The Experts below are selected from a list of 294 Experts worldwide ranked by ideXlab platform

Pong Zhang - One of the best experts on this subject based on the ideXlab platform.

  • synthesis and Antitussive evaluation of verticinone cholic acid salt a novel and potential cough therapeutic Agent
    Acta Pharmacologica Sinica, 2007
    Co-Authors: Chang Chen, Yonghui Zhang, Hanli Ruan, Pong Zhang
    Abstract:

    Aim: To seek a novel and potent Antitussive drug based on Shedan—Chuanbei powder, a complex of traditional Chinese medicine preparation for cough therapy. Methods: Verticinone—cholic acid (Ver—CA) salt, a novel, salifying derivative of verticinone and cholic acid, both of which are the major bioactive components in Shedan—Chuanbei powder, was synthesized. We then evaluated the Antitussive activity and the acute toxicity of the salt. Results: The new compound, with good solubility in water, has much more potent Antitussive activity in comparison with the same dose of single verticinone and single cholic acid. The administration 3 mg/kg of Ver—CA could result in over 50% reduction of a citric acid-induced cough. Pretreatment with naloxone (0.8 mg/kg, ip) can only partially antagonize its anti-tussive effect. On the other hand, glybenclamide (3 mg/kg, ip), an ATP-sensitive K + channel blocker, can also significantly reduce the Antitussive effect of Ver—CA. A further acute toxicity study showed that the LD50 values of Ver—CA were 3 times that of verticinone. Conclusion: Based on the studies of pharmacology and acute toxicity, the salt has a synergic and attenuated toxicity compared with single verticinone and cholic acid. Moreover, the present study also suggests that Ver—CA, a potential novel Antitussive Agent, may exert its Antitussive effect via both the peripheral (modulated by ATP-sensitive K + channels) and central mechanisms (modulated by the opioid receptor).

  • Synthesis and Antitussive evaluation of verticinone-cholic acid salt, a novel and potential cough therapeutic Agent
    ACTA PHARMACOLOGICA SINICA, 2007
    Co-Authors: Chang Chen, Yonghui Zhang, Hanli Ruan, Pong Zhang
    Abstract:

    Aim: To seek a novel and potent Antitussive drug based on Shedan-Chuanbei powder, a complex of traditional Chinese medicine preparation for cough therapy. Methods: Verticinone-cholic acid (Ver-CA) salt, a novel, salifying derivative of verticinone and cholic acid, both of which are the major bioactive components in Shedan-Chuanbei powder, was synthesized. We then evaluated the Antitussive activity and the acute toxicity of the salt. Results: The new compound, with good solubility in water, has much more potent Antitussive activity in comparison with the same dose of single verticinone and single cholic acid. The administration 3 mg/kg of Ver-CA could result in over 50% reduction of a citric acid-induced cough. Pretreatment with naloxone (0.8 mg/kg, ip) can only partially antagonize its anti-tussive effect. On the other hand, glybenclamide (3 mg/kg, ip), an ATP-sensitive K+ channel blocker, can also significantly reduce the Antitussive effect of Ver-CA. A further acute toxicity study showed that the LD50 values of Ver-CA were 3 times that of verticinone. Conclusion: Based on the studies of pharmacology and acute toxicity, the salt has a synergic and attenuated toxicity compared with single verticinone and cholic acid. Moreover, the present study also suggests that Ver-CA, a potential novel Antitussive Agent, may exert its Antitussive effect via both the peripheral (modulated by ATP-sensitive K+ channels) and central mechanisms (modulated by the opioid receptor).SCI(E)中国科技核心期刊(ISTIC)ARTICLE101591-15962

Chang Chen - One of the best experts on this subject based on the ideXlab platform.

  • synthesis and Antitussive evaluation of verticinone cholic acid salt a novel and potential cough therapeutic Agent
    Acta Pharmacologica Sinica, 2007
    Co-Authors: Chang Chen, Yonghui Zhang, Hanli Ruan, Pong Zhang
    Abstract:

    Aim: To seek a novel and potent Antitussive drug based on Shedan—Chuanbei powder, a complex of traditional Chinese medicine preparation for cough therapy. Methods: Verticinone—cholic acid (Ver—CA) salt, a novel, salifying derivative of verticinone and cholic acid, both of which are the major bioactive components in Shedan—Chuanbei powder, was synthesized. We then evaluated the Antitussive activity and the acute toxicity of the salt. Results: The new compound, with good solubility in water, has much more potent Antitussive activity in comparison with the same dose of single verticinone and single cholic acid. The administration 3 mg/kg of Ver—CA could result in over 50% reduction of a citric acid-induced cough. Pretreatment with naloxone (0.8 mg/kg, ip) can only partially antagonize its anti-tussive effect. On the other hand, glybenclamide (3 mg/kg, ip), an ATP-sensitive K + channel blocker, can also significantly reduce the Antitussive effect of Ver—CA. A further acute toxicity study showed that the LD50 values of Ver—CA were 3 times that of verticinone. Conclusion: Based on the studies of pharmacology and acute toxicity, the salt has a synergic and attenuated toxicity compared with single verticinone and cholic acid. Moreover, the present study also suggests that Ver—CA, a potential novel Antitussive Agent, may exert its Antitussive effect via both the peripheral (modulated by ATP-sensitive K + channels) and central mechanisms (modulated by the opioid receptor).

