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Sandra Mockoviak – One of the best experts on this subject based on the ideXlab platform.

  • RWJ-22108 — a novel airway tissue — selective calcium channel blocker
    Agents and Actions, 1993
    Co-Authors: John B. Moore, William C. Miller, Sandra Mockoviak

    Abstract:

    RWJ-22108 is a novel calcium entry blocker that has potential therapeutic use as an Antiasthmatic Agent. Although displaying typical potent inhibition of^45Ca uptake into aortic rings (IC_50=7.1 n M ) and displacement of [^3H]nitrendipine from cardiac membranes (IC_50=137 n M ), RWJ-22108 demonstrates tissue selectivity in the inhibition of KCl-induced contractions. RWJ-22108 inhibits the calcium-dependent contraction of canine bronchiolar smooth muscle with an IC_50 of 5.7 n M . The IC_50 femoral artery/IC_50 bronchiolar ratios are 2.85, 8.02, 1.47 and 1.96 for nifedipine, RWJ-22108, verapamil, and gallopamil, respectively. Furthermore, this selectivity ratio (range 2.8–5.5) of RWJ-22108 is also observed when inhibition of other pulmonary and cardiovascular smooth muscles are compared. Using canine tracheal muscle and rabbit aortae, the IC_50 aorta/IC_50 trachea ratio is 1.75 for RWJ-22108 compared to approximately 0.5 for several calcium blocker standards. These results indicate that in vitro RWJ-22108 is a bronchoselective calcium channel blocker.

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  • RWJ-22108–a novel airway tissue–selective calcium channel blocker.
    Agents and Actions, 1993
    Co-Authors: John B. Moore, William C. Miller, Sandra Mockoviak

    Abstract:

    RWJ-22108 is a novel calcium entry blocker that has potential therapeutic use as an Antiasthmatic Agent. Although displaying typical potent inhibition of 45Ca uptake into aortic rings (IC50 = 7.1 nM) and displacement of [3H]nitrendipine from cardiac membranes (IC50 = 137 nM), RWJ-22108 demonstrates tissue selectivity in the inhibition of KCl-induced contractions. RWJ-22108 inhibits the calcium-dependent contraction of canine bronchiolar smooth muscle with an IC50 of 5.7 nM. The IC50 femoral artery/IC50 bronchiolar ratios are 2.85, 8.02, 1.47 and 1.96 for nifedipine, RWJ-22108, verapamil, and gallopamil, respectively. Furthermore, this selectivity ratio (range 2.8-5.5) of RWJ-22108 is also observed when inhibition of other pulmonary and cardiovascular smooth muscles are compared. Using canine tracheal muscle and rabbit aortae, the IC50 aorta/IC50 trachea ratio is 1.75 for RWJ-22108 compared to approximately 0.5 for several calcium blocker standards. These results indicate that in vitro RWJ-22108 is a bronchoselective calcium channel blocker.

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John B. Moore – One of the best experts on this subject based on the ideXlab platform.

  • RWJ-22108 — a novel airway tissue — selective calcium channel blocker
    Agents and Actions, 1993
    Co-Authors: John B. Moore, William C. Miller, Sandra Mockoviak

    Abstract:

    RWJ-22108 is a novel calcium entry blocker that has potential therapeutic use as an Antiasthmatic Agent. Although displaying typical potent inhibition of^45Ca uptake into aortic rings (IC_50=7.1 n M ) and displacement of [^3H]nitrendipine from cardiac membranes (IC_50=137 n M ), RWJ-22108 demonstrates tissue selectivity in the inhibition of KCl-induced contractions. RWJ-22108 inhibits the calcium-dependent contraction of canine bronchiolar smooth muscle with an IC_50 of 5.7 n M . The IC_50 femoral artery/IC_50 bronchiolar ratios are 2.85, 8.02, 1.47 and 1.96 for nifedipine, RWJ-22108, verapamil, and gallopamil, respectively. Furthermore, this selectivity ratio (range 2.8–5.5) of RWJ-22108 is also observed when inhibition of other pulmonary and cardiovascular smooth muscles are compared. Using canine tracheal muscle and rabbit aortae, the IC_50 aorta/IC_50 trachea ratio is 1.75 for RWJ-22108 compared to approximately 0.5 for several calcium blocker standards. These results indicate that in vitro RWJ-22108 is a bronchoselective calcium channel blocker.

