HU225236B1 - Pharmaceutical formulations containing darifenacin - Google Patents
Pharmaceutical formulations containing darifenacin Download PDFInfo
- Publication number
- HU225236B1 HU225236B1 HU9802339A HUP9802339A HU225236B1 HU 225236 B1 HU225236 B1 HU 225236B1 HU 9802339 A HU9802339 A HU 9802339A HU P9802339 A HUP9802339 A HU P9802339A HU 225236 B1 HU225236 B1 HU 225236B1
- Authority
- HU
- Hungary
- Prior art keywords
- darifenacin
- released
- pharmaceutically acceptable
- acceptable salt
- dosage form
- Prior art date
Links
- HXGBXQDTNZMWGS-RUZDIDTESA-N darifenacin Chemical compound C=1C=CC=CC=1C([C@H]1CN(CCC=2C=C3CCOC3=CC=2)CC1)(C(=O)N)C1=CC=CC=C1 HXGBXQDTNZMWGS-RUZDIDTESA-N 0.000 title claims description 60
- 229960002677 darifenacin Drugs 0.000 title claims description 57
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims description 31
- 239000002552 dosage form Substances 0.000 claims description 27
- 238000000576 coating method Methods 0.000 claims description 21
- 239000011248 coating agent Substances 0.000 claims description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 15
- 239000011159 matrix material Substances 0.000 claims description 11
- 210000001035 gastrointestinal tract Anatomy 0.000 claims description 10
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 9
- NWUYHJFMYQTDRP-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene;1-ethenyl-2-ethylbenzene;styrene Chemical compound C=CC1=CC=CC=C1.CCC1=CC=CC=C1C=C.C=CC1=CC=CC=C1C=C NWUYHJFMYQTDRP-UHFFFAOYSA-N 0.000 claims description 7
- -1 hydroxypropyl Chemical group 0.000 claims description 7
- 239000003456 ion exchange resin Substances 0.000 claims description 7
- 229920003303 ion-exchange polymer Polymers 0.000 claims description 7
- 239000002671 adjuvant Substances 0.000 claims description 6
- 239000003085 diluting agent Substances 0.000 claims description 6
- 210000003750 lower gastrointestinal tract Anatomy 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 6
- VOJUXHHACRXLTD-UHFFFAOYSA-N 1,4-dihydroxy-2-naphthoic acid Chemical compound C1=CC=CC2=C(O)C(C(=O)O)=CC(O)=C21 VOJUXHHACRXLTD-UHFFFAOYSA-N 0.000 claims description 5
- 230000003628 erosive effect Effects 0.000 claims description 5
- 238000009792 diffusion process Methods 0.000 claims description 4
- 230000002035 prolonged effect Effects 0.000 claims description 3
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical class Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 description 34
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 20
- 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 16
- 239000008101 lactose Substances 0.000 description 16
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 15
- 238000009472 formulation Methods 0.000 description 13
- UQAVIASOPREUIT-VQIWEWKSSA-N darifenacin hydrobromide Chemical compound Br.C=1C=CC=CC=1C([C@H]1CN(CCC=2C=C3CCOC3=CC=2)CC1)(C(=O)N)C1=CC=CC=C1 UQAVIASOPREUIT-VQIWEWKSSA-N 0.000 description 11
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1611—Inorganic compounds
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- A—HUMAN NECESSITIES
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- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- A—HUMAN NECESSITIES
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- A61K9/20—Pills, tablets, discs, rods
