201 results about "Montelukast Sodium" patented technology

The invention relates to a rapidly-dissolving and stabile montelukast oral solid preparation and a preparation method thereof, wherein the preparation uses montelukast as a raw material drug, is added with a diluents, a disintegrating agent, an additive, an adhesive and a lubricant as auxiliary materials, and uses a pharmaceutically acceptable preparation technology. The preparation and the preparation technology can raises a dissolving speed of the oral preparation, enables the oral preparation to substantially raise the dissolving speed in a dissolving mediums of pH1.0 and pH 4.5, and can raises the medicament stability.

The invention belongs to the technical field of medicines and particularly relates to a montelukast sodium chewable tablet and a preparation method thereof. The montelukast sodium chewable tablet provided by the invention is composed of montelukast sodium, a diluting agent, a lubricating agent, a binding agent, a disintegrating agent, a coloring agent, a sweetening agent and a corrigent. A preparation process of the montelukast sodium chewable tablet adopts absolute ethyl alcohol as a solvent to prepare the binding agent and then the binding agent is mixed with powder of other raw materials and auxiliary materials to carry out wet-method granulation. After being dried, wet grains are mixed with the corrigent and the lubricating agent and then a mixture is tabletted. According to the montelukast sodium chewable tablet prepared by using the process method provided by the invention, the color and the luster of the appearance of the tablet are uniform and bright, the stability is good, the disintegrating speed is high and the bioavailability is high.

The invention relates to montelukast sodium chewing tablets and a preparation process thereof. The tablets comprise montelukast sodium and a filling agent, a diluting agent, a bonding agent, a disintegrating agent, and a flavoring. The tablets are prepared with a powder direct tabletting method. The fluidity and compressibility are good. The chewing tablets have long-term storage stability. The tablets are used in prevention and long-term treatment of asthma of children aged 2 to 14, and are used in relieving symptoms caused by allergic rhinitis.

The invention relates to a stable pharmaceutical composition containing montelukast or salt of the montelukast and a method for preparing the composition. The montelukast sodium is easily affected by moist heat and light and degraded into sulfoxide and cis-isomer, so as to become a problem for development of a pharmaceutical preparation. A stabilizer is added to the stable montelukast sodium tablet disclosed by the invention to coexist with the montelukast sodium. Therefore, increase of the sulfoxide and the cis-isomer can be restrained to the maximal extent.

An amorphous form of montelukast sodium and a montelukast sodium lactose co-precipitate, processes for producing same, pharmaceutical compositions containing same and methods of treatment utilizing same are disclosed.

The invention provides a method for preparing and purifying Montelukast sodium. The method comprises the following steps: A. preparing a disodium salt of 2-[1-(mercapto methyl) cyclopropyl] acetic acid; B. preparing an Montelukast free acid; C. preparing an Montelukast di-n-propylamine salt; D. preparing an Montelukast dicyclohexylamine salt; E. converting the Montelukast dicyclohexylamine salt into an Montelukast sodium salt. The synthesis method is simple in process conditions, good in impurity removal effect and small in risk factor, the sulfoxide impurity is less than 0.1%, other impurities are less than 0.05%, and even a certain impurity cannot be detected, and the purity of the Montelukast sodium is larger than 99.8%. All impurities of the Montelukast sodium can be effectively controlled to be less than 0.05%.

The invention relates to a chemical synthesis drug technology, especially relates to a novel technology for synthesizing montelukast sodium, the invention also relates to a novel intermediate of the synthesized montelukast sodium. The method has the advantages of cheap raw material and easy acquisition, short synthesis route and simple operation, and is suitable for industrial production.

This invention relates to novel compounds and a process for preparation of montelukast sodium.

The invention discloses a preparation method for a montelukast sodium intermediate. The preparation method comprises the steps of reacting 7-chloroquinaldine with m-phthalaldehyde to generate a compound shown in formula II; reacting the compound shown in formula II with vinyl magnesium halide to generate a compound shown in formula III; reacting the compound shown in formula III with a compound shown in formula IV to generate a compound shown in formula V; carrying out a reduction reaction on the compound shown in formula V to generate a compound shown in formula VI; and reacting the compound shown in formula VI with methyl magnesium halide to generate a compound shown in formula I. According to the preparation method disclosed by the invention, production cost is further reduced, and a technological basis is laid for large-scale industrialized production for the intermediate.

The invention provides a montelukast sodium tablet which is prepared by the following method: dissolving montelukast sodium and mycose in alcohol, drying to remove alcohol, and sieving dried substances; then, mixing with alginic acid and pharmaceutically common auxiliary materials, and pressing into tablets. Compared with the prior art, the preparation process disclosed by the invention is simple, and the tablet is quick to disintegrate and good in stability.

