Pharmaceutical composition for treating skin itching and preparation method thereof
By mixing the total saponin, hawthorn leaf flavonoids, and chloroplastin in a specific proportion, a drug composition for treating itching of the skin is prepared to solve the problem of poor effects of existing drug compositions and achieved the effect of poor effects and achieved it. A significant anti -inflammatory, antipruritic and anti -perverted effects are better than traditional drugs.
Patent Information
- Application Number
- CN202310566851.1
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2023-05-19
- Publication Date
- 2025-01-28
- Estimated Expiration
- 2043-05-19
AI Technical Summary
The existing pharmaceutical compositions are not effective in treating skin itching, and it is difficult to effectively solve the anti-inflammatory, anti-it-it-and-anti-allergic problems of skin itching.
Adopt a drug composition, including the total saponin, total flavonoids of ingredients, and chloroplasma totaling. By extracting the essence of these ingredients, and mixing according to a specific proportion, prepare anti -inflammatory, antipruritic and anti -anti -anti -anti -anti -itching, anti -itching and anti -anti -anti -anti -anti -itching, anti -itching, anti -itching and anti -anti -anti -anti -anti -itching, anti -itching and anti -anti -anti -anti -anti -itching, anti -itching and anti -anti -anti -anti -anti -itching, anti -itching and anti -anti -anti -anti -anti -itching, anti -itching and anti -anti -anti -anti -itching, anti -itching and anti -anti -anti -anti -itching and anti -anti -anti -itching and anti -anti -anti -itching and anti -anti -itchings anti -itching and anti -itching anti -itching and anti -itching and anti -anti -anti -items Pharmaceutical composition with perverted reaction effect.
This drug composition significantly improves the treatment effect on skin itching. It has significant anti -perverted reactions, swelling and itching effects, and is better than traditional positive control drug dermatitis.
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Figure BDA0004236989810000041 
Figure BDA0004236989810000051
Abstract
Description
Technical Field
[0001] The invention relates to the technical field of pharmaceuticals, and in particular to a pharmaceutical composition for treating skin itching. Background Art
[0002] Skin pruritus is often caused by inflammation of the epidermis and superficial dermis caused by various internal and external factors such as eczema, mosquito bites, allergic skin itch, bacterial and fungal infections, etc., and local treatment is often used. From the perspective of pathogenesis, skin pruritus is a delayed allergic reaction caused by complex internal and external stimulating factors. The present invention conducts pharmacodynamic studies on anti-inflammatory, antipruritic, anti-allergic reactions, etc., and explores its pharmacological effects for preventing and treating skin pruritus.
[0003] Centella asiatica has the effects of clearing away heat and dampness, detoxifying and reducing swelling, and is used to treat damp-heat jaundice, sand and stone stranguria, carbuncle, sore, and injuries from falls. Total flavonoids from hawthorn leaves have anti-inflammatory and anti-edema effects. White peony root has the effects of nourishing blood, nourishing yin, antibacterial, and anti-inflammatory. At present, the pharmaceutical composition for treating skin itching is usually mixed with multiple ingredients, and the effect of the current pharmaceutical composition for treating skin itching often does not meet expectations. Summary of the invention
[0004] The purpose of the present invention is to solve the above-mentioned problems and disclose a pharmaceutical composition for treating skin itching, comprising the following ingredients:
[0005] Centella asiatica total saponins: 0.5-3 parts;
[0006] Total flavonoids from hawthorn leaves: 1 part;
[0007] Total glucosides of white peony: 0.5-3 parts.
[0008] In a preferred embodiment, the total saponins of Centella asiatica are refined extracts extracted from Centella asiatica containing more than 80% by weight of saponins.
[0009] In a preferred embodiment, the total flavonoids from hawthorn leaves refer to an extract extracted from hawthorn leaves containing more than 80% by weight of flavonoid components.
