CA2453111A1 - Formulation pharmaceutique pour l'administration intramusculaire de fulvestrant - Google Patents
Formulation pharmaceutique pour l'administration intramusculaire de fulvestrant Download PDFInfo
- Publication number
- CA2453111A1 CA2453111A1 CA002453111A CA2453111A CA2453111A1 CA 2453111 A1 CA2453111 A1 CA 2453111A1 CA 002453111 A CA002453111 A CA 002453111A CA 2453111 A CA2453111 A CA 2453111A CA 2453111 A1 CA2453111 A1 CA 2453111A1
- Authority
- CA
- Canada
- Prior art keywords
- per volume
- formulation
- weight
- fulvestrant
- weight per
- 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.)
- Abandoned
Links
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 title claims abstract description 183
- 229960002258 fulvestrant Drugs 0.000 title claims abstract description 180
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 110
- 238000007918 intramuscular administration Methods 0.000 title description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 278
- JBTWLSYIZRCDFO-UHFFFAOYSA-N ethyl methyl carbonate Chemical compound CCOC(=O)OC JBTWLSYIZRCDFO-UHFFFAOYSA-N 0.000 claims abstract description 36
- 229940066675 ricinoleate Drugs 0.000 claims abstract description 35
- WBHHMMIMDMUBKC-QJWNTBNXSA-M ricinoleate Chemical compound CCCCCC[C@@H](O)C\C=C/CCCCCCCC([O-])=O WBHHMMIMDMUBKC-QJWNTBNXSA-M 0.000 claims abstract description 35
- 238000002347 injection Methods 0.000 claims abstract description 20
- 239000007924 injection Substances 0.000 claims abstract description 20
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 claims description 296
- 239000000203 mixture Substances 0.000 claims description 296
- 238000009472 formulation Methods 0.000 claims description 276
- SESFRYSPDFLNCH-UHFFFAOYSA-N benzyl benzoate Chemical compound C=1C=CC=CC=1C(=O)OCC1=CC=CC=C1 SESFRYSPDFLNCH-UHFFFAOYSA-N 0.000 claims description 204
- 239000003981 vehicle Substances 0.000 claims description 134
- 229960002903 benzyl benzoate Drugs 0.000 claims description 102
- 235000019445 benzyl alcohol Nutrition 0.000 claims description 99
- 229960004217 benzyl alcohol Drugs 0.000 claims description 90
- 239000004359 castor oil Substances 0.000 claims description 86
- 235000019438 castor oil Nutrition 0.000 claims description 86
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 86
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 39
- 239000007927 intramuscular injection Substances 0.000 claims description 37
- 238000010255 intramuscular injection Methods 0.000 claims description 35
- 210000002381 plasma Anatomy 0.000 claims description 14
- 238000002360 preparation method Methods 0.000 claims description 6
- 210000000481 breast Anatomy 0.000 claims description 5
- 201000010099 disease Diseases 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 230000003211 malignant effect Effects 0.000 claims description 5
- 210000005000 reproductive tract Anatomy 0.000 claims description 5
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 claims description 4
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 claims description 4
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 claims description 4
- 229940093471 ethyl oleate Drugs 0.000 claims description 4
- 229940074928 isopropyl myristate Drugs 0.000 claims description 3
- XUGNVMKQXJXZCD-UHFFFAOYSA-N isopropyl palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC(C)C XUGNVMKQXJXZCD-UHFFFAOYSA-N 0.000 claims description 3
- 229940075495 isopropyl palmitate Drugs 0.000 claims description 3
- 238000013160 medical therapy Methods 0.000 claims description 2
- 239000000243 solution Substances 0.000 abstract description 46
- 150000001875 compounds Chemical class 0.000 abstract description 21
- 238000013268 sustained release Methods 0.000 abstract description 3
- 239000012730 sustained-release form Substances 0.000 abstract description 3
- 229960004756 ethanol Drugs 0.000 description 76
- 239000000523 sample Substances 0.000 description 75
- 238000004128 high performance liquid chromatography Methods 0.000 description 18
- 239000003814 drug Substances 0.000 description 14
- 239000003921 oil Substances 0.000 description 14
- 235000019198 oils Nutrition 0.000 description 14
- 239000000262 estrogen Substances 0.000 description 13
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 12
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 12
- 229940079593 drug Drugs 0.000 description 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 8
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 description 8
- 239000003480 eluent Substances 0.000 description 8
- 230000003637 steroidlike Effects 0.000 description 8