  • Synthesis and Antitussive evaluation of verticinone-cholic acid salt, a novel and potential cough therapeutic Agent
    ACTA PHARMACOLOGICA SINICA, 2007
    Co-Authors: Chang Chen, Yonghui Zhang, Hanli Ruan, Pong Zhang
    Abstract:

    Aim: To seek a novel and potent Antitussive drug based on Shedan-Chuanbei powder, a complex of traditional Chinese medicine preparation for cough therapy. Methods: Verticinone-cholic acid (Ver-CA) salt, a novel, salifying derivative of verticinone and cholic acid, both of which are the major bioactive components in Shedan-Chuanbei powder, was synthesized. We then evaluated the Antitussive activity and the acute toxicity of the salt. Results: The new compound, with good solubility in water, has much more potent Antitussive activity in comparison with the same dose of single verticinone and single cholic acid. The administration 3 mg/kg of Ver-CA could result in over 50% reduction of a citric acid-induced cough. Pretreatment with naloxone (0.8 mg/kg, ip) can only partially antagonize its anti-tussive effect. On the other hand, glybenclamide (3 mg/kg, ip), an ATP-sensitive K+ channel blocker, can also significantly reduce the Antitussive effect of Ver-CA. A further acute toxicity study showed that the LD50 values of Ver-CA were 3 times that of verticinone. Conclusion: Based on the studies of pharmacology and acute toxicity, the salt has a synergic and attenuated toxicity compared with single verticinone and cholic acid. Moreover, the present study also suggests that Ver-CA, a potential novel Antitussive Agent, may exert its Antitussive effect via both the peripheral (modulated by ATP-sensitive K+ channels) and central mechanisms (modulated by the opioid receptor).SCI(E)中国科技核心期刊(ISTIC)ARTICLE101591-15962

Paul Richert - One of the best experts on this subject based on the ideXlab platform.

  • Simulated moving bed chromatographic resolution of a chiral Antitussive
    Journal of chromatography. A, 1998
    Co-Authors: Eric Francotte, Paul Richert, Marco Mazzotti, Massimo Morbidelli
    Abstract:

    The behavior of a laboratory simulated moving bed (SMB) unit for continuous chromatographic separation of enantiomers has been considered. This was applied to the resolution of a chiral Antitussive Agent, guaifenesin, on Chiralcel OD, during an experimental campaign involving nineteen runs. The application of recently developed criteria for the design and optimization of SMB units allows us to understand and rationalize the experimental results, as well as to indicate how to optimize the separation performances. A three-step procedure to determine the adsorption isotherms needed to apply these criteria is proposed; it is reliable and may be applied also where pure components are not available.

  • Simulated moving bed chromatographic resolution of a chiral Antitussive
    'Elsevier BV', 1998
    Co-Authors: Eric Francotte, Paul Richert, Marco Mazzotti, Massimo Morbidelli
    Abstract:

    The behavior of a laboratory simulated moving bed (SMB) unit for continuous chromatographic separation of enantiomers has been considered, This was applied to the resolution of a chiral Antitussive Agent, guaifenesin, on Chiralcel OD, during an experimental campaign involving nineteen runs. The application of recently developed criteria for the design and optimization of SMB units allows us to understand and rationalize the experimental results, as well as to indicate how to optimize the separation performances. A three-step procedure to determine the adsorption isotherms needed to apply these criteria is proposed: it is reliable and may be applied also where pure components are not available. (C) 1998 Elsevier Science B.V

  • applications of simulated moving bed chromatography to the separation of the enantiomers of chiral drugs
    Journal of Chromatography A, 1997
    Co-Authors: Eric Francotte, Paul Richert
    Abstract:

    Although most preparative chiral separations have been performed in the conventional batch-mode process, interest in simulated moving-bed (SMB) chromatography is growing, because it permits large amounts of mobile phase to be saved and productivity increased, thus reducing production costs. Based on the examples of three different drugs, the usefulness of this technique for the separation of enantiomers on a preparative scale has been demonstrated. Compared to the batch elution chromatography, a reduction of the mobile phase consumption of respectively 81% and 84% has been achieved for the separation of the enantiomers of the antiasthmatic Agent formoterol and of the Antitussive Agent guaifenesin. Furthermore, a higher throughput could be reached under SMB conditions. The influence of feed rate and extract on the separation has also been investigated. The results show that these two factors considerably affect purity and productivity, and constitute important parameters for finely adjusting the chromatographic conditions depending on the requirements. For all racemates, both enantiomers could be obtained with a purity ranging between 99 and 99.9%.

