CN112137935B - Composition and application thereof - Google Patents
Composition and application thereof Download PDFInfo
- Publication number
- CN112137935B CN112137935B CN202011159114.2A CN202011159114A CN112137935B CN 112137935 B CN112137935 B CN 112137935B CN 202011159114 A CN202011159114 A CN 202011159114A CN 112137935 B CN112137935 B CN 112137935B
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- extract
- hemp
- sweet wormwood
- composition
- cannabis
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Abstract
The application discloses a composition, which is characterized by comprising a hemp extract and a sweet wormwood extract, wherein the ratio of the hemp extract to the sweet wormwood extract is 10: 1 to 1: 10. the application also discloses the use of the composition in the preparation of a medicament for acne, inflammatory reactions and/or allergic erythema, antibacterials.
Description
Technical Field
The invention relates to the field of biological medicines, in particular to a cannabis sweet wormwood composition and application thereof.
Background
The skin is the tissue with the largest area of the human body, is positioned on the outermost layer of the body surface, and has the functions of barrier, absorption, secretion, excretion, metabolism, immunity, thermoregulation and sensation. The skin barrier is a basic function and comprises an epidermal penetration barrier, an immune barrier, a pigment barrier and the like, and simultaneously, the skin microecology and the acidic environment are also in contact with the skin barrier, so that the normal physiological metabolism of the skin is maintained.
The epidermis has the function of a penetration barrier, can resist the invasion of antigen substances, microorganisms, sunlight and the like to the outside, and can prevent the loss of nutrients and water in the body to the inside. The epidermal permeability barrier is impaired, transepidermal water loss (TEWL) increases, and the skin becomes dry and desquamating. Meanwhile, the resistance to external antigens and microorganisms is reduced, which can lead to various skin diseases. The epidermal penetration barrier, the immune barrier, the acidic barrier and the microecology form an integral defense system, the epidermal microecology and the pH value can influence the epidermal penetration barrier, the epidermal penetration barrier is damaged, and other barrier functions can be influenced.
The epidermal permeability barrier is affected by various factors, such as intrinsic factors like age, and extrinsic factors like ultraviolet light. The epidermal permeability barrier is damaged, the elderly are easy to have pruritus and skin inflammatory reaction, and infants are easy to suffer from atopic dermatitis. Ultraviolet light is a major extrinsic factor affecting the epidermal permeability barrier. Many studies currently show that the occurrence of skin diseases such as atopic dermatitis, polymorphous light eruptions, acne, rosacea, eczema, photoaging, etc. are all associated with impaired epidermal penetration barrier, suggesting that attention should be paid to repair the impaired epidermal penetration barrier function in the clinical treatment of such skin diseases.
Disclosure of Invention
To achieve the above object, the present application provides a composition characterized by comprising a cannabis extract and a artemisia apiacea extract in a ratio of 10: 1 to 1: 10.
in certain embodiments, the composition has at least one of the following functions:
a) antioxidation;
b) protection against damage to the skin by UVA and/or UVB;
c) relieving inflammatory or allergic reactions;
d) inhibiting the growth of bacteria.
In certain embodiments, the cannabis extract is from cannabis mosaic, cannabis kernel, cannabis seed oil, and/or cannabis stem powder.
In certain embodiments, the artemisia apiacea extract is from artemisia apiacea leaves.
In certain embodiments, the cannabis extract is cannabidiol.
In certain embodiments, the cannabidiol is not less than 95% pure (by mass).
In certain embodiments, the artemisia apiacea extract is artemisinin.
In certain embodiments, the artemisinin is not less than 95% (mass ratio).
In certain embodiments, the cannabis extract is prepared by: selecting hemp flowers and leaves of 9-10 months old, preparing a dry product, adding 10 times of 95% ethanol by weight of the dry product, carrying out ultrasonic extraction, separating an extracting solution, and carrying out vacuum concentration and drying.
In some embodiments, the method for preparing the artemisia apiacea extract comprises the following steps: selecting leaves of Artemisia annua of 9-10 months old, preparing into dry product, adding 10 times of 95% ethanol, ultrasonic extracting to separate extractive solution, vacuum concentrating, and drying.
In certain embodiments, the ratio of cannabis extract and artemisia apiacea extract is 10: 1.
in certain embodiments, the ratio of cannabis extract and artemisia apiacea extract is 5: 1.
in certain embodiments, the ratio of cannabis extract and artemisia apiacea extract is 1: 1.
in certain embodiments, the ratio of cannabis extract to artemisia apiacea extract is 1: 5.
in certain embodiments, the ratio of cannabis extract and artemisia apiacea extract is 1: 10.
in certain embodiments, the composition is prepared by a method comprising: a) mixing hemp fruit and sweet wormwood leaf 1: 1 mixing and preparing volatile oil by a distillation method; or, b) hemp leaf and artemisia apiacea leaf 2: 1, mixing, drying at 40-50 ℃, carrying out superfine grinding, and then sieving with a 300-mesh sieve.