[0010] In a preferred embodiment, the total glucosides of white paeony refer to an extract extracted from white paeony medicinal material containing more than 80% by weight of monoterpene glycosides.
[0011] In a preferred embodiment, the pharmaceutical composition contains excipients, and the excipients are selected from sucrose, starch, dextrin, magnesium stearate, sorbitol, mannitol, lactose, microcrystalline cellulose, and carboxymethyl cellulose.
[0012] In a preferred embodiment, the pharmaceutical composition contains chemical drugs or active ingredients of traditional Chinese medicine that improve the efficacy of the pharmaceutical composition.
[0013] The present invention also discloses a method for preparing a pharmaceutical composition for treating skin itching, the steps comprising:
[0014] 1) extracting total saponins of Centella asiatica from Centella asiatica, wherein the total saponins of Centella asiatica contain more than 80% saponin components by weight;
[0015] 2) extracting a refined extract containing more than 80% by weight of flavonoid components from the hawthorn leaf medicinal material to obtain total flavonoids from the hawthorn leaf;
[0016] 3) extracting from white peony root a refined extract containing more than 80% by weight of monoterpene glycosides to obtain white peony total glycosides;
[0017] 4) Mix 0.5-3 parts of total saponins of Centella asiatica, 1 part of total flavonoids of hawthorn leaves, and 0.5-3 parts of total glucosides of white peony to prepare a pharmaceutical composition for treating skin itching.
[0018] In a preferred embodiment, the steps of extracting total saponins of Centella asiatica from Centella asiatica are as follows:
[0019] 1) Take Centella asiatica, add 10-15 times the weight of 20%-70% ethanol solution, heat and reflux to extract 1-3 times, each time for 0.5-2 hours, and combine the extracts.
[0020] 2) The extract is concentrated under reduced pressure until there is no alcohol taste, and then eluted with water or an ethanol solution with a concentration not exceeding 10% through a macroporous resin until the effluent is transparent, and then eluted with a 20%-70% ethanol solution for 4-6 times the column volume, and the 20%-70% ethanol eluate is collected. Preferably, the macroporous adsorption resin is AB-8 or D101 macroporous adsorption resin. The MCI GEL reverse phase filler is 50-75u or 30-50u.
[0021] 3) Concentrate the 20%-70% ethanol eluate until it has no alcohol smell, pass it through an MCI GEL reverse phase resin column, elute with 10%-20% ethanol for 3-4 times the column volume, discard it, elute with 30%-60% ethanol for 5-6 times the column volume, detect it by HPLC, collect the eluate rich in asiaticoside B, madecassoside and asiaticoside, concentrate and dry it, and obtain total saponins of Centella asiatica with a content of 80%-90%.
[0022] In a preferred embodiment, the step of extracting total flavonoids from hawthorn leaves comprises:
[0023] 1) Take hawthorn leaf medicinal material, add 10-15 times the weight of 30%-90% ethanol solution, heat and reflux to extract 1-3 times, each time for 0.5-2 hours, and combine the extracts.
[0024] 2) The extract is concentrated under reduced pressure until there is no alcohol taste, and then eluted with water or an ethanol solution with a concentration not exceeding 10% by a macroporous adsorption resin until the effluent is transparent, and then eluted with an ethanol solution with a concentration of 20%-60% by 4-6 times the column volume, and the ethanol eluate with a concentration of 20%-60% is collected. Preferably, the macroporous adsorption resin is AB-8 type or D101 type macroporous adsorption resin, and the MCI GEL reverse phase filler is 50-75u or 30-50u.
[0025] 3) The 20%-60% ethanol eluate is concentrated until there is no alcohol smell, passed through an MCI GEL reverse phase resin column, eluted with 10%-20% ethanol for 3-4 times the column volume, discarded, and eluted with 40%-70% ethanol for 5-6 times the column volume, and detected by HPLC, and the eluate rich in vitexin rhamnoside, vitexin glucoside, vitexin and hyperoside was collected, concentrated and dried to obtain a total flavonoid content of 60%-90%.
