CN115400081B - O/W type emulsion spray for resisting inflammation and detumescence - Google Patents
O/W type emulsion spray for resisting inflammation and detumescence Download PDFInfo
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- CN115400081B CN115400081B CN202210937341.6A CN202210937341A CN115400081B CN 115400081 B CN115400081 B CN 115400081B CN 202210937341 A CN202210937341 A CN 202210937341A CN 115400081 B CN115400081 B CN 115400081B
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- 230000004054 inflammatory process Effects 0.000 title claims abstract description 36
- 239000000839 emulsion Substances 0.000 title claims abstract description 26
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- 229920001282 polysaccharide Polymers 0.000 claims abstract description 56
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- PHEDXBVPIONUQT-RGYGYFBISA-N phorbol 13-acetate 12-myristate Chemical compound C([C@]1(O)C(=O)C(C)=C[C@H]1[C@@]1(O)[C@H](C)[C@H]2OC(=O)CCCCCCCCCCCCC)C(CO)=C[C@H]1[C@H]1[C@]2(OC(C)=O)C1(C)C PHEDXBVPIONUQT-RGYGYFBISA-N 0.000 description 1
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- 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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Abstract
The invention provides an O/W emulsion spray for resisting inflammation and relieving swelling. Consists of an aqueous phase carrying polysaccharide components of fungal and plant origin and an oily phase carrying anthocyanidin and plant essential oils. The aqueous phase carrying the polysaccharide component of fungal and plant origin consists of the polysaccharide component of fungal and plant origin, 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. The invention loads the polysaccharide components, the plant essential oil and the anthocyanin which are derived from fungi and plants together in the same delivery system to be applied to the spray for treating local inflammation and swelling, ensures the stability of various different soluble components, simultaneously plays the multicomponent synergistic treatment effect, and simultaneously meets the requirements of safety, effectiveness, convenience and economy of clinical treatment.
Description
Technical Field
The invention relates to an anti-inflammatory detumescence preparation, in particular to an O/W emulsion spray for resisting inflammation and detumescence.
Background
Localized swelling due to inflammation is a common symptom commonly found in limbs such as legs, arms, feet and hands, and sometimes also in the back, neck or shoulders. The local inflammation and swelling not only can cause pain, but also can cause local skin itching and redness, even rash and the like, and seriously affect the life quality of patients.
Chemical analgesic and anti-inflammatory drugs, while effective against localized inflammatory swelling, have significant side effects. Compared with chemical synthetic drugs, the polysaccharide component of fungi and plant sources has better treatment effect on local inflammation and swelling, has the advantages of high biological activity, mild effect, small irritation and the like, and is particularly suitable for long-term application (Liu Xiaoying, ma Shijing, han Ping, and the like; research on the inhibition of tyrosinase activity and anti-inflammatory effect by pachyman with different molecular weights [ J ]. Chinese edible fungi, 2021,40 (9): 47-53; han Lina, fan Yanli, tian Jianwen. Anti-inflammatory effect of wolfberry polysaccharide and mechanism progress [ J ]. Modern immunology, 2018,38 (4): 342-345; fan Xinhui, plum, yang Yidan, and the like; preliminary research on the structure and activity of anti-inflammatory components in astragalus polysaccharide [ J ]. University of mountain and western medicine university, 2021,52 (10): 1346-1356). However, polysaccharide components of fungal and plant origin have a high molecular weight and poor permeability and thus act very slowly. In addition, aqueous solutions of polysaccharide components of fungal and plant origin are susceptible to degradation and deterioration by environmental influences, and aqueous solutions of polysaccharide components of fungal and plant origin are subject to evaporation of water after topical application, and thus cannot be directly used for the treatment of local inflammation and swelling. The traditional polysaccharide oral preparation of fungi and plant sources is convenient to apply, but can not effectively reach local inflammatory diseases and swelling parts, so that the traditional polysaccharide oral preparation can not play a role of medicine.
The plant essential oil and anthocyanin have a certain treatment effect on local inflammation and swelling, but the plant essential oil is too strong in irritation and easy to volatilize, and cannot be directly coated on local inflammation and swelling parts for application. The anthocyanin is easy to oxidize, has poor stability and is difficult to play a long-acting role. Therefore, if the fungus and plant-derived polysaccharide component, the plant essential oil and the anthocyanin can be combined, the synergistic treatment effect of the fungus, the plant essential oil and the anthocyanin on local inflammation and swelling can be exerted. However, the polysaccharide components of fungi and plant sources, plant essential oil and anthocyanin have obvious solubility difference, and the direct mixing can lead to aggregation and activity loss of the three components.
