A plant anti-allergic, antipruritic and analgesic composition, preparation method and application thereof

Abstract

The present invention relates to the technical field of plant compositions, and in particular to a plant anti-allergic, antipruritic and analgesic composition and its application. The present application discloses a plant anti-allergic, antipruritic and analgesic composition, which comprises the following raw materials by weight percentage: gentiana cyanus extract: 0.5%-5%, kava root extract: 1%-10%, prickly pear cactus leaf extract: 0.5%-5%, Centella asiatica extract: 1%-10%, and the balance is water. The present application provides a plant anti-allergic, antipruritic and analgesic composition, which achieves the effects of anti-inflammatory, anti-allergic, antipruritic and analgesic by inhibiting NO generation, inhibiting histamine pathways and inhibiting TRPV1 ion channels.

Description

Technical Field

[0001] The invention relates to the technical field of plant compositions, and in particular to a plant anti-allergic, antipruritic and analgesic composition and application thereof. Background Art

[0002] With the development of society and the continuous improvement of people's living standards, industrialization has led to changes in people's living environment, and the frequency of skin problems has become higher and higher, especially when the skin is troubled by symptoms such as redness, swelling, itching, and pain, which makes people miserable. Such as sensitive skin, small red papules after mosquito bites, itchy skin diseases (dermatitis, urticaria, psoriasis, eczema, dry skin disease, etc.), and renal dialysis and visceral diseases without skin diseases (such as diabetes, blood diseases, kidney disease, hyperthyroidism, multiple sclerosis, etc.). The itching makes people scratch unbearable, which then causes skin infection or inflammation. This is because scratching the skin will lead to defects in the skin barrier function, making it extremely vulnerable to physical and chemical stimuli and bacterial infection. At the same time, pain follows the skin damage.

[0003] In the prior art, the anti-allergic, antipruritic and analgesic products are mostly hormone products (such as antihistamines, topical preparations of adrenocortical steroids, non-steroidal anti-inflammatory drugs, etc.), which are highly dependent and have large side effects. Especially, long-term use of steroids can cause defects and adverse reactions such as adrenal cortex hypofunction and rebound phenomenon, and infants and young children need to use them with caution. Although there are also some natural Chinese medicine ingredients, they are dark in color, pungent in smell, slow in onset, and unsatisfactory in anti-allergic and antipruritic effects. It can be seen that the existing market products still have defects in use, and people's demand for safe and effective natural anti-allergic, antipruritic and analgesic products is also increasing.

[0004] In view of the shortcomings and deficiencies of the above-mentioned technologies, the present invention provides a plant anti-allergic, antipruritic and analgesic composition. The composition is composed of gentiana cyanus extract, kava root extract, opuntia cochinchinensis leaf extract and Centella asiatica extract. It can solve the problems of redness, swelling, itching and pain of the skin through the four major mechanisms of anti-inflammatory, anti-allergic, antipruritic and analgesic. Summary of the invention

[0005] In order to overcome the deficiencies of the prior art, the present invention provides a plant anti-allergic, antipruritic and analgesic composition, a preparation method and its application. The composition achieves the effects of anti-inflammatory, anti-allergic, antipruritic and analgesic by inhibiting NO generation, inhibiting histamine pathways and inhibiting TRPV1 ion channels.

[0006] The technical solution adopted by the present invention to solve its technical problem is:

[0007] A plant anti-allergic, antipruritic and analgesic composition, comprising the following raw materials by weight percentage:

[0008] Blue Gentiana Extract: 0.5%-5%

[0009] Kava root extract: 1%-10%

[0010] Opuntia cactus leaf extract: 0.5%-5%

[0011] Centella asiatica extract: 1%-10%

[0012] The balance is water.

[0013] Furthermore, the plant anti-allergic, antipruritic and analgesic composition comprises the following raw materials by weight percentage:

[0014] Gentiana caerulea extract: 0.15%-4%

[0015] Kava root extract: 3%-8%

[0016] Opuntia cactus leaf extract: 0.15%-4%

[0017] Centella asiatica extract: 3%-8%

[0018] The balance is water.

