioavailability.

The invention relates to a preparation method of a losartan potassium impurity. In the production process, a novel losartan alkylation impurity is found, and the impurity has obvious influence on the quality of a finished product and is a key impurity in the preparation process. A synthesis method of the impurity is not reported at present. The invention provides a synthesis method of the losartan impurity, and the synthesis method has the advantages of short reaction steps, easily available raw materials, high yield and good regioselectivity.

The present invention discloses a compound preparation containing losartan potassium and a preparation method of the compound preparation. The compound preparation is prepared by the following method:dissolving losartan potassium and kollicoat IR in a methanol aqueous solution and conducting granulation on auxiliary materials to obtain losartan potassium granules wrapped by the kollicoat IR; dissolving hydrochlorothiazide in acetone and conducting granulation on the auxiliary materials; mixing the two granules and conducting tableting to obtain a finished product. The prepared compound preparation containing the losartan potassium can fully isolate the losartan potassium and hydrochlorothiazide, and besides, the drug is added in a state of the solution and fully dispersed on the surfacesof the auxiliary materials and dissolves rapidly. The compound preparation containing the losartan potassium prepared by the process steps has a simple and feasible process, stable quality, improved product quality, and guaranteed product stability during long-term storage.