Through searching, no report of jointly encapsulating the polysaccharide components of fungi and plant sources, the plant essential oil and the anthocyanin on the same delivery system for treating local inflammation and swelling is currently seen, so that the prior art cannot exert the synergistic treatment effect of the polysaccharide components of fungi and plant sources, the plant essential oil and the anthocyanin on the local inflammation and swelling.
Disclosure of Invention
In order to overcome the limitation bottleneck of the existing treatment technology of local inflammation and swelling and overcome the defects of the prior art (namely, the technology of jointly encapsulating polysaccharide components of fungi and plant sources, plant essential oil and anthocyanin in the same delivery system), the invention aims to provide a spray for jointly encapsulating the polysaccharide components of fungi and plant sources, the plant essential oil and the anthocyanin in the same delivery system to be applied to the treatment of local inflammation and swelling, so that the stability of various different soluble components is ensured, the multicomponent synergistic treatment effect is exerted at the same time, and the requirements of safety, effectiveness, convenience and economy of clinical treatment are met.
The inventor experiments find that the plant essential oil and anthocyanin have better repairing effect on local inflammation and swelling tissues, but the plant essential oil is easy to volatilize, and the anthocyanin has poor stability, and neither can play a long-acting role. Polysaccharide components of fungal and plant origin have a durable therapeutic effect on local inflammation and swelling, but slow onset. If the fungus and plant-derived polysaccharide component, the plant essential oil and the anthocyanin can be combined for application, the stability of each component is ensured, the multicomponent advantage is exerted, the synergistic treatment effect is formed, and the effective treatment of local inflammation and swelling can be realized.
Through a great deal of experimental study, the inventor provides an O/W emulsion for resisting inflammation and relieving swelling.
The emulsion provided by the invention consists of an aqueous phase carrying polysaccharide components of fungi and plant sources and an oil phase carrying anthocyanin and plant essential oil.
The above aqueous phase carrying the polysaccharide component of fungal and plant origin consists of the polysaccharide component of fungal and plant origin, polylysine, poloxamer and water,
wherein, polysaccharide components of fungal and plant origin: polylysine: the mass ratio of poloxamer is 1:1-8:100, and the mass of water is 4-8 times of the mass of polysaccharide components of fungi and plant sources, polylysine and poloxamer Sha Mzong.
The oil phase carrying the anthocyanin and the plant essential oil is formed by dissolving the anthocyanin and the plant essential oil in the mass ratio of 1-5:1 in mineral oil with the mass ratio of 4-6 times;
the mass ratio of the water phase carrying the polysaccharide components of fungi and plant sources to the oil phase carrying anthocyanin and plant essential oil in the emulsion is 1-3:1;
the polysaccharide components of fungal and plant origin described above include: one or more of Auricularia polysaccharide, tremella polysaccharide, ganoderma polysaccharide, lentinan, pachyman, astragalus polysaccharides and Lycium barbarum polysaccharide.
The plant essential oil comprises: tea tree essential oil, vanilla essential oil, flos Caryophylli essential oil, lavender essential oil, or rose essential oil.
The mineral oil mentioned above includes one or a combination of several of liquid paraffin 400, liquid paraffin 600 and silicone oil.
Preferably, the polysaccharide component of fungal and plant origin described above: polylysine: the mass ratio of the poloxamer is 1:3-5:100.
Preferably, 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 3:1 in mineral oil of 5 times.
Preferably, the mass ratio of the aqueous phase carrying the polysaccharide component of fungal and plant origin to the oily phase carrying the anthocyanin and plant essential oil in the emulsion is 2:1.
The O/W emulsion for resisting inflammation and relieving swelling is prepared by a method comprising the following steps:
a) Dispersing polylysine and poloxamer in water, slowly dissolving, adding polysaccharide components of fungi and plant sources, and mixing to form water phase carrying polysaccharide components of fungi and plant sources;
b) Heating mineral oil to 50-60 ℃ (specifically 55 ℃), adding anthocyanin and plant essential oil, dissolving and mixing uniformly to form an oil phase carrying anthocyanin and plant essential oil, adding the water phase carrying fungus and plant-derived polysaccharide components prepared in step a) when the temperature is reduced to 35-45 ℃, and grinding and mixing uniformly to prepare the O/W emulsion.
In the above preparation method, polysaccharide components of fungal and plant origin: polylysine: the mass ratio of poloxamer is 1:1-8:100, preferably 1:3-5:100;
the mass of water is 4-8 times, preferably 6 times, the total mass of polysaccharide components of fungi and plant sources, polylysine and poloxamer;
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 plant essential oil, the mass of the mineral oil is 4-6 times, preferably 5 times, of the total mass of the anthocyanin and the plant essential oil;
the mass ratio of the aqueous phase carrying the polysaccharide component of fungal and plant origin to the oil phase carrying the anthocyanin and the plant essential oil is 1-3:1, preferably 2:1.
