34 results about "Antitussive drugs" patented technology

Methods and compositions are disclosed utilizing metabolic derivatives of astemizole for the treatment of allergic disorders while avoiding the concomitant liability of adverse effects associated with the astemizole. The metabolic derivatives of astemizole are also useful for the treatment of retinopathy and other small vessel disorders associated with diabetes mellitus and such other conditions as may be related to the antihistamine activity of astemizole. For example, the metabolic derivatives of astemizole are useful for the treatment of asthma, motion sickness, and vertigo, without the concomitant liability of adverse effects associated with astemizole. Furthermore, the metabolic derivatives of astemizole, in combination with non-steroidal anti-inflammatory agents or other non-narcotic analgesics, or in combination with a decongestant, cough suppressant/antitussive or expectorant, are useful for the treatment of cough, cold, cold-like, and/or flu symptoms and the discomfort, headache, pain, fever, and general malaise associated therewith, without the concomitant liability of adverse effects associated with astemizole.

The invention relates to a method for resolving 1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline through enzyme catalysis dynamic kinetics. Specifically, the invention provides a method for resolving 1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline racemate into a single configuration product (S)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline through dynamic kinetics and by utilizing cyclohexane oxidase and a mutant thereof, wherein (S)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline is a key intermediate for synthesizing the central antitussive drug dextromethorphan. The method has the outstanding characteristics of high yield, good stereoselectivity, mild reaction conditions and the like.

The invention discloses imine reductase AtIR(WP_027931121.1) derived from Amycolatopsis thermoflava, imine reductase StIR(WP_023587323.1) derived from Streptomyces thermolilacinus, imine reductase PmIR(WP_091804541.1) derived from Prauserella marina, imine reductase SmIR(WP_020496004.1) derived from Sciscionella marina, imine reductase AaIR(WP_020635634.1) derived from Amycolatopsis alba or iminereductase ShIR(SHE96216.1) derived from Streptoalloteichus hindustanus, and the imine reductase is adopted as a biocatalyst for preparing a key intermediate (S)-1-(4-methoxy benzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline of a central antitussive, namely dextromethorphan. A 5-50g/L substrate can be catalyzed by using corresponding imine reductase, the conversion rate is greater than 99%, and the method has remarkable characteristics of being high in yield, good in stereoselectivity, mild in reaction condition, and the like.

The invention discloses a preparation process for a key intermediate 1-(4-methoxyl)benzyl-1,2,3,4,5,6,7,8-octahydro isoquinoline (mixed isomer) of dextromethorphan hydrobromide serving as a cough relieving medicine, which comprises the following steps of: performing acylation reaction to obtain 1-(4-methoxyl)benzyl-2-alkylacyl-1,2,3,4,5,6,7,8-octahydro isoquinoline (laevo isomer); and racemizing under the alkaline condition to obtain 1-(4-methoxyl)benzyl-2-alkylacyl-1,2,3,4,5,6,7,8-octahydro isoquinoline (mixed isomer); and hydrolyzing under the alkaline condition to obtain the 1-(4-methoxyl)benzyl-1,2,3,4,5,6,7,8-octahydro isoquinoline (mixed isomer). The process aims to overcome the defect of the synthetic process and reduce cost, so that the process is simply and safely operated, the industrial production is qualified, and the yield of products is between 55 and 69 percent.

The invention discloses a method for preparing high-purity dimemorfan and phosphate, relating to a new method for preparing and purifying raw material dimemorfan of an antitussive drug and a relative intermediate. The invention aims to avoid high vacuum degree distillation operation in the preparation of an US3786054 step five intermediate (2-(p-methylbenzyl)-octahydro isoquinolined-(+)tartrate) so as to avoid the disadvantage that individual impurity can not be removed through column separation. The step five intermediate with high purity and high yield is obtained by using acetone and the like as solvents to recrystallize cyclized reaction mixture.

The invention provides an application of licorice flavonoids in preparing antitussives for treating acute and chronic cough caused by a plurality of reasons. The related acute and chronic cough comprises cough symptoms caused by various diseases such as acute and chronic tracheitis, asthma, chronic obstructive disease of lung, idiopathic pulmonary fibrosis, tuberculosis, bacterial pneumonia, bronchiectasis and the like. The licorice flavonoids extracted from liquorice proves to have very strong effect in preventing cough according to pharmacological tests; drug potency thereof is similar to the drug potency of codein in narcotic antitussive; the function mechanism analyses indicate that the licorice flavonoids plays the role of preventing cough through the non-narcotic nerve centre. In addition, the licorice flavonoids extracted from natural plants can also be prepared into health food. The invention solves the problem that the non-narcotic potent antitussives are badly needed, provides a non-narcotic potent antitussives which has fine social and economical benefits.

The invention belongs to the technical field of medicinal preparations, and discloses dextromethorphan chewing gum tablets and an industrially applicable preparation method thereof. The preparation is delivered through a chewing process, so that the defects of the marketed products at present can be overcome, and the tablets have the advantages of no need of water for taking, convenience in taking, good mouthfeel, less adverse effects, quick response, capability of eliminating thirst and the like. The dextromethorphan chewing gum tablets prepared by the invention are mainly used for dry coughand are suitable for cold, acute or chronic bronchitis, bronchial asthma, faucitis, phthisis and cough during other upper respiratory tract infections. The dextromethorphan chewing gum tablets provided by the invention have the advantages of simple preparation process, low cost, easiness in control and easiness for industrial production.