In another aspect, the present application also provides the use of a composition as described herein for the preparation of a medicament for the prevention, alleviation or treatment of acne, inflammatory reactions and/or allergic erythema, antibacterial.
In certain embodiments, the pharmaceutical product is configured for transdermal administration.
In certain embodiments, the pharmaceutical product comprises a suitable excipient.
In certain embodiments, the pharmaceutical product comprises a suitable excipient.
In certain embodiments, the composition is present in the pharmaceutical product at a mass fraction of 0.5% to 10%.
In certain embodiments, the pharmaceutical product is configured as a cream, emulsion, suspension, aqua, powder, mask.
The combination of the hemp extract and the artemisia apiacea extract has good effects of resisting oxidation, relieving inflammatory reaction or allergic reaction and inhibiting bacterial growth, the effect of the combination is obviously superior to the effect of the single hemp extract or the artemisia apiacea extract, the synergistic effect is achieved, and unexpected technical effects are achieved.
Detailed Description
The present invention will now be further described with reference to the following examples, which are intended to be illustrative only, and the invention may be embodied in many different forms and should not be construed as being limited to the embodiments set forth herein.
Example 1 preparation of extracts of cannabis and Artemisia annua
Hemp extract: selecting hemp flower leaves with bud emergence within 9-10 months, and naturally drying in the sun, or drying in a forced air oven at 50 deg.C until the water content is less than 10%. Weighing 100 g of dry leaves in a triangular flask with a plug, adding 1L of 95% ethanol, performing ultrasonic extraction (Shanghai ultrasonic generator), setting the extraction power at 60K and the temperature at 60 deg.C for 30min, filtering, separating the extractive solution, and vacuum concentrating and drying until no liquid flows out.
The preparation method of cannabidiol comprises the following steps: the above hemp extract was dissolved in 500ml of chloroform and extracted 4 times with pure water (75 ml each time). Separating chloroform soluble part (3g) with silica gel chromatography, developing with 4% ethanol-containing chloroform, determining the development position with cannabidiol standard, scraping off silica gel at corresponding position, dissolving with chloroform, adding 20% ethanol, and crystallizing to obtain cannabidiol with content of above 95%.
Sweet wormwood herb extract: selecting folium Artemisiae Annuae before budding in 9-10 months, and naturally drying in the sun, or oven drying in a forced air oven at 50 deg.C until water content is less than 10%. Weighing 100 g of dry leaves by using a triangular bottle with a plug, adding 1L of 95% ethanol, performing ultrasonic extraction (Shanghai Xin ultrasonic generator), setting the extraction power at 60K and the temperature at 60 ℃, extracting for 30min, filtering and separating the extract, and performing vacuum concentration and drying until no liquid flows out.
The preparation method of the artemisinin comprises the following steps: dissolving the sweet wormwood extract by using petroleum ether, adsorbing by using a silica gel column, washing by using petroleum ether with 2 times of column volume, and then adding the petroleum ether: acetone 3: 1, collecting the eluate, vacuum drying, dissolving with ethanol, and crystallizing to obtain artemisinin extract with artemisinin content of more than 95%.
Example 2 antioxidant Activity assay
The currently established chemical model methods include Trolox Equivalent Antioxidant Capacity (TEAC), 1-diphenyl-2-trinitrophenylhydrazine (DPPH), total-free-radical-capturing antioxidant parameter (TRAP), and total-oxygen-radical scavenging capacity (TOSC). These methods only measure the anti-oxidation ability of a single plant natural component based on its physicochemical properties (e.g., water solubility or lipid solubility), and do not use lipids that are easily oxidized by free radicals as a standard reference, and thus it is difficult to truly reflect the anti-oxidation activity of the plant natural active component. The Oxygen Radical Absorbance Capacity (ORAC) method can determine the inhibition and elimination effect of an antioxidant on superoxide radicals generated by azodiamidinopropane hydrochloride (ABAP), is a classical method for evaluating the antioxidant activity of an antioxidant by the capacity of eliminating free radicals such as ROO-, OH-and the like generated by ABAP through hydrogen atom transfer, and uses the area under the attenuation curve (AUC) of a fluorescence indicator as a quantitative means. This method can combine the inhibition time and inhibition of free radicals by the antioxidant in a single amount as compared to other antioxidant evaluation methods. The ORAC method is a commonly used method for evaluating antioxidant activity internationally, and is now an important standard for evaluating antioxidant capacity of food by the United states department of agriculture, the United states national institutes of health, and the United states Food and Drug Administration (FDA). ORAC is widely used as an important evaluation standard of functional food in food and functional food industries of America, Europe, Japan and the like.
The antioxidant activities of the cannabis extracts and artemisia apiacea extracts obtained in example 1, used alone and in formulations thereof, were compared using the oxygen free radical scavenging assay (ORAC) and methods reference literature (Yuxinke, Ming Jian, Zhilinging, Liyuzhou, Yan Huiming, Wangqiming, Zhaojichun. effect of vacuum freeze-drying on the polyphenol content of chrysanthemum and its antioxidant activity [ J ] food and machinery, 2020,36(6): 138-: 144.) see Table 1.
