HRP20110863T1 - Oblik produljenog oslobađanja paliperidona - Google Patents
Oblik produljenog oslobađanja paliperidona Download PDFInfo
- Publication number
- HRP20110863T1 HRP20110863T1 HR20110863T HRP20110863T HRP20110863T1 HR P20110863 T1 HRP20110863 T1 HR P20110863T1 HR 20110863 T HR20110863 T HR 20110863T HR P20110863 T HRP20110863 T HR P20110863T HR P20110863 T1 HRP20110863 T1 HR P20110863T1
- Authority
- HR
- Croatia
- Prior art keywords
- tablet
- release
- cellulose
- paliperidone
- polymer
- Prior art date
Links
- PMXMIIMHBWHSKN-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCC(O)C4=NC=3C)=NOC2=C1 PMXMIIMHBWHSKN-UHFFFAOYSA-N 0.000 title claims abstract 11
- 229960001057 paliperidone Drugs 0.000 title claims abstract 11
- 239000000203 mixture Substances 0.000 title claims 8
- 238000013268 sustained release Methods 0.000 title abstract 2
- 239000012730 sustained-release form Substances 0.000 title abstract 2
- 238000009472 formulation Methods 0.000 title 1
- 238000000034 method Methods 0.000 claims abstract 7
- 239000003826 tablet Substances 0.000 claims 20
- 229920000642 polymer Polymers 0.000 claims 12
- -1 poly(ethylene oxide) Polymers 0.000 claims 10
- 238000013265 extended release Methods 0.000 claims 8
- 239000000546 pharmaceutical excipient Substances 0.000 claims 5
- 229940124531 pharmaceutical excipient Drugs 0.000 claims 5
- 239000001856 Ethyl cellulose Substances 0.000 claims 4
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims 4
- 229920001249 ethyl cellulose Polymers 0.000 claims 4
- 235000019325 ethyl cellulose Nutrition 0.000 claims 4
- 239000000314 lubricant Substances 0.000 claims 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 4
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 3
- 229920002678 cellulose Polymers 0.000 claims 3
- 230000001934 delay Effects 0.000 claims 3
- 239000000945 filler Substances 0.000 claims 3
- 239000003002 pH adjusting agent Substances 0.000 claims 3
- 239000007939 sustained release tablet Substances 0.000 claims 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 claims 2
- BAPJBEWLBFYGME-UHFFFAOYSA-N Methyl acrylate Chemical compound COC(=O)C=C BAPJBEWLBFYGME-UHFFFAOYSA-N 0.000 claims 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 2
- 235000021355 Stearic acid Nutrition 0.000 claims 2
- 229920001577 copolymer Polymers 0.000 claims 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 2
- 239000008117 stearic acid Substances 0.000 claims 2
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims 1
- 229920001747 Cellulose diacetate Polymers 0.000 claims 1
- 229920002284 Cellulose triacetate Polymers 0.000 claims 1
- JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 claims 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- NNLVGZFZQQXQNW-ADJNRHBOSA-N [(2r,3r,4s,5r,6s)-4,5-diacetyloxy-3-[(2s,3r,4s,5r,6r)-3,4,5-triacetyloxy-6-(acetyloxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6s)-4,5,6-triacetyloxy-2-(acetyloxymethyl)oxan-3-yl]oxyoxan-2-yl]methyl acetate Chemical compound O([C@@H]1O[C@@H]([C@H]([C@H](OC(C)=O)[C@H]1OC(C)=O)O[C@H]1[C@@H]([C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O1)OC(C)=O)COC(=O)C)[C@@H]1[C@@H](COC(C)=O)O[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]1OC(C)=O NNLVGZFZQQXQNW-ADJNRHBOSA-N 0.000 claims 1
- WNLRTRBMVRJNCN-UHFFFAOYSA-L adipate(2-) Chemical compound [O-]C(=O)CCCCC([O-])=O WNLRTRBMVRJNCN-UHFFFAOYSA-L 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 229920003118 cationic copolymer Polymers 0.000 claims 1
- 239000001913 cellulose Substances 0.000 claims 1
- 229920002301 cellulose acetate Polymers 0.000 claims 1
- 229920003086 cellulose ether Polymers 0.000 claims 1
- 239000011248 coating agent Substances 0.000 claims 1
- 238000000576 coating method Methods 0.000 claims 1
- 239000003086 colorant Substances 0.000 claims 1
- 230000006835 compression Effects 0.000 claims 1
- 238000007906 compression Methods 0.000 claims 1
- 125000004185 ester group Chemical group 0.000 claims 1
- 150000002170 ethers Chemical class 0.000 claims 1
- 239000000796 flavoring agent Substances 0.000 claims 1
- 235000019634 flavors Nutrition 0.000 claims 1
