HRP20150350T1 - Tekuä†i pripravak koji sadrži biokompatibilne pripravke oligomer-polimer - Google Patents
Tekuä†i pripravak koji sadrži biokompatibilne pripravke oligomer-polimer Download PDFInfo
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- HRP20150350T1 HRP20150350T1 HRP20150350TT HRP20150350T HRP20150350T1 HR P20150350 T1 HRP20150350 T1 HR P20150350T1 HR P20150350T T HRP20150350T T HR P20150350TT HR P20150350 T HRP20150350 T HR P20150350T HR P20150350 T1 HRP20150350 T1 HR P20150350T1
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- ch2ch2o
- och2ch2
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- 229920000642 polymer Polymers 0.000 title claims 7
- 239000000203 mixture Substances 0.000 title claims 6
- 230000009969 flowable effect Effects 0.000 title 1
- 239000007788 liquid Substances 0.000 claims 21
- 238000002360 preparation method Methods 0.000 claims 14
- -1 oxy, imino Chemical group 0.000 claims 13
- 229920000728 polyester Polymers 0.000 claims 13
- 125000002947 alkylene group Chemical group 0.000 claims 10
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 8
- 239000013543 active substance Substances 0.000 claims 8
- 239000002207 metabolite Substances 0.000 claims 8
- 239000000651 prodrug Substances 0.000 claims 8
- 229940002612 prodrug Drugs 0.000 claims 8
- 229920001169 thermoplastic Polymers 0.000 claims 8
- 239000004416 thermosoftening plastic Substances 0.000 claims 8
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 4
- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- JBKVHLHDHHXQEQ-UHFFFAOYSA-N epsilon-caprolactam Chemical compound O=C1CCCCCN1 JBKVHLHDHHXQEQ-UHFFFAOYSA-N 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 230000003115 biocidal effect Effects 0.000 claims 3
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 239000002327 cardiovascular agent Substances 0.000 claims 3
- 229940125692 cardiovascular agent Drugs 0.000 claims 3
- 239000000824 cytostatic agent Substances 0.000 claims 3
- 239000002934 diuretic Substances 0.000 claims 3
- 230000001882 diuretic effect Effects 0.000 claims 3
- 239000004083 gastrointestinal agent Substances 0.000 claims 3
- 229940125695 gastrointestinal agent Drugs 0.000 claims 3
- 229940088597 hormone Drugs 0.000 claims 3
- 239000005556 hormone Substances 0.000 claims 3
- 239000002955 immunomodulating agent Substances 0.000 claims 3
- 239000003018 immunosuppressive agent Substances 0.000 claims 3
- 229940125721 immunosuppressive agent Drugs 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- DEQANNDTNATYII-OULOTJBUSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 DEQANNDTNATYII-OULOTJBUSA-N 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- HNPFPERDNWXAGS-LZCJLJQNSA-N (e)-7-[3,5-dihydroxy-2-(3-hydroxy-5-phenylpentyl)cyclopentyl]hept-5-enoic acid Chemical compound C=1C=CC=CC=1CCC(O)CCC1C(O)CC(O)C1C\C=C\CCCC(O)=O HNPFPERDNWXAGS-LZCJLJQNSA-N 0.000 claims 2
- XYLJNLCSTIOKRM-UHFFFAOYSA-N Alphagan Chemical compound C1=CC2=NC=CN=C2C(Br)=C1NC1=NCCN1 XYLJNLCSTIOKRM-UHFFFAOYSA-N 0.000 claims 2
- 229940097420 Diuretic Drugs 0.000 claims 2
- 108010000817 Leuprolide Proteins 0.000 claims 2
