Patent Application
20250235391
The present invention relates to a lip balm formulation, and more particularly to a lip balm formulation having a high emulsifier-content Cannabaceae derivative, nicotine, testosterone or caffeine delivery system.
The present invention provides a formulation capable of being topically administered to a mucous membrane surface of the body as a lip balm containing one or more derivates of Cannabaceae, or nicotine, testosterone or caffeine, that may be applied to the mucous membrane surface of lip skin. It also provides a Cannabaceae derivative, nicotine, testosterone or caffeine formulation.
Cannabinoids are compounds derived from the cannabis sativa plant, which is part of the larger group of plants known as Cannabaceae, also commonly known as marijuana. Derivatives of Cannabaceae and more specifically, the plant cannabis sativa contain more than 400 chemicals and approximately 60 cannabinoids. These include cannabidiol and cannabinol. The most active chemical compound of the naturally occurring cannabinoids is tetrahydrocannabinol (THC), particularly A9-THC.
Currently, A9-tetrahydrocannabinol, also known as Dronabinol, is available commercially in Marinol® soft gelatin capsules which have been approved by the Food and Drug Administration (FDA) for the control of nausea and vomiting associated with chemotherapy and for appetite stimulation of AIDS patients suffering from the wasting syndrome. The A9-tetrahydrocannabinol shows other biological activities, which lend themselves to possible therapeutic applications, such as in the treatment of glaucoma, migraine headaches, spasticity, anxiety, analgesia, and drug addiction.
In Marinol®, A9-THC is dissolved in sesame oil and encapsulated in gelatin capsules for oral administration. After oral administration, Dronabinol has an onset of action of approximately 0.5 to 1 hour, with a peak effect at 2-4 hours. The duration of action for psychoactive effects is 4-6 hours, but the appetite stimulant effect may continue for 24 hours or longer after administration. The maximal plasma levels after oral dosing of 20 mg A9-THC in a sesame oil formulation are around 10 ng/ml.
At the present time, some cancer patients manage to obtain prescriptions for marijuana in order to alleviate pain as well as nausea and vomiting due to chemotherapy. This latter situation arises due to poor or partial response from oral therapy, which often requires oral administration two to three times a day to obtain equivalent acute psychological and physiological effects obtained from smoking marijuana.
When administered orally, A9-THC or Dronabinol is almost completely absorbed (90-95%) after a single oral dose. However, due to the combined effect of first pass hepatic metabolism and high lipid solubility, only about 10-20% of an administered dose reaches systemic circulation with highly variable maximal concentrations. It has been found that fasting or food deprivation may decrease the rate of absorption of A9-THC from the sesame oil capsules currently available in the market. Previous studies have reported that another limitation of orally administered A9-THC is the large inter-subject variability in absorption.
U.S. Pat. No. 7,560,465 discloses a lip balm that delivers dissolved caffeine. The caffeine is dissolved in a solvent (water) which is then dispersed in a lipid or wax to make the lip balm. Prior art lip balms used micronized particles of caffeine. This patent fails to even mention a surfactant as part of the lip balm composition.
U.S. Pat. No. 5,085,856 discloses a cosmetic water-in-oil emulsion lipstick comprising a phospholipid and glycerol fatty acid esters emulsifying system. This patent teaches away from using greater than about 10% emulsifier in its lipstick.
U.S. Pat. No. 6,663,853 discloses a lip care moisturizing product in the form of a water-in-oil emulsion, containing at least one fatty acid ester, at least one wax, the total of said at least one fatty acid ester and said at least one wax being at least about 1.0%, liposomes containing water therein, and an emulsifier. The emulsifier content is up to 7.5%.
WO9426234 Patent Application discloses water-in-oil emulsions having a petrolatum base for use as lip balm compositions. The emulsions contain up to about 5 weight percent water and are preferably formulated as microemulsions. The compositions preferably also contain a wax, an oil, and a humectant component. The emulsions contain up to 10% surfactants. The present invention is neither taught nor suggested in the above cited references.
Therefore, a route of administration that avoids first pass hepatic metabolism would represent a significant advance in the art.
