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Vaporizable psychoactive alkaloid composition and preparation thereof

a technology of psychoactive alkaloids and compositions, which is applied in the direction of dispersing, plant/algae/fungi/lichens ingredients, organic active ingredients, etc., can solve the problems of long onset of action, and difficulty in delivering dosage forms via oral routes, etc., and achieves rapid delivery of psychoactive alkaloids

Pending Publication Date: 2022-10-06
PSILO SCI LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The vaporizable composition achieves higher bioavailability and faster onset of psychoactive effects compared to traditional oral administration, with the ability to standardize psychoactive alkaloid content and bypass hepatic metabolism, suitable for various patient groups including children and geriatrics.

Problems solved by technology

Enteric routes of administration also pose challenges such as long onset of action, gastric irritation, etc.
Further, the ingestion of dosage forms via the oral route, which involves chewing or swallowing, is problematic for children and geriatric patients.
However, parenteral routes of administration do not facilitate the dephosphorylation of phosphorylated psychoactive alkaloids because they are delivered to an area of the body where little to no dephosphorylation occurs.
Additionally, psychoactive alkaloid extracts are often present in form of a sticky tar, which is difficult to handle or standardize into compositions with specific amounts of psychoactive alkaloids that can be formulated into desired dosage forms.

Method used

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  • Vaporizable psychoactive alkaloid composition and preparation thereof
  • Vaporizable psychoactive alkaloid composition and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

n Process with Promotion of Dephosphorylation

[0124]2.5 kilograms of Psilocybe cubensis were dried in a forced air oven at 25° C. for 10 hours to result in 140 grams of dried biomass. The dried biomass was then pulverized to a size of 200 mesh with a hammer mill.

[0125]An acidified solvent, i.e. a pH-adjusted, hydro-ethanol mixture, was prepared. 144 g of anhydrous citric acid was placed into a 5 L vessel with 1.25 L of reverse osmosis water, followed by the addition of 3.75 L of ethanol. The contents were mixed until completely dissolved. An acidified solvent with a pH of 2 was obtained.

[0126]The dried powdered biomass was placed into an agitated, heat-controlled vessel with 5 L of the acidified solvent and mixed for the extraction of psychoactive alkaloid. The extraction was controlled to a constant 75° C., and the duration of extraction was 1 hour. The extraction slurry was then filtered. Filtration resulted in a filtrate, i.e. the psychoactive alkaloid liquid, and a filter residue...

example 2.1

n with a Non-Ionic Macroporous Resin

[0127]The pH of the psychoactive alkaloid extract of example 1, in aqueous form, was adjusted to pH 4.0 (+ / −0.5) by adding 2 M phosphoric acid and centrifuged for 15 minutes at 3000 g to remove any solid precipitate. The pH of 4 corresponds to the isoelectric point of psilocybin, and psilocin's polarity is such that it is partitioned onto the resin, thus allowing effective binding of the psychoactive alkaloids psilocybin (if present, i.e. dephosphorylation is not used or is incomplete) and psilocin to the macroporous resin. Norbaeocystin and baeocystin are phosphorylated and if present would behave in the same way as psilocybin. The supernatant obtained was loaded onto a column of Amberlite® XAD4, a non-ionic macroporous resin (50.34 g of dry resin) at a flow rate of 2 bed volumes per hour, to allow components in the supernatant to be adsorbed onto the macroporous resin. After all 2.5 L of the extract was loaded onto the column of macroporous resi...

example 2.2

n with Cation Exchange and Non-Ionic Macroporous Resins

[0130]The pH of the psychoactive alkaloid extract of example 1, in aqueous form, was adjusted to a pH of 3.0 (+ / −0.5) by adding 1M HCl. It was then mixed with 200 g of Amberlite® MAC-3 H, a strong cationic ion-exchange resin in its hydrogen form, to result in a filtrate-resin mixture, in which components of the psychoactive alkaloid filtrate were adsorbed onto the cation exchange resin. Psilocin's polarity is such that it is partitioned onto the resin. The pH of 3 would also ensure that psilocybin, if present, was in its protonated form, and thus also adsorbed onto the cationic exchange resin efficiently. The filtrate-resin mixture was agitated for 4 hours at room temperature (21° C.-25° C.) and then filtered. The filtrate was discarded, and the resin was rinsed with 2.0 L of 100% EtOH and then 2.0 L of H2O to remove any impurities. Finally, the psilocin (and, in other cases, psilocybin) fraction was eluted with 2.0 L of 2% HCl / ...

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Abstract

This liquid composition includes a psychoactive alkaloid extract or synthetic psychoactive alkaloid. The alkaloids in the extract are predominantly dephosphorylated rather than phosphorylated. The vaporizble psychoactive alkaloid composition includes an alcohol or polyol carrier, fatty acid, fatty alcohol, optional antioxidant, optional flavorant, and optional further excipients. A process for obtaining a vaporizble psychoactive alkaloid composition includes dephosphorylating the alkaloid during extraction, purifying the extracted alkaloid, and standardizing it to a specific concentration by adding measured quantities of excipients.

Description

RELATED APPLICATIONS[0001]This application is a continuation of International Application No. PCT / CA2021 / 051876 filed Dec. 22, 2021, which claims the benefit of U.S. Provisional Patent Application No. 63 / 131,028 filed on Dec. 28, 2020, and U.S. Provisional Patent Application No. 63 / 139,453 filed on Jan. 20, 2021. This application also claims priority to Canadian Application No. 3113240 filed Mar. 24, 2021, Canadian Application No. 3123774 filed Jul. 1, 2021, International Application No. PCT / CA2021 / 051702 filed Nov. 29, 2021, International Application No. CA / 2021 / 051701 filed Nov. 29, 2021, and International Application No. PCT / CA2021 / 051891 filed Dec. 28, 2021, each of which are incorporated by reference in their entireties.TECHNICAL FIELD[0002]This application relates to a vaporizable composition. More specifically, the present invention relates to a vaporizable composition of psychoactive alkaloids for human intake. The present invention also relates to a process for preparing th...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/675A61K9/00A61K31/4045A61K47/10A61K47/12A61K31/355A61K36/07A61K31/375
CPCA61K31/675A61K9/0078A61K31/4045A61K47/10A61K47/12A61K31/355A61K36/07A61K31/375A61K2236/39A61K2236/17A61K2236/15A61K31/405A61K9/0019A61K47/22A61K47/26A61K9/08A61K45/06A61K9/0053A61K9/2095A61K2236/53A61K9/7023
Inventor MOSS, RYANLIGHTBURN, BENJAMINRANKEN, LISA
Owner PSILO SCI LTD