DE69720055T2 - Verabreichungsform zur abgabe von steigenden wirkstoffdosen - Google Patents
Verabreichungsform zur abgabe von steigenden wirkstoffdosenInfo
- Publication number
- DE69720055T2 DE69720055T2 DE69720055T DE69720055T DE69720055T2 DE 69720055 T2 DE69720055 T2 DE 69720055T2 DE 69720055 T DE69720055 T DE 69720055T DE 69720055 T DE69720055 T DE 69720055T DE 69720055 T2 DE69720055 T2 DE 69720055T2
- Authority
- DE
- Germany
- Prior art keywords
- layer
- drug
- dosage form
- molecular weight
- average molecular
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 239000013543 active substance Substances 0.000 title description 2
- 230000000630 rising effect Effects 0.000 title description 2
- 239000003814 drug Substances 0.000 claims abstract description 230
- 229940079593 drug Drugs 0.000 claims abstract description 220
- 239000002552 dosage form Substances 0.000 claims abstract description 119
- -1 Theomethylphenidate Chemical compound 0.000 claims description 109
- 239000000203 mixture Substances 0.000 claims description 63
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 59
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 40
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 40
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 40
- 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 description 40
- 239000011248 coating agent Substances 0.000 claims description 32
- 238000000576 coating method Methods 0.000 claims description 32
- 229920002125 Sokalan® Polymers 0.000 claims description 19
- DUGOZIWVEXMGBE-UHFFFAOYSA-N Methylphenidate Chemical compound C=1C=CC=CC=1C(C(=O)OC)C1CCCCN1 DUGOZIWVEXMGBE-UHFFFAOYSA-N 0.000 claims description 17
- 229960001344 methylphenidate Drugs 0.000 claims description 17
- 150000003943 catecholamines Chemical class 0.000 claims description 9
- KWTSXDURSIMDCE-QMMMGPOBSA-N (S)-amphetamine Chemical compound C[C@H](N)CC1=CC=CC=C1 KWTSXDURSIMDCE-QMMMGPOBSA-N 0.000 claims description 8
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 8
- 229920001477 hydrophilic polymer Polymers 0.000 claims description 8
- 229920000233 poly(alkylene oxides) Polymers 0.000 claims description 8
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 7
- 239000002269 analeptic agent Substances 0.000 claims description 7
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 7
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 7
- 229930003827 cannabinoid Natural products 0.000 claims description 6
- 239000003557 cannabinoid Substances 0.000 claims description 6
- 239000012530 fluid Substances 0.000 claims description 6
- 239000004094 surface-active agent Substances 0.000 claims description 6
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 5
- 229920013821 hydroxy alkyl cellulose Polymers 0.000 claims description 5
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 5
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 5
- 229940025084 amphetamine Drugs 0.000 claims description 4
- 229960000632 dexamfetamine Drugs 0.000 claims description 4
- AIVSIRYZIBXTMM-UHFFFAOYSA-N ethylphenidate Chemical compound C=1C=CC=CC=1C(C(=O)OCC)C1CCCCN1 AIVSIRYZIBXTMM-UHFFFAOYSA-N 0.000 claims description 4
- MYWUZJCMWCOHBA-VIFPVBQESA-N methamphetamine Chemical compound CN[C@@H](C)CC1=CC=CC=C1 MYWUZJCMWCOHBA-VIFPVBQESA-N 0.000 claims description 4
- 229960001252 methamphetamine Drugs 0.000 claims description 4
- FRCFWPVMFJMNDP-UHFFFAOYSA-N n-propan-2-ylaniline Chemical compound CC(C)NC1=CC=CC=C1 FRCFWPVMFJMNDP-UHFFFAOYSA-N 0.000 claims description 4
