METHOD OF ACTIVATION OF CANNABIS TO RENDER STANDARDIZED PREPARATIONS FOR THERAPEUTIC ADMINISTRATION, OTHER THAN SMOKING

METHODE D'ACTIVATION DU CANNABIS POUR RENDRE LES PREPARATIONS NORMALISEES PLUS EFFICACES AUX FINS D'ADMINISTRATION THERAPEUTIQUE SANS AVOIR A FUMER

English Abstract

A method is described whereby the latent cannabinoids in the cannabis plant
(sativa or
indiga) can be activated to make them more efficacious as an orally
administered
medicine or for sublingual, suppository or patch applications. The process
described is
primarily a decarboxylation of the acid form of a number of cannabinoid
molecules to the
alcohol moiety. This decarboxylation step is performed by heating the ground
cannabis
leaves and flowers for a specific time- period and temperature in a custom
designed
container.
The decarboxylation of Tetrahydrocannabinolic Acid (THC-A) to Delta-9
Tetrohydrocannabinol (THC) transforms the THC-A from a compound with no known
physiological activity to THC with very well characterized immune, anti-
inflammatory
and psycho-activity. Similarly, the decarboxylation of cannabidiolic acid to
cannabidiol
activates these molecules that, in turn, is thought to modulate the effects of
THC.
These activated compounds are now useful for making standardized dosages of
cannabis
medicine. The resultant preparations from this process can be used in either
oral,
sublingual, suppository or patch administrations.

Claims

Claims:
What is claimed:
Claim 1: A process for converting the flowers and leaves of the cannabis plant
(flowers
and leaves) by specific heating, time and containment protocols yields a
product that is
amenable to standardization and administrative routes other than smoking.
A method of claim 1 whereby cannabis material (leaves and flowers) is ground
to a mesh
size that allows for consistent heating.
A method of claim 2 whereby ground cannabis material is heated to a specific
temperature to allow conversion (de-carboxylation).
A method of claim 3 whereby heated ground cannabis material is kept at a
specific
temperature for a specific time to allow optimal conversion of the THC-A to
THC.
A method of claim 4 whereby the percentage conversion of the THC-A to THC can
be
optimized to allow maximum efficiency and efficacy in the finished product.
A method of claim 5 whereby the concentration of converted THC can be
determined and
thus allow standardization of cannabis in to known dosages of active THC.
A method of claim 6 whereby the standardized cannabis can be used as medicines
administered orally, in a sublingual fashion, as a suppository or in a patch.

Description

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Background to the Invention:
Patent No. ZA200306794 speaks of an invention that ultilises organic solvents
to prepare
extracts from cannabis. This patent uses no organic solvent or extraction
procedure in its
formulation.
Patent No. W02004016277 teaches an extraction method using super critical
fluid extraction of
cannabinoids from plant material the method described here uses no fluid
extraction procedure
and does not substitute with synthetic analogues if extracted material is not
available.

CA 02503310 2005-04-08
Patent No. US2003191180 speaks again of organic solvent extraction of
cannabinoids from
plant material plus the use of the invention for synthetic analogues. The
patent described here
references only natural product material and no organic solvent is required
for extraction.
Patent No. W003063847 teaches an anti-nausea formulation based on solvent
extraction of
THC-A. In the patent described here no extraction proceeds activation of THC-A
to THC.
Patent No. US2002086438 again teaches an organic solvent extraction of
cannabinoids to be
used in medicinal formulations. This patent describes the use of no organic
solvent and any stage
in the preparation of the product.
Cannabis (Sativa and Indiga) has been used for many thousands of years as
medicine to
treat a multitude of ailments from arthritis to multiple sclerosis. For the
most part the
administrative route has been in the smoked form. By burning the dried
cannabis leaves
and flowers the medicinal compounds within the plant matrix become activated
and
hence elicit their physiological effects. If the cannabis is not heated as in
smoking or
baking into brownies, the THC is not activated and the medicinal properties of
the
cannabinoids do not present.
Heating of cannabis to activate the major cannbinoid constituents must be done
within a
rather narrow temperature window. Not heating the cannabis enough will allow
only
partial conversion of the acids to the alcohols, heating too much will cause
conversion
and subsequent loss of the converted cannabinoids to atmosphere through
vaporization.
With the invention described here, one can take a known weight of cannabis
plant, place
it in a special container, heat the container and cannabis for a set time at a
specified
temperature and accomplish the same degree of conversion each time.
This reproducible conversion method allows the creation of standardized
cannabis
medicine, with known dosages, that can be used for oral applications.
The standardization of cannabis medicine for oral administration requires two
analytical
steps. One must determine the concentration of the THC-A in the starting raw
material
before grinding and conversion. This pre-determination of THC-A allows for
better
adjustment of the subsequent heating temperature to be applied to the
preparation.
More importantly, identification and quantification of the individual
cannabinoids in the
post-heating mixture is not only vital to the standardization process, but is
also required
to note the percentage conversion of THC-A to THC. If conversion is not
complete,
temperature can be reapplied until conversion optimized per unit time. If
however, the
sample has been over-heated then the THC concentration in the finished product
will be
lower because of burn-off and cannot be recovered.
The design of the container for holding the cannabis during heating is also
paramount to
the efficiency of conversion. Optimally, conversion should mean the removal of
carbon
dioxide from the acidic cannabinoids and little else. Since the heating
process will
vaporize other low molecular weight and boiling point compounds that may also
be
therapeutic, loss of these compounds is to be avoided. As stated previously,
the optimal

CA 02503310 2005-04-08
conversion removes only C02. 'The container design is such that optimum
efficiency is
achieved.
The THC level of the converted cannabis can also be modulated by this method.
That is
an exact concentration of THC can be achieved in each preparation, by
adjusting the
heating time interval. By utitilizing, this method the THC to THC-A ratio can
be adjusted
to any desired level be using specified temperature and time settings. Thus,
specific
dosages of THC can be achieve within a raw material, making the formulation of
standardized products more feasible and cost efficient.
Objectives of the Invention:
1.) An objective of this invention is to allow reproducible conversions of
quantifiable
amounts of cannabinoid acids in cannabis leaves and flowers to equivalent
amounts of
their individual alcohols.
2.) A further objective of this invention is to allow activation of specific
cannabinoid
compounds by a heating/decarboxylation method that allows high yields of the
activated
cannabinoids.
3.) A further objective is to provide a method whereby formerly non-psycho-
active
cannabinoids are decarboxylated to their psycho-active moiety and hence become
useful
in the treatment of symptoms of many ailments.
4.) A further objective is to provide a method whereby the THC content of a
therapeutic
sample can be modulated to achieve a specific dosage of said active in a
standardized
formula.
5.) A further objective of this invention is to provide a means of
standardizing cannabis
medicines with known dosages of active THC per gram of raw material. Since the
degree
of conversion by the described method can be determined by High Pressure
Liquid
Chromatography (HPLC) in a raw material preparation a fixed dosage can be made
and
the product standardized.
6.) A further objective is to allow production of activated standardized raw
material for
use in oral, sublingual, suppository or patch applications.
7.) A further objective is to produce formulations without the use of organic
solvents or
supercritical fluids to extract cannabinoids from plant material.

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Summary of the Invention:
Described here is a method/process whereby the medicinal compounds contained
in
cannabis plant material (leaves and flowers) are activated to be useful for
administrative
routes other than smoking. Such an application also allows for the
standardization of the
converted material into known dosages of activated THC.