CN103841994A - 适用于pet成像的氟化茋的配方 - Google Patents
适用于pet成像的氟化茋的配方 Download PDFInfo
- Publication number
- CN103841994A CN103841994A CN201280030986.6A CN201280030986A CN103841994A CN 103841994 A CN103841994 A CN 103841994A CN 201280030986 A CN201280030986 A CN 201280030986A CN 103841994 A CN103841994 A CN 103841994A
- Authority
- CN
- China
- Prior art keywords
- ethyoxyl
- phenyl
- amine
- methyl
- vinyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- PJANXHGTPQOBST-UHFFFAOYSA-N stilbene Chemical class C=1C=CC=CC=1C=CC1=CC=CC=C1 PJANXHGTPQOBST-UHFFFAOYSA-N 0.000 title claims abstract description 54
- 239000000203 mixture Substances 0.000 title claims abstract description 39
- 238000009472 formulation Methods 0.000 title abstract description 7
- 238000003384 imaging method Methods 0.000 title description 2
- PJANXHGTPQOBST-VAWYXSNFSA-N Stilbene Natural products C=1C=CC=CC=1/C=C/C1=CC=CC=C1 PJANXHGTPQOBST-VAWYXSNFSA-N 0.000 claims abstract description 52
- 235000021286 stilbenes Nutrition 0.000 claims abstract description 52
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims abstract description 39
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims abstract description 39
- 239000003446 ligand Substances 0.000 claims abstract description 39
- 238000000034 method Methods 0.000 claims abstract description 14
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 83
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 68
- 239000008194 pharmaceutical composition Substances 0.000 claims description 60
- 229920002554 vinyl polymer Polymers 0.000 claims description 56
- 235000010323 ascorbic acid Nutrition 0.000 claims description 34
- 239000011668 ascorbic acid Substances 0.000 claims description 34
- 229960005070 ascorbic acid Drugs 0.000 claims description 34
- 235000010378 sodium ascorbate Nutrition 0.000 claims description 33
- 229960005055 sodium ascorbate Drugs 0.000 claims description 33
- PPASLZSBLFJQEF-RKJRWTFHSA-M sodium ascorbate Substances [Na+].OC[C@@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RKJRWTFHSA-M 0.000 claims description 33
- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 claims description 33
- 150000003839 salts Chemical class 0.000 claims description 26
- 239000000700 radioactive tracer Substances 0.000 claims description 21
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 20
- 229920001223 polyethylene glycol Polymers 0.000 claims description 20
- 238000001914 filtration Methods 0.000 claims description 19
- 229920000570 polyether Polymers 0.000 claims description 19
- 230000001954 sterilising effect Effects 0.000 claims description 17
- 238000002360 preparation method Methods 0.000 claims description 10
- BQCIDUSAKPWEOX-UHFFFAOYSA-N 1,1-Difluoroethene Chemical group FC(F)=C BQCIDUSAKPWEOX-UHFFFAOYSA-N 0.000 claims description 7
- 230000001476 alcoholic effect Effects 0.000 claims description 5
- 239000000463 material Substances 0.000 claims description 5
- 238000002414 normal-phase solid-phase extraction Methods 0.000 claims description 4
- 238000000746 purification Methods 0.000 claims description 4
- 238000010828 elution Methods 0.000 claims description 2
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims 4
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 claims 4
- 229950000845 politef Drugs 0.000 claims 4
- 239000002033 PVDF binder Substances 0.000 claims 2
- 229920002981 polyvinylidene fluoride Polymers 0.000 claims 2
- 238000012879 PET imaging Methods 0.000 abstract description 8
- 241000124008 Mammalia Species 0.000 abstract description 3
- 238000011146 sterile filtration Methods 0.000 abstract 1
- 229940125904 compound 1 Drugs 0.000 description 22
- 238000002600 positron emission tomography Methods 0.000 description 15
- 150000001875 compounds Chemical class 0.000 description 14
- 239000000243 solution Substances 0.000 description 12
- 238000010521 absorption reaction Methods 0.000 description 11
- 239000003814 drug Substances 0.000 description 11
- 229940125782 compound 2 Drugs 0.000 description 10
- 229910052731 fluorine Inorganic materials 0.000 description 10
- 229920001343 polytetrafluoroethylene Polymers 0.000 description 10
- 239000004810 polytetrafluoroethylene Substances 0.000 description 10
- 239000002202 Polyethylene glycol Substances 0.000 description 9
- 229910052799 carbon Inorganic materials 0.000 description 9
- 230000000968 intestinal effect Effects 0.000 description 8
- 239000000126 substance Substances 0.000 description 7
- 125000001153 fluoro group Chemical group F* 0.000 description 6
- -1 polytetrafluoroethylene Polymers 0.000 description 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 4
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 description 4
- 239000011737 fluorine Substances 0.000 description 4
- 230000002209 hydrophobic effect Effects 0.000 description 4
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- SJRJJKPEHAURKC-UHFFFAOYSA-N N-Methylmorpholine Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
- 239000003153 chemical reaction reagent Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 238000002372 labelling Methods 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- 238000003860 storage Methods 0.000 description 3
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 2
- NCWZOASIUQVOFA-NSCUHMNNSA-N CNc1ccc(/C=C/c(cc2)ccc2OCCOCCOCCF)cc1 Chemical compound CNc1ccc(/C=C/c(cc2)ccc2OCCOCCOCCF)cc1 NCWZOASIUQVOFA-NSCUHMNNSA-N 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 239000003513 alkali Substances 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 2
- 229910052794 bromium Inorganic materials 0.000 description 2
- DMBHHRLKUKUOEG-UHFFFAOYSA-N diphenylamine Chemical compound C=1C=CC=CC=1NC1=CC=CC=C1 DMBHHRLKUKUOEG-UHFFFAOYSA-N 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000000428 dust Substances 0.000 description 2
- 125000001033 ether group Chemical group 0.000 description 2
- 239000000706 filtrate Substances 0.000 description 2
- 229910052736 halogen Inorganic materials 0.000 description 2
- 150000002367 halogens Chemical class 0.000 description 2
- 238000001990 intravenous administration Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- 230000002285 radioactive effect Effects 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- 239000008215 water for injection Substances 0.000 description 2
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 description 1
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 239000004475 Arginine Substances 0.000 description 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- XBPCUCUWBYBCDP-UHFFFAOYSA-N Dicyclohexylamine Chemical compound C1CCCCC1NC1CCCCC1 XBPCUCUWBYBCDP-UHFFFAOYSA-N 0.000 description 1
- QUSNBJAOOMFDIB-UHFFFAOYSA-N Ethylamine Chemical compound CCN QUSNBJAOOMFDIB-UHFFFAOYSA-N 0.000 description 1
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 description 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 1
- UEEJHVSXFDXPFK-UHFFFAOYSA-N N-dimethylaminoethanol Chemical compound CN(C)CCO UEEJHVSXFDXPFK-UHFFFAOYSA-N 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 229920002535 Polyethylene Glycol 1500 Polymers 0.000 description 1
- 229920002556 Polyethylene Glycol 300 Polymers 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 1
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 description 1
- 229940022663 acetate Drugs 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 150000001447 alkali salts Chemical class 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 229910021529 ammonia Inorganic materials 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 1
- 229940077388 benzenesulfonate Drugs 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 159000000007 calcium salts Chemical class 0.000 description 1
- 150000001721 carbon Chemical group 0.000 description 1