In the above preparation method, the aqueous phase of step b) may further be added: one or more of thickener, emulsifier, pH buffer and antioxidant.
The use of the emulsion described above for the preparation of a product for the treatment of local inflammation and swelling is also within the scope of the present invention.
The product can be skin care product or medicine.
The emulsion can be made into various dosage forms, such as spray.
The emulsion spray is sprayed on local inflammation and swelling parts, and is used for treating local inflammation and swelling.
The O/W emulsion spray for resisting inflammation and relieving swelling has the following advantages: (1) the O/W emulsion has high stability, anthocyanin and plant essential oil are dissolved in mineral oil to form an internal phase (oil phase), and polysaccharide components of fungi and plant sources are dissolved in aqueous solution composed of polylysine and poloxamer to be used as an external phase, so that the emulsion has good stability; (2) the effect is quick, the acting time is long, and the multi-component synergistic treatment effect of quick acting and long acting is exerted on the premise of ensuring the stability of various different soluble components; (3) the sterilization of local inflammation and swelling parts is ensured, nutrition is provided for treatment, and polylysine is a nutritional bacteriostat, and has the dual 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) convenient and quick storage, transportation and use and safety.
Detailed Description
Hereinafter, specific embodiments of the present invention will be described in detail. It should be noted that the technical features or combinations of technical features described in the following embodiments should not be regarded as being isolated, and they may be combined with each other to achieve a better technical effect.
Example 1 preparation of an O/W emulsion spray with anti-inflammatory and repercussive effects
According to the design of table 1, a spray of the experimental group was prepared, comprising the following steps:
a: dispersing polylysine and poloxamer in 15 deg.C distilled water, slowly dissolving, adding polysaccharide components of fungi and plant sources, mixing well to form water phase carrying polysaccharide components of fungi and plant sources;
b: adding anthocyanin and plant essential oil into 55deg.C oil of 5 times mass, dissolving and mixing to form oil phase carrying anthocyanin and plant essential oil, adding water phase carrying polysaccharide component of fungus and plant source prepared in step a when temperature is reduced to 40deg.C, grinding and mixing to obtain spray.
Referring to the design and preparation method of the experimental group, a control formulation was prepared according to table 1. Each experimental group is configured according to the components and the proportion within the protection scope of the application, and each control group is a component with a missing or component mass percent which is beyond the protection scope of the application.
Table 1 design of experimental and control groups
Note that: and (2) the following steps: the item accords with the parameter setting corresponding to the header; /: the item is absent; * : the item component or parameter is changed; a: vanilla essential oil; b: butyl essential oil; c: lavender essential oil; d: tea tree essential oil; liquid paraffin 400, liquid paraffin 600 and silicone oil all belong to mineral oil; flax oil belongs to vegetable oil; shark liver oil belongs to animal oil; trehalose is a disaccharide; chitosan is a polysaccharide of animal crusta origin. The mass of water in the aqueous phase is 6 times the total mass of polysaccharide components of fungal and vegetable origin, polylysine and poloxamer.
EXAMPLE 2 Effect of application of formulations of the groups
(1) Mouse auricle swelling model
The phorbol ester (TPA) induction method is adopted to prepare the auricle swelling model of the mice: the Kunming mice are taken, male and the weight is 18-22 g, the acetone solution of TPA is smeared on the inner side and the outer side of the ears, the dosage of TPA of each ear is 2.5 mug, and the model of auricle swelling of the mice is prepared after 6 hours.
(2) Evaluation of therapeutic Effect of each group of formulations on model animals
Each group of experiments was performed with 5 animals per group, each group of formulations at 80mg/cm at the auricle swelling site of model animals according to the design of Table 1 2 The dosage is sprayed, the same professional physician is asked to evaluate the resolution of auricle swelling, the skin color recovery degree and the rat state in percentage system by adopting a double-blind method after the administration, the comprehensive score of the treatment effect is given by combining the overall recovery condition of the rat, and the higher the score is, the better the treatment effect is.
Experimental results: the therapeutic effect of each of the above groups of formulations on local inflammation and swelling is shown in table 2.
Table 2 evaluation of therapeutic effect of each group of formulations for localized 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, especially the treatment effect of the experimental groups 4 and 5 on inflammation and swelling has the advantages of rapid fading, normal skin color recovery, good rat state and no agitation. Compared with the experimental group, the control group has obviously poorer treatment effect on local inflammation and swelling, particularly the control groups 1, 11 and 12 have slow resolution of inflammation and swelling, the skin color can not be recovered to be normal, and the rat is restless and has bad state.
