CN115400081A - O/W emulsion spray for anti-inflammation and detumescence - Google Patents
O/W emulsion spray for anti-inflammation and detumescence Download PDFInfo
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- CN115400081A CN115400081A CN202210937341.6A CN202210937341A CN115400081A CN 115400081 A CN115400081 A CN 115400081A CN 202210937341 A CN202210937341 A CN 202210937341A CN 115400081 A CN115400081 A CN 115400081A
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- polysaccharide
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- oil
- essential oil
- anthocyanin
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Classifications
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- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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Abstract
The invention provides an O/W emulsion spray for resisting inflammation and diminishing swelling. Consists of an aqueous phase carrying polysaccharide components of fungal and plant origin and an oil phase carrying anthocyanins and plant essential oils. The aqueous phase carrying the fungal and plant-derived polysaccharide component consists of the fungal and plant-derived polysaccharide component, polylysine, poloxamer and water; the oil phase carrying the anthocyanin and the plant essential oil is formed by dissolving the anthocyanin and the plant essential oil in mineral oil. According to the invention, the fungi and polysaccharide components derived from plants, plant essential oil and anthocyanin are encapsulated in the same delivery system and applied to the spray for treating local inflammation and swelling, so that the stability of various different soluble components is ensured, and the multi-component synergistic treatment effect is exerted, and the requirements of safety, effectiveness, convenience and economy of clinical treatment are met.
Description
Technical Field
The invention relates to an anti-inflammatory and detumescent preparation, in particular to an O/W type emulsion spray for anti-inflammatory and detumescent.
Background
Local swelling due to inflammation is a common symptom, and is usually seen in limbs such as legs, arms, feet and hands, and sometimes also in the back, neck or shoulders. Local inflammation and swelling can not only cause pain, but also cause local skin itching and redness, even skin rash and other phenomena, and seriously affect the life quality of patients.
Although effective against local inflammatory swelling, chemical analgesic and anti-inflammatory drugs, the side effects are large. Compared with chemical synthetic drugs, the polysaccharide component of fungus and plant sources has better therapeutic action on local inflammation and swelling, has the advantages of high biological activity, mild action, small irritation and the like, and is particularly suitable for long-term application (Liu Xiaoying, ma Shijing, han Ping and the like; research on inhibition of tyrosinase activity and anti-inflammatory effect of pachyman with different molecular weights [ J ]. Chinese edible fungus, 2021,40 (9): 47-53; han Lina, fan Yanli, tian Jianwen; medlar polysaccharide anti-inflammatory action and mechanism progress [ J ]. Modern 2018,38 (4): 342-345; fan Xinhui, prunaceae, yang Yidan, and the like; preliminary research on structure and activity of anti-inflammatory component in astragalus polysaccharide [ J ]. Shanxi science university report, 2021,52 (1346): 1356). However, the polysaccharide components of fungal and plant origin have a high molecular weight and poor permeability and therefore have a slow onset of action. In addition, the aqueous solution of the polysaccharide components of fungal and plant origin is susceptible to degradation and deterioration by environmental influences, and is volatile in water after topical application, and thus cannot be directly applied to the treatment of local inflammation and swelling. Although the traditional polysaccharide oral preparation of fungal and plant sources is convenient to apply, the traditional polysaccharide oral preparation cannot effectively reach local inflammation and swelling parts, so that the traditional polysaccharide oral preparation cannot play a medicinal role.
The plant essential oil and anthocyanin have certain treatment effect on local inflammation and swelling, but the plant essential oil is too strong in irritation and volatile and cannot be directly coated on local inflammation and swelling parts for application. Anthocyanins are easily oxidized, have poor stability and are difficult to exert long-acting effects. Therefore, if fungus and plant-derived polysaccharide components, plant essential oil and anthocyanidin can be used in combination, the synergistic therapeutic effect of the three components on local inflammation and swelling can be exerted. However, the polysaccharide components of fungal and plant origin, plant essential oils and anthocyanins have significant differences in solubility, and direct mixing can cause aggregation of the three components and loss of activity.
Through search, no report that polysaccharide components, plant essential oils and anthocyanins of fungal and plant sources are encapsulated in the same delivery system together for treating local inflammation and swelling is seen at present, so that the synergistic treatment effect of the polysaccharide components, the plant essential oils and the anthocyanins of fungal and plant sources on the local inflammation and swelling cannot be exerted in the prior art.
Disclosure of Invention
In order to overcome the limiting bottleneck of the current treatment technology of local inflammation and swelling and overcome the defects of the prior art (namely, the technology that polysaccharide components from fungi and plants and plant essential oil and anthocyanin are jointly encapsulated in the same delivery system is lacked), the invention aims to provide the aerosol for applying the polysaccharide components from fungi and plants, the plant essential oil and the anthocyanin to the local inflammation and swelling treatment by jointly encapsulating the polysaccharide components from fungi and plants, the plant essential oil and the anthocyanin in the same delivery system, so that the stability of various different soluble components is ensured, the multi-component synergistic treatment effect is exerted, and the requirements of safety, effectiveness, convenience and economy of clinical treatment are met.
The inventor finds that the plant essential oil and the anthocyanin have good repairing effect on local inflammation and swollen tissues, but the plant essential oil is volatile, the anthocyanin is poor in stability, and the plant essential oil and the anthocyanin cannot play a long-acting role. Polysaccharide fractions of fungal and plant origin have a long lasting therapeutic effect on local inflammation and swelling, but a slow onset of action. If the fungi, the polysaccharide component from the plant source, the plant essential oil and the anthocyanin can be jointly applied, the stability of each component is ensured, the advantages of multiple components are exerted, the synergistic treatment effect is formed, and the effective treatment of local inflammation and swelling can be realized.
The inventor provides an O/W type emulsion for resisting inflammation and reducing swelling through a large amount of experimental researches.
The emulsion provided by the invention consists of an aqueous phase carrying polysaccharide components of fungal and plant origin and an oil phase carrying anthocyanins and plant essential oils.
The water phase carrying the polysaccharide components of fungal and plant origin consists of polysaccharide components of fungal and plant origin, polylysine, poloxamer and water,
wherein the polysaccharide component of fungal and plant origin: polylysine: the weight ratio of the poloxamer is 1:1-8, and the water is 4-8 times of the total weight of the polysaccharide component, the polylysine and the poloxamer which are derived from fungi and plants.
The oil phase carrying the anthocyanin and the plant essential oil is formed by dissolving the anthocyanin and the plant essential oil in a mass ratio of 1-5:1 in mineral oil with the mass of 4-6 times;
the mass ratio of the water phase carrying fungi and plant-derived polysaccharide components and the oil phase carrying anthocyanin and plant essential oil in the emulsion is 1-3:1;
the above polysaccharide components of fungal and plant origin include: one or more of Auricularia polysaccharide, tremella polysaccharide, ganoderma polysaccharide, lentinan, pachyman, astragalus polysaccharide, and Lycium Bararum polysaccharide.
The plant essential oil comprises: one or more of tea tree essential oil, vanilla essential oil, clove essential oil, lavender essential oil and rose essential oil.
The mineral oil comprises one or more of liquid paraffin 400, liquid paraffin 600 and silicone oil.
Preferably, the above mentioned polysaccharide components of fungal and plant origin: polylysine: the weight ratio of the poloxamer is 1:3-5.
Preferably, the oil phase carrying the anthocyanin and the plant essential oil is formed by dissolving the anthocyanin and the plant essential oil in 5 times of mineral oil by mass ratio of 3:1.
Preferably, the ratio of the mass of the aqueous phase carrying the polysaccharide components of fungal and plant origin and the oil phase carrying the anthocyanins and plant essential oils in the above emulsion is 2:1.
The O/W type emulsion for resisting inflammation and diminishing swelling is prepared by the following steps:
a) Dispersing polylysine and poloxamer in water, slowly dissolving, adding polysaccharide components derived from fungi and plants, and mixing to form water phase carrying polysaccharide components derived from fungi and plants;
b) Heating mineral oil to 50-60 deg.C (55 deg.C), adding anthocyanidin and plant essential oil, dissolving and mixing to form oil phase carrying anthocyanidin and plant essential oil, adding water phase carrying fungi and plant polysaccharide prepared in step a) when the temperature is reduced to 35-45 deg.C, grinding and mixing to obtain O/W type emulsion.
In the above preparation method, the polysaccharide component of fungal and plant origin: polylysine: the weight ratio of the poloxamer is 1:1-8, preferably 1:3-5;
the mass of the water is 4 to 8 times, preferably 6 times of the total mass of the polysaccharide component, the polylysine and the poloxamer which are derived from fungi and plants;
the mass ratio of the anthocyanin to the plant essential oil is 1-5:1, preferably 3:1;
in the oil phase carrying the anthocyanin and the vegetable essential oil, the mass of the mineral oil is 4-6 times, preferably 5 times of the total mass of the anthocyanin and the vegetable essential oil;
the mass ratio of the water phase carrying the polysaccharide component of fungus and plant origin to the oil phase carrying the anthocyanin and plant essential oil is 1-3:1, preferably 2:1.
In the preparation method, the water phase in the step b) can be further added with: one or more of thickener, emulsifier, pH value buffer and antioxidant.
The application of the emulsion in the preparation of products for treating local inflammation and swelling also belongs to the protection scope of the invention.
The product can be skin care product and medicine.
The emulsion can be made into various dosage forms, such as spray.
The emulsion spray can be sprayed on local inflammation and swelling parts for treating local inflammation and swelling.
The O/W type emulsion spray for resisting inflammation and diminishing swelling has the following advantages: (1) the O/W type emulsion has high stability, the anthocyanin and the plant essential oil are dissolved in the mineral oil to form an inner phase (oil phase), the stability is high, and the polysaccharide components of fungus and plant sources are dissolved in the aqueous solution consisting of polylysine and poloxamer to be used as an outer phase, so that the stability is good; (2) the quick-acting and long-acting multi-component synergistic therapeutic effect is achieved on the premise of ensuring the stability of various components with different dissolvability; (3) the sterility of local inflammation and swelling parts is ensured, and meanwhile, nutrition is provided for treatment, and polylysine is a nutritional bacteriostatic agent and has double functions of nutrition and bacteriostasis; (4) the O/W emulsion spray is easy to spray local inflammation and swelling parts, and has good coverage and high permeability; (5) the storage, the transportation and the use are convenient, fast and safe.
Detailed Description
Hereinafter, specific embodiments of the present invention will be described in detail. It should be noted that technical features or combinations of technical features described in the following embodiments should not be considered as being isolated, and they may be combined with each other to achieve better technical effects.
Example 1 preparation of O/W emulsion spray for anti-inflammatory and detumescence
The sprays of the experimental group were prepared according to the design of table 1, specifically comprising the following steps:
a: dispersing polylysine and poloxamer in distilled water of 15 deg.C, slowly dissolving, adding fungi and plant-derived polysaccharide components, and mixing to form water phase carrying fungi and plant-derived polysaccharide components;
b: and (b) adding the anthocyanin and the plant essential oil into 55 ℃ grease with the mass of 5 times, dissolving and uniformly mixing to form an oil phase carrying the anthocyanin and the plant essential oil, adding the water phase carrying the eumycete and the plant-derived polysaccharide prepared in the step a when the temperature is reduced to 40 ℃, grinding and uniformly mixing to prepare the spray.
Referring to the design and preparation method of the experimental group, a control group formulation was prepared according to table 1. The experimental groups are configured according to the components and the proportion within the protection range of the specification, and the control groups are the deletion of a certain component or the mass percentage of the component beyond the protection range of the specification.
TABLE 1 design of experimental and control groups
Note: v: the item is in accordance with the parameter setting corresponding to the header; /: this item is not present; * : the component or parameter is changed; a: vanilla essential oil; b: clove essential oil; c: lavender essential oil; d: tea tree essential oil; the liquid paraffin 400, the liquid paraffin 600 and the silicone oil belong to mineral oil; the flax oil belongs to vegetable oil; shark liver oil belongs to animal oil; trehalose belongs to the disaccharide; chitosan is a polysaccharide derived from animal crustaceans. The water in the water phase has a mass 6 times of the total mass of the polysaccharide component, polylysine and poloxamer of fungal and plant origin.
Example 2 Effect of the application of the respective formulations
(1) Mouse auricle swelling model
Preparing a mouse auricle swelling model by adopting a phorbol ester (TPA) induction method: taking Kunming mouse, male, weighing 18-22 g, smearing acetone solution of TPA on the inner and outer sides of ear, the dose of TPA per ear is 2.5 μ g, and making into mouse auricle swelling model after 6 hr.
(2) Evaluation of therapeutic Effect of Each group of formulations on model animals
Each experiment was conducted according to the design of Table 1,5 animals per group, and the preparation was applied to the swelling area of auricle of model animal at 80mg/cm 2 The dose is sprayed, the same professional doctor is asked to evaluate the fading condition of auricle swelling, the skin color recovery degree and the rat state in percentage by adopting a double-blind method after administration, a comprehensive treatment effect score is given by combining the whole recovery condition of the rat, and the higher the score is, the better the treatment effect is.
The experimental results are as follows: the therapeutic effect of the above groups of formulations on local inflammation and swelling is shown in table 2.
TABLE 2 evaluation of the efficacy of the various groups of formulations for the treatment of local inflammation and swelling
As can be seen from the experimental results in Table 2, the spray of the experimental group has good treatment effect on local inflammation and swelling, particularly the spray of the experimental groups 4 and 5 has the advantages of fast fading of inflammation and swelling, normal skin color recovery, good rat state and no agitation. Compared with the experimental group, the control group has obviously poor treatment effect on local inflammation and swelling, particularly the control groups 1, 11 and 12, the fading of inflammation and swelling is slow, the skin color can not be recovered to be normal, and rats are agitated and have poor states.
The experimental results in table 2 prove that any component and condition in the technical protection scheme of the invention are synergistic and indispensable, and that the lack of any component and condition in the technical protection scheme of the invention can obviously affect the treatment effect on local inflammation and swelling. The spray of the invention can resist inflammation and reduce swelling, and has good application prospect.
Example 3 quality evaluation of the respective preparations
The quality of the formulations of each group in example 1 was evaluated from the aspects of uniformity, coating ductility, centrifugal stability, cold resistance stability and heat resistance, respectively, for the formulations of each experimental group and control group, and the evaluation index and score criteria are shown in table 3.
TABLE 3 evaluation index and score criterion
The evaluation method of each index comprises the following steps: 1) Uniformity. Taking a proper amount of preparation samples of each group, observing whether the color and luster of the preparation are uniform and the texture is smooth, and standing for 1h to judge whether the preparation is naturally layered; 2) Coating ductility. Taking a proper amount of samples, coating the samples on a glass slide, and observing whether agglomeration exists or not and whether particles are generated or not in the coating process; 3) And (4) centrifugal stability. Respectively putting each group of the same amount of preparation into 2mL centrifuge tubes, 4000r.min -1 Centrifuging for 15min (the centrifugal radius is 5 cm), and separating oil from water without bubbles, layering, discoloration and the like; 4) And (5) cold resistance stability. Respectively placing each group of the preparation in 2mL centrifuge tubes, sealing, storing at-20 deg.C for 24 hr, taking out, standing to room temperature, observing whether there is bubble, and whether layering and discoloration occurOil-water separation phenomenon; 5) And (3) respectively taking each group of equivalent preparations into 3 centrifugal tubes of 2mL, sealing, placing in a 50-degree incubator, keeping the constant temperature for 6h, and observing whether the phenomena of oil-water separation such as layering, color change and the like occur or not.
Finally, comprehensive scores are given through various evaluation scores, and the quality evaluation results of various groups of preparations are shown in table 4.
Table 4 quality evaluation results of each group of preparations
As can be seen from the data results of table 4, the formulation combination score was the highest in the experimental group 4, the formulation combination score was the lowest in the control group 9, and the O/W emulsion spray was not formed in the control groups 11 and 12.
It will be apparent to those skilled in the art that various changes and modifications may be made in the present invention without departing from the spirit and scope of the invention. Thus, if such modifications and variations of the present invention fall within the scope of the claims of the present invention and their equivalents, the present invention is intended to include such modifications and variations.
Claims (10)
1. An anti-inflammatory and repercussive O/W emulsion, which comprises an aqueous phase carrying a polysaccharide fraction of fungal and plant origin and an oil phase carrying anthocyanins and plant essential oils; the aqueous phase carrying the fungal and plant-derived polysaccharide component consists of the fungal and plant-derived polysaccharide component, polylysine, poloxamer and water; the oil phase carrying the anthocyanin and the plant essential oil is formed by dissolving the anthocyanin and the plant essential oil in mineral oil.
2. An emulsion according to claim 1, characterized in that: polysaccharide fractions of fungal and plant origin: polylysine: the weight ratio of the poloxamer is 1:1-8, and the water is 4-8 times of the total weight of the polysaccharide component, the polylysine and the poloxamer which are derived from fungi and plants.
3. An emulsion according to claim 1 or 2, characterized in that: the oil phase carrying the anthocyanin and the plant essential oil is formed by dissolving the anthocyanin and the plant essential oil in mineral oil with the mass ratio of 1-5:1 in 4-6 times of the mass.
4. An emulsion according to any of claims 1-3, characterized in that: the mass ratio of the water phase carrying the polysaccharide components of fungi and plants to the oil phase carrying the anthocyanin and the plant essential oil in the emulsion is 1-3:1.
5. An emulsion according to any of claims 1-4, characterized in that: the polysaccharide component of fungal and plant origin comprises: one or more of Auricularia polysaccharide, tremella polysaccharide, ganoderma polysaccharide, lentinan, pachyman, radix astragali polysaccharide, and fructus Lycii polysaccharide;
the plant essential oil comprises: one or more of tea tree essential oil, vanilla essential oil, clove essential oil, lavender essential oil and rose essential oil;
the mineral oil comprises one or more of liquid paraffin 400, liquid paraffin 600 and silicone oil.
6. A process for preparing an emulsion according to any one of claims 1 to 5, comprising the steps of:
a) Dispersing polylysine and poloxamer in water, slowly dissolving, adding polysaccharide components derived from fungi and plants, and mixing to form water phase carrying polysaccharide components derived from fungi and plants;
b) Heating mineral oil to 50-60 ℃, adding anthocyanin and plant essential oil, dissolving and uniformly mixing to form an oil phase carrying anthocyanin and plant essential oil, adding the water phase carrying fungi and plant-derived polysaccharide components prepared in the step a) when the temperature is reduced to 35-45 ℃, grinding and uniformly mixing to prepare the O/W type emulsion.
7. The method of claim 6, wherein: the water phase in the step b) can be further added with: one or more of thickener, emulsifier, pH value buffer and antioxidant.
8. Use of an emulsion according to any one of claims 1-5 in the manufacture of a product for the treatment of local inflammation and swelling.
9. Use according to claim 8, characterized in that: the product is skin care product and medicine.
10. Use according to claim 8 or 9, characterized in that: the emulsion can be made into various dosage forms, such as spray.
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