[0019] Furthermore, the plant anti-allergic, antipruritic and analgesic composition comprises the following raw materials by weight percentage:

[0020] Gentiana caerulea extract: 3%

[0021] Kava root extract: 6%

[0022] Opuntia cactus leaf extract: 2%

[0023] Centella asiatica extract: 5%

[0024] The balance is water.

[0025] Furthermore, the blue gentian extract is made from wild blue gentian flowers from Tibet, and its gentiopicroside content is controlled at 10%-15%, which is higher than the gentiopicroside content of other gentian extracts on the market of 0.3%-5%.

[0026] Furthermore, the kava root extract is carefully selected from the roots of kava grown on South Pacific islands, and the kavalactone content of the kava root extract is controlled at 3%-10%, which is much higher than the kavalactone content in the stems and fresh leaves.

[0027] Furthermore, the Opuntia serrata leaf extract is made from carefully selected Mexican edible cactus, and the flavonoid content is controlled at 0.05%-0.2%, and the alkaloid content is controlled at 0.05%-0.15%.

[0028] Furthermore, the Centella asiatica extract is made from wild leaves of Centella asiatica from the Madagascar Plateau, and the content of madecassoside and asiaticoside thereof is greater than 70%.

[0029] The mechanism of action of gentiana jasminoides extract, kava root extract, opuntia cochinchinensis leaf extract, and centella asiatica extract is broken down as follows, and their combination has a synergistic effect.

[0030] Blue gentian extract is extracted from wild blue gentian flowers in the plateau. In addition to high content of gentiopicroside, it also contains a series of active ingredients for scavenging free radicals and self-repairing. The content of these ingredients in gentian flowers is much higher than that in gentian roots and leaves. The extract can act on the receptors of inflammatory response and interfere with Ca 2+ The influx of inflammatory cells inhibits the early stage of inflammatory response, quickly blocks the histamine channel, inhibits inflammation from the source and relieves the itching of the skin. At the same time, Gentiana can reduce the pain of persistent inflammation by downregulating the expression of NR2B subunit in NMDA, thus achieving the analgesic effect.

[0031] When the skin is stimulated, TRPV1 receptors are activated, causing a burning and stinging sensation on the skin. Kava root extract can bind to lipid membranes and non-specifically regulate GABA receptors, causing Cl - Channel open, Cl - Influx causes neurons to hyperpolarize and depolarize, inhibits cell excitation, relieves peripheral pain, and has no dependence effect. At the same time, it stabilizes the Na+ channels of nerve cells, reduces nerve cell excitation, and blocks nerve impulse conduction, thus playing a role of local anesthesia and rapid analgesia.

[0032] The extract of Opuntia cactus leaves can significantly inhibit the activity of hyaluronidase, inhibit inflammatory response, scavenge reactive oxygen species, inhibit DNA damage caused by -OH, stimulate fibroblast migration, accelerate collagen formation and blood vessel production, and promote the healing of damaged skin.

[0033] Centella asiatica extract can reduce the excessive synthesis of inflammatory mediators (1L-1α, PGE2), reduce the adhesion of polynuclear neutrophils (PNN) to keratinocytes (adhesion is related to autologous induced inflammation), reduce the skin anti-leukocyte protease SKALP, retain the proliferation potential of keratinocytes, to protect cells and soothe the skin.

[0034] A method for preparing a plant anti-allergic, antipruritic and analgesic composition comprises the following steps: weighing raw materials of corresponding weight percentage, dissolving them in the remaining amount of water, and fully mixing them to obtain the composition.

[0035] The invention discloses an application of a plant anti-allergic, antipruritic and analgesic composition, wherein the prepared composition is applied to the preparation of an external skin care preparation.

[0036] The external preparation is a facial cream, lotion, toner, facial cleanser, spray or essence.

[0037] The beneficial effects of the present invention are:

[0038] The present application provides a plant anti-allergic, antipruritic and analgesic composition, which is composed of gentiana cyanus extract, kava root extract, opuntia spinulosa leaf extract and Centella asiatica extract. The composition achieves anti-inflammatory, anti-allergic, antipruritic and analgesic effects through multi-pathway simultaneous action (inhibiting NO production, inhibiting histamine pathways, inhibiting TRPV1 ion channels). The composition can be applied to various aqueous and cream-based topical preparations. DETAILED DESCRIPTION

[0039] In order to facilitate the understanding of those skilled in the art, the present invention is further described below in conjunction with embodiments, and the contents mentioned in the implementation modes are not intended to limit the present invention.

