HRP20201055T1 - Farmaceutske formulacije nitazoksanida s kontroliranim oslobađanjem - Google Patents
Farmaceutske formulacije nitazoksanida s kontroliranim oslobađanjem Download PDFInfo
- Publication number
- HRP20201055T1 HRP20201055T1 HRP20201055TT HRP20201055T HRP20201055T1 HR P20201055 T1 HRP20201055 T1 HR P20201055T1 HR P20201055T T HRP20201055T T HR P20201055TT HR P20201055 T HRP20201055 T HR P20201055T HR P20201055 T1 HRP20201055 T1 HR P20201055T1
- Authority
- HR
- Croatia
- Prior art keywords
- nitazoxanide
- preparation
- polymorph
- amide
- ester
- Prior art date
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- YQNQNVDNTFHQSW-UHFFFAOYSA-N acetic acid [2-[[(5-nitro-2-thiazolyl)amino]-oxomethyl]phenyl] ester Chemical compound CC(=O)OC1=CC=CC=C1C(=O)NC1=NC=C([N+]([O-])=O)S1 YQNQNVDNTFHQSW-UHFFFAOYSA-N 0.000 title claims 20
- 229960002480 nitazoxanide Drugs 0.000 title claims 20
- 238000013270 controlled release Methods 0.000 title claims 8
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- -1 polymorph Chemical class 0.000 claims 19
- 238000002360 preparation method Methods 0.000 claims 19
- 150000001408 amides Chemical class 0.000 claims 16
- 150000002148 esters Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 16
- 239000010410 layer Substances 0.000 claims 15
- 239000000203 mixture Substances 0.000 claims 10
- 239000011230 binding agent Substances 0.000 claims 7
- 238000009472 formulation Methods 0.000 claims 6
- 229920000642 polymer Polymers 0.000 claims 5
- 239000013543 active substance Substances 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 239000003085 diluting agent Substances 0.000 claims 4
- 239000000945 filler Substances 0.000 claims 4
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 4
- 239000000314 lubricant Substances 0.000 claims 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 4
- 239000007787 solid Substances 0.000 claims 4
- HSHXDCVZWHOWCS-UHFFFAOYSA-N N'-hexadecylthiophene-2-carbohydrazide Chemical compound CCCCCCCCCCCCCCCCNNC(=O)c1cccs1 HSHXDCVZWHOWCS-UHFFFAOYSA-N 0.000 claims 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 3
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- 235000019739 Dicalciumphosphate Nutrition 0.000 claims 2
- 208000005176 Hepatitis C Diseases 0.000 claims 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 2
- 102000014150 Interferons Human genes 0.000 claims 2
- 108010050904 Interferons Proteins 0.000 claims 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 2
- 239000003443 antiviral agent Substances 0.000 claims 2
- 239000001506 calcium phosphate Substances 0.000 claims 2
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims 2
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 claims 2
- 229910000390 dicalcium phosphate Inorganic materials 0.000 claims 2
- 229940038472 dicalcium phosphate Drugs 0.000 claims 2
- 239000008187 granular material Substances 0.000 claims 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 2
- 229940079322 interferon Drugs 0.000 claims 2
- 235000019359 magnesium stearate Nutrition 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 239000000741 silica gel Substances 0.000 claims 2
- 229910002027 silica gel Inorganic materials 0.000 claims 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 229920002261 Corn starch Polymers 0.000 claims 1
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 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
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- FDTZUTSGGSRHQF-UHFFFAOYSA-N Desacetyl-nitazoxanide Chemical compound OC1=CC=CC=C1C(=O)NC1=NC=C([N+]([O-])=O)S1 FDTZUTSGGSRHQF-UHFFFAOYSA-N 0.000 claims 1
- 239000004375 Dextrin Substances 0.000 claims 1
- 229920001353 Dextrin Polymers 0.000 claims 1
- 239000005715 Fructose Substances 0.000 claims 1
- 229930091371 Fructose Natural products 0.000 claims 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical compound N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 claims 1
- 229920002472 Starch Polymers 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims 1
- 238000010521 absorption reaction Methods 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- 235000010216 calcium carbonate Nutrition 0.000 claims 1
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000011247 coating layer Substances 0.000 claims 1
- 239000008120 corn starch Substances 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- 229940096516 dextrates Drugs 0.000 claims 1
- 235000019425 dextrin Nutrition 0.000 claims 1
- 239000008121 dextrose Substances 0.000 claims 1
- 235000019700 dicalcium phosphate Nutrition 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 150000002334 glycols Chemical class 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 239000000832 lactitol Substances 0.000 claims 1
- 235000010448 lactitol Nutrition 0.000 claims 1
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 claims 1
- 229960003451 lactitol Drugs 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 238000002203 pretreatment Methods 0.000 claims 1
- 229960000329 ribavirin Drugs 0.000 claims 1
- HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 239000008107 starch Substances 0.000 claims 1
- 235000019698 starch Nutrition 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 239000000375 suspending agent Substances 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
- 235000012222 talc Nutrition 0.000 claims 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims 1
- 235000019731 tricalcium phosphate Nutrition 0.000 claims 1
- 239000000811 xylitol Substances 0.000 claims 1
- 235000010447 xylitol Nutrition 0.000 claims 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims 1
- 229960002675 xylitol Drugs 0.000 claims 1
Classifications
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/19—Cytokines; Lymphokines; Interferons
- A61K38/21—Interferons [IFN]
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
-
- 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
-
- 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
- A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- 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
- A61K2121/00—Preparations for use in therapy
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Claims (21)
1. Farmaceutski pripravak u obliku čvrste oralne doze koji sadrži:
(a) prvi obrok koji sadrži prvu količinu nitazoksanida ili njegove soli, polimorfa, estera ili amida u formulaciji s kontroliranim oslobađanjem, pri čemu formulacija s kontroliranim oslobađanjem sadrži vezivo koje je polimer male viskoznosti; te
(b) drugi obrok koji sadrži drugu količinu nitazoksanida ili njegove soli, polimorfa, estera ili amida u formulaciji s trenutačnim oslobađanjem, gdje je nitazoksanid ili njegova sol, polimorf, ester ili amid pripravljen tako da je bioraspoloživ bez značajne odgode,
pri čemu omjer prve količine nitazoksanida ili njegove soli, polimorfa, estera ili amida i druge količine nitazoksanida ili njegove soli, polimorfa, estera ili amida jest 2.5:1 do 4:1 w/w.
2. Pripravak iz patentnog zahtjeva 1, naznačeno time da je čvrsta oralna doza u obliku tablete.
3. Pripravak iz patentnog zahtjeva 2, naznačeno time da prvi obrok (a) tvori prvi sloj tablete, a drugi obrok (b) tvori drugi sloj deponiran iznad prvog sloja (a).
4. Pripravak iz patentnog zahtjeva 2, naznačeno time da prvi obrok (a) tvori prvi sloj tablete; drugi obrok (b) tvori drugi sloj koji je deponiran iznad prvog sloja (a) da tvore jezgru tablete koja sadrži prvi sloj i drugi sloj; te (c) vanjski sloj ovojnice koja je deponirana iznad jezgre tablete.
5. Pripravak iz patentnog zahtjeva 1, naznačeno time da je čvrsta oralna doza u obliku kapsule.
6. Pripravak iz patentnog zahtjeva 5, naznačeno time da je prvi obrok (a) u obliku granula s kontroliranim oslobađanjem koje sadrže prvu količinu nitazoksanida ili njegove soli, polimorfa, estera ili amida, te da je drugi obrok (b) u obliku granula s trenutačnim oslobađanjem koje sadrže drugu količinu nitazoksanida ili njegove soli, polimorfa, estera ili amida.
7. Pripravak iz patentnog zahtjeva 1, naznačeno time da prvi obrok dalje sadrži jedan ili više razrjeđivača, dezintegrirajućih sredstava, veziva, sredstava za tvorbu suspenzije, glidanata, lubrikanata, punila ili dodatne ekscipijense.
8. Pripravak iz patentnog zahtjeva 7, naznačeno time da prvi obrok dalje sadrži hidroksipropilcelulozu i hidroksipropilmetilcelulozu kao veziva, dikalcijev fosfat dehidrat kao punilo, koloidni bezvodni silikagel kao glidant, te magnezijev stearat kao lubrikant.
9. Pripravak iz patentnog zahtjeva 1, naznačeno time da drugi obrok dalje sadrži jedan ili više razrjeđivača, dezintegrirajućih sredstava, veziva, sredstava za suspenziju, glidanata, lubrikanata, punila ili dodatne ekscipijense.
10. Pripravak iz patentnog zahtjeva 9, naznačeno time da drugi obrok dalje sadrži hidroksipropilcelulozu i mikrokristalnu celulozu kao veziva, kukuruzni škrob kao razrjeđivač, natrijevu kroskarmelozu kao dezinegrirajuće sredstvo, koloidni bezvodni silikagel kao glidant, te magnezijev stearat kao lubrikant.
11. Pripravak iz patentnog zahtjeva 1, naznačeno time da polimer male viskoznosti jest hidroksipropilmetilceluloza male viskoznosti ili hidroksietilceluloza male viskoznosti.