- 241001237728 Precis Species 0.000 description 7
- 241000283973 Oryctolagus cuniculus Species 0.000 description 6
- 238000006073 displacement reaction Methods 0.000 description 6
- 238000001556 precipitation Methods 0.000 description 6
- 150000003431 steroids Chemical class 0.000 description 6
- 206010006187 Breast cancer Diseases 0.000 description 5
- 208000026310 Breast neoplasm Diseases 0.000 description 5
- 235000004443 Ricinus communis Nutrition 0.000 description 5
- 150000001298 alcohols Chemical class 0.000 description 5
- 239000011521 glass Substances 0.000 description 5
- 238000001727 in vivo Methods 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical class OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 4
- -1 Benzyl Benzyl Chemical group 0.000 description 4
- 230000009471 action Effects 0.000 description 4
- MTZQAGJQAFMTAQ-UHFFFAOYSA-N benzoic acid ethyl ester Natural products CCOC(=O)C1=CC=CC=C1 MTZQAGJQAFMTAQ-UHFFFAOYSA-N 0.000 description 4
- 239000000470 constituent Substances 0.000 description 4
- 238000013265 extended release Methods 0.000 description 4
- 238000000338 in vitro Methods 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 229910052757 nitrogen Inorganic materials 0.000 description 4
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 4
- 239000004033 plastic Substances 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- 239000004094 surface-active agent Substances 0.000 description 4
- 229960001603 tamoxifen Drugs 0.000 description 4
- 238000002679 ablation Methods 0.000 description 3
- 239000003963 antioxidant agent Substances 0.000 description 3
- 230000003078 antioxidant effect Effects 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 229930182833 estradiol Natural products 0.000 description 3
- 238000005259 measurement Methods 0.000 description 3
- 238000007911 parenteral administration Methods 0.000 description 3
- 238000012421 spiking Methods 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 201000009273 Endometriosis Diseases 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 241000700159 Rattus Species 0.000 description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 2
- 229910052782 aluminium Inorganic materials 0.000 description 2
- 239000004411 aluminium Substances 0.000 description 2
- 230000001833 anti-estrogenic effect Effects 0.000 description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 2
- 230000037182 bone density Effects 0.000 description 2
- 239000003086 colorant Substances 0.000 description 2
- 239000013068 control sample Substances 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 230000008021 deposition Effects 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 238000010586 diagram Methods 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 238000001914 filtration Methods 0.000 description 2
- 239000011159 matrix material Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 230000036470 plasma concentration Effects 0.000 description 2
- 229940071643 prefilled syringe Drugs 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 230000002335 preservative effect Effects 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- WBHHMMIMDMUBKC-XLNAKTSKSA-N ricinelaidic acid Chemical compound CCCCCC[C@@H](O)C\C=C\CCCCCCCC(O)=O WBHHMMIMDMUBKC-XLNAKTSKSA-N 0.000 description 2
- 229960003656 ricinoleic acid Drugs 0.000 description 2
- FEUQNCSVHBHROZ-UHFFFAOYSA-N ricinoleic acid Natural products CCCCCCC(O[Si](C)(C)C)CC=CCCCCCCCC(=O)OC FEUQNCSVHBHROZ-UHFFFAOYSA-N 0.000 description 2
- 230000004936 stimulating effect Effects 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- 150000003626 triacylglycerols Chemical class 0.000 description 2
- 230000001836 utereotrophic effect Effects 0.000 description 2
- 230000000007 visual effect Effects 0.000 description 2
- 238000011179 visual inspection Methods 0.000 description 2
- VWUXBMIQPBEWFH-SNMGGSQJSA-N (7r,8r,9s,13s,14s)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-SNMGGSQJSA-N 0.000 description 1
- 235000003911 Arachis Nutrition 0.000 description 1
- 244000105624 Arachis hypogaea Species 0.000 description 1
- 238000012371 Aseptic Filling Methods 0.000 description 1
- 241000282693 Cercopithecidae Species 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 206010060800 Hot flush Diseases 0.000 description 1
- 206010027304 Menopausal symptoms Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 241001670273 Ooia Species 0.000 description 1
- PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 230000008484 agonism Effects 0.000 description 1
