Physical trapping type polymeric micelle drug preparation
First Claim
1. A polymeric micelle type pharmaceutical composition, comprising a hydrophobic drug and a drug carrier, said hydrophobic drug physically trapped within and not covalently bonded to said drug carrier, and said drug carrier composed of a block copolymer represented by the formula I or II:
- ##STR7## wherein;
R1 is selected from the group consisting of H and methyl;
R2 is selected from the group consisting of NH, CO andR6 (CH2)q R7 whereR6 is selected from the group consisting of --OC(O)--, --OC(O)N(H)--, --N(H)C(O)--, --N(H)C(O)O--, --N(H)C(O)N(H)--, --C(O)N(H)-- and --C(O)O--;
R7 is NH or CO; and
q is 1-6;
R3 is selected from the group consisting of H, --CH3, --CH2 CO2 H, --CH2 CH2 CO2 H, --CH2 CO2 CH2 φ
, --CH2 CH2 CO2 CH2 φ
, --CH2 CH(CH3)CH3, --CH(CH3)CH2 CH3, --CH(CH3)2, --(CH2)P C6 H5, --(CH2)P COOR5 and --CH2 C(O)N(H)R5 ;
wherep is 1 or 2;
R5 is selected from the group consisting of benzyl and C1 -C20 alkyl group, said C1 -C20 alkyl group being optionally substituted with a benzyl group; and
R4 is selected from the group consisting of H, --OH, --C(O)-alkyl, --N(H)-alkyl and --O-alkyl, wherein said alkyl is a C1 -C20 alkyl group;
m=4-2500; and
n=2-300.
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Abstract
The present invention relates to drug carriers composed of a block copolymer having hydrophilic and hydrophobic segments, a polymeric micelle type drug comprising hydrophobic drugs trapped by physical treatments in said drug carrier and methods for trapping hydrophobic drugs in the drug carrier. The drugs carrier composed of the block copolymer according to the invention forms a stable polymeric micelle structure with which hydrophobic drugs can be incorporated very efficiently via physical trapping. It was found that the incorporated drug is stably maintained in micelles even in the presence of serum. In addition, a drug difficult to administer into the living body owing to sparing water-solubility for its high hydrophobicity can be administered in the form of polymeric micelle drug.
195 Citations
5 Claims
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1. A polymeric micelle type pharmaceutical composition, comprising a hydrophobic drug and a drug carrier, said hydrophobic drug physically trapped within and not covalently bonded to said drug carrier, and said drug carrier composed of a block copolymer represented by the formula I or II:
- ##STR7## wherein;
R1 is selected from the group consisting of H and methyl;R2 is selected from the group consisting of NH, CO and R6 (CH2)q R7 where R6 is selected from the group consisting of --OC(O)--, --OC(O)N(H)--, --N(H)C(O)--, --N(H)C(O)O--, --N(H)C(O)N(H)--, --C(O)N(H)-- and --C(O)O--; R7 is NH or CO; and q is 1-6; R3 is selected from the group consisting of H, --CH3, --CH2 CO2 H, --CH2 CH2 CO2 H, --CH2 CO2 CH2 φ
, --CH2 CH2 CO2 CH2 φ
, --CH2 CH(CH3)CH3, --CH(CH3)CH2 CH3, --CH(CH3)2, --(CH2)P C6 H5, --(CH2)P COOR5 and --CH2 C(O)N(H)R5 ;
wherep is 1 or 2; R5 is selected from the group consisting of benzyl and C1 -C20 alkyl group, said C1 -C20 alkyl group being optionally substituted with a benzyl group; and R4 is selected from the group consisting of H, --OH, --C(O)-alkyl, --N(H)-alkyl and --O-alkyl, wherein said alkyl is a C1 -C20 alkyl group; m=4-2500; and n=2-300. - View Dependent Claims (2, 3, 4, 5)
- ##STR7## wherein;
Specification
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- Resources
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Current AssigneeResearch Development Corporation Of Japan (Japan Science And Technology Agency)
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Original AssigneeResearch Development Corporation Of Japan (Japan Science And Technology Agency)
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InventorsKataoka, Kazunori, Okano, Teruo, Yokoyama, Masayuki, Sakurai, Yasuhisa
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Primary Examiner(s)Nutter, Nathan M.
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Application NumberUS08/105,535Time in Patent Office762 DaysField of Search424/78.08, 424/78.17, 424/450, 424/451, 424/489, 424/501US Class Current424/78.08CPC Class CodesA61K 9/1075 Microemulsions or submicron...C08G 69/10 Alpha-amino-carboxylic acid...Y10T 428/2985 Solid-walled microcapsule f...Y10T 428/2989 Microcapsule with solid cor...
