Parenteral Formulation
The present invention relates to parenteral formulations, and kits and methods suitable for the preparation of such parenteral formulations. The parenteral formulations comprise a freebase of a deuterium-substituted dimethyltryptamine optionally substituted at position 4 or 5 with acetoxy or methoxy. The parenteral formulations also comprise a biocompatible excipient. Such formulations are suitable for inhalation and have uses in the treatment of psychiatric or neurological disorders. They are metabolised more slowly than their protio analogues, allowing for a longer lasting therapeutic effect.
1 . A parenteral formulation comprising a freebase of a deuterium-substituted dimethyltryptamine optionally substituted at position 4 or 5 with acetoxy or methoxy, and a biocompatible excipient.
2 . The formulation of claim 1 , wherein the formulation is suitable for inhalation.
3 . The formulation of claim 1 , wherein the freebase is of Formula I
wherein:
one x H is D and the other is H or D;
each Y H is independently selected from H and D; and
R 4 and R 5 are both H or one of R 4 and R 5 is H and the other is acetoxy (—OC(O)CH 3 ) or methoxy (—OCH 3 ).
4 . The formulation of claim 3 wherein both Y H are H.
5 . The formulation of claim 3 wherein R 4 and R 5 are both H.
6 . The formulation of claim 3 wherein R 4 is acetoxy and R 5 is H.
7 . The formulation of claim 3 wherein R 4 is H and R 5 is methoxy.
8 . The formulation of claim 1 wherein the freebase has a purity of greater than or equal to 99% when measured by HPLC.
9 .- 33 (canceled)
34 . The formulation of claim 1 further comprising a solvent comprising propylene glycol, glycerine and polyethylene glycol, or a mixture thereof.
35 . The formulation of claim 34 , wherein the solvent is a mixture of propylene glycol and glycerine in a ratio of from about 50:50 to about 30:70 by weight.
36 . The formulation of claim 1 further comprising a taste-masking agent.
37 . The formulation of claim 1 wherein the formulation has an oxygen content of less than 2 ppm.
38 . A kit suitable for preparing a parenteral formulation of claim 3 , said kit comprising:
a container adapted to prevent penetration of ultraviolet light.
39 . A method of preparing a parenteral formulation of claim 1 , comprising contacting a freebase of a deuterium-substituted dimethyltryptamine optionally substituted at position 4 or 5 with acetoxy or methoxy, with a biocompatible excipient.
40 . The method of claim 39 wherein the freebase is dissolved in a solvent selected from propylene glycol, glycerine and polyethylene glycol, or a mixture thereof to form a solution.
41 . The method of claim 40 wherein the solvent is a mixture of propylene glycol and glycerine in a ratio of from about 50:50 to about 30:70 by weight.
42 . The method of claim 40 further comprising stirring the freebase in the solvent at a temperature of from about 25° C. to about 50° C.
43 . The method of claim 40 further comprising sparging the solution resultant from the contacting with an inert gas.
44 . A method of treating a psychiatric or neurological disorder comprising pulmonary administration to a patient in need thereof of the parenteral formulation of claim 1 .
45 . The method of claim 44 wherein the psychiatric or neurological disorder is selected from the group consisting of (i) an obsessive compulsive disorder, (ii) a depressive disorder, (iii) an anxiety disorder, (iv) substance abuse, and (v) an avolition disorder.