U.S. patent application number 17/202126 was filed with the patent office on 2021-07-01 for therapeutic cannabis extracts.
The applicant listed for this patent is Jenny's Rose, LLC. Invention is credited to James Castillo.
Application Number | 20210196774 17/202126 |
Document ID | / |
Family ID | 1000005459050 |
Filed Date | 2021-07-01 |
United States Patent
Application |
20210196774 |
Kind Code |
A1 |
Castillo; James |
July 1, 2021 |
THERAPEUTIC CANNABIS EXTRACTS
Abstract
The present invention may be one of several formulations
containing cannabinoids and non-cannabinoid compounds. Cannabis
plants are subjected to extraction, and the resulting extract may
be supplemented with additional ingredients to achieve a desired
chemical profile. Dose titration may be used to find an appropriate
dose of cannabis extract to be ingested in treating medical
conditions.
Inventors: |
Castillo; James; (San Diego,
CA) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
Jenny's Rose, LLC |
Los Angeles |
CA |
US |
|
|
Family ID: |
1000005459050 |
Appl. No.: |
17/202126 |
Filed: |
March 15, 2021 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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16596287 |
Oct 8, 2019 |
10946054 |
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17202126 |
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Current U.S.
Class: |
1/1 |
Current CPC
Class: |
A61K 31/352 20130101;
A61K 31/015 20130101; A61K 31/05 20130101; A61K 31/685 20130101;
A61K 36/185 20130101 |
International
Class: |
A61K 36/185 20060101
A61K036/185; A61K 31/015 20060101 A61K031/015; A61K 31/05 20060101
A61K031/05; A61K 31/352 20060101 A61K031/352; A61K 31/685 20060101
A61K031/685 |
Claims
1. A therapeutic formulation comprising a cannabis extract wherein
a weight of remainder equal to at least 10% to 40% by weight of
total measured cannabinoids is added.
2. A therapeutic formulation comprising 70% to 95% by weight of
total measured cannabinoids, wherein a weight of remainder is added
to the total cannabinoid weight to bring total weight up to 100% by
weight.
3. A therapeutic formulation comprising about 20% CBD by weight,
about 60% .DELTA.8-THC by weight and about less than about 5% by
weight of other cannabinoids, where the listed percentages are
weight percentage.
4. The therapeutic formulation of claim 3 further comprising at
least 15% remainder by weight.
5. The therapeutic formulation of claim 3 further comprising 1-4%
by weight added terpenoid compounds.
6. The therapeutic formulation of claim 5, wherein the added
terpenoid compounds consist essentially of about 0.05%-1% linalool
by weight, about 0.05%-1% .alpha.-pinene by weight and about
0.05%-1% .beta.-myrcene by weight.
7. A therapeutic formulation comprising about 24% THCA by weight,
about 48% CBDA by weight
8. The therapeutic formulation of claim 7 and at least 20%
remainder by weight.
9. The therapeutic formulation of claim 7 further comprising about
2% THC by weight, about 1% CBD by weight, about 3% CBN by weight,
about 4% .DELTA.8-THC by weight, about 3% CBG by weight and about
1-3% THCV by weight.
10. The therapeutic formulation of claim 9 further comprising about
1-4% by weight added terpenoid compounds.
11. The therapeutic formulation of claim 10, wherein the added
terpenoid compounds consist essentially of about 0.05%-1% linalool
by weight, about 0.05%-1% .alpha.-pinene by weight and about
0.05%-1% .beta.-myrcene by weight.
12. A therapeutic formulation comprising about 24% THC by weight
and about 48% CBD by weight.
13. The therapeutic formulation of claim 12 further comprising at
least 20% by weight remainder.
14. The therapeutic formulation of claim 12 further comprising
about 2% THCA by weight, about 1% CBDA by weight, about 3% CBN by
weight, about 3% CBG by weight and about 1-3% THCV by weight.
15. The therapeutic formulation of claim 12 further comprising
about 1-4% by weight added terpenoid compounds.
16. The therapeutic formulation of claim 15, wherein the added
terpenoid compounds consist essentially of about 0.05%-1% linalool
by weight, about 0.05%-1% .alpha.-pinene by weight and about
0.05%-1% .beta.-myrcene by weight.
17. The therapeutic formulation of claim 12 further comprising
about 0.05%-3% black pepper extract by volume.
18. The therapeutic formulation of claim 14 further comprising
about 0.05-3% cassia cinnamon oil by volume.
19. The therapeutic formulation of claim 14 further comprising
about 0.05-3% Ceylon cinnamon bark oil by volume.
20. A therapeutic formulation comprising about 10% THCA and about
60% CBD.
21. The therapeutic formulation of claim 20 further comprising at
least 20% by weight remainder.
22. The therapeutic formulation of claim 20 further comprising
about 3% THC by weight, about 1% CBDA by weight, about 3% CBN by
weight, about 1% .DELTA.8-THC by weight, about 4% CBG by weight and
about 1-3% THCV by weight.