- 108010016076 Octreotide Proteins 0.000 claims 2
- 150000001345 alkine derivatives Chemical class 0.000 claims 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- NWIUTZDMDHAVTP-UHFFFAOYSA-N betaxolol Chemical compound C1=CC(OCC(O)CNC(C)C)=CC=C1CCOCC1CC1 NWIUTZDMDHAVTP-UHFFFAOYSA-N 0.000 claims 2
- 229960004324 betaxolol Drugs 0.000 claims 2
- 210000001124 body fluid Anatomy 0.000 claims 2
- 239000010839 body fluid Substances 0.000 claims 2
- 229960003679 brimonidine Drugs 0.000 claims 2
- HCRKCZRJWPKOAR-JTQLQIEISA-N brinzolamide Chemical compound CCN[C@H]1CN(CCCOC)S(=O)(=O)C2=C1C=C(S(N)(=O)=O)S2 HCRKCZRJWPKOAR-JTQLQIEISA-N 0.000 claims 2
- 229960000722 brinzolamide Drugs 0.000 claims 2
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical class OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 238000013270 controlled release Methods 0.000 claims 2
- 229920001577 copolymer Polymers 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- IAVUPMFITXYVAF-XPUUQOCRSA-N dorzolamide Chemical compound CCN[C@H]1C[C@H](C)S(=O)(=O)C2=C1C=C(S(N)(=O)=O)S2 IAVUPMFITXYVAF-XPUUQOCRSA-N 0.000 claims 2
- 229960003933 dorzolamide Drugs 0.000 claims 2
- WWSWYXNVCBLWNZ-QIZQQNKQSA-N fluprostenol Chemical compound C([C@H](O)\C=C\[C@@H]1[C@H]([C@@H](O)C[C@H]1O)C\C=C/CCCC(O)=O)OC1=CC=CC(C(F)(F)F)=C1 WWSWYXNVCBLWNZ-QIZQQNKQSA-N 0.000 claims 2
- 235000013773 glyceryl triacetate Nutrition 0.000 claims 2
- 239000001087 glyceryl triacetate Substances 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 239000007943 implant Substances 0.000 claims 2
- GGXICVAJURFBLW-CEYXHVGTSA-N latanoprost Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCC1=CC=CC=C1 GGXICVAJURFBLW-CEYXHVGTSA-N 0.000 claims 2
- 229960001160 latanoprost Drugs 0.000 claims 2
- GFIJNRVAKGFPGQ-LIJARHBVSA-N leuprolide Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 GFIJNRVAKGFPGQ-LIJARHBVSA-N 0.000 claims 2
- 229960004338 leuprorelin Drugs 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229960002700 octreotide Drugs 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- RUOJZAUFBMNUDX-UHFFFAOYSA-N propylene carbonate Chemical compound CC1COC(=O)O1 RUOJZAUFBMNUDX-UHFFFAOYSA-N 0.000 claims 2
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 2
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 2
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 claims 2
- 229960001534 risperidone Drugs 0.000 claims 2
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 2
- 229960002930 sirolimus Drugs 0.000 claims 2
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 2
- DOMXUEMWDBAQBQ-WEVVVXLNSA-N terbinafine Chemical compound C1=CC=C2C(CN(C\C=C\C#CC(C)(C)C)C)=CC=CC2=C1 DOMXUEMWDBAQBQ-WEVVVXLNSA-N 0.000 claims 2
- 229960002722 terbinafine Drugs 0.000 claims 2
- 229920001897 terpolymer Polymers 0.000 claims 2
- MKPLKVHSHYCHOC-AHTXBMBWSA-N travoprost Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)COC1=CC=CC(C(F)(F)F)=C1 MKPLKVHSHYCHOC-AHTXBMBWSA-N 0.000 claims 2
- 229960002368 travoprost Drugs 0.000 claims 2
- 229960002622 triacetin Drugs 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Polymers OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims 1
