Showing papers on "Antitussive Agent published in 2003"
TL;DR: It is demonstrated, for the first time, that compounds 1 and 5 showed significant antitussive activities in guinea pig after cough induction by citric acid aerosol stimulation.
Abstract: Bioactivity-directed fractionation of the crude extract of Stemona tuberosa led to the isolation and characterization of four new stenine-type Stemona alkaloids, namely tuberostemonine J ( 2), tuberostemonine H ( 3), epi-bisdehydrotuberostemonine J ( 4) and neostenine ( 5), together with the known neotuberostemonine ( 1). These five isolated alkaloids were examined for antitussive activity in guinea pig after cough induction by citric acid aerosol stimulation. In this report, we demonstrated, for the first time, that compounds 1 and 5 showed significant antitussive activities. Further study of the structure-activity relationship on these isolated alkaloids and two synthetic analogues revealed that the saturated tricyclic pyrrolo[3,2,1- jk] benzazepine nucleus is the primary key structure contributing to the antitussive activity and all cis configurations at the three ring junctions are the optimal structure for the antitussive activity of stenine-type Stemona alkaloids.
121 citations
TL;DR: The results showed that the cough suppressive activity of E. officinalis is dose-dependent, and a higher dose of this substance perorally was more effective, especially in decreasing the number of cough efforts, frequency of cough, and the intensity of cough attacks in inspirium and expirium was more pronounced.
63 citations
Patent•
25 Apr 2003
TL;DR: A consumable film adapted to adhere to and dissolve in the oral cavity of a consumer comprising at least one water-soluble polymer, one antitussive agent, and a mucosa-coating effective amount of a coccoating agent is defined in this article.
Abstract: 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.
54 citations
TL;DR: The methanol extract of Ficus racemosa Linn (Moraceae) (stem bark) (MEFR) was tested for its antitussive potential against a cough induced model by sulphur dioxide gas in mice and demonstrated significant antitussives activity at all tested dose levels when compared with the control.
Abstract: The methanol extract of Ficus racemosa Linn (Moraceae) (stem bark) (MEFR) was tested for its antitussive potential against a cough induced model by sulphur dioxide gas in mice. The extract demonstrated significant (p < 0.001) antitussive activity at all tested dose levels when compared with the control. The antitussive activity of the extract was comparable to that of codeine phosphate (10 mg), a standard antitussive agent. The extract exhibited maximum inhibition of 56.9% at a dose of 200 mg/kg (p.o.) 90 min after administration. Copyright © 2003 John Wiley & Sons, Ltd.
43 citations
TL;DR: The methanol extract of A. webbiana Lindl was evaluated for its effect on a cough model induced by sulphur dioxide gas in mice and exhibited significant antitussive activity compared with the control in a dose dependent manner.
Abstract: The methanol extract of A. webbiana Lindl was evaluated for its effect on a cough model induced by sulphur dioxide gas in mice. When administered orally it exhibited significant antitussive activity compared with the control in a dose dependent manner. The antitussive activity of the extract was compared with that of codeine phosphate, a prototype antitussive agent. The A. webbiana leaf extract (400 and 600 mg/kg) showed maximum inhibition of cough frequency by 71.69% and 78.67%, respectively, when compared with the control group and was comparable in effect to codeine phosphate.
25 citations
TL;DR: The results indicate that the antitussive effect of WIN 55212-2 is mediated by the activation of cannabinoid CB(1) receptors and mu(2) (naloxonazine-insensitive)-opioid receptors, but not mu (1) ( nalox onazine-sensitive)- or kappa-opioids receptors.
16 citations
TL;DR: The antitussive activity of methanol extract of Ionidium suffruticosam Ging.
Abstract: The present study was carried out to evaluate the antitussive potential of methanol extract of Ionidium suffruticosam Ging. (Violaceae) which was investigated for its effect on a cough model induced by sulfur dioxide gas in albino mice. It exhibited significant dose-dependent antitussive activity when compared with the control, 250 and 500 mg/kg (p.o.) of the extract showing 28.37% and 54.16% inhibition of the cough with respect to control group. The antitussive activity of the extract was comparable to that of codeine phosphate, a prototype antitussive agent.
9 citations
TL;DR: The development of novel drugs that maintain or improve upon the antitussive efficacy of the opioids and do not possess MOP liabilities would represent a substantial improvement over currently available cough treatments.
