Showing papers on "Antitussive Agent published in 1997"

Transdermally administered dextromethorphan as antitussive agent

Abstract: Device for transdermal administration of dextromethorphan, (+)-3-methoxy-17-methyl-9a,13a,14a-morphinan, optionally encompassing salts, prodrugs and metabolites thereof, optionally together with pharmaceutically acceptable carrier(s) to a human being or an animal in order to achieve an antitussive effect. Use of an antitussive compound comprising dextromethorphan, (+)-3-methoxy-17-methyl-9a,13a,14a-morphinan, optionally encompassing salts, prodrugs and metabolites thereof, and optionally together with pharmaceutically acceptable carrier(s), for the manufacture of a composition to be administered transdermally for achieving an antitussive effect. Method for achieving an antitussive effect in a living body by transdermal administration of a compound comprising dextromethorphan, (+)-3-methoxy-17-methyl-9a,13a,14a-morphinan, optionally encompassing salts, prodrugs and metabolites thereof, and optionally together with pharmaceutically acceptable carrier(s).

Experimental studies on the antitussive properties of the new xanthine derivative 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]. 1st communication: in vivo demonstration of the effects on animal models of cough and of mucociliary clearance.

Abstract: CH-13584 (formerly: KHL-8425, 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl)methyl], CAS 115779-20-9) is a new xanthine derivative synthesized with the purpose to develop a highly safe compound against several pulmonary disorders, especially for the treatment of acute and chronic cough CH-13584 showed acute and chronic antitussive activity on citric acid spray-evoked cough model in guinea-pig CH-13584 was also effective on capsaicine spray and mechanical irritation-induced cough in guinea-pig and rabbit, respectively The effectivity of CH-13584 on antitussive tests reached and in some cases even exceeded the effectivity of the reference compounds The compound increased the mucociliary clearance at lower doses than bromhexine

Experimental studies on the antitussive properties of the new xanthine derivative 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]. 2nd communication: investigations on theophylline-like activities.

Abstract: CH-13584 (formerly: KHL-8425, 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl)methyl], CAS 115779-20-9) is a new xanthine derivative, structurally related to theophylline. Potent antitussive activity in the 4 to 8 mg/kg dose range, by the oral route, was already demonstrated for this compound. In the present work, it is shown that contrary to theophylline, CH-13584 does not interact with adenosine A 1 receptor and is a weaker inhibitor of cyclic nucleotide phosphodiesterase. In addition, CH-13584 is a less active bronchodilator in vitro and in vivo. It is also devoid of the cardiovascular and behaviour side-effects of theophylline and of effects on diuresis at dosage well above the antitussive dose. CH-13584, therefore, has a different pharmacological profile compared to theophylline and is devoid of the known side-effects of the latter. Such differences could result from a different biochemical profile.

Oral liquid preparation

Abstract: PROBLEM TO BE SOLVED: To obtain an oral liquid preparation masked in strong bitterness and specific bitterness, improved in flavor and capable of readily ingesting without accompanying pain by including a bitterness ingredient and maple flavors. SOLUTION: This oral liquid preparation reduced in bitterness and capable of readily ingesting is obtained by including a bitterness ingredient such as remedy for the cold, antipyretic, analgesic, antiphlogistic, antitussive agent, expectorant, antihistamic agent, hemostatic agent or vitamin Bs and maple flavors and preferably further, coffee flavors. COPYRIGHT: (C)1998,JPO