ES2248272T5 - Formulación de fulvestrant - Google Patents
Formulación de fulvestrant Download PDFInfo
- Publication number
- ES2248272T5 ES2248272T5 ES01900186.6T ES01900186T ES2248272T5 ES 2248272 T5 ES2248272 T5 ES 2248272T5 ES 01900186 T ES01900186 T ES 01900186T ES 2248272 T5 ES2248272 T5 ES 2248272T5
- Authority
- ES
- Spain
- Prior art keywords
- formulation
- fulvestrant
- oil
- volume
- castor
- 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.)
- Expired - Lifetime
Links
- 238000009472 formulation Methods 0.000 title description 30
- 239000000203 mixture Substances 0.000 title description 30
- 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 description 21
- 229960002258 fulvestrant Drugs 0.000 title description 21
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 23
- 239000003921 oil Substances 0.000 description 13
- 235000019198 oils Nutrition 0.000 description 13
- SESFRYSPDFLNCH-UHFFFAOYSA-N benzyl benzoate Chemical compound C=1C=CC=CC=1C(=O)OCC1=CC=CC=C1 SESFRYSPDFLNCH-UHFFFAOYSA-N 0.000 description 8
- 238000010255 intramuscular injection Methods 0.000 description 7
- 239000007927 intramuscular injection Substances 0.000 description 7
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 6
- DOMWKUIIPQCAJU-LJHIYBGHSA-N Hydroxyprogesterone caproate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)CCCCC)[C@@]1(C)CC2 DOMWKUIIPQCAJU-LJHIYBGHSA-N 0.000 description 6
- 239000003981 vehicle Substances 0.000 description 6
- 239000008194 pharmaceutical composition Substances 0.000 description 5
- WBHHMMIMDMUBKC-QJWNTBNXSA-M ricinoleate Chemical compound CCCCCC[C@@H](O)C\C=C/CCCCCCCC([O-])=O WBHHMMIMDMUBKC-QJWNTBNXSA-M 0.000 description 5
- 229940066675 ricinoleate Drugs 0.000 description 5
- 229960002903 benzyl benzoate Drugs 0.000 description 4
- 239000004359 castor oil Substances 0.000 description 4
- 235000019438 castor oil Nutrition 0.000 description 4
- 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 description 4
- 229950000801 hydroxyprogesterone caproate Drugs 0.000 description 4
- 239000000583 progesterone congener Substances 0.000 description 4
- 150000003431 steroids Chemical class 0.000 description 4
- 235000017060 Arachis glabrata Nutrition 0.000 description 3
- 244000105624 Arachis hypogaea Species 0.000 description 3
- 235000010777 Arachis hypogaea Nutrition 0.000 description 3
- 235000018262 Arachis monticola Nutrition 0.000 description 3
- 235000004443 Ricinus communis Nutrition 0.000 description 3
- 150000001298 alcohols Chemical class 0.000 description 3
- 239000000470 constituent Substances 0.000 description 3
- 150000002148 esters Chemical class 0.000 description 3
- 235000020232 peanut Nutrition 0.000 description 3
- 210000002381 plasma Anatomy 0.000 description 3
- APTGJECXMIKIET-WOSSHHRXSA-N Norethindrone enanthate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)CCCCCC)[C@@]1(C)CC2 APTGJECXMIKIET-WOSSHHRXSA-N 0.000 description 2
- 244000000231 Sesamum indicum Species 0.000 description 2
- 235000003434 Sesamum indicum Nutrition 0.000 description 2
- 239000003098 androgen Substances 0.000 description 2
- 235000019445 benzyl alcohol Nutrition 0.000 description 2
- 229960004766 estradiol valerate Drugs 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 229960002082 norethindrone enanthate Drugs 0.000 description 2
- 229940071643 prefilled syringe Drugs 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 235000015112 vegetable and seed oil Nutrition 0.000 description 2
