NO304406B1 - Preparat med regulert frigivelse og kapsel omfattende dette - Google Patents
Preparat med regulert frigivelse og kapsel omfattende dette Download PDFInfo
- Publication number
- NO304406B1 NO304406B1 NO923128A NO923128A NO304406B1 NO 304406 B1 NO304406 B1 NO 304406B1 NO 923128 A NO923128 A NO 923128A NO 923128 A NO923128 A NO 923128A NO 304406 B1 NO304406 B1 NO 304406B1
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- Prior art keywords
- controlled release
- diltiazem
- preparation according
- cores
- preparation
- Prior art date
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- 239000002775 capsule Substances 0.000 title claims description 4
- 239000003405 delayed action preparation Substances 0.000 title description 3
- 238000013270 controlled release Methods 0.000 claims abstract description 22
- 238000000576 coating method Methods 0.000 claims abstract description 20
- 239000011248 coating agent Substances 0.000 claims abstract description 19
- HSUGRBWQSSZJOP-RTWAWAEBSA-N diltiazem Chemical compound C1=CC(OC)=CC=C1[C@H]1[C@@H](OC(C)=O)C(=O)N(CCN(C)C)C2=CC=CC=C2S1 HSUGRBWQSSZJOP-RTWAWAEBSA-N 0.000 claims abstract description 19
- 229960004166 diltiazem Drugs 0.000 claims abstract description 18
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 8
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 8
- 239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 8
- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 8
- 150000003839 salts Chemical class 0.000 claims abstract description 8
- 239000004014 plasticizer Substances 0.000 claims abstract description 6
- 239000001856 Ethyl cellulose Substances 0.000 claims abstract description 5
- 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 abstract description 5
- 235000019325 ethyl cellulose Nutrition 0.000 claims abstract description 5
- 229920001249 ethyl cellulose Polymers 0.000 claims abstract description 5
- 239000004094 surface-active agent Substances 0.000 claims abstract description 4
- 239000003607 modifier Substances 0.000 claims abstract 2
- 238000002360 preparation method Methods 0.000 claims description 17
- 239000000463 material Substances 0.000 claims description 8
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 6
- 230000001105 regulatory effect Effects 0.000 claims description 4
- PYGXAGIECVVIOZ-UHFFFAOYSA-N Dibutyl decanedioate Chemical compound CCCCOC(=O)CCCCCCCCC(=O)OCCCC PYGXAGIECVVIOZ-UHFFFAOYSA-N 0.000 claims description 3
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 3
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 3
- 229920000053 polysorbate 80 Polymers 0.000 claims description 3
- 229940068968 polysorbate 80 Drugs 0.000 claims description 3
- 239000000377 silicon dioxide Substances 0.000 claims description 3
- 235000000346 sugar Nutrition 0.000 claims description 3
- 150000005846 sugar alcohols Chemical class 0.000 claims description 3
- 229920003176 water-insoluble polymer Polymers 0.000 claims description 2
- 239000000853 adhesive Substances 0.000 claims 1
- 230000001070 adhesive effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 abstract description 6
- 239000003795 chemical substances by application Substances 0.000 abstract description 3
- 239000000126 substance Substances 0.000 description 10
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- 206010002383 Angina Pectoris Diseases 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- 239000011230 binding agent Substances 0.000 description 3
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 2
- 206010020772 Hypertension Diseases 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 2
- 235000010980 cellulose Nutrition 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- FLKPEMZONWLCSK-UHFFFAOYSA-N diethyl phthalate Chemical compound CCOC(=O)C1=CC=CC=C1C(=O)OCC FLKPEMZONWLCSK-UHFFFAOYSA-N 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 239000000975 dye Substances 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 229920000642 polymer Polymers 0.000 description 2
- 229920000136 polysorbate Polymers 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 229920003169 water-soluble polymer Polymers 0.000 description 2
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 1
- FEDJGPQLLNQAIY-UHFFFAOYSA-N 2-[(6-oxo-1h-pyridazin-3-yl)oxy]acetic acid Chemical compound OC(=O)COC=1C=CC(=O)NN=1 FEDJGPQLLNQAIY-UHFFFAOYSA-N 0.000 description 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 1
- XZIIFPSPUDAGJM-UHFFFAOYSA-N 6-chloro-2-n,2-n-diethylpyrimidine-2,4-diamine Chemical compound CCN(CC)C1=NC(N)=CC(Cl)=N1 XZIIFPSPUDAGJM-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- 229940127291 Calcium channel antagonist Drugs 0.000 description 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 description 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 description 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 description 1
- 229920003134 Eudragit® polymer Polymers 0.000 description 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 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 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 description 1
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 1
- 239000004147 Sorbitan trioleate Substances 0.000 description 1
- PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 description 1
- 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 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000012736 aqueous medium Substances 0.000 description 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 description 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000000480 calcium channel blocker Substances 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 229960005316 diltiazem hydrochloride Drugs 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 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 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 238000005453 pelletization Methods 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 229920000193 polymethacrylate Polymers 0.000 description 1
- 229940035044 sorbitan monolaurate Drugs 0.000 description 1
- 235000019337 sorbitan trioleate Nutrition 0.000 description 1
- 229960000391 sorbitan trioleate Drugs 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 238000005563 spheronization Methods 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 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
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K9/501—Inorganic compounds
-
- 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
- A61K9/5015—Organic compounds, e.g. fats, sugars
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Fertilizers (AREA)
- Compounds Of Unknown Constitution (AREA)
Description
Foreliggende oppfinnelse gjelder et preparat for kontrollert frigiving. Nærmere bestemt gjelder den et preparat for kontrollert frigiving som inneholder diltiazem.