TABLE 1 antioxidant Activity
As shown in Table 1, the antioxidant activity of the compound is superior to the effect of single use of sweet wormwood or hemp, and is also superior to the simple addition of 2 kinds of sweet wormwood or hemp, and the compound has a synergistic effect.
Example 3 anti-inflammatory and antiallergic Activity assay of active ingredients of Cannabis sativa and Artemisia annua extracts
Cannabidiol and artemisinin prepared as in example 1 were used to verify their anti-inflammatory and anti-allergic effects. Mast cells, which are derived from hematopoietic progenitor cells and are widely distributed in connective tissues, are found in many cases under the skin, are large in size, contain chromophilous coarse particles in the cytoplasm, and when stimulated, mediators (histamine, heparin, Protease, hydrolytic enzymes, etc.) stored in the cells are released to participate in various immune reactions, including inflammatory reactions and allergic reactions. The inflammatory response is closely related to mast cell degranulation and is also a key step in the allergic reaction process, and inhibition of mast cell degranulation and histamine release can reduce the intensity of the inflammatory response, and thus can be used to verify the anti-inflammatory and anti-allergic effects of certain active ingredients. The results are shown in Table 2.
TABLE 2 anti-inflammatory and antiallergic results
In table 2, mast cell degranulation (%) × 100 (degranulated mast cell number/total mast cell number); histamine release rate (%) (histamine release/total histamine release) × 100; compound 1: cannabidiol: 1, artemisinin: 1; and (3) compound preparation 2: cannabidiol: artemisinin 10: 1; compound 3: cannabidiol: 1, artemisinin: 10; DMSO is dimethyl sulfoxide; LPS: a lipopolysaccharide.
The results show that the artemisinin and the cannabidiol have good anti-inflammatory and anti-allergic effects, and the artemisinin and the cannabidiol are combined in different proportions to have a synergistic effect.
Example 4 detection of the bacteriostatic action of active ingredients of extracts of Cannabis sativa and Artemisia annua
The sterilized solid LB medium was heated to melt and when cooled to 50 ℃ each 20ml of medium was poured into a sterile petri dish. After the plates were allowed to air dry, 0.1mL of the test drug (containing 20% of the cannabis sativa or artemisia annua extract prepared in example 1) and 0.1mL of the test bacterial suspension (10 mL) were removed separately 6 Pieces/ml), evenly spread on a dosing plate, each treatment was repeated 3 times, spreading for 30min and inverting. A control group was additionally set, and the drug solution was replaced with an equal amount of sterile water (dissolved drug substance) by applying bacteria. The above operation is performed in a clean bench. And culturing the prepared bacterial plate at the constant temperature of 37 ℃ for 24h, counting the number of colonies, and calculating the bacteriostasis rate according to the following formula.
TABLE 3
The results show that the composition of the cannabis sweet wormwood herb extract has better bacteriostatic effect.
Example 5 preparation of the composition
Preparation of sweet wormwood cannabis composition, cannabis fruit and sweet wormwood leaves 1: 1 mixing, and preparing volatile oil by a distillation method.
Example 6 preparation of the composition
The preparation of the sweet wormwood and hemp combination comprises the steps of preparing hemp leaves and sweet wormwood leaves 2: 1, mixing, drying at 45 ℃ for 2 hours, micronizing and sieving by a 300-mesh sieve.
The foregoing detailed description of the preferred embodiments of the invention has been presented. It should be understood that numerous modifications and variations could be devised by those skilled in the art in light of the present teachings without departing from the inventive concepts. Therefore, the technical solutions that can be obtained by a person skilled in the art through logical analysis, reasoning or limited experiments based on the prior art according to the concepts of the present invention should be within the scope of protection determined by the claims.
Claims (3)
1. Use of the composition in the manufacture of a medicament for the prevention, alleviation or treatment of inflammatory reactions and/or allergic erythema, antibacteria; the composition comprises a hemp extract and a sweet wormwood extract, wherein the ratio of the hemp extract to the sweet wormwood extract is 10: 1 to 1: 10; the preparation method of the hemp extract comprises the following steps: selecting hemp flowers and leaves of 9-10 months old, preparing a dry product, adding 10 times of 95% ethanol by weight of the dry product, carrying out ultrasonic extraction, separating an extracting solution, and carrying out vacuum concentration and drying; the preparation method of the sweet wormwood herb extract comprises the following steps: selecting leaves of Artemisia annua of 9-10 months old, preparing into dry product, adding 10 times of 95% ethanol, ultrasonic extracting to separate extractive solution, vacuum concentrating, and drying.
2. The use of claim 1, wherein the cannabis extract is cannabidiol.
3. The use of claim 1, wherein the artemisia apiacea extract is artemisinin.
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