- VRLWSGRTKABVDF-DADHALBJSA-N (8S,9S,10R,13S,14S,17R)-17-acetyl-16-hydroxy-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one heptanoic acid Chemical compound CCCCCCC(O)=O.C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC(O)[C@H](C(=O)C)[C@@]1(C)CC2 VRLWSGRTKABVDF-DADHALBJSA-N 0.000 description 1
- KXUGUWTUFUWYRS-UHFFFAOYSA-N 1-methylimidazole-4-sulfonyl chloride Chemical compound CN1C=NC(S(Cl)(=O)=O)=C1 KXUGUWTUFUWYRS-UHFFFAOYSA-N 0.000 description 1
- DBPWSSGDRRHUNT-UHFFFAOYSA-N 17alpha-hydroxy progesterone Natural products C1CC2=CC(=O)CCC2(C)C2C1C1CCC(C(=O)C)(O)C1(C)CC2 DBPWSSGDRRHUNT-UHFFFAOYSA-N 0.000 description 1
- DBPWSSGDRRHUNT-CEGNMAFCSA-N 17α-hydroxyprogesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)C)(O)[C@@]1(C)CC2 DBPWSSGDRRHUNT-CEGNMAFCSA-N 0.000 description 1
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound 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 1
- ORGPUALGNXTPAW-UHFFFAOYSA-N 2,6-dichloro-n-(1-cyanocycloheptyl)benzamide Chemical compound ClC1=CC=CC(Cl)=C1C(=O)NC1(C#N)CCCCCC1 ORGPUALGNXTPAW-UHFFFAOYSA-N 0.000 description 1
- UYIFTLBWAOGQBI-BZDYCCQFSA-N Benzhormovarine Chemical compound C([C@@H]1[C@@H](C2=CC=3)CC[C@]4([C@H]1CC[C@@H]4O)C)CC2=CC=3OC(=O)C1=CC=CC=C1 UYIFTLBWAOGQBI-BZDYCCQFSA-N 0.000 description 1
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 1
- RSEPBGGWRJCQGY-RBRWEJTLSA-N Estradiol valerate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 RSEPBGGWRJCQGY-RBRWEJTLSA-N 0.000 description 1
- 240000007817 Olea europaea Species 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- PPYHLSBUTAPNGT-BKWLFHPQSA-N Testosterone isocaproate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCC(C)C)[C@@]1(C)CC2 PPYHLSBUTAPNGT-BKWLFHPQSA-N 0.000 description 1
- PDMMFKSKQVNJMI-BLQWBTBKSA-N Testosterone propionate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CC)[C@@]1(C)CC2 PDMMFKSKQVNJMI-BLQWBTBKSA-N 0.000 description 1
- NKJYZYWCGKSMSV-BDPSOKNUSA-N [(8r,9s,10r,13s,14s,17r)-17-acetyl-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthren-17-yl] heptanoate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)CCCCCC)[C@@]1(C)CC2 NKJYZYWCGKSMSV-BDPSOKNUSA-N 0.000 description 1
- GRAAWEGTURLYKP-MVTMSODMSA-N [(8r,9s,10r,13s,14s,17s)-13-methyl-3-oxo-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-17-yl] undecanoate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCCCCCC)[C@@]1(C)CC2 GRAAWEGTURLYKP-MVTMSODMSA-N 0.000 description 1
- IVRCALGRJCHPRV-BZDYCCQFSA-N [(8r,9s,13s,14s,17s)-3-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] cyclohexanecarboxylate Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H](C4=CC=C(O)C=C4CC3)CC[C@@]21C)C(=O)C1CCCCC1 IVRCALGRJCHPRV-BZDYCCQFSA-N 0.000 description 1
- 239000003125 aqueous solvent Substances 0.000 description 1
- MTZQAGJQAFMTAQ-UHFFFAOYSA-N benzoic acid ethyl ester Natural products CCOC(=O)C1=CC=CC=C1 MTZQAGJQAFMTAQ-UHFFFAOYSA-N 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 125000001743 benzylic group Chemical group 0.000 description 1
- 239000003433 contraceptive agent Substances 0.000 description 1
- 230000002254 contraceptive effect Effects 0.000 description 1
- STORWMDPIHOSMF-UHFFFAOYSA-N decanoic acid;octanoic acid;propane-1,2,3-triol Chemical compound OCC(O)CO.CCCCCCCC(O)=O.CCCCCCCCCC(O)=O STORWMDPIHOSMF-UHFFFAOYSA-N 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229960005309 estradiol Drugs 0.000 description 1
- 229930182833 estradiol Natural products 0.000 description 1
- JBTWLSYIZRCDFO-UHFFFAOYSA-N ethyl methyl carbonate Chemical compound CCOC(=O)OC JBTWLSYIZRCDFO-UHFFFAOYSA-N 0.000 description 1
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 1
