Traditional Chinese medicine composition for treating hyperplasia of mammary glands as well as preparation method and external preparation thereof
By using topical preparations of traditional Chinese medicine compositions such as cloves, asarum, safflower, yamus, Wangbuli, musk and borneol, they are directly absorbed into the breast locally through the skin, solving the adverse reactions and high recurrence rates of breast hyperplasia treatment in the prior art, and achieving efficient and safe therapeutic effects.
Patent Information
- Application Number
- CN202311335665.3
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2023-10-16
- Publication Date
- 2025-04-18
AI Technical Summary
The prior art has problems such as adverse drug reactions, high recurrence rates, expensive treatment costs, and the need for drug to pass through the digestive system to cause toxic and side effects.
Traditional Chinese medicine compositions such as lilac, asarum, safflower, yamus, Wangbuli, musk and borneol are used to treat the drug directly through the skin through the transdermal absorption, and directly enter the blood circulation, acting on the breast, regulating the circulation of qi and blood throughout the body, and improving breast microcirculation.
It improves the efficacy of treating breast hyperplasia, reduces the impact of drugs on the digestive system, reduces the risk of adverse reactions, has fast effect and good stability, and has wide application value.
Smart Images
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Abstract
Description
Technical Field
[0001] The present application relates to a traditional Chinese medicine composition for treating breast hyperplasia, a preparation method thereof and an external preparation thereof, and belongs to the technical field of traditional Chinese medicine. Background Art
[0002] Traditional Chinese medicine believes that breast hyperplasia is caused by anger and depression that damages the liver, worry and anxiety that damages the spleen, qi stagnation and blood stasis, and phlegm condensation and nucleation. Chinese medicine calls it "breast disease". Breast hyperplasia is a benign proliferative disease of breast tissue. It is neither an inflammation nor a tumor. It is the most common breast disease in women of childbearing age, with an incidence rate of about 40% in women of childbearing age and 75% of all breast diseases. In addition, the incidence rate has been increasing year by year, seriously affecting women's physical and mental health. Among them, atypical breast hyperplasia belongs to the category of precancerous lesions, with a canceration rate of more than 10%, and is the focus of research on breast hyperplasia.
[0003] At present, the main Western medicine drugs for the treatment of breast hyperplasia are hormone drugs, iodine preparations and tamoxifen, which can relieve pain, but may cause adverse reactions, causing patients to panic and confuse, and are very likely to relapse after stopping the drug. Long-term use may have the risk of inducing endometrial cancer and may also cause imbalance between human hormones; oral drug treatment is not very purposeful, the treatment cost is expensive, and it is easy to relapse after stopping the drug. In addition, the existing oral drug formulations are numerous and the preparation methods are complicated. When treating breast hyperplasia, the drugs must pass through the digestive system and have relatively large toxic and side effects; surgical treatment can remove the hyperplastic mass, but it cannot eliminate the cause of the hyperplastic mass in the human body or blood, and is also prone to relapse. Summary of the invention
[0004] In order to solve the above problems, a Chinese medicine composition for treating breast hyperplasia, a preparation method thereof and an external preparation thereof are provided. The present application selects clove and asarum as the main medicines. Clove warms the kidney and assists yang, promotes qi and relieves pain, and asarum warms the meridians, dispels cold and relieves pain. The two medicines are used together to warm the meridians, activate blood circulation and regulate qi; safflower, corydalis and vetch are the auxiliary medicines. Safflower promotes blood circulation and removes blood stasis, promotes menstruation and relieves pain, corydalis promotes blood circulation and relieves blood stasis in the middle and qi, and vetch promotes blood circulation and promotes menstruation, relieves swelling in the breast, and is a medicine for the yangming, Chong and Ren meridians. The three medicines assist the main medicine to promote blood circulation, relieve swelling and relieve pain; borneol opens all orifices, relieves swelling and relieves pain, and musk opens the orifices, relieves pain, promotes blood circulation and disperses nodules; the two medicines are together the adjuvant medicine. The combination of these medicines can warm the meridians and promote blood circulation, regulate qi and relieve pain, disperse stagnation and reduce swelling; when applied externally through the skin, the drug can reach the lesion directly through transdermal absorption, and the drug can directly enter the blood circulation and act on the local breast, which helps to improve the efficacy and reduce the impact of the human digestive and absorption system on the drug; it can also regulate the circulation of qi and blood throughout the body through meridian stimulation and improve breast microcirculation.