- 229920000954 Polyglycolide Polymers 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 239000012736 aqueous medium Substances 0.000 claims 1
- 230000001085 cytostatic effect Effects 0.000 claims 1
- 239000000539 dimer Substances 0.000 claims 1
- 125000004185 ester group Chemical group 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 229920001519 homopolymer Polymers 0.000 claims 1
- 229920000747 poly(lactic acid) Polymers 0.000 claims 1
- 229920001610 polycaprolactone Polymers 0.000 claims 1
- 239000004632 polycaprolactone Substances 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A61P5/00—Drugs for disorders of the endocrine system
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L67/00—Compositions of polyesters obtained by reactions forming a carboxylic ester link in the main chain; Compositions of derivatives of such polymers
- C08L67/04—Polyesters derived from hydroxycarboxylic acids, e.g. lactones
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Claims (12)
1. Tekući pripravak koji sadrži:
biorazgradivi termoplastični poliesterski polimer koji je barem uglavnom netopiv u tjelesnoj tekućini;
biokompatibilnu zaklopljenu oligomernu tekućinu; te
biološki aktivno sredstvo, metabolit, ili njegov predlijek,
pri čemu biokompatibilna zaklopljena oligomerna tekućina ima formulu I, II, III, IV, ili V:
[image]
[image]
pri čemu:
svaki R1 je neovisno (C1-C12)alkil, ili (C1-C12)alkilenkarboksilni(C1-C12)alkilester;
svaki R2 je neovisno (C1-C12)alkil, karbonil(C1-C12)alkil, ili karboksilni(C1-C12)alkilester;
svaki R3 je neovisno (C1-C12)alkilen;
R4 je (C1-C12)alkilen, karbonil(C1-C12)alkilkarbonil, ili (C3-C12)cikloalkadiil;
R5 je (C1-C12)alkatriil ili (C3-C12)cikloalkatriil;
R6 je (C1-C12)alkilen, (C1-C12)alkin, (C3-C12)cikloalkadiil, (C1-C12)alkatriil, ili (C3-C12)cikloalkatriil;
R7 je (C1-C12)alkilen ili (C1-C12)alkatriil,
X je odsutan ili kisik;
W je odsutan, karbonil, ili karboniloksi; i
bilo koji alkil ili alkilen iz R1, R2, R3, R4, R5, R6 i R7 može biti proizvoljno supstituiran na ugljiku s jednim ili više okso, halogen, nitro, cijano, (C1-C12)alkil, (C1-C6)alkoksi, trifluorometil, te proizvoljno prekinut na ugljiku s jednim ili više oksi, imino, ili tio, te je proizvoljno djelomično nezasićen; i
svaki a, b, c, i d je neovisno 0, 1, 2, 3, 4, ili 5.
2. Tekući pripravak prema zahtjevu 1, naznačen time da
svaki R1 je neovisno -(CH2)mCH3, -CH2CH2(OCH2CH2)mO(CH2)nCH3, -CH2CH2(OCH2CH2)mOCOCH3, -CH2COOY, -CH(CH3)COOY, -CH2CH2COOY,-CH2CH2CH2COOY, -CH2CH2CH2CH2COOY, -CH2CH2CH2CH2CH2COOY, -CH2CH(CH3)Y, ili -(cikloC6H11)-, pri čemu svaki m i n je neovisno 0, 1, 2, 3, 4, 5, 6, ili 7; poželjno, pri čemu svaki R1 je neovisno -CH3, -CH2CH3, -(CH2)2CH3, -(CH2)3CH3, -(CH2)4CH3, -(CH2)5CH3, -(CH2)6CH3, -(CH2)7CH3, -CH2CH2(OCH2CH2)2OCH3, -CH2CH2(OCH2CH2)2OCH2CH3, ili -CH2CH2(OCH2CH2)2OCOCH3;
svaki R2 je neovisno -CH3, -CH2CH3, -(CH2)oCH3, -CH2CH2(OCH2CH2)oOCH3, -CH2CH2(OCH2CH2)oOCH2CH3, -CH2CH2(OCH2CH2)oOCOCH3, -COCH3, -CO(CH2)oCH3, -COO(CH2)oCH3, ili - CO(OCH2CH2)oCH3, pri čemu o je 0, 1, 2, 3, 4, 5, 6, ili 7; poželjno pri čemu svaki R2 je neovisno -CH3, -CH2CH3, -(CH2)2CH3, -(CH2)3CH3, -(CH2)4CH3, -(CH2)5CH3, -(CH2)6CH3, -(CH2)7CH3,-CH2CH2(OCH2CH2)2OCH3, -CH2CH2(OCH2CH2)2OCH2CH3, ili -CH2CH2(OCH2CH2)2OCOCH3;
