Claims
- 1. A pharmaceutical formulation comprising:
a core having a rapid release DFMO-containing granules and a slow release granule, said granules comprising (+)-DFMO, (−)-DFMO or a defined ratio thereof, or pharmaceutically acceptable salts thereof; and an outer layer surrounding said core comprising a pH responsive coating.
- 2. The pharmaceutical formulation of claim 1 wherein the rapid release granule is capable of releasing DFMO within two hours after dissolution of the outer layer and the slow release granule is capable of releasing DFMO within eight hours after dissolution of the outer layer in an animal.
- 3. The pharmaceutical formulation of claim 1 or 2 wherein the pH responsive coating is further defined as responsive to a pH of about 6.0.
- 4. An oral solid multiple drug release pharmaceutical formulation comprising:
a core comprising DFMO-containing granules; and a pH-responsive outer layer surrounding the core; wherein the granules comprise (+)-DFMO, (−)-DFMO or a defined ratio thereof, or pharmaceutically acceptable salts thereof.
- 5. The pharmaceutical formulation of claim 1 wherein the DFMO-containing granules are further defined as comprising:
a gastric release granule; an enteric release granule; and a colorectal release granule, wherein each granule comprises (+)-DFMO, (−)-DFMO or a defined ratio thereof, or pharmaceutically acceptable salts thereof.
- 6. A pharmaceutical formulation core comprising:
a rapid release granule having a binder, and a slow release granule having a polymer, each granule comprising (+)-DFMO, (−)-DFMO or a defined ratio thereof or pharmaceutically acceptable salts thereof; and an outer layer surrounding said granule comprising a pH-responsive coating, said pH responsive coating providing for release of the core granules at or above a pH of about 6.
- 7. A multiple drug release profile pharmaceutical formulation comprising:
a core comprising a gastric release granule having a binder and an excipient; an enteric release granule comprising a polymer suitable for enteric drug delivery; a colorectal release granule comprising a polymer which dissolves at a pH greater than or equal to about 6; and an outer layer surrounding the core, wherein each granule comprises a therapeutic amount of (+) DFMO, (−)-DFMO pharmaceutically acceptable salts thereof.
- 8. The pharmaceutical formulation of claim 1, 2 or 6 wherein the formulation is capable of providing a detectable plasma concentration of DFMO in the range of about 0.1 μM to about 1000 μM.
- 9. The sustained release pharmaceutical formulation of claim 8 wherein the formulation is capable of providing a detectable plasma concentration of DFMO in the range of about 1 μM to about 100 μM.
- 10. The solid multiple drug release profile pharmaceutical formulation of claim 4 wherein the formulation is capable of providing a plasma concentration level of DFMO of about 0.1 μM to about 1000 μM.
- 11. The solid multiple drug release pharmaceutical formulation of claim 4 further defined as an oral solid multiple drug release pharmaceutical formulation, wherein the detectable plasma level of DFMO is about 1 μM to about 100 μM.
- 12. A multi-coated pharmaceutical formulation comprising a core pellet of DFMO-containing granules in a slow-release matrix,
a first coat of a colonic protective material; a second coat comprising a pore forming agent;
a rapidly dissolving polymeric material and DFMO; a third coat comprising an acid resistant polymer; and a fourth coat comprising a pore-forming agent and DFMO.
- 13. The multi-coated pharmaceutical formulation of claim 12 wherein the DFMO-containing granules comprise coated DFMO-containing granules and uncoated DFMO-containing granules.
Priority Claims (4)
Number |
Date |
Country |
Kind |
PCT/US97/20424 |
Oct 1997 |
US |
|
97946915.2 |
Oct 1997 |
EP |
|
2/241,896 |
Oct 1997 |
CA |
|
10-520855 |
Oct 1997 |
JP |
|
Parent Case Info
[0001] This application is related to PCT No. US97/20424, filed Oct. 31, 1997, designating the United States, the EP Application No. 97946915.2, filed Oct. 31, 1997, the Canadian Application No. 2/241,896, filed Oct. 31, 1997, the Japanese Application No. 10-520855, filed Oct. 31, 1997, and the Mexican Application No. 985376, filed Jul. 1, 1998.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60030266 |
Nov 1996 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
09210345 |
Dec 1998 |
US |
Child |
09927772 |
Aug 2001 |
US |