- NRNCYVBFPDDJNE-UHFFFAOYSA-N pemoline Chemical compound O1C(N)=NC(=O)C1C1=CC=CC=C1 NRNCYVBFPDDJNE-UHFFFAOYSA-N 0.000 claims description 4
- 229960000761 pemoline Drugs 0.000 claims description 4
- 206010027336 Menstruation delayed Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 abstract description 35
- 239000010410 layer Substances 0.000 description 211
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 64
- 239000004615 ingredient Substances 0.000 description 38
- 235000019359 magnesium stearate Nutrition 0.000 description 32
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 28
- 239000008187 granular material Substances 0.000 description 27
- 239000003826 tablet Substances 0.000 description 26
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 22
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 20
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 description 20
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 18
- 229960003447 pseudoephedrine hydrochloride Drugs 0.000 description 18
- BALXUFOVQVENIU-KXNXZCPBSA-N pseudoephedrine hydrochloride Chemical compound [H+].[Cl-].CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 BALXUFOVQVENIU-KXNXZCPBSA-N 0.000 description 18
- JUMYIBMBTDDLNG-OJERSXHUSA-N hydron;methyl (2r)-2-phenyl-2-[(2r)-piperidin-2-yl]acetate;chloride Chemical compound Cl.C([C@@H]1[C@H](C(=O)OC)C=2C=CC=CC=2)CCCN1 JUMYIBMBTDDLNG-OJERSXHUSA-N 0.000 description 17
- 229960001033 methylphenidate hydrochloride Drugs 0.000 description 17
- 238000002156 mixing Methods 0.000 description 16
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 15
- 230000002459 sustained effect Effects 0.000 description 15
- 239000011324 bead Substances 0.000 description 14
- 238000006073 displacement reaction Methods 0.000 description 14
- JEIPFZHSYJVQDO-UHFFFAOYSA-N iron(III) oxide Inorganic materials O=[Fe]O[Fe]=O JEIPFZHSYJVQDO-UHFFFAOYSA-N 0.000 description 14
- 229920001223 polyethylene glycol Polymers 0.000 description 14
- 239000003937 drug carrier Substances 0.000 description 12
- 239000007787 solid Substances 0.000 description 12
- 239000002202 Polyethylene glycol Substances 0.000 description 11
- 235000019441 ethanol Nutrition 0.000 description 11
- 239000011780 sodium chloride Substances 0.000 description 11
- 239000002904 solvent Substances 0.000 description 11
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 10
- 229920002301 cellulose acetate Polymers 0.000 description 10
- 229920000642 polymer Polymers 0.000 description 10
- 239000000843 powder Substances 0.000 description 10
- 239000007788 liquid Substances 0.000 description 9
- 239000000314 lubricant Substances 0.000 description 9
- 230000003204 osmotic effect Effects 0.000 description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 9
- 229920002678 cellulose Polymers 0.000 description 8
- 239000001913 cellulose Substances 0.000 description 8
- 230000008569 process Effects 0.000 description 8
- 238000004519 manufacturing process Methods 0.000 description 7
- 239000012528 membrane Substances 0.000 description 7
- 229940127240 opiate Drugs 0.000 description 7
- 239000000243 solution Substances 0.000 description 7
- 230000001225 therapeutic effect Effects 0.000 description 7
- 238000011282 treatment Methods 0.000 description 7
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 6
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 6
- 150000001298 alcohols Chemical class 0.000 description 6
- 229940125717 barbiturate Drugs 0.000 description 6