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- A—HUMAN NECESSITIES
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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Description
Komponensek | Specifikálás | mg/egység (elméleti) | g/tétel (tényleges) |
Darifenacin- hidrobromid | Pfizer | 23,810 | 30,19 |
Methocel K4M | Európai Gyógyszer- könyv | 12,000 | 15,00 |
Methocel K100 LV Prémium | USP | 28,000 | 35,00 |
Fást flo Lactose | Európai Gyógyszer- könyv | 134,190 | 167,70 |
Magnézium- sztearát | Európai Gyógyszer- könyv | 2,000 | 2,50 |
Összesen | 200,000 mg |
Komponensek | Specifikálás | mg/egység (elméleti) | g/tétel (tényleges) |
Darifenacin- hidrobromid | Pfizer | 23,810 | 30,19 |
Methocel K4M | Európai Gyógyszer- könyv | 30,000 | 37,50 |
Methocel E4M | Európai Gyógyszer- könyv | 30,000 | 37,50 |
Fást flo Lactose | Európai Gyógyszer- könyv | 114,190 | 142,70 |
Magnézium- sztearát | Európai Gyógyszer- könyv | 2,000 | 2,50 |
Összesen | 200,000 mg |
Komponensek | Specifikálás | mg/egység (elméleti) | g/tétel (tényleges) |
Darifenacin- hidrobromid | Pfizer | 23,810 | 30,19 |
Vízmentes, kétszer bázisos kalciumfoszfát | USP | 59,790 | 74,70 |
Methocel K4M | Európai Gyógyszer- könyv | 114,400 | 143,00 |
Magnézium- sztearát | Európai Gyógyszer- könyv | 2,000 | 2,50 |
Összesen | 200,000 mg |
Komponen- sek | Specifikálás | g/kg (elméleti) | g/tétel (tényleges) |
Darifena- cin-hidro- bromid | Pfizer | 119,048 | 119,76 |
Avicel PH101 | Európai Gyógyszer- könyv | 359,499 | 359,50 |
Lactose Regular | Európai Gyógyszer- könyv | 359,499 | 359,50 |
Fumársav | NF* | 161,954 | 161,95 |
Tisztított víz | Európai Gyógyszer- könyv | (500,000) | 500,0 |
Összesen | 1000,000 g | 1000,71 |
Komponensek | Specifikálás | mg/egység (elméleti) | g/tétel (tényleges) |
Darifenacin (bevonat nélküli magvak) | Pfizer | 200,000 | 150,30 |
Etil-cellulóz N-10 | NF* | 17,750 | 13,32 |
Klucel EF | NF* | 7,250 | 5,44 |
Etil-acetát | NF* | 237,500 | 178,2 |
Izopropanol | NF* | 237,500 | 178,1 |
Összesen | 225,000 |
Komponensek | g/tétel |
Darifenacin-hidrobromid | 60,39 |
Nátrium-poli(sztirol-szulfonát) | 187,00 |
Dinátrium-edetát-dihidrát | 1,53 |
Víz | 2000,00 |
Komponensek | Specifikálás | mg/egység (elméleti) | g/tétel (tényleges) |
Darifenacin- hidrobromid | Pfizer | 8,929 | 547,46 |
Laktóz | Európai Gyógyszer- könyv | 104,453 | 6267,20 |
Kukoricake- ményítő | Európai Gyógyszer- könyv | 34,818 | 2089,10 |
Aerosil 200 | Európai Gyógyszer- könyv | 0,300 | 18,00 |
Magnézium- sztearát | Európai Gyógyszer- könyv | 1,500 | 84,88 |
Összesen | 150,000 |
Idő (óra) | Felszabadult mennyiség %-a (tartomány) |
1 | 65(52-81) |
2 | 80 (72-92) |
4 | 91(87-96) |
Idő (óra) | Felszabadult mennyiség %-a (tartomány) |
1 | 41 (38-46) |
4 | 77 (73-81) |
8 | 95 (94-96) |
Idő (óra) | Felszabadult mennyiség %-a (tartomány) |
1 | 6 (5-7) |
8 | 42 (36-44) |
16 | 67 (59-70) |
Idő (óra) | Felszabadult mennyiség %-a (tartomány) |
1 | 11 (9-15) |
4 | 58 (50-70) |
8 | 98 (95-103) |
Idő (óra) | Felszabadult mennyiség %-a (tartomány) |
1 | 11 (10-12) |
2 | 25 (24-27) |
Idő (óra) | Felszabadult mennyiség %-a (tartomány) |
6 | 55 (51-59) |
12 | 79 (77-82) |
18 | 90(89-91) |
24 | 94 (93-95) |
Idő (óra) | Felszabadult mennyiség %-a (tartomány) |
0,25 | 94 |
0,5 | 99 |
0,75 | 98 |
Készítmény | 6. példa (azonnali felszabadulású) | 1. példa | 2. példa | 3. példa |