[0005] According to one aspect of the present application, a traditional Chinese medicine composition for treating breast hyperplasia is provided, which includes, by weight: 10 to 30 parts of cloves, 5 to 20 parts of asarum, 5 to 20 parts of Corydalis yanhusuo, 10 to 30 parts of safflower, 10 to 30 parts of fenugreek, 0.1 to 2 parts of musk and 0.2 to 1.8 parts of borneol.
[0006] Optionally, the composition comprises, by weight: 15-25 parts of cloves, 6-15 parts of asarum, 6-15 parts of Corydalis yanhusuo, 13-25 parts of safflower, 15-30 parts of fenugreek, 0.2-1.8 parts of musk and 0.3-1.6 parts of borneol.
[0007] Optionally, the composition comprises, by weight: 18 parts of cloves, 8 parts of asarum, 8 parts of yanhusuo, 15 parts of safflower, 18 parts of fenugreek, 0.5 parts of musk and 0.5 parts of borneol;
[0008] Or, 20 parts of cloves, 10 parts of asarum, 10 parts of Corydalis yanhusuo, 20 parts of safflower, 20 parts of fenugreek, 1 part of musk and 1 part of borneol;
[0009] Or, 22 parts of cloves, 8 parts of asarum, 12 parts of Corydalis yanhusuo, 18 parts of safflower, 24 parts of fenugreek, 1.4 parts of musk and 1.2 parts of borneol;
[0010] Or, 24 parts of cloves, 13 parts of asarum, 14 parts of Corydalis yanhusuo, 25 parts of safflower, 28 parts of fenugreek, 1.6 parts of musk and 1.5 parts of borneol.
[0011] According to another aspect of the present application, a method for preparing the above-mentioned Chinese medicine composition for treating breast hyperplasia is provided, comprising the following steps:
[0012] (1) Weighing Chinese medicinal materials according to weight;
[0013] (2) Clove and asarum are crushed, soaked in water, extracted with water to obtain volatile oil, and then encapsulated with cyclodextrin to obtain a volatile oil inclusion compound for later use; the first extract and the residue are reserved; Vaccaria segetalis is taken, and the residue and Vaccaria segetalis are extracted with water to obtain a second extract; the first extract and the second extract are mixed and concentrated to a clear paste, ethanol is added, allowed to stand, and filtered to obtain an alcohol precipitate;
[0014] (3) extracting safflower and corydalis with ethanol respectively, filtering and combining the ethanol extracts;
[0015] (4) combining the alcohol precipitate in step (2) and the alcohol extract in step (3), and concentrating them to obtain a Chinese medicine extract;
[0016] (5) Grind musk into fine powder and set aside;
[0017] (6) stirring and dissolving borneol in a solvent to obtain a borneol solution;
[0018] (7) Slowly add borneol solution, volatile oil inclusion compound, musk powder and auxiliary materials to the Chinese herbal medicine extract and stir evenly.
[0019] Optionally, the extraction time of the volatile oil by water extraction in step (2) does not exceed 8 hours.
[0020] Optionally, the extraction time of the volatile oil by water extraction in step (2) is 2 to 8 hours.
[0021] Optionally, the solvent in step (6) includes ethanol, propylene glycol or isopropyl myristate; the auxiliary material in step (7) is an auxiliary material that assists the components to be mixed and dispersed uniformly, including: one or more of propylene glycol, glycerol, liquid paraffin, Tween 80 or Span 80.
[0022] Optionally, the relative density of the clear paste in step (2) is 1.05-1.35;
[0023] In step (2), ethanol is added until the alcohol content reaches 50% to 80%;
[0024] The dissolution temperature of borneol in step (6) is 40 to 80° C.;
[0025] The stirring temperature in step (7) is 40 to 80° C.;
[0026] The concentration temperature in step (2) and step (4) is 50 to 100°C.