- 229940093471 ethyl oleate Drugs 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 229940062451 progesterone 50 mg Drugs 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 229960003410 testosterone decanoate Drugs 0.000 description 1
- 229960001642 testosterone isocaproate Drugs 0.000 description 1
- 229960001712 testosterone propionate Drugs 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- MEHHPFQKXOUFFV-OWSLCNJRSA-N trenbolone Chemical compound C1CC(=O)C=C2CC[C@@H]([C@H]3[C@@](C)([C@H](CC3)O)C=C3)C3=C21 MEHHPFQKXOUFFV-OWSLCNJRSA-N 0.000 description 1
- 229960000312 trenbolone Drugs 0.000 description 1
- GQJSFWYQKNQCIK-APFRJGHOSA-N trenbolone hexahydrobenzylcarbonate Chemical compound O([C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CCC4=C3C=C[C@@]21C)C(=O)OCC1CCCCC1 GQJSFWYQKNQCIK-APFRJGHOSA-N 0.000 description 1
- 229950005402 trenbolone hexahydrobenzylcarbonate Drugs 0.000 description 1
Classifications
-
- 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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
- TABLA 1 -Inyecciones intramusculares de acción prolongada, a base de aceite
- Nombre del producto
- Esteroide Dosis Tipo Comp. Fuente Aceite BzBz BzOH EtOH Dosis Dosificación
- SUSTANON100
- Propionato de testosterona 30 mg Andrógeno Organon Comp. Hoja datos ABPI 1999 Cacahuete 0,1 ml 1 ml 3 semanas
- Fenilpropionato de testosterona
- 60 mg
- Isocaproato de testosterona
- 60 mg
- Decanoato de testosterona
- 100 mg
- PROLUTONDEPOT
- Hexanoato de hidroxiprogesterona 250 mgml-1 Progestágeno Schering HC Comp. Hoja datos ABPI 1999 Ricino Hasta46% 1 ó 2 ml 1 semana
4
- TABLA 1 (continuación) -Inyecciones intramusculares de acción prolongada, a base de aceite
- Nombre del producto
- Esteroide Dosis Tipo Comp. Fuente Aceite BzBz BzOH EtOH Dosis Dosificación
- TOCOGESTAN
- Enantato de hidroxiprogesterona 200 mg Progestágeno Theramax Dicc. Vidal 1999 Oleato de etilo *40 % 2 ml < 1 semana
- Progesterona
- 50 mg
- -Tocoferol
- 250 mg
- TROPHOBOLE NE
- Estrapronicato 1,3 mg Mixto Theramax Dicc. Vidal 1997 Oliva 45% 1 ml 15 a 30 días
- Undecanoato de nandrolona
- 50 mg
- Heptanoato de hidroxiprogesterona
- 80 mg
- NORISTERAT
- Enantoato de noretisterona 200 mg Anticonceptivo Schering HC Comp. Hoja datos ABPI 1999 Ricino SÍ 1 ml 8 semanas
- TABLA 1 (continuación) -Inyecciones intramusculares de acción prolongada, a base de aceite
- Nombre del producto
- Esteroide Dosis Tipo Comp. Fuente Aceite BzBz BzOH EtOH Dosis Dosificación
- BENZO-GYNOESTRYL PROGESTERO NA -RETARD GRAVIBINAN
- Hexahidrobenzoato de estradiol 5 mg Estradiol Roussel Dicc. Vidal 1998 Cacahuete 1 ml 1 semana
- Caproato de hidroxiprogesterona
- 250 mgml-1 Progestágeno Pharlon Dicc. Vidal 1999 Ricino SÍ 1 ó 2 ml 1 semana
- 17-Valerato de estradiol
- 5 mgml-1 Mixto Shering HC Dicc. Vidal 1995 Ricino SÍ 1 ó 2 ml 1 – 2 semanas
- Caproato de hidroxiprogesterona
- 250 mgml-1
- PARABOLAN
- Trenbolona 76 mg Andrógeno Negma Dicc. Vidal 1997 Cacahuete 75 mg 45 mg 1,5 ml 2 semanas
- TABLA 1 (continuación) -Inyecciones intramusculares de acción prolongada, a base de aceite
- Nombre del producto
- Esteroide Dosis Tipo Comp. Fuente Aceite BzBz BzOH EtOH Dosis Dosificación
- DELESTROGE N
- Valerato de estradiol 20 mgml-1 Estradiol BMS J.Pharm. Sci (1964) 53(8)891 Ricino 78% 20% 2%
- 40 mgml-1
- 58% 40% 2%
- DELALUTIN
- 17-Hidroxiprogesterona 250 mgml-1 Progestágeno DMS J. Pharm. Sci (1964) 53(8)891 Ricino SÍ SÍ Hasta 2%
- BzBz = benzoato de bencilo; BzOH = alcohol bencílico; EtOH = etanol; Dicc. Vidal = Diccionario Vidal Los % son p/v y * aproximado, medido directamente a partir de una única muestra.