AUCdar/AUCmet arány | 0,66 | 0,58 | 0,82 | 1,03 |
^~rel darifenacin | na | 0,88 | 1,10 | 1,17 |
Fjei metabolit | na | 0,98 | 0,82 | 0,70 |
Claims (12)
- SZABADALMI IGÉNYPONTOK1. Orális adagolásra szánt gyógyszer-adagolási forma, amely darifenacint vagy annak gyógyászati szempontból elfogadható sóját, valamint gyógyászati szempontból elfogadható adjuvánst, hígítószert vagy vivőanyagot tartalmaz, ahol az említett adagolási formában a darifenacin vagy gyógyászati szempontból elfogadható sója (a) mátrixba ágyazott, amelyből diffúzió vagy erózió útján szabadul fel;(b) többszemcsés magban van jelen;(c) egy impermeábilis bevonatban lévő nyíláson át szabadul fel;(d) csekély vízoldékonyságú bevonaton keresztül szabadul fel;(e) féligáteresztő (szemipermeábilis) bevonaton keresztül szabadul fel;(f) ioncserélő gyantaként van jelen; vagy (g) a gyomor-bél rendszer specifikus pontjainál pulzáló eszközök segítségével szabadul fel, azzal jellemezve, hogy az adagolási forma olyan kialakítású, hogy a darifenacinnak vagy gyógyászati szempontból elfogadható sójának legalább 10 tömeg%-át a beteg gyomor-bél rendszerének alsó szakaszába juttatja.
- 2. Az 1. igénypont szerinti adagolási forma, amely olyan kialakítású, hogy a darifenacinnak vagy gyógyászati szempontból elfogadható sójának legalább 50 tömeg%-át a gyomor-bél rendszer alsó részébe juttatja.
- 3. Az 1. vagy 2. igénypont szerinti adagolási forma, amely olyan kialakítású, hogy a darifenacin vagy gyógyászati szempontból elfogadható sója a betegnek történő adagolást követően tartós időn át vagy hosszabb idő elteltével szabadul fel a beteg gyomor-bél rendszerében.
- 4. A 3. igénypont szerinti adagolási forma, ahol a darifenacin vagy gyógyászati szempontból elfogadható sójának legfeljebb 90 tömeg%-a az adagolás utáni 4 óra elteltével szabadul fel.
- 5. A 4. igénypont szerinti adagolási forma, ahol a darifenacin vagy gyógyászati szempontból elfogadható sójának legfeljebb 90 tömeg%-a az adagolás utáni 8 óra elteltével szabadul fel.
- 6. Az 5. igénypont szerinti adagolási forma, ahol a darifenacin vagy gyógyászati szempontból elfogadható sójának legfeljebb 90 tömeg%-a az adagolás utáni 16 óra elteltével szabadul fel.
- 7. Orális adagolásra szánt gyógyszer-adagolási forma, amely darifenacint vagy annak gyógyászati szempontból elfogadható sóját, valamint gyógyászati szempontból elfogadható adjuvánst, hígítószert vagy vivőanyagot tartalmaz, ahol az említett adagolási formában a darifenacin vagy gyógyászati szempontból elfogadható sója (a) mátrixba ágyazott, amelyből diffúzió vagy erózió útján szabadul fel;HU 225 236 Β1 (b) többszemcsés magban van jelen;(c) egy impermeábilis bevonatban lévő nyíláson át szabadul fel;(d) csekély vízoldékonyságú bevonaton keresztül szabadul fel;(e) féligáteresztő (szemipermeábilis) bevonaton keresztül szabadul fel;(f) ioncserélő gyantaként van jelen; vagy (g) a gyomor-bél rendszer specifikus pontjainál pulzáló eszközök segítségével szabadul fel, azzal jellemezve, hogy az adagolási forma olyan kialakítású, hogy a darifenacin vagy annak gyógyászati szempontból elfogadható sójának az Amerikai Egyesült Államok Gyógyszerkönyvének XXII. kiadása 1578. oldalán leírt 1. berendezésben - amelynek 381 pm nyílásméretű (40 mesh) kosarai vannak, fordulatszáma 100 fordulat/perc, és oldóközege 37 °C hőmérsékletű víz - legfeljebb 90 tömeg%-a 4 óra elteltével szabadul fel.
