55 results about "Antitussive Agent" patented technology

A consumable film adapted to adhere to and dissolve in the oral cavity of a consumer comprising at least one water soluble polymer, at least one antitussive agent and a mucosa-coating effective amount of a mucosa-coating agent.

The present invention is drawn to a device for the transdermal administration of dextromethorphan, (+)-3-methoxy-17-methyl-9a,13a,14a-morphanin, and salts, prodrugs and metabolites thereof, together with a pharmaceutically acceptable carrier, to a human being or animal in need thereof, to achieve an antitussive effect. The present invention is further drawn to a method of achieving an antitussive effect in a human being or animal which comprises transdermally administering dextromethorphan, (+)-3-methoxy-17-methyl-9a,13a,14a-morphanin, and salts, prodrugs and metabolites thereof, together with a pharmaceutically acceptable carrier.

The present invention relates to compositions comprising an antitussive, a decongestant and an expectorant, and in a specific embodiment comprising hydrocodone, phenylephrine hydrochloride and guaifenesin, wherein the composition may be substantially free of added sugar and added alcohol, and methods for using these compositions for the treatment of patients suffering from, for example and without limitation, coughing, sneezing, rhinorrhea, and/or nasal obstruction.

The present invention relates to compositions that comprise an expectorant, an extended release antitussive, and an extended release decongestant, in liquid. Specifically, the compositions may comprise guaifenesin, and the tannate salts of phenylephrine and dextromethorphan. The present invention also includes methods for using these compositions for treatment of patients suffering from, for example and without limitation, coughing, sneezing, rhinorrhea, and/or nasal obstruction.

A novel composition of three recognized antitussive agents, when used in combination, work in an additive fashion to suppress cough. Each drug has a desirable effect of suppressing cough in a unique fashion. However, undesirable side effects can occur in humans at concentrations at which the drug has its maximal antitussive effect. Pharmaceutical compositions of theobromine, dextromethorphan, and an antihistamine with central nervous system effect, such as dexbrompheniramine, maximize cough suppression while decreasing the likelihood of side effects when used in combination.

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 present invention relates to a method, which comprises that (R)-(-)-3-chloro-1,2-propanediol and a phosphocholine tetramethyl ammonium salt are subjected to a substitution reaction, and ion exchange resin purification is performed to obtain a L-alpha-choline glycerophosphate pure product. According to the present invention, the used chiral intermediate (R)-(-)-3-chloro-1,2-propanediol is further a key chiral intermediate of an antitussive agent levodropropizine, has characteristics of stable chemical property and convenient and easy obtaining, and is especially for L-alpha-choline glycerophosphate industrial production.

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 present invention provides an organoleptically pleasing lozenge containing an antitussive selected from the group consisting of dextromethorphan, diphenhydramine, caramiphen, carbapentane, ethylmorphine, noscapine, codeine, and mixtures thereof, complexed with an ion exchange resin wherein the particle size of the resin is 38 μm or less in diameter. Also provided is a process for producing the lozenge and methods of administering the lozenge.

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 relates to a method for preparing a safe and effective antibechic dimimorfan phosphate. The method comprises steps of reacting dextrorphane with trifluoro-methylsulfonyl chloride in triethylamine so as to generate dextrorphane trifluoro-methyl sulfone chloride ester; reacting the dextrorphane trifluoro-methyl sulfone chloride ester with tetramethyltin in methylbenzene so as to generate (9s, 13s, 14s)-3, 17-dimethyl morphinan (or adding the dextrorphane trifluoro-methyl sulfone chloride ester into mixed solvent of THF and N-methyl-2-pyrrolidone, adding catalyst ferric acetylacetonate and methyl magnesium bromide, stirring and heating reflux for 12 hours, so as to prepare (9s, 13s, 14s)-3, 17-dimethyl morphinan), furthermore, reacting with phosphoric acid so as to salify to prepare target product (9s, 13s, 14s)-3, 17-dimethyl morphine phosphate-dimimorfan phosphate. The method takes commercially available dextrorphane as the raw material, and prepares the target product through three steps of esterification, methylation and salification. The method has advantages of easily obtained raw materials, few synthesis steps, simple technology, low cost, high yield, high purity of the product and strong economic practicability, and is applicable to industrial production.

