IL312859A - Injectable and inhalable formulations - Google Patents
Injectable and inhalable formulationsInfo
- Publication number
- IL312859A IL312859A IL312859A IL31285924A IL312859A IL 312859 A IL312859 A IL 312859A IL 312859 A IL312859 A IL 312859A IL 31285924 A IL31285924 A IL 31285924A IL 312859 A IL312859 A IL 312859A
- Authority
- IL
- Israel
- Prior art keywords
- formulation
- dimethyltryptamine
- salt
- compound
- optionally substituted
- Prior art date
Links
- 238000009472 formulation Methods 0.000 title claims 64
- 239000000203 mixture Substances 0.000 title claims 64
- -1 dimethyltryptamine compound Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 23
- 238000000034 method Methods 0.000 claims 16
- 239000003795 chemical substances by application Substances 0.000 claims 12
- 239000002585 base Substances 0.000 claims 11
- 239000012929 tonicity agent Substances 0.000 claims 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 10
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims 9
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical group [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 9
- 239000003002 pH adjusting agent Substances 0.000 claims 9
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 6
- 239000012458 free base Substances 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 4
- DMULVCHRPCFFGV-UHFFFAOYSA-N N,N-dimethyltryptamine Chemical compound C1=CC=C2C(CCN(C)C)=CNC2=C1 DMULVCHRPCFFGV-UHFFFAOYSA-N 0.000 claims 4
- 208000012902 Nervous system disease Diseases 0.000 claims 4
- 208000020016 psychiatric disease Diseases 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- 150000001860 citric acid derivatives Chemical class 0.000 claims 3
- 239000000843 powder Substances 0.000 claims 3
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-L Phosphate ion(2-) Chemical compound OP([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-L 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical group [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 2
- 159000000021 acetate salts Chemical class 0.000 claims 2
- 235000011054 acetic acid Nutrition 0.000 claims 2
- 239000007864 aqueous solution Substances 0.000 claims 2
- 235000015165 citric acid Nutrition 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000001530 fumaric acid Substances 0.000 claims 2
- 235000011087 fumaric acid Nutrition 0.000 claims 2
- 238000010255 intramuscular injection Methods 0.000 claims 2
- 239000007927 intramuscular injection Substances 0.000 claims 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims 2
- 238000001671 psychotherapy Methods 0.000 claims 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- JWDYCNIAQWPBHD-UHFFFAOYSA-N 1-(2-methylphenyl)glycerol Chemical compound CC1=CC=CC=C1OCC(O)CO JWDYCNIAQWPBHD-UHFFFAOYSA-N 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010002942 Apathy Diseases 0.000 claims 1
- 239000007848 Bronsted acid Substances 0.000 claims 1
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 claims 1
- 208000020401 Depressive disease Diseases 0.000 claims 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 1
- 208000001613 Gambling Diseases 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- YZCKVEUIGOORGS-IGMARMGPSA-N Protium Chemical compound [1H] YZCKVEUIGOORGS-IGMARMGPSA-N 0.000 claims 1
- 241000720974 Protium Species 0.000 claims 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 1
- 239000008186 active pharmaceutical agent Substances 0.000 claims 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 239000013011 aqueous formulation Substances 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 239000006184 cosolvent Substances 0.000 claims 1
- 229910052805 deuterium Inorganic materials 0.000 claims 1
- 239000008121 dextrose Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940088679 drug related substance Drugs 0.000 claims 1
- 238000001035 drying Methods 0.000 claims 1
- 238000004108 freeze drying Methods 0.000 claims 1
- 239000000174 gluconic acid Substances 0.000 claims 1
- 235000012208 gluconic acid Nutrition 0.000 claims 1
- 238000004128 high performance liquid chromatography Methods 0.000 claims 1
- 239000011261 inert gas Substances 0.000 claims 1
- 239000004310 lactic acid Substances 0.000 claims 1
- 235000014655 lactic acid Nutrition 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000003755 preservative agent Substances 0.000 claims 1
- 230000002335 preservative effect Effects 0.000 claims 1
- 230000001337 psychedelic effect Effects 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 201000009032 substance abuse Diseases 0.000 claims 1
- 231100000736 substance abuse Toxicity 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 239000011975 tartaric acid Substances 0.000 claims 1
- 235000002906 tartaric acid Nutrition 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0078—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Addiction (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dispersion Chemistry (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Claims (54)
1.PCT/EP2022/0824
2.CLAIMS 1. A pharmaceutical formulation suitable for intramuscular injection and/or nebuliser inhalation, comprising a salt of an optionally substituted dimethyltryptamine compound, a base agent, water and optionally a buffer which is separate to the salt; wherein the formulation has a pH of from about 5 to about 6.5, a concentration of about 10 mg/ml as freebase or greater, and an osmolality of from about 250 to about 350 mOsm/Kg; and wherein the formulation comprises a dose of the optionally substituted dimethyltryptamine compound within a volume of ml or less. 2. The formulation of claim 1, wherein the formulation has a pH of from about 5 to about 6.
3. The formulation of claim 1 or claim 2, wherein the formulation is suitable for intramuscular injection.
4. The formulation of any preceding claim, wherein the formulation comprises an effective dose of an optionally substituted dimethyltryptamine compound for use in psychedelic assisted therapy within a volume of 5 ml or less.
5. The formulation of any preceding claim, wherein the volume is 3 ml or less.
6. The formulation of any preceding claim, wherein the volume is 2.5 ml or less.
7. The formulation of any preceding claim, wherein the formulation has an osmolality of from about 275 to about 325 mOsm/Kg.
8. The formulation of any one of claims 1 to 7, wherein the salt of the optionally substituted dimethyltryptamine compound comprises a Brønsted acid having a pKa of from about 3 to about 5 and a compound of Formula IB: PCT/EP2022/0824 Formula IB wherein: R1b is independently selected from –R4b, -OH, -OR4b, -O(CO)R4b, monohydrogen phosphate, -F, -Cl, -Br and –I; n is selected from 0, 1, 2, 3 or 4; R2b is C(xbH)3; R3b is C(xbH)3; each R4b is independently selected from C1-C4alkyl; and each xbH, ybH and zH is independently selected from protium or deuterium.
9. The formulation of claim 8, wherein the salt of the optionally substituted dimethyltryptamine compound comprises a compound of Formula IB, wherein n is 0; or n is 1 and R1b is in the 4- or 5-position.
10. The formulation of claim 8 or claim 9, wherein the salt of the optionally substituted dimethyltryptamine compound comprises a compound of Formula IB, wherein each R1b is independently selected from -OH, -OMe, -OCD3, -OAc, -O(CO)Me, and monohydrogen phosphate.
11. The formulation of any one of claims 8 to 10, wherein the salt of the optionally substituted dimethyltryptamine compound comprises a compound of Formula IB, wherein R2b is CD3 and R3b is CD3.
12. The formulation of any one of claims 8 to 11, wherein the salt of the optionally substituted dimethyltryptamine compound comprises a compound of Formula IB, wherein each ybH is D.
13. The formulation of any one of claims 8, 9, 11 or 12 wherein n is 0. PCT/EP2022/0824
14. The formulation of any one of claims 8 to 12 wherein n is 1 and R1b is 4-acetoxy.
15. The formulation of any one of claims 8 to 12 wherein n is 1 and R1b is 5-methoxy or trideutero-5-methoxy.
16. The formulation of any one of claims 1 to 8, wherein the optionally substituted dimethyltryptamine compound is N,N-dimethyltryptamine.
17. The formulation of any one of claims 1 to 8, wherein the optionally substituted dimethyltryptamine compound is α,α-dideutero-N,N-dimethyltryptamine.
18. The formulation of any one of claims 1 to 17, wherein the salt of the optionally substituted dimethyltryptamine compound is of an optionally substituted dimethyltryptamine compound and an acid selected from the group consisting of fumaric acid, tartaric acid, citric acid, acetic acid, lactic acid and gluconic acid.
19. The formulation of claim 18, wherein the acid is fumaric acid.
20. The formulation of any one of claims 1 to 19 comprising a drug substance which comprises the salt of the optionally substituted dimethyltryptamine compound at a purity of greater than or equal to 99% when measured by HPLC.
21. The formulation of any one of claims 1 to 20, wherein the concentration of the optionally substituted dimethyltryptamine is from about 10 mg/mL to about 1mg/mL (as the freebase equivalent).
22. The formulation of any one of claims 1 to 20, wherein the concentration of the optionally substituted dimethyltryptamine is from about 15 mg/mL to about mg/mL (as the freebase equivalent).
23. The formulation of any one of claims 1 to 20, wherein the concentration of the optionally substituted dimethyltryptamine compound is from about 20 mg/mL to about 40 mg/mL (as the freebase equivalent). PCT/EP2022/0824
24. The formulation of any one of claims 1 to 20, wherein the concentration of the optionally substituted dimethyltryptamine compound is about 25 mg/mL (as the freebase equivalent).
25. The formulation of any preceding claim, wherein the formulation comprises a buffer which is separate to the salt.
26. The formulation of claim 25, wherein the buffer comprises an acetate salt and acetic acid; or a citrate salt and citric acid; or a phosphate salt and phosphoric acid; or the buffer comprises an acetate salt, a citrate salt, or a phosphate salt.
27. The formulation of any preceding claim, wherein the base agent is sodium hydroxide or potassium hydroxide.
28. The formulation of any one of claims 1 to 27, wherein the formulation further comprises a tonicity agent and/or a pH adjuster.
29. The formulation of any preceding claim, wherein the formulation consists essentially of the salt of the optionally substituted dimethyltryptamine compound, water, and the base agent, and optionally one or more agents selected from a pH adjuster, a tonicity agent, a buffer, a co-solvent, a preservative, and an antioxidant.
30. The formulation of any preceding claim, wherein the formulation consists essentially of the salt of the optionally substituted dimethyltryptamine compound, water, the base agent and optionally a buffer and/or a tonicity agent and/or a pH adjuster.
31. The formulation of any preceding claim, wherein the formulation consists of the salt of the optionally substituted dimethyltryptamine compound, water, the base agent and optionally a buffer and/or a tonicity agent and/or pH adjuster.
32. The formulation of any one of claims 28 to 31, wherein the tonicity agent is sodium chloride or dextrose. 35 PCT/EP2022/0824
33. The formulation of any one of claims 1 to 32, having an oxygen content of less than 5 ppm, preferably less than 2 ppm.
34. The formulation of any one of claims 1 to 33, stored in a container having a volume of 5 ml or less.
35. The formulation of any one of claims 1 to 33, stored in a container having a volume of 2 ml or less.
36. The formulation of any one of claims 1 to 35, comprising a salt of an optionally substituted dimethyltryptamine compound, a base agent, water, a buffer which is separate to the salt, and a tonicity agent or pH adjuster
37. The formulation of claim 36, comprising a salt of an optionally substituted dimethyltryptamine compound; a base agent selected from potassium hydroxide and sodium hydroxide; water; a buffer which is a citrate salt; and a tonicity agent or pH adjuster which is an acid.
38. A kit suitable for preparing a formulation of any one of claims 1 to 37, said kit comprising a salt of an optionally substituted dimethyltryptamine compound; optionally a tonicity agent and/or a pH adjuster; a base agent and optionally a buffer which is separate to the salt.
39. A method of preparing a pharmaceutical formulation as defined in any one of claims 1 to 37, comprising contacting the salt of the optionally substituted dimethyltryptamine compound, water, a base agent and optionally a buffer which is separate to the salt, and optionally a tonicity agent and/or pH adjuster.
40. The method of claim 39 wherein an aqueous solution of the buffer is contacted with the salt of the optionally substituted dimethyltryptamine compound, wherein the aqueous solution has a pH as defined in claim 1.
41. The method of claim 39 or 40, wherein the method comprises contacting the optionally substituted dimethyltryptamine compound with water and optionally a buffer and/or tonicity agent and/or pH adjuster. 35 PCT/EP2022/0824
42. The method of any one of claims 39 to 41, further comprising adjusting the pH of the formulation.
43. The method of claim 42 wherein the pH is adjusted with a base agent which is sodium hydroxide or potassium hydroxide.
44. The method of any one of claims 39 to 43 further comprising sparging the formulation with an inert gas.
45. A formulation as defined in any one of claims 1 to 37 or the kit of claim 38 for use as a medicament, or in combination with psychotherapy.
46. A formulation as defined in any one of claims 1 to 37 or the kit of claim 38 for use in a method of treating a psychiatric or neurological disorder in a patient.
47. The formulation for the use, or kit for use, of claim 46 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 gambling disorders, and (v) an avolition disorder.
48. A method of treating a psychiatric or neurological disorder comprising administering to a patient in need thereof a formulation as defined in any one of claims 1 to 37.
49. The method of claim 48, wherein the psychiatric or neurological disorder is as defined in claim 47.
50. The method of claim 48, wherein the formulation as defined in any one of claims to 37 is administered in combination with psychotherapy.
51. A lyophilised powder formulation comprising the formulation according to any one of claims 1 to 37 which has been lyophilised.
52. A method of preparing a lyophilised powder formulation comprising drying the formulation according to any one of claims 1 to 37 by lyophilisation. PCT/EP2022/0824
53. A method of preparing an aqueous formulation comprising mixing the lyophilised powder formulation as defined in claim 51 or as prepared by the method of claim into water to provide a formulation comprising the salt of an optionally substituted dimethyltryptamine compound, the base agent, water, and optionally the buffer which is separate to the salt to provide a formulation having a pH of from about 5 to about 6.5, a concentration of about 10 mg/ml as freebase or greater, and an osmolality of from about 250 to about 350 mOsm/Kg.
54. The method of claim 53, wherein the method provides a formulation having a pH of from about 5 to about 6.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2021/082227 WO2022117359A1 (en) | 2020-12-01 | 2021-11-18 | Deuterated or partially deuterated n,n-dimethyltryptamine compounds |
| TW110143066A TW202237565A (en) | 2020-12-01 | 2021-11-18 | Deuterated compounds |
| GBGB2119021.0A GB202119021D0 (en) | 2021-11-18 | 2021-12-24 | Injectable and inhalable formulations |
| US202217574424A | 2022-01-12 | 2022-01-12 | |
| EP2022055324 | 2022-03-02 | ||
| PCT/EP2022/082486 WO2023089132A1 (en) | 2021-11-18 | 2022-11-18 | Injectable and inhalable formulations |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL312859A true IL312859A (en) | 2024-07-01 |
Family
ID=84440034
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL312859A IL312859A (en) | 2021-11-18 | 2022-11-18 | Injectable and inhalable formulations |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP4433049A1 (en) |
| KR (1) | KR20240110836A (en) |
| AU (1) | AU2022393234A1 (en) |
| CA (1) | CA3238583A1 (en) |
| CO (1) | CO2024007518A2 (en) |
| IL (1) | IL312859A (en) |
| MX (1) | MX2024005955A (en) |
| WO (1) | WO2023089132A1 (en) |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2666149A1 (en) * | 2006-10-19 | 2008-04-24 | Auspex Pharmaceuticals, Inc. | Substituted indoles |
| PE20220015A1 (en) * | 2019-02-22 | 2022-01-11 | Gh Res Ireland Limited | 5-METHOXY-N,N-DIMETHYLTRYPTAMINE (5-MEO-DMT) FOR THE TREATMENT OF DEPRESSION |
| GB201907871D0 (en) | 2019-06-03 | 2019-07-17 | Small Pharma Ltd | Therapeutic compositions |
| MX2022005399A (en) | 2019-11-07 | 2022-07-05 | Small Pharma Ltd | Compounds. |
| EP3902541B1 (en) | 2020-06-02 | 2022-09-14 | Small Pharma Ltd | Therapeutic compositions comprising deuterated or partially deuterated n,n-dimethyltryptamine compounds |
| AU2021334933B2 (en) * | 2020-08-28 | 2023-01-19 | Cybin Uk Ltd | Injectable formulation |
| WO2022117359A1 (en) * | 2020-12-01 | 2022-06-09 | Small Pharma Ltd | Deuterated or partially deuterated n,n-dimethyltryptamine compounds |
-
2022
- 2022-11-18 KR KR1020247020007A patent/KR20240110836A/en unknown
- 2022-11-18 MX MX2024005955A patent/MX2024005955A/en unknown
- 2022-11-18 AU AU2022393234A patent/AU2022393234A1/en active Pending
- 2022-11-18 IL IL312859A patent/IL312859A/en unknown
- 2022-11-18 EP EP22818741.5A patent/EP4433049A1/en active Pending
- 2022-11-18 WO PCT/EP2022/082486 patent/WO2023089132A1/en active Application Filing
- 2022-11-18 CA CA3238583A patent/CA3238583A1/en active Pending
-
2024
- 2024-06-14 CO CONC2024/0007518A patent/CO2024007518A2/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2022393234A1 (en) | 2024-06-06 |
| CO2024007518A2 (en) | 2024-07-29 |
| KR20240110836A (en) | 2024-07-16 |
| MX2024005955A (en) | 2024-06-11 |
| EP4433049A1 (en) | 2024-09-25 |
| CA3238583A1 (en) | 2023-05-25 |
| WO2023089132A1 (en) | 2023-05-25 |
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