svaki R3 je neovisno -(CH2)p , -CH(CH3)-, -(CH2CH2O)pCH2-, -(CH(CH3)CH2)-, ili -(CH(CH2CH3)CH2)-, pri čemu p je 0, 1, 2, 3, 4, 5, 6, ili 7; poželjno pri čemu svaki R3 je neovisno -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -CH(CH3)-, -(CH(CH3)CH2)-, -(CH(CH2CH3)CH2)-, ili -(CH2CH2OCH2)-;
R4 je -(CH2)q-, -CO(CH2)qCO-, -(CH2CH2O)qCH2CH2-, -CH2CH2CH2CH2CH2CH2-, -(CH2)qCH(CH3)-, -((CH2)qO)q, -CH2CH(Y)CH2-, cikloheksan-1,2-diil, cikloheksan-1,3-diil ili cikloheksan-1,4-diil, pri čemu q je 1, 2, 3, 4, 5, 6, ili 7; poželjno R4 je -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -COCH2CO-, -CO(CH2)2CO-, -CO(CH2)3CO-, -CO(CH2)4CO-, -CO(CH2)5CO-, -CO(CH2)6CO-, CO(CH2)7CO-, -CO(CH2)8CO-, -(CH2CH2O)2CH2CH2-, -(CH2CH2O)3CH2CH2-, -(CH2CH2O)4CH2CH2-, -(CH2CH2O)5CH2CH2-, -(CH2CH2O)6CH2CH2-, ili -CH2CH2CH2CH2CH2CH2-;
R5 je (-CH2)2CH-, (-CH2)3CCH3, (-CH2)3CCH2CH3, ili 1,2,6-heksantriil; poželjno R5 je (-CH2)2CH-;
R6 je -CH=CH-, -(CH2)r-, -O(CH2CH2O)r- pri čemu r je 1, 2, 3, 4, 5, 6, ili 7; poželjno R6 je -CH=CH-, -(CH2)-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -O(CH2CH2O)-, -O(CH2CH2O)2-, -O(CH2CH2O)3-, -O(CH2CH2O)4-, -O(CH2CH2O)5-, ili -O(CH2CH2O)6-;
R7 je (-CH2)2CH-, (-CH2)2COH-, (-CH2)(-CHOH)CH-, (-CH2)(-CO)CH-, ili (-CH2)(-CH=)C-; poželjno R7 je (-CH2)2CH-, (-CH2)2COH-, (-CH2)(-CHOH)CH-, (-CH2)(-CO)CH-, ili (-CH2)(-CH=)C-;
X je odsutan ili kisik;
W je odsutan, karbonil, ili karboniloksi;
Y je -CH3, -C2H5, -C3H7, ili -C4H9; i
poželjno svaki a, b, c, i d je neovisno 0, 1, 2, 3, ili 4.
3. Tekući pripravak prema zahtjevu 1, naznačen time da je biokompatibilna zaklopljena oligomerna tekućina prisutna u količini 10 tež. % do 90 tež. % pripravka.
4. Tekući pripravak prema zahtjevu 1, naznačen time da biorazgradivi termoplastični poliesterski polimer je poliester sa jednom ili više C2 do C10 hidroksikarboksilnih kiselina, poliester sa kombinacijom jednog ili više C2 do C12 diola i jedne ili više C3 do C12 dikarboksilnih kiselina, poliester sa kombinacijom jednog ili više C3 do C12 triola i jedne ili više C3 to C12 dikarboksilnih kiselina, ili njihova kombinacija.
5. Tekući pripravak prema zahtjevu 4,
naznačen time da su hidroksikarboksilna kiselina ili kiseline proizvoljno u obliku dimera; ili
pri čemu poliester je polilaktid, poliglikolid, polikaprolakton, njihov kopolimer, njihov terpolimer, ili njihova kombinacija; ili
pri čemu biorazgradivi termoplastični poliester je 50/50, 55/45, 65/35, 75/25, 85/15, 90/10, ili 95/5 poli(DL-laktid-ko-glikolid) koji ima karboksi završnu skupinu, ili je 50/50, 55/45, 65/35, 75/25, 85/15, 90/10, ili 95/5 poli(DL-laktid-ko-glikolid) bez karboksi završne skupine, te proizvoljno poliester bez završne karboksilne skupine je produžen sa C2 do C12 diolom; ili
pri čemu biorazgradivi termoplastični poliesterski polimer je prisutan u količini 0 tež % do 95 tež %, te proizvoljno biorazgradivi termoplastični poliester ima prosječnu molekulsku težinu od 10,000 do 45,000 Daltona.