- 150000004676 glycans Chemical class 0.000 claims 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000010981 methylcellulose Nutrition 0.000 claims 1
- 230000007935 neutral effect Effects 0.000 claims 1
- PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 claims 1
- 229920001610 polycaprolactone Polymers 0.000 claims 1
- 229920000728 polyester Polymers 0.000 claims 1
- 229920001282 polysaccharide Polymers 0.000 claims 1
- 239000005017 polysaccharide Substances 0.000 claims 1
- 229920002689 polyvinyl acetate Polymers 0.000 claims 1
- 239000011118 polyvinyl acetate Substances 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 125000001453 quaternary ammonium group Chemical group 0.000 claims 1
- 239000000377 silicon dioxide Substances 0.000 claims 1
- 235000012239 silicon dioxide Nutrition 0.000 claims 1
- 230000008961 swelling Effects 0.000 claims 1
- 239000002552 dosage form Substances 0.000 abstract 1
Classifications
-
- 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
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
-
- 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
-
- 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
- A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
- A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
-
- 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
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
-
- 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
- A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
- A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Tableta paliperidona s produljenim oslobađanjem u obliku uložene tablete koja obuhvaća: (a) uloženu jezgru koja sadrži neobloženi paliperidon i barem jedan polimer koji može odgoditi oslobađanje paliperidona iz uložene jezgre i koji može nabubriti kada se navlaži; i (b) vanjski sloj koji sadrži farmaceutsku pomoćnu tvar koja je u biti netopljiva u vodi, pri čemu vanjski sloj samo djelomično okružuje uloženu jezgru. Patent sadrži još 14 patentnih zahtjeva.
Claims (15)
1. Tableta paliperidona s produljenim oslobađanjem u obliku uložene tablete koja obuhvaća:
(a) uloženu jezgru koja sadrži neobloženi paliperidon i barem jedan polimer koji može odgoditi oslobađanje paliperidona iz uložene jezgre i koji može nabubriti kada se navlaži; i
(b) vanjski sloj koji sadrži farmaceutsku pomoćnu tvar koja je u biti netopljiva u vodi, pri čemu vanjski sloj samo djelomično okružuje uloženu jezgru.
2. Tableta s produljenim oslobađanjem prema zahtjevu 1, gdje se barem jedan polimer za jezgru tablete izabire iz grupe koja obuhvaća polivinilpirolidon, poli(etilen oksid), polisaharide, hidrofilne derivate celuloze, metilcelulozu, etil celulozu, hidroksipropil metilcelulozu, hidroksietil celulozu, hidroksipropil celulozu, hidroksietil metilcelulozu, karboksi metilcelulozu i natrij karboksi metilcelulozu, poželjno se taj barem jedan polimer za jezgru tablete izabire iz grupe koja obuhvaća metil celulozu, etil celulozu, hidroksipropilmetilcelulozu, hidroksietil celulozu, hidroksipropil celulozu, hidroksietil metilcelulozu, karboksi metilcelulozu i natrij karboksi metilcelulozu, poželjnije se taj barem jedan polimer za jezgru tablete izabire iz grupe koja obuhvaća poli(etilen oksid) i hidroksipropil metilcelulozu.
3. Tableta s produljenim oslobađanjem prema zahtjevu 1 ili zahtjevu 2, pri čemu je farmaceutska pomoćna tvar za vanjski sloj, i koja je u biti netopljiva u vodi, farmaceutski prihvatljivi polimer koji je u biti netopljiv u vodi, poželjno se taj farmaceutski prihvatljivi polimer koji je u biti netopljiv u vodi izabire iz grupe koja obuhvaća kationske kopolimere etilakrilata i metilakrilata s kvartarnim amonijevim skupinama, etilakrilat metilmetakrilat kopolimer s neutralnim esterskim skupinama, estere celuloze, etere celuloze i esteretere celuloze, etil celuloze kao što su celuloza acetat, celuloza diacetat, celuloza triacetat i poliesterske polimere, poli(ε-kaprolakton)e, poli(alkilen glikol adipat)e, poli(etilen glikol adipat), poli(propilen glikol adipat) i poli(butilen glikol adipat), polivinil acetat te njihove mješavine i kopolimere.