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  • RWJ-22108–a novel airway tissue–selective calcium channel blocker.
    Agents and Actions, 1993
    Co-Authors: John B. Moore, William C. Miller, Sandra Mockoviak

    Abstract:

    RWJ-22108 is a novel calcium entry blocker that has potential therapeutic use as an Antiasthmatic Agent. Although displaying typical potent inhibition of 45Ca uptake into aortic rings (IC50 = 7.1 nM) and displacement of [3H]nitrendipine from cardiac membranes (IC50 = 137 nM), RWJ-22108 demonstrates tissue selectivity in the inhibition of KCl-induced contractions. RWJ-22108 inhibits the calcium-dependent contraction of canine bronchiolar smooth muscle with an IC50 of 5.7 nM. The IC50 femoral artery/IC50 bronchiolar ratios are 2.85, 8.02, 1.47 and 1.96 for nifedipine, RWJ-22108, verapamil, and gallopamil, respectively. Furthermore, this selectivity ratio (range 2.8-5.5) of RWJ-22108 is also observed when inhibition of other pulmonary and cardiovascular smooth muscles are compared. Using canine tracheal muscle and rabbit aortae, the IC50 aorta/IC50 trachea ratio is 1.75 for RWJ-22108 compared to approximately 0.5 for several calcium blocker standards. These results indicate that in vitro RWJ-22108 is a bronchoselective calcium channel blocker.

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Amit Kumar Singh – One of the best experts on this subject based on the ideXlab platform.

  • DEVELOPMENT OF MUCOADHESIVE CARBOHYDRATE HETEROPOLYMER MICROBEADS FOR SUSTAIN RELEASE OF THEOPHYLLINE
    International Journal of Pharmacy and Pharmaceutical Sciences, 2015
    Co-Authors: Gaganpreet Kaur, K. Prabhudas Kiran, Amit Kumar Singh

    Abstract:

    Objective: The aim of present study was to develop and evaluate mucoadhesive microbeads for oral sustained release of an Antiasthmatic Agent “theophylline” using natural gums such as sodium alginate and sesbania gum. Methods: The compatibility studies of drug with different polymers were investigated by using DSC (Differential Scanning Calorimeter) and FTIR (Fourier Transform Infrared Spectroscopy). Carbohydrate heteropolymer microbeads of alginate and sesbania gums were prepared by ionotropic gelation technique, where calcium chloride is used as a source of counter ions. Prepared beads were characterized for particle size, entrapment efficiency, surface morphology, swelling index, in vitro release studies and release kinetics. Results: Final optimized formulation consists of a polymer blend of alginate and sesbania gum with hydroxy propyl cellulose as release modifier. Microbeads exhibited good swelling index and high percentage of drug entrapment efficiency. The developed formulation showed a maximum drug release of 92% in 11 h using 0.1 N hydrochloric acid buffer (pH 1.2). The formulation followed Korsmeyer-Peppas and Higuchi release mechanism, releasing the drug by non-fickian diffusion. Prepared beads showed significant mucoadhesion in acidic buffer. Conclusion: The sustained release microbeads were successfully designed for oral administration of theophylline which may be used for the treatment of nocturnal asthma.

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  • DEVELOPMENT OF MUCOADHESIVE CARBOHYDRATE HETEROPOLYMER MICROBEADS FOR SUSTAIN RELEASE OF THEOPHYLLINE Original Article
    , 2015
    Co-Authors: Gaganpreet Kaur, K. Prabhudas Kiran, Amit Kumar Singh

    Abstract:

    Objective: The aim of present study was to develop and evaluate mucoadhesive microbeads for oral sustained release of an Antiasthmatic Agent “theophylline” using natural gums such as sodium alginate and sesbania gum. Methods: The compatibility studies of drug with different polymers were investigated by using DSC (Differential Scanning Calorimeter) and FTIR (Fourier Transform Infrared Spectroscopy). Carbohydrate heteropolymer microbeads of alginate and sesbania gums were prepared by ionotropic gelation technique, where calcium chloride is used as a source of counter ions. Prepared beads were characterized for particle size, entrapment efficiency, surface morphology, swelling index, in vitro release studies and release kinetics. Results: Final optimized formulation consists of a polymer blend of alginate and sesbania gum with hydroxy propyl cellulose as release modifier. Microbeads exhibited good swelling index and high percentage of drug entrapment efficiency. The developed formulation showed a maximum drug release of 92% in 11 h using 0.1 N hydrochloric acid buffer (pH 1.2). The formulation followed Korsmeyer-Peppas and Higuchi release mechanism, releasing the drug by non-fickian diffusion. Prepared beads showed significant mucoadhesion in acidic buffer. Conclusion: The sustained release microbeads were successfully designed for oral administration of theophylline which may be used for the treatment of nocturnal asthma.

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