Sceletium extract and uses thereof
A composition including as an active ingredient an extract of a plant of the family Mesembryanthemaceae with mesembrenol and mesembrenone as the two major alkaloids present. The invention also relates to the use of the composition as a PDE4 inhibitor and as a serotonin-uptake inhibitor, preferably applied in formulations for the use of the composition as a dual serotonin-uptake inhibitor and PDE4 inhibitor. The invention extends to compositions, such as pharmaceutical compositions or compositions used as dietary supplements, the total alkaloid content of which includes at least 80% (w/w) combined content of mesembrenol and mesembrenone, less than 5% (w/w) mesembrine, and at least 7% (w/w) mesembranol.
1. A composition, in unit dosage form, for reducing one or more conditions selected from the group consisting of anxiety, stress, tension, sleep disturbance, and depression in a patient in need thereof, said composition comprising an effective amount of a Sceletium tortuosum extract, wherein the extract contains the alkaloids mesembrenol and mesembrenone, wherein combined content of mesembrenol and mesembrenone is greater than 80% (w/w) of the total alkaloid content in the extract, wherein the content of the alkaloid mesembrine is less than 15% (w/w) of the total alkaloid content in the extract, and wherein the unit dosage form is selected from the group consisting of an aqueous-ethanolic tincture, a tablet, an enteric coated tablet, a capsule, a dissolvable wafer, a lotion, a cream, an ointment, and a skin patch.
2. The composition of claim 1 , wherein the mesembrine content in the extract is less than 8% (w/w) of the total alkaloid content.
3. The composition of claim 2 , wherein the mesembrine content in the extract is less than 5% (w/w) of the total alkaloid content.
4. The composition of claim 3 , wherein the extract includes trace amounts of mesembrine.
5. The composition of claim 1 , wherein the extract further includes alkaloid mesembranol, and wherein mesembranol content in the extract is not less than 1% of the total alkaloid content.
6. The composition of claim 5 , wherein the mesembranol content in the extract is not less than 5% of the total alkaloid content.
7. The composition of claim 5 , wherein the mesembranol content in the extract is not less than 7% of the total alkaloid content.
8. The composition of claim 1 , in which the total alkaloid content of the extract is between 0.20% and 0.60% (by weight) of weight of the composition.
9. The composition of claim 8 , in which the total alkaloid content of the extract is between 0.20% and 0.50% (by weight) of the weight of the composition.
10. The composition of claim 9 , in which the total alkaloid content of the extract is between 0.35% and 0.45% (by weight) of the weight of the composition.
11. The composition of claim 1 , wherein the composition inhibits serotonin uptake and PDE-4 activity in the patient.
12. The composition of claim 11 , wherein the administration regimen comprises administering a daily dose of the total Mesembrvanthemaceae alkaloid content from 5 micrograms to 5 milligrams.
13. The composition of claim 1 , wherein the unit dose of the composition contains 1.0 microgram to 100 micrograms of the total alkaloid content in the extract.
14. The composition of claim 13 , wherein the unit dosage form is an oral unit dosage form.
15. The composition of claim 1 , wherein the composition further comprises a pharmaceutically acceptable excipient.
16. A method of inhibiting serotonin uptake and PDE4 activity in a patient in need thereof comprising administering to the patient effective amount of the composition of claim 1 .
17. The method of claim 16 , wherein a daily dose of the administered composition contains a total alkaloid content from 5 micrograms to 5 milligrams.