- 239000003326 hypnotic agent Substances 0.000 description 6
- 230000000147 hypnotic effect Effects 0.000 description 6
- 239000002357 osmotic agent Substances 0.000 description 6
- 239000003368 psychostimulant agent Substances 0.000 description 6
- 210000003169 central nervous system Anatomy 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 210000001035 gastrointestinal tract Anatomy 0.000 description 5
- 238000013268 sustained release Methods 0.000 description 5
- 239000012730 sustained-release form Substances 0.000 description 5
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 4
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 description 4
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 description 4
- ZBBHBTPTTSWHBA-UHFFFAOYSA-N Nicardipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN(C)CC=2C=CC=CC=2)C1C1=CC=CC([N+]([O-])=O)=C1 ZBBHBTPTTSWHBA-UHFFFAOYSA-N 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 4
- 230000001154 acute effect Effects 0.000 description 4
- 239000003513 alkali Substances 0.000 description 4
- LSQZJLSUYDQPKJ-NJBDSQKTSA-N amoxicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=C(O)C=C1 LSQZJLSUYDQPKJ-NJBDSQKTSA-N 0.000 description 4
- 229960003022 amoxicillin Drugs 0.000 description 4
- 230000008901 benefit Effects 0.000 description 4
- 229940065144 cannabinoids Drugs 0.000 description 4
- 230000001684 chronic effect Effects 0.000 description 4
- 239000003086 colorant Substances 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- 239000006184 cosolvent Substances 0.000 description 4
- 238000012377 drug delivery Methods 0.000 description 4
- 238000005469 granulation Methods 0.000 description 4
- 230000003179 granulation Effects 0.000 description 4
- 239000008240 homogeneous mixture Substances 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 229960001783 nicardipine Drugs 0.000 description 4
- LSQZJLSUYDQPKJ-UHFFFAOYSA-N p-Hydroxyampicillin Natural products O=C1N2C(C(O)=O)C(C)(C)SC2C1NC(=O)C(N)C1=CC=C(O)C=C1 LSQZJLSUYDQPKJ-UHFFFAOYSA-N 0.000 description 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- HZZVJAQRINQKSD-UHFFFAOYSA-N Clavulanic acid Natural products OC(=O)C1C(=CCO)OC2CC(=O)N21 HZZVJAQRINQKSD-UHFFFAOYSA-N 0.000 description 3
- 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 3
- 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 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 3
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 description 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
- 229920013820 alkyl cellulose Polymers 0.000 description 3
- 239000013060 biological fluid Substances 0.000 description 3
- 239000003576 central nervous system agent Substances 0.000 description 3
- 229940090805 clavulanate Drugs 0.000 description 3
- HZZVJAQRINQKSD-PBFISZAISA-N clavulanic acid Chemical compound OC(=O)[C@H]1C(=C/CO)/O[C@@H]2CC(=O)N21 HZZVJAQRINQKSD-PBFISZAISA-N 0.000 description 3
- 230000007812 deficiency Effects 0.000 description 3
- SWXVUIWOUIDPGS-UHFFFAOYSA-N diacetone alcohol Chemical compound CC(=O)CC(C)(C)O SWXVUIWOUIDPGS-UHFFFAOYSA-N 0.000 description 3
- 239000000975 dye Substances 0.000 description 3
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 3
- 229920003063 hydroxymethyl cellulose Polymers 0.000 description 3
- 229940031574 hydroxymethyl cellulose Drugs 0.000 description 3
- 230000000873 masking effect Effects 0.000 description 3
- 238000002483 medication Methods 0.000 description 3
