Aerosol formulation
Technical Field
The invention relates to the field of medicines, in particular to an aerosol.
Background
The use of cannabis as a drug and medicine dates back to 440 B.C., but the psychoactive drug, Tetrahydrocannabinol (THC), was used in the past. The side effects of tetrahydrocannabinol, such as hallucinography and psychosis, limit its medical application. In the last decade, along with the research and discovery of a brand new pharmacological action mechanism of Cannabidiol (CBD) without a mental action component in cannabis sativa, the research and application of cannabinol compounds are restarted under the guidance of Europe and America all over the world, and particularly the research on Cannabidiol extracted from low-THC and low-toxicity industrial cannabis sativa and the like. Modern pharmaceutical research proves that cannabidiol has opposite effects with tetrahydrocannabinol, can treat pain, epilepsy, spasm, psychosis and depression, has slight side effect, can be used for a long time, and has good tolerance and no addiction. Cannabidiol based drugs, such as epididolex and Sativex, have been approved for marketing in the united states and europe, respectively.
In recent years, patients who have used cannabis for medical purposes in the past because of spasticity, depression and pain have gradually begun to switch to the use of the psychoactive, safer cannabidiol products. However, in western countries, there are limitations to production costs, process technology and western habits. Many cannabidiol products, including the functional ingredients of Epidiolex and Sativex described above, are highly purified, even chemically synthesized, with only 1, or 2 chemical components in the product. Wherein the characteristic aroma of the hemp has been completely removed. Thus, the former patients who use natural cannabis for medical purposes have a reduced acceptance of odorless products, and odorless cannabidiol products require patient re-adaptation, and most importantly, lack of psychological comfort and cueing of the drugs that are very useful during treatment.
Disclosure of Invention
The invention aims to provide an aerosol which is added with micromolecular perfuming ingredients and solves the problem that the acceptance of odorless products of patients who originally use natural medical cannabis is reduced due to odorless cannabidiol products.
In order to solve the technical problems, the invention adopts the following technical scheme:
an aerosol comprises essential oil of industrial hemp flower and leaf and medicinal components.
Preferably, the industrial hemp flower and leaf essential oil is obtained by primary extraction and fine extraction of industrial hemp flower and leaf, wherein,
carrying out initial extraction: performing supercritical extraction on industrial hemp to obtain a primary extract;
fine extraction: and carrying out chromatography treatment on the primary extract to obtain the industrial cannabis sativa leaf essential oil.
Preferably, the initial extraction step is carried out in an extraction kettle, the flow of the supercritical carbon dioxide fluid is one extraction kettle volume every 3-10 minutes, for example, the volume of the extraction kettle is 25 liters, the flow rate of the carbon dioxide is 25 liters every 3-10 minutes, the temperature in the extraction kettle is 25-60 ℃, the pressure in the extraction kettle is 10-40MPa, and the extraction time is 20-360 min.
Preferably, an entrainer is added in the supercritical extraction step, the entrainer is at least one of ethanol, n-hexane, cyclohexane or ethyl acetate, and the mass ratio of the use amount of the entrainer to the materials is 0.1-10: 100.
Preferably, the industrial hemp flower and leaf essential oil is a first distillation section obtained by rectifying industrial hemp flower and leaf by a rectification method, the rectification method comprises the steps of extracting a primary extract from powder obtained by grinding industrial hemp flower and leaf by using an organic solvent, and rectifying the extract at the temperature of 110-190 ℃, wherein the organic solvent comprises gasoline, n-hexane, cyclohexane, alcohol, chloroform or ethyl acetate.
Preferably, the industrial hemp flower and leaf and water are boiled together, the distillation product is subjected to co-distillation, and the upper-layer component obtained after the distillation product is condensed and layered is the industrial hemp flower and leaf essential oil, wherein the weight ratio of the industrial hemp flower and leaf to the water is 1: 1-2.