23. The therapeutic formulation of claim 22 about 1-4% by weight
added terpenoid compounds of 1-4% by weight
24. The therapeutic formulation of claim 23, wherein the added
terpenoid compounds consist essentially of about 0.05%-1% linalool
by weight, about 0.05%-1% .alpha.-pinene by weight and about
0.05%-1% .beta.-myrcene by weight.
25. A therapeutic formulation comprising: a cannabinoid component
selected to provide less than 0.3% THC by weight and less than 0.3%
THCA by weight, about 65-75% CBD by weight, and about 5-15% CBN by
weight; at least 10% by weight remainder; and about 1-4% by weight
added terpenoid compounds.
26. The therapeutic formulation of claim 25, wherein the added
terpenoid compounds consist essentially of about 0.05%-1% linalool
by weight, about 0.05%-1% .alpha.-pinene by weight and about
0.05%-1% .beta.-myrcene by weight.
27. A therapeutic formulation comprising: a cannabinoid component
selected to provide about 35% THC by weight, about 35% CBD by
weight, about 3% CBN by weight, about 3% .DELTA.8-THC by weight,
and about 4% CBG by weight; at least 15% by weight remainder; and
about 1-4% by weight added terpenoid compounds.
28. The therapeutic formulation of claim 27, wherein the added
terpenoid compounds consist essentially of about 0.05%-1% linalool
by weight, about 0.05%-1% .alpha.-pinene by weight and about
0.05%-1% .beta.-myrcene by weight.
29. A therapeutic formulation comprising: a cannabinoid component
selected to provide about 35% THC by weight, about 35% CBD by
weight, about 3% CBN by weight, about 3% .DELTA.8-THC by weight,
and about 4% THCV by weight; at least 15% by weight remainder; and
about 1-4% by weight added terpenoid compounds.
30. The therapeutic formulation of claim 29 wherein the added
terpenoid compounds consist essentially of about 0.05%-1% linalool
by weight, about 0.05%-1% .alpha.-pinene by weight and about
0.05%-1% .beta.-myrcene by weight.
31. A therapeutic formulation comprising a cannabinoid component
selected to provide about equal amounts by THC and CBD and less
than 5% by weight each of CBN, THC, and CBG.
32. The therapeutic formulation of claim 31 wherein the total
weight of cannabinoids is at least 80% and said formulation further
comprises at least 15% by weight remainder.
33. The therapeutic formulation of claim 31, wherein the cannabis
extract provides at least 30% THC by weight, and at least 30% CBD
by weight.
34. The therapeutic formulation of claim 33 further comprising
about 1-4% by weight added terpenoid compounds.
35. The therapeutic formulation of claim 34, wherein the added
terpenoid compounds consist essentially of about 0.05%-1% linalool
by weight, about 0.05%-1% .alpha.-pinene by weight and about
0.05%-1% .beta.-myrcene by weight.
36. A therapeutic formulation comprising a cannabis component
selected to provide about 24% THC by weight and about 48% CBD by
weight
37. The therapeutic formulation of claim 36 further comprising at
least 20% remainder by weight.
38. A therapeutic formulation comprising: a cannabinoid component
selected to provide about 60% THC by weight, about 20% CBD by
weight, about 3% CBN by weight, about 3% .DELTA.8-THC by weight,
and about 4% CBG by weight.
39. The therapeutic formulation of claim 38 further comprising
about 10% remainder by weight.
40. The therapeutic formulation of claim 38 further comprising
about 1-4% by weight added terpenoid compounds.
41. The therapeutic formulation of claim 40, wherein the added
terpenoid compounds consist essentially of about 0.05%-1% linalool
by weight, about 0.05%-1% .alpha.-pinene by weight and about
0.05%-1% .beta.-myrcene by weight.
42. A therapeutic formulation comprising a cannabinoid component
selected to provide about 20% CBD by weight and about 60% CBN by
weight.
43. The therapeutic formulation of claim 42 and at least 10%
remainder by weight.
44. The therapeutic formulation of claim 42 further comprising:
about 3% THC by weight, about 1% THCA by weight, about 1% A8-THC by
weight, and about 4% CBG by weight; added terpenoid compounds of
1%-4% by weight wherein the added terpenoid compounds consist
essentially of about 2% limonene, about 9% linalool, about 6.5%
.alpha.-pinene, about 2% .alpha.-terpineol, about 5% valencene,
about 4.5% .alpha.-bisabolol, about 43% .beta.-myrcene, about 13%
.beta.-caryophyllene, about 5% .beta.-ocimene and about 8%
.alpha.-humulene by weight; and about 5% lecithin by volume.
Description
CROSS-REFERENCE TO PRIOR APPLICATION
[0001] This application is a continuation of and claims priority
and benefit of U.S. patent application Ser. No. 16/596,287 filed
Oct. 8, 2019, which issued as U.S. Pat. No. 10,946,054 on Mar. 16,
2021.