- 229920001451 polypropylene glycol Polymers 0.000 description 3
- 230000002035 prolonged effect Effects 0.000 description 3
- 239000013557 residual solvent Substances 0.000 description 3
- 150000003839 salts Chemical class 0.000 description 3
- 239000000600 sorbitol Substances 0.000 description 3
- 238000002560 therapeutic procedure Methods 0.000 description 3
- 238000005303 weighing Methods 0.000 description 3
- 238000005550 wet granulation Methods 0.000 description 3
- QPFMBZIOSGYJDE-UHFFFAOYSA-N 1,1,2,2-tetrachloroethane Chemical compound ClC(Cl)C(Cl)Cl QPFMBZIOSGYJDE-UHFFFAOYSA-N 0.000 description 2
- WSLDOOZREJYCGB-UHFFFAOYSA-N 1,2-Dichloroethane Chemical compound ClCCCl WSLDOOZREJYCGB-UHFFFAOYSA-N 0.000 description 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 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 description 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 239000001856 Ethyl cellulose Substances 0.000 description 2
- 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 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 2
- 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 2
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 description 2
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 2
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 description 2
- 229910019142 PO4 Inorganic materials 0.000 description 2
- 239000004698 Polyethylene Substances 0.000 description 2
- 229920001213 Polysorbate 20 Polymers 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 2
- 235000021355 Stearic acid Nutrition 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 239000002280 amphoteric surfactant Substances 0.000 description 2
- 125000000129 anionic group Chemical group 0.000 description 2
- 239000003945 anionic surfactant Substances 0.000 description 2
- 238000000498 ball milling Methods 0.000 description 2
- 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 2
- 230000036765 blood level Effects 0.000 description 2
- DKPFZGUDAPQIHT-UHFFFAOYSA-N butyl acetate Chemical compound CCCCOC(C)=O DKPFZGUDAPQIHT-UHFFFAOYSA-N 0.000 description 2
- 238000003490 calendering Methods 0.000 description 2
- 125000002091 cationic group Chemical group 0.000 description 2
- 239000003093 cationic surfactant Substances 0.000 description 2
- 230000003111 delayed effect Effects 0.000 description 2
- 239000011928 denatured alcohol Substances 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- WGLUMOCWFMKWIL-UHFFFAOYSA-N dichloromethane;methanol Chemical compound OC.ClCCl WGLUMOCWFMKWIL-UHFFFAOYSA-N 0.000 description 2
- 238000002651 drug therapy Methods 0.000 description 2
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- 229920001249 ethyl cellulose Polymers 0.000 description 2
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- 239000008101 lactose Substances 0.000 description 2
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- KWGKDLIKAYFUFQ-UHFFFAOYSA-M lithium chloride Chemical compound [Li+].[Cl-] KWGKDLIKAYFUFQ-UHFFFAOYSA-M 0.000 description 2
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- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- XNLICIUVMPYHGG-UHFFFAOYSA-N pentan-2-one Chemical compound CCCC(C)=O XNLICIUVMPYHGG-UHFFFAOYSA-N 0.000 description 2
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- 238000002360 preparation method Methods 0.000 description 2
- 229960003908 pseudoephedrine Drugs 0.000 description 2
- KWGRBVOPPLSCSI-WCBMZHEXSA-N pseudoephedrine Chemical compound CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WCBMZHEXSA-N 0.000 description 2