[0026] In a preferred embodiment, the method for extracting total glucosides of paeony root from white peony root medicinal material comprises:
[0027] 1) Take white peony root, add 10-15 times of 30%-90% ethanol solution by weight, heat and reflux to extract 1-3 times, each time for 0.5-2 hours, and combine the extracts.
[0028] 2) The extract is concentrated under reduced pressure until there is no alcohol taste, and passed through a macroporous resin, first eluted with water or an ethanol solution with a concentration not exceeding 10% until the effluent is transparent, and then eluted with a 30%-60% ethanol solution for 4-6 times the column volume, and subjected to HPLC detection, and the eluate rich in paeoniflorin, paeoniflorin, isopaeoniflorin, gallopaeoniflorin and benzoylpeoniflorin is collected, concentrated and dried to obtain total glucosides of white peony with a content of 80%-90%. Preferably, the macroporous adsorption resin is AB-8 type or D101 type macroporous adsorption resin.
[0029] The pharmaceutical composition of the present invention has the effects of anti-allergic reaction, detumescence and antipruritic, and has significantly superior effects compared with existing pharmaceutical compositions. The anti-allergic reaction, detumescence and antipruritic effects of the composition of the present invention are better than those of the positive control Pi Yan Ping and the positive control Qu Mi Xin. DETAILED DESCRIPTION
[0030] The present invention is described in detail below.
[0031] Example 1
[0032] preparation:
[0033] 1. Preparation of total saponins from Centella asiatica.
[0034] Centella asiatica powder is taken, and 13 times of 50% ethanol solution is added according to weight, and the powder is heated under reflux for extraction twice, each time for 1 hour, and the extracts are combined; the extract is concentrated under reduced pressure until there is no alcohol taste, and the extract is passed through a macroporous resin, and firstly eluted with water until the effluent is transparent, and then eluted with 60% ethanol solution for 6 times of column volume, and the 60% ethanol eluate is collected; the 60% ethanol eluate is concentrated until there is no alcohol taste, and passed through an MCI GEL reverse phase resin column, and eluted with 20% ethanol for 3-4 times of column volume, which is discarded, and eluted with 50% ethanol for 5-6 times of column volume, and HPLC detection is performed, and the eluate rich in asiaticoside B, hydroxymadecassoside and asiaticoside is collected, and concentrated and dried to obtain total saponins with a content of 86.3%.
[0035] 2. Preparation of total flavonoids from hawthorn leaves.
[0036] Take hawthorn leaf medicinal material, crush it, add 15 times of 60% ethanol solution, reflux extraction for 1.5 hours, filter, repeat extraction once for the filter residue, and combine the filtrate. The extract is concentrated under reduced pressure until there is no alcohol taste, pass through D101 macroporous adsorption resin, first elute with water until the effluent is transparent, then elute with 60% ethanol solution for 4 times column volume, and collect 60% ethanol eluate. The 60% ethanol eluate is concentrated until there is no alcohol taste, pass through MCI GEL reverse phase resin column, elute with 10% ethanol for 3 times column volume, discard, elute with 50% ethanol for 5 times column volume, HPLC detection, collect eluate rich in vitexin rhamnoside, vitexin glucoside, vitexin and hyperoside, concentrate and dry, and obtain total flavonoids with a content of 82.6%.
[0037] 3. Preparation method of total glycosides of white peony root:
[0038] Take white peony powder, add 15 times the weight of 30% ethanol solution, heat reflux extraction 3 times, each time for 1 hour, and combine the extracts; reduce the pressure and concentrate the extract until there is no alcohol taste, pass it through AB-8 macroporous resin, first elute with aqueous solution until the effluent is transparent, then elute with 50% ethanol solution for 6 times the column volume, perform HPLC detection, collect the eluate rich in paeoniflorin, paeoniflorin lactone glycosides, isopaeoniflorin, gallopeoniflorin and benzoylpeoniflorin, concentrate and dry, and obtain total white peony glucosides with a content of 86.8%.