6. Tekući pripravak prema zahtjevu 1, naznačen time da biološki aktivno sredstvo, metabolit, ili njegov predlijek, sadrži hormon, imunomodulacijsko sredstvo, imunosupresijsko sredstvo, antibiotik, citostatik, diuretik, gastrointestinalno sredstvo, kardiovaskularno sredstvo, ili neurofarmaceutsko sredstvo, ili njihovu kombinaciju; ili pri čemu biološki aktivno sredstvo, metabolit, ili njegov predlijek, sadrži leuprolid, oktreotid, brimonidin, latanoprost, kiselinu latanoprosta, travoprost, kiselinu travoprosta, brinzolamid, dorzolamid, betaksolol, terbinafin, risperidon, rapamicin, ili njihovu kombinaciju, pri čemu je, proizvoljno, biološki aktivno sredstvo, metabolit, ili njegov predlijek, prisutno sa 0.1 tež. % do 50 tež. % pripravka.
7. Tekući pripravak prema zahtjevu 1, naznačen time da dodatno sadrži biokompatibilnu polarnu aprotičnu organsku tekućinu koja sadrži N-metil-2-pirolidon, 2-pirolidon, N,N-dimetilformamid, dimetil sulfoksid, propilen karbonat, kaprolaktam, triacetin, ili bilo koju njihovu kombinaciju.
8. Tekući pripravak prema zahtjevu 1 naznačen time da je injektibilna supkutana formulacija, te proizvoljno ima volumen od 0.20 mL do 2.0 mL, te je poželjno formuliran za davanje oko jednom mjesečno.
9. Tekući pripravak prema zahtjevu 1, naznačen time da biorazgradivi termoplastični poliesterski polimer je homopolimer, kopolimer ili terpolimer ponavljajućih monomernih jedinica povezanih sa skupinama estera.
10. Postupak za formiranje tekućeg pripravka prema zahtjevu 1 naznačen time da je za uporabu kao implantat s kontroliranim oslobađanjem, koji sadrži korak miješanja, u bilo kojem redoslijedu:
biorazgradivog termoplastičnog poliesterskog polimera koji je barem uglavnom netopiv u vodenom mediju ili u tjelesnoj tekućini;
biokompatibilne zaklopljene oligomerne tekućine; te
biološki aktivnog sredstva, metabolita, ili njegovog predlijeka,
pri čemu se miješanje provodi tijekom dovoljnog vremenskog razdoblja da se dobije tekući pripravak za uporabu kao implantat s kontroliranim oslobađanjem, pri čemu biokompatibilna zaklopljena oligomerna tekućina ima formulu I, II, III, IV, ili V:
[image]
[image]
[image]
pri čemu:
svaki R1 je neovisno (C1-C12)alkil, ili (C1-C12)alkilenkarboksilni(C1-C12)alkilester;
svaki R2 je neovisno (C1-C12)alkil, karbonil(C1-C12)alkil, ili karboksilni(C1-C12)alkilester;
svaki R3 je neovisno (C1-C12)alkilen;
R4 je (C1-C12)alkilen, karbonil(C1-C12)alkilkarbonil, ili (C3-C12)cikloalkadiil;
R5 je (C1-C12)alkatriil ili (C3-C12)cikloalkatriil;
R6 je (C1-C12)alkilen, (C1-C12)alkin, (C3-C12)cikloalkadiil, (C1-C12)alkatriil, ili (C3-C12)cikloalkatriil;
R7 je (C1-C12)alkilen ili (C1-C12)alkatriil,
X je odsutan ili kisik;
W je odsutan, karbonil, ili karboniloksi; i
bilo koji alkil ili alkilen iz R1, R2, R3, R4, R5, R6 i R7 može biti proizvoljno supstituiran na ugljiku s jednim ili više okso, halogen, nitro, cijano, (C1-C12)alkil, (C1-C6)alkoksi, trifluorometil, te proizvoljno prekinut na ugljiku s jednim ili više oksi, imino, ili tio, te je proizvoljno djelomično nezasićen; te
svaki a, b, c, d, e, f, g, h, te i je neovisno 0, 1, 2, 3, 4, ili 5.