The invention provides a drug composition with the active components of levodropropizine, guaifenesin and pseudoephedrine or acceptable salts on the drugs and a preparation method, which is used for treating nasopharynx mucosa hyperemia, nasal obstruction, sneeze, snivel caused by cold and other diseases, cough and expectoration and other symptoms caused by bronchitis. Compared with the common used centrally antitussive drugs on market, the peripherally antitussive drugs of levodropropizine adopted by the invention have the advantages of obvious antitussive effect and less adverse reaction.

The invention provides oral formulations for the treatment of cold and allergy symptoms. Each formulation combines an antihistamine, an antitussive, and/or a decongestant into one extended release composition. The invention further provides for methods of making and using such formulations, as well as for methods for preventing abuse or extraction of a single drug present in an oral extended release composition comprising two or more of an antihistamine, antitussive, and/or decongestant.

The invention discloses a component ratio and a preparation method of a paracetamol and dihydrocodeine tatrate tablet. The preparation method comprises the following steps: adding auxiliary materials comprising pregelatinized starch, lactose, hydroxypropyl cellulose, HPMC, sodium carboxymethyl starch and magnesium to a prescription dose of main components comprising stearate dihydrocodeine tartrate and paracetamol, carrying out balanced mixing, granulating, drying, finishing, mixing, tabletting, and packaging the obtained material in an aluminum plastic. The tablet has analgesic, antipyretic and antitussive effects, has the advantages of fast efficacies and effectiveness, long action time, good safety, variety of curative effects, reduction of the occurrence of untoward effects, and very extensive clinical application, and is worthy of popularization and application.

The invention is directed to pharmaceutical compositions comprising dextromethorphan and methods of use thereof. Formulations of the present invention include dextromethorphan or a pharmaceutically acceptable salt thereof in a sustained release formulation comprising a controlled release agent. Formulations of the present invention include a core tablet, optionally an active coating and, optionally a film coating. The pharmaceutical compositions may be used as an antitussive, and the invention further relates to the treatment of cough in a patient in need thereof.

The invention discloses a benazolin compound preparation for treating cough and a preparation method of the benazolin compound preparation. The compound preparation comprises the following components: benpipralin and cimetidine in a ratio of (0.01-0.03): (0.1-0.3). The raw material medicines in corresponding parts are taken, proper auxiliary materials are added according to corresponding preparation methods of pharmaceutics, and the raw material medicines can be respectively prepared into dosage forms such as tablets, capsules, solutions, syrup, dry suspensions or granules. Benpipralin is a peripheral non-addictive cough relieving medicine and is mainly used for relieving cough caused by various reasons. The cimetidine is a histamine H2 receptor impedance agent, is a hepatodrug enzyme inhibitor, and can inhibit the activity of hepatodrug enzyme and slow down the metabolism of benpipralin, so that the blood concentration of benpipralin is improved, and the curative effect of benpipralin is enhanced; and the cimetidine alleviates the stimulation of the benpipralin to the stomach by inhibiting gastric acid secretion, and reduces the gastrointestinal tract side effect of the benpipralin.

The present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of guaifenesin, naproxen and at least one further active which is selected to be an antitussive, a decongestant or an antihistamine.

The invention discloses a preparation method of pure vegetoanimal antitussive liquid. The preparation method comprises the following steps: mixing and adding raw materials (65.67% of acetic acid, 0.17% of porcine gall powder, 8.33% of flos chrysanthemi indici, 8.33% of fructus xanthii , 0.8% of pulvis fumi carbonisatus, 8.33% of herba menthae and 8.3% of herba taraxaci) into an acetic acid solution, putting the mixture in a basement at 25 DEG C or below for one year or more to make the mixture undergo a sufficient chemical reaction, and then performing distilling to obtain the antitussive liquid with a very obvious antitussive effect. it is determined that the acidity is PH3 or below after the antitussive liquid stands in a storehouse for three months, and then a finished-product antitussive drug is obtained. The preparation method has simple preparation steps, and compared with a traditional Chinese medicine, the antitussive liquid can kill broader bacteria, has a stronger bacteria killing effect, and is efficient and free of side effects.

The invention discloses application of marmesine in preparation of a cough relieving medicine. According to the invention, marmesine has an obvious cough relieving effect and is found for the first time; furthermore, the cough relieving manner is a non-central cough relieving manner; side effects of conventional central cough relieving medicines in the aspect of a central nervous system are avoided; the invention provides a brand-new selection and idea for current cough treatment, expands selection fields of cough relieving medicines and also makes a contribution to development in the technical field; the marmesine disclosed by the invention is a compound having a definite chemical structure; for pharmacy, the marmesine can be quantitatively fed and is used for preparing modern dosage forms; and furthermore, the marmesine is high in medicine safety and has a potential to develop the cough relieving medicine.