NO333572B1 - Ropinirolholdig hydrofil/lipofil polymer matriksdoseringsformulering - Google Patents
Ropinirolholdig hydrofil/lipofil polymer matriksdoseringsformulering Download PDFInfo
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- NO333572B1 NO333572B1 NO20024919A NO20024919A NO333572B1 NO 333572 B1 NO333572 B1 NO 333572B1 NO 20024919 A NO20024919 A NO 20024919A NO 20024919 A NO20024919 A NO 20024919A NO 333572 B1 NO333572 B1 NO 333572B1
- Authority
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- Norway
- Prior art keywords
- layer
- tablet
- controlled release
- ropinirole
- barrier
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 61
- UHSKFQJFRQCDBE-UHFFFAOYSA-N ropinirole Chemical compound CCCN(CCC)CCC1=CC=CC2=C1CC(=O)N2 UHSKFQJFRQCDBE-UHFFFAOYSA-N 0.000 title claims description 111
- 229960001879 ropinirole Drugs 0.000 title claims description 110
- 229920000642 polymer Polymers 0.000 title claims description 31
- 238000009472 formulation Methods 0.000 title abstract description 23
- 239000011159 matrix material Substances 0.000 title description 10
- 239000000126 substance Substances 0.000 claims abstract description 76
- 239000013543 active substance Substances 0.000 claims abstract description 67
- 239000002671 adjuvant Substances 0.000 claims abstract description 13
- 239000000463 material Substances 0.000 claims abstract description 9
- 230000004888 barrier function Effects 0.000 claims description 171
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 72
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 72
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 69
- 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 69
- 238000013270 controlled release Methods 0.000 claims description 48
- 239000002585 base Substances 0.000 claims description 44
- 238000007906 compression Methods 0.000 claims description 41
- 230000006835 compression Effects 0.000 claims description 41
- 229920001477 hydrophilic polymer Polymers 0.000 claims description 34
- 238000002360 preparation method Methods 0.000 claims description 34
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 28
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 25
- 238000004519 manufacturing process Methods 0.000 claims description 25
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 21
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- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 18
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- 229940049654 glyceryl behenate Drugs 0.000 claims description 17
- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical class CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 claims description 16
- 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 description 16
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 15
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 15
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- 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 description 8
- 239000001856 Ethyl cellulose Substances 0.000 claims description 8
- 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 description 8
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- 235000013871 bee wax Nutrition 0.000 claims description 5
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- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 4
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- 235000021122 unsaturated fatty acids Nutrition 0.000 claims description 3
- FLPJVCMIKUWSDR-UHFFFAOYSA-N 2-(4-formylphenoxy)acetamide Chemical compound NC(=O)COC1=CC=C(C=O)C=C1 FLPJVCMIKUWSDR-UHFFFAOYSA-N 0.000 claims description 2
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 claims description 2
- 229920001450 Alpha-Cyclodextrin Polymers 0.000 claims description 2
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.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 WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 2
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- HFHDHCJBZVLPGP-RWMJIURBSA-N alpha-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO HFHDHCJBZVLPGP-RWMJIURBSA-N 0.000 claims description 2
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- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 2
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- GDSRMADSINPKSL-HSEONFRVSA-N gamma-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO GDSRMADSINPKSL-HSEONFRVSA-N 0.000 claims description 2
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- FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical class OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 claims description 2
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- XDXHAEQXIBQUEZ-UHFFFAOYSA-N Ropinirole hydrochloride Chemical group Cl.CCCN(CCC)CCC1=CC=CC2=C1CC(=O)N2 XDXHAEQXIBQUEZ-UHFFFAOYSA-N 0.000 claims 1
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Applications Claiming Priority (3)
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IT2000MI000852A IT1318470B1 (it) | 2000-04-14 | 2000-04-14 | Matrici polimeriche idrofile/lipofile, in grado di cedere sostanzefarmacologiamente attive a velocita' predeterminata. |
IT2000MI001963A IT1318687B1 (it) | 2000-09-07 | 2000-09-07 | Matrici polimeriche idrofile/lipofile, in grado di cedere sostanzefarmacologicamente attive a velocita' predeterminata. |
PCT/GB2001/001726 WO2001078688A1 (en) | 2000-04-14 | 2001-04-12 | Hydrophilic/lipophilic polymeric matrix dosage formulation |
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NO20024919D0 NO20024919D0 (no) | 2002-10-11 |
NO20024919L NO20024919L (no) | 2002-12-06 |
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NO20024919A NO333572B1 (no) | 2000-04-14 | 2002-10-11 | Ropinirolholdig hydrofil/lipofil polymer matriksdoseringsformulering |
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EP (4) | EP1681051B1 (sl) |
JP (2) | JP5073907B2 (sl) |
KR (4) | KR20070065922A (sl) |
CN (1) | CN1198598C (sl) |
AR (1) | AR030557A1 (sl) |
AT (1) | ATE401867T1 (sl) |
AU (3) | AU779623B2 (sl) |
BR (1) | BRPI0110038C1 (sl) |
CA (1) | CA2405508C (sl) |
CZ (1) | CZ303943B6 (sl) |
DE (1) | DE60134964D1 (sl) |
DK (1) | DK1272167T3 (sl) |
ES (2) | ES2307608T3 (sl) |
HK (1) | HK1053602A1 (sl) |
HU (1) | HU228269B1 (sl) |
IL (2) | IL152184A0 (sl) |
MX (1) | MXPA02010151A (sl) |
NO (1) | NO333572B1 (sl) |
NZ (1) | NZ521902A (sl) |
PL (1) | PL202689B1 (sl) |
PT (1) | PT1272167E (sl) |
SI (1) | SI1272167T1 (sl) |
WO (1) | WO2001078688A1 (sl) |
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