- 229910052938 sodium sulfate Inorganic materials 0.000 description 2
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- OUSKVHOYPHDTIA-XZBKPIIZSA-N (3r,4s,5r,6r)-3,4,5,6,7-pentahydroxyheptan-2-one Chemical compound CC(=O)[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO OUSKVHOYPHDTIA-XZBKPIIZSA-N 0.000 description 1
- ODIGIKRIUKFKHP-UHFFFAOYSA-N (n-propan-2-yloxycarbonylanilino) acetate Chemical compound CC(C)OC(=O)N(OC(C)=O)C1=CC=CC=C1 ODIGIKRIUKFKHP-UHFFFAOYSA-N 0.000 description 1
- ICLYJLBTOGPLMC-KVVVOXFISA-N (z)-octadec-9-enoate;tris(2-hydroxyethyl)azanium Chemical compound OCCN(CCO)CCO.CCCCCCCC\C=C/CCCCCCCC(O)=O ICLYJLBTOGPLMC-KVVVOXFISA-N 0.000 description 1
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 1
- KNKRKFALVUDBJE-UHFFFAOYSA-N 1,2-dichloropropane Chemical compound CC(Cl)CCl KNKRKFALVUDBJE-UHFFFAOYSA-N 0.000 description 1
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 1
- JSZOAYXJRCEYSX-UHFFFAOYSA-N 1-nitropropane Chemical compound CCC[N+]([O-])=O JSZOAYXJRCEYSX-UHFFFAOYSA-N 0.000 description 1
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- MLICVSDCCDDWMD-KVVVOXFISA-M potassium;(z)-octadec-9-enoate Chemical compound [K+].CCCCCCCC\C=C/CCCCCCCC([O-])=O MLICVSDCCDDWMD-KVVVOXFISA-M 0.000 description 1
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- MUPFEKGTMRGPLJ-ZQSKZDJDSA-N raffinose 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[C@@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O2)O)O1 MUPFEKGTMRGPLJ-ZQSKZDJDSA-N 0.000 description 1
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- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
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- OKUCEQDKBKYEJY-UHFFFAOYSA-N tert-butyl 3-(methylamino)pyrrolidine-1-carboxylate Chemical compound CNC1CCN(C(=O)OC(C)(C)C)C1 OKUCEQDKBKYEJY-UHFFFAOYSA-N 0.000 description 1
- RBTVSNLYYIMMKS-UHFFFAOYSA-N tert-butyl 3-aminoazetidine-1-carboxylate;hydrochloride Chemical compound Cl.CC(C)(C)OC(=O)N1CC(N)C1 RBTVSNLYYIMMKS-UHFFFAOYSA-N 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
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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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0004—Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (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)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2328696P | 1996-08-16 | 1996-08-16 | |
| PCT/US1997/013816 WO1998006380A2 (en) | 1996-08-16 | 1997-08-08 | Dosage form for providing ascending dose of drug |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE69720055D1 DE69720055D1 (de) | 2003-04-24 |
| DE69720055T2 true DE69720055T2 (de) | 2003-09-11 |
Family
ID=21814183
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69720055T Expired - Lifetime DE69720055T2 (de) | 1996-08-16 | 1997-08-08 | Verabreichungsform zur abgabe von steigenden wirkstoffdosen |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP0957899B1 (enExample) |
| JP (1) | JP4393587B2 (enExample) |
| CN (2) | CN100484518C (enExample) |
| AT (1) | ATE234602T1 (enExample) |
| AU (1) | AU3909597A (enExample) |
| CA (1) | CA2263558A1 (enExample) |
| CY (1) | CY2475B1 (enExample) |
| DE (1) | DE69720055T2 (enExample) |
| DK (1) | DK0957899T3 (enExample) |
| ES (1) | ES2194210T3 (enExample) |
| PT (1) | PT957899E (enExample) |
| WO (1) | WO1998006380A2 (enExample) |
| ZA (1) | ZA977254B (enExample) |