[0039] The total saponins of Centella asiatica, the total flavonoids of hawthorn leaves, the total glucosides of white paeony and / or the cream base are uniformly mixed according to a certain proportion to obtain the pharmaceutical composition for treating skin itching of the present invention.
[0040] 2. Effect Test
[0041] 1. Antipruritic effect test
[0042] 90 guinea pigs were selected. 24 hours after the hair removal of the right hind foot of the animals, the hind foot dorsum was scratched with sandpaper until a small amount of bleeding occurred. Then the animals were randomly divided into 9 groups, and the prepared total saponins of Centella asiatica 2g / kg, total flavonoids of Hawthorn leaves 2g / kg, total glycosides of white peony 2g / kg, the combination of the three 2g / kg, Centella asiatica and Hawthorn leaves 2g / kg, Centella asiatica and white peony combination, Hawthorn leaves and white peony combination, Piyanping ointment 2g / kg and matrix 2g / kg were evenly applied to the scratched parts. After 30 minutes, 0.05ml / animal of histamine hydrochloride with a mass volume concentration (ug / ml) of 10, 20, 30 to 100 was applied to the scratched parts of the guinea pigs, and the interval time for each time was 3 minutes. The histamine concentration when each animal had a foot-licking reaction was recorded. This concentration was the itch threshold. The results are shown in Table 1.
[0043]
[0044] Table 1 Effect of histamine hydrochloride on the itch threshold of guinea pig feet
[0045] Analysis of results: As can be seen from the table, compared with the control group, P<0.05, the combination of Centella asiatica total saponins, hawthorn leaf total flavonoids and white peony total glucosides can increase the antipruritic threshold of histamine hydrochloride in guinea pigs, and the combination of the three has a very significant synergistic effect.
[0046] 2. Effect of p-xylene on ear swelling in mice
[0047] Take 90 mice and randomly divide them into 9 groups, Centella asiatica total saponins group, Hawthorn leaf total flavonoids group, white peony total glucosides group, three composition groups, Centella asiatica Hawthorn leaf composition group, Centella asiatica white peony composition group, Hawthorn leaf white peony composition group, positive control group and blank control group, each group formula is the same as the above embodiment, 10 in each group. The right ear of each group of mice is coated with xylene to cause inflammation, 0.05ml for each. Centella asiatica total saponins, Hawthorn leaf total flavonoids, white peony total glucosides and four composition groups are evenly coated on the right ear, respectively, and the positive control group is given Qu Mixin cream 2.0g / kg, and the blank group is given blank matrix 2.0g / kg. After applying the medicine for 30min, each administration group washes off the liquid, and the cotton swab is cleaned, and the mice are killed, and the left and right ears are cut off respectively, and the left ear is used as a control. The same area of the two ears is taken off with a 1cm puncher, and the swelling degree is expressed by the difference of the left and right ear weights, and the swelling degree of each group is calculated.
[0048] Group Dosage (g / kg) Number of mice Quality difference of two ear tablets (mg) Matrix (blank) 2.0 10 6.31±1.25 Centella asiatica total saponins group 2.0 10 4.66±1.12 Total flavonoids from hawthorn leaves 2.0 10 4.85±1.04 Total glycosides of white peony 2.0 10 4.36±1.16 Centella asiatica and hawthorn leaf combination 2.0 10 3.75±1.09 Centella asiatica and white peony root combination 2.0 10 3.46±1.13 Hawthorn leaf and white peony root combination 2.0 10 3.67±1.03 A combination of the three 2.0 10 2.78±1.26 Qumixin cream 2.0 10 2.96±1.03
[0049] Table 2 Xylene-induced ear swelling in mice
[0050] The results in Table 2 show that compared with the blank control group, the total saponins group of Centella asiatica, the total flavonoids group of Crataegus pinnatifida, the total glycosides of Paeony dahurica and the combination groups were statistically significant, and the combination group of the three had a very obvious inhibitory effect on xylene-induced ear swelling and inflammation in mice, and the effect was better than the positive control Qumixin cream.