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E01900186
23-07-2015
trant en un alcohol. La solubilidad del fulvestrant es también más baja en disolventes no acuosos de tipo éster de lo que es la solubilidad del fulvestrant en aceite de ricino.
Por consiguiente, se presenta como una característica de la invención una formulación farmacéutica que comprende fulvestrant (el fulvestrant está presente, preferiblemente, en una concentración de 3-10 % peso/volumen (p/v), 4-9 % p/v, 4-8 % p/v, 4-7 % p/v, 4-6 % p/v, y, lo más preferiblemente; alrededor de 5 % p/v) en un vehículo de ricinoleato, un disolvente no acuoso de tipo éster farmacéuticamente aceptable, y un alcohol farmacéuticamente aceptable, estando dicha formulación adaptada para administración intramuscular y consiguiendo una concentración terapéuticamente significativa de fulvestrant en plasma sanguíneo durante al menos 2 semanas.
Otra característica de la invención es una formulación farmacéutica que comprende fulvestrant, estando dicha formulación adaptada para inyección intramuscular en un ser humano y que es capaz, tras la inyección, de conseguir una concentración terapéuticamente significativa de fulvestrant en plasma sanguíneo durante al menos 2 semanas.
Características adicionales de la invención incluyen una formulación farmacéutica adaptada para inyección intramuscular que comprende fulvestrant, 30% o menos ,en peso, de un alcohol farmacéuticamente aceptable por volumen de formulación, al menos 1% en peso de un disolvente no acuoso de tipo éster farmacéuticamente aceptable, miscible en un vehículo de ricinoleato, por volumen de formulación, y una cantidad suficiente de un vehículo de ricinoleato para preparar de este modo una formulación que es capaz, tras la inyección, de conseguir una concentración terapéuticamente significativa de fulvestrant en plasma sanguíneo durante al menos 2 semanas.
Otras características adicionales de la invención incluyen una formulación farmacéutica adaptada para inyección intramuscular que comprende fulvestrant; 35% (preferiblemente 30% e idealmente 25%) o menos, en peso, de un alcohol farmacéuticamente aceptable por volumen de formulación, al menos 1% (preferiblemente al menos 5% o idealmente 10%), en peso, de un disolvente no acuoso de tipo éster farmacéuticamente aceptable miscible con un vehículo de ricinoleato por volumen de formulación, y una cantidad suficiente de un vehículo de ricinoleato para preparar de este modo una formulación de al menos 45 mg.ml-1 de fulvestrant.
Para evitar cualquier duda cuando se utiliza el termino % en peso por volumen de formulación para los constituyentes de la formulación, se quiere decir que, dentro de una unidad de volumen de la formulación, estará presente un cierto porcentaje en peso de constituyente, por ejemplo, un 1 % en peso por volumen de formulación contendrá, dentro de un volumen de 100 ml de formulación, 1g del constituyente. Para ilustración adicional:
- % en peso de x por volumen de formulación
- Peso de x en un 1 ml de formulación
- 30 % 20 % 10 % 5 % 1 %
- 300 mg 200 mg 100 mg 50 mg 10 mg
Las formulaciones farmacéuticas preferidas usadas en la invención son, según se ha descrito anteriormente en esta memoria:
- 1.
- El volumen total de la formulación es 6 ml ó menos, y la concentración de fulvestrant es al menos 45 mg.ml-1 .
- 2.
- La cantidad total de fulvestrant en la formulación es 250 mg, o más, y el volumen total de la formulación es 6 ml, o menos.
- 3.
- La cantidad total de fulvestrant en la formulación es 250 mg, y el volumen total de la formulación es 5-5,25 ml.
Se aprecia que, en la formulación, se puede incluir un exceso de formulación para permitir que el medico practicante
o cuidador sea capaz de suministrar la dosis requerida. Por tanto, cuando se requiera una dosis de 5 ml, se apreciará que también esté presente en la formulación un exceso de hasta 0,25 ml, preferiblemente hasta 0,15 ml. Típicamente, la formulación estará presente en un vial o jeringa precargada, preferiblemente una jeringa precargada, que contiene una dosis unitaria de la formulación como se describe en la presente memoria, siendo éstas características adicionales de la invención.
Las concentraciones preferidas de un alcohol farmacéuticamente aceptable, presente en cualquiera de las formula
9
E01900186
23-07-2015
TABLA 3 Efecto del benzoato de bencilo sobre la solubilidad del fulvestrant en aceite de ricino a 25ºC
- % p/v
- Etanol 5
- 5 10 10 10 10 15 15
- (96 %)
- Alcohol 5
- 5 5 5 10 10 15 15
- bencílico
- Benzoato de bencilo
- 15 15 15 15
- Aceite de hasta 100
- hasta 100 hasta 100 hasta 100 hasta 100 hasta 100 hasta 100 hasta 100
- ricino
- Solubilidad del fulves27
- 36 46 54 45 65 76 102
- trant [mg.ml-1]
La Tabla 4 que figura a continuación muestra la solubilidad del fulvestrant en una serie de formulaciones de base oleosa que contienen las mismas cantidades de alcohol y de benzoato de bencilo, pero en las que se ha cambiado el aceite. Los datos muestran también la solubilidad del fulvestrant después de eliminar los alcoholes.
TABLA 4
- Comparaciones de la solubilidad del fulvestrant en formulaciones de base oleosa, con o sin alcoholes
- Solubilidad del fulvestrant mg.ml-1 a 25° C.
- Formulación(a)
- Vehículo completo Vehículo menos alcoholes
- A base de aceite de ricino
- 81,2 12,6
- A base de Miglyol 812-N
- 86,8 1,7
- A base de aceite de semilla de sésamo/aceite de ricino (1:1)
- 70,1 4,4
- A base de aceite de semilla de sésamo
- 45,7 0,7
- A base de aceite de cacahuete
- 40,2 <0,2
(a) Vehículo completo: Las formulaciones comprendían etanol [96 %] (10 %), alcohol bencílico (10 %) y benzoato de
bencilo (15 %) y se completaron hasta el volumen previsto con el aceite establecido. Se añadió fulvestrant en exceso 10 a cada mezcla de disolventes, y se determinó la solubilidad.
12
E01900186
23-07-2015
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15
Claims (1)
-
imagen1 imagen2
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0000313.7A GB0000313D0 (en) | 2000-01-10 | 2000-01-10 | Formulation |
| GB0000313 | 2000-01-10 | ||
| GBGB0008837.7A GB0008837D0 (en) | 2000-01-10 | 2000-04-12 | Formulation |
| GB0008837 | 2000-04-12 | ||
| PCT/GB2001/000049 WO2001051056A1 (en) | 2000-01-10 | 2001-01-08 | Fulvestrant formulation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2248272T3 ES2248272T3 (es) | 2006-03-16 |
| ES2248272T5 true ES2248272T5 (es) | 2015-08-19 |
Family
ID=26243352
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10180667.7T Expired - Lifetime ES2543384T3 (es) | 2000-01-10 | 2001-01-08 | Formulación de fulvestrant |
| ES01900186.6T Expired - Lifetime ES2248272T5 (es) | 2000-01-10 | 2001-01-08 | Formulación de fulvestrant |
| ES200100057A Expired - Fee Related ES2186517B2 (es) | 2000-01-10 | 2001-01-10 | Formulacion farmaceutica que contiene fulvestrant. |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10180667.7T Expired - Lifetime ES2543384T3 (es) | 2000-01-10 | 2001-01-08 | Formulación de fulvestrant |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES200100057A Expired - Fee Related ES2186517B2 (es) | 2000-01-10 | 2001-01-10 | Formulacion farmaceutica que contiene fulvestrant. |