The invention relates to the field of medicinal preparations and particularly relates to a montelukast sodium chewable tablet, apreparation method and a determination method of a dissolution rate. Raw materials of the montelukast sodium chewable tablet comprise montelukast sodium, mannitol, microcrystalline cellulose, hydroxy propyl cellulose, crosslinking sodium carboxymethylcellulose, aspartame, ferric oxide, magnesium stearate and cherry essence. The hydroxy propyl cellulose is prepared into a solution with a mass percentage content being 6-8% through water being a solvent and a disintegrating agent is prepared through a wet process of an internal addition method. The montelukast sodium chewable tablet is significantly increased in disintegrating speed and in-vitro dissolution rate. By means of a dissolution curve detection method, quality differences among products in each batch can be effectively distinguished. Differences between products in each batch can be reduced better and a quality risk of the products can be controlled in a controllable range.

A process for the preparation of novel amorphous montelukast sodium by dissolving montelukast free acid in an organic solvent, converting into its alkali salt followed by vacuum drying or spray drying the solution. Alternatively by dissolution of montelukast sodium in organic solvent followed by vacuum drying or spray drying the solution.

The invention relates to an oral solid drug dosage form containing montelukast sodium as a single active drug. The dosage form is prepared from a slow-release kernel and a quick-release outer layer, wherein the slow-release kernel can be prepared from blank-pellets coated by slow-release garments after loading a drug, also can be prepared from a main drug and other proper slow-release macromolecule after extrusion and spheronization, and then the quick-release outer layer is prepared on the slow-release kernel in a manner of loading the drug; the pellets can be filled into the capsules or tabletted. Compared with a common preparation, the novel pulsed release capsules disclosed by the invention achieve the peak plasma concentration at the moment that asthma easily breaks out before dawn; the target of enough time to treat can be met; the medication availability and security of an asthma patient are improved.

The invention belongs to the technical filed of a medicine, and particularly relates to a pharmaceutical composition containing montelukast sodium. The pharmaceutical composition contains montelukast sodium, sucrose fatty acid ester, and L-ascorbic acid. The pharmaceutical composition is good in stability and has excellent quality. The production operation of the pharmaceutical composition is simple and easy, and is suitable for industrial production.

The invention provides a Montelukast sodium film-like preparation, comprising a strip film belt and a treatment effective dose of an active medicine loratadine loaded on the strip film belt, wherein the strip film belt comprises acidic strip film belts and alkaline strip film belts, the acidic strip film belts and the alkaline strip film belts are connected to form one body and alternately arranged, each acidic strip film belt uses a highly water-soluble polymer film forming material as a main body and contains 1 to 20% of an acidic agent on the basis of the weight of the acidic strip film belt, and each alkaline strip film belt uses the highly water-soluble polymer film forming material as a main body and contains 1 to 20% by weight of an alkaline agent on the basis of the weight of the alkaline strip film belt. In the presence of water, the Montelukast sodium film-like preparation provided by the invention becomes an effervescent film, generates considerable bubbles, paralyzes olfactory sensation of people so as to mask odor and is accelerated in dissolving-out.

Disclosed is a process for the preparation of montelukast sodium. The process comprises a) reacting 2-(2-(3(S)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-hydroxypropyl)phenyl)-2-propanol with methane sulfonyl chloride and coupling the resultant mesylate compound with 1-(mercaptomethyl)cyclopropane acetic acid in presence of a base and free alkali source followed by saltification with an amine in a single step reaction and b) converting the montelukast amine salt to montelukast sodium salt.

The invention discloses a pharmaceutical composition taking ambroxol hydrochloride and montelukast sodium as active ingredients and the application of the pharmaceutical composition. The composition can be made into oral preparations including tablets, capsules, granules, chewable tablets, oral solutions and dry suspensions. As the ambroxol hydrochloride and the montelukast sodium are synergistic, the composition has an unexpected effect of treating asthma and is very good in application prospect.

The invention discloses stable montelukast sodium chewable-tablets. The stable montelukast sodium chewable-tablets are composed of montelukast sodium and an adhesive. A preparation method of the stable montelukast sodium chewable-tablets comprises the following steps: blending the montelukast sodium and the adhesive so as to obtain a mixed solution; and then, carrying out granulation by adopting awet method. In addition, the invention further provides a preparation method of the stable montelukast sodium chewable-tablets. The preparation method provided by the invention is simple, controllable, easy to amplify, and good in reproducibility; moreover, the prepared montelukast sodium chewable-tablets are uniform in appearance, color and luster, small in inter-batch differences, and stable inin-vitro dissolution and release.

The invention relates to a chewable tablet containing montelukast sodium and a preparation method of the chewable tablet. The chewable tablet consists of montelukast sodium and pharmaceutically acceptable adjuvants, and the chewable tablet is characterized in that a mannitol-pharmaceutical compound is formed from a montelukast sodium raw material which is micronized and from mannitol; and a microcrystalline cellulose source is optimized, so that the content of impurity sulfoxide and the content of total impurities are reduced, and moreover the preparation is good in dissolution consistency and uniformity in vitro and is greatly high in quality stability.