The lip balm formulation of the present invention comprises at least one lipid, at least one surfactant, and one or more Cannabaceae derivative, caffeine, nicotine or testosterone, or a combination thereof. The formulation contains greater than about 10 wt. % surfactant. In a preferred embodiment, the formulation contains greater than about 25 wt. % surfactant. In a more preferred embodiment, the formulation contains from about 25 to 60 wt. % surfactant. In another preferred embodiment, the formulation contains from about 30 to 60 wt. % surfactant.
In a preferred embodiment, the components are present in the formulation such that the w/w ratio of surfactant to lipid is in the range of from about 3/1 to 1/3. In a more preferred embodiment, the lipid is present in the range of about 30 wt. % to 60 wt. %; the surfactant is present in the range of about 60 wt. % to 25 wt. %, and the Cannabaceae derivative, caffeine, nicotine or testosterone is present in the range of about 0.1 to 40 wt. %. Preferably, caffeine is present in the formulation from about 5 to 40 wt. %, nicotine or testosterone are present in the formulation of from about 0.1 to 30 wt. %, and the Cannabaceae derivative is present in the formulation from about 0.1 to 25 wt. %. In a more preferred embodiment, the formulation includes other excipients including stabilizers, melting point adjusters, oils, flavorings, colorings, sun screens, additional nutrients or pharmaceuticals, and glycerine.
The lip balm does not contain an aqueous phase. The water content of the lip balm is less than 1.0 wt. %. Preferably, the water content is less than 0.8 wt. %, and more preferably, the water content is less than about 0.5 wt. %.
Further areas of applicability of the present invention will become apparent from the detailed description provided hereinafter. It should be understood that the detailed description and specific examples, while indicating the preferred embodiment of the invention, are intended for purposes of illustration only and are not intended to limit the scope of the invention.
The following description of the preferred embodiment(s) is merely exemplary in nature and is in no way intended to limit the invention, its application, or uses. The present invention provides a formulation comprising one or more Cannabaceae derivative, or nicotine, testosterone or caffeine, capable of being topically administered to a mucous membrane surface of the body as a lip balm that may be applied to the surface of lip skin. Thus, one can combine the standard benefits of a lip balm, such as protecting the lips from heat, cold, sun and wind, with providing a dose of one or more Cannabaceae derivative, or nicotine, testosterone or caffeine. This invention also provides a Cannabaceae derivative, caffeine, testosterone and a nicotine formulation.
The lipids of the present invention may be of animal, vegetable or mineral origin, which are water-insoluble, inert, non-toxic hydrocarbon fats and oils and derivatives thereof, and may comprise any of the commonly commercially available fats or oils approved by the Food & Drug Administration, having melting points in the range of about 90 to 160° F. The lipid may comprise a vegetable oil base commonly known as hard butter. Hard butters are hydrogenated, press fractionated or other processed oils that are processed or recombined to have a solid fat index (percent solid fat vs. temperature) similar to that of cocoa butter. However, other lipids may be used that are relatively hard or solid at room temperature, but melt rapidly in the mouth at a temperature of about 98° F. (mouth temperature). In a preferred embodiment, the lipid is employed in the amounts within the range of from about 30 to 60 wt. %.
Examples of suitable lipids include tallow, hydrogenated tallow, hydrogenated vegetable oil, almond oil, coconut oil, corn oil, cottonseed oil, light liquid petrolatum, heavy liquid petrolatum, olein, olive oil, palm oil, peanut oil, persic oil, sesame oil, vitamin E, soybean oil or safflower oil. Additionally, stearines can be used as a lipid in the present invention. The addition of stearines to the product provides the favorable property of mold-release. Further, the addition of stearines raise the melting point of the composition as high as about 100° F., which is particularly beneficial when the product is shipped or stored in unrefrigerated compartments.
