372 results about "AMBROXOL HYDROCHLORIDE" patented technology

The invention provides a simple method for synthesizing ambroxol hydrochloride, which is characterized in that the ambroxol product is obtained conveniently from amide, the precursor of ambroxol, by a proper reduction method.

The invention relates to an ambroxol hydrochloride freeze-dried powder injection and a preparation method thereof. The freeze-dried powder injection comprises ambroxol hydrochloride and mannitol. The ambroxol hydrochloride freeze-dried powder injection prepared by a freeze-drying technology has good stability and high dissolution velocity while all other indexes accord with regulation.

The invention discloses an oral disintegration tablet of alcaine aminobromisuo, which contains alcaine aminobromisuo with effective dosage and pharmacological findings, wherein the alcaine aminobromisuo is processed by metarchon with rate of aminobromisuo and metarchon at 1: 0. 1-1. 5, which is blended with pharmacologically acceptable findings; the metarchon can be medically inorganic oxide or / and medicinal organic acid and salt; the acceptable findings is filler, corrigent, disintegration agent, adhesive and lubricant; the oral disintegration tablet of alcaine aminobromisuo hasn't bitterness and numb sense to disintegrate within one minute with stripping degree not less than 90%. The invention is convenient and simple to control with high yield and low energy consumption, which widens the resource of metarchon to save cost.

The invention relates to a preparation method of ambroxol hydrochloride. The preparation method comprises the steps of: directly obtaining a compound in formula (2) from simple intermediate 1,3-cyclohexadiene under the catalysis of palladium acetate, reacting with a compound in formula (3) to obtain a compound in formula (4), hydrolyzing the compound in the formula (4) in the presence of potassium carbonate, reducing by sodium borohydride, and carrying out salt forming with hydrochloric acid to obtain ambroxol hydrochloride. Therefore, synthesis of key intermediate trans-4-amino cyclohexanol in a common process is avoided and the separation of racemic products is avoided. The method is simple and feasible in operation, mild in conditions, mature in process and high in product yield and purity, and is suitable for industrialized mass production.

The invention relates to a medicinal composition of ambroxol in a non-salt form. Particularly, the invention especially relates to a composition comprising ambroxol in a base form and other oral substances with or without physiological activity or a drug container. The inventor surprisingly finds that when ambroxol is prepared into an oral preparation in a non-salt form, and especially a preparation such as a suspension, a dry suspension, a granule and the like needing to be diluted and prepared with water before drinking, the mouthfeel is significantly improved when compared with that of an ambroxol hydrochloride solution, and the ambroxol preparation has significantly slower absorption in vivo than an ambroxol hydrochloride preparation; and the realization of a slow-release effect which requires great effort on preparation process can be easily achieved. It is well known that the slow release of a drug can reduce drug side effects and increase security with the guarantee of curative effects.

The invention discloses an oral liquid for treating a respiratory disease. The oral liquid is aqueous solution, does not comprise a preservative but comprises the following components: 1-8g / L ambroxol hydrochloride and 250 to 350 g / L xylitol. A preparation method for the oral liquid comprises the following steps of: 1) adding the xylitol in the amount into water, and stirring until dissolving completely; 2) adding the ambroxol hydrochloride, or adding the ambroxol hydrochloride and clenbuterol hydrochloride into the solution obtained in the step 1) in turn, and stirring until dissolving; and 3) adding a pH regulator into the solution obtained in the step 2), regulating the pH of the oral liquid to be between 4.0 and 6.0; adding one or a combination of a sweetening agent, an antioxidant and an aromatizer; and stirring uniformly to obtain the oral liquid. The oral liquid obtained by the preparation method does not comprise the preservative but has adequate chemical stability and microbial stability, avoids a series of toxic and harmful effects caused by using the preservative, and ensures the safety of medication.

The invention provides an ambroxol hydrochloride atomization inhalant and a preparation method and application thereof. The ambroxol hydrochloride atomization inhalant uses injection water as a solvent and contains ambroxol hydrochloride with a concentration of 7.5 mg / ml and a pharmaceutically acceptable carrier with a concentration of 18 to 28 mg / ml; the carrier comprises a pH value stabilizing agent which is one or more selected from the group consisting of sodium pyrosulfite, sodium hydrosulphite and sodium hydrogen sulfite. The preparation method comprises the following steps: weighing ambroxol hydrochloride and the pharmaceutically acceptable carrier, adding a proper amount of injection water to dissolve ambroxol hydrochloride and the pharmaceutically acceptable carrier, carrying out cooling, then adjusting a pH value by using the pH value stabilizing agent containing sodium pyrosulfite, sodium hydrosulphite and / or sodium hydrogen sulfite and adding water until a desired total amount is almost obtained; then carrying out full stirring with medicinal carbon, carrying out filtering to remove carbon and adding water until the desired total amount is obtained; carrying out filtering with a microfiltration membrane; and filling each bottle with 2 ml, 4ml, 10 ml or 20 ml of the atomization inhalant, then introducing nitrogen and carrying out autoclaved sterilization. The invention further relates to application of the atomization inhalant in preparation of drugs used for treating diseases of the respiratory system.

The invention discloses an ambroxol hydrochloride orally disintegrating tablet. The orally disintegrating tablet comprises ambroxol hydrochloride and is prepared by proportioning the following raw auxiliary materials in part by weight: ambroxol hydrochloride flavor masking particles are prepared by coating and contain 1 part of ambroxol hydrochloride agents, 1-2 parts of filling agents, 0.1-0.25 part of disintegrating agents, 0.5-1 part of flavoring agents, 0.01-0.05 part of mouth cooling agents, 0.029-0.05 part of lubricating agents and 0.03-0.05 part of flow agents. The ambroxol hydrochloride orally disintegrating tablet has a good disintegrating effect and good dissolution rate. As a certain proportion of mouth cooling agents are added in the auxiliary materials, the discomfort generated to an oral cavity and a throat part is effectively alleviated after drug taking. The ambroxol hydrochloride orally disintegrating tablet has good mouthfeel and short duration of bad mouthfeel, can bring good drug taking process to a patient after being taken and is suitable for industrialization production.

The invention relates to a synthesis method of an ambroxol hydrochloride compound, comprising the following steps of: 1) taking a compound of a formula (I) as a starting raw material; taking DMAP (Dimethylaminopyridine) and 4-dimethylamino cyclohexanol as catalysts to react with p-amino cyclohexanol under the condition of the presence of absolute methanol and anhydrous potassium carbonate to obtain an intermediate; and 2) under the condition of the presence of a solvent ethanol, water and glacial acetic acid, taking the intermediate and concentrated hydrochloric acid to react to generate ambroxol hydrochloride. According to the synthesis method disclosed by the invention, diacetylamido is used for carrying out complete protection on active nitrogen atoms of the starting raw material to avoid a benzene ring 2-substituents amino secondary reaction; the difficulties of the prior art that more condensation secondary reactions, low yield, high catalyst cost, harsh process conditions and the like are overcome to form a novel process with a short reaction line, moderate conditions and small pollution; the yield is higher than 67%; impurity types and contents are obviously reduced; and only one of five known impurities exists and the product purity is more than 99.9%. The formula (I) is shown as the specification.