Diltiazem er en kalsiumantagonist som har vist seg anvendbar i behandling av kronisk hjertesykdom som angina, og hypertensjon og angina.
EP 322277 beskriver en diltiazem-holdige sfæroid som krever nærvær av et bindemiddel. Bindemidlet er f.eks. polyvinylpyrrolidon, metylhydroksypropylcellulose og fortrinnsvis karboksymetylcellulose. Et preparat er beskrevet i denne publikasjon, omfattende på vektbasis 80% diltiazem, 19% mikrokrystallinsk cellulose og 1% karboksymetylcellulose som bindemiddel .
Et formål med foreliggende oppfinnelse er å tilveie-bringe et diltiazempreparat med kontrollert frigiving egnet for tilførsel én gang daglig, for behandling av hypertensjon og angina.
Foreliggende oppfinnelse angår således et preparat med regulert frigivelse, hvilket preparat er kjennetegnet ved at det omfatter sfæroide kjerner bestående av 60 til 98 vekt% diltiazem eller et farmasøytisk akseptabelt salt derav, mikrokrystallinsk cellulose og, eventuelt, et sukker og/eller en sukkeralkohol og/eller et fargestoff, hvilke kjerner er belagt med et materiale med regulert frigivelse.
Egnede farmasøytisk akseptable diltiazemsalter omfatter farmasøytisk akseptable syreaddisjonssalter. Hydro-kloridsaltet er spesielt foretrukket.
Et farmasøytisk preparat for kontrollert frigiving ifølge foreliggende oppfinnelse er et som gir langsom frigiving av et medikament over et forlenget tidsrom, og som for-lenger varigheten av medikamentets virkning i forhold til det som oppnås ved vanlig tilførsel.
Begrepet "sfæroide" er vanlig brukt innen farmasien og betegner et sfærisk korn med diameter på mellom 0,1 mm og 2,5 mm, helst mellom 0,5 mm og 2 mm.
De sfæroide kjerner for anvendelse ifølge foreliggende oppfinnelse inneholder fortrinnsvis mellom 60% og 85%, spesielt foretrukket mellom 70% og 85% (vekt/vekt) diltiazem eller dets farmasøytisk akseptable salter.
Det kuledannende stoff kan med fordel være ethvert farmasøytisk akseptabelt stoff som kan danne kuler sammen med den aktive bestanddel, slik at sfæroide kjerner dannes. Et foretrukket kuledannende stoff er mikrokrystallinsk cellulose. Den benyttede mikrokrystallinske cellulose kan f.eks. være "Avicel" PH 101 eller "Avicel" PH 102 (FMC Corporation). Dersom det kuledannende stoff er til stede, kan det med fordel foreligge i en mengde på fra 1% til 60%, fortrinnsvis 15% til 40% (vekt/vekt) av de sfæroide kjerner.
Om ønskelig kan de sfæroide kjerner også inneholde andre farmasøytisk akseptable eksipienser og fortynningsmidler som letter kuledannelse, som sukkere (f.eks. sukrose, deks-trose, maltose eller laktose) eller sukkeralkoholer (f.eks. mannitol, xylitol eller sorbitol). Fargestoffer kan også inngå i den sfæroide kjerne.
De sfæroide kjerner er overtrukket med et stoff som tillater frigiving av diltiazem med kontrollert hastighet i et vandig medium. Egnede overtrekksstoffer for kontrollert frigiving omfatter dem vel kjent innen faget, som vannuløse-lige vokser og polymerer som polymetacrylater (f.eks. "Eudragit"-polymerer) eller fortrinnsvis vannuløselige cell-uloser, særlig etylcellulose. Overtrekket kan også omfatte vannløselige polymerer som polyvinylpyrrolidon, eller fortrinnsvis en vannløselig cellulose som hydroksypropylmetyl-cellulose og hydroksypropylcellulose. Det er åpenbart at forholdet mellom vannuløselige og vannløselige stoffer vil avhenge av den påkrevde frigivingshastighet og løseligheten av de valgte stoffer. Forholdet mellom vannløselig polymer og vannuløselig polymer er fortrinnsvis 1:20 til 1:2.
Overtrekket for kontrollert frigiving omfatter fortrinnsvis ett eller flere plastifiseringsmidler vanlig brukt innen faget som diétylftalat, men særlig dibutylsebacat, overflateaktive stoffer som sorbitantrioleat, sorbitanmono-laurat eller, fortrinnsvis, polysorbat 80 ("Tween" 80), og klebeevne-endrende stoffer som talkum, eller fortrinnsvis kolloidal, vannfri kisel.