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| GB817241A (en) | 1957-08-21 | 1959-07-29 | Vismara Francesco Spa | Oily solutions for parenteral administration containing adreno-cortical hormones |
| FR6241E (fr) | 1905-04-19 | 1906-10-10 | Ktiengesellschaft | Système de refroidissement du piston des moteurs à explosions et des compresseurs |
| DE947335C (de) | 1954-10-19 | 1956-08-16 | Schering Ag | Verfahren zur Herstellung stabiler oeliger Loesungen von Oestron |
| US2983649A (en) | 1957-10-15 | 1961-05-09 | Francesco Vismara Societa Per | Ricinoleic acid ester solutions of adreno-cortical hormones |
| GB1060632A (en) * | 1962-09-11 | 1967-03-08 | Olin Mathieson | Steroid compositions |
| US3164520A (en) † | 1962-10-29 | 1965-01-05 | Olin Mathieson | Injectable steroid compositions containing at least 75% benzyl benzoate |
| JPS4327327Y1 (es) | 1965-01-07 | 1968-11-12 | ||
| NL151903B (nl) | 1965-03-24 | 1977-01-17 | Schering Ag | Werkwijze ter bereiding van een injectievloeistof door een steroid op te lossen in een mengsel van ricinusolie en benzylbenzoaat. |
| USRE28690E (en) * | 1965-05-05 | 1976-01-20 | Schering Aktiengesellschaft | 17α-Ethinyl-18-methyl-19-nortestosterone esters |
| GB1207571A (en) * | 1967-01-13 | 1970-10-07 | Takeda Chemical Industries Ltd | Injectable composition |
| SU549118A1 (ru) | 1973-04-02 | 1977-03-05 | Способ синхронизации половой охоты у циклирующих свиноматок | |
| SU676284A1 (ru) | 1975-06-26 | 1979-07-30 | Научно-Исследовательский Институт Животноводства | Способ синхронизации половой охоты у самок домашних животных |
| DE2548413A1 (de) | 1975-10-27 | 1977-04-28 | Schering Ag | Depotpraeparate in oeliger ungesaettigter loesung zur intramuskulaeren injektion |
| US4048310A (en) | 1976-02-24 | 1977-09-13 | E. R. Squibb & Sons, Inc. | Topical steroid formulation in form of lotion or cream |
| US4048309A (en) | 1976-02-24 | 1977-09-13 | E. R. Squibb & Sons, Inc. | Topical steroid ointment formulations |
| NL7711916A (nl) | 1977-10-29 | 1979-05-02 | Akzo Nv | Werkwijze ter bereiding van sterk geconcen- treerde farmaceutische preparaten van steroiden. |
| DE2907460A1 (de) * | 1978-03-07 | 1979-09-13 | Sandoz Ag | Neue resorbierbare galenische kompositionen |
| GB8327256D0 (en) | 1983-10-12 | 1983-11-16 | Ici Plc | Steroid derivatives |
| DE3708942A1 (de) | 1987-03-18 | 1988-09-29 | Schering Ag | 19,11ss-ueberbrueckte steroide, deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3733478A1 (de) | 1987-10-01 | 1989-04-13 | Schering Ag | Antigestagen- und antioestrogenwirksame verbindungen zur geburtseinleitung und zum schwangerschaftsabbruch sowie zur behandlung gynaekologischer stoerungen und hormonabhaengiger tumore |
| EP0310542B1 (de) † | 1987-10-01 | 1994-06-08 | Schering Aktiengesellschaft | Antigestagen- und antiöstrogenwirksame Verbindungen zur Behandlung hormonabhängiger Tumoren |
| GB8813353D0 (en) * | 1988-06-06 | 1988-07-13 | Ici Plc | Therapeutic product |
| JPH04327327A (ja) | 1991-04-25 | 1992-11-16 | Toyoda Gosei Co Ltd | スリーブとホースの加締め用ダイス |
| CN1102095A (zh) | 1993-10-30 | 1995-05-03 | 浙江医科大学 | 长效雄激素类制剂——十一酸睾丸注射液 |
| IL111991A (en) | 1994-01-28 | 2000-07-26 | Abbott Lab | Liquid pharmaceutical composition of HIV protease inhibitors in organic solvent |
| ZA9510926B (en) * | 1994-12-23 | 1996-07-03 | Schering Ag | Compounds with progesterone-antagonistic and antiestrogenic action to be used together for female contraception |
| DE19510861A1 (de) | 1995-03-16 | 1996-09-19 | Schering Ag | Einmonatsspritze als Depot-Kontrazeptivum und für die Hormonersatztherapie für peri- und praemenopausale Frauen |