- 8. A 7. igénypont szerinti adagolási forma, ahol a darifenacin vagy gyógyászati szempontból elfogadható sójának legfeljebb 90 tömeg%-a 8 óra elteltével szabadul fel.
- 9. A 7. igénypont szerinti adagolási forma, ahol a darifenacin vagy gyógyászati szempontból elfogadható sójának legfeljebb 90 tömeg%-a 16 óra elteltével szabadul fel.
- 10. Az 1-9. igénypontok bármelyike szerinti adagolási forma, ahol a darifenacin hidrobromidsója alakjában van.
- 11. Az 1. (a) igénypont vagy a 7. (a) igénypont szerinti adagolási forma, amelyből a darifenacin vagy annak gyógyászati szempontból elfogadható sója diffúzió útján szabadul fel, ahol a mátrix 85 000-95 000 tömegegységű (hidroxi-propil)-metil-cellulóz.
- 12. Eljárás a 11. igénypont szerinti adagolási forma előállítására, azzal jellemezve, hogy darifenacint vagy annak gyógyászati szempontból elfogadható sóját nagy molekulatömegű (hidroxi-propil)-metil-cellulózzal, amelynek molekulatömege 85 000-95 000 tömegegységű, elegyítünk.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB9518953.6A GB9518953D0 (en) | 1995-09-15 | 1995-09-15 | Pharmaceutical formulations |
PCT/EP1996/003719 WO1997009980A1 (en) | 1995-09-15 | 1996-08-21 | Pharmaceutical formulations containing darifenacin |
Publications (3)
Publication Number | Publication Date |
---|---|
HUP9802339A2 HUP9802339A2 (hu) | 1999-08-30 |
HUP9802339A3 HUP9802339A3 (en) | 1999-09-28 |
HU225236B1 true HU225236B1 (en) | 2006-08-28 |
Family
ID=10780813
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Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0500976A HU227397B1 (en) | 1995-09-15 | 1996-08-21 | Pharmaceutical formulations containing darifenacin |
HU9802339A HU225236B1 (en) | 1995-09-15 | 1996-08-21 | Pharmaceutical formulations containing darifenacin |
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Application Number | Title | Priority Date | Filing Date |
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HU0500976A HU227397B1 (en) | 1995-09-15 | 1996-08-21 | Pharmaceutical formulations containing darifenacin |
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EP (2) | EP1245231B1 (hu) |
JP (1) | JP3403203B2 (hu) |
KR (1) | KR100348585B1 (hu) |
CN (1) | CN1303998C (hu) |
AR (1) | AR005231A1 (hu) |
AT (2) | ATE233090T1 (hu) |
BR (2) | BR9610153A (hu) |
CA (1) | CA2230314C (hu) |
CO (1) | CO4750822A1 (hu) |
CY (3) | CY2468B1 (hu) |
CZ (1) | CZ294024B6 (hu) |
DE (4) | DE69632753T2 (hu) |
DK (2) | DK0850059T3 (hu) |
EG (1) | EG23826A (hu) |
ES (2) | ES2188782T3 (hu) |
FR (1) | FR05C0019I2 (hu) |
GB (1) | GB9518953D0 (hu) |
HU (2) | HU227397B1 (hu) |
IL (1) | IL122746A (hu) |
LU (1) | LU91163I2 (hu) |
MY (1) | MY125662A (hu) |
NL (1) | NL300190I2 (hu) |
NO (2) | NO314783B1 (hu) |
NZ (1) | NZ316924A (hu) |
PL (1) | PL185604B1 (hu) |
PT (1) | PT1245231E (hu) |
RU (1) | RU2163803C2 (hu) |
TR (1) | TR199800461T1 (hu) |
TW (1) | TW442300B (hu) |
WO (1) | WO1997009980A1 (hu) |
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US5233053A (en) * | 1989-03-17 | 1993-08-03 | Pfizer Inc. | Pyrrolidine derivatives |
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PT93637A (pt) * | 1989-04-20 | 1990-11-20 | Procter & Gamble | Metodo para o tratamento de desordens funcionais intestinais/colonicas, especialmente o sindrome de irritacao intestinal |
GB9400600D0 (en) * | 1994-01-14 | 1994-03-09 | Pfizer Ltd | Treatment of motion seckness |
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