[0040] In the following examples and comparative groups, the raw materials involved are all commercially available:

[0041] Among them, the blue gentian extract is made from selected wild blue gentian flowers from Tibet;

[0042] Kava Root Extract is made from kava roots grown in the South Pacific Islands;

[0043] Opuntia cactus leaf extract is a selected Mexican edible cactus;

[0044] Centella asiatica extract is made from wild Centella asiatica leaves grown in the highlands of Madagascar;

[0045] Example 1

[0046] A plant anti-allergic, antipruritic and analgesic composition, comprising the following raw materials by weight percentage:

[0047] Gentiana caerulea extract: 0.5%

[0048] Kava root extract: 1%

[0049] Opuntia cactus leaf extract: 0.5%

[0050] Centella asiatica extract: 1%

[0051] The balance is water;

[0052] Wherein, the content of gentiopicroside in the gentiana cyanus extract is controlled at 10%-15%, preferably 12%; the content of kavalactone in the kava root extract is controlled at 3%-10%, preferably 8%;

[0053] The content of flavonoids in the Opuntia thorni leaf extract is controlled at 0.05%-0.2%, and the content of alkaloids is controlled at 0.05%-0.15%, preferably the content of flavonoids is 0.15%, and the content of alkaloids is controlled at 0.12%;

[0054] The sum of the contents of hydroxymadecassoside and asiaticaside in the Centella asiatica extract is ≥75%.

[0055] Prepare the raw materials of the above composition in corresponding weight percentage, dissolve them in the remaining water, and mix them thoroughly to obtain the composition.

[0056] Example 2

[0057] A plant anti-allergic, antipruritic and analgesic composition, comprising the following raw materials by weight percentage:

[0058] Gentiana caerulea extract: 5%

[0059] Kava root extract: 10%

[0060] Opuntia cactus leaf extract: 5%

[0061] Centella asiatica extract: 10%

[0062] The balance is water;

[0063] Wherein, the content of gentiopicroside in the gentiana cyanus extract can be controlled at 10%-15%; the content of kavalactone in the kava root extract can be controlled at 3%-10%;

[0064] The content of flavonoids in the Opuntia thornii leaf extract can be controlled at 0.05%-0.2%, and the content of alkaloids can be controlled at 0.05%-0.15%;

[0065] The sum of the content of madecassoside and asiaticoside in the Centella asiatica extract is greater than 70%;

[0066] Prepare the raw materials of the above composition in corresponding weight percentage, dissolve them in the remaining water, and mix them thoroughly to obtain the composition.

[0067] Example 3

[0068] A plant anti-allergic, antipruritic and analgesic composition, comprising the following raw materials by weight percentage:

[0069] Gentiana caerulea extract: 0.15%

[0070] Kava root extract: 3%

[0071] Opuntia cactus leaf extract: 0.15%

[0072] Centella asiatica extract: 3%

[0073] The balance is water.

[0074] Wherein, the content of gentiopicroside in the gentiana cyanus extract can be controlled at 10%-15%; the content of kavalactone in the kava root extract can be controlled at 3%-10%;

[0075] The content of flavonoids in the Opuntia thornii leaf extract can be controlled at 0.05%-0.2%, and the content of alkaloids can be controlled at 0.05%-0.15%;

[0076] The sum of the content of madecassoside and asiaticoside in the Centella asiatica extract is greater than 70%;

[0077] Prepare the raw materials of the above composition in corresponding weight percentage, dissolve them in the remaining water, and mix them thoroughly to obtain the composition.

[0078] Example 4

[0079] A plant anti-allergic, antipruritic and analgesic composition, comprising the following raw materials by weight percentage:

[0080] Gentiana caerulea extract: 4%

[0081] Kava root extract: 8%

[0082] Opuntia cactus leaf extract: 4%

[0083] Centella asiatica extract: 8%

[0084] The balance is water.

[0085] Wherein, the content of gentiopicroside in the gentiana cyanus extract can be controlled at 10%-15%; the content of kavalactone in the kava root extract can be controlled at 3%-10%;

[0086] The content of flavonoids in the Opuntia thornii leaf extract can be controlled at 0.05%-0.2%, and the content of alkaloids can be controlled at 0.05%-0.15%;

[0087] The sum of the content of madecassoside and asiaticoside in the Centella asiatica extract is greater than 70%;

[0088] Prepare the raw materials of the above composition in corresponding weight percentage, dissolve them in the remaining water, and mix them thoroughly to obtain the composition.

[0089] Example 5

[0090] A plant anti-allergic, antipruritic and analgesic composition, comprising the following raw materials by weight percentage:

[0091] Gentiana caerulea extract: 3%

[0092] Kava root extract: 6%

[0093] Opuntia cactus leaf extract: 2%

[0094] Centella asiatica extract: 5%

[0095] The balance is water.

[0096] Wherein, the content of gentiopicroside in the gentiana cyanus extract can be controlled at 10%-15%; the content of kavalactone in the kava root extract can be controlled at 3%-10%;

[0097] The content of flavonoids in the Opuntia thornii leaf extract can be controlled at 0.05%-0.2%, and the content of alkaloids can be controlled at 0.05%-0.15%;

[0098] The sum of the content of madecassoside and asiaticoside in the Centella asiatica extract is greater than 70%;

[0099] Prepare the raw materials of the above composition in corresponding weight percentage, dissolve them in the remaining water, and mix them thoroughly to obtain the composition.

[0100] Example 6

[0101] A plant anti-allergic, antipruritic and analgesic composition, comprising the following raw materials by weight percentage:

[0102] Glycerin: 5%

[0103] Sodium polyacrylate: 0.15%

[0104] Gentiana caerulea extract: 0.5%

[0105] Kava root extract: 1%

[0106] Opuntia cactus leaf extract: 0.5%

[0107] Centella asiatica extract: 1%

[0108] Pentylene glycol: 2%

[0109] Deionized water: 89.85%.

[0110] Wherein, the content of gentiopicroside in the gentiana cyanus extract can be controlled at 10%-15%; the content of kavalactone in the kava root extract can be controlled at 3%-10%;

[0111] The content of flavonoids in the Opuntia thornii leaf extract can be controlled at 0.05%-0.2%, and the content of alkaloids can be controlled at 0.05%-0.15%;

[0112] The sum of the content of madecassoside and asiaticoside in the Centella asiatica extract is greater than 70%;

[0113] Prepare the raw materials of the above composition in corresponding weight percentage, dissolve them in the remaining water, and mix them thoroughly to obtain the composition.

[0114] Example 7

[0115] A plant anti-allergic, antipruritic and analgesic composition, comprising the following raw materials by weight percentage:

[0116] Glycerin: 5%

[0117] Sodium polyacrylate: 0.15%

[0118] Gentiana caerulea extract: 5%

[0119] Kava root extract: 10%

[0120] Opuntia cactus leaf extract: 5%

[0121] Centella asiatica extract: 10%

[0122] Pentylene glycol: 2%

[0123] Deionized water: 62.85%.

[0124] Wherein, the content of gentiopicroside in the gentiana cyanus extract can be controlled at 10%-15%; the content of kavalactone in the kava root extract can be controlled at 3%-10%;

[0125] The content of flavonoids in the Opuntia thornii leaf extract can be controlled at 0.05%-0.2%, and the content of alkaloids can be controlled at 0.05%-0.15%;

[0126] The sum of madecassoside and asiatica glycoside in the Centella asiatica extract is greater than 70%. Prepare raw materials of corresponding weight percentage of the above composition, dissolve them in the remaining amount of water, and fully mix them to obtain the composition.

[0127] In addition, the raw materials were prepared according to the corresponding weight percentages of the negative control group, comparison group 1, comparison group 2, comparison group 3, comparison group 4, Example 6, and Example 7 in the following Table 1 to study the anti-inflammatory effect, anti-allergic effect, antipruritic effect, and analgesic effect of the composition.

