IP Library Granted Patent US 7,550,628
Granted Patent B2
US 7,550,628 · App. 10/806,022 · Granted Jun 23, 2009

Process for preparing phenolic acid salts of gabapentin

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Quick Facts
Patent No.
US 7,550,628
App. No.
10/806,022
Granted
Jun 23, 2009
Kind
B2
Abstract

The present invention provides a novel process for preparation of the tannate salt of gabapentin for human and veterinary pharmaceutical use. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. However, the prior art neither discloses nor suggests the preparation of gabapentin tannate. The process for preparing gabapentin tannate includes the mixing of gabapentin and tannic acid together in the presence of one or more solvents. The method may further include the step of selecting the one or more solvents from a group consisting of purified water, ethanol, glycerin, propylene glycol, diethylether, methylene chloride, acetone, isopropyl alcohol and mixtures thereof. The process may also include the steps of isolating and purifying the tannate salt. This may be accomplished by filtration, drying, centrifugation and lyophilization. The process may utilize either natural or synthetic tannic acid.

Claims (15)

1. A process for preparing gabapentin tannate, comprising: mixing gabapentin and tannic acid to obtain gabapentin tannate wherein the tannic acid component is of either natural or synthetic origin, and wherein said gabapentin and said tannic acid are mixed together while maintaining a temperature of between about 15 to about 150 degrees C.

2. A process for preparing gabapentin tannate, comprising: mixing gabapentin and tannic acid to obtain gabapentin tannate wherein the tannic acid component is of either natural or synthetic origin, and wherein the weight ratio of said tannic acid to said gabapentin is between about 0.1:1 to about 10:1.

3. A process for preparing gabapentin tannate, comprising: mixing gabapentin and tannic acid to obtain gabapentin tannate wherein the tannic acid component is of either natural or synthetic origin, and wherein said mixing is performed while maintaining a pH of between about 2 to about 11.

4. The process of claim 1 , further comprising the step of isolating and purifying the gabapentin tannate.

5. The process of claim 4 , wherein said isolating and purifying is performed by a procedure selected from a group consisting of filtering, drying, centrifuging, and lyophilizing.

6. The process of claim 1 , wherein the gabapentin and tannic acid are mixed together in the presence of a solvent, and wherein the solvent is selected from a group consisting of purified water, ethanol, glycerin, propylene glycol, diethylether, methylene chloride, acetone, isopropyl alcohol, and mixtures thereof; and isolating and purifying the gabapentin tannate.

7. The process of claim 6 , wherein said isolating and purifying step is performed by a procedure selected from a group consisting of filtering, drying, centrifuging, and lyophilizing.

8. The process of claim 2 , further comprising the step of isolating and purifying the gabapentin tannate.

9. The process of claim 8 , wherein said isolating and purifying is performed by a procedure selected from a group consisting of filtering, drying, centrifuging, and lyophilizing.

10. The process of claim 3 , further comprising the step of isolating and purifying the gabapentin tannate.

11. The process of claim 10 , wherein said isolating and purifying is performed by a procedure selected from a group consisting of filtering, drying, centrifuging, and lyophilizing.

12. The process of claim 2 , wherein the gabapentin and tannic acid are mixed together in the presence of a solvent, and wherein the solvent is selected from a group consisting of purified water, ethanol, glycerin, propylene glycol, diethylether, methylene chloride, acetone, isopropyl alcohol, and mixtures thereof; and isolating and purifying the gabapentin tannate.

13. The process of claim 12 , wherein said isolating and purifying step is performed by a procedure selected from a group consisting of filtering, drying, centrifuging, and lyophilizing.

14. The process of claim 3 , wherein the gabapentin and tannic acid are mixed together in the presence of a solvent, and wherein the solvent is selected from a group consisting of purified water, ethanol, glycerin, propylene glycol, diethylether, methylene chloride, acetone, isopropyl alcohol, and mixtures thereof; and isolating and purifying the gabapentin tannate.

15. The process of claim 14 , wherein said isolating and purifying step is performed by a procedure selected from a group consisting of filtering, drying, centrifuging, and lyophilizing.

Assignments (2)
SECURITY AGREEMENT Recorded Dec 14, 2005
From: KIEL LABORATORIES, INC.
To: WACHOVIA BANK, NATIONAL ASSOCIATION
Reel/Frame 017115/0658 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 27, 2004
From: KIEL, JEFFREY S.; THOMAS, H. GREG; MANI, NARASIMHAN
To: KIEL LABORATORIES, INC.
Reel/Frame 015089/0420 →