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.

A pharmaceutical composition for use in relieving cold and cough symptoms in a mammal includes ibuprofen, hydrocodone bitartrate and an antihistamine (or a decongestant). The ibuprofen is in a therapeutically effective amount sufficient to act as an analgesic and an anti-inflammatory. The hydrocodone bitartrate is in a therapeutically effective amount sufficient to act as an antitussive and an analgesic. The antihistamine is in a therapeutically effective amount to act as an antihistamine. A fatty excipient may be added to the active ingredients to facilitate encapsulation. Multiple layers of the fatty excipient may be employed in varying release formulations and to facilitate identification of the composition.

The invention provides a method for simultaneously detecting contents of four effective ingredients (including schisandrin, praeruptorin A, praeruptorin and shionone) in an officinal antitussive tablet. The method comprises the steps of applying a modern high performance liquid chromatography technology, and taking octodecyl silane bonded silica gel as a filling agent; taking acetonitrile as a mobile phase A, and water as a mobile phase B; and calculating the number of theoretical plates to be not less than 5000 according to a schisandrin peak. In an elution process, gradient elution that allows a concentration proportion of the mobile phase A to the mobile phase B to change gradually is combined with isocratic elution that allows a proportion of the mobile phase A to the mobile phase B to be constant, so that a specific gradient elution procedure is formed; two or three gradient elutions are conducted; and the change detection is conducted on wavelength in a gradient elution process. The method can simultaneously detect the contents of schisandrin, praeruptorin A, praeruptorin and shionone in the antitussive tablet qualitatively and quantitatively, is simple, convenient, quick and high in specificity, and can raise the quality control level of the antitussive tablet effectively.

The invention discloses a slow-release dry suspension of dextromethorphan hydrobromide which is slowly released in the gastrointestinal tract environment. The formulation contains dextromethorphan hydrobromide and a pharmaceutically acceptable polymer. According to weight percentage, the preparation contains 10-90% of dextromethorphan hydrobromide and 10-90% of auxiliary materials. The supplementary materials for sustained release are one or more of cation exchange resin, methyl cellulose, ethyl cellulose, acrylic resin and hydroxypropyl methyl cellulose. Compared with the immediate-release preparation, the controlled-release preparation of the present invention can maintain the effective blood drug concentration within 24 hours, improve the curative effect, have less toxic and side effects, be convenient to take and carry, and reduce the number of times of taking. The sustained-release preparation of the invention can maintain a more stable blood drug concentration within 24 hours, improve curative effect, and have less toxic and side effects. This preparation only needs to be administered once a day. The controlled-release preparation of the present invention will be clinically used as an antitussive.

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 relates to new morphine derivatives deuterated at the 7,8-position of the morphine ring, furthermore to a process for the preparation thereof, and to pharmaceutical compositions comprising them. The new deuterated morphine derivatives show high and selective μ-opioid receptor binding activity leading to the benefit of higher analgesic activity at lower dosages inducing thereby reduced adverse effects compared to the hydrogenated derivatives. The compounds of the invention are useful for example in the treatment of pain or can be used as antitussive agents with a reduced risk of the possibility of drug abuse.

The invention discloses an antihistamine and sleep promotion composition and soft capsules. The composition comprises the following components in percentage by weight: 5-45% of diphenhydramine hydrochloride, 30-90% of polyethylene glycol and 1-25% of polyalcohol. Each soft capsule comprises soft capsule rubber cover and content, wherein the content comprises the following components in percentage by weight: 5-45% of diphenhydramine hydrochloride, 30-90% of polyethylene glycol and 1-25% of polyalcohol; the soft capsule rubber cover comprises the following components in percentage by weight: 50-90% of gelatin, 5-70% of plasticizer, 5-15% of purified water and 0-0.5% of coloring agent. The invention aims at providing an antihistamine and sleep promotion composition which is simple in composition, stable and effective and fast in dissolution and absorption, and soft capsules containing the antihistamine and sleep promotion composition. The soft capsules disclosed by the invention are suitable for the allergy of the skin mucosa, prevention of motion sickness, Parkinson's disease and extrapyramidal symptoms for calming and hypnosis, enhance the effects of cough medicines, and are suitable for the cough caused by cold or allergy.