CONTROLLED RELEASE LIPOIC ACID
A controlled release formulation of lipoic acid is disclosed. The lipoic acid is combined with excipient materials in such a way that those materials provide for gradual release of the lipoic acid in a manner which makes it possible to substantially increase the period of time over which therapeutic levels of lipoic acid are maintained relative to a quick release formulation. These features make it possible to use lipoic acid to reduce serum glucose levels and maintain those levels over time thereby obtaining a range of desired therapeutic results.
1 .- 20 . (canceled)
21 . A controlled release oral dosage formulation, comprising:
a therapeutically effective amount of an orally active antidiabetic chosen from a sulfonylurea, a biguanide and a thiazolidinedione;
a therapeutically effective amount of lipoic acid; and
an excipient material.
22 . The formulation of claim 21 , wherein the formulation is characterized by releasing the lipoic acid in a manner so as to increase a period of time over which a therapeutic level of lipoic acid is maintained as compared to a quick release formulation
23 . The formulation of claim 22 , wherein the releasing is in an manner which maintains the therapeutic level of lipoic acid for a period which is 10% or more longer as compared to a quick release formulation.
24 . The formulation of claim 22 wherein the releasing is in a manner which maintains the therapeutic level of lipoic acid for a period which is 50% or more longer as compared to a quick release formulation.
25 . The formulation of claim 22 , wherein the releasing is in an manner which maintains the therapeutic level of lipoic acid for a period which is 100% or more longer as compared to a quick release formulation.
26 . The formulation of claim 22 , wherein the releasing is in an manner which maintains the therapeutic level of lipoic acid for a period which is 200% or more longer as compared to a quick release formulation.
27 . The formulation of claim 22 ,wherein the releasing is sufficiently slow that a maximum level of lipoic acid obtained is less as compared to a maximum level obtained with a quick release formulation.
28 . The formulation of claim 21 , wherein the orally active antidiabetic is metformin hydrochloride.
29 . The formulation of claim 22 , wherein the lipoic acid is present as a racemic mixture and the therapeutic level is maintained over a period of four hours or more.
30 . The formulation of claim 22 , wherein the lipoic acid is present as substantially pure R-(+) enantiomer and the therapeutic level is maintained over a period of four hours or more.
31 . The formulation of claim 22 , wherein the releasing of the lipoic acid is at a rate of about 25% or less per hour after an initial release rate within 30 minutes following administration as compared to a quick release formulation.
32 . The formulation of claim 22 , wherein the releasing of the lipoic acid is at a rate of about 50% or less per hour after an initial release rate within 30 minutes following administration as compared to a quick release formulation.
33 . A method of treating a human patient, comprising:
administering to a human patient a controlled release formulation of an orally active antidiabetic chosen from a sulfonylurea, a biguanide and a thiazolidinedione, and lipoic acid.
34 . The method of claim 33 , wherein the formulation is characterized by maintaining a therapeutic level of lipoic acid in the patient's circulatory system over a period of time greater than that obtained with a quick release formulation.
35 . The method of claim 34 , further comprising:
repeating the administering on three or more consecutive days thereby maintain a therapeutic level of lipoic acid in the patient's circulatory system over a therapeutically effective period of time on three or more consecutive days.
36 . The method of claim 34 , wherein the therapeutic level is maintained over a period of time which is 10% or more than that obtained with a quick release formulation and further wherein the repeating is over thirty or more consecutive days.
37 . The method of claim 34 , wherein the therapeutic level is maintained over a period of time which is 100% or more than that obtained with a quick release formulation and further wherein the repeating is over thirty or more consecutive days.
38 . The method of claim 34 , wherein the therapeutic level is a level sufficient to obtain measurable vasodilation in a human patient.
39 . The method of claim 34 , wherein the therapeutic level is a level sufficient to obtain a measurable reduction in a human patient's serum glucose level.
40 . A method of reducing a human patient's serum glucose level, comprising:
administering a therapeutically effective amount of an orally active antidiabetic selected from the group consisting of a sulfonylurea, a biguanide and a thiazolidinedione; and
administering an oral controlled release formulation of lipoic acid.
41 . The method of claim 40 , further comprising:
repeatedly administering the antidiabetic and the lipoic acid on a daily basis for three or more days.
42 . The method of claim 41 , wherein the antidiabetic is metformin hydrochloride which is administered in an amount in a range of about 500 mg to about 1,000 mg per day.