Når plastifiseringsmiddel foreligger, vil mengden avhenge av det valgte plastifiseringsmiddel. Generelt foreligger plastifiseringsmidlet i en mengde på fra 1% til 25%
(vekt/vekt) av overtrekkshinnen for kontrollert frigiving. Når overflateaktivt stoff er til stede, foreligger det med fordel i en mengde på fra 1% til 25% (vekt/vekt) av overtrekkshinnen for kontrollert frigiving. Det klebeevne-endrende stoff vil når det er til stede, med fordel foreligge i en mengde på fra 1% til 25% (vekt/vekt) av overtrekkshinnen for kontrollert frigiving.
En foretrukket overtrekkshinne for kontrollert frigiving omfatter 50% til 95% etylcellulose, 5% til 15% kolloidal, vannfri kisel, 5% til 15% dibutylsebacat og 5% til 15% polysorbat 80 ("Tween" 80).
Overtrekkshinnen for kontrollert frigiving kan dannes på overflaten av de diltiazemholdige, sfæroide kjerner ved bruk av vanlige overtrekksfremgangsmåter, f.eks. "fluidi-sed bed"- eller panneovertrekking. Overtrekksstoffene kan tilføres som en løsning eller en suspensjon. Egnede løse-middelsystemer omfatter vann, diklormetan, etanol, metanol, isopropylalkohol og aceton, eller blandinger av disse. Over-trekksløsningen eller -suspensjonen inneholder fortrinnsvis fra 2% til 60%, helst fra 2% til 20% (vekt/vekt) av over-trekksstof f er .
Mengden av overtrekksstoff for kontrollert frigiving vil avhenge av den ønskede frigivingshastighet, men ligger generelt i området fra 1% til 25%, fortrinnsvis fra 2% til 8%
(vekt/vekt) av preparatet.
Preparatet for kontrollert frigiving ifølge oppfinnelsen kan fremstilles ved: (a) granulering av en blanding som omfatter diltiazem eller et farmasøytisk akseptabelt salt av dette, vann og, om ønskelig, et kuledannende stoff; (b) ekstrudering av den granulerte blanding slik at et
ekstrudat dannes;
(c) "sfæronisering" av ekstrudatet inntil sfæroide
kjerner dannes;
(d) tørking av de sfæroide kjerner; og
(e) overtrekking av de sfæroide kjerner
Preparater ifølge oppfinnelsen kan fylles i kapsler eller puter, eller sammenpresses til tabletter ved bruk av vanlige farmasøytiske teknikker.
Preparatet ifølge foreliggende oppfinnelse er egnet for tilførsel én gang daglig. For tilførsel én gang daglig inneholder doseringsformen med fordel fra 120 mg til 300 mg diltiazem eller et farmasøytisk akseptabelt salt av dette, fortrinnsvis diltiazem-hydroklorid.
For å lette forståelsen av oppfinnelsen gis de følgende eksempler for å forklare den.
Eksempel 1
Kapsler med følgende sammensetning ble fremstilt Diltiazemholdige, sfæroide kjerner
Overtrekkshinne for kontrollert frigiving
Diltiazem og mikrokrystallinsk cellulose ble blandet ved bruk av en blander med høy forskyvningskraft. Blandingen ble våtgranulert og ekstrudert, og det dannede ekstrudat ble "sfæronisert" og tørket i en "fluid bed" tørkemaskin. Sfær-oidene ble siktet for å oppnå en partikkelstørrelse på 0,85 til 1,7 mm.
Bestanddelene i overtrekkshinnen for kontrollert frigiving ble dispersert i løsemiddelsystemet diklormetan/- metanol og tilført de diltiazemholdige, sfæroide kjerner i en "fluid bed" overtrekksmaskin. De resulterende, overtrukne sfæroider ble siktet. De overtrukne sfæroider ble fylt i gelatinkapselskall.
Oppløsningshastigheten av det resulterende produkt ble målt i et EP-kurvapparat med 100 rpm i EP-fosfatbuffer, pH 4,5. De oppnådde resultater er gitt nedenfor.
Oppløsningshastighet for diltiazem
Claims (9)
1. Preparat med regulert frigivelse,karakterisert vedat det omfatter sfæroide kjerner bestående av 60 til 98 vekt% diltiazem eller et far-masøytisk akseptabelt salt derav, mikrokrystallinsk cellulose og, eventuelt, et sukker og/eller en sukkeralkohol og/eller et fargestoff, hvilke kjerner er belagt med et materiale med regulert frigivelse.
2. Preparat ifølge krav 1,
karakterisert vedat de sfæroide kjerner omfatter mellom 70 og 85 vekt% diltiazem eller et farmasøytisk akseptabelt salt derav.
3. Preparat ifølge hvilket som helst av kravene 1 eller 2,
karakterisert vedat den mikrokrystallinske cellulose er til stede i en mengde på fra 15 til 40 vekt% av de sfæroide kjerner.
4. Preparat ifølge hvilket som helst av kravene 1 til 3,karakterisert vedat belegningsmaterialet med regulert frigivelse omfatter en vannuløselig polymer.
5. Preparat ifølge krav 4,
karakterisert vedat belegningsmaterialet omfatter etylcellulose.
6. Preparat ifølge hvilket som helst av kravene 1 til 5,karakterisert vedat belegningsmaterialet med regulert frigivelse ytterligere omfatter én eller flere myknere, overflateaktive midler og klebemodifiseringsmidler.
