WO2019210402A1

WO2019210402A1 - Selective delivery of volatile terpenes/terpenoids inhalants

Info

Publication number: WO2019210402A1
Application number: PCT/CA2019/050553
Authority: WO
Inventors: Michael WILLINSKY
Original assignee: Willinsky Michael
Priority date: 2018-05-01
Filing date: 2019-04-29
Publication date: 2019-11-07

Abstract

A hollow terpene/terpenoid delivery inhalation appurtenance has a mouth piece and an opposed, longitudinally spaced apart upstream end providing an opening for engaging a smoking appliance in an inlet, and an intermediate interior portion extending longitudinally between the mouth piece and the inlet at the upstream end and adapted to receive a terpene/terpenoid-absorbed matrix adapted for dispersal of terpene / terpenoid volatiles into an air stream during inspiration by a user.

Description

SELECTIVE DELIVERY OF VOLATILE TERPENES/TERPENOIDS

INHALANTS

FIELD OF THE INVENTION:

The present invention relates to inhalation therapy employing terpenes/terpenoids generally, but more particularly to co-inhalation therapies employing cannabinoid volatiles.

BACKGROUND OF THE INVENTION:

5,033,484 discloses ventilated filter cigarettes for providing an American-blend flavor. The cigarettes comprise Virginia tobacco with main stream smoke having a condensate/nicotine ratio of 5:1 to 9:1 , a condensate value of 10 mg maximum, a pH- value greater than 6.0, and a pollutant index of less than 35. A secondary air supply corresponding to a filter ventilation level to 20 to 45%.

US 2008/00291 12 A1 discloses a Fibrous material suitable for incorporation into filter elements of cigarettes which are impregnated with additives and agents such as flavorants, flavorant enhancers and/or free radical scavengers. The fibrous material is contacted with the additive dispersed in a high-pressure gas or supercritical fluid (SCF) held at elevated pressures. The high-pressure gas or SCF swells the fibrous matrix and enables the additive to be incorporated within the matrix. When pressure is reduced, the gas or SCF vaporizes and leaves the additive embedded in the fiber interstices. As a result, the additive is slowly released over a finite period of time. When incorporated into a cigarette filter, the additive is released at a desired rate from the interior of the fibrous filter into the cigarette smoke.

US 4715390 discloses a composition for flavouring smoking articles which contains a soluble flavoring material, triacetin and a moisture-releasing hydrophilic polymer. US6761 174B2 discloses a cigarette comprising a tobacco rod and a multi- component filter comprising a bed of adsorbent and a flavor-releasing filter segment located downstream of the bed of adsorbent. In the preferred embodiment, the adsorbent is also flavor-bearing and comprises high surface area, activated carbon. As mainstream smoke is drawn through the upstream portion of the filter, gas phase smoke constituents are removed, and flavor is released from the adsorbent bed. Thereafter additional flavor is released into the mainstream smoke as it passes through the flavor- releasing filter segment. Ventilation is provided to limit the amount of tobacco being combusted during each puff and is arranged at a location spaced downstream from the adsorbent bed to lower mainstream smoke velocity through the adsorbent bed. Preferably, the carbon bed comprises at least 90 to 120 mg or greater of carbon in a fully filled condition or 160 to 180 mg or greater of carbon in a 85 filled condition or better, which in combination with other features provides a flavorful cigarette that achieves significant reductions in gas phase constituents of the mainstream smoke, including 90% reductions or greater in 1 , 3 butadiene, acrolein, isoprene, propionaldehyde, acrylonitrile, benzene, toluene, styrene, and 80% reductions or greater in acetaldehyde and hydrogen cyanide.

US 6,048,404 relates to improved flavorful and aromatic tobacco materials and processes for producing flavorful and aromatic components from tobacco material are provided. The processes involve subjecting substantially dry, liquid free tobacco materials directly to heat treatment in an enclosed pressure- controlled environment at a temperature for a period of time such that flavorful and/or aromatic Substances are provided while excess weight loss in the tobacco material is avoided.

SUMMARY OF THE INVENTION:

The present invention is related to the selective delivery of volatile terpenes and/or terpenoids - employing one or more selected terpene/terpenoid extracts deployed on an absorbent matrix for dispersal of terpene/terpenoid volatiles into an air stream during inspiration by a user. An aspect of the invention is to provide for this selective delivery of terpenes and/or terpenoids and includes a hollow terpene/terpenoid delivery inhalation appurtenance.