[0027] According to another aspect of the present application, a Chinese medicine composition external preparation for treating breast hyperplasia is provided, wherein the Chinese medicine composition external preparation contains the Chinese medicine composition according to any one of claims 1 to 3.
[0028] Optionally, the external preparation of the traditional Chinese medicine composition includes an ointment, a liniment, a cream, a paint, a gel, a film coating, a gel patch or a lotion.
[0029] The beneficial effects of this application include but are not limited to:
[0030] 1. According to the Chinese medicine composition for treating breast hyperplasia of the present application, clove and asarum are selected as the main medicines. Clove warms the kidney and assists yang, promotes qi and relieves pain, and asarum warms the meridians and dispels cold and relieves pain. The two medicines are used together to warm the meridians, activate blood circulation and regulate qi; safflower, corydalis and cyperus rotundus are used as the assistant medicines. Safflower promotes blood circulation and removes blood stasis, promotes menstruation and relieves pain, corydalis promotes blood circulation and causes stagnation in the middle of the body and blood stasis in the qi, and cyperus rotundus promotes blood circulation and promotes menstruation, relieves swelling in the breast, and is a medicine for the yangming Chong and Ren meridians. The three medicines assist the main medicine to promote blood circulation, relieve swelling and relieve pain; borneol opens all the orifices, relieves swelling and relieves pain, and musk opens the orifices, relieves pain, activates blood circulation and disperses nodules; the two medicines are used as adjuvants. All the medicines are used together to warm the meridians and activate blood circulation, regulate qi and relieve pain, and disperse nodules and relieve swelling.
[0031] 2. According to the external preparation of the Chinese medicine composition for treating breast hyperplasia of the present application, the drug is administered through the skin through external application, reaches the lesion directly through transdermal absorption, and the drug directly enters the blood circulation and acts on the local breast, which helps to improve the efficacy, avoid the first-pass effect of the liver and the inactivation of the drug in the gastrointestinal tract, and the absorption of the drug is not affected by gastrointestinal factors; it can also regulate the circulation of qi and blood throughout the body through meridian stimulation and improve breast microcirculation.
[0032] 3. The external preparation of the Chinese medicine composition according to the present application has scientific compatibility, fine drug selection, safety and no toxic side effects, significant efficacy, rapid effect, good stability and easy use, and has wide application value.
[0033] 4. According to the preparation method of the Chinese medicine composition for treating breast hyperplasia of the present application, the process is stable, the yield is high, the quality is good, the cost and energy consumption are low, the raw materials are extensive, and the process is simple and economical; the production can be completed using existing equipment, which reduces the equipment requirements and has zero pollution to the environment; in addition, according to the chemical composition and properties of the compatible medicinal materials, the volatile oil is first extracted, then water extraction, and alcohol extraction is used, so that the content of effective ingredients is high, and impurities such as starch, sugar and tannins are less, and the effect is better. DETAILED DESCRIPTION
[0034] The present application is described in detail below with reference to embodiments, but the present application is not limited to these embodiments.
[0035] Unless otherwise defined, all professional and scientific terms used herein have the same meanings as those familiar to those skilled in the art. The reagents or raw materials used in the present invention can be purchased through conventional channels. Unless otherwise specified, the reagents or raw materials used in the present invention are used in a conventional manner in the art or in accordance with the product instructions. In addition, any method and material similar or equivalent to the described content can be applied to the method of the present invention. The preferred implementation methods and materials described in this patent are for demonstration purposes only.