Preferred examples include petrolatum, a mineral oil (Vaseline oil), which may be any petroleum based product; modified or unmodified vegetable oils such as peanut oil, wheat germ oil, linseed oil, jojoba oil, apricot kernel oil, walnut oil, palm oil, pistachio oil, sesame oil, colza oil, cade oil, corn germ oil, peach kernel oil, poppy seed oil, pine oil, castor oil, soya oil, safflower oil, coconut oil, hazelnut oil, grapeseed oil, avocado oil, soy oil, sweet almond oil, calophyllum oil, castor oil, olive oil, sunflower oil, or animal oils such as whale oil, seal oil, menhaden oil, halibut liver oil, cod liver oil, cod, tuna, turtle tallow, horse's hoof, sheep's foot, mink, otter, marmot oil and the like; synthetic oils such as silicon oil such as dimethylpolysiloxane; alkyl and alkenyl esters of fatty acids, such as isopropyl esters of myristic, palmitic and stearic acids and fatty esters which are solid at room temperature; waxes such as lanolin wax, candelilla wax, spermaceti, cocoa butter, karite butter, silicon waxes, hydrogenated oils which are solid at room temperature, sucro-glycerides, oleates, myristates, linoleates, stearates, paraffin, beeswax, carnauba wax, ozokerite, candelilla wax, microcrystalline wax; fatty alcohols such as lauryl, cetyl, myristyl, stearyl, palmityl and oleyl alcohols; polyoxyethylated fatty alcohols; and wax esters, lanolin and its derivatives, perhydrosqualene and saturated esters, ethyl palmitate, isopropyl palmitate, alkyl myristates such as isopropyl myristate, butyl myristate and decyl myristate, hexyl stearate, triglyceride esters, triglycerides of octanoic and decanoic acid, cetyl ricinoleate, stearyl octanoate (Purcellin oil), fatty acids, polyhydric alcohols, polyether derivatives, fatty acid monoglycerides, and hydrogenated palm oil (PARAMOUNT XX and PARAMOUNT X oil), and mixtures of waxes and oils. The preferred lipids are a combination of hydrogenated palm oil and vitamin E. The preferred oils contain less than about 0.2 wt. % water.
Any emulsifier or surfactant or combination thereof approved for use in foods by the Food and Drug Administration and having a relatively low hydrophobic lipophilic balance (HLB) value, in the range of about 0 to 6, is suitable for use in the present invention. The appropriate surfactant minimizes the surface tension of the lipid, allowing it to oil wet and encapsulate the non-oil solid particles. Suitable surfactants include alkyl aryl sulfonate, or alkyl sulfonates, or sulfonated amides or amines, or sulfated or sulfonated esters or ethers, or alkyl sulfonates, of dioctyl sulfonosuccinate and the like, or a hydrated aluminum silicate such as bentonite or kaolin, triglycerol monostearate, triglycerol monoshortening, mono- and di-glyceride and propylene glycol with an HLB of less than 4, octaglycerol monooleate, octaglyceron monostearate, and decaglycerol decaloeate.
The surfactant is preferably a non-water-soluble surfactant having an HLB number of less than about 6 and includes emulsifiers. A preferred surfactant is commercially sold as ATMOS® 300K and is a combination of mono-and di-glycerides made from edible food sources and propylene glycol with an HLB of 2.8. Another preferred surfactant is Defospum E100, a defoamer which is a combination of mono-and di-glycerides sold by Defotec. A third preferred surfactant is Lucrafoam E100, a defoamer which is a combination of mono-, di-and tri-glycerides sold by Levaco Chemicals.
The lip balm may also include other pharmaceutically acceptable agents, such as sweetening agents, including hydrogenated starch hydrolysates, synthetic sweeteners such as sorbitol, xylitol, saccharin salts, L-aspartyl-L-phenylalanine methyl ester, as well as coloring agents, other binding agents, lubricants, such as calcium stearate, stearic acid, magnesium stearate, antioxidants such as butylated hydroxyl-toluene and the like. A sunscreen, well known in the art, can also be added to the lip balm. A stabilizer, such as 27 STEARINE, a glyceryl tristearate may also be used.