In particular, the present invention contemplates the use of cannabis terpenoids: wherein limonene, myrcene, a-pinene, linalool, b-caryophyllene, caryophyllene oxide, nerolidol and phytol are examples of phyto-therapeutic agents. T erpenoids are potent affecters of behavior when inhaled even in small doses. Their inhalation manifests often unique therapeutic effects and contributes meaningfully to the entourage effect of cannabinoids: phytocannabinoid-terpenoid interactions may produce synergy with respect to treatment of pain, inflammation, depression, anxiety, addiction, epilepsy, cancer, fungal and bacterial infections (including methicillin-resistant Staphylococcus aureus). Non-cannabinoid terpenes/terpenoids may also counter the intoxicating effects of THC, which could in turn increase its therapeutic index.

In an aspect of the invention such an appurtenance comprises a mouth piece having flattened tapering mouthpiece exterior at a downstream end, adapted to be engaged by a user’s mouth and providing an outlet facilitating the draw of a user inhalation.

Another aspect includes an opposed, longitudinally spaced apart, and generally cylindrical upstream end providing an opening into an inwardly tapering interior for engaging a smoking appliance in an inlet. Smoking appliance herein includes a cannabis“hand rolled joint”,“pre-rolled joint” or the like - typically for example, a“cigarette”.

Yet another aspect includes an intermediate interior portion extending longitudinally between the mouth piece and the inlet at the upstream end which is adapted to receive a terpene/terpenoid-absorbed matrix adapted for dispersal of terpene/terpenoid volatiles into an air stream during inspiration by a user. ln still another aspect of the invention, an airflow channel constriction is provided, communicating between the intermediate portion and the outlet opening, adapted to restrict the cross-section area of the air flow channel to less equal to about 25% (and preferable in the range of from about 20% to about 35 %) of the cross section of the inlet.

Another aspect involves the use of at least one venturi opening through the appurtenance for admitting ambient air into the intermediate interior portion for comingling ambient air with air drawn through the inlet during user inspiration. Moreover, in another aspect, a seat is provided for seating the terpene/terpenoid- absorbed matrix downstream of the venturi opening into the intermediate interior portion and within the airflow channel constriction.

In a particular embodiment of the invention, the airflow channel constriction comprises a conical seat for a corresponding terpene/terpenoid-absorbed matrix comprising a truncated hollow right circular cone, with both the smaller and larger annular openings communicating in flow-through relation through the interior of the cone. The side walls of the cone are adapted to register in seated relation against the conical seat.

The invention also includes such a terpene/terpenoid absorbing matrix in the form of such a truncated hollow right circular cone defining a generally conical exterior and interior, with both smaller and larger annular openings communicating in flow-through relation through the interior of the cone.

Also provided in accordance with the present invention, is a co-pack comprising at least one terpene/terpenoid matrix and a terpene/terpenoid dispenser of selected one or more liquid terpenes/terpenoids for dosing said matrix prior to use. Preferably, such a co-pack includes liquid terpenes/terpenoids in an amount of at least some (effective amount), up to 100ppm of one or more selected terpenes/terpenoids in an ethanolic solution comprising about 5% water and a humectant such as propylene glycol.

For the present purposes, terpenes and terpenoids are associated with prenyl- lipids - as a subclass comprised of small molecular species, preferably and most often derived as phytoextracts, although chemical synthetics may be employed. Terpenoids, (or isoprenoids), are similar to terpenes, but typically differ to the extent that methyl groups are absent or differently positioned, or which include additional oxygen moieties.

More particularly, the present invention relates to the selective delivery of mono and sesquiterpenes and preferably those derived as phytoextracts, especially cannabis phytoextracts. In the latter case particularly, the selective delivery of terpenes/terpenoids may variously facilitate synergistic and/or antagonistic modulation of phytochemical interactions - where modulation mechanisms may variously include: impact on bioavailability, interventions in cellular transport, activation or inactivation of compounds, synergistic partnering at different points of the same signaling cascade (multi-target effects), or inhibition of binding to target proteins.