[0036] Example 1 A Chinese medicine composition for treating breast hyperplasia 1#
[0037] (1) Weigh the following Chinese medicinal materials by weight: 10 parts of cloves, 5 parts of asarum, 5 parts of Corydalis yanhusuo, 10 parts of safflower, 10 parts of fenugreek, 0.1 parts of musk and 0.2 parts of borneol, each part is calculated as 15 g;
[0038] (2) Clove and Asarum were crushed, soaked with 6 times water, extracted with water for 2 hours to obtain volatile oil, and then encapsulated with cyclodextrin for later use, thereby obtaining a first extract and a residue; Vaccaria segetalis was taken, and the residue and Vaccaria segetalis were extracted with water twice to obtain a second extract; the first extract and the second extract were mixed and concentrated to a clear paste at a concentration temperature of 70° C. The relative density of the clear paste was 1.05, ethanol was added until the alcohol content reached 50%, and the mixture was allowed to stand for 24 hours, and filtered to obtain an alcohol precipitate;
[0039] (3) Take safflower and Corydalis yanhusuo, extract them twice with 8 times and 6 times the volume fraction of 60% ethanol, respectively, for 40 minutes each time, filter, and combine the alcohol extracts;
[0040] (4) combining the alcohol precipitate in step (2) and the alcohol extract in step (3), and concentrating the mixture at a temperature of 70° C. to obtain a Chinese medicine extract;
[0041] (5) Grind musk into fine powder and set aside;
[0042] (6) stirring and dissolving borneol in ethanol at a dissolution temperature of 40° C. to obtain a borneol solution;
[0043] (7) Slowly add borneol solution, volatile oil inclusion compound, musk powder and Tween 80 to the Chinese herbal medicine extract and stir evenly at 40°C.
[0044] Example 2 A Chinese medicine composition for treating breast hyperplasia 2#
[0045] (1) Weigh the following Chinese medicinal materials by weight: 15 parts of cloves, 6 parts of asarum, 6 parts of Corydalis yanhusuo, 13 parts of safflower, 15 parts of fenugreek, 0.2 parts of musk and 0.3 parts of borneol, each part is calculated as 15 g;
[0046] (2) Clove and Asarum were crushed, soaked with 6 times water, and extracted with water for 8 hours to obtain volatile oil, which was encapsulated with cyclodextrin and used as a first extract and a residue; Vaccaria segetalis was taken, and the residue and Vaccaria segetalis were extracted with water twice to obtain a second extract; the first extract and the second extract were mixed and concentrated to a clear paste at a concentration temperature of 80° C. The relative density of the clear paste was 1.15, ethanol was added until the alcohol content reached 80%, and the mixture was allowed to stand for 24 hours, and filtered to obtain an alcohol precipitate;
[0047] (3) Take safflower and Corydalis yanhusuo, extract them twice with 8 times and 6 times the volume fraction of 60% ethanol, respectively, for 40 minutes each time, filter, and combine the alcohol extracts;
[0048] (4) combining the alcohol precipitate in step (2) and the alcohol extract in step (3), and concentrating the mixture at a temperature of 80° C. to obtain a Chinese medicine extract;
[0049] (5) Grind musk into fine powder and set aside;
[0050] (6) stirring and dissolving borneol in propylene glycol at a dissolution temperature of 55° C. to obtain a borneol solution;
[0051] (7) Slowly add borneol solution, volatile oil inclusion compound, musk powder and Tween 80 to the Chinese herbal medicine extract and stir evenly at 55°C.
[0052] Example 3 A Chinese medicine composition for treating breast hyperplasia 3#
[0053] (1) Weigh the following Chinese medicinal materials by weight: 18 parts of cloves, 8 parts of asarum, 8 parts of yanhusuo, 15 parts of safflower, 18 parts of fenugreek, 0.5 parts of musk and 0.5 parts of borneol, each part is calculated as 15 g;
[0054] (2) Clove and Asarum were crushed, soaked with 6 times water, and extracted with water for 5 hours to obtain volatile oil, which was encapsulated with cyclodextrin and used as a first extract and a residue; Vaccaria segetalis was taken, and the residue and Vaccaria segetalis were extracted with water twice to obtain a second extract; the first extract and the second extract were mixed and concentrated to a clear paste at a concentration temperature of 75° C. The relative density of the clear paste was 1.10, ethanol was added until the alcohol content reached 60%, and the mixture was allowed to stand for 24 hours, and filtered to obtain an alcohol precipitate;
[0055] (3) Take safflower and Corydalis yanhusuo, extract them twice with 8 times and 6 times the volume fraction of 60% ethanol, respectively, for 40 minutes each time, filter, and combine the alcohol extracts;
[0056] (4) combining the alcohol precipitate in step (2) and the alcohol extract in step (3), and concentrating the mixture at a temperature of 75° C. to obtain a Chinese medicine extract;
[0057] (5) Grind musk into fine powder and set aside;
[0058] (6) stirring and dissolving borneol in propylene glycol at a dissolution temperature of 50° C. to obtain a borneol solution;
[0059] (7) Slowly add borneol solution, volatile oil inclusion compound, musk powder and Span 80 to the Chinese herbal medicine extract and stir evenly at 50°C.
