Gastric retained gabapentin dosage form
View Patent ↗A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.
1. A dosage form, comprising:
a matrix comprising gabapentin, wherein upon ingestion of the dosage form by a human subject gabapentin is released from the matrix into the upper gastrointestinal tract over about 5-12 hours at a rate sufficient to achieve a lower maximum plasma concentration than that provided by an immediate release dosage form comprising an equal amount of gabapentin, and bioavailability of gabapentin is at least 80% of that provided by the immediate release dosage form comprising an equal amount of gabapentin as measured by the area under the plasma concentration-time curve, AUC inf .
2. The dosage form of claim 1 , wherein the time to reach maximum plasma concentration is at least 5.6 hours±34.9%.
3. The dosage form of claim 1 , comprising a dose of gabapentin of between about 300-600 mg.
4. The dosage form of claim 1 , wherein the matrix is a polymer matrix.
5. The dosage form of claim 4 , wherein the polymer matrix is comprised of a swellable, hydrophilic polymer.
6. The dosage form of claim 5 , wherein the gabapentin is released from the polymer matrix by diffusion.
7. The dosage form of claim 1 , wherein the gabapentin is released from the matrix at a rate sufficient to achieve a maximum plasma concentration of at least about 3 μg/mL.
8. The dosage form of claim 1 , wherein the ratio of the maximum plasma concentration to the plasma concentration at 15 hours after administration is no more than about 2.
9. A dosage form, comprising:
a matrix comprising 300 mg or 600 mg gabapentin, wherein upon ingestion by a human subject of one 600 mg dosage form or upon ingestion of two 300 mg dosage forms gabapentin is released from the matrix into the upper gastrointestinal tract over about 5-12 hours at a rate sufficient to achieve a lower maximum plasma concentration than that provided by an immediate release dosage form comprising an equal amount of gabapentin, and bioavailability of gabapentin is at least 80% of that provided by the immediate release dosage form comprising an equal amount of gabapentin as measured by the area under the plasma concentration-time curve, AUC inf .
10. The dosage form of claim 9 , wherein the time to reach maximum plasma concentration is at least 5.6 hours±34.9%.
11. The dosage form of claim 9 , wherein the matrix is a polymer matrix.
12. The dosage form of claim 11 , wherein the polymer matrix is comprised of a swellable, hydrophilic polymer.
13. The dosage form of claim 12 , wherein the gabapentin is released from the polymer matrix by diffusion.
14. The dosage form of claim 9 , wherein the gabapentin is released from the matrix at a rate sufficient to achieve a maximum plasma concentration of at least about 3 μg/mL.
15. A method of treating a condition responsive to a therapeutic dose of gabapentin, comprising:
orally administering to a human subject a dosage form comprising a matrix comprising gabapentin, wherein upon ingestion of the dosage form gabapentin is released from the matrix into the upper gastrointestinal tract over about 5-12 hours at a rate sufficient to achieve a lower maximum plasma concentration than that provided by an immediate release dosage form comprising an equal amount of gabapentin, and bioavailability of gabapentin is at least 80% of that provided by the immediate release dosage form comprising an equal amount of gabapentin as measured by the area under the plasma concentration-time curve, AUC inf .
16. The method of claim 15 , wherein the time to reach maximum plasma concentration is at least 5.6 hours±34.9%.
17. The method of claim 15 , wherein the matrix is a polymer matrix.
18. The method of claim 17 , wherein the polymer matrix is comprised of a swellable, hydrophilic polymer.
19. The method of claim 15 , wherein the condition is pain.
20. The method of claim 15 , wherein the condition is neuropathic pain.
21. The method of claim 15 , wherein the gabapentin is released from the matrix at a rate sufficient to achieve a maximum plasma concentration of at least about 3 μg/mL.
22. A method of treating a condition responsive to a therapeutic dose of gabapentin, comprising:
orally administering to a human subject a dosage form comprising a matrix comprising gabapentin, wherein gabapentin is released from the matrix into the upper gastrointestinal tract over about 5-12 hours at a rate sufficient to achieve a longer time to the maximum plasma concentration than that provided by an immediate release dosage form comprising an equal amount of gabapentin, and bioavailability of gabapentin is at least 80% of that provided by the immediate release dosage form comprising an equal amount of gabapentin as measured by the area under the plasma concentration-time curve, AUC inf .
23. The method of claim 22 , wherein the matrix is a polymer matrix.
24. The method of claim 23 , wherein the polymer matrix is comprised of a swellable, hydrophilic polymer.
25. The method of claim 22 , wherein the condition is pain.
26. The method of claim 25 , wherein the condition is neuropathic pain.
27. The method of claim 22 , wherein the gabapentin is released from the matrix at a rate sufficient to achieve a maximum plasma concentration of at least about 3 μg/mL.