[0051] 3. Effects on delayed-type hypersensitivity reaction induced by 2,4-dinitrochlorobenzene in mice
[0052] 72 mice were taken, and after grouping, the abdomen of each group of mice was depilated, with an area of about 2-3cm*2-3cm. The depilated area was administered once, and 0.02ml of 7% 2,4-dinitrochlorophenylacetone solution was subcutaneously injected into the back of each mouse 24 hours later. Sensitization was repeated once 3 days later. Subsequently, each group was smeared once in the morning and evening every day for 8 consecutive days. On the 9th day, 0.02ml of 1% 2,4-dinitrochlorophenylacetone solution was evenly applied to the right ear of the mouse. After 24 hours, 8 mice in each group were blooded by enucleation, and serum was obtained after centrifugation. The content of IL-4 in the serum was determined by enzyme-linked immunosorbent assay. The mice were killed, and the left and right ear pieces of the same part were removed with a 1cm diameter puncher, accurately weighed, and the swelling degree of each group was calculated. The concentration of the composition was the same as that in the above embodiment.
[0053]
[0054] Table 3 Delayed-type hypersensitivity of mice in each group
[0055] As can be seen from Table 3, compared with the blank control group, total saponins of Centella asiatica, total flavonoids of hawthorn leaves, total glucosides of white peony, and each combination group can improve the ear swelling of mice, with statistically significant differences.
[0056] Total saponins of Centella asiatica, total flavonoids of hawthorn leaves and total glucosides of white paeony all have obvious inhibitory effects on allergic dermatitis induced by 2,4-dinitrobenzene in mice, and the combination of the three has a very significant synergistic effect; total saponins of Centella asiatica, total flavonoids of hawthorn leaves, total glucosides of white paeony and their mutual combination can significantly reduce the content of IL-4 in serum, and the combination of the three has a very significant synergistic effect.
[0057] This study confirmed that total saponins of Centella asiatica, total flavonoids of hawthorn leaves, and total glucosides of white peony have anti-allergic, anti-edema, and antipruritic effects, and the combination of the three has a very significant synergistic effect. The anti-allergic, anti-edema, and antipruritic effects of the composition of the present invention are better than those of the positive control drug Piyanping and the positive control drug Qumixin.
Claims
1. A pharmaceutical composition for treating skin itching, characterized in that: According to weight parts, it is made of the following materials: Centella asiatica total saponins: 0.5-3 parts; Total flavonoids from hawthorn leaves: 1 part; Total glucosides of white peony: 0.5-3 parts.
2. The pharmaceutical composition for treating skin itching according to claim 1, characterized in that: The Centella asiatica total saponin is a refined extract extracted from Centella asiatica containing more than 80% saponin components by weight.
3. The pharmaceutical composition for treating skin itching according to claim 2, characterized in that: The total flavonoids from hawthorn leaves refer to the refined extract extracted from hawthorn leaves containing more than 80% flavonoid components by weight.
4. The pharmaceutical composition for treating skin itching according to claim 3, characterized in that: The total glucosides of white paeony refer to the refined extract extracted from white peony medicinal material, which contains more than 80% by weight of monoterpene glycosides.
5. The pharmaceutical composition for treating skin itching according to any one of claims 1 to 4, characterized in that: The pharmaceutical composition contains auxiliary materials, and the auxiliary materials are selected from sucrose, starch, dextrin, magnesium stearate, sorbitol, mannitol, lactose, microcrystalline cellulose, and carboxymethyl cellulose.
