Sustained-release preparation
AssigneeTakeda Chemical Industries, Ltd.
InventorsYoshio Hata, Hikaru Taira, Jun Sato, Satoshi Iinuma
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Abstract
A sustained-release preparation comprising a bioactive substance having an acidic group and a biodegradable polymer having an optionally protected basic group which improves the rate of incorporation of the bioactive substance, suppresses its leakage early after administration, and exhibits constantly suppressed release for an extended period of time.
Claims3
A sustained-release preparation which comprises a bioactive substance having an acidic group and a biodegradable polymer selected from the group consisting of biodegradable polymers (Ia)-(Ig) having the following formulae:
- POLY-CO—A—X (Ia)
- wherein, in formula (Ia), POLY represents the principal chain of the biodegradable polymer:
- A represents O, NH or S:
- and X represents a hydrocarbon group having 1 to 3 amino groups,
- wherein, in formula (Ib), POLY represents the principal chain of the biodegradable polymer;
- X represents a hydrocarbon group having 1 to 3 amino groups;
- and ring A1 is a 5- to 7-membered ring,
- wherein, in formula (Ic), POLY represents the principal chain of the biodegradable polymer:
- Y represents a hydrocarbon group having 1 to 3 amino groups;
- and ring A2 is a 5- to 7-membered ring,
- X—CO—O-POLY-CO—A—X (Id)
- wherein, in formula (Id), POLY represents the principal chain of the biodegradable polymer;
- A represents O, NH or S;
- and X represents a hydrocarbon group having 1 to 3 amino groups,
- wherein, in formula (Ie), POLY represents the principal chain of the biodegradable polymer:
- X represents a hydrocarbon group having 1 to 3 amino groups:
- and ring A1 is a 5- to 7-membered ring,
- wherein, in formula (If), POLY represents the principal chain of the biodegradable polymer;
- X and Y represent a hydrocarbon group having 1 to 3 amino groups:
- and ring A2 is a 5- to 7-membered ring, and
- X—CO—O-POLY-CO—R0 (Ig)
- wherein, in formula (Ig), POLY represents the principal chain of the biodegradable polymer;
- X represents a hydrocarbon group having 1 to 3 amino groups;
- and R0 represents a hydrocarbon group.
A biodegradable polymer selected from the group consisting of biodegradable polymers (Ia)-(Ig) having the following formulae:
- POLY-CO—A—X (Ia)
- wherein, in formula (Ia), POLY represents the principal chain of the biodegradable polymer other than polyamides and polyamino acids;
- A represents O, NH or S;
- and X represents a hydrocarbon group having 1 to 3 amino groups,
- wherein, in formula (Ib), POLY represents the principal chain of the biodegradable polymer;
- X represents a hydrocarbon group having 1 to 3 amino groups;
- and ring A1 is a 5- to 7-membered ring,
- wherein, in formula (Ic), POLY represents the principal chain of the biodegradable polymer;
- Y represents a hydrocarbon group having 1 to 3 amino groups;
- and ring A2 is a 5- to 7-membered ring,
- X—CO—O-POLY-CO—A—X (Id)
- wherein, in formula (Id), POLY represents the principal chain of the biodegradable polymer other than polyamides and polyamino acids;
- A represents O, NH or S;
- and X represents a hydrocarbon group having 1 to 3 amino groups,
- wherein, in formula (Ie), POLY represents the principal chain of the biodegradable polymer, X represents a hydrocarbon group having 1 to 3 amino groups;
- and ring A1 is a 5- to 7-membered ring,
- wherein, in formula (If), POLY represents the principal chain of the biodegradable polymer;
- X and Y represent a hydrocarbon group having 1 to 3 amino groups;
- and ring A2 is a 5- to 7-membered ring, and
- X—CO—O-POLY-CO—R0 (Ig)
- wherein, in formula (Ig), POLY represents the principal chain of the biodegradable polymer;
- X represents a hydrocarbon group having 1 to 3 amino groups;
- and R0 represents a hydrocarbon group.
Dependencies are inferred from the claim text.