Preferred Cannabaceae derivatives include, but are not limited to, tetrahydrocannabinol (THC), Delta(9)-tetrahydrocannabinol, cannabidiol, cannabichromene, cannabinol, cabbabigerol, tetrahydrocannabivarin, cannabidivarin, Delta(8)-tetrahydrocannabinol, tetrahydrocannabinol acid, cannabidiol acid, cannabigerol acid, cannabigerovarin, cannabinovarin, and tetrahydrocannabivarin acid or combinations thereof. Sources of THC include THC extracted in the form of plant oils using various solvents including CO2 and butane, and include Super (77.7%), Distillate (85%), Vape (60%), and Crude (63%) oils. These sources of THC are a mixture of oils that include flavonoids, terpenoids and cannabidiol. The derivatives of Cannabaceae that include THC, CBD, CBN, CBG, CBC, THCV as well as other current and yet to be isolated cannabinoids are present in the lip balm in the range of about 0.1 to about 25.0 wt. %.
The Cannabaceae derivative, caffeine, nicotine or testosterone can be added in any suitable form. A solution comprising Cannabaceae derivatives, caffeine, nicotine or testosterone or micronized Cannabaceae derivative, caffeine, nicotine or testosterone particles may be used.
The lip balm is prepared by means well known in the art. A preferred method is melting the lipid and mixing in the remaining ingredients, then allowing the mixture to cool.
The lip balm formulation contains greater than 10 wt. % surfactant. In a preferred embodiment, the lipid and surfactant components are present in the formulation such that the w/w ratio of surfactant to lipid is in the range of from about 2/1 to 1/2. In a more preferred embodiment, the lipid is present in the range of about 30 wt. % to 60 wt. %; the surfactant is present in the range of about 60 wt. % to 25 wt. %, and the active is present in the range of about 0.1 to 40 wt. %.
The lip balm delivers the Cannabaceae derivatives, caffeine, nicotine or testosterone to the body rapidly, typically in less than about one (1) minute, and preferably in less than about 45 seconds. Testosterone is typically delivered in less than about ten (10) minutes, and preferably from about one (1) to ten (10) minutes.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
A lip balm was prepared according to the following list of ingredients.
The lip balm of Example 7 was tested for effectiveness in administering nicotine. Push tubes of the lip balm were provided to ten (10) test subjects who were trained to detect and note the time to sense the nicotine in their system (the time to satisfaction). Each dose provided about 60 mg of lip balm delivering 1.2 mg of Nicotine to the lips. The time to satisfaction for each test subject is given below.
Tests were run using the lip balm of Example 7. The results are shown in Table 1-5. For Table 1, rapid dissolve mesh pouches were filled with the lip balm. The lip balm was given by sublabial administration of the pouch to five (5) test subjects who were trained to detect and note the time to sense the nicotine in their system (the time to satisfaction). The time for satisfaction data is shown in Table 1, below.
In Table 1, the lip balm was a lump placed in the pouch.
The taste, texture and acceptability were evaluated as well, and found to be acceptable.
Mini chips of lip balm (100 mg lip balm chips containing 2 mg of nicotine per chip) were administered sublabial to five (5) test subjects who were trained to detect and note the time to sense the nicotine in their system (the time to satisfaction). The time for satisfaction data is shown in Table 2, below.
Flat discs of lip balm (200 mg lip balm chips containing 4 mg of nicotine per chip) were administered sublabial to five (5) test subjects who were trained to detect and note the time to sense the nicotine in their system (the time to satisfaction). The time for satisfaction data is shown in Table 3, below.
Rounded drops of lip balm (400 mg lip balm chips containing 9 mg of nicotine per drop) were administered sublabial to five (5) test subjects who were trained to detect and note the time to sense the nicotine in their system (the time to satisfaction). The time for satisfaction data is shown in Table 4, below.
Larger flat discs of lip balm (500 mg lip balm discs containing 10 mg of nicotine per drop) were administered sublabial to five (5) test subjects who were trained to detect and note the time to sense the nicotine in their system (the time to satisfaction). The time for satisfaction data is shown in Table 5, below.
The taste and mouth feel for each of the above samples were found to be acceptable.
The lip balm of Example 4 was tested, and the data is shown in Tables 6-12. For Table 6, rapid dissolve mesh pouches were filled with the lip balm formula of Example 4, 500 mg lip balm containing 70 mg of caffeine. The lip balm was given by sublabial administration to five (5) test subjects who were trained to detect and note the time to sense the caffeine in their system (the time to satisfaction). The time to satisfaction data is shown below.
