Orally administered dosage forms of GABA analog prodrugs having reduced toxicity
AssigneeXenoPort, Inc.
InventorsKenneth C. Cundy, Mark A. Gallop
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Abstract
The present invention provides an extended release oral dosage form of prodrugs of gabapentin and other GABA analogs, which dosage forms exhibit reduced toxicity. The dosage forms are particularly useful in administering those prodrugs of gabapentin and other GABA analogs that are metabolized to form an aldehyde. The dosage forms of the invention are useful for treating or preventing diseases and/or disorders for which the parent gabapentin or other GABA analog are known to be therapeutically effective.
Claims29
A method of reducing toxicity of an orally administered therapeutic GABA analog, comprising:
- formulating the GABA analog as a prodrug comprised of the therapeutic GABA analog covalently bound to a cleavable promoiety;
- placing the prodrug in a sustained release oral dosage form;
- introducing the dosage form into the intestinal lumen of a patient by having the patient swallow the dosage form;
- releasing the prodrug gradually into the intestinal lumen of the patient over a period of hours;
- and
- cleaving the promoiety from the prodrug to provide a therapeutic concentration of the GABA analog in the plasma of the patient, wherein the dosage form releases from 0 to 20% of the prodrug in 0 to 2 hours, from 20 to 50% of the prodrug in 2 to 12 hours, from 50 to 85% of the prodrug in 3 to 20 hours and greater than 75% of the prodrug in 5 to 18 hours.
A method of orally administering a GABA analog prodrug, comprising:
- formulating the GABA analog as a prodrug comprised of the therapeutic GABA analog covalently bound to a cleavable promoiety;
- placing the prodrug in a sustained release oral dosage form;
- introducing the dosage form into the intestinal lumen of a patient by having the patient swallow the dosage form;
- releasing the prodrug gradually from the swallowed dosage form into the intestinal lumen of the patient over a period of hours;
- and
- allowing the GABA analog to be cleaved from the promoiety after said swallowing to provide a therapeutic concentration of the GABA analog in the plasma of the patient wherein the dosage form releases from 0 to 20% of the prodrug in 0 to 2 hours, from 20 to 50% of the prodrug in 2 to 12 hours, from 50 to 85% of the prodrug in 3 to 20 hours and greater than 75% of the prodrug in 5 to 18 hours.
Dependencies are inferred from the claim text.