BACKGROUND OF THE INVENTION
[0002] The cannabis plant (Cannabis sativa L.) ("cannabis")
naturally produces a complex mixture of compounds (often called
"natural products" or "secondary metabolites"), including
cannabinoids, flavonoids and terpenoids which are present in much
higher concentrations in the female inflorescences than in other
parts of the plant. The precise function of these compounds within
the plant is largely unknown; it is generally hypothesized that
many of the compounds are used defensively to prevent predation by
animals and attack by fungi and bacteria. After cannabis is
harvested, these compounds can be isolated by means of an
extraction process. Cannabinoids are natural products that are
largely exclusive to the cannabis plant. While over one hundred
cannabinoids are known, only the most prevalent ones are generally
analyzed when characterizing cannabis for medicinal or recreational
purposes.
[0003] Some cannabinoids ("primary cannabinoids") are present in
the common cultivars (AKA "strains") of cannabis known to date and
include cannabidiolic acid ("CBDA"), cannabigerol acid ("CBGA"),
and tetrahydrocannabinolic acid ("THCA"). It will be appreciated
that the cannabis plant produces the carboxylic acid form of
cannabinoids (e.g., THCA). During the extraction processes, the
naturally occurring acidic forms are typically converted into
physiologically active decarboxylated forms (e.g., CBD, THC, CBG)
for the final extract. Some of the other cannabinoids ("common
cannabinoids") are also commonly found in cannabis, but they
usually exist at lower overall concentrations, with greater
variation in concentration from strain to strain and their
availability in the final extract may also be contingent on the
extraction process. These include cannabinoid compounds such as:
.DELTA.8-tetrahydrocannabinolic acid (".DELTA.8-THCA");
tetratetrahydrocannabivarin ("THCV"); tetrahydrocannabivarinic acid
("THCVA"); cannabichromene ("CBC"); cannabichromenic acid ("CBCA").
Cannabinol (CBN), typically formed as a breakdown product of THC,
is found in aging cannabis plants, as the endogenous cannabinoid is
exposed to high temperature and sunlight. CBDA is present at a
relatively high level in a few medicinal/recreational cannabis
cultivars but is generally associated with "hemp" cannabis
cultivars which normally contain appreciable levels of CBDA (and
the decarboxylated form CBD). Terpenoids common in cannabis include
compounds such as: D-limonene; linalool; eucalyptol (also known as
1,8-cineol); .alpha.-pinene; terpinen-4-ol (also known as
4-terpineol); p-cymene; borneol; .DELTA.-3-carene; pulegone;
.beta.-myrcene; humulene; and .beta.-sitosterol (a phytosterol).
Flavonoids present in cannabis include cannflavin A; apigenin; and
quercetin. The level of the various terpenoids and flavonoids vary
greatly from cultivar to cultivar. In summary,
medicinal/recreational cultivars of cannabis contain high levels of
one or more of the primary cannabinoids. They also contain variable
levels of the one or more of the "common cannabinoids." Generally,
the primary and common cannabinoids are the ones that are analyzed
for in the industry. The other seventy-five or more "minor
cannabinoids" are typically not currently analyzed in the industry,
but it is believed that most cultivars contain at least some of the
minor cannabinoids.
[0004] Although terpenoids and flavonoids are known to have
potential medical benefit, medical as well as recreational effects
of cannabis have been generally attributed to
cannabinoids--particularly the primary cannabinoids. The major
psychoactive cannabinoid is THC. While CBD is not considered to
have the significant psychoactive properties as does THC, it is now
known to interact with THC and modulate the biological effect of
THC. The story is even more complicated because it is becoming
recognized that major and minor cannabinoids interact with each
other as well as with terpenoids and possibly other plant natural
products to produce medical and recreational effects that cannot be
attributed to cannabinoids alone. This interaction or synergy
resulting from the complex mixture of compounds present within
cannabis is variously known as the "entourage effect," in which a
mixture of compounds demonstrates greater efficacy in treating a
medical condition than any of its constituent compounds in
isolation.
[0005] The existence of the entourage effect calls into question
the conventional wisdom underlying commercial cannabis-derived
pharmaceuticals, which dictates that particular compounds should be
isolated from cannabis and refined to high purity. For example, the
drug Epidiolex.RTM. (marketed by GW Pharmaceuticals, plc)
identifies only CBD as the active pharmaceutical ingredient on its
label. The drug Sativex.RTM. (marketed by GW Pharmaceuticals, plc),
which is currently undergoing clinical trials, indicates that a
mixture of CBD and .DELTA.9-THC, both from plant derived sources,
as are the active pharmaceutical ingredients.
[0006] Extraction processes, especially those directed at
pharmaceutical compositions, have focused on preparing plant
extracts that are rich in individual cannabinoids at the expense of
other plant natural products. Typical extraction processes involve
a "winterization" step where waxes and lipids that are extracted
when the plant cells and organelles are ruptured during the
extraction process and are removed from the extract by subjecting
the extract to subzero temperatures which solidifies or freezes the
waxes and lipids. Such waxes and lipids are viewed in the industry
as undesirable impurities that affect the stability, potency, and
overall desirability of the cannabis extract.
