Scopolamine Production

Abstract

The invention provides an improved method for the production of Scopolamine by extraction.

Claims

1. A method for the production of Scopolamine, which method includes the steps of: grinding plant material which contains Scopolamine; adding the grinded plant material to a Sulfuric acid solution and allowing to stand in the solution for 1 to 4 days, filtration separation of the acid solution from the plant material; repeating the previous steps with the residue plant material and combining the acidic filtrates; neutralising with a alkaline solution to a pH of between 7.5 and 9.5; addition of dichloromethane for the extraction of the alkaloids in the neutralised solution to the organic layer and allowing to stand for 1 to 4 days; separation of the bottom organic layer from the upper aqueous layer; evaporation of the dichloromethane solvent to obtain the coloured scopolamine rich extract; adding the scopolamine rich extract to dichloromethane solvent and mixing with a NaOH solution and separating the layers; and evaporation of the dichloromethane solvent to obtain the less coloured scopolamine rich extract.

2. The method for the production of Scopolamine as claimed in claim 1, wherein the Sulfuric acid solution is 1%.

3. The method for the production of Scopolamine as claimed in claim 1, wherein the Sulfuric acid solution is allowed to stand for 2 to 3 days.

4. The method for the production of Scopolamine as claimed in claim 2, wherein the Sulfuric acid solution is allowed to stand for 2 to 3 days.

5. The method for the production of Scopolamine as claimed in claim 1, wherein the alkaline solution is a sodium bicarbonate solution at a pH of between 8 and 9.

6. The method for the production of Scopolamine as claimed in claim 2, wherein the alkaline solution is a sodium bicarbonate solution at a pH of between 8 and 9.

7. The method for the production of Scopolamine as claimed in claim 3, wherein the alkaline solution is a sodium bicarbonate solution at a pH of between 8 and 9.

8. The method for the production of Scopolamine as claimed in claim 1, wherein the Dichloromethane is added immediately.

9. The method for the production of Scopolamine as claimed in claim 2, wherein the Dichloromethane is added immediately.

10. The method for the production of Scopolamine as claimed in claim 3, wherein the Dichloromethane is added immediately.

11. The method for the production of Scopolamine as claimed in claim 5, wherein the Dichloromethane is added immediately.

12. The method for the production of Scopolamine as claimed in claim 1, wherein the organic layer is allowed to stand for 2 to 3 days.

13. The method for the production of Scopolamine as claimed in claim 2, wherein the organic layer is allowed to stand for 2 to 3 days.

14. The method for the production of Scopolamine as claimed in claim 3, wherein the organic layer is allowed to stand for 2 to 3 days.

15. The method for the production of Scopolamine as claimed in claim 5, wherein the organic layer is allowed to stand for 2 to 3 days.

16. The method for the production of Scopolamine as claimed in claim 8, wherein the organic layer is allowed to stand for 2 to 3 days.

17. The method for the production of Scopolamine as claimed in claim 1, wherein the NaOH solution is 1%.

18. The method for the production of Scopolamine as claimed in claim 2, wherein the NaOH solution is 1%.

19. The method for the production of Scopolamine as claimed in claim 3, wherein the NaOH solution is 1%.

20. The method for the production of Scopolamine as claimed in claim 5, wherein the NaOH solution is 1%.

21. The method for the production of Scopolamine as claimed in claim 8, wherein the NaOH solution is 1%.

22. The method for the production of Scopolamine as claimed in claim 12, wherein the NaOH solution is 1%.

23. The method for the production of Scopolamine as claimed in claim 1, wherein the less coloured scopolamine rich extract is added to dichloromethane solvent and mixed with a 1% sodium bicarbonate solution and the layers separated and the dichloromethane solvent evaporated to obtain the final scopolamine rich extract.

24. The method for the production of Scopolamine as claimed in claim 2, wherein the less coloured scopolamine rich extract is added to dichloromethane solvent and mixed with a 1% sodium bicarbonate solution and the layers separated and the dichloromethane solvent evaporated to obtain the final scopolamine rich extract.

25. The method for the production of Scopolamine as claimed in claim 3, wherein the less coloured scopolamine rich extract is added to dichloromethane solvent and mixed with a 1% sodium bicarbonate solution and the layers separated and the dichloromethane solvent evaporated to obtain the final scopolamine rich extract.

26. The method for the production of Scopolamine as claimed in claim 5, wherein the less coloured scopolamine rich extract is added to dichloromethane solvent and mixed with a 1% sodium bicarbonate solution and the layers separated and the dichloromethane solvent evaporated to obtain the final scopolamine rich extract.

27. The method for the production of Scopolamine as claimed in claim 8, wherein the less coloured scopolamine rich extract is added to dichloromethane solvent and mixed with a 1% sodium bicarbonate solution and the layers separated and the dichloromethane solvent evaporated to obtain the final scopolamine rich extract.

28. The method for the production of Scopolamine as claimed in claim 12, wherein the less coloured scopolamine rich extract is added to dichloromethane solvent and mixed with a 1% sodium bicarbonate solution and the layers separated and the dichloromethane solvent evaporated to obtain the final scopolamine rich extract.

29. The method for the production of Scopolamine as claimed in claim 17, wherein the less coloured scopolamine rich extract is added to dichloromethane solvent and mixed with a 1% sodium bicarbonate solution and the layers separated and the dichloromethane solvent evaporated to obtain the final scopolamine rich extract.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0022] The invention is now described by way of example.

[0023] 500 Grams of Flos Daturae seeds were grinded and added to 1 500 ml of a 1% Sulfuric acid solution and allowed to stand in the solution for 2 days. The mixture was filtered and 700 ml of the acid solution was recovered. This step can preferably be repeated to increase the yield. The filtrate was neutralised with sodium bicarbonate to a pH of 9. A 1000 ml of dichloromethane was mixed with the filtrate and allowed to stand for 2 days. The bottom organic layer was separated from the upper aqueous layer and the dichloromethane solvent was evaporated using a roto evaporator to obtain the coloured scopolamine rich extract. Once off, adding the scopolamine rich extract to 1000 ml dichloromethane solvent and mixing with a 1% NaOH 1000 ml, solution and separating the layers. The dichloromethane solvent was again removed in a roto evaporator to obtain the less coloured scopolamine rich extract. The less coloured scopolamine rich extract was added to 1000 ml dichloromethane solvent and mixed with a 1000 ml 1% sodium bicarbonate solution and the layers were separated. This step is also once off. The dichloromethane solvent was evaporated to obtain 12 grams of the final scopolamine rich extract, which contains 70% scopolamine in a pharmaceutically acceptable mixture.

[0024] The use of sulphuric add in the first step removes fat soluble impurities. The long extraction time of 2 days improves the yield significantly and it appears that the conversion from organic acid to salt is relatively slow. The selective neutralisation to pH of 8 to 9 avoided neutralising other compounds and their subsequent extraction to yield a purer product. Again, longer than normal extraction time improved the yield and the further steps improved the purity compared to known extraction methods.

[0025] It shall be understood that the example is provided for illustrating the invention further and to assist a person skilled in the art with understanding the invention and is not meant to be construed as unduly limiting the reasonable scope of the invention.