Terpenes form the largest group of phytochemicals, with more than 100 molecules identified in Cannabis (Rothschild et al., 2005; Brenneisen, 2007). Terpenes are responsible for the odor and flavor of different Cannabis strains. They have therefore likely contributed to the selection of Cannabis narcotic strains under human domestication (Small, 2015). Terpenes are classified in diverse families according to the number of repeating units of 5-carbon building blocks (isoprene units), such as monoterpenes with 10 carbons, sesquiterpenes with 15 carbons, and triterpenes derived from a 30-carbon skeleton. T erpene yield and distribution in the plant vary according to numerous parameters, such as processes for obtaining essential oil, environmental conditions, or maturity of the plant (Meier and Mediavilla, 1998; Brenneisen, 2007). Mono- and sesquiterpenes have been detected in flowers, roots, and leaves of Cannabis, with the secretory glandular hairs as the main production site. Monoterpenes dominate generally. The volatile terpene profile (from 3.1 to 28.3 mg g-1 of flower dry weight, (Fischedick et al., 2010) include mainly d- limonene, b-myrcene, a- and b-pinene, terpinolene and linalool. Sesquiterpenes, and b-caryophyllene and a- humulene in particular, occur also to a large extent in Cannabis extracts (from 0.5 to10.1 mg g-1 of flower dry weight, Fischedick et al., 2010). Triterpenes have also been detected in hemp roots, as friedelin and epifriedelanol (Slatkin et al., 1971 ), in hemp fibers as b- amyrin (Gutierrez and del Rio, 2005) and in hempseed oil as cycloartenol, b- amyrin, and dammaradienol (Paz et al., 2014). Terpenes for example, may alter the pharmacokinetics of THC by increasing the blood- brain barrier permeability. This characteristic has notably been used to patent a transdermal patch, which delivers cannabinoids into the bloodstream by using a terpene as a permeation agent (US20150297556A1 ). Terpenes may also modulate the affinity of THC for the CB1 receptor and interact with neurotransmitter receptors, which may support contributions of terpenes on cannabinoid- mediated analgesic and psychotic effects (McPartland J. M., Russo E. B. (2001 ). Cannabis and Cannabis extracts: greater than the sum of their parts? J. Cannabis Therapeut. 1 103-132.

10.1300/J175v01 n03_08; Russo E. B. (201 1 ). Taming THC: potential cannabis synergy and phytocannabinoid-terpenoid entourage effects. Br. J. Pharmacol. 163 1344-1364.

10.1 1 1 1 /j .1476-5381.201 1.01238.x). There is a recognized need in the art for tailored therapeutic treatments, such as CBD-terpene, to be used against acne, MRSA, depression, anxiety, insomnia, dementia and addiction (Russo E. B. (201 1 ). Taming THC: potential cannabis synergy and phytocannabinoid- terpenoid entourage effects. Br. J. Pharmacol. 163 1344-1364. 10.111 1/j.1476- 5381 .201 1.01238.x).

More generally, phytoterpenes are lipophilic compounds that easily cross membranes and the blood-brain barrier, in particular (Fukumoto et al., 2006). They present a wide- array of pharmacological properties, which have recently been described in several reviews (Russo, 201 1 ; Singh and Sharma, 2015). The biological activities of D- limonene, also commonly found in citrus essential oils, have been well described in the literature. It notably exhibits potent anti- cancer, anxiolytic and immune-stimulating properties in humans (Komori et al., 1995). b-myrcene, a terpene commonly found in hop, is recognized as a potent anti-inflammatory, analgesic, and anxiolytic component (Cleemput et al., 2009). a-Pinene is an acetylcholinesteral inhibitor, and may thereby aid memory abilities (Kennedy et al., 201 1 ), which could counteract the memory deficits induced by THC. Linalool, commonly found in Lavandula angustifolia, possesses similar properties to those described for its monoterpene counterparts, i.e., analgesic, anti-anxiety, anti-inflammatory, and anticonvulsant (Russo, 201 1 ). b-caryophyllene, a well- known active principle of black pepper and Copaiba balsam, possesses potent anti- inflammatory and gastric cytoprotector activities (Singh and Sharma, 2015). Interestingly, it selectively binds to the CB2 receptor and could therefore technically be considered as a phytocannabinoid (Gertsch et al., 2008). Pentacyclic triterpenes such as b- amyrin and cycloartenol have been shown to possess numerous biological activities including anti-bacterial, anti-fungal, anti-inflammatory and anti-cancer properties (Vazquez et al., 2012; Moses et al., 2013). These triterpenes are key contributors to the pharmacological properties of numerous medicinal herbs (Kirby et al., 2008; Yadav et al., 2010; Sawai and Saito, 201 1 ).