[0128] Table 1

[0129]

[0130] The preparation method of the composition corresponding to Table 1 is: add water into a reaction kettle, add sodium polyacrylate, and stir to disperse evenly; add the remaining raw materials into the reaction kettle in sequence and stir evenly.

[0131] 1. Anti-inflammatory, anti-allergic, antipruritic and analgesic effects tests

[0132] 1. Anti-inflammatory effect: NO inhibition test

[0133] Principle: When immune cells are stimulated by inflammatory mediators, a large amount of inducible nitric oxide synthase (INOS) is generated, producing NO for immune response. Therefore, inhibiting NO production is a direct indicator of the anti-inflammatory activity of the composition.

[0134] Test method: RAW264.7 cells were inoculated into 96-well plates, induced with 1 μg / ml LPS, and the test compound (final concentration 50 μg / ml and 500 μg / ml) was added for treatment, and negative control and positive control (50 μmL-NMMA inhibitor) were set. After overnight cell culture, the culture medium was taken to detect NO generation, and the absorbance was measured at 570 nm. MTS was added to the remaining culture medium for cell viability detection to exclude the toxic effects of the composition on the cells.

[0135] NO production inhibition rate (%) = (OD570nm of negative control group - OD570nm of test group) / OD570nm of negative control group;

[0136] Test results:

[0137]

[0138] The test data results show that the composition has a significant effect of inhibiting NO generation, and the effect is better than the control group with the same concentration. The change of the formula ratio also has a significant effect on the efficacy.

[0139] 2. Anti-allergic effect: histamine tolerance test

[0140] This test mainly involves applying histamine to the dorsum of the guinea pig's foot, with the concentration increasing cumulatively at one time. When the guinea pig has an itchy reaction, it licks the wound on the right foot. At this time, the cumulative amount of histamine given to each guinea pig is the amount of histamine that the guinea pig tolerates, and this is used as an indicator for T test statistical processing to evaluate the anti-allergic effect of the product.

[0141] Test method: Apply histamine on the dorsum of guinea pigs' feet

[0142] Test subjects: 10 guinea pigs per group, half male and half female, weighing 250-300g

[0143] Test results:

[0144]

[0145]

[0146] The test data showed that the composition significantly increased the histamine tolerance of guinea pigs, had significant anti-allergic effects, and was better than the control group with the same concentration, and was also better than the positive control group. The change in the proportion of the composition also had a significant effect on the efficacy.

[0147] 3. Anti-itching effect: scratching inhibition test

[0148] Test method: Tail vein injection of dextran

[0149] Test subjects: 10 guinea pigs per group, half male and half female, weighing 250-300g

[0150] Test results:

[0151]

[0152] The test data show that the composition has significant antipruritic effect, and the effect is better than the control group with the same concentration, and the effect is better than the positive control group. The change of the formula ratio of the composition also has a significant effect on the efficacy.

[0153] 4. Analgesic effect:

[0154] Principle: Capsaicin can activate TRPV1 receptors in mice and induce peripheral pain and swelling. By injecting capsaicin into the soles of mice's feet, a chemical stimulation-induced pain model in mice is established, and then the analgesic effect of the composition is investigated.

[0155] Test method: 0.2 ml / day of drug was administered to the back of each group of mice for 7 consecutive days. One hour after the last administration, capsaicin (3.2ug20ul) was injected into the right foot. The number of times and duration of mice licking their right feet within 5 minutes were observed and recorded. The duration of licking the right foot was used as an indicator to analyze the significance of the differences among the groups and calculate the inhibition rate.

[0156] Test results:

[0157]

[0158] The test data results show that the combination has significant analgesic effect, and the effect is better than the control group with the same concentration. The change of the formula ratio also has a significant effect on the efficacy.

[0159] 2. Application test of the composition

[0160] 1. Prepared the following cream

[0161]

[0162]

[0163] The preparation process of the cream is as follows:

[0164] Add deionized water to reactor A, add glycerol while stirring and heating, raise the temperature to 65-70℃ and keep warm for 20 minutes;

[0165] Add GTCC, A165, 16 / 18 alcohol and squalane to reactor B in sequence, stir and heat to 65-70°C, then add EMT10 to reactor B and stir until evenly dispersed;

[0166] Start homogenization in reactor A, pump the raw materials in reactor B into reactor A, stir and homogenize under vacuum for 5-10 minutes until the state is uniform, and cool down;

[0167] After the temperature drops to 45°C, the corresponding composition and preservative are added to the reaction kettle A in sequence and stirred until they are evenly dissolved.

[0168] 2. Arm test

[0169] Test method: recruit 10 volunteers (5 males and 5 females, aged 25-35), apply histamine stimulant on the inside of the arm until itching, redness, swelling or pimples and papules appear, which usually take about 3-15 minutes, and then apply the products of test group 1, test group 2, and test group 3 to the affected area respectively, and record the time when itching, pain, redness and swelling disappear.

[0170]

[0171] Test results:

[0172] The test data show that the cream containing the composition has significant antipruritic, analgesic and detumescent effects, which are comparable to those of the positive control group. At the same time, the change in the composition formula ratio also has a significant effect on the efficacy.

[0173] 3. Trial test

[0174] Test method: recruit 6 volunteers with problematic skin (sensitive skin, dermatitis, eczema), apply 3 samples of the test group to the affected area every morning and evening for 7 consecutive days, observe and record the skin's performance and state changes, and evaluate the skin change indicators on a 5-point scale.

[0175] Test Scoring Itching pain Redness dry Chipping Overall skin condition Before use 4.8 4 4.8 4.7 3.9 1.2 After 1 day of use 1.2 0.8 3.9 3.4 2.6 2.3 After 7 days of use 0.5 0.3 1.9 2.2 1.8 4.2

[0176] Test results:

[0177] From the evaluation results, it can be seen that the composition cream can quickly relieve itching and analgesia, and it also has a certain effect on redness and dryness of the skin, and the overall condition of the skin is significantly improved.

[0178] The above embodiments are preferred implementation schemes of the present invention. In addition, the present invention may also be implemented in other ways. Any obvious replacement without departing from the concept of the present invention is within the protection scope of the present invention.

Claims

1. A plant anti-allergic, antipruritic and analgesic composition, characterized in that: In terms of weight percentage, the following raw materials are included: Blue Gentiana Extract: 0.5%-5% Kava root extract: 1%-10% Opuntia cactus leaf extract: 0.5%-5% Centella asiatica extract: 1%-10% The balance is water; The content of gentiopicroside in the gentiana cyanus extract is controlled at 10%-15%; the content of kavalactone in the kava root extract is controlled at 3%-10%; The content of flavonoids in the Opuntia thorni leaf extract is controlled at 0.05%-0.2%, and the content of alkaloids is controlled at 0.05%-0.15%; The sum of the contents of madecassoside and asiatica glycoside in the Centella asiatica extract is greater than 70%.

2. A plant anti-allergic, antipruritic and analgesic composition according to claim 1, characterized in that: The plant anti-allergic, antipruritic and analgesic composition comprises the following raw materials by weight percentage: Blue Gentiana Extract: 0.5%-4% Kava root extract: 3%-8% Opuntia cactus leaf extract: 0.5%-4% Centella asiatica extract: 3%-8% The balance is water.

3. A plant anti-allergic, antipruritic and analgesic composition according to claim 1 or 2, characterized in that: The plant anti-allergic, antipruritic and analgesic composition comprises the following raw materials by weight percentage: Gentiana caerulea extract: 3% Kava root extract: 6% Opuntia cactus leaf extract: 2% Centella asiatica extract: 5% The balance is water.

4. A method for preparing a plant anti-allergic, antipruritic and analgesic composition, characterized in that: The method comprises the following steps: weighing the raw materials of the composition according to any one of claims 1 to 3 in corresponding weight percentage, dissolving them in the remaining amount of water, and fully mixing them to obtain the composition.

5. Application of a plant anti-allergic, antipruritic and analgesic composition, characterized in that: The composition according to any one of claims 1 to 3 or the composition prepared according to claim 4 is applied to prepare an external skin care preparation.

6. The use of a plant anti-allergic, antipruritic and analgesic composition according to claim 5, characterized in that: The external skin care preparation is a face cream, lotion, toner, cleanser, spray or essence.

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