7. Preparat ifølge krav 6,
karakterisert vedat belegget med regulert frigivelse omfatter 50% til 95% etylcellulose, 5% til 15% kol-loidalt, vannfritt silika, 5% til 15% dibutylsebakat og 5% til 15% polysorbat 80.
8. Preparat ifølge hvilket som helst av kravene 1 til 7,karakterisert vedat belegningsmaterialet med regulert frigivelse er til stede i en mengde på fra 2 til 8 vekt% av preparatet.
9. Kapsel,
karakterisert vedat den omfatter belagte, sfæroide kjerner med regulert frigivelse ifølge hvilket som helst av kravene 1 til 8.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB919117361A GB9117361D0 (en) | 1991-08-12 | 1991-08-12 | Oral dosage form |
| GB919122967A GB9122967D0 (en) | 1991-10-29 | 1991-10-29 | Pharmaceutical composition |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| NO923128D0 NO923128D0 (no) | 1992-08-11 |
| NO923128L NO923128L (no) | 1993-02-15 |
| NO304406B1 true NO304406B1 (no) | 1998-12-14 |
Family
ID=26299395
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO923128A NO304406B1 (no) | 1991-08-12 | 1992-08-11 | Preparat med regulert frigivelse og kapsel omfattende dette |
Country Status (14)
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|---|---|
| US (2) | US5670172A (no) |
| EP (1) | EP0527637B1 (no) |
| JP (1) | JP3019235B2 (no) |
| KR (1) | KR100221695B1 (no) |
| CN (1) | CN1052398C (no) |
| AT (1) | ATE165513T1 (no) |
| AU (1) | AU651715B2 (no) |
| CA (1) | CA2075356A1 (no) |
| DE (1) | DE69225278D1 (no) |
| ES (1) | ES2115643T3 (no) |
| FI (1) | FI923582A (no) |
| IL (1) | IL102778A (no) |
| NO (1) | NO304406B1 (no) |
| PH (1) | PH31288A (no) |
Families Citing this family (92)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5266331A (en) * | 1991-11-27 | 1993-11-30 | Euroceltique, S.A. | Controlled release oxycodone compositions |
| US5681585A (en) * | 1991-12-24 | 1997-10-28 | Euro-Celtique, S.A. | Stabilized controlled release substrate having a coating derived from an aqueous dispersion of hydrophobic polymer |
| US20080075781A1 (en) * | 1992-11-25 | 2008-03-27 | Purdue Pharma Lp | Controlled release oxycodone compositions |
| FR2702160B1 (fr) * | 1993-03-02 | 1995-06-02 | Biovecteurs As | Vecteurs particulaires synthétiques et procédé de préparation. |
| SE9301220D0 (sv) * | 1993-04-14 | 1993-04-14 | Kabi Pharmacia Ab | Manufacturing matrices |
| US20070275062A1 (en) * | 1993-06-18 | 2007-11-29 | Benjamin Oshlack | Controlled release oxycodone compositions |
| IL110014A (en) * | 1993-07-01 | 1999-11-30 | Euro Celtique Sa | Solid controlled-release oral dosage forms of opioid analgesics |
| US7740881B1 (en) | 1993-07-01 | 2010-06-22 | Purdue Pharma Lp | Method of treating humans with opioid formulations having extended controlled release |
| US5834024A (en) * | 1995-01-05 | 1998-11-10 | Fh Faulding & Co. Limited | Controlled absorption diltiazem pharmaceutical formulation |
| GB9519363D0 (en) | 1995-09-22 | 1995-11-22 | Euro Celtique Sa | Pharmaceutical formulation |
| US5914134A (en) * | 1997-01-27 | 1999-06-22 | Wockhardt Europe Limited | Process for the pulsatile delivery of diltiazem HCL and product produced thereby |
| WO1999012526A1 (en) * | 1997-09-09 | 1999-03-18 | Alza Corporation | Pharmaceutical coating composition and method of use |
| US7060734B1 (en) | 1997-09-09 | 2006-06-13 | Alza Corporation | Pharmaceutical coating composition and method of use |
| US5891845A (en) * | 1997-11-21 | 1999-04-06 | Fuisz Technologies Ltd. | Drug delivery systems utilizing liquid crystal structures |
| PL193273B1 (pl) | 1997-12-22 | 2007-01-31 | Euro Celtique Sa | Postać dawkowania doustnego |
| PL341309A1 (en) * | 1997-12-22 | 2001-04-09 | Euro Celtique | Method of preventing overdosage of opioidic preparations |
| US6524620B2 (en) | 1998-07-20 | 2003-02-25 | Andrx Pharmaceuticals, Inc. | Diltiazem controlled release formulation and method of manufacture |
| US6806294B2 (en) | 1998-10-15 | 2004-10-19 | Euro-Celtique S.A. | Opioid analgesic |
| US6432448B1 (en) | 1999-02-08 | 2002-08-13 | Fmc Corporation | Edible coating composition |
