Sustained-release preparation

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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Details

424499, 514 3, 514 12, 530399, A61K 2818

Patent

active

060873248

ABSTRACT:
According to a first embodiment, there is provided a sustained-release preparation comprising a water-insoluble or slightly water-soluble polyvalent metal salt of a water-soluble physiologically active substance which is not an endothelin antagonist, and a biodegradable polymer. The sustained-release preparation of the first embodiment is highly efficient in incorporating the water-soluble physiologically active substance and suppresses the initial burst of the water-soluble physiologically active substance. The sustained-release preparation of the present invention is capable of releasing the water-soluble physiologically active substance while retaining its bioactivity after administration in vivo. Furthermore, the water-soluble physiologically active substance in the sustained-release preparation is kept stable for a long period of time, with little loss of bioactivity.
According to a second embodiment, there is provided a sustained-release preparation comprising an anti-endothelin substance and a biodegradable polymer. The sustained-release preparation of the present invention sustainedly releases an anti-endothelin substance, serving well in the treatment of endothelin-associated diseases.

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Patent Abstract of JP 4-288099.
Lam et al., "Cochinmicins, Novel and Potent Cyclodepsipeptide Endothelin Antagonists from A Microbisphora sp. I. Production, Isolation and Characterization", The Journal of Antibiotics, vol. 45, No. 11, pp. 1709-1716, May 1992.
Zink et al., "Cochinmicins, Novel and Potent Cyclodepsipeptide Endothelin Antagonists from A Microbispora sp. II. Structure Determination", The Journal of Antibiotics, vol. 45, No. 11, pp. 1717-1722, May 1992.
U.S. Patent application No. 071 984,323of Henry Auer, et al., Controlled Released Growth Hormone Containing Microspheres, Filed Dec. 2, 1992.

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