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| US6440457B1 (en) | 1993-05-27 | 2002-08-27 | Alza Corporation | Method of administering antidepressant dosage form |
| US5837284A (en) | 1995-12-04 | 1998-11-17 | Mehta; Atul M. | Delivery of multiple doses of medications |
| WO1998014168A2 (en) * | 1996-09-30 | 1998-04-09 | Alza Corporation | Dosage form providing a sustained and ascending drug release |
| EP1690531A3 (en) * | 1996-09-30 | 2010-01-20 | Alza Corporation | Dosage form and method for administering drug |
| US6919373B1 (en) | 1996-11-12 | 2005-07-19 | Alza Corporation | Methods and devices for providing prolonged drug therapy |
| CN1182839C (zh) * | 1996-11-25 | 2005-01-05 | 阿尔萨公司 | 递增剂量的剂型 |
| US6962997B1 (en) | 1997-05-22 | 2005-11-08 | Celgene Corporation | Process and intermediates for resolving piperidyl acetamide steroisomers |
| KR100827254B1 (ko) * | 1998-06-03 | 2008-05-07 | 알자 코포레이션 | 연장된 약물 치료를 제공하기 위한 방법 및 장치 |
| KR100890537B1 (ko) * | 1998-06-03 | 2009-03-27 | 알자 코포레이션 | 연장된 약물 치료를 제공하기 위한 방법 및 장치 |
| NZ508567A (en) * | 1998-06-03 | 2004-02-27 | Alza Corp | Methods and devices for providing prolonged drug therapy |
| AU2012232984B2 (en) * | 1998-06-03 | 2015-10-29 | Alza Corporation | Methods and devices for providing prolonged drug therapy |
| AU2004200938B2 (en) * | 1998-06-03 | 2006-09-14 | Alza Corporation | Methods and devices for providing prolonged drug therapy |
| CA2653839A1 (en) | 1998-11-02 | 2000-05-11 | John G. Devane | Multiparticulate modified release composition |
| US6419960B1 (en) | 1998-12-17 | 2002-07-16 | Euro-Celtique S.A. | Controlled release formulations having rapid onset and rapid decline of effective plasma drug concentrations |
| US6673367B1 (en) * | 1998-12-17 | 2004-01-06 | Euro-Celtique, S.A. | Controlled/modified release oral methylphenidate formulations |
| WO2000059481A1 (en) | 1999-04-06 | 2000-10-12 | Pharmaquest Ltd. | PHARMACEUTICAL DOSAGE FORM FOR PULSATILE DELIVERY OF d-threo-METHYLPHENIDATE AND A SECOND CNS STIMULANT |
| KR20020072290A (ko) * | 2000-01-20 | 2002-09-14 | 델시스 파머수티컬 코포레이션 | 다단계 약물 투여 형태 |
| US20050232995A1 (en) | 2002-07-29 | 2005-10-20 | Yam Nyomi V | Methods and dosage forms for controlled delivery of paliperidone and risperidone |
| PL210119B1 (pl) * | 2002-07-29 | 2011-12-30 | Alza Corp | Lek do leczenia stanu wrażliwego na paliperidon |
| US20040091538A1 (en) * | 2002-10-31 | 2004-05-13 | Crystal Pollock-Dove | Dosage form providing ascending release of liquid formulation |
| US7988993B2 (en) | 2002-12-09 | 2011-08-02 | Andrx Pharmaceuticals, Inc. | Oral controlled release dosage form |
| ATE544447T1 (de) | 2003-09-26 | 2012-02-15 | Alza Corp | Arzneistoffcoating mit hohem wirkstoffanteil sowie methoden zu dessen herstellung |
| EP1677769A1 (en) * | 2003-09-26 | 2006-07-12 | Alza Corporation | Controlled release formulations exhibiting an ascending rate of release |
| US8541026B2 (en) | 2004-09-24 | 2013-09-24 | Abbvie Inc. | Sustained release formulations of opioid and nonopioid analgesics |
| PL116330U1 (en) | 2005-10-31 | 2007-04-02 | Alza Corp | Method for the reduction of alcohol provoked rapid increase in the released dose of the orally administered opioide with prolonged liberation |
| US9226907B2 (en) | 2008-02-01 | 2016-01-05 | Abbvie Inc. | Extended release hydrocodone acetaminophen and related methods and uses thereof |
| WO2015001488A1 (en) | 2013-07-01 | 2015-01-08 | Ranbaxy Laboratories Limited | Extended-release tablets of paliperidone and processes of preparation thereof |