Eric Francotte - One of the best experts on this subject based on the ideXlab platform.

  • Simulated moving bed chromatographic resolution of a chiral Antitussive
    Journal of chromatography. A, 1998
    Co-Authors: Eric Francotte, Paul Richert, Marco Mazzotti, Massimo Morbidelli
    Abstract:

    The behavior of a laboratory simulated moving bed (SMB) unit for continuous chromatographic separation of enantiomers has been considered. This was applied to the resolution of a chiral Antitussive Agent, guaifenesin, on Chiralcel OD, during an experimental campaign involving nineteen runs. The application of recently developed criteria for the design and optimization of SMB units allows us to understand and rationalize the experimental results, as well as to indicate how to optimize the separation performances. A three-step procedure to determine the adsorption isotherms needed to apply these criteria is proposed; it is reliable and may be applied also where pure components are not available.

  • Simulated moving bed chromatographic resolution of a chiral Antitussive
    'Elsevier BV', 1998
    Co-Authors: Eric Francotte, Paul Richert, Marco Mazzotti, Massimo Morbidelli
    Abstract:

    The behavior of a laboratory simulated moving bed (SMB) unit for continuous chromatographic separation of enantiomers has been considered, This was applied to the resolution of a chiral Antitussive Agent, guaifenesin, on Chiralcel OD, during an experimental campaign involving nineteen runs. The application of recently developed criteria for the design and optimization of SMB units allows us to understand and rationalize the experimental results, as well as to indicate how to optimize the separation performances. A three-step procedure to determine the adsorption isotherms needed to apply these criteria is proposed: it is reliable and may be applied also where pure components are not available. (C) 1998 Elsevier Science B.V

  • applications of simulated moving bed chromatography to the separation of the enantiomers of chiral drugs
    Journal of Chromatography A, 1997
    Co-Authors: Eric Francotte, Paul Richert
    Abstract:

    Although most preparative chiral separations have been performed in the conventional batch-mode process, interest in simulated moving-bed (SMB) chromatography is growing, because it permits large amounts of mobile phase to be saved and productivity increased, thus reducing production costs. Based on the examples of three different drugs, the usefulness of this technique for the separation of enantiomers on a preparative scale has been demonstrated. Compared to the batch elution chromatography, a reduction of the mobile phase consumption of respectively 81% and 84% has been achieved for the separation of the enantiomers of the antiasthmatic Agent formoterol and of the Antitussive Agent guaifenesin. Furthermore, a higher throughput could be reached under SMB conditions. The influence of feed rate and extract on the separation has also been investigated. The results show that these two factors considerably affect purity and productivity, and constitute important parameters for finely adjusting the chromatographic conditions depending on the requirements. For all racemates, both enantiomers could be obtained with a purity ranging between 99 and 99.9%.

Massimo Morbidelli - One of the best experts on this subject based on the ideXlab platform.

  • Simulated moving bed chromatographic resolution of a chiral Antitussive
    Journal of chromatography. A, 1998
    Co-Authors: Eric Francotte, Paul Richert, Marco Mazzotti, Massimo Morbidelli
    Abstract:

    The behavior of a laboratory simulated moving bed (SMB) unit for continuous chromatographic separation of enantiomers has been considered. This was applied to the resolution of a chiral Antitussive Agent, guaifenesin, on Chiralcel OD, during an experimental campaign involving nineteen runs. The application of recently developed criteria for the design and optimization of SMB units allows us to understand and rationalize the experimental results, as well as to indicate how to optimize the separation performances. A three-step procedure to determine the adsorption isotherms needed to apply these criteria is proposed; it is reliable and may be applied also where pure components are not available.

  • Simulated moving bed chromatographic resolution of a chiral Antitussive
    'Elsevier BV', 1998
    Co-Authors: Eric Francotte, Paul Richert, Marco Mazzotti, Massimo Morbidelli
    Abstract:

    The behavior of a laboratory simulated moving bed (SMB) unit for continuous chromatographic separation of enantiomers has been considered, This was applied to the resolution of a chiral Antitussive Agent, guaifenesin, on Chiralcel OD, during an experimental campaign involving nineteen runs. The application of recently developed criteria for the design and optimization of SMB units allows us to understand and rationalize the experimental results, as well as to indicate how to optimize the separation performances. A three-step procedure to determine the adsorption isotherms needed to apply these criteria is proposed: it is reliable and may be applied also where pure components are not available. (C) 1998 Elsevier Science B.V