| US20010006963A1 (en) | 1995-03-16 | 2001-07-05 | Ursula Lachnit-Fixson | Once-a-month injection as a depot contraceptive and for hormone replacement therapy for perimenopausal and premenopausal women |
| EP0760237A1 (en) | 1995-08-30 | 1997-03-05 | Cipla Limited | Oil-in-water microemulsions |
| GB9525194D0 (en) * | 1995-12-12 | 1996-02-07 | Zeneca Ltd | Pharmaceutical composition |
| JPH09208496A (ja) * | 1996-01-30 | 1997-08-12 | Takeda Chem Ind Ltd | Ｌｈ−ｒｈ拮抗物質含有組成物 |
| DE19613972A1 (de) | 1996-04-09 | 1997-10-16 | Bayer Ag | Injektionsformulierungen von Avermectinen und Milbemycinen auf Basis von Rizinusöl |
| GB9608719D0 (en) | 1996-04-26 | 1996-07-03 | Scherer Ltd R P | Pharmaceutical compositions |
| KR980008226A (ko) | 1996-07-05 | 1998-04-30 | 다케다 쿠니오 | 시각기능장애의 예방 및 치료제 |
| JPH10203982A (ja) * | 1996-07-05 | 1998-08-04 | Takeda Chem Ind Ltd | 視機能障害の予防・治療剤 |
| DE19635525A1 (de) * | 1996-08-20 | 1998-02-26 | Schering Ag | 7alpha-(xi-Aminoalkyl)-estratriene, Verfahren zu deren Herstellung, pharmazeutische Präparate, die diese 7alpha(xi-Aminoalkyl-estratriene enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln |
| DE19638045A1 (de) | 1996-09-18 | 1998-03-19 | Bayer Ag | Injektionsformulierungen von Avermectinen und Milbemycinen |
| JPH10152438A (ja) * | 1996-11-22 | 1998-06-09 | Takeda Chem Ind Ltd | １−アザキサントン誘導体またはその塩の安定化方法および１−アザキサントン誘導体含有組成物 |
| US6191107B1 (en) | 1997-09-26 | 2001-02-20 | Takeda Chemical Industries, Ltd. | Complex of human growth hormone and zinc |
| JPH11158200A (ja) * | 1997-09-26 | 1999-06-15 | Takeda Chem Ind Ltd | ヒト成長ホルモン・亜鉛複合体及びその用途 |
| ME00855B (me) | 1997-12-03 | 2008-08-07 | Merck & Co Inc | Injektibilne formulacije dugog dejstva koje sadrže hidrogenisano ricinusovo ulje |
| WO2000059473A1 (en) | 1999-04-01 | 2000-10-12 | Inex Pharmaceuticals Corp. | Compositions and methods for treating lymphoma |
| GB0000313D0 (en) | 2000-01-10 | 2000-03-01 | Astrazeneca Uk Ltd | Formulation |
| JP4327327B2 (ja) | 2000-04-03 | 2009-09-09 | ロボテック株式会社 | 固定スプレー揺動装置 |
| HUP0400115A3 (en) | 2001-07-07 | 2005-11-28 | Astrazeneca Ab | Pharmaceutical composition for the intramuscular administration of fulvestrant |
| GB0912999D0 (en) | 2009-07-27 | 2009-09-02 | Astrazeneca Ab | Method-803 |
-
2000
- 2000-01-10 GB GBGB0000313.7A patent/GB0000313D0/en not_active Ceased
- 2000-04-12 GB GBGB0008837.7A patent/GB0008837D0/en not_active Ceased
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2001
- 2001-01-08 HK HK03101532.0A patent/HK1049286B/en not_active IP Right Cessation
- 2001-01-08 HU HU0204137A patent/HU230162B1/hu not_active IP Right Cessation
- 2001-01-08 IL IL15023001A patent/IL150230A0/xx active IP Right Grant
- 2001-01-08 CN CNB018035469A patent/CN1222292C/zh not_active Ceased
- 2001-01-08 US US10/169,777 patent/US20030125387A1/en not_active Abandoned
- 2001-01-08 WO PCT/GB2001/000049 patent/WO2001051056A1/en not_active Ceased
- 2001-01-08 PT PT101806677T patent/PT2266573E/pt unknown
- 2001-01-08 DK DK10180667.7T patent/DK2266573T3/en active
- 2001-01-08 EP EP10180661.0A patent/EP2286818B1/en not_active Expired - Lifetime
- 2001-01-08 BR BRPI0107445-8A patent/BR0107445B1/pt active IP Right Grant
- 2001-01-08 DK DK01900186.6T patent/DK1250138T4/en active
- 2001-01-08 EP EP10180667.7A patent/EP2266573B1/en not_active Expired - Lifetime
- 2001-01-08 AT AT01900186T patent/ATE306928T1/de active
- 2001-01-08 EP EP05016921A patent/EP1669073A3/en not_active Withdrawn
- 2001-01-08 MX MXPA02006698A patent/MXPA02006698A/es active IP Right Grant