[0007] U.S. Pat. No. 10,195,159 (the '159 Patent) describes a
process for removing what it describes as the unwanted "ballast"
from cannabis plant extracts. The ballast described therein
includes plant cell constituents comprising "fats, waxes,
carbohydrates, proteins and sugars." The inventors explain that
"[t]he presence of these substances results in botanical extracts
which may be hygroscopic, difficult to reduce to a powder and
generally intractable as starting materials for pharmaceutical
preparations." The '159 Patent explains "that presence of ballast
may also limit the shelf-life of pharmaceutical products formulated
from such extracts." The '159 Patent also explains that some
elements of ballast can be "removed by an additional step
post-extraction referred to as "winterization", which involves
making a concentrated solution of the extract and cooling it to a
temperature at which a proportion of waxes and lipid components may
be precipitated, typically -20.degree. C."
[0008] WO2018187500A1 (the '500 Application) describes a process
for removing waxes and lipids from crude cannabis extracts before
the process of decarboxylation and purification of the extracts to
obtain purified cannabis extracts. The '500 Application explains
that crude cannabis extracts are known to contain high
concentration of waxes and hydrocarbons from plant materials. Such
waxes and plant materials are typically removed or reduced by a
"winterization process" prior to decarboxylation and purification
of the cannabis extract. The "winterization process" is typically
performed by dissolving the distillate in alcohol which is then
subjected to subzero temperatures to separate out the fats and
waxes. In the '500 Application, the winterization process involves
dissolving the distillate in 200-proof ethanol and then placing in
the resulting solution in a freezer at -20.degree. C. for 4 hours.
While cold, the precipitated material containing the unwanted fats
and waxes was filtered using a filter funnel, and the filter was
rinsed with 100 ml of ice cold ethanol. The filtered ethanolic
solution of the distillate was evaporated to dryness to give 84.0 g
residue (78% CBD content). The '500 Application described that the
CBD recovery in this step is 99.0%, demonstrating that the typical
extraction process focuses on removing waxes and lipids during the
extraction process, in favor of producing a concentrated
cannabinoid.
[0009] Surprisingly, it has been found that the fraction that is
typically discarded, containing the waxes and lipids, is important
to the therapeutic value of the extract. This is because it is
becoming recognized that the plant's therapeutic value may not be
attributable to the major cannabinoids alone. Rather, the
therapeutic value may lie in a synergistic effect between numerous
chemical components present in the cannabis plants. This
interaction or synergy resulting from the complex mixture of
compounds present within the cannabis plant is variously known as
the "entourage effect," in which a mixture of compounds present
demonstrates greater therapeutic efficacy than any of its
constituent compounds in isolation. Accordingly, there is a need
for therapeutic cannabis products which recognize the importance of
having multiple cannabinoids, terpenoids, and other active
molecules including waxes and lipids that facilitate entourage
effects.
SUMMARY OF THE INVENTION
[0010] The present invention encompasses novel cannabinoid
formulations--primarily for oral administration--that contain
target concentrations of cannabinoids, and other cannabis-plant
derived fractions which show synergistic activities not found in
combinations of purified cannabinoids. The formulations may be
prepared by combining the individual cannabinoids, terpenoids, and
the "remainder fraction," to achieve the target composition. The
cannabinoids and terpenoids can be derived from various types of
extracts of cannabis and other plants.
[0011] The formulations may also be prepared by selecting cannabis
cultivars known to have cannabinoid profiles close to the target
combinations and supplementing the extracts as needed to reach the
target formulations. The cannabis extracts may be produced by
subjecting harvested cannabis from known cultivars such as afghani,
skunk, white widow, blue dream, and AC/DC (also known as ACDC)
strains to an extraction process. It will be appreciated that using
certain known cultivars as starting materials may facilitate
producing extracts with certain preferred levels of active
ingredients. These named cultivars are merely examples, and the
cultivar of choice will depend on the target concentrations of
active compounds desired in the final formulation. The extraction
process may use an alcohol, such as ethanol, or a non-polar
compound, such as butane, as the extraction solvent. The cannabis
extract may also be supplemented by adding active compounds from
independent sources. Alternatively, purified extracts of individual
cannabinoids, terpenoids and other active plant compounds may be
combined to create the formulations to obtain improved therapeutic
outcomes.
[0012] A goal of the inventive formulations is to take advantage of
the entourage effect. In the typical extraction process, the goal
is to obtain purified extracts containing high concentrations of
the cannabinoids, and discarding portions of the extract containing
waxes, lipids, and other components of plant materials that do not
contain the desired cannabinoids. As such portions of the extracts
do not contain cannabinoids, they are not believed to possess
therapeutic or commercial value.
[0013] For example, cold liquid butane or cold ethanol may be used
to extract ground cannabis material. The plant material is retained
by an about 220 .mu.m screen or similar filter, and the extraction
solvent is allowed to flow through. Prior to removal of the
extraction solvent, the extract mixture is filtered to remove small
particles of plant material. The inventor has found that filtration
using filters having about a 45 .mu.m pore size removes the vast
majority of plant solids (i.e., insoluble bits of plant tissue).
Next, the extract is optionally filtered through a filter having a
5 .mu.m pore size which passes the dissolved extract compounds and
retains a "remainder" fraction. Details of this process are found
in copending U.S. patent application Ser. No. 16/569,535, titled
"NOVEL ACTIVE FRACTION FROM THERAPEUTIC CANNABIS PLANT EXTRACTS,
filed 12 Sep. 2019, the contents of which are incorporated herein
by reference. The majority of the solvent extract which passes
through the filter(s) is used to produce a "mixed cannabinoid"
fraction. The "remainder" fraction recovered from the 5 .mu.m
filter consists of particles or micelles of waxes and/or other
lipids and would normally be discarded. The inventor has made the
surprising discovery that adding a significant percentage of the
"remainder" to the final formulation greatly enhances the
effectiveness of the formulation--showing a magnified
"entourage-like" effect. The reason for this effect is under
current investigation. It is possible that the presence of certain
waxes and/or other lipids may improve the absorption of the
formulation by the individual, thereby enhancing the physiological
actions of the cannabinoid formulation.
[0014] The cannabis formulations described herein can be
administered to a patient to alleviate a variety of maladies
including Parkinson's disease, pain symptoms, inadequate appetite,
inflammation, and sleep disorders. For any given patient, the
optimal dosage of the formulation may be determined by performing a
dose titration over an extended period.
DETAILED DESCRIPTION OF THE INVENTION
[0015] Definitions: The following terms may be used as a shorthand
to discuss cannabinoids. They are for convenience only. "Primary
cannabinoids" are found in many or most cannabis cultivars
currently available. These are CBDA, CBGA, and THCA, or their
decarboxylated equivalents. Most cultivars have high levels
(greater than about 5% by weight of dried plant material) of one or
more of the primary cannabinoids or their decarboxylated
equivalents. "Common cannabinoids" are present at lower levels in
most cultivars and include .DELTA.8-THC, THCVA, CBCA and their
decarboxylated equivalents; any cannabinoid that is routinely
analyzed for and is not a primary cannabinoid is considered a
common cannabinoid. "Minor cannabinoids" are those cannabinoids not
routinely analyzed for. It will be appreciated that the list of
"routinely" analyzed cannabinoids is influenced by several factors.
Regulations may dictate that .DELTA.9-THC content and the content
of some other primary cannabinoids be listed on the product.
Experimental or anecdotal evidence may suggest the efficacy of
certain minor cannabinoids--this creates the impetus to analyze for
those cannabinoids. As a result, the newly analyzed cannabinoids
move from the "minor cannabinoid" grouping to the "common
cannabinoid" grouping. "Mixed cannabinoids fraction" is the
fraction produced when a crude cannabis extract is refined to
remove solvents and other undesirable components.
[0016] "Remainder" fraction is the fraction removed from crude
cannabis extracts by filtration or an equivalent separation
technique (e.g., centrifugation). After the extraction process the
crude extract (solvent and dissolved plant compounds) is cloudy
indicating that it still contains undissolved material. Filtration
of the crude cannabis extract through a filter having about a 45
.mu.m pore size removes most of the undissolved plant material
yielding a somewhat cloudy filtrate. Filtration of the 45 .mu.m
filtrate through a filter having about a 5 .mu.m pore size yields a
clear filtrate containing the dissolved cannabinoids and other
dissolved cannabis compounds. The material remaining on the 5 .mu.m
filter is the remainder fraction. This remainder fraction contains
active compounds, probably in the form of micelles or compounds
absorbed to very small particles of plant material that
significantly enhance the effectiveness of a given formulation
through an entourage-like effect. The remainder fraction may be
scraped off the filter and used immediately. If the remainder
fraction is to be stored for an appreciable period of time, it
should be washed off the filter with solvent and stored at low
temperatures. For use, the remainder fraction is recovered from the
suspension by filtration or centrifugation.
[0017] For example, quantity of harvested cannabis is first
converted to cannabis extract. Production of the cannabis extract
may be performed using the method set forth in co-pending U.S.
patent application Ser. No. 16/365,614, entitled "Producing
Cannabis Extracts via Selective Decarboxylation" which was filed on
Mar. 26, 2019, the contents of which are incorporated herein by
reference. Alternatively, extraction may be performed using butane
as a solvent or any other extraction method practiced in the art of
producing plant extracts.
[0018] Unless otherwise stated, the concentration of any compound
in a cannabis extract (oil) or cannnabis formulation is stated as a
percentage based on weight. Thus, a .DELTA.9-THC concentration of
24% by weight means that 24 mg of .DELTA.9-THC are present in every
100 mg. Likewise, a formulation having a CBD concentration of 48%
by weight means 48 mg of CBD are present in every 100 mg of the
formulation. The therapeutic formulation may be supplemented by the
addition of active compounds from separate sources (e.g., black
pepper extract). Unless otherwise stated, the amounts of separately
added liquid ingredients in a cannabis extract or formulation are
expressed as a percentage based on volume. Thus, a formulation that
contains 1% black pepper extract by volume contains 1 ml of black
pepper extract in every 100 ml of the formulation.
[0019] According to the present invention a cannabis formulation
typically is supplemented with remainder fraction at a
concentration of 10%-40% by weight (i.e., the added remainder
accounts for 10-40 mg of weight in every 100 mg of the
formulation). The presence of remainder compounds in a cannabis
formulation allows the formulation to exhibit an enhanced entourage
effect in therapeutic use. To further enhance the entourage effect,
a cannabis formulation may be supplemented with
terpene/terpenoids-containing extracts. Such extracts can be
obtained from RICCA Chemical Company, LLC of Arlington, Tex. Unless
otherwise indicated, extracts containing linalool, .alpha.-pinene,
.beta.-myrcene, and D-limonene were supplied by RICCA. A cannabis
formulation may also be supplemented with black pepper extract and
Ceylon cinnamon bark oil supplied, for example, by Botanicals by
the Sea LLC of Carlsbad, Calif.; and cinnamon cassia oil supplied
by Botanicals by the Sea LLC of Carlsbad, Calif. Equivalent
extracts are readily available from other suppliers and are equally
suitable.
[0020] The following formulations are those tested and perfected by
the inventor. They are but exemplars of the general principles
presented here. Although based on cannabis extract (or cannabis
"oil" as it is often known in the trade) the final volume of a
formulation is reached by adding cannabinoid-free hemp oil as a
diluent/carrier. The various active compounds are soluble in the
carrier which decreases the viscosity of the formulation while
significantly increasing the absorption and bioavailability of the
formulation. Lecithin, such as natural sunflower lecithin, may be
added as an emulsifier.
[0021] Each formulation is built around the ratios of different
cannabinoids. For example, the ratio of CBD to THC. The addition of
terpenoids further promotes the entourage effect established by the
cannabinoids. It is possible to establish the desired ratio of the
cannabinoids by combining purified cannabinoids (e.g., from
cannabis extracts or distillates). The ratios may also be achieved
by using mixed cannabinoid fractions from defined cultivars. Active
terpenoids may come from the cannabis extracts. Additional active
terpenoids from other botanical sources are added to make the final
formulation. Finally "remainder" fraction, preferably from defined
cultivars, is added to complete the formulation. In general, after
the required amounts of the cannabinoids have been added, a
sufficient weight of remainder fraction is added to bring the total
weight of the cannabinoid component to 100%. (It should be
understood that while the remainder fraction may not contain
cannainoids, it is treated like a cannabinoid from weight percent
basis for formulation purposes.)
Formulation Examples.
[0022] 1) .DELTA.8-THC Enriched Formulation ("Formulation C"). In
this embodiment, cannabis component contains about: 0.3% or less
.DELTA.9-THC by weight; 20% CBD by weight; 1% CBDA by weight; 3%
CBN by weight; and 60% .DELTA.8-THC by weight (approximately 84%
total cannabinoids by weight) plus about 16% by weight remainder
fraction to make approximately 100%. The final formulation may
compounded by supplementing this base extract, using
cannabis-derived or compounds derived from other botanicals, to
contain: 0.05%-1% linalool by weight; 0.05%-1% .alpha.-pinene by
weight; and 0.05%-1% .beta.-myrcene by weight. The resulting
cannabis formulation may additionally be supplemented to contain:
0.05%-3% black pepper extract (source of .beta. caryophyllene) by
volume; be 0.05-3% cassia cinnamon oil (Cinnamomum aromaticum) by
volume; and 0.05-3% Ceylon cinnamon bark oil (Cinnamomum verum) by
volume.
[0023] 2) High CBD Non-psychoactive, Non-decarboxylated
Formulation. In this embodiment, the cannabinoid component is
preferably derived from an extract of white widow or AC/DC
cultivars. The cannabis component contains about: 2% .DELTA.9-THC
by weight; 24% THCA by weight; 1% CBD by weight; 48% CBDA by
weight; 3% CBN by weight; 4% .DELTA.8-THC by weight; 3% CBG by
weight; and 1%-3% THCV by weight. These cannabinoids can be derived
from other sources. Remainder fraction is added to bring the
cannabinoid total weight to about 100%. The final formulation is
compounded by supplementing this base, using cannabis-derived or
compounds derived from other botanicals, to contain: 0.05%-1%
linalool by weight; 0.05%-1% .alpha.-pinene by weight; and 0.05%-1%
.beta.-myrcene by weight. The resulting cannabis formulation may
additionally be supplemented to contain: 0.05%-3% black pepper
extract (source of .beta. caryophyllene) by volume; 0.05-3% cassia
cinnamon oil (Cinnamomum aromaticum) by volume; and 0.05-3% Ceylon
cinnamon bark oil (Cinnamomum verum) by volume.
[0024] 3) CBD Decarboxylated Formulation. A quantity of cannabis
extract produced from the white widow or AC/DC cultivars is first
subjected to decarboxylation through heat treatment as is
well-known in the art. After decarboxylation, the cannabis extract
contains about: 24% .DELTA.9-THC by weight; 2% THCA by weight; 48%
CBD by weight; 1% CBDA by weight; 3% CBN by weight; 4% .DELTA.8-THC
by weight; 3% CBG by weight; and 1-3% THCV by weight. (The basic
THC:CBD ratio is about 1:2.) Remainder fraction is added to bring
the cannabinoid total weight to about 100%.The final formulation is
compounded by supplementing this base extract, using
cannabis-derived or compounds derived from other botanicals, to
contain: 0.05%-1% linalool by weight; 0.05%-1% .alpha.-pinene by
weight; and 0.05%-1% .beta.-myrcene by weight. The resulting
cannabis formulation may additionally be supplemented to contain:
0.05%-3% black pepper extract (source of .beta. caryophyllene) by
volume; 0.05-3% cassia cinnamon oil (Cinnamomum aromaticum) by
volume; and 0.05-3% Ceylon cinnamon bark oil (Cinnamomum verum) by
volume.
[0025] 4) AC/DC Non-Decarboxylated Formulation. In this embodiment,
harvested cannabis from the AC/DC strain is subjected to an
extraction process. The resulting cannabis extract contains about:
3% .DELTA.9-THC by weight; 10% THCA by weight; 60% CBD by weight;
1% CBDA by weight; 3% CBN by weight; 1% .DELTA.8-THC by weight; 4%
CBG by weight; and 1%-3% THCV by weight. Remainder fraction is
added to bring the cannabinoid total weight to about 100%. The
final formulation is compounded by supplementing this base extract,
using cannabis-derived or compounds derived from other botanicals,
to contain: 0.05%-1% linalool by weight; 0.05%-1% .alpha.-pinene by
weight; and 0.05%-1% .beta.-myrcene by weight. The resulting
cannabis formulation may additionally be supplemented to contain:
0.05%-3% black pepper extract (source of .beta. caryophyllene) by
volume; 0.05-3% cassia cinnamon oil (Cinnamomum aromaticum) by
volume; and 0.05-3% Ceylon cinnamon bark oil (Cinnamomum verum) by
volume.
[0026] 5) Hemp-based Formulation. In this embodiment, harvested
cannabis meeting the definition of "hemp" set forth in the
Agriculture Improvement Act of 2018 is subjected to an extraction
process. The resulting cannabis extract contains .DELTA.9-THC and
THCA that are within the legal limit for hemp (i.e., less than 0.3%
on a dry weight basis). The cannabis extract additionally contains
about: 65%-75% CBD by weight; 1% CBDA by weight; 5%-15% CBN by
weight. The cannabis extract contains essentially no .DELTA.8-THC,
CBG, or THCV. Remainder fraction is added to bring the cannabinoid
total weight to about 100%. The final formulation is compounded by
supplementing this base extract, using cannabis-derived or
compounds derived from other botanicals, to contain: 0.05%-1%
linalool by weight; 0.05%-1% .alpha.-pinene by weight; and 0.05%-1%
.beta.-myrcene by weight. The resulting cannabis formulation may
additionally be supplemented to contain: 0.05%-3% black pepper
extract (source of .beta. caryophyllene) by volume; 0.05-3% cassia
cinnamon oil (Cinnamomum aromaticum) by volume; and 0.05-3% Ceylon
cinnamon bark oil (Cinnamomum verum) by volume.
[0027] 6) Blue Dream plus AC/DC Formulation ("Formulation A"). In
this embodiment, harvested cannabis from the blue dream and AC/DC
strains (approximately equal quantities of each strain) are
subjected to an extraction process. The resulting cannabis extract
contains about: 35% .DELTA.9-THC by weight; 35% CBD by weight; 3%
CBN by weight; 3% .DELTA.8-THC by weight; and 4% CBG by weight. The
THC:CBD ratio is about 1:1. The cannabis extract contains
essentially no CBDA or THCV. Remainder fraction is added to bring
the cannabinoid total weight to about 100%.The final formulation is
compounded by supplementing this base extract, using
cannabis-derived or compounds derived from other botanicals, to
contain: 0.05%-1% linalool by weight; 0.05%-1% .alpha.-pinene by
weight; and 0.05%-1% .beta.-myrcene by weight. The resulting
cannabis formulation may additionally be supplemented to contain:
0.05%-3% black pepper extract (source of .beta. caryophyllene) by
volume; 0.05-3% cassia cinnamon oil (Cinnamomum aromaticum) by
volume; and 0.05-3% Ceylon cinnamon bark oil (Cinnamomum verum) by
volume.
[0028] 7) Afghani plus Skunk plus AC/DC Formulation ("Formulation
B"). In this embodiment, harvested cannabis from the afghani,
skunk, and AC/DC cultivars (approximately equal quantities of each
strain) is subjected to an extraction process. The resulting
cannabis extract contains about: 35% .DELTA.9-THC by weight; 35%
CBD by weight; 3% CBN by weight; 3% .DELTA.8-THC by weight; and 4%
THCV by weight. The THC:CBD ratio is about 1:1. The cannabis
extract contains essentially no CBG. Remainder fraction is added to
bring the cannabinoid total weight to about 100%. The final
formulation is compounded by supplementing this base extract, using
cannabis-derived or compounds derived from other botanicals, to
contain: 0.05%-1% linalool by weight; 0.05%-1% .alpha.-pinene by
weight; and 0.05%-1% .beta.-myrcene by weight. The resulting
cannabis formulation may additionally be supplemented to contain:
0.05%-3% black pepper extract (source of .beta. caryophyllene) by
volume; 0.05-3% cassia cinnamon oil (Cinnamomum aromaticum) by
volume; and 0.05-3% Ceylon cinnamon bark oil (Cinnamomum verum) by
volume.
[0029] 8) Critical Mass Formulation. In this embodiment, harvested
cannabis from the critical mass strain is subjected to an
extraction process. The resulting cannabis extract contains about:
3% CBN by weight; 3% .DELTA.8-THC by weight; and 4% CBG by weight.
The final formulation should contain .DELTA.9-THC and CBD at a
1-to-1 ratio, or 45% by weight each. Remainder fraction is added to
bring the cannabinoid total weight to about 100%. The final
formulation is compounded by supplementing this base extract, using
cannabis-derived or compounds derived from other botanicals, to
contain: 0.05%-1% linalool by weight; 0.05%-1% .alpha.-pinene by
weight; and 0.05%-1% .beta.-myrcene by weight. The resulting
cannabis formulation may additionally be supplemented to contain:
0.05%-3% black pepper extract (source of .beta. caryophyllene) by
volume; 0.05-3% cassia cinnamon oil (Cinnamomum aromaticum) by
volume; and 0.05-3% Ceylon cinnamon bark oil (Cinnamomum verum) by
volume.
[0030] 9) Catatonic Formulation. In this embodiment, harvested
cannabis from the catatonic strain is subjected to an extraction
process. The resulting cannabis extract contains about: 3% CBN by
weight; 3% .DELTA.8-THC by weight; and 4% CBG by weight. The final
cannabis formulation should contain .DELTA.9-THC and CBD at a
2-to-1 ratio, or 60% by weight of THC and 20% by weight of CBD.
Remainder fraction is added to bring the cannabinoid total weight
to about 100%. The final formulation is compounded by supplementing
this base extract, using cannabis-derived or compounds derived from
other botanicals, to contain: 0.05%-1% linalool by weight; 0.05%-1%
.alpha.-pinene by weight; and 0.05%-1% .beta.-myrcene by weight.
The resulting cannabis formulation may additionally be supplemented
to contain: 0.05%-3% black pepper extract (source of .beta.
caryophyllene) by volume; 0.05-3% cassia cinnamon oil (Cinnamomum
aromaticum) by volume; and 0.05-3% Ceylon cinnamon bark oil
(Cinnamomum verum) by volume.
[0031] 10) Sleep Aid Formulation. This embodiment is intended as a
sleep aid. The dominant cannabinoid is CBN (about 60%). It also
contains a relatively high percentage of CBD--about 20% plus about
1% CBDA. In addition, it contains about 3% THC and about 1% THCA.
The formula also contains about 4% CBG and about 1% .DELTA.8-THC
with about 10% remainder. The desired terpenoid content is between
about 1% and 4% by weight terpenoids. The percentage breakdown of
the terpenoids is about 2% limonene, about 9% linalool, about 6.5%
.alpha.-pinene, about 5% .alpha.-terpineol, about 5% valencene,
about 4.5% .alpha.-bisabolol, about 43% .beta.-myrcene, about 13%
.beta.-caryophyllene, about 5% .beta.-ocimene and about 8%
.alpha.-humulene. In addition, the formulation contains 5% lecithin
by volume and may additionally be supplemented to contain: 0.05%-3%
black pepper extract (source of .beta. caryophyllene) by volume;
0.05-3% cassia cinnamon oil (Cinnamomum aromaticum) by volume; and
0.05-3% Ceylon cinnamon bark oil (Cinnamomum verum) by volume.
[0032] The following claims are thus to be understood to include
what is specifically illustrated and described above, what is
conceptually equivalent, what can be obviously substituted and what
incorporates the essential idea of the invention. Those skilled in
the art will appreciate that various adaptations and modifications
of the just-described preferred embodiments can be configured
without departing from the scope of the invention. The illustrated
embodiment has been set forth only for the purposes of example and
that should not be taken as limiting the invention.
* * * * *