The experimental results in table 2 prove that any component and condition in the technical protection scheme of the invention are mutually synergistic and indispensable, and the lack of any component and condition in the technical protection scheme of the invention can obviously influence the treatment effect of local inflammation and swelling. The spray provided by the invention can resist inflammation and detumescence, and has a good application prospect.
Example 3 quality assessment of formulations of each group
The formulations of each experimental group and control group were evaluated for the quality of each group formulation in example 1 in terms of uniformity, coating ductility, centrifugal stability, cold resistance stability and heat resistance stability, respectively, and the evaluation index and score criteria are shown in table 3.
Table 3 evaluation index and score criteria
The evaluation method of each index comprises the following steps: 1) Uniformity. Taking a proper amount of each group of preparation samples, observing whether the color and luster of each group of preparation are uniform, whether the texture is smooth, and standing for 1h to naturally delaminate; 2) Coating ductility. Proper amount of sample is coated on a glass slide, and whether agglomeration exists or not and whether particles are generated or not is observed in the coating process; 3) Centrifugal stability. Taking the same amount of the preparation in each group into 2 centrifuge tubes of 2mL, respectively, and measuring 4000r.min -1 Centrifuging for 15min (centrifugal radius 5 cm), wherein bubbles are generated, and oil-water separation such as layering, color change and the like is performed; 4) Cold resistance stability. Respectively taking each group of equivalent preparations into 3 2mL centrifuge tubes, sealing, storing for 24h at-20 ℃, taking out, cooling to room temperature, observing whether bubbles are generated or not, and judging whether oil-water separation phenomena such as layering, color change and the like occur; 5) And (3) heat-resistant stability, respectively taking the same amount of preparation of each group into 3 centrifuge tubes with the volume of 2mL, sealing, placing the centrifuge tubes into a 50-degree incubator, keeping the temperature for 6 hours, and observing whether bubbles are generated or not, and whether oil-water separation phenomena such as layering, color change and the like occur or not.
And finally, giving a comprehensive score through each evaluation score, wherein the quality evaluation results of each group of preparations are shown in Table 4.
Table 4 results of quality evaluation of each group of formulations
As can be seen from the data in table 4, the formulation combination score was highest in experimental group 4, worst in control group 9, and no O/W type emulsion spray was formed in control groups 11 and 12.
It will be apparent to those skilled in the art that various modifications and variations can be made to the present invention without departing from the spirit or scope of the invention. Thus, it is intended that the present invention also include such modifications and alterations insofar as they come within the scope of the appended claims or the equivalents thereof.
Claims (5)
1. An anti-inflammatory detumescence O/W emulsion, characterized in that the O/W emulsion is composed of an aqueous phase carrying polysaccharide components of fungi and plant origin and an oil phase carrying anthocyanin and plant essential oil; the aqueous phase carrying the polysaccharide component of fungal and plant origin consists of the polysaccharide component of fungal and plant origin, 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; the polysaccharide component of the fungi and plant sources is astragalus polysaccharide; polysaccharide components of fungal and plant origin: polylysine: the mass ratio of poloxamer is 1:4:100; the mass of water in the aqueous phase is 6 times of the total mass of polysaccharide components of fungal and plant origin, polylysine and poloxamer;
the oil phase carrying the anthocyanin and the plant essential oil is formed by dissolving the anthocyanin and the plant essential oil with the mass ratio of 3:1 in mineral oil with the mass ratio of 5 times;
the plant essential oil is tea tree essential oil;
the mineral oil is liquid paraffin 400;
the mass ratio of the water phase carrying the polysaccharide components of fungi and plant sources to the oil phase carrying anthocyanin and plant essential oil in the emulsion is 2:1.
2. A method of preparing the emulsion of claim 1, comprising the steps of:
a) Dispersing polylysine and poloxamer in water, slowly dissolving, adding polysaccharide components of fungi and plant sources, and mixing to form water phase carrying polysaccharide components of fungi and plant sources;
b) Heating mineral oil to 50-60 ℃, adding anthocyanin and plant essential oil, dissolving and mixing uniformly to form an oil phase carrying the anthocyanin and the plant essential oil, adding the water phase carrying the polysaccharide components of fungi and plant sources prepared in the step a) when the temperature is reduced to 35-45 ℃, grinding and mixing uniformly to prepare the O/W emulsion.
3. Use of the emulsion of claim 1 for the preparation of a product for the treatment of localized inflammation and swelling.
4. A use according to claim 3, characterized in that: the product is skin care product or medicine.
5. A use according to claim 3, characterized in that: the emulsion is prepared into spray.
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