4. Tableta s produljenim oslobađanjem prema zahtjevu 3, gdje je farmaceutski prihvatljivi polimer, koji je u biti netopljiv u vodi, etil celuloza.
5. Tableta s produljenim oslobađanjem prema bilo kojem od zahtjeva 1 do 3, gdje je uložena jezgra u obliku tablete ili komprimiranog umetka.
6. Tableta s produljenim oslobađanjem prema bilo kojem od zahtjeva 1 do 3, gdje jezgra i/ili vanjski sloj nezavisno dalje sadrže barem jednu drugu farmaceutsku pomoćnu tvar.
7. Tableta s produljenim oslobađanjem prema zahtjevu 6, gdje se ta barem jedna druga farmaceutski pomoćna tvar izabire iz grupe koja obuhvaća farmaceutski prihvatljiva punila, nosače, modifikatore pH, sredstva za kliženje, lubrikante, veziva, boje i arome.
8. Tableta s produljenim oslobađanjem prema bilo kojem od zahtjeva 1 do 7, gdje jezgra sadrži paliperidon u količini od oko 1-3% w/w, punilo oko 2-5% w/w, modifikator pH oko 5-15% w/w, polimer koji regulira oslobađanje oko 5-20% w/w, lubrikant oko 0-1% w/w i sredstvo za kliženje oko 0-1% w/w; a vanjski sloj sadrži polimer koji regulira oslobađanje u količini od oko 50-90% w/w, boju oko 0-1% w/w i lubrikant oko 0-1% w/w.
9. Tableta s produljenim oslobađanjem prema zahtjevu 8, gdje uložena jezgra sadrži paliperidon u količini od oko 1-3% w/w, STARLAC oko 2-5% w/w, magnezijev karbonat USP oko 5-15% w/w, poli(etilen oksid) oko 5-20% w/w, stearinsku kiselinu NF oko 0-1% w/w i silicijev dioksid NF oko 0-1% w/w; a vanjski sloj sadrži etil celulozu u količini od oko 50-90% w/w, žuti željezov oksid NF oko 0-1% w/w i stearinsku kiselinu NF oko 0-1% w/w.
10. Postupak izrade tablete s produljenim oslobađanjem prema bilo kojem od zahtjeva 1 do 9, koji obuhvaća
(1) miješanje paliperidona i barem jednog polimera koji odgađa oslobađanje paliperidona i koji može nabubriti kada se navlaži; i
(2) djelomično pokrivanje smjese iz koraka (1) s vanjskim slojem koji sadrži farmaceutsku pomoćnu tvar koja je u biti netopljiva u vodi, da se dobije tableta s produljenim oslobađanjem u obliku djelomično obložene tablete.
11. Postupak prema zahtjevu 10, gdje se mješavina iz koraka (1) komprimira u umetak ili tabletu prije koraka (2).
12. Postupak prema zahtjevu 10, gdje se mješavina iz koraka (1) komprimira u umetak ili tabletu prije koraka (2); umetak ili tableta se miješa s barem jednim polimerom, koji odgađa oslobađanje paliperidona i koji može nabubriti kada se navlaži, radi formiranja smjese; i smjesa se komprimira u tabletu prije koraka (2).
13. Postupak prema bilo kojem od zahtjeva 10 do 12, gdje se punilo, modifikator pH, sredstvo za kliženje i/ili lubrikant dodaju u koraku (1).
14. Postupak prema zahtjevu 11 ili 12, gdje se umetak ili tableta nastali kompresijom melju prije miješanja s barem jednim polimerom, koji odgađa oslobađanje paliperidona i koji može nabubriti kada se navlaži, radi formiranja smjese koja se komprimira u tabletu prije koraka (2).
15. Postupak prema bilo kojem od zahtjeva 10 do 14, gdje se proizvod iz koraka (2) komprimira da se dobije umetnuta tableta.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US93559707P | 2007-08-21 | 2007-08-21 | |
PCT/US2008/010014 WO2009025859A1 (en) | 2007-08-21 | 2008-08-21 | Paliperidone sustained release formulation |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20110863T1 true HRP20110863T1 (hr) | 2011-12-31 |
Family
ID=39853528
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20110863T HRP20110863T1 (hr) | 2007-08-21 | 2011-11-21 | Oblik produljenog oslobađanja paliperidona |
Country Status (8)
Country | Link |
---|---|
US (1) | US20090087487A1 (hr) |
EP (1) | EP2079446B1 (hr) |
AT (1) | ATE530170T1 (hr) |
ES (1) | ES2374200T3 (hr) |
HR (1) | HRP20110863T1 (hr) |
PL (1) | PL2079446T3 (hr) |
PT (1) | PT2079446E (hr) |
WO (1) | WO2009025859A1 (hr) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP5825786B2 (ja) | 2007-12-19 | 2015-12-02 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap | 長時間作用型注入可能パリペリドンエステルに関連する投薬計画 |
BRPI0906754A2 (pt) * | 2008-02-04 | 2015-07-07 | Torrent Pharmaceuticals Ltd | Formulário de dosage prolongado da libertação de paliperidone |
WO2010009900A1 (en) * | 2008-07-25 | 2010-01-28 | Krka, D.D. Novo Mesto | Paliperidone composition comprising solid matrix particles |
EP2161019A1 (en) * | 2008-09-05 | 2010-03-10 | KRKA, D.D., Novo Mesto | Prolonged release multiparticulate pharmaceutical composition comprising paliperidone |
WO2010089775A2 (en) * | 2009-02-05 | 2010-08-12 | Getz Pharma Research | Improved drug dosage form for controlled delivery of one or more pharmaceutically active agent |
WO2011018246A2 (en) | 2009-08-13 | 2011-02-17 | Synthon B.V. | Controlled release paliperidone composition |
US20110052687A1 (en) * | 2009-08-26 | 2011-03-03 | Glenmark Generics Ltd | Extended release pharmaceutical composition of paliperidone |
US20130129827A1 (en) * | 2009-10-16 | 2013-05-23 | Ranbaxy Laboratories Limited | Extended release pharmaceutical compositions of paliperidone and processes of preparation thereof |
US9271939B2 (en) * | 2010-03-15 | 2016-03-01 | Inventia Healthcare Private Limited | Stabilized prolonged release pharmaceutical composition comprising atypical antipsychotic |
US20120201886A1 (en) * | 2010-07-30 | 2012-08-09 | Micro Labs Limited | Coated Extended Release Pharmaceutical Compositions Containing Paliperidone |
US20130034605A1 (en) * | 2011-08-01 | 2013-02-07 | Micro Labs Limited | Extended release pharmaceutical compositions containing paliperidone |
WO2013038268A1 (en) * | 2011-09-16 | 2013-03-21 | Purdue Pharma L.P. | Tamper resistant immediate release formulations |
CA2847611A1 (en) * | 2011-09-16 | 2013-03-21 | Purdue Pharma L.P. | Tamper resistant pharmaceutical formulations |
WO2014027973A1 (en) | 2012-08-14 | 2014-02-20 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Paliperidone oral solution |
WO2014027974A1 (en) | 2012-08-17 | 2014-02-20 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Orally disintegrating formulation of paliperidone |
GR1008842B (el) | 2015-08-06 | 2016-09-05 | Φαρματεν Ανωνυμος Βιομηχανικη Και Εμπορικη Εταιρεια Φαρμακευτικων Ιατρικων Και Καλλυντικων Προϊοντων | Φαρμακευτικο σκευασμα περιεχον εναν ατυπο αντιψυχωσιμο παραγοντα και μεθοδος για την παρασκευη αυτου |
MA42799A (fr) * | 2015-12-29 | 2018-07-25 | Sanovel Ilac Sanayi Ve Ticaret As | Mini comprimés de palipéridone |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4352811A (en) * | 1981-11-12 | 1982-10-05 | Hoechst-Roussel Pharmaceuticals Inc. | 3-(1-Substituted-4-piperidyl)-1,2-benzisoxazoles |
