Title:
PHARMACEUTICAL FORMULATIONS WITH DIFFERENT RELEASE TIMES
Document Type and Number:
WIPO Patent Application WO/2001/013898
Kind Code:
A2
Abstract:
The application discloses novel pharmaceutical formulations adapted for delaying the release of a pharmaceutically active agent. A delayed-release drug formulation encapsulates the active ingredient, which may be applied to microparticles or in tableted form, in a release-delaying coat comprising polymeric materials of predetermined swelling/permeability characteristics. In particular, acrylate and/or acrylic acid polymer blends modified with ionic groups may be used. One preferred embodiment uses a polymer of pH dependent permeability as a more permeable element of the coat. The delayed-release formulations are deployed in a single dosage form together with instant release or sustained release formulations, so that a unit dosage form, preferably an oral dosage form, can effectively administer two doses to a patient at different times.
Inventors:
ANDINA CHRISTIAN (IE)
FANNING NIALL (IE)
PALMER FIONA (IE)
STARK PAUL (IE)
FANNING NIALL (IE)
PALMER FIONA (IE)
STARK PAUL (IE)
Application Number:
PCT/GB2000/003309
Publication Date:
March 01, 2001
Filing Date:
August 29, 2000
Export Citation:
Assignee:
ELAN CORP PLC (IE)
ANDINA CHRISTIAN (IE)
FANNING NIALL (IE)
PALMER FIONA (IE)
STARK PAUL (IE)
ANDINA CHRISTIAN (IE)
FANNING NIALL (IE)
PALMER FIONA (IE)
STARK PAUL (IE)
International Classes:
A61K9/16; A61K9/20; A61K9/28; A61K9/48; A61K9/50; A61K9/52; A61K39/39; (IPC1-7): A61K9/50; A61K9/16; A61K9/20; A61K9/28; A61K9/48
Domestic Patent References:
| WO2000019985A2 | 2000-04-13 |
Foreign References:
| US5326570A | 1994-07-05 | |||
| US5470584A | 1995-11-28 | |||
| US5158777A | 1992-10-27 |
Attorney, Agent or Firm:
Stoner, Patrick G. (Mewburn Ellis York House 23 Kingsway London
WC2B 6HP, GB)
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Claims:
CLAIMS:
| 1. | A dosage form containing pharmaceutically active agent in two or more different formulations having different respective release times for the pharmaceutically active agent under enteric conditions. |
| 2. | A dosage form according to claim 1 in which the different formulations contain the same pharmaceutically active agent. |
| 3. | A dosage form according to claim 1 or 2 in which one set formulation is an instant release formulation and another said formulation is a delayed release formulation. |
| 4. | A dosage form according to any one of the preceding claims in which one said formulation is a sustained release formulation and another said formulation is a delayed release formulation. |
| 5. | A dosage form according to claim 3 or claim 4 in which the delayed release formulation has the pharmaceutically active agent surrounding by a release delaying coat of polymeric material. |
| 6. | A dosage form according to claim 5 in which the releasedelaying coat comprises a blend of two polymers having different permeabilities. |
| 7. | A dosage form according to claim 6 in which a more soluble of the two polymers is an acrylate or acrylic acid polymer modified with ionic groups. |
| 8. | A dosage form according to claim 6 or claim 7 in which the more soluble of the two polymers has a pH dependent permeability, being more soluble under alkaline conditions than under acidic conditions. |
| 9. | A dosage form according to any one of the preceding claims in which one or more of said different formulations is/are provided as a plurality of particulates, a plurality of the particulates of the respective formulation being contained in a unit dosage form. |
| 10. | A dosage form according to claim 9 which has a capsule containing said plural particulates. |
| 11. | A delayed release pharmaceutical dosage form comprising pharmaceutically active agent and a release modifying coating containing a blend of polymeric materials having different permeabilities, a more permeable of the polymeric materials having a pH dependent permeability, being more permeable under alkaline conditions than under acidic conditions. |
| 12. | A delayed release dosage form according to claim 11 in which said more permeable polymeric material comprises an acrylate and/or acrylic acid polymer, modified with ionic groups such as quaternary ammonium groups. |
| 13. | A method comprising the preparation of a dosage form according to any one of claims 1 to 12. |
| 14. | A method of administering a delayed dose of pharmaceutically active agent, or plural temporally spaced doses of pharmaceutically active agent, comprising administering a single dosage form according to any one of claims 1 to 12. |
Description:
INTERNATIONAL SEARCH REPORT Int. tionaí Appíication No PCT/GB 00/03309 C. (Continuation) DOCUMENTS CONSIDERED TO BE RELEVANT Category ° Citation of document, with indication, where appropriate, of the relevant passages Relevant to claim No. P, X WO 00 19985 A (NOVARTIS) 1-3,5,9, 13 April 2000 (2000-04-13) 13,14 claims 1,4-6,11 1 INTERNATIONAL SEARCH r , , -------) lntt ional Application No PCT/GB 00/03309 Patent document Publication Patent family Publication cited in search report date member (s) date US 5326570 A 05-07-1994 AT 185268 T 15-10-1999 CA 2114014 A 24-01-1993 DE 69230112 D 11-11-1999 DE 69230112 T 02-03-2000 DK 660705 T 20-12-1999 EP 0660705 A 05-07-1995 ES 2137948 T 01-01-2000 GR 3031448 T 31-01-2000 JP 6511484 T 22-12-1994 WO 9301804 A 04-02-1993 US 5912013 A 15-06-1999 US 5912013 A 15-06-1999 US 5470584 A 28-11-1995 US 5439689 A 08-08-1995 US 5286497 A 15-02-1994 AT 147982 T 15-02-1997 AU 653223 B 22-09-1994 AU 1632692 A 26-11-1992 CA 2068980 A 21-11-1992 DE 69216910 D 06-03-1997 DE 69216910 T 22-05-1997 DK 514814 T 10-02-1997 EP 0514814 A 25-11-1992 ES 2099764 T 01-06-1997 FI 922270 A 21-11-1992 GR 3022927 T 30-06-1997 IL 101896 A 04-08-1996 JP 5178747 A 20-07-1993 KR 244010 B 02-03-2000 NO 921973 A 23-11-1992 NZ 242730 A 27-09-1994 ZA 9203474 A 27-01-1993 ZA 9203474 A 27-01-1993 US 5158777 A 27-10-1992 NONE WO 0019985 A 13-04-2000 AU 6332199 A 26-04-2000