- 2001-01-08 CZ CZ2002-2384A patent/CZ304689B6/cs not_active IP Right Cessation
- 2001-01-08 SK SK984-2002A patent/SK287221B6/sk not_active IP Right Cessation
- 2001-01-08 PL PL356030A patent/PL202525B1/pl unknown
- 2001-01-08 HK HK03105241.3A patent/HK1052884B/zh not_active IP Right Cessation
- 2001-01-08 ES ES10180667.7T patent/ES2543384T3/es not_active Expired - Lifetime
- 2001-01-08 ES ES01900186.6T patent/ES2248272T5/es not_active Expired - Lifetime
- 2001-01-08 EG EG20010017A patent/EG24074A/xx active
- 2001-01-08 KR KR1020027008855A patent/KR100802366B1/ko not_active Expired - Lifetime
- 2001-01-08 RU RU2002121507A patent/RU2263507C9/ru active
- 2001-01-08 JP JP2001551480A patent/JP3713237B2/ja not_active Expired - Lifetime
- 2001-01-08 EE EEP200200387A patent/EE05421B1/xx unknown
- 2001-01-08 SI SI200131044T patent/SI2266573T1/sl unknown
- 2001-01-08 CA CA002351004A patent/CA2351004C/en not_active Expired - Fee Related
- 2001-01-08 DE DE60114145.8T patent/DE60114145T3/de not_active Expired - Lifetime
- 2001-01-08 SI SI200130446T patent/SI1250138T2/sl unknown
- 2001-01-08 AU AU23863/01A patent/AU762080B2/en not_active Expired
- 2001-01-08 EP EP01900186.6A patent/EP1250138B2/en not_active Expired - Lifetime
- 2001-01-08 GB GB0100407A patent/GB2359254B/en not_active Expired - Lifetime
- 2001-01-09 BE BE2001/0021A patent/BE1013477A3/fr not_active IP Right Cessation
- 2001-01-09 US US09/756,291 patent/US6774122B2/en not_active Expired - Lifetime
- 2001-01-09 IT IT000005A patent/ITTO20010005A1/it unknown
- 2001-01-09 PT PT102548A patent/PT102548A/pt not_active Application Discontinuation
- 2001-01-10 IT IT2001TO000008A patent/ITTO20010008A1/it unknown
- 2001-01-10 TW TW090100514A patent/TWI259086B/zh not_active IP Right Cessation
- 2001-01-10 MY MYPI20010107A patent/MY118583A/en unknown
- 2001-01-10 ES ES200100057A patent/ES2186517B2/es not_active Expired - Fee Related
- 2001-01-10 AR ARP010100100A patent/AR027510A1/es not_active Application Discontinuation
- 2001-01-10 NL NL1017075A patent/NL1017075C2/nl not_active IP Right Cessation
- 2001-01-10 DE DE10100779A patent/DE10100779A1/de not_active Ceased
- 2001-01-10 CH CH00029/01A patent/CH696260A5/de not_active IP Right Cessation
- 2001-01-10 FR FR0100248A patent/FR2803516B1/fr not_active Expired - Lifetime
- 2001-01-10 CO CO01001317A patent/CO5280206A1/es not_active Application Discontinuation
- 2001-08-01 UA UA2002086628A patent/UA75879C2/uk unknown
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2002
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- 2002-06-13 IL IL150230A patent/IL150230A/en unknown
- 2002-06-18 BG BG106833A patent/BG65776B1/bg unknown
- 2002-07-03 IS IS6454A patent/IS2932B/is unknown
- 2002-07-03 NO NO20023227A patent/NO336286B1/no not_active IP Right Cessation
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2003
- 2003-10-23 JP JP2003362875A patent/JP2004107353A/ja not_active Ceased
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2004
- 2004-06-22 US US10/872,784 patent/US7456160B2/en not_active Expired - Lifetime
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2008
- 2008-10-15 US US12/285,887 patent/US8329680B2/en not_active Expired - Fee Related
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2011
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2012
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2015
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- 2015-07-22 CY CY20151100648T patent/CY1116520T1/el unknown
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