Preferably, the industrial hemp flower and leaf is obtained by drying flower and leaf of industrial hemp at 90-120 deg.C until the water content is less than 10%, and pulverizing to 50-200 mesh.
Preferably, the aerosol also comprises a penetrating agent and a propellant, wherein the industrial cannabis sativa leaf essential oil accounts for less than 3% of the total mass of the aerosol.
Preferably, the osmotic agent is at least one of azone, menthol and chondroitin sulfate; the propellant is compressed gas of nitrogen, carbon dioxide or nitrous oxide, hydrocarbons, fluorochloroalkanes or hydrofluorocarbons.
Preferably, the penetrating agent, the industrial hemp flower and leaf essential oil, the medicinal components and the solvent are mixed to prepare a solution; filling the obtained solution into an aerosol can, sealing, and filling propellant.
The invention uses methods such as steam distillation, rectification or supercritical extraction separation and the like to prepare the 'essential oil of industrial hemp flower leaves' from the industrial hemp flowers, and the essential oil only contains micromolecular aromatizing components, which is the key or core step of the application.
Compared with the prior art, the invention has the beneficial effects that:
the industrial hemp flower and leaf essential oil added in the invention only contains micromolecular aromatizing components and does not contain diterpene compounds, such as cannabidiol, tetrahydrocannabinol and other medicinal active components, so that the biological activity of the added object is not obviously influenced. However, after the industrial hemp flower and leaf essential oil is added, all odorless hemp phenolic products can have the characteristic aroma of natural industrial hemp, and the odorless hemp phenolic products complement sensory loss, psychological comfort and suggestion effects. The market value of the original product and the cognition degree of the consumer can be greatly improved. The addition of the industrial hemp flower and leaf essential oil in the odorless hemp phenol aerosol can improve the acceptance of patients using natural medical hemp on odorless products.
The industrial hemp flower and leaf essential oil in the application mainly comprises sesquiterpenes and monoterpenes, mainly comprises caryophyllene (caryophylelene), trans α -bergamotene (trans- α -bergamotene), humulene (humulene), cis β -farnesene (cis- β -farnesene) and α -pinene (α -pinene), d-limonene (d-limonene), p-cymol (p-cymol 0.65%) and cineol (cineole) and the like, and the extraction rate of the industrial hemp flower and leaf essential oil can reach 0.1% of the total weight of the industrial hemp flower and leaf essential oil, wherein the identified aromatizing components account for 80% of the industrial hemp flower and leaf essential oil and are far superior to the prior art.
Detailed Description
In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention is further described in detail with reference to the following embodiments. It should be understood that the specific embodiments described herein are merely illustrative of the invention and are not intended to limit the invention.
Comparative example:
an aerosol comprises aromatic cannabinol product as medicinal component, penetrant and propellant, wherein the penetrant is at least one of azone, menthol and chondroitin sulfate; the propellant is at least one of compressed gas of nitrogen, carbon dioxide or nitrous oxide, hydrocarbons, chlorofluorocarbons, hydrochlorofluorocarbons or hydrofluorocarbon compounds; mixing penetrant, industrial hemp flower and leaf essential oil, medicinal components and solvent to prepare solution; filling the obtained solution into an aerosol can, sealing, and filling propellant. Parts not mentioned or not described in detail in this comparative example, such as how to prepare the solution, how to seal, how to fill the propellant, whether or not a solvent is required, the kind of solvent, etc., are within the prior art.
Example 1:
on the basis of the comparative example 1, the industrial hemp flower and leaf essential oil is added, and the industrial hemp flower and leaf essential oil is obtained by carrying out primary extraction and fine extraction on industrial hemp leaves, wherein,
carrying out initial extraction: carrying out supercritical extraction on industrial hemp, wherein an entrainer is added in the supercritical extraction step, the entrainer can be at least one of ethanol, n-hexane, cyclohexane or ethyl acetate, and the mass ratio of the use amount of the entrainer to the materials is 0.1-10: 100; the primary extraction step is carried out in an extraction kettle, the flow of supercritical carbon dioxide fluid is one extraction kettle volume every 3-10 minutes, the temperature in the extraction kettle is 25-60 ℃, the pressure in the extraction kettle is 10-40MPa, and the extraction time is 20-360min, so as to obtain a primary extract;
fine extraction: and carrying out chromatography treatment on the primary extract to obtain the industrial cannabis sativa leaf essential oil.