| US6723342B1 (en) | 1999-02-08 | 2004-04-20 | Fmc Corporation | Edible coating composition |
| US6410255B1 (en) * | 1999-05-05 | 2002-06-25 | Aurora Biosciences Corporation | Optical probes and assays |
| PT1178952E (pt) | 1999-05-14 | 2007-12-04 | Univ California | Novos moduladores da interleucina-1 e do factor alfa de necrose tumoral, síntese dos referidos moduladores e métodos de utilização dos referidos moduladores |
| GB9913979D0 (en) | 1999-06-17 | 1999-08-18 | Univ Wales Medicine | Spheroid preparation |
| US10179130B2 (en) | 1999-10-29 | 2019-01-15 | Purdue Pharma L.P. | Controlled release hydrocodone formulations |
| KR101476574B1 (ko) | 1999-10-29 | 2014-12-24 | 유로-셀티크 소시에떼 아노뉨 | 서방성 하이드로코돈 제형 |
| US6500462B1 (en) | 1999-10-29 | 2002-12-31 | Fmc Corporation | Edible MCC/PGA coating composition |
| US7108866B1 (en) | 1999-12-10 | 2006-09-19 | Biovall Laboratories International Srl | Chronotherapeutic diltiazem formulations and the administration thereof |
| US20060153914A1 (en) * | 1999-12-10 | 2006-07-13 | Biovail Laboratories International S.R.L. | Chronotherapeutic diltiazem formulations and the administration thereof |
| CN1423559A (zh) | 2000-02-08 | 2003-06-11 | 欧罗赛铁克股份有限公司 | 包含阿片样激动剂和拮抗剂的控释组合物 |
| EP1259608B1 (en) | 2000-02-23 | 2009-08-12 | Life Technologies Corporation | Modified fluorescent proteins |
| US6852031B1 (en) * | 2000-11-22 | 2005-02-08 | Igt | EZ pay smart card and tickets system |
| US6635277B2 (en) | 2000-04-12 | 2003-10-21 | Wockhardt Limited | Composition for pulsatile delivery of diltiazem and process of manufacture |
| GB0025208D0 (en) * | 2000-10-13 | 2000-11-29 | Euro Celtique Sa | Delayed release pharmaceutical formulations |
| MXPA03003895A (es) | 2000-10-30 | 2003-07-28 | Euro Celtique Sa | Formulaciones de hidrocodona de liberacion controlada. |
| JP4395549B2 (ja) * | 2000-11-16 | 2010-01-13 | ザ レジェンツ オブ ザ ユニヴァースティ オブ カリフォルニア | 薬物及び発酵生成物の発見のための海洋放線菌分類群 |
| IL155959A0 (en) | 2000-11-28 | 2003-12-23 | Fmc Corp | Edible pga (propylene glycol alginate) coating composition |
| US20110104214A1 (en) | 2004-04-15 | 2011-05-05 | Purdue Pharma L.P. | Once-a-day oxycodone formulations |
| UA81224C2 (uk) * | 2001-05-02 | 2007-12-25 | Euro Celtic S A | Дозована форма оксикодону та її застосування |
| DE60238756D1 (de) | 2001-05-11 | 2011-02-10 | Endo Pharmaceuticals Inc | Opioid enthaltende arzneiform gegen missbrauch |
| US7943173B2 (en) | 2001-07-18 | 2011-05-17 | Purdue Pharma L.P. | Pharmaceutical combinations of oxycodone and naloxone |
| US20030044458A1 (en) | 2001-08-06 | 2003-03-06 | Curtis Wright | Oral dosage form comprising a therapeutic agent and an adverse-effect agent |
| WO2003013433A2 (en) | 2001-08-06 | 2003-02-20 | Euro-Celtique S.A. | Sequestered antagonist formulations |
| DE60232417D1 (de) | 2001-08-06 | 2009-07-02 | Euro Celtique Sa | Opioid-agonist-formulierungen mit freisetzbarem und sequestriertem antagonist |
| US20030181488A1 (en) * | 2002-03-07 | 2003-09-25 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Administration form for the oral application of 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester and the salts thereof |
| CA2478523A1 (en) | 2002-04-05 | 2003-10-16 | Euro-Celtique S.A. | Matrix for sustained, invariant and independent release of active compounds |
| US7176232B2 (en) | 2002-06-24 | 2007-02-13 | The Regents Of The University Of California | Salinosporamides and methods for use thereof |
| EP2422772A3 (en) * | 2002-09-20 | 2012-04-18 | Alpharma, Inc. | Sequestering subunit and related compositions and methods |
| US7112581B2 (en) * | 2002-09-27 | 2006-09-26 | Nereus Pharmaceuticals, Inc. | Macrocyclic lactams |
| US20040202717A1 (en) | 2003-04-08 | 2004-10-14 | Mehta Atul M. | Abuse-resistant oral dosage forms and method of use thereof |
| US20040208932A1 (en) * | 2003-04-17 | 2004-10-21 | Ramachandran Thembalath | Stabilized paroxetine hydrochloride formulation |
| TWI347201B (en) | 2003-04-21 | 2011-08-21 | Euro Celtique Sa | Pharmaceutical products,uses thereof and methods for preparing the same |