- 150000001735 carboxylic acids Chemical class 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000003638 chemical reducing agent Substances 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 239000000460 chlorine Substances 0.000 description 1
- 229940001468 citrate Drugs 0.000 description 1
- 238000005352 clarification Methods 0.000 description 1
- 150000003983 crown ethers Chemical class 0.000 description 1
- 229960002887 deanol Drugs 0.000 description 1
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 1
- HPNMFZURTQLUMO-UHFFFAOYSA-N diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 229940035422 diphenylamine Drugs 0.000 description 1
- 229950007655 esilate Drugs 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 229940050411 fumarate Drugs 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 238000002513 implantation Methods 0.000 description 1
- 230000008676 import Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 239000007951 isotonicity adjuster Substances 0.000 description 1
- 229940001447 lactate Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 159000000003 magnesium salts Chemical class 0.000 description 1
- 229940049920 malate Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 229950005216 napadisilate Drugs 0.000 description 1
- 238000012633 nuclear imaging Methods 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
- 229960004919 procaine Drugs 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 229950004288 tosilate Drugs 0.000 description 1
- 239000012905 visible particle Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0404—Lipids, e.g. triglycerides; Polycationic carriers
- A61K51/0406—Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines
-
- 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
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
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- A—HUMAN NECESSITIES
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- A61K49/00—Preparations for testing in vivo
- A61K49/0004—Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/041—Heterocyclic compounds
- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0455—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/041—Heterocyclic compounds
- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/12—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules
- A61K51/121—Solutions, i.e. homogeneous liquid formulation
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Optics & Photonics (AREA)
- Physics & Mathematics (AREA)
- Engineering & Computer Science (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Dermatology (AREA)
- Pathology (AREA)
- Biomedical Technology (AREA)
- Gastroenterology & Hepatology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Toxicology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Dispersion Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
GBq | 千兆贝可勒尔 |
RT | 室温 |
PBS | 磷酸盐缓冲盐 |
PET | 正电子放射断层摄影术 |
WFI | 注射用水 |
成分 | 配方1 |
化合物1 | 30μg |
96%乙醇 | 1.5mL |
聚乙二醇(PEG400) | 2g |
抗坏血酸 | 0.044g |
抗坏血酸钠 | 0.288g |
水 | 加至10mL |
pH | 约5.5 |
配方1 | 配方2 | 标准配方 | |
滤液(%) | 98.8±0.6 | 74.7±6 | 42.8±2.4 |
吸附 | 1.2% | 25.3% | 57.2% |
配方1 | 配方2 | 标准配方 | |
滤液(%) | 94.0±0.7 | 55.9±2.3 | 40.8±0.8 |
吸附 | 6.0% | 44.1% | 59.2% |
Claims (10)
Priority Applications (1)
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CN201610227155.8A CN105833303A (zh) | 2011-06-21 | 2012-06-21 | 适用于pet成像的氟化茋的制剂 |
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EP11005047 | 2011-06-21 | ||
EP11005047.3 | 2011-06-21 | ||
PCT/EP2012/062034 WO2012175641A1 (en) | 2011-06-21 | 2012-06-21 | Formulations of fluorinated stilbene suitable for pet imaging |
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CN201610227155.8A Division CN105833303A (zh) | 2011-06-21 | 2012-06-21 | 适用于pet成像的氟化茋的制剂 |
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CN103841994A true CN103841994A (zh) | 2014-06-04 |
CN103841994B CN103841994B (zh) | 2016-05-11 |
Family
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CN201610227155.8A Pending CN105833303A (zh) | 2011-06-21 | 2012-06-21 | 适用于pet成像的氟化茋的制剂 |
CN201280030986.6A Active CN103841994B (zh) | 2011-06-21 | 2012-06-21 | 适用于pet成像的氟化茋的制剂 |
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CN201610227155.8A Pending CN105833303A (zh) | 2011-06-21 | 2012-06-21 | 适用于pet成像的氟化茋的制剂 |
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US (1) | US9308284B2 (zh) |
EP (1) | EP2723394B1 (zh) |
JP (1) | JP6081997B2 (zh) |
KR (1) | KR101869129B1 (zh) |
CN (2) | CN105833303A (zh) |
AU (1) | AU2012274076B2 (zh) |
BR (1) | BR112013032610B1 (zh) |
CA (1) | CA2839961C (zh) |
DK (1) | DK2723394T3 (zh) |
ES (1) | ES2683818T3 (zh) |
HK (2) | HK1197031A1 (zh) |
HR (1) | HRP20181081T1 (zh) |
HU (1) | HUE039909T2 (zh) |
IL (1) | IL230042A (zh) |
MX (1) | MX344954B (zh) |
MY (1) | MY183997A (zh) |
PL (1) | PL2723394T3 (zh) |
PT (1) | PT2723394T (zh) |
RU (1) | RU2623867C2 (zh) |
SI (1) | SI2723394T1 (zh) |
WO (1) | WO2012175641A1 (zh) |
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EP2836241B1 (en) * | 2012-04-10 | 2019-02-20 | Lantheus Medical Imaging, Inc. | Radiopharmaceutical synthesis methods |
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DE69920409T2 (de) * | 1998-02-20 | 2005-10-06 | Ciba Speciality Chemicals Holding Inc. | Verfahren zur herstellung von stilbenverbindungen |
DE10012120A1 (de) * | 2000-03-13 | 2001-09-27 | Ktb Tumorforschungs Gmbh | Therapeutische und diagnostische Ligandensysteme mit Transportmolekülbindenden Eigenschaften und diese enthaltende Arzneimittel |
EP1432453B1 (en) * | 2001-08-27 | 2013-08-14 | The Trustees of The University of Pennsylvania | Stilbene derivatives and their use for binding and imaging amyloid plaques |
SI2213652T1 (sl) | 2004-12-17 | 2015-03-31 | The Trustees Of The University Of Pennsylvania | Derivati stilbena in njihova uporaba za vezavo in prikaz amiloidnih plakov |
PL2381967T3 (pl) * | 2008-12-31 | 2017-06-30 | Avid Radiopharmaceuticals, Inc. | Synteza styrylopirydyn radioznakowanych 18F z prekursorów tosylanowych i ich stabilne kompozycje farmaceutyczne |
US8658129B2 (en) * | 2009-06-04 | 2014-02-25 | General Electric Company | Agents and methods for the imaging of myelin basic protein |
KR101718164B1 (ko) | 2009-12-17 | 2017-03-20 | 엘지전자 주식회사 | 인증 절차를 고려한 핸드오버 수행 방법 및 장치 |
AR079687A1 (es) * | 2009-12-23 | 2012-02-15 | Bayer Schering Pharma Ag | Formulaciones adecuadas para el diagnostico por imagenes con pet |
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- 2012-06-21 CN CN201610227155.8A patent/CN105833303A/zh active Pending
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Publication number | Publication date |
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CA2839961A1 (en) | 2012-12-27 |
IL230042A (en) | 2017-06-29 |
KR101869129B1 (ko) | 2018-06-19 |
SI2723394T1 (sl) | 2018-10-30 |
MX2013015074A (es) | 2014-11-10 |
WO2012175641A1 (en) | 2012-12-27 |
PL2723394T3 (pl) | 2018-11-30 |
CA2839961C (en) | 2019-08-13 |
JP2014517054A (ja) | 2014-07-17 |
EP2723394A1 (en) | 2014-04-30 |
AU2012274076A1 (en) | 2014-01-16 |
HRP20181081T1 (hr) | 2018-09-21 |
EP2723394B1 (en) | 2018-05-23 |
MX344954B (es) | 2017-01-12 |
AU2012274076B2 (en) | 2017-06-15 |
KR20140061347A (ko) | 2014-05-21 |
RU2623867C2 (ru) | 2017-06-29 |
RU2014101557A (ru) | 2015-07-27 |
HK1225648A1 (zh) | 2017-09-15 |
HK1197031A1 (zh) | 2015-01-02 |
BR112013032610B1 (pt) | 2022-05-31 |
DK2723394T3 (en) | 2018-08-13 |
US9308284B2 (en) | 2016-04-12 |
ES2683818T3 (es) | 2018-09-28 |
BR112013032610A2 (pt) | 2017-01-24 |
US20140241986A1 (en) | 2014-08-28 |
PT2723394T (pt) | 2018-07-30 |
CN105833303A (zh) | 2016-08-10 |
CN103841994B (zh) | 2016-05-11 |
HUE039909T2 (hu) | 2019-02-28 |
NZ618977A (en) | 2015-07-31 |
JP6081997B2 (ja) | 2017-02-15 |
MY183997A (en) | 2021-03-17 |
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