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 method of treating a patient suffering from a psychological or psychiatric disorder selected from one or more of a group consisting of anxiety, stress, tension or sleep disturbance, comprising administering to the patient in need thereof an effective amount of a composition comprising as an active ingredient an extract of a plant or plants from family Mesembryanthemaceae, genus Sceletium , as a dual serotonin uptake inhibitor and PDE4 inhibitor, the extract including alkaloids mesembrenol and mesembrenone and having a total Mesembryanthemaceae alkaloid content, wherein combined content of mesembrenol and mesembrenone in the extract is greater than 80% (w/w) of the total Mesembryanthemaceae alkaloid content and mesembrine content in the extract is less than 15% (w/w) of the total Mesembryanthemaceae alkaloid content, wherein the composition is in unit dosage form, and wherein a unit dose of the composition contains 1 microgram to 1000 micrograms of the total Mesembryanthemaceae alkaloid content.
2. The method of claim 1 , wherein the mesembrine content in the extract is less than 8% (w/w) of the total alkaloid content.
3. The method of claim 2 , wherein the mesembrine content in the extract is less than 5% (w/w) of the total alkaloid content.
4. The method of claim 3 , wherein the extract includes trace amounts of mesembrine.
5. The method of claim 1 , wherein the extract includes alkaloid mesembranol, and wherein mesembranol content in the extract is not less than 1% of the total alkaloid content.
6. The method of claim 5 , wherein the mesembranol content in the extract is not less than 5% of the total alkaloid content.
7. The method of claim 5 , wherein the mesembranol content in the extract is not less than 7% of the total alkaloid content.
8. A method of claim 1 , in which the plant from which the extract is derived is Sceletium tortuosum (L.) N.E.Br.
9. The method 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.
10. The method of claim 9 , in which the total alkaloid content of the extract is between 0.20% and 0.50% (by weight) of the weight of the composition.
11. The method of claim 10 , in which the total alkaloid content of the extract is between 0.35% and 0.45% (by weight) of the weight of the composition.
12. The method of claim 1 , wherein the unit dose of the composition contains 4 micrograms to 200 micrograms of the total Mesembryanthemaceae alkaloid content.
13. The method of claim 1 , wherein the unit dose of the composition contains 6 micrograms to 100 micrograms of the total Mesembryanthemaceae alkaloid content.
14. The method of claim 1 , wherein the unit dose of the composition contains 20 micrograms to 200 micrograms of the total Mesembryanthemaceae alkaloid content.
15. The method of claim 1 , wherein the unit dose of the composition contains 40 micrograms to 120 micrograms of the total Mesembryanthemaceae alkaloid content.
16. The method of claim 1 , wherein the unit dose of the composition contains 2 micrograms to 20 micrograms of the total Mesembryanthemaceae alkaloid content.
17. The method of claim 1 , wherein the unit dose of the composition contains 6 micrograms to 12 micrograms of the total Mesembryanthemaceae alkaloid content.
18. The method of claim 1 , wherein the unit dose of the composition contains 5 micrograms to 500 micrograms of the total Mesembryanthemaceae alkaloid content.
19. The method of claim 1 , wherein the unit dose of the composition contains 20 micrograms to 100 micrograms of the total Mesembryanthemaceae alkaloid content.
20. The method of claim 1 , wherein administered daily dose of the total Mesembryanthemaceae alkaloid content is from 5 micrograms to 5 milligrams.
21. The method of claim 1 , wherein administered daily dose of the total Mesembryanthemaceae alkaloid content is from 20 micrograms to 200 micrograms.
22. The method of claim 1 , wherein the composition is administered orally.