12. Pripravak iz patentnog zahtjeva 1 u obliku dvoslojne tablete za oralno davanje, koji sadrži:
(a) prvi sloj koji sadrži oko 500 mg nitazoksanida u formulaciji s kontroliranim oslobađanjem, pri čemu formulacija s kontroliranim oslobađanjem sadrži vezivo koje je polimer male viskoznosti; te
(b) drugi sloj koji sadrži oko 175 mg nitazoksanida u formulaciji s trenutačnim oslobađanjem, gdje je nitazoksanid ili njegova sol, polimorf, ester ili amid pripravljen tako da je bioraspoloživ bez značajne odgode, drugi je sloj deponiran iznad prvog sloja i prešan je s prvim slojem da tvori jezgru tablete; te
(c) vanjska ovojnica deponirana iznad jezgre tablete;
pri čemu polimer male viskoznosti jest hidroksipropilmetilceluloza male viskoznosti.
13. Pripravak prema patentnom zahtjevu 1 za upotrebu u liječenju hepatitisa C.
14. Produkt koji sadrži:
(i) prvi pripravak u obliku čvrste oralne doze koji sadrži nitazoksanid ili njegovu sol, polimorf, ester ili amid kao prvu aktivnu tvar, gdje prvi pripravak sadrži (a) prvi obrok koji sadrži prvu količinu nitazoksanida ili njegove soli, polimorfa, estera ili amida u formulaciji s kontroliranim oslobađanjem, pri čemu formulacija s kontroliranim oslobađanjem sadrži vezivo koje je polimer male viskoznosti, te (b) drugi obrok koji sadrži drugu količinu nitazoksanida ili njegove soli, polimorfa, estera ili amida u formulaciji s trenutačnim oslobađanjem, pri čemu je nitazoksanid ili njegova sol, polimorf, ester ili amid pripravljen tako da je bioraspoloživ bez značajne odgode, pri čemu omjer prve količine nitazoksanida ili njegove soli, polimorfa, estera ili amida i druge količine nitazoksanida ili njegove soli, polimorfa, estera ili amida jest 2.5:1 do 4:1 w/w, te
(ii) drugi pripravak koji sadrži terapeutski učinkovitu količinu druge aktivne tvari,
za upotrebu u liječenju hepatitisa C, rečena upotreba obuhvaća prethodni tretman s prvim pripravkom, nakon čega slijedi davanje drugog pripravka.
15. Produkt iz patentnog zahtjeva 14, naznačeno time da druga aktivna tvar jest interferon ili polietilen-glikolski derivat interferona.
16. Produkt iz patentnog zahtjeva 14, naznačeno time da drugi pripravak dalje sadrži treću aktivnu tvar, gdje treća aktivna tvar sadrži jedno ili više protuvirusnih sredstava.
17. Produkt iz patentnog zahtjeva 16, naznačeno time da drugi pripravak dalje sadrži ribavirin kao protuvirusno sredstvo.
18. Pripravak prema patentnom zahtjevu 1 ili 6 za reduciranje jedne ili više nuspojava povezanih s liječenjem nitazoksanidom ili tizoksanidom.
19. Pripravak prema patentnom zahtjevu 1 ili 6 za povećanje bioraspoloživosti nitazoksanida ili njegove soli, polimorfa, estera ili amida.
20. Pripravak prema patentnom zahtjevu 1 ili 6 za povećanje apsorpcije nitazoksanida ili njegove soli, polimorfa, estera ili amida.
21. Pripravak iz patentnog zahtjeva 6, koji dalje sadrži farmaceutski prihvatljiv razrjeđivač ili punilo, koji je preferirano, škrob, laktoza, ksilitol, sorbitol, šećer u prahu, prešani šećer, dekstrati, dekstrin, dekstroza, frukoza, laktitol, manitol, saharoza, talk, mikrokristalna celuloza, kalcijev karbonat, dvobazni ili trobazni kalcijev fosfat, dikalcijev fosfat dehidrat, te kalcijev sulfat.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US20228509P | 2009-02-13 | 2009-02-13 | |
| PCT/US2010/024000 WO2010093854A1 (en) | 2009-02-13 | 2010-02-12 | Controlled release pharmaceutical formulations of nitazoxanide |
| EP10741758.6A EP2395840B1 (en) | 2009-02-13 | 2010-02-12 | Controlled release pharmaceutical formulations of nitazoxanide |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20201055T1 true HRP20201055T1 (hr) | 2020-10-30 |
Family
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| HRP20201055TT HRP20201055T1 (hr) | 2009-02-13 | 2020-07-03 | Farmaceutske formulacije nitazoksanida s kontroliranim oslobađanjem |
Country Status (23)
| Country | Link |
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| US (5) | US8524278B2 (hr) |