6. A method for preparing a pharmaceutical composition for treating skin itching, characterized in that the steps include: 1) extracting total saponins of Centella asiatica from Centella asiatica, wherein the total saponins of Centella asiatica contain more than 80% saponin components by weight; 2) extracting a refined extract containing more than 80% by weight of flavonoid components from the hawthorn leaf medicinal material to obtain total flavonoids from the hawthorn leaf; 3) extracting a refined extract containing more than 80% by weight of monoterpenoid glycosides from white peony root to obtain total glycosides of white peony root; 4) Mix 0.5-3 parts of total saponins of Centella asiatica, 1 part of total flavonoids of hawthorn leaves, and 0.5-3 parts of total glucosides of white peony to prepare a pharmaceutical composition for treating skin itching.
7. The method for preparing the pharmaceutical composition for treating skin itching according to claim 6, characterized in that: The steps of extracting total saponins from Centella asiatica are as follows: 1) Take Centella asiatica, add 10-15 times the weight of 20%-70% ethanol solution, heat and reflux to extract 1-3 times, each time for 0.5-2 hours, and combine the extracts; 2) The extract is concentrated under reduced pressure until it has no alcohol taste, and passed through a macroporous resin. First, it is eluted with water or an ethanol solution with a concentration not exceeding 10% until the effluent is transparent, and then eluted with an ethanol solution with a concentration of 20%-70% for 4-6 times the column volume, and the 20%-70% ethanol eluate is collected; 3) Concentrate the 20%-70% ethanol eluate until it has no alcohol smell, pass it through an MCI GEL reverse phase resin column, elute with 10%-20% ethanol for 3-4 column volumes, elute with 30%-60% ethanol for 5-6 column volumes, and perform HPLC detection. Collect the eluate rich in asiaticoside B, madecassoside and asiaticoside, concentrate and dry it to obtain 80%-90% total saponins of Centella asiatica.
8. The method for preparing the pharmaceutical composition for treating skin itching according to claim 7, characterized in that: The steps of extracting total flavonoids from hawthorn leaves include: 1) Take hawthorn leaf medicinal material, add 10-15 times the weight of 30%-90% ethanol solution, heat and reflux to extract 1-3 times, each time for 0.5-2 hours, and combine the extracts; 2) The extract is concentrated under reduced pressure until it has no alcohol taste, and then passed through a macroporous adsorption resin. First, it is eluted with water or an ethanol solution with a concentration not exceeding 10% until the effluent is transparent, and then eluted with a 20%-60% ethanol solution for 4-6 times the column volume, and the 20%-60% ethanol eluate is collected; 3) Concentrate the 20%-60% ethanol eluate until it has no alcohol smell, pass it through an MCI GEL reverse phase resin column, elute with 10%-20% ethanol for 3-4 times the column volume, discard, elute with 40%-70% ethanol for 5-6 times the column volume, detect with HPLC, collect the eluate rich in vitexin rhamnoside, vitexin glucoside, vitexin and hyperoside, concentrate and dry, and obtain a total flavonoid content of 60%-90%.
9. The method for preparing the pharmaceutical composition for treating skin itching according to any one of claims 6 to 8, characterized in that: The method for extracting total glycosides of paeony root from white peony root medicinal material comprises: 1) Take white peony root, add 10-15 times the weight of 30%-90% ethanol solution, heat and reflux to extract 1-3 times, each time for 0.5-2 hours, and combine the extracts; 2) The extract is concentrated under reduced pressure until it has no alcohol taste, and passed through a macroporous resin. It is first eluted with water or an ethanol solution with a concentration not exceeding 10% until the effluent is transparent, and then eluted with an ethanol solution with a concentration of 30%-60% for 4-6 times the column volume. HPLC detection is performed, and the eluate rich in paeoniflorin, paeoniflorin, isopaeoniflorin, gallopaeoniflorin and benzoylpeoniflorin is collected, concentrated and dried to obtain total glucosides of white peony with a content of 80%-90%.
Citation Information
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