11. Postupak prema zahtjevu 10, naznačen time da se zajedno miješaju biokompatibilan termoplastični poliesterski polimer i biokompatibilna zaklopljena oligomerna tekućina tako da tvore smjesu i smjesa se miješa s biološki aktivnim sredstvom, metabolitom, ili njihovim predlijekom, tako da se dobije tekući pripravak; ili
pri čemu biološki aktivno sredstvo, metabolit, ili njihov predlijek, sadrži hormon, imunomodulacijsko sredstvo, imunosupresijsko sredstvo, antibiotik, citostatik, diuretik, gastrointestinalno sredstvo, kardiovaskularno sredstvo, ili neurofarmaceutsko sredstvo, ili njihovu kombinacija; ili
pri čemu biološki aktivno sredstvo, metabolit, ili njegov predlijek, sadrži leuprolid, oktreotid, brimonidin, latanoprost, kiselinu latanoprosta, travoprost, kiselinu travoprosta, brinzolamid, dorzolamid, betaksolol, terbinafin, risperidon, rapamicin, ili njihovu kombinaciju; ili dodatno sadrži dodavanje biokompatibilne polarne aprotične tekućine koja sadrži N-metil-2-pirolidon, 2-pirolidon, N,N-dimetilformamid, dimetil sulfoksid, propilen karbonat, kaprolaktam, triacetin, ili njihovu kombinaciju.
12. Tekući pripravak prema bilo kojem zahtjevu od 1-9, naznačen time da je za uporabu u farmaceutskoj formulaciji, poželjno pri čemu farmaceutska formulacija sadrži hormon, imunomodulacijsko sredstvo, imunosupresijsko sredstvo, antibiotik, citostatik, diuretik, gastrointestinalno sredstvo, kardiovaskularno sredstvo, ili neurofarmaceutsko sredstvo, ili bilo koju njihovu kombinaciju.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5845808P | 2008-06-03 | 2008-06-03 | |
| PCT/US2009/003363 WO2009148581A1 (en) | 2008-06-03 | 2009-06-03 | Biocompatible oligomer-polymer compositions |
| EP09758745.5A EP2291174B1 (en) | 2008-06-03 | 2009-06-03 | Flowable composition comprising biocompatible oligomer-polymer compositions |
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| US (1) | US9308162B2 (hr) |
| EP (1) | EP2291174B1 (hr) |
| CY (1) | CY1116196T1 (hr) |
| DK (1) | DK2291174T3 (hr) |
| ES (1) | ES2535330T3 (hr) |
| HR (1) | HRP20150350T1 (hr) |
| PL (1) | PL2291174T3 (hr) |
| PT (1) | PT2291174E (hr) |
| SI (1) | SI2291174T1 (hr) |
| WO (1) | WO2009148581A1 (hr) |
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| US8852638B2 (en) | 2005-09-30 | 2014-10-07 | Durect Corporation | Sustained release small molecule drug formulation |
| AU2007207618B2 (en) | 2006-01-18 | 2011-03-24 | Foresee Pharmaceuticals Co., Ltd. | Pharmaceutical compositions with enhanced stability |
| BRPI0811319A2 (pt) | 2007-05-25 | 2015-02-10 | Tolmar Therapeutics Inc | Composição fluida, método de formação de uma composição fluida, implante biodegrádavel formado in situ, método de formação de um implante biodegradável in situ, kit, implante e método de trataento |
| SI2291174T1 (sl) | 2008-06-03 | 2015-05-29 | Tolmar Therapeutics, Inc. | Tekoči sestavek, ki vsebuje biokompatibilne sestavke oligomer-polimer |
| US8822546B2 (en) * | 2008-12-01 | 2014-09-02 | Medtronic, Inc. | Flowable pharmaceutical depot |
| US9272044B2 (en) | 2010-06-08 | 2016-03-01 | Indivior Uk Limited | Injectable flowable composition buprenorphine |
| GB2481017B (en) | 2010-06-08 | 2015-01-07 | Rb Pharmaceuticals Ltd | Microparticle buprenorphine suspension |
| US20160120877A1 (en) * | 2010-07-16 | 2016-05-05 | James S Rowe | Pharmaceutical compositions for sustained delivery of benzodiazepine antagonists |
| EA201300514A1 (ru) * | 2010-12-15 | 2013-11-29 | 3М Инновейтив Пропертиз Компани | Разлагаемые волокна |