| CA3018328A1 (en) | 2014-10-31 | 2016-04-30 | Purdue Pharma | Methods and compositions particularly for treatment of attention deficit disorder |
| MX2018007977A (es) * | 2015-12-31 | 2018-11-09 | Cadila Healthcare Ltd | Forma farmaceutica osmotica de liberacion extendida que contiene una carga de clorhidrato de metilfenidato alta. |
| EP3501504A1 (en) | 2017-12-22 | 2019-06-26 | Pharmacia Polonica sp. z o.o. | Modified release tablet of paliperidone and a process for the preparation thereof |
| US10722473B2 (en) | 2018-11-19 | 2020-07-28 | Purdue Pharma L.P. | Methods and compositions particularly for treatment of attention deficit disorder |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4327725A (en) * | 1980-11-25 | 1982-05-04 | Alza Corporation | Osmotic device with hydrogel driving member |
| US4842867A (en) * | 1986-05-09 | 1989-06-27 | Alza Corporation | Pulsed drug delivery of doxylamine |
| GB2206046B (en) * | 1987-06-25 | 1991-04-03 | Alza Corp | Multi-unit delivery system |
| US4874388A (en) * | 1987-06-25 | 1989-10-17 | Alza Corporation | Multi-layer delivery system |
| US4814181A (en) * | 1987-09-03 | 1989-03-21 | Alza Corporation | Dosage form comprising fast agent delivery followed by slow agent delivery |
| US4915954A (en) * | 1987-09-03 | 1990-04-10 | Alza Corporation | Dosage form for delivering a drug at two different rates |
| US5017381A (en) * | 1990-05-02 | 1991-05-21 | Alza Corporation | Multi-unit pulsatile delivery system |
| EP0621032B1 (en) * | 1993-04-23 | 2000-08-09 | Novartis AG | Controlled release drug delivery device |
| GB9402203D0 (en) * | 1994-02-04 | 1994-03-30 | Smithkline Beecham Plc | Pharmaceutical formulation |
-
1997
- 1997-08-08 JP JP50984198A patent/JP4393587B2/ja not_active Expired - Lifetime
- 1997-08-08 ES ES97936421T patent/ES2194210T3/es not_active Expired - Lifetime
- 1997-08-08 AU AU39095/97A patent/AU3909597A/en not_active Abandoned
- 1997-08-08 AT AT97936421T patent/ATE234602T1/de active
- 1997-08-08 CN CNB97197439XA patent/CN100484518C/zh not_active Expired - Lifetime
- 1997-08-08 CN CN200910129895.8A patent/CN101518517B/zh not_active Expired - Lifetime
- 1997-08-08 EP EP97936421A patent/EP0957899B1/en not_active Expired - Lifetime
- 1997-08-08 PT PT97936421T patent/PT957899E/pt unknown
- 1997-08-08 DE DE69720055T patent/DE69720055T2/de not_active Expired - Lifetime
- 1997-08-08 CA CA002263558A patent/CA2263558A1/en not_active Abandoned
- 1997-08-08 DK DK97936421T patent/DK0957899T3/da active
- 1997-08-08 WO PCT/US1997/013816 patent/WO1998006380A2/en not_active Ceased
- 1997-08-13 ZA ZA9707254A patent/ZA977254B/xx unknown
-
2004
- 2004-08-27 CY CY0400067A patent/CY2475B1/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2263558A1 (en) | 1998-02-19 |
| CY2475B1 (en) | 2005-06-03 |
| WO1998006380A3 (en) | 1998-05-14 |
| ES2194210T3 (es) | 2003-11-16 |
| ZA977254B (en) | 1998-05-11 |
| JP2000516610A (ja) | 2000-12-12 |
| ATE234602T1 (de) | 2003-04-15 |
| WO1998006380A2 (en) | 1998-02-19 |
| CN100484518C (zh) | 2009-05-06 |
| CN101518517B (zh) | 2014-11-26 |
| AU3909597A (en) | 1998-03-06 |
| CN1228691A (zh) | 1999-09-15 |
| CN101518517A (zh) | 2009-09-02 |
| HK1021886A1 (zh) | 2000-07-14 |
| EP0957899A2 (en) | 1999-11-24 |
| EP0957899B1 (en) | 2003-03-19 |
| HK1137355A1 (zh) | 2010-07-30 |
| DE69720055D1 (de) | 2003-04-24 |
| JP4393587B2 (ja) | 2010-01-06 |
| DK0957899T3 (da) | 2003-04-22 |
| PT957899E (pt) | 2003-07-31 |
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