- 230000001270 agonistic effect Effects 0.000 description 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 239000003886 aromatase inhibitor Substances 0.000 description 1
- 229940046844 aromatase inhibitors Drugs 0.000 description 1
- 230000006399 behavior Effects 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 239000008364 bulk solution Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229960000935 dehydrated alcohol Drugs 0.000 description 1
- 239000008367 deionised water Substances 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 239000003759 ester based solvent Substances 0.000 description 1
- 229940011871 estrogen Drugs 0.000 description 1
- 230000001076 estrogenic effect Effects 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 229940087861 faslodex Drugs 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 239000013022 formulation composition Substances 0.000 description 1
- 229940027974 fulvestrant 50 mg/ml Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 230000002267 hypothalamic effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000002050 international nonproprietary name Substances 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 238000012417 linear regression Methods 0.000 description 1
- 150000002634 lipophilic molecules Chemical class 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 238000003760 magnetic stirring Methods 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 230000036961 partial effect Effects 0.000 description 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 239000004417 polycarbonate Substances 0.000 description 1
- 229920000515 polycarbonate Polymers 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000003439 radiotherapeutic effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000008844 regulatory mechanism Effects 0.000 description 1
- QEVHRUUCFGRFIF-MDEJGZGSSA-N reserpine Chemical compound O([C@H]1[C@@H]([C@H]([C@H]2C[C@@H]3C4=C(C5=CC=C(OC)C=C5N4)CCN3C[C@H]2C1)C(=O)OC)OC)C(=O)C1=CC(OC)=C(OC)C(OC)=C1 QEVHRUUCFGRFIF-MDEJGZGSSA-N 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 238000011146 sterile filtration Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 229960005026 toremifene Drugs 0.000 description 1
- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 description 1
- 230000002103 transcriptional effect Effects 0.000 description 1
- 230000001228 trophic effect Effects 0.000 description 1
- 210000004291 uterus Anatomy 0.000 description 1
Classifications
-
- 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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- 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
-
- 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
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Dermatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
La présente invention concerne une formulation pharmaceutique à libération prolongée, adaptée à l'administration par injection, contenant le composé de fulvestrant, 7 a-[9-(4,4,5,5,5-pentafluoropentylsulphiny1)nony1]oestra-1,3,5(10)-triène-3,17 .szlig.-diol, à une concentration d'au moins 100mg/ml en solution dans un excipient de ricinoléate qui comprend également au moins un alcool et un solvant ester non aqueux miscible dans l'excipient de ricinoléate.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0116619.8A GB0116619D0 (en) | 2001-07-07 | 2001-07-07 | Formulation |
| GB0116619.8 | 2001-07-07 | ||
| US31571101P | 2001-08-30 | 2001-08-30 | |
| US60/315,711 | 2001-08-31 | ||
| PCT/GB2002/003092 WO2003006064A1 (fr) | 2001-07-07 | 2002-07-03 | Formulation pharmaceutique pour l'administration intramusculaire de fulvestrant |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2453111A1 true CA2453111A1 (fr) | 2003-01-23 |
Family
ID=26246290
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002453111A Abandoned CA2453111A1 (fr) | 2001-07-07 | 2002-07-03 | Formulation pharmaceutique pour l'administration intramusculaire de fulvestrant |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP1406662A1 (fr) |
| JP (1) | JP2004534093A (fr) |
| CN (1) | CN1553815A (fr) |
| AR (1) | AR037138A1 (fr) |
| BR (1) | BR0210898A (fr) |
| CA (1) | CA2453111A1 (fr) |
| CO (1) | CO5560585A2 (fr) |
| HU (1) | HUP0400115A3 (fr) |
| IL (1) | IL159576A0 (fr) |
| IS (1) | IS7097A (fr) |
| MX (1) | MXPA04000028A (fr) |
| NO (1) | NO20040047L (fr) |
| PL (1) | PL367624A1 (fr) |
| RU (1) | RU2004102393A (fr) |
| WO (1) | WO2003006064A1 (fr) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0000313D0 (en) | 2000-01-10 | 2000-03-01 | Astrazeneca Uk Ltd | Formulation |