| US20050049294A1 (en) * | 2003-06-20 | 2005-03-03 | Michael Palladino | Methods of using [3.2.0] heterocyclic compounds and analogs thereof |
| US8217072B2 (en) * | 2003-06-20 | 2012-07-10 | The Regents Of The University Of California | Salinosporamides and methods for use thereof |
| US7727752B2 (en) | 2003-07-29 | 2010-06-01 | Life Technologies Corporation | Kinase and phosphatase assays |
| CA2445420A1 (en) * | 2003-07-29 | 2005-01-29 | Invitrogen Corporation | Kinase and phosphatase assays |
| US7619059B2 (en) * | 2003-07-29 | 2009-11-17 | Life Technologies Corporation | Bimolecular optical probes |
| JP2007505315A (ja) * | 2003-09-12 | 2007-03-08 | インヴィトロジェン コーポレーション | 多重結合および活性アッセイ |
| KR20060132698A (ko) * | 2004-01-23 | 2006-12-21 | 니리어스 파마슈티컬즈, 인코퍼레이션 | 항균제로 유용한 비스-인돌 피롤 |
| US7276530B2 (en) | 2004-04-30 | 2007-10-02 | Nereus Pharmaceuticals, Inc. | [3.2.0] Heterocyclic compounds and methods of using the same |
| US7579371B2 (en) | 2004-04-30 | 2009-08-25 | Nereus Pharmaceuticals, Inc. | Methods of using [3.2.0] heterocyclic compounds and analogs thereof |
| EP1604666A1 (en) | 2004-06-08 | 2005-12-14 | Euro-Celtique S.A. | Opioids for the treatment of the Chronic Obstructive Pulmonary Disease (COPD) |
| EP1827385B1 (en) | 2004-11-23 | 2013-03-27 | Adamas Pharmaceuticals, Inc. | Pharmaceutical composition comprising memantine in an extended dosage release form for use in the treatment of dementias |
| US7619007B2 (en) | 2004-11-23 | 2009-11-17 | Adamas Pharmaceuticals, Inc. | Method and composition for administering an NMDA receptor antagonist to a subject |
| WO2006058236A2 (en) | 2004-11-24 | 2006-06-01 | Neuromolecular Pharmaceuticals, Inc. | Composition comprising an nmda receptor antagonist and levodopa and use thereof for treating neurological disease |
| CN103230394B (zh) * | 2004-12-03 | 2016-04-20 | 达纳-法伯癌症研究公司 | 治疗肿瘤性疾病的化合物及其用途 |
| EP1702558A1 (en) | 2005-02-28 | 2006-09-20 | Euro-Celtique S.A. | Method and device for the assessment of bowel function |
| CA2603031A1 (en) * | 2005-03-31 | 2006-10-05 | Rafael Armament Development Authority Ltd. | Apparatus for treating particles and liquids by ultrasound |
| JP5666087B2 (ja) | 2005-04-06 | 2015-02-12 | アダマス・ファーマシューティカルズ・インコーポレーテッド | Ｃｎｓ関連疾患の治療のための方法及び組成物 |
| WO2007015757A2 (en) | 2005-07-21 | 2007-02-08 | Nereus Pharmaceuticals, Inc. | Interleukin-1 and tumor necrosis factor-a modulators; syntheses of such modulators and methods of using such modulators |
| HUE032156T2 (en) | 2006-06-19 | 2017-09-28 | Alpharma Pharmaceuticals Llc | Pharmaceutical preparations |
| EP2068840A2 (en) * | 2006-07-21 | 2009-06-17 | LAB International SRL | Hydrophobic abuse deterrent delivery system |
| EP1920767A1 (en) * | 2006-11-09 | 2008-05-14 | Abbott GmbH & Co. KG | Melt-processed imatinib dosage form |
| WO2008095195A2 (en) * | 2007-02-02 | 2008-08-07 | Nereus Pharmaceuticals, Inc. | Lyophilized formulations of salinosporamide a |
| US20090017167A1 (en) * | 2007-07-11 | 2009-01-15 | Herbalife International Inc. | Mixture and beverage made therefrom for protecting cellular hydration |
| US8394816B2 (en) * | 2007-12-07 | 2013-03-12 | Irene Ghobrial | Methods of using [3.2.0] heterocyclic compounds and analogs thereof in treating Waldenstrom's Macroglobulinemia |
| AU2008346870A1 (en) * | 2007-12-17 | 2009-07-16 | Alpharma Pharmaceuticals, Llc | Pharmaceutical composition |
| US20100151014A1 (en) * | 2008-12-16 | 2010-06-17 | Alpharma Pharmaceuticals, Llc | Pharmaceutical composition |
| US8623418B2 (en) | 2007-12-17 | 2014-01-07 | Alpharma Pharmaceuticals Llc | Pharmaceutical composition |
| BRPI0821732A2 (pt) * | 2007-12-17 | 2015-06-16 | Labopharm Inc | Formulações de liberação controlada , forma de dosagem sólida, e, uso da formulação de liberação controlada |
| WO2009140287A1 (en) * | 2008-05-12 | 2009-11-19 | Nereus Pharmaceuticals, Inc. | Salinosporamide derivatives as proteasome inhibitors |
| SI2317991T1 (sl) * | 2008-07-07 | 2017-09-29 | Euro-Celtique S.A. | Uporaba opioidnih antagonistov za zdravljenje retencije urina |