Abstract: Cough is frequently associated with a wide array of respiratory infections, ailments and disorders. Consequently, cough is the number one symptomatic reason why people visit medical healthcare providers. Nonetheless, when cough-suppressant therapy is required by patients, many physicians are limited primarily to a single pharmacological class of antitussive agent, namely, opioids. Opioids, such as codeine, dominate the antitussive prescription market. These drugs act centrally within the CNS to attenuate cough due to a variety of causes. However, opioids often elicit significant receptor-related μopioid (MOP) untoward side effects such as constipation, respiratory depression, sedation, tolerance and addiction. The development of novel drugs that maintain or improve upon the antitussive efficacy of the opioids and do not possess MOP liabilities would represent a substantial improvement over currently available cough treatments. New antitussive pharmacological targets include non-MOP opioids, specifically, ...
9 citations
TL;DR: Antibodies to bradykinin in ultralow doses were most potent in relieving capsaicin-induced cough, and antibodies to serotonin and, particularly, to histamine produced a smaller effect.
Abstract: We studied antitussive activity of antibodies to inflammatory mediators (bradykinin, histamine, and serotonin) in ultralow doses Experiments were performed on guinea pigs with cough induced by citric acid and capsaicin Test preparations suppressed cough produced by citric acid Antibodies to bradykinin in ultralow doses were most potent in relieving capsaicin-induced cough (up to 85%); antibodies to serotonin and, particularly, to histamine produced a smaller effect Potentiated histamine and serotonin possessed polymodal properties
8 citations
Patent•
19 Nov 2003
TL;DR: In this paper, the authors proposed a medicinal composition containing the antitussive agent, which contains following methylophiopogonanone A of formula (I) and/or MOGONanone B of formula(II).
Abstract: PROBLEM TO BE SOLVED: To provide an antitussive agent almost without having central adverse effect and also having potent antitussive activity, and a medicinal composition containing the antitussive agent SOLUTION: This antitussive agent contains following methylophiopogonanone A of formula (I) and/or methylophiopogonanone B of formula (II) COPYRIGHT: (C)2004,JPO
5 citations
Patent•
28 Apr 2003
TL;DR: In this article, a composition for relieving, preventing and/or treating cough includes a sufficient amount of Cynanchi Atrati Radix extract as an active component, which is prepared by extracting water, ethanol, hexane, ethyl acetate or a combination thereof.
Abstract: An antitussive agent. A composition for relieving, preventing and/or treating cough includes a sufficient amount of Cynanchi Atrati Radix extract as an active component. The effective Cynanchi Atrati Radix extract is prepared by extracting Cynanchi Atrati Radix with water, ethanol, hexane, ethyl acetate or a combination thereof. The crude extract can be further fractioned by ultrafiltration or reverse phase column.
Patent•
28 Apr 2003
TL;DR: In this article, an antitussive agent consisting of Cynanchi atratiradix extract (A) and carrier or excipient was used for preparation of (A).
Abstract: An antitussive agent comprises Cynanchi atratiradix extract (A) and carrier or excipient. An independent claim is included for preparation of (A). ACTIVITY : Antitussive. Pulverized dry material of Cynanchum atraturm (1 kg) was heated to boil and refluxed twice With 10 L of the following solvents: water (test-1), 50% ethanol (test-2), 95% ethanol (test-3), ethyl acetate (EA) (test-4) and hexane (test-5), respectively. The extracts were then filtered with 350 mesh sieve and the filtrates were collected, respectively. The filtrates were further centrifuged continuously at 1089xg ( Avanti J-251(RTM, High performance centrifuge)) for 3 hr to precipitate micropartic1es and impurities. The supernatants were further concentrated and freeze-dried. The inhibition activity of extracts (1 g/kg dosage) on citric acid induced cough was evaluated. The antitussive inhibition assessment showed at least 60% of citric acid-induced coughs. MECHANISM OF ACTION : None given.
Patent•
27 Jun 2003
TL;DR: In this article, an antitussive agent consisting of Cynanchi atratiradix extract (A) and carrier or excipient was used for preparation of (A).
Abstract: An antitussive agent comprises Cynanchi atratiradix extract (A) and carrier or excipient. An independent claim is included for preparation of (A). ACTIVITY : Antitussive. Pulverized dry material of Cynanchum atraturm (1 kg) was heated to boil and refluxed twice With 10 L of the following solvents: water (test-1), 50% ethanol (test-2), 95% ethanol (test-3), ethyl acetate (EA) (test-4) and hexane (test-5), respectively. The extracts were then filtered with 350 mesh sieve and the filtrates were collected, respectively. The filtrates were further centrifuged continuously at 1089xg ( Avanti J-251(RTM, High performance centrifuge)) for 3 hr to precipitate micropartic1es and impurities. The supernatants were further concentrated and freeze-dried. The inhibition activity of extracts (1 g/kg dosage) on citric acid induced cough was evaluated. The antitussive inhibition assessment showed at least 60% of citric acid-induced coughs. MECHANISM OF ACTION : None given.