[0060] Example 4 A Chinese medicine composition for treating breast hyperplasia 4#
[0061] (1) Weigh the following Chinese medicinal materials by weight: 20 parts of cloves, 10 parts of asarum, 10 parts of yanhusuo, 20 parts of safflower, 20 parts of fenugreek, 1 part of musk, and 1 part of borneol, each part is calculated as 15 g;
[0062] (2) Clove and Asarum were crushed, soaked with 6 times water, and extracted with water for 4 hours to obtain volatile oil, which was encapsulated with cyclodextrin and used as a first extract and a residue; Vaccaria segetalis was taken, and the residue and Vaccaria segetalis were extracted with water twice to obtain a second extract; the first extract and the second extract were mixed and concentrated to a clear paste at a concentration temperature of 75° C. The relative density of the clear paste was 1.15, ethanol was added until the alcohol content reached 70%, and the mixture was allowed to stand for 24 hours, and filtered to obtain an alcohol precipitate;
[0063] (3) Take safflower and Corydalis yanhusuo, extract them twice with 8 times and 6 times the volume fraction of 60% ethanol, respectively, for 40 minutes each time, filter, and combine the alcohol extracts;
[0064] (4) combining the alcohol precipitate in step (2) and the alcohol extract in step (3), and concentrating the mixture at a temperature of 75° C. to obtain a Chinese medicine extract;
[0065] (5) Grind musk into fine powder and set aside;
[0066] (6) stirring and dissolving borneol in propylene glycol at a dissolution temperature of 55° C. to obtain a borneol solution;
[0067] (7) Slowly add borneol solution, volatile oil inclusion compound, musk powder, propylene glycol and Tween 80 to the Chinese herbal medicine extract and stir evenly at 55°C.
[0068] Example 5 A Chinese medicine composition for treating breast hyperplasia 5#
[0069] (1) Weigh the following Chinese medicinal materials by weight: 22 parts of cloves, 8 parts of asarum, 12 parts of yanhusuo, 18 parts of safflower, 24 parts of fenugreek, 1.4 parts of musk, and 1.2 parts of borneol, each part is calculated as 15 g;
[0070] (2) Clove and asarum are crushed, soaked with 6 times water, and extracted with water for 3 hours to obtain volatile oil, which is encapsulated with cyclodextrin and used as a first extract and a residue; Vaccaria segetalis is taken, and the residue and Vaccaria segetalis are extracted with water twice to obtain a second extract; the first extract and the second extract are mixed and concentrated to a clear paste at a concentration temperature of 50° C. The relative density of the clear paste is 1.20, ethanol is added until the alcohol content reaches 70%, the mixture is allowed to stand for 24 hours, and an alcohol precipitate is obtained by filtering;
[0071] (3) Take safflower and Corydalis yanhusuo, extract them twice with 8 times and 6 times the volume fraction of 60% ethanol, respectively, for 40 minutes each time, filter, and combine the alcohol extracts;
[0072] (4) combining the alcohol precipitate in step (2) and the alcohol extract in step (3), and concentrating the mixture at a temperature of 50° C. to obtain a Chinese medicine extract;
[0073] (5) Grind musk into fine powder and set aside;
[0074] (6) stirring and dissolving borneol in propylene glycol at a dissolution temperature of 60° C. to obtain a borneol solution;
[0075] (7) Slowly add borneol solution, volatile oil inclusion compound, musk powder and glycerin to the Chinese herbal medicine extract and stir evenly at 60°C.