| ES2706407T3 (es) | 2009-03-10 | 2019-03-28 | Euro Celtique Sa | Composiciones farmacéuticas de liberación inmediata que comprenden oxicodona y naloxona |
| CA2782556C (en) | 2009-12-02 | 2018-03-27 | Adamas Pharmaceuticals, Inc. | Amantadine compositions and methods of use |
| CA2835293C (en) | 2011-06-08 | 2020-08-18 | Sti Pharma, Llc | Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration |
| ITFI20110172A1 (it) * | 2011-08-08 | 2013-02-09 | Valpharma Sa | Formulazione multiparticolata a rilascio modificato di diltiazem hcl. |
| WO2014204933A1 (en) | 2013-06-17 | 2014-12-24 | Adamas Pharmaceuticals, Inc. | Amantadine compositions and methods of use |
| AU2014295042B2 (en) | 2013-07-23 | 2017-03-30 | Mundipharma Pty Limited | A combination of oxycodone and naloxone for use in treating pain in patients suffering from pain and a disease resulting in intestinal dysbiosis and/or increasing the risk for intestinal bacterial translocation |
| CA2959965A1 (en) | 2014-09-02 | 2016-03-10 | Bhupinder Singh | Pharmaceutical formulations comprising tetrahydrocurcumin and lipids |
| CA2963923A1 (en) | 2014-10-08 | 2016-04-14 | Pacific Northwest Research Institute | Methods and compounds for increasing the potency of antifungal agents |
| US10973783B2 (en) | 2015-12-30 | 2021-04-13 | Adamas Pharmaceuticals, Inc. | Methods and compositions for the treatment of seizure-related disorders |
| WO2018200885A1 (en) | 2017-04-26 | 2018-11-01 | Neurocentria, Inc. | Magnesium compositions and methods of use |
| EP3773612A4 (en) | 2018-03-28 | 2022-01-12 | Herbalife International of America, Inc. | ACETYLATION OF POLYSACCHARIDS |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4456628A (en) * | 1981-01-07 | 1984-06-26 | Bauer Kurt H | Process for film-coating a particulate solid, and emulsions for conducting the process |
| DK152744C (da) * | 1982-08-13 | 1988-10-31 | Benzon As Alfred | Fremgangsmaade til fremstilling af et farmaceutisk peroralt polydepotpraeparat |
| US4898729A (en) * | 1983-12-09 | 1990-02-06 | Euroceltique, S.A. | Treatment of hypertension, compounds and compositions for antihypertension and diuresis |
| IE56999B1 (en) * | 1983-12-22 | 1992-03-11 | Elan Corp Plc | Pharmaceutical formulation |
| US4894240A (en) * | 1983-12-22 | 1990-01-16 | Elan Corporation Plc | Controlled absorption diltiazem formulation for once-daily administration |
| US5364620A (en) * | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US5002776A (en) * | 1983-12-22 | 1991-03-26 | Elan Corporation, Plc | Controlled absorption diltiazem formulations |
| US4917899A (en) * | 1983-12-22 | 1990-04-17 | Elan Corporation Plc | Controlled absorption diltiazem formulation |
| DE3403329A1 (de) * | 1984-02-01 | 1985-08-01 | Horst Dr. 4019 Monheim Zerbe | Pharmazeutisches produkt in form von pellets mit kontinuierlicher, verzoegerter wirkstoffabgabe |
| US4643731A (en) * | 1985-08-16 | 1987-02-17 | Alza Corporation | Means for providing instant agent from agent dispensing system |
| JPS62103012A (ja) * | 1985-10-23 | 1987-05-13 | Eisai Co Ltd | 多重顆粒 |
| IT1200217B (it) * | 1986-09-30 | 1989-01-05 | Valducci Roberto | Membrana per uso farmaceutico ed industriale |
| DE3709188A1 (de) * | 1987-03-20 | 1988-09-29 | Mannesmann Ag | Ausgiessrohr fuer metallurgische gefaesse |
| GB8707421D0 (en) * | 1987-03-27 | 1987-04-29 | Wellcome Found | Pharmaceutical formulations |
| CA1323833C (en) * | 1987-04-28 | 1993-11-02 | Yatindra M. Joshi | Pharmaceutical compositions in the form of beadlets and method |
| US4808413A (en) * | 1987-04-28 | 1989-02-28 | E. R. Squibb & Sons, Inc. | Pharmaceutical compositions in the form of beadlets and method |
| BE1000794A4 (nl) * | 1987-07-30 | 1989-04-04 | Schelde Delta Bv Met Beperkte | Werkwijze voor het bij chemische processen immobiliseren van komponenten in een fluidumstroom, en inrichtingen die deze werkwijze toepassen. |
| US4814181A (en) * | 1987-09-03 | 1989-03-21 | Alza Corporation | Dosage form comprising fast agent delivery followed by slow agent delivery |