| EP2417975A4 (fr) | 2009-08-31 | 2012-11-14 | Xi An Libang Medical Technology Co Ltd | Nanosphère/microsphère de fulvestrant, procédé de préparation et utilisation associés |
| CN102600064A (zh) * | 2012-03-31 | 2012-07-25 | 西安力邦制药有限公司 | 氟维司群或其衍生物缓释制剂及其制备方法 |
| CN102600065B (zh) * | 2012-03-31 | 2014-08-13 | 莱普德制药有限公司 | 一种氟维司群或其衍生物油性制剂及其制备方法 |
| CN102600073B (zh) * | 2012-03-31 | 2014-01-01 | 莱普德制药有限公司 | 以乳酸酯为基础的氟维司群或其衍生物油性制剂及其制备方法 |
| US9271990B2 (en) | 2014-02-14 | 2016-03-01 | Fresenius Kabi Usa, Llc | Fulvestrant formulations |
| EP3441073B1 (fr) * | 2016-04-06 | 2022-02-23 | FUJIFILM Corporation | Composition médicinale comprenant du fulvestrant |
| IL285928B2 (en) * | 2016-05-06 | 2025-06-01 | Eagle Pharmaceuticals Inc | Fulvestrant formulations and methods of their use |
| US11590077B2 (en) | 2016-05-06 | 2023-02-28 | Eagle Pharmaceuticals, Inc. | Fulvestrant formulations and methods of their use |
| EP3466430B1 (fr) | 2016-05-31 | 2020-04-29 | FUJIFILM Corporation | Préparation pharmaceutique |
| JP7220712B2 (ja) | 2017-11-08 | 2023-02-10 | イーグル ファーマスーティカルズ、インク． | フルベストラント製剤とその使用方法 |
| US20210169897A1 (en) * | 2017-12-07 | 2021-06-10 | Nevakar Inc. | Concentrated Fulvestrant Compositions |
| WO2019151353A1 (fr) * | 2018-01-31 | 2019-08-08 | 富士フイルム株式会社 | Méthode de production de préparation pour injection |
| CN111481559B (zh) * | 2019-01-25 | 2021-10-08 | 江苏恒瑞医药股份有限公司 | 一种高浓度的氟维司群组合物及其制备方法 |
| US12377049B2 (en) | 2019-12-11 | 2025-08-05 | Shanghai Bocimed Pharmaceutical Co., Ltd. | Fulvestrant pharmaceutical composition, preparation method therefor, and application thereof |
| WO2023121232A1 (fr) * | 2021-12-20 | 2023-06-29 | 주식회사 삼양홀딩스 | Composition pharmaceutique de fulvestrant ayant une solubilité améliorée, et son procédé de préparation |
| CN118717660B (zh) * | 2024-06-12 | 2025-02-28 | 湖州亚瑟制药有限公司 | 一种注射用氟维司群药物组合物及其制备方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8813353D0 (en) * | 1988-06-06 | 1988-07-13 | Ici Plc | Therapeutic product |
| GB9525194D0 (en) * | 1995-12-12 | 1996-02-07 | Zeneca Ltd | Pharmaceutical composition |
| GB0000313D0 (en) * | 2000-01-10 | 2000-03-01 | Astrazeneca Uk Ltd | Formulation |
| GB0008172D0 (en) * | 2000-04-05 | 2000-05-24 | Astrazeneca Ab | Therapy |
-
2002
- 2002-07-03 CA CA002453111A patent/CA2453111A1/fr not_active Abandoned
- 2002-07-03 CN CNA028171888A patent/CN1553815A/zh active Pending
- 2002-07-03 RU RU2004102393/15A patent/RU2004102393A/ru not_active Application Discontinuation
- 2002-07-03 HU HU0400115A patent/HUP0400115A3/hu unknown
- 2002-07-03 PL PL02367624A patent/PL367624A1/xx not_active Application Discontinuation
- 2002-07-03 BR BR0210898-4A patent/BR0210898A/pt not_active IP Right Cessation
- 2002-07-03 WO PCT/GB2002/003092 patent/WO2003006064A1/fr not_active Ceased
- 2002-07-03 IL IL15957602A patent/IL159576A0/xx unknown
- 2002-07-03 JP JP2003511869A patent/JP2004534093A/ja active Pending
- 2002-07-03 EP EP02740940A patent/EP1406662A1/fr not_active Withdrawn
- 2002-07-05 AR ARP020102523A patent/AR037138A1/es not_active Application Discontinuation
-
2004
- 2004-01-05 IS IS7097A patent/IS7097A/is unknown
- 2004-01-06 NO NO20040047A patent/NO20040047L/no not_active Application Discontinuation
- 2004-01-07 CO CO04000761A patent/CO5560585A2/es not_active Application Discontinuation
- 2004-01-07 MX MXPA04000028A patent/MXPA04000028A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2004534093A (ja) | 2004-11-11 |
| HUP0400115A2 (hu) | 2004-06-28 |
| IS7097A (is) | 2004-01-05 |
| EP1406662A1 (fr) | 2004-04-14 |
| PL367624A1 (en) | 2005-03-07 |
| RU2004102393A (ru) | 2005-03-27 |
| NO20040047L (no) | 2004-02-23 |
| BR0210898A (pt) | 2004-06-22 |
| WO2003006064A1 (fr) | 2003-01-23 |
| CO5560585A2 (es) | 2005-09-30 |
| AR037138A1 (es) | 2004-10-27 |
| IL159576A0 (en) | 2004-06-01 |
| CN1553815A (zh) | 2004-12-08 |
| MXPA04000028A (es) | 2004-05-21 |
| HUP0400115A3 (en) | 2005-11-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DK1250138T4 (en) | Fulvestrantformulering | |
| EP1406662A1 (fr) | Formulation pharmaceutique pour l'administration intramusculaire de fulvestrant | |
| ES2294146T3 (es) | Formulacion que comprende fulvestrant. | |
| PT1457208E (pt) | Métodos e composições farmacêuticas para obtenção fidedigna de níveis aceitáveis de testosterona no soro | |
| AU2002314368A1 (en) | Pharmaceutical formulation for the intramuscular administration of fulvestrant | |
| ZA200400079B (en) | Pharmaceutical formulation for the intramuscular administration of fulvestrant. | |
| HK1153393A (en) | Fulvestrant formulation | |
| HK1150021B (en) | Fulvestrant formulation |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |