HRP20100111T1 - Nova formulacija doze - Google Patents
Nova formulacija doze Download PDFInfo
- Publication number
- HRP20100111T1 HRP20100111T1 HR20100111T HRP20100111T HRP20100111T1 HR P20100111 T1 HRP20100111 T1 HR P20100111T1 HR 20100111 T HR20100111 T HR 20100111T HR P20100111 T HRP20100111 T HR P20100111T HR P20100111 T1 HRP20100111 T1 HR P20100111T1
- Authority
- HR
- Croatia
- Prior art keywords
- lower alkyl
- tablet composition
- hydrogen
- composition according
- pharmaceutical tablet
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract 10
- 238000009472 formulation Methods 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims abstract 20
- 239000007916 tablet composition Substances 0.000 claims abstract 17
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 12
- 239000001257 hydrogen Substances 0.000 claims abstract 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract 8
- 150000002431 hydrogen Chemical class 0.000 claims abstract 8
- 229920001983 poloxamer Polymers 0.000 claims abstract 7
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims abstract 6
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 6
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 6
- 229910052736 halogen Inorganic materials 0.000 claims abstract 6
- 150000002367 halogens Chemical class 0.000 claims abstract 6
- 238000002360 preparation method Methods 0.000 claims abstract 6
- 125000001424 substituent group Chemical group 0.000 claims abstract 6
- 239000011593 sulfur Chemical group 0.000 claims abstract 6
- 229910052717 sulfur Chemical group 0.000 claims abstract 6
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical compound O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 claims abstract 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract 4
- -1 cyclic tertiary amine Chemical class 0.000 claims abstract 4
- 125000005842 heteroatom Chemical group 0.000 claims abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 4
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 4
- 239000001301 oxygen Substances 0.000 claims abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 4
- 238000000034 method Methods 0.000 claims abstract 3
- 238000002156 mixing Methods 0.000 claims abstract 3
- 239000008213 purified water Substances 0.000 claims abstract 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims abstract 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 2
- 239000002253 acid Substances 0.000 claims abstract 2
- 239000008186 active pharmaceutical agent Substances 0.000 claims abstract 2
- 125000002947 alkylene group Chemical group 0.000 claims abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 230000008878 coupling Effects 0.000 claims abstract 2
- 238000010168 coupling process Methods 0.000 claims abstract 2
- 238000005859 coupling reaction Methods 0.000 claims abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 2
- 239000007888 film coating Substances 0.000 claims abstract 2
- 238000009501 film coating Methods 0.000 claims abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 2
- 238000009474 hot melt extrusion Methods 0.000 claims abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 2
- 239000004615 ingredient Substances 0.000 claims abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims abstract 2
- 150000003462 sulfoxides Chemical class 0.000 claims abstract 2
- 229920002261 Corn starch Polymers 0.000 claims 3
- 239000006057 Non-nutritive feed additive Substances 0.000 claims 3
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 3
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 3
- 239000008120 corn starch Substances 0.000 claims 3
- 239000000945 filler Substances 0.000 claims 3
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 3
- 239000000463 material Substances 0.000 claims 3
- 229960000502 poloxamer Drugs 0.000 claims 3
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- GOOHAUXETOMSMM-UHFFFAOYSA-N Propylene oxide Chemical compound CC1CO1 GOOHAUXETOMSMM-UHFFFAOYSA-N 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 2
- 235000019359 magnesium stearate Nutrition 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 229910002019 Aerosil® 380 Inorganic materials 0.000 claims 1
- 229920003084 Avicel® PH-102 Polymers 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 235000019888 Vivapur Nutrition 0.000 claims 1
- 229920001400 block copolymer Polymers 0.000 claims 1
- 229940047889 isobutyramide Drugs 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 239000002245 particle Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 238000007873 sieving Methods 0.000 claims 1
- 150000005846 sugar alcohols Chemical class 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Psychiatry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Proces za pripremu farmaceutskog tabletnog sastava, naznačen time, da aktivni farmaceutski sastojak ima formulu Igdje jeR niži alkil, niži alkoksi, halogen ili trifluorometilR1 je halogen ili vodik; i kada je p 1, R1 se može pored gornjih supstituenata također uzeti s R za tvorbu -CH=CH-CH=CH-;R2 i R2 su svaki neovisno vodik, halogen, trifluorometil, niži alkoksi ili cijano; i kada je n 1, R2 i R2 mogu pored gornjih supstituenata tvoriti -CH=CH-CH=CH-, nesupstituiran ili supstituiran s jednim ili dva supstituenta izabranih od nižeg alkila ili nižeg alkoksi; R3 i R3 su vodik, niži alkil ili uzeti zajedno s pričvršćenim ugljikovim atomom tvore cikloalkilnu skupinu; R4 je vodik, -N(R5)(CH2)nOH, -N(R5)S(O)2-niži alkil, -N(R5)S(O)2fenil, -N=CH-N(R5)2, -N(R5)C(O)R5, R5 je vodik, C3-6-cikloalkil, benzil, ili niži alkil; R6 je vodik, hidroksi, niži alkil, -(CH2)nCOO-(R5), -N(R5)CO-niži alkil, hidroksi-niži alkil, -(CH2)nCN, -(CH2)nO(CH2)nOH, -CHO ili heterociklički prsten s 5- ili 6- članova koji sadrži 1 do 4 heteroatoma izabranih iz skupine koja se sastoji od kisika, dušika i sumpora i s jednim od ugljikovih atoma u spomenutom prstenu koji je nesupstituiran ili supstituiran s okso skupinom, gdje je heterociklički prsten izravno spojen ili spojen putem alkilenske skupine na ostatak molekule; je ciklički tercijarni amin koji može sadržavati jedan dodatni heteroatom izabran iz skupine koja se sastoji od kisika, dušika ili sumpora, gdje je bilo koji sumpor prisutan u prstenu tio ili se može oksidirati do sulfoksida ili sumpornog dioksida s kojim je spomenuti ciklički tercijarni amin direktno spojen na ostatak molekule ili je pričvršćen putem spojnice -(CH2)nN(R5)-;X je -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, ili -N(R5)(CH2)m-;n, p, i q su svaki neovisno 1 do 4; m je 1 ili 2; i"Niži alkil" označava ravnu ili razgranatu lančanu alkilnu skupinu koja sadrži od 1 do 7 ugljikovih atoma; ili su njihove farmaceutski prihvatljive soli uz dodatak kiseline i poloksameri topivi u vodi zajedno procesirani ekstruzijom vruće taline prije miješanja s drugim sastojkom i gdje se nakon toga sastav tablete može prevući sa sastavom koji sadrži sustav prevlake s filmom za brzo otpuštanje i pročišćenu vodu. Patent sadrži još 13 patentnih zahtjeva.
Claims (14)
1. Proces za pripremu farmaceutskog tabletnog sastava, naznačen time, da aktivni farmaceutski sastojak ima formulu I
[image]
gdje je
R niži alkil, niži alkoksi, halogen ili trifluorometil
R1 je halogen ili vodik; i kada je p 1, R1 se može pored gornjih supstituenata također uzeti s R za tvorbu -CH=CH-CH=CH-;
R2 i R2 su svaki neovisno vodik, halogen, trifluorometil, niži alkoksi ili cijano;
i kada je n 1, R2 i R2 mogu pored gornjih supstituenata tvoriti -CH=CH-CH=CH-, nesupstituiran ili supstituiran s jednim ili dva supstituenta izabranih od nižeg alkila ili nižeg alkoksi;
R3 i R3 su vodik, niži alkil ili uzeti zajedno s pričvršćenim ugljikovim atomom tvore cikloalkilnu skupinu;
R4 je vodik, -N(R5)(CH2)nOH, -N(R5)S(O)2-niži alkil, -N(R5)S(O)2fenil, -N=CH—N(R5)2, -N(R5)C(O)R5,
[image]
R5 je vodik, C3-6-cikloalkil, benzil, ili niži alkil;
R6 je vodik, hidroksi, niži alkil, -(CH2)nCOO-(R5), -N(R5)CO-niži alkil, hidroksi-niži alkil, -(CH2)nCN, -(CH2)nO(CH2)nOH, -CHO ili heterociklički prsten s 5- ili 6- članova koji sadrži 1 do 4 heteroatoma izabranih iz skupine koja se sastoji od kisika, dušika i sumpora i s jednim od ugljikovih atoma u spomenutom prstenu koji je nesupstituiran ili supstituiran s okso skupinom, gdje je heterociklički prsten izravno spojen ili spojen putem alkilenske skupine na ostatak molekule;
[image]
je ciklički tercijarni amin koji može sadržavati jedan dodatni heteroatom izabran iz skupine koja se sastoji od kisika, dušika ili sumpora, gdje je bilo koji sumpor prisutan u prstenu tio ili se može oksidirati do sulfoksida ili sumpornog dioksida s kojim je spomenuti ciklički tercijarni amin direktno spojen na ostatak molekule ili je pričvršćen putem spojnice -(CH2)nN(R5)-;
X je -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, ili -N(R5)(CH2)m-;
n, p, i q su svaki neovisno 1 do 4;
m je 1 ili 2; i
"Niži alkil" označava ravnu ili razgranatu lančanu alkilnu skupinu koja sadrži od 1 do 7 ugljikovih atoma;
ili su njihove farmaceutski prihvatljive soli uz dodatak kiseline i poloksameri topivi u vodi zajedno procesirani ekstruzijom vruće taline prije miješanja s drugim sastojkom i gdje se nakon toga sastav tablete može prevući sa sastavom koji sadrži sustav prevlake s filmom za brzo otpuštanje i pročišćenu vodu.
2. Proces za pripremu farmaceutskog tabletnog sastava prema zahtjevu 1, naznačen time, da sadrži slijedeće korake
1). pripremu smjese aktivnog farmaceutskog sastava s Poloksamerom topivim u vodi,
2). pripremu vrućih rastaljenih ekstrudata primjenom smjese u prahu iz koraka 1,
3). prolazak ekstrudiranog materijala kroz mašinu za prosijavanje da bi se dobio mljeveni materijal. Može biti potrebno više od jednog koraka prosijavanja da bi se dobio materijal u željenom rasponu veličine čestica,
4). pripremu smjese mljevenog ekstrudata iz koraka 3 u prvom koraku s punjenjem(ima) i sredstvom za rastvaranje,
5). priprema konačne smjese miješanjem smjese iz koraka 4 uz pomoćno sredstvo za procesiranje i glidante,
6). kompresiranje konačne smjese pripremljene u koraku 5 u tablete.
3. Farmaceutski tabletni sastav pripremljen prema zahtjevima 1 ili 2, naznačen time, da sadrži
[image]
4. Farmaceustki tabletni sastav prema zahtjevu 3, naznačen time, da tableta sadrži 400 mg aktivnog sastojka formule I.
5. Farmaceutski tabletni sastav prema zahtjevu 3, naznačen time, da je aktivni sastojak 2-(3,5-bis-trifluorometil-fenil)-N-metil-N-(6-morfolin-4-il-4-o-tolil-piridin-3-il)-izobutiramid.
6. Farmaceutski tabletni sastav prema zahtjevu 3, naznačen time, da je poloksamer topiv u vodi blok kopolimer od etilen oksida (POE) ili propilen oksida (POP).
7. Farmaceutski tabletni sastav prema zahtjevu 6, naznačen time, da je poloksamer topiv u vodi Lutrol F68.
8. Farmaceutski tabletni sastav prema zahtjevu 3, naznačen time, da je punilo smjesa kukuruznog škroba, mikrokristalne celuloze i šećernog alkohola.
9. Farmaceutski tabletni sastav prema zahtjevu 8, naznačen time, da je punilo "pure-Cote" ili "Pure-Bind" ili "Pure-Dent" ili "Pure Gel" ili "Pure-Set" ili "Melojel" ili "Meritena" ili "Payge155" ili "perfectamylD6PH" ili "Purity 21" ili "Purity 826" ili "Tablet White" i "Avicel" ili "Vivapur" ili "Vivacel" ili "Emcocel" i "Parteck M 200".
10. Farmaceutski tabletni sastav prema zahtjevu 3, naznačen time, da je pomoćno sredstvo za procesiranje koloidalni silikonski dioksid.
11. Farmaceustki tabletni sastav prema zahtjevu 10, naznačen time, da je pomoćno sredstvo za procesiranje "Aerosil 380" ili "Cab-O-Sil".