| US5219621A (en) * | 1987-10-16 | 1993-06-15 | Elan Corporation, Plc | Methods of treatment with diltiazem formulations |
| ATE241987T1 (de) * | 1987-10-16 | 2003-06-15 | Elan Corp Plc | Diltiazem-zusammensetzungen mit kontrollierter wirkstoffabsorption |
| IL88083A (en) * | 1987-11-06 | 1992-11-15 | Tanabe Seiyaku Co | Controlled release pharmaceutical dosage form and its preparation |
| DE3739779A1 (de) * | 1987-11-24 | 1989-06-08 | Beiersdorf Ag | Pharmazeutische praeparate |
| FR2623714B1 (fr) * | 1987-11-26 | 1990-04-20 | Ethypharm Sa | Forme a liberation prolongee du diltiazem, et son medicament ainsi obtenu |
| FR2624732B1 (fr) * | 1987-12-21 | 1991-02-15 | Synthelabo | Formulation pharmaceutique a liberation prolongee |
| JP2643222B2 (ja) * | 1988-02-03 | 1997-08-20 | エーザイ株式会社 | 多重層顆粒 |
| GB8805695D0 (en) * | 1988-03-10 | 1988-04-07 | Nycomed As | Enteric coated spheroidal granules |
| FI101344B1 (fi) * | 1988-03-31 | 1998-06-15 | Tanabe Seiyaku Co | Menetelmä valmistaa valmiste, josta kontrolloidusti vapautuu farmaseuttisesti aktiivista ainetta |
| FR2630647B1 (fr) * | 1988-04-27 | 1991-08-16 | Sanofi Sa | Microbilles de diltiazem, leur procede de fabrication et compositions pharmaceutiques a liberation prolongee les contenant |
| ZA899071B (en) * | 1988-11-30 | 1990-08-29 | Schering Corp | Sustained release diltiazem formulation |
| SE506179C2 (sv) * | 1989-01-23 | 1997-11-17 | Ciba Geigy Ag | Farmaceutisk lågkomposition av benazepril och ett tiaziddiuretikum |
| SE8902699D0 (sv) * | 1989-08-09 | 1989-08-09 | Lejus Medical Ab | Diltiazem containing pharmaceutical compositios |
| JPH0674206B2 (ja) * | 1989-12-28 | 1994-09-21 | 田辺製薬株式会社 | 放出制御型製剤およびその製法 |
| IT1241417B (it) * | 1990-03-06 | 1994-01-14 | Vectorpharma Int | Composizioni terapeutiche a rilascio controllato di farmaci supportatisu polimeri reticolati e rivestiti con film polimerici,e loro processodi preparazione |
| ZA923474B (en) * | 1991-05-20 | 1993-01-27 | Marion Merrell Dow Inc | Diltiazem formulation |
| US5286497A (en) * | 1991-05-20 | 1994-02-15 | Carderm Capital L.P. | Diltiazem formulation |
-
1992
- 1992-08-04 KR KR1019920013984A patent/KR100221695B1/ko not_active IP Right Cessation
- 1992-08-05 CA CA002075356A patent/CA2075356A1/en not_active Abandoned
- 1992-08-06 AU AU20880/92A patent/AU651715B2/en not_active Expired
- 1992-08-10 PH PH44791A patent/PH31288A/en unknown
- 1992-08-10 JP JP4234295A patent/JP3019235B2/ja not_active Expired - Lifetime
- 1992-08-10 IL IL10277892A patent/IL102778A/en not_active IP Right Cessation
- 1992-08-11 DE DE69225278T patent/DE69225278D1/de not_active Expired - Lifetime
- 1992-08-11 AT AT92307333T patent/ATE165513T1/de active
- 1992-08-11 NO NO923128A patent/NO304406B1/no not_active IP Right Cessation
- 1992-08-11 FI FI923582A patent/FI923582A/fi unknown
- 1992-08-11 EP EP92307333A patent/EP0527637B1/en not_active Expired - Lifetime
- 1992-08-11 ES ES92307333T patent/ES2115643T3/es not_active Expired - Lifetime
- 1992-08-12 CN CN92105698A patent/CN1052398C/zh not_active Expired - Lifetime
-
1995
- 1995-04-21 US US08/426,065 patent/US5670172A/en not_active Expired - Lifetime
-
1996
- 1996-06-18 US US08/666,636 patent/US5601845A/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| EP0527637A1 (en) | 1993-02-17 |
| KR100221695B1 (ko) | 1999-09-15 |
| KR930003906A (ko) | 1993-03-22 |
| AU651715B2 (en) | 1994-07-28 |
| DE69225278D1 (de) | 1998-06-04 |
| US5601845A (en) | 1997-02-11 |
| NO923128D0 (no) | 1992-08-11 |
| IL102778A (en) | 1999-05-09 |
| JP3019235B2 (ja) | 2000-03-13 |
| AU2088092A (en) | 1993-02-18 |
| ES2115643T3 (es) | 1998-07-01 |
| CN1052398C (zh) | 2000-05-17 |
| CN1069408A (zh) | 1993-03-03 |
| NO923128L (no) | 1993-02-15 |
| CA2075356A1 (en) | 1993-02-13 |
| PH31288A (en) | 1998-07-06 |
| JPH05201867A (ja) | 1993-08-10 |
| EP0527637B1 (en) | 1998-04-29 |
| FI923582A0 (fi) | 1992-08-11 |
| ATE165513T1 (de) | 1998-05-15 |
| FI923582A (fi) | 1993-02-13 |
| IL102778A0 (en) | 1993-01-31 |
| US5670172A (en) | 1997-09-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK1K | Patent expired |