Studies of Drug Delivery Systems for a Therapeutic Agent Used in Osteoporosis. I. Pharmacodynamics (Hypocalcemic Effect) of Elcatonin in Rabbits Following Rectal Administration of Hollow-Type Suppositories Containing Elcatonin
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概要
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In this study, we developed a new hollow-type suppository containing elcatonin ((Asu^<1,7>)-eel calcitonin, ECT), a synthetic derivative of eel calcitonin, which produces hypocalcemia, as a pharmaceutical preparation for self administration, to be used instead of parenteral injections for patients with osteoporosis. The absorption of ECT from the rectal mucous membrane was evaluated by observation of the decrease in serum calcium (Ca) concentrations following rectal administration in rabbits. ECT was efficiently absorbed from the rectum and effectively decreased serum Ca concentrations. The data of the area under the percent decrease in serum Ca concentration (ΔCa%)-time curve (ΔCa%-AUC), assumed to be an index of the pharmacodynamics (pharmacological effect) of ECT, indicated that similar hypocalcemic effects were obtained following rectal and intravenous administrations of ECT. In regard to the effect of coadministration of other compounds on rectal absorption of ECT, no significant difference in the ΔCa%-AUC between rectal ECT administration with or without nafamostat mesilate (a protease inhibitor) was observed. However, the coadministration of ECT with cytochalasin B or monensin (endocytosis inhibitors) significantly decreased the ΔCa%-AUC, indicating that rectal ECT absorption is probably inhibited by endocytosis inhibitors by endocytosis inhibitors. On the other hand, it was found that sodium decanoate, a mediumchain fatty acid (sodium salt), significantly enhanced the rectal absorption of ECT. We conclude that this ECT hollow-type suppository offers promise as a new method for the administartion of ECT.
- 公益社団法人日本薬学会の論文
- 1998-11-15
著者
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Matsumoto M
Osaka Medical Center For Cancer And Cardiovascular Diseases Osaka
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Matsumoto Misako
Department Of Immunology Osaka Medical Center For Cancer And Cardiovascular Diseases
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Matsumoto Mitsuo
Department of Pharmaceutics, Showa Pharmaceutical University
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Matsumoto Mitsuharu
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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UTOGUCHI Naoki
Department of Pharmaceutics and Biopharmaceutics, Showa Pharmaceutical University
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Watanabe Yoshiteru
Department Of Pharmaceutics And Biopharmaceutics Showa Pharmaceutical University
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Watanabe Y
Showa Pharmaceutical Univ.
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Watanabe Yoshiteru
Showa Pharmaceutical Univ.
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WATANABE Yoshitetu
Department of Pharmaceutics, Showa College of Pharmaceutical Sciences
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MIZUFUNE Yuko
Department of Pharmaceutics, Showa College of Pharmaceutical Sciences
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KUBOMURA Aki
Department of Pharmaceutics, Showa College of Pharmaceutical Sciences
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KIRIYAMA Miyuki
Department of Pharmaceutics, Showa College of Pharmaceutical Sciences
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Utoguchi Naoki
Department Of Biopharmaceutics School Of Pharmaceutical Sciences Teikyo University
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Matsumoto Mitsuhiro
First Department Of Internal Medicine Kumamoto University School Of Medicine
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Matsumoto Mitsuo
Department Of Pharmaceutics And Biopharmaceutics Showa Pharmaceutical University
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Kubomura Aki
Department Of Pharmaceutics Showa College Of Pharmaceutical Sciences
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Mizufune Yuko
Department Of Pharmaceutics Showa College Of Pharmaceutical Sciences
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Kuriyama M
Department Of Pharmaceutics Showa College Of Pharmaceutical Sciences
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Matsumoto Mitsuo
Department Of Ophthalmology Hirosaki University School Of Medicine
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Matsumoto Mitsuo
Department of Hydrocarbon Chemistry, Faculty of Engineering, Kyoto University
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