EP0583955A2
Expired / Lapsed
EP
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Physical trapping type polymeric micelle drug preparation
Assignee: Japan Science and Technology Agency
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Filing: 1993-08-13
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Granted: —
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Expires: 2013-08-13
Abstract
Abstract A polymeric micelle type drug comprises at least one hydrophobic drug physically trapped in a drug carrier comprising a block copolymer represented by formula I or II: <CHEM> <CHEM> wherein R1 is hydrogen or an alkyl group having 1 to 20 carbo atoms, R2 is NH, CO, R6(CH2)qR7 (in which R6 represents OCO, OCONH, NHCO, NHCOO, NHCONH, CONH or COO, R7 represents NH or CO, and q is 1 to 6), R3 is hydrogen, an alkyl group having 1 to 20 carbon atoms, (CH2)pC6H5, (CH2)pCOOR5 or CH2CONHR5 (in which p is 1 or 2, R5 represents a C1-20 alkyl group, a benzyl-substituted C1-20 alkyl group or a benzyl group), R4 is hydrogen, hydroxyl, RCO-, RNH- or RO- where R is an alkyl group having 1 to 20 carbon atoms, m is 4-2500, and n is 2-300.
Inventors
- 👤 Masayuki Yokoyama
- 👤 Yasuhisa Sakurai
- 👤 Teruo Okano
- 👤 Kazunori Kataoka
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-03 13:04
CPC Classifications
C; C08; C08G; C08G69/00; C08G69/02; C08G69/08; C08G69/10; D; D06; D06F; D06F58/00; D06F58/10; A; A61; A61K; A61K9/00; A61K9/10; A61K9/107; A61K9/1075; A61L; A61L2/00; A61L2/02; A61L2/08; A61L2/10; D06F34/00; D06F34/14; D06F34/26; D06F2103/00; D06F2103/28; D06F2103/32; D06F2105/00; D06F2105/30; Y; Y10; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2984; Y10T428/2985; Y10T428/2989
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
168 words
A polymeric micelle type drug composition which comprises at least one hydrophobic drug physically trapped in a drug carrier comprising a block copolymer represented by formula I or II: wherein R 1 is hydrogen or an alkyl group having 1 to 20 carbon atoms, R 2 is NH, CO, R 6 (CH 2 )qR 7 (in which R 6 represents OCO, OCONH, NHCO, NHCOO, NHCONH, CONH or COO, R 7 represents NH or CO, and q is 1 to 6), R 3 is hydrogen, an alkyl group having 1 to 20 carbon atoms, (CH 2 ) P C 6 H 5 , (CH 2 )pCOOR 5 or CH 2 CONHR 5 (in which p is 1 or 2, R 5 represents a C 1-20 alkyl group, a benzyl-substituted C 1-20 alkyl group or a benzyl group), R 4 is hydrogen, hydroxyl, RCO-, RNH- or RO- where R is an alkyl group having 1 to 20 carbon atoms, m is 4 to 2500, and n is 2 to 300.
Claim 2
Dependent Claim
168 words
A polymeric micelle type drug composition which comprises at least one hydrophobic drug physically trapped in a drug carrier comprising a block copolymer represented by formula I or II: wherein R 1 is hydrogen or an alkyl group having 1 to 20 carbon atoms, R 2 is NH, CO, R 6 (CH 2 )qR 7 (in which R 6 represents OCO, OCONH, NHCO, NHCOO, NHCONH, CONH or COO, R 7 represents NH or CO, and q is 1 to 6), R 3 is hydrogen, an alkyl group having 1 to 20 carbon atoms, (CH 2 ) P C 6 H 5 , (CH 2 )pCOOR 5 or CH 2 CONHR 5 (in which p is 1 or 2, R 5 represents a C 1-20 alkyl group, a benzyl-substituted C 1-20 alkyl group or a benzyl group), R 4 is hydrogen, hydroxyl, RCO-, RNH- or RO- where R is an alkyl group having 1 to 20 carbon atoms, m is 4 to 2500, and n is 2 to 300.
Claim 3
Dependent Claim
30 words
A composition according to claim 1, in which the block copolymer is a compound represented by formula III: wherein m is 4 to 2500 and n is 2 to 300.
Claim 4
Dependent Claim
25 words
A composition according to claim 1 or 2, in which the hydrophobic drug is at least one of adriamycin, daunomycin, methotrexate, mitomycin C or indomethacin.
Claim 5
Dependent Claim
15 words
A composition according to claim 3 in which the hydrophobic drug is indomethacin or adinamycin.
Claim 6
Independent Claim
40 words
A method for trapping hydrophobic drugs, which comprises the heating, ultrasonication or organic solvent treatment of hydrophobic drugs and drug carrier of formula I, II or III to physically trap said hydrophobic drugs in polymeric micelles comprising said drug carrier.
Claim 7
Independent Claim
40 words
A method for trapping hydrophobic drugs, which comprises the heating, ultrasonication or organic solvent treatment of hydrophobic drugs and drug carrier of formula I, II or III to physically trap said hydrophobic drugs in polymeric micelles comprising said drug carrier.
References Cited (Backward Citations)
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