| EP (1) | EP2395840B1 (hr) |
| JP (3) | JP5726766B2 (hr) |
| KR (1) | KR101697800B1 (hr) |
| CN (2) | CN107260695A (hr) |
| AU (3) | AU2010213678B2 (hr) |
| BR (1) | BRPI1007945C8 (hr) |
| CA (1) | CA2752233C (hr) |
| CO (1) | CO6501159A2 (hr) |
| CY (1) | CY1123162T1 (hr) |
| DK (1) | DK2395840T3 (hr) |
| EA (1) | EA029018B1 (hr) |
| ES (1) | ES2797493T3 (hr) |
| HR (1) | HRP20201055T1 (hr) |
| HU (1) | HUE049501T2 (hr) |
| IL (1) | IL214624A0 (hr) |
| LT (1) | LT2395840T (hr) |
| MX (1) | MX348282B (hr) |
| PL (1) | PL2395840T3 (hr) |
| PT (1) | PT2395840T (hr) |
| SI (1) | SI2395840T1 (hr) |
| UA (1) | UA107564C2 (hr) |
| WO (1) | WO2010093854A1 (hr) |
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| AP2907A (en) * | 2006-01-09 | 2014-05-31 | Romark Lab Lc | Viral hepatitis treatment |
| SI2395840T1 (sl) * | 2009-02-13 | 2020-08-31 | Romark Laboratories, L.C. | Farmacevtske formulacije nitazoksanida z nadzorovanim sproščanjem |
| BR112014018149B1 (pt) | 2012-01-27 | 2020-09-29 | Siegfried Rhein S.A. De C.V | Composição farmacêutica de nitazoxanida |
| CA2864858A1 (en) * | 2012-02-20 | 2013-08-29 | Lupin Limited | Bilayer tablet of dronedarone |
| KR101639692B1 (ko) * | 2013-12-13 | 2016-07-14 | 제일약품주식회사 | 2 이상의 유효성분을 포함하는 구강 내 속붕해 다중유닛 약제학적 조성물 |
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| US10905680B2 (en) * | 2016-04-11 | 2021-02-02 | Genfit | Methods of treatment for cholestatic and fibrotic diseases |
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| US20200121652A1 (en) * | 2017-06-16 | 2020-04-23 | The Doshisha | Compounds having caspase inhibitory activity, pharmaceutical agent containing said compounds and for treating or preventing corneal endothelial symptoms, disorders, or diseases, and application of said pharmaceutical agent |
| CN108524460B (zh) * | 2018-05-14 | 2021-01-01 | 佛山市南海东方澳龙制药有限公司 | 烯啶虫胺双层片 |
| CN110025621A (zh) * | 2019-03-13 | 2019-07-19 | 中国农业科学院上海兽医研究所(中国动物卫生与流行病学中心上海分中心) | 替唑尼特和硝唑尼特在制备抗炎药物中的应用 |
| CN111012788B (zh) * | 2019-12-12 | 2021-01-15 | 武汉职业技术学院 | 硝唑尼特和替唑尼特在制备抗猪繁殖与呼吸综合征病毒药物中的应用 |
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- 2010-02-12 JP JP2011550246A patent/JP5726766B2/ja active Active
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- 2010-02-12 EP EP10741758.6A patent/EP2395840B1/en active Active
- 2010-02-12 DK DK10741758.6T patent/DK2395840T3/da active
- 2010-02-12 LT LTEP10741758.6T patent/LT2395840T/lt unknown
- 2010-02-12 KR KR1020117020973A patent/KR101697800B1/ko active IP Right Grant
- 2010-02-12 CA CA2752233A patent/CA2752233C/en not_active Expired - Fee Related
- 2010-02-12 CN CN201710263825.6A patent/CN107260695A/zh active Pending
- 2010-02-12 AU AU2010213678A patent/AU2010213678B2/en not_active Ceased
- 2010-02-12 US US12/656,704 patent/US8524278B2/en not_active Expired - Fee Related
- 2010-02-12 PT PT107417586T patent/PT2395840T/pt unknown
- 2010-02-12 MX MX2011008530A patent/MX348282B/es active IP Right Grant
- 2010-02-12 EA EA201190127A patent/EA029018B1/ru not_active IP Right Cessation
- 2010-02-12 CN CN2010800164251A patent/CN102395276A/zh active Pending
- 2010-02-12 WO PCT/US2010/024000 patent/WO2010093854A1/en active Application Filing
- 2010-02-12 BR BRPI1007945A patent/BRPI1007945C8/pt not_active IP Right Cessation
- 2010-02-12 ES ES10741758T patent/ES2797493T3/es active Active
- 2010-12-02 UA UAA201110567A patent/UA107564C2/uk unknown
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- 2011-09-07 CO CO11115308A patent/CO6501159A2/es not_active Application Discontinuation
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- 2015-04-01 JP JP2015075264A patent/JP6117845B2/ja active Active
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- 2016-04-29 US US15/141,921 patent/US9827227B2/en active Active - Reinstated
- 2016-12-09 JP JP2016239374A patent/JP6491174B2/ja active Active
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