12. Farmaceutski tabletni sastav prema zahtjevu 3, naznačen time, da je sredstvo za rastvaranje "polyplasdone XL".
13. Farmaceutski tabletni sastav prema zahtjevu 3, naznačen time, da je glidant magnezijev stearat.
14. Farmaceutski tabletni sastav prema zahtjevu 3, naznačen time, da sadrži
- 2-(3,5-Bis-trifluorometil-fenil)-N-metil-N-(6-morfolin-4-il-4-o-tolil-piridin-3-il)-izobutiramid klorovodik 400.00 mg
- "Lutrol F68" 133.35 mg
- Mikrokristalna Celuloza (Avicel PH 102) 162.65 mg
- "Parteck 200" (Mannitol) 30.00 mg
- "Polyplasdone XL" 16.00 mg
- Koloidalni Silikonski Dioksid (Aorosil 380) 16.00 mg
- Kukuruzni škrob 30.00 mg
- kukuruzni škrob 30.00 mg
- Magnezijev Stearat 12.00 mg
- "Opadry Yellow" 03K 12429 25.00 mg
- Pročišćena Voda 131.25 ml
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71979305P | 2005-09-23 | 2005-09-23 | |
| PCT/EP2006/066310 WO2007039420A1 (en) | 2005-09-23 | 2006-09-13 | Novel dosage formulation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20100111T1 true HRP20100111T1 (hr) | 2010-04-30 |
Family
ID=37671050
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20100111T HRP20100111T1 (hr) | 2005-09-23 | 2010-03-02 | Nova formulacija doze |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US20070071813A1 (hr) |
| EP (1) | EP1928427B1 (hr) |
| JP (2) | JP5523706B2 (hr) |
| KR (1) | KR20080043852A (hr) |
| CN (2) | CN101267808A (hr) |
| AR (1) | AR056198A1 (hr) |
| AT (1) | ATE453384T1 (hr) |
| AU (1) | AU2006298898B2 (hr) |
| BR (1) | BRPI0616108A2 (hr) |
| CA (1) | CA2623237C (hr) |
| DE (1) | DE602006011485D1 (hr) |
| DK (1) | DK1928427T3 (hr) |
| ES (1) | ES2335922T3 (hr) |
| HK (1) | HK1198914A1 (hr) |
| HR (1) | HRP20100111T1 (hr) |
| IL (1) | IL189929A (hr) |
| MY (1) | MY143784A (hr) |
| NO (1) | NO340473B1 (hr) |
| NZ (1) | NZ566419A (hr) |
| PL (1) | PL1928427T3 (hr) |
| PT (1) | PT1928427E (hr) |
| RU (1) | RU2431473C2 (hr) |
| SI (1) | SI1928427T1 (hr) |
| TW (1) | TWI375572B (hr) |
| WO (1) | WO2007039420A1 (hr) |
| ZA (1) | ZA200802272B (hr) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2395002T1 (sl) | 2005-11-08 | 2014-10-30 | Vertex Pharmaceuticals Incorporated | Farmacevtski sestavek, vsebujoč heterociklični modulator prenašalcev z ATP-vezavno kaseto |
| US7671221B2 (en) | 2005-12-28 | 2010-03-02 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| US7754739B2 (en) | 2007-05-09 | 2010-07-13 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
| JP5497633B2 (ja) | 2007-05-09 | 2014-05-21 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｃｆｔｒのモジュレーター |
| DE102007027067A1 (de) * | 2007-06-12 | 2008-12-18 | Ratiopharm Gmbh | Verfahren zur Herstellung eines Arzneimittels enthaltend Vardenafil Hydrochlorid Trihydrat |
| PL2639223T3 (pl) | 2007-12-07 | 2017-09-29 | Vertex Pharmaceuticals Incorporated | Sposób wytwarzania kwasów cykloalkilokarboksyamido-pirydyno-benzoesowych |
| SI2225230T1 (sl) | 2007-12-07 | 2017-03-31 | Vertex Pharmaceuticals Incorporated | Trdne oblike 3-(6-(1-2,2-difluorobenzo(d)(1,3)dioxol-5-il)ciklopropan- karboksamido)-3-metilpiridin-2-il) benzojske kisline |
| KR20100134557A (ko) * | 2008-01-11 | 2010-12-23 | 씨아이피엘에이 엘티디. | 고체 약제학적 투여 제형 |
| CA2931134C (en) | 2008-02-28 | 2019-07-30 | Vertex Pharmaceuticals Incorporated | Heteroaryl derivatives as cftr modulators |
| JP2013523833A (ja) | 2010-04-07 | 2013-06-17 | バーテックス ファーマシューティカルズ インコーポレイテッド | ３−（６−（１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）シクロプロパンカルボキサミド）−３−メチルピリジン−２−イル）安息香酸の医薬組成物およびその投与 |
| EP2455068A1 (en) * | 2010-11-09 | 2012-05-23 | F. Hoffmann-La Roche AG | Pharmaceutical composition for treating HCV infections |
| JP5917964B2 (ja) * | 2012-03-19 | 2016-05-18 | 富士ゼロックス株式会社 | 錠剤、錠剤の製造方法、錠剤管理装置、錠剤照合装置及びプログラム |
| EP3067349B1 (en) | 2013-11-08 | 2018-02-28 | Kissei Pharmaceutical Co., Ltd. | Carboxymethyl piperidine derivative |
| RU2016122882A (ru) | 2013-11-12 | 2017-12-19 | Вертекс Фармасьютикалз Инкорпорейтед | Способ получения фармацевтических композиций для лечения опосредованных cftr заболеваний |
| TWI649307B (zh) | 2014-05-07 | 2019-02-01 | 日商橘生藥品工業股份有限公司 | Cyclohexylpyridine derivative |
| EP3505163B1 (en) * | 2014-09-08 | 2023-01-18 | University of Central Lancashire | Solid dosage form production |
| RU2691136C2 (ru) | 2014-11-18 | 2019-06-11 | Вертекс Фармасьютикалз Инкорпорейтед | Способ проведения высокопроизводительной тестовой высокоэффективной жидкостной хроматографии |
| CN104586770A (zh) * | 2014-12-30 | 2015-05-06 | 山东博迈康药物研究有限公司 | 一种盐酸帕唑帕尼的热熔挤出制剂及其制备方法 |
| CN111344287B (zh) | 2017-11-14 | 2023-12-19 | 默沙东有限责任公司 | 作为吲哚胺2，3-双加氧酶(ido)抑制剂的新型取代的联芳基化合物 |
| CN108159008B (zh) * | 2018-02-27 | 2021-03-23 | 河北化工医药职业技术学院 | 缬沙坦咀嚼片的制备方法 |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1557420A (en) | 1977-03-10 | 1979-12-12 | Soc D Etudes Prod Chimique | Preparation of isobutyramide derivatives |
| EP0089765A3 (en) | 1982-03-17 | 1984-05-23 | Smith Kline & French Laboratories Limited | Pyridine derivatives |
| JPS60184008A (ja) * | 1984-03-02 | 1985-09-19 | Eisai Co Ltd | テオフイリンまたはアミノフイリン含有組成物 |
| US4745123A (en) | 1986-02-18 | 1988-05-17 | Warner-Lambert Company | Substituted tetrahydro-3-pyridine-carboxylic acid, ester, and amide cholinergic agents |
| GB8607313D0 (en) | 1986-03-25 | 1986-04-30 | Ici Plc | Pharmaceutical compositions |
| GB8607312D0 (en) | 1986-03-25 | 1986-04-30 | Ici Plc | Therapeutic agents |
| CA1339423C (en) | 1988-09-14 | 1997-09-02 | Yuji Ono | Pyridine compounds and pharmaceutical use thereof |
| US4994456A (en) | 1989-03-01 | 1991-02-19 | Nisshin Flour Milling Co., Ltd. | Pyridinecarboxylic acid amide derivatives and pharmaceutical compositions comprising same |
| US4973597A (en) | 1989-06-30 | 1990-11-27 | Eli Lilly And Company | Anticonvulsant agents |
| HU207047B (en) | 1989-11-07 | 1993-03-01 | Richter Gedeon Vegyeszet | Process for producing new pyridine derivatives and pharmaceutical copositions comprising same |
| US5364943A (en) | 1991-11-27 | 1994-11-15 | Pfizer Inc. | Preparation of substituted piperidines |
| GB9021056D0 (en) | 1990-09-27 | 1990-11-07 | Pfizer Ltd | Antiarrhythmic agents |
| GB9214120D0 (en) | 1991-07-25 | 1992-08-12 | Ici Plc | Therapeutic amides |
| US5281420A (en) * | 1992-05-19 | 1994-01-25 | The Procter & Gamble Company | Solid dispersion compositions of tebufelone |
| US5719147A (en) * | 1992-06-29 | 1998-02-17 | Merck & Co., Inc. | Morpholine and thiomorpholine tachykinin receptor antagonists |
| AU4718093A (en) * | 1992-07-31 | 1994-03-03 | Merck Sharp & Dohme Limited | Substituted amines as tachykinin receptor antagonists |
| US5387595A (en) * | 1992-08-26 | 1995-02-07 | Merck & Co., Inc. | Alicyclic compounds as tachykinin receptor antagonists |
| GB9305672D0 (en) | 1993-03-19 | 1993-05-05 | Wyeth John & Brother Ltd | Amide derivatives |
| AU6807994A (en) | 1993-05-28 | 1994-12-20 | Taisho Pharmaceutical Co., Ltd. | Medicinal use of pyridine derivative |
| US5506248A (en) * | 1993-08-02 | 1996-04-09 | Bristol-Myers Squibb Company | Pharmaceutical compositions having good dissolution properties |
| NZ264063A (en) | 1993-08-13 | 1995-11-27 | Nihon Nohyaku Co Ltd | N-(2-phenylpyrid-3-yl)- and n-(4-phenylpyrimidin-5-yl)-n'-phenylurea derivatives and pharmaceutical compositions |
| IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| EP1462450B1 (en) * | 1993-12-29 | 2007-06-13 | MERCK SHARP & DOHME LTD. | Substituted morpholine derivatives and their use as therapeutic agents |
| TW385308B (en) | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| DE69523154T2 (de) | 1994-06-06 | 2002-06-06 | Warner Lambert Co | Tachykinin (nk1) rezeptor antagonisten |
| AU2753195A (en) | 1994-06-24 | 1996-01-19 | Taisho Pharmaceutical Co., Ltd. | Pyridine derivative |
| US5965161A (en) * | 1994-11-04 | 1999-10-12 | Euro-Celtique, S.A. | Extruded multi-particulates |
| US6294537B1 (en) * | 1995-03-17 | 2001-09-25 | Sanofi-Synthelabo | Compounds which are specific antagonists of the human NK3 receptor and their use as medicinal products and diagnostic tools |
| ATE242243T1 (de) | 1995-03-24 | 2003-06-15 | Takeda Chemical Industries Ltd | Zyklische verbindungen, ihre herstellung und ihre verwendung als tachykininrezeptorantagonisten |
| DK0891332T3 (da) | 1996-03-29 | 2004-07-05 | Pfizer | 6-phenylpyridyl-2-aminderivater |
| US5834472A (en) * | 1996-05-24 | 1998-11-10 | Schering Corporation | Antifungal composition with enhanced bioavailability |
| WO1998021185A1 (fr) | 1996-11-08 | 1998-05-22 | Sankyo Company, Limited | Arylurees ou derives d'arylmethylcarbamyle |
| CO4920215A1 (es) | 1997-02-14 | 2000-05-29 | Novartis Ag | Tabletas de oxacarbazepina recubiertas de una pelicula y metodo para la produccion de estas formulaciones |
| US5972938A (en) * | 1997-12-01 | 1999-10-26 | Merck & Co., Inc. | Method for treating or preventing psychoimmunological disorders |
| JPH11189546A (ja) | 1997-12-25 | 1999-07-13 | Saitama Daiichi Seiyaku Kk | 経皮吸収促進剤 |
| JPH11189548A (ja) * | 1997-12-25 | 1999-07-13 | Toshio Sato | 無晶性医薬組成物及びその製造方法 |
| WO2000050398A2 (en) | 1999-02-24 | 2000-08-31 | F. Hoffmann-La Roche Ag | Phenyl- and pyridinyl derivatives as neurokinin 1 antagonists |
| EP1035115B1 (en) * | 1999-02-24 | 2004-09-29 | F. Hoffmann-La Roche Ag | 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists |
| DE60006340T2 (de) | 1999-11-29 | 2004-09-09 | F. Hoffmann-La Roche Ag | 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramid |
| US6303790B1 (en) * | 1999-11-29 | 2001-10-16 | Hoffman-La Roche Inc. | Process for the preparation of pyridine derivatives |
| WO2002089835A2 (en) * | 2001-05-03 | 2002-11-14 | F. Hoffmann-La Roche Ag | Pharmaceutical dosage form of amorphous nelfinavir mesylate |
| KR100810320B1 (ko) | 2005-06-16 | 2008-03-04 | 삼성전자주식회사 | 디지털 방송 재생기가 방송 중에 제공되는 전화번호를이용하여 발신하는 방법 및 그 디지털 방송 시스템 |
-
2006
- 2006-09-13 CN CNA2006800344737A patent/CN101267808A/zh active Pending
- 2006-09-13 AU AU2006298898A patent/AU2006298898B2/en active Active
- 2006-09-13 RU RU2008109823/15A patent/RU2431473C2/ru active
- 2006-09-13 JP JP2008531674A patent/JP5523706B2/ja active Active
- 2006-09-13 MY MYPI20080629A patent/MY143784A/en unknown
- 2006-09-13 PT PT06793473T patent/PT1928427E/pt unknown
- 2006-09-13 KR KR1020087006745A patent/KR20080043852A/ko not_active Application Discontinuation
- 2006-09-13 CA CA2623237A patent/CA2623237C/en active Active
- 2006-09-13 DE DE602006011485T patent/DE602006011485D1/de active Active
- 2006-09-13 ES ES06793473T patent/ES2335922T3/es active Active
- 2006-09-13 NZ NZ566419A patent/NZ566419A/en unknown
- 2006-09-13 BR BRPI0616108-1A patent/BRPI0616108A2/pt not_active Application Discontinuation
- 2006-09-13 EP EP06793473A patent/EP1928427B1/en active Active
- 2006-09-13 SI SI200630551T patent/SI1928427T1/sl unknown
- 2006-09-13 WO PCT/EP2006/066310 patent/WO2007039420A1/en active Application Filing
- 2006-09-13 AT AT06793473T patent/ATE453384T1/de active
- 2006-09-13 DK DK06793473.7T patent/DK1928427T3/da active
- 2006-09-13 PL PL06793473T patent/PL1928427T3/pl unknown
- 2006-09-13 CN CN201410122989.3A patent/CN103893145A/zh active Pending
- 2006-09-20 TW TW095134853A patent/TWI375572B/zh active
- 2006-09-21 AR ARP060104126A patent/AR056198A1/es not_active Application Discontinuation
- 2006-09-21 US US11/524,981 patent/US20070071813A1/en not_active Abandoned
-
2008
- 2008-03-04 IL IL189929A patent/IL189929A/en active IP Right Grant
- 2008-03-10 ZA ZA200802272A patent/ZA200802272B/xx unknown
- 2008-03-13 NO NO20081325A patent/NO340473B1/no unknown
-
2010
- 2010-03-02 HR HR20100111T patent/HRP20100111T1/hr unknown
- 2010-11-29 US US12/954,970 patent/US20110070303A1/en not_active Abandoned
-
2012
- 2012-10-19 JP JP2012231933A patent/JP2013049686A/ja active Pending
-
2013
- 2013-03-07 US US13/787,870 patent/US8852634B2/en active Active
-
2014
- 2014-12-09 HK HK14112383.4A patent/HK1198914A1/xx unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20100111T1 (hr) | Nova formulacija doze | |
| RU2420290C2 (ru) | Твердые, пригодные для орального употребления фармацевтические формы применения, содержащие ривароксабан с модифицированным высвобождением | |
| CA2578438C (en) | Pharmaceutical compositions comprising 4-(4-(3-(4-chloro-3-trifluoromethyl-phenyl)-ureido)-3-fluoro-phenoxy)-pyridine-2-carboxylic acid | |
| TWI415634B (zh) | 固態醫藥組成物 | |
| US9345712B2 (en) | Solid oral compositions of tolvaptan | |
| TW202112376A (zh) | 一種含有布魯頓氏酪胺酸激酶抑制劑的口服固體錠劑及其製備方法 | |
| UA85359C2 (ru) | Таблетка, содержащая гранулированный материал с kmd-3213 | |
| WO2009013237A2 (en) | Stable solid pharmaceutical composition comprising candesartan or pharmaceutically acceptable forms thereof | |
| US20150045400A1 (en) | Ritonavir compositions | |
| CA2547274A1 (en) | Stable desloratadine compositions | |
| EP3620156A1 (en) | Composition having improved water solubility and bioavailability | |
| KR20170054446A (ko) | 약학적 조성물 | |
| US20070004671A1 (en) | Stable desloratadine compositions | |
| WO2024096838A1 (en) | A pharmaceutical composition comprising solid dispersion of empagliflozin | |
| AU2011244932B2 (en) | New pharmaceutical compositions comprising 4-(4-(3-(4-chloro-3-trifluoromethyl-phenyl)-ureido)-3-fluoro-phenoxy)-pyridine-2-carboxylic acid for the treatment of hyper-proliferative disorders | |
| TR201820835A1 (tr) | Deksrabeprazol İçeren Bir Formülasyon. | |
| JP2022113343A (ja) | アキシチニブを有効成分とする医薬錠剤 |