Pharmaceutical compositions containing dds compounds
AssigneeDaiichi Pharmaceutical Co., Ltd.
InventorsMasayuki Takahashi, Shuichi Sugie, Masahito Takeuchi
Life of this patent
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Abstract
A pharmaceutical composition having an ensured preservation stability, which contains a compound, wherein a polysaccharide derivative having a carboxyl group is bonded to a camptothecin derivative via a spacer or without mediated by any spacer, and a sugar or a sugar alcohol optionally together with a pH-adjusting substance.
Claims17
A pharmaceutical composition containing a compound wherein a polysaccharide derivative having a carboxyl group is bonded to (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-10,13(9H,15H)-dione via a spacer consisting of one amino acid or a spacer consisting of 2 to 8 amino acids bonded to each other via peptide bonds, or a compound wherein a polysaccharide derivative having a carboxyl group is bonded to (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-10,13(9H,15H)-dione without mediated by any spacer and one or more sugars or sugar alcohols selected from the following group:
- maltose,
- glucose,
- lactose,
- trehalose,
- saccharose,
- mannitol,
- inositol,
- galactose,
- ribose,
- xylose,
- mannose,
- sucrose,
- cellobiose,
- raffinose and
- maltotriose.
A pharmaceutical composition containing a compound wherein a polysaccharide derivative having a carboxyl group is bonded to (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-10,13(9H,15H)-dione via a spacer consisting of one amino acid or a spacer consisting of 2 to 8 amino acids bonded to each other via peptide bonds, or a compound wherein a polysaccharide derivative having a carboxyl group is bonded to (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-10,13(9H,15H)-dione without mediated by any spacer, one or more sugars or sugar alcohols selected from the following group, and a pH-adjusting substance:
- maltose,
- glucose,
- lactose,
- trehalose,
- saccharose,
- mannitol,
- inositol,
- galactose,
- ribose,
- xylose,
- mannose,
- sucrose,
- cellobiose,
- raffinose and
- maltotriose.
A pharmaceutical composition containing a compound wherein carboxymethyldextran polyalcohol is bonded to (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-10,13(9H,15H)-dione via a spacer consisting of amino acids represented by the amino acid sequence (N end)-Gly-Gly-Phe-Gly-(C end) and maltose, wherein the molecular weight of said carboxymethyldextran polyalcohol ranges from 50,000 to 500,000, said carboxymethyldextran polyalcohol has a degree of carboxymethylation of from 0.2 to 0.5, (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-10,13(9H,15H)-dione is introduced in an amount of 2 to 10% by weight based on the weight of said compound, the content of maltose, in terms of the weight as maltose monohydrate, is thrice or more as much as the weight of said compound, and the pH value is from 6.0 to 9.0.
A pharmaceutical composition containing a compound wherein carboxymethyldextran polyalcohol is bonded to (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-10,13(9H,15H)-dione via a spacer consisting of amino acids represented by the amino acid sequence (N end)-Gly-Gly-Phe-Gly-(C end), maltose and a pH-adjusting substance, wherein the molecular weight of said carboxymethyldextran polyalcohol ranges from 50,000 to 500,000, said carboxymethyldextran polyalcohol has a degree of carboxymethylation of from 0.2 to 0.5, (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-10,13(9H,15H)-dione is introduced in an amount of 2 to 10% by weight based on the weight of said compound, the content of maltose, in terms of the weight as maltose monohydrate, is thrice or more as much as the weight of said compound, said pH-adjusting substance is hydrochloric acid or sodium hydroxide, and the pH value is from 6.0 to 9.0.
Dependencies are inferred from the claim text.