For Table 7, rapid dissolve mesh pouches were filled with the lip balm formula of Example 4, 400 mg lip balm containing 56 mg of caffeine. The lip balm was given by sublabial administration to five (5) test subjects who were trained to detect and note the time to sense the caffeine in their system (the time to satisfaction). The time for satisfaction data is shown, below.
For Table 8, rapid dissolve mesh pouches were filled with the lip balm formula of Example 4, 300 mg lip balm containing 42 mg of caffeine. The lip balm was given by sublabial administration to five (5) test subjects who were trained to detect and note the time to sense the caffeine in their system (the time to satisfaction). The time for satisfaction data is shown below.
Mini chips of lip balm (100 mg lip balm chips containing 14 mg of caffeine per chip) were administered sublabial to five (5) test subjects who were trained to detect and note the time to sense the caffeine in their system (the time to satisfaction). The time for satisfaction data is shown in Table 9, below.
Chips of lip balm (200 mg lip balm chips containing 28 mg of caffeine per chip) were administered sublabial to five (5) test subjects who were trained to detect and note the time to sense the caffeine in their system (the time to satisfaction). The time for satisfaction data is shown in Table 10, below.
Flat discs of lip balm (400 mg lip balm chips containing 56 mg of caffeine per chip) were administered sublabial to five (5) test subjects who were trained to detect and note the time to sense the caffeine in their system (the time to satisfaction). The time for satisfaction data is shown in Table 11, below.
Flat discs of lip balm blended with hard cinnamon candy (400 mg lip balm chips containing 52 mg of caffeine per chip) were administered sublabial to five (5) test subjects who were trained to detect and note the time to sense the caffeine in their system (the time to satisfaction). The time for satisfaction data is shown in Table 12, below.
Lip balms are prepared according to the following list of ingredients: a surfactant (for example ATMOS 300K), a lipid (for example PARAMOUNT XX), a stabilizer (for example 27 STEARINE) and different amounts of a Cannabaceae derivative (for example THC). The lip balms are tested for effectiveness in administering the Cannabaceae derivative. Push tubes of the lip balm are provided to test subjects who are trained to detect and note the time to sense the Cannabaceae derivative in their system (the time to satisfaction).
The embodiments were chosen and described to best explain the principles of the invention and its practical application to persons who are skilled in the art. As various modifications could be made to the exemplary embodiments, as described above with reference to the corresponding illustrations, without departing from the scope of the invention, it is intended that all matter contained in the foregoing description and shown in the accompanying drawings shall be interpreted as illustrative rather than limiting. Thus, the breadth and scope of the present invention should not be limited by any of the above-described exemplary embodiments but should be defined only in accordance with the following claims appended hereto and their equivalents.
This application is a continuation-in-part of U.S. patent application Ser. No. 18/951,096, which is a continuation of U.S. patent application Ser. No. 18/781,282 filed Jul. 23, 2024, now issued as U.S. Pat. No. 12,171,847, which is a divisional of U.S. patent application Ser. No. 17/403,679 filed Aug. 16, 2021, now issued as U.S. Pat. No. 12,053,535, which is a continuation-in-part of U.S. patent application Ser. No. 16/538,866 filed Aug. 13, 2019, abandoned, which claims priority to U.S. Provisional Patent Application 62/718,261 filed Aug. 13, 2018, the entire contents of each of which are hereby incorporated by reference as if fully set forth herein.
| Number | Date | Country | |
|---|---|---|---|
| 62718261 | Aug 2018 | US |
| Number | Date | Country | |
|---|---|---|---|
| Parent | 17403679 | Aug 2021 | US |
| Child | 18781282 | US |
| Number | Date | Country | |
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| Parent | 18781282 | Jul 2024 | US |
| Child | 18951096 | US |
| Number | Date | Country | |
|---|---|---|---|
| Parent | 18951096 | Nov 2024 | US |
| Child | 19177144 | US | |
| Parent | 16538866 | Aug 2019 | US |
| Child | 17403679 | US |