[0076] Example 6 A Chinese medicine composition for treating breast hyperplasia 6#
[0077] (1) Weigh the following Chinese medicinal materials by weight: 24 parts of cloves, 13 parts of asarum, 14 parts of Corydalis yanhusuo, 25 parts of safflower, 28 parts of fenugreek, 1.6 parts of musk, and 1.5 parts of borneol, each part is calculated as 15 g;
[0078] (2) Clove and Asarum were crushed, soaked with 6 times water, and extracted with water for 6 hours to obtain volatile oil, which was encapsulated with cyclodextrin and used as a first extract and a residue; Vaccaria segetalis was taken, and the residue and Vaccaria segetalis were extracted with water twice to obtain a second extract; the first extract and the second extract were mixed and concentrated to a clear paste at a concentration temperature of 60° C. The relative density of the clear paste was 1.25, ethanol was added until the alcohol content reached 50%, and the mixture was allowed to stand for 24 hours, and filtered to obtain an alcohol precipitate;
[0079] (3) Take safflower and Corydalis yanhusuo, extract them twice with 8 times and 6 times the volume fraction of 60% ethanol, respectively, for 40 minutes each time, filter, and combine the alcohol extracts;
[0080] (4) combining the alcohol precipitate in step (2) and the alcohol extract in step (3), and concentrating the mixture at a temperature of 60° C. to obtain a Chinese medicine extract;
[0081] (5) Grind musk into fine powder and set aside;
[0082] (6) stirring and dissolving borneol in isopropyl myristate at a dissolving temperature of 60° C. to obtain a borneol solution;
[0083] (7) Slowly add borneol solution, volatile oil inclusion compound, musk powder, liquid paraffin, Tween 80 and Span 80 to the Chinese herbal medicine extract and stir evenly at 60°C.
[0084] Example 7 A Chinese medicine composition for treating breast hyperplasia 7#
[0085] (1) Weigh the following Chinese medicinal materials by weight: 25 parts of cloves, 15 parts of asarum, 15 parts of yanhusuo, 25 parts of safflower, 30 parts of fenugreek, 1.8 parts of musk, and 1.6 parts of borneol, each part is calculated as 15 g;
[0086] (2) Clove and Asarum were crushed, soaked with 6 times water, and extracted with water for 7 hours to obtain volatile oil, which was encapsulated with cyclodextrin and used as a first extract and a residue; Vaccaria segetalis was taken, and the residue and Vaccaria segetalis were extracted with water twice to obtain a second extract; the first extract and the second extract were mixed and concentrated to a clear paste at a concentration temperature of 90° C. The relative density of the clear paste was 1.30, ethanol was added until the alcohol content reached 70%, and the mixture was allowed to stand for 24 hours, and filtered to obtain an alcohol precipitate;
[0087] (3) Take safflower and Corydalis yanhusuo, extract them twice with 8 times and 6 times the volume fraction of 60% ethanol, respectively, for 40 minutes each time, filter, and combine the alcohol extracts;
[0088] (4) combining the alcohol precipitate in step (2) and the alcohol extract in step (3), and concentrating the mixture at a temperature of 90° C. to obtain a Chinese medicine extract;
[0089] (5) Grind musk into fine powder and set aside;
[0090] (6) stirring and dissolving borneol in isopropyl myristate at a dissolution temperature of 70° C. to obtain a borneol solution;
[0091] (7) Slowly add borneol solution, volatile oil inclusion compound, musk powder and Tween 80 to the Chinese herbal medicine extract and stir evenly at 70°C.
[0092] Example 8 A Chinese medicine composition for treating breast hyperplasia 8#
[0093] (1) Weigh the following Chinese medicinal materials by weight: 30 parts of cloves, 20 parts of asarum, 20 parts of yanhusuo, 30 parts of safflower, 30 parts of fenugreek, 2 parts of musk, and 1.8 parts of borneol, each part is calculated as 15 g;
[0094] (2) Clove and Asarum were crushed, soaked with 6 times water, and extracted with water for 6 hours to obtain volatile oil, which was encapsