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US 7,125,546 B2Granted
Polymeric micelle containing cisplatin enclosed therein and use thereof
AssigneeToudai TLO, Ltd.
InventorsKazunori Kataoka, Nobuhiro Nishiyama, Masayuki Yokoyama, Teruo Okano
Life of this patent
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Abstract
Provided is a complex comprising cisplatin encapsulated therein in a form in which a chlorine ion thereof is ligand-exchanged with a carboxyl anion of a block copolymer comprising poly(ethylene glycol)-poly(glutamic acid). This complex can be a medicinal preparation to which a novel dosage form decreased in toxicity can be applied.
Claims21
A complex which comprises a block copolymer represented by Formula I or II:
- wherein in Formula I and II, R1 represents independently a hydrogen atom, a C1-20 alkyl group or a C1-20 alkyl group substituted with one or two substituents selected from the group consisting of acetal, hydroxyl, aldehyde, amino and mercapto;
- A represents independently NH, CO or R5(CH2)pR6, in which R5 is O, OCO, OCONH, NHCO, NHCOO, NHCONH, CONH or COO;
- R6 is NH or CO;
- and p is an integer of 1 to 6;
- R2 represents independently a hydrogen atom or an alkyl group or an aralkyl group, provided that a hydrogen atom accounts for 95% or more of all R2;
- R3 represents independently a hydrogen atom or in the case of Formula I, R3 is C8-16 alkylcarbonyl, phenylacetyl, diphenylacetyl or pyrenesulfonyl, and in the case of Formula II, R3 is C8-16 alkyl, benzyl, benzhydryl, adamantyl or cholesteryl;
- m is independently an integer of 50 to 5000;
- and n is independently an integer of 5 to 500;
- and cisplatin, wherein one or two chlorine ions in the cisplatin are replaced with the carboxyl anion of the block copolymer.
6 more elements
A medicinal preparation comprising a medicinally effective amount of a complex which comprises a block copolymer represented by Formula I or II:
- wherein in Formula I and II, R1 represents independently a hydrogen atoms, a C1-20 alkyl group or a C1-20 alkyl group substituted with one or two substituents selected from the group consisting of acetal, hydroxyl, aldehyde, amino and mercapto;
- A represents independently NH, CO or R5(CH2)pR6, in which R5 is O, OCO, OCONH, NHCO, NHCOO, NHCONH, CONH or COO;
- R6 is NH or CO;
- and p is an integer of 1 to 6;
- R2 represents independently a hydrogen atom or an alkyl group or an axailcyl group, provided that a hydrogen atom accounts for 95% or more of all R2;
- R3 represents independently a hydrogen atom or in the case of Formula I, R3 is C8-16 alkylcarbonyl, phenylacetyl, diphenylacetyl or pyrenesulfonyl, and in the case of Formula II R3 is C8-16 alkyl, benzyl, benzhvdryl, adamantyl or cholesteryl;
- in is independently an integer of 50 to 5000;
- and n is independently an integer of 5 to 500;
- and cisplatin, wherein one or two chlorine ions in the cisplatin are replaced with the carboxyl anion of the block copolymer;
- together with a filler or a diluent.
7 more elements
Dependencies are inferred from the claim text.