US4458076A (en) * | 1983-05-31 | 1984-07-03 | Hoechst-Roussel Pharmaceuticals | 3-(4-Piperidinyl)-1,2-benzisothiazoles |
US4804663A (en) * | 1985-03-27 | 1989-02-14 | Janssen Pharmaceutica N.V. | 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles |
US5254556A (en) * | 1988-11-07 | 1993-10-19 | Janssen Pharmaceutica N.V. | 3-piperidinyl-1,2-benzisoxazoles |
US5158952A (en) * | 1988-11-07 | 1992-10-27 | Janssen Pharmaceutica N.V. | 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use |
JP3553951B2 (ja) * | 1993-11-23 | 2004-08-11 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 新規な9−ヒドロキシ−ピリド[1,2−a]ピリミジン−4−オンエーテル誘導体 |
ATE373472T1 (de) * | 2002-07-29 | 2007-10-15 | Alza Corp | Verfahren und dosierformen für die kontrollierte abgabe von paliperidon |
WO2004108067A2 (en) * | 2003-04-03 | 2004-12-16 | Sun Pharmaceutical Industries Limited | Programmed drug delivery system |
EP1776089A2 (en) * | 2003-12-31 | 2007-04-25 | Actavis Group hf | Donepezil formulations |
JP2008509144A (ja) * | 2004-08-04 | 2008-03-27 | アルザ・コーポレーシヨン | 上昇するゼロ次放出パターンを示す持続薬剤放出組成物、そのような組成物を製造する方法 |
US20060189635A1 (en) * | 2005-02-04 | 2006-08-24 | Michelle Kramer | Enhanced efficacy benzisoxazole derivative dosage forms and methods |
US20080034927A1 (en) * | 2006-08-04 | 2008-02-14 | Emerson Electric Co. | Basin wrench |
-
2008
- 2008-08-21 WO PCT/US2008/010014 patent/WO2009025859A1/en active Application Filing
- 2008-08-21 PL PL08795541T patent/PL2079446T3/pl unknown
- 2008-08-21 ES ES08795541T patent/ES2374200T3/es active Active
- 2008-08-21 AT AT08795541T patent/ATE530170T1/de not_active IP Right Cessation
- 2008-08-21 PT PT08795541T patent/PT2079446E/pt unknown
- 2008-08-21 US US12/229,344 patent/US20090087487A1/en not_active Abandoned
- 2008-08-21 EP EP08795541A patent/EP2079446B1/en not_active Not-in-force
-
2011
- 2011-11-21 HR HR20110863T patent/HRP20110863T1/hr unknown
Also Published As
Publication number | Publication date |
---|---|
PL2079446T3 (pl) | 2012-04-30 |
US20090087487A1 (en) | 2009-04-02 |
ES2374200T3 (es) | 2012-02-14 |
ATE530170T1 (de) | 2011-11-15 |
EP2079446A1 (en) | 2009-07-22 |
WO2009025859A1 (en) | 2009-02-26 |
PT2079446E (pt) | 2011-12-23 |
EP2079446B1 (en) | 2011-10-26 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20110863T1 (hr) | Oblik produljenog oslobađanja paliperidona | |
AU2003211146B2 (en) | Controlled release dosage forms | |
AU2003264002B2 (en) | Modified-release tablet of bupropion hydrochloride | |
CN102548544B (zh) | 同时具有速效特性和长效特性的药物组合物 | |
TWI354569B (en) | Coated tablet formulation and method | |
US9028862B2 (en) | Enhanced moisture barrier immediate release film coating systems and substrates coated therewith | |
JPH11508587A (ja) | 難溶性薬物の制御放出製剤 | |
AU2008324466A1 (en) | Sustained release tablets with hydromorphone | |
US20160287541A1 (en) | Modified Release Tranexamic Acid Formulation | |
AU2014237934B2 (en) | Controlled release pharmaceutical dosage forms | |
CN111920956A (zh) | 靶向定位型薄膜包衣预混剂及其制备方法 | |
KR20070000439A (ko) | 벤라팍신 히드로클로라이드의 방출연장형 코팅 미니정제 | |
US8030355B2 (en) | Tablet composition with a prolonged release of tamsulosin | |
CN103800334B (zh) | 甲磺酸伊马替尼的药物组合物及其制备方法 | |
CN104873457A (zh) | 缓释剂型 | |
KR20060060371A (ko) | 선택적 세로토닌 재흡수 억제제의 연장방출 제제 및 그제조방법 | |
WO2010072401A1 (en) | Low dose controlled release tablet | |
WO2013098831A2 (en) | Controlled release formulations of nisoldipine | |
CA2651696A1 (en) | Modified release tablets comprising tramadol | |
JP2011231121A (ja) | アクリル系ポリマーの水性分散液で被膜した放出制御型製剤及びその方法 | |
ZA200509051B (en) | Modified-release tablet of bupropion hydrochloride | |
JP2008024708A (ja) | アクリル系ポリマーの水性分散液で被膜した放出制御型製剤及びその方法 |