BRIEF DESCRIPTION OF THE DRAWINGS:

Figure 1 is a perspective view of the exterior of an embodiment of the appurtenance according to an aspect of the present invention;

Figure 2 is a top view of the appurtenance represented in Figure 1 ;

Figure 3 is a cross section through line F-F of Figure 2;

Figure 4 is an elevated side view of the appurtenance illustrated in the other figures;

Figure 5 is a cross section view through line G-G for Figure 4; Figure 6 is an end view of one end of the appurtenance;

Figure 7 is a view of the opposite end of the appurtenance shown in Figure 6; and,

Figure 8 is a view of a preferred conical matrix.

DETAILED DESCRIPTION OF THE INVENTION:

Referring now to the drawings in general, there is disclosed a hollow terpene/terpenoid delivery inhalation appurtenance 1 comprising a mouth piece 2 having a flattened tapering mouthpiece exterior 3 at a downstream end 4, adapted to be engaged by a user’s mouth and providing an outlet opening 5 facilitating the draw of a user inhalation.

An opposed, longitudinally spaced apart, and generally cylindrical upstream end 6 provides an opening 7 into an inwardly tapering interior 8 for engaging a smoking appliance (not shown) in an inlet 9.

An intermediate interior portion 10 extends longitudinally between the mouth piece 2 and the inlet 9 at the upstream end 6. Portion 10 is adapted to receive a terpene/terpenoid-absorbed matrix 1 1 adapted for release/dispersal of terpene/terpenoid volatiles into an air stream during inspiration by a user.

An airflow channel 12 constriction 12a, (communicating between said intermediate portion 10 and outlet opening 5), is adapted to restrict the cross- section area of air flow channel 12 to between less than equal to about 20% (and preferably in the range of from about 25 to about 35 %) of the cross-section area of inlet 9.

At least one venturi opening 13 through appurtenance 1 is adapted to admit ambient air into the intermediate interior portion 10 for comingling ambient air with air (smoking appliance output) drawn through the inlet 9 during (in response to) user inspiration. The airflow channel 12 constriction 12a cooperate to moderate the draw on the smoking appliance, by restricting the air flow through the channel 12, but also by pulling ambient air in through the venturi opening 13. This reduces the amount of air that is drawn into the smoking appliance and hence the temperature and rate of consumption of the cannabis. Moreover, the venturi opening is preferably sized to drop the temperature of the (mixed) airflow admitted into said upstream end 6 opening 7, by about 80 degrees C relative to the temperature of the pyrolyzed cannabis in the smoking appliance. This reduces the rate of uptake of the absorbed terpene/terpenoid from the matrix, prolonging the release of same over the smoking activity. It, along with the heat consumed in volatilizing the absorbed terpene/terpenoid from the matrix, also reduces the temperature of the air that is introduced into the user’s mouth.

In a preferred form, a seat 14 is provided for seating terpene/terpenoid- absorbed matrix 1 1 , downstream of venturi opening 13 into intermediate interior portion 10 and within airflow channel constriction 12a. As illustrated in this embodiment of the present invention, the airflow channel constriction 12a comprises a conical seat for a corresponding terpene/terpenoid-absorbed matrix 1 1 comprising a truncated hollow right circular cone, with both the smaller and larger annular openings of the matrix 1 1 cone communicating in flow-through relation through the interior of that cone with the side walls of the cone registered in seated relation against said conical seat provided by airflow restriction channel 12a.

A terpene/terpenoid-absorbed matrix 1 1 according to the present invention and comprising a truncated hollow right circular cone defining a generally conical exterior and interior, with both smaller and larger annular openings communicating in flow- through relation through said interior of the cone, is shown in Figure 8.

Preferably, the matrix 1 1 comprises a cellulose filter material (e.g. Whatman #5) or a random woven polypropylene material for absorbing an applied terpene/terpenoid material. In an aspect of the present invention, a co-pack is sold, comprising at least one terpene/terpenoid matrix 1 1 and a terpene/terpenoid dispenser of selected one or more liquid terpenes/terpenoids for dosing said matrix prior to use. The co- pack according to claim 6, wherein said liquid terpenes/terpenoids comprise at least some, up to 100ppm of one or more selected terpenes/terpenoids in an ethanolic solution comprising about 5% water and a humectant such as propylene glycol.

In operation of the present invention, and according to a method thereof, co- delivery of a terpene/terpenoid inhalation supplement is provided by operation of a smoking appliance such as that exemplified in the drawings. The method includes directing output from said smoking appliance (the smoke drawn from the pyrolysis of cannabis) into an appurtenance; introducing ambient air into said appurtenance to reduce the temperature of the output; and, passing the cooled output to a matrix carrying absorbed terpene/terpenoid and humectant to further reduce the temperature of the output and collaterally volatilize of at least a portion of said absorbed terpene / terpenoid and humectant into mixed relation with output to produce a further cooled terpene/terpenoid supplemented smoking appliance output to a mouthpiece for inhalation by a user.

Claims

CLAIMS:

1 . A hollow terpene/terpenoid delivery inhalation appurtenance comprising:

a. a mouth piece having flattened tapering mouthpiece exterior at a downstream end, adapted to be engaged by a user’s mouth and providing an outlet facilitating the draw of a user inhalation, and

b. an opposed, longitudinally spaced apart, and generally cylindrical upstream end providing an opening into an inwardly tapering interior for engaging a smoking appliance in an inlet, and

c. an intermediate interior portion extending longitudinally between the mouth piece and the inlet at the upstream end, and adapted to receive a terpene/terpenoid-absorbed matrix adapted for dispersal of terpene/terpenoid volatiles into an air stream during inspiration by a user; and d. an airflow channel constriction communicating between said intermediate portion and said outlet opening, adapted to restrict the cross- section area of said airflow channel to less equal to about 20% (and preferable in the range of from about 25 to about 35 %) of the cross section of said inlet.

e. at least one venturi opening through said appurtenance for admitting ambient air into said intermediate interior portion for comingling ambient air with air drawn through said inlet during user inspiration; and,

f. a seat for seating said terpene/terpenoid-absorbed matrix downstream of said venturi opening into said intermediate interior portion and within said airflow channel constriction.

2. The appurtenance according to claim 1 wherein said airflow channel constriction comprises a conical seat for a corresponding terpene/terpenoid-absorbed matrix comprising a truncated hollow right circular cone, with both the smaller and larger annular openings communicating in flow- through relation through the interior of the cone and side walls of said cone registered in seated relation against said conical seat.

3. The appurtenance according to claim 1 , wherein said at least one venturi, is adapted to drop the temperature of the airflow admitted into said upstream end opening, by about 80 degrees C.

4. A terpene/terpenoid-absorbed matrix comprising a truncated hollow right circular cone defining a generally conical exterior and interior, with both smaller and larger annular openings communicating in flow-through relation through said interior of the cone.

5. The matrix according to claim 1 or 4 and comprising a cellulose filter or a random woven polypropylene material adapted for absorbing an applied terpene/terpenoid material.

6. A co-pack comprising at least one terpene/terpenoid matrix and a terpene/terpenoid dispenser of selected one or more liquid terpenes/terpenoids for dosing said matrix prior to use.

7. The co-pack according to claim 6, wherein said liquid terpenes/terpenoids comprise at least some, up to 100ppm of one or more selected terpenes/terpenoids in an ethanolic solution comprising about 5% water and a humectant such as propylene glycol.

8. A method for co-delivering a terpene/terpenoid inhalation supplement in operation of a smoking appliance, comprising directing output from said smoking appliance into an appurtenance, introducing ambient air into said appurtenance to reduce the temperature of the output and passing the cooled output to a matrix carrying absorbed terpene/terpenoid, to further reduce the temperature of said output and collaterally volatilize at least a portion of said absorbed terpene/terpenoid into mixed relation with output to produce a further cooled terpene/terpenoid supplemented smoking appliance output to a mouthpiece for inhalation by a user.