| FR2973386B1 (fr) * | 2011-03-28 | 2013-04-26 | Valagro Carbone Renouvelable Poitou Charentes | Utilisation d'un oligomere de lactide biodegradable comme plastifiants |
| US10675376B2 (en) | 2012-05-24 | 2020-06-09 | Ethicon Llc | Mechanically strong absorbable polymeric blend compositions of precisely controllable absorption rates, processing methods, and products therefrom |
| US9757330B2 (en) | 2013-10-18 | 2017-09-12 | Industrial Technology Research Institute | Recipe for in-situ gel, and implant, drug delivery system formed thereby |
| AU2014355033B2 (en) | 2013-11-27 | 2018-05-24 | Ethicon Llc | Absorbable polymeric blend compositions with precisely controllable absorption rates, processing methods, and dimensionally stable medical devices therefrom |
| WO2015119976A1 (en) * | 2014-02-04 | 2015-08-13 | Abbott Cardiovascular Systems Inc. | Modified pla polymer and method of making and using |
| GB201404139D0 (en) | 2014-03-10 | 2014-04-23 | Rb Pharmaceuticals Ltd | Sustained release buprenorphine solution formulations |
| EP3554494A4 (en) | 2016-12-19 | 2021-02-17 | Cellixbio Private Limited | COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATION |
| WO2020018888A1 (en) | 2018-07-20 | 2020-01-23 | The Board Of Regents Of The University Of Oklahoma | Antimicrobial peptides and methods of use |
| CN111249298B (zh) * | 2020-04-08 | 2021-03-12 | 曲阜师范大学 | 一种含有马杜霉素和顺铂的抗癌药物组合物 |
| CN112812520B (zh) * | 2021-01-07 | 2022-08-23 | 江南大学 | 一种提高聚合物加工流动性能的方法 |
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| US2371281A (en) * | 1945-03-13 | Lactyuactic esters and process of | ||
| DE1020324B (de) | 1954-12-17 | 1957-12-05 | Boehringer Sohn Ingelheim | Verfahren zur Herstellung von esterartigen Milchsaeurederivaten mit definierter Kettenlaenge und endstaendiger Ester-, Amid- oder Nitrilgruppe |
| US7033608B1 (en) * | 1995-05-22 | 2006-04-25 | The United States Of America As Represented By The Secretary Of The Army | “Burst-free” sustained release poly-(lactide/glycolide) microspheres |
| US6126919A (en) * | 1997-02-07 | 2000-10-03 | 3M Innovative Properties Company | Biocompatible compounds for pharmaceutical drug delivery systems |
| US6565874B1 (en) * | 1998-10-28 | 2003-05-20 | Atrix Laboratories | Polymeric delivery formulations of leuprolide with improved efficacy |
| DE19908753C2 (de) * | 1999-02-20 | 2003-10-02 | Jenapharm Gmbh | Bioabbaubare, injizierbare Oligomer-Polymer-Zusammensetzung |
| US20040001889A1 (en) * | 2002-06-25 | 2004-01-01 | Guohua Chen | Short duration depot formulations |
| MXPA05001242A (es) * | 2002-07-31 | 2005-06-08 | Alza Corp | Composiciones de deposito inyectable y usos de las mismas. |
| US8313763B2 (en) * | 2004-10-04 | 2012-11-20 | Tolmar Therapeutics, Inc. | Sustained delivery formulations of rapamycin compounds |
| SI2291174T1 (sl) | 2008-06-03 | 2015-05-29 | Tolmar Therapeutics, Inc. | Tekoči sestavek, ki vsebuje biokompatibilne sestavke oligomer-polimer |
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| ES2535330T3 (es) | 2015-05-08 |
| EP2291174B1 (en) | 2015-01-28 |
| SI2291174T1 (sl) | 2015-05-29 |
| US9308162B2 (en) | 2016-04-12 |
| DK2291174T3 (en) | 2015-03-09 |
| CY1116196T1 (el) | 2017-02-08 |
| US20110245172A1 (en) | 2011-10-06 |
| WO2009148581A1 (en) | 2009-12-10 |
| EP2291174A1 (en) | 2011-03-09 |
| PL2291174T3 (pl) | 2015-06-30 |
| PT2291174E (pt) | 2015-05-20 |
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