Wherein the volume ratio of the entrainer to the cyclohexane is 2:1, the ratio of the entrainer flow rate to the supercritical carbon dioxide fluid flow rate is 0.02, the supercritical carbon dioxide fluid flow rate is 6 minutes and one extraction kettle volume, the temperature in the extraction kettle is 40 ℃, the pressure in the extraction kettle is 25MPa, and the extraction time is 220 minutes, the effect is optimal, the extraction rate of the industrial hemp flower and leaf essential oil can reach 0.103 percent of the total weight of the industrial hemp flower and leaf, and the identified fragrance-providing component accounts for 82.1 percent of the industrial hemp flower and leaf essential oil.
Example 2:
on the basis of the comparative example 1, the industrial hemp flower and leaf essential oil is added, the industrial hemp flower and leaf essential oil is a first distillation section obtained by rectifying the industrial hemp flower and leaf by using a rectification method, the rectification method specifically comprises the steps of extracting a primary extract from powder obtained by grinding hemp flower and leaf by using an organic solvent, and rectifying the extract at the temperature of 110-190 ℃, wherein the organic solvent comprises gasoline, normal hexane, cyclohexane, alcohol, chloroform or ethyl acetate.
Wherein the organic solvent is cyclohexane, the effect is optimal when the rectification temperature is 155 ℃, the extraction rate of the essential oil of the leaves of the industrial hemp flowers and leaves can reach 0.93 percent of the total weight of the leaves of the industrial hemp flowers and leaves, and the identified proportion of the aromatizing components in the essential oil of the leaves of the industrial hemp can reach 78.7 percent.
Example 3:
adding essential oil of flowers and leaves of industrial hemp on the basis of the comparative example 1, drying the flowers and leaves of the industrial hemp at 90-120 ℃ until the water content is less than 10%, then crushing the flowers and leaves of the industrial hemp to 50-200 meshes, boiling the crushed flowers and leaves together with water according to the weight ratio of 1:1-2, co-distilling the crushed flowers and leaves, and condensing and layering the distillate to obtain an upper-layer component, namely the essential oil of the flowers and leaves of the industrial hemp, wherein the weight ratio of the flowers and leaves of the industrial hemp to the water is 1: 1-2.
Wherein, flowers and leaves of industrial hemp are dried at 105 ℃ until the water content is less than 8 percent, then are crushed into 70-80 meshes, and are boiled together with water according to the weight ratio of 1:1.5, and the effect is optimal. The extraction rate of the essential oil of the industrial hemp flowers and leaves can reach 0.91 percent of the total weight of the industrial hemp flowers and leaves, wherein the identified perfuming ingredients account for 77.8 percent of the essential oil of the industrial hemp flowers and leaves.
The components of the industrial hemp flower and leaf essential oil obtained with the best results in examples 1-3 were tested and the results are shown in the following table, wherein the control group was a non-odorous cannabinol product.
The results of counting the usage effects of the aerosols obtained in examples 1 to 3 and the control group are shown in the following table.
As can be seen from the above table, the therapeutic effects of examples 1 to 3 on pain, epilepsy, convulsions, psychosis and depression were all significantly improved as compared with the control group.
Although the invention has been described herein with reference to a number of illustrative embodiments thereof, it should be understood that numerous other modifications and embodiments can be devised by those skilled in the art that will fall within the spirit and scope of the principles of this disclosure. More specifically, various variations and modifications are possible in the component parts and/or arrangements of the subject combination arrangement within the scope of the disclosure and claims of this application. In addition to variations and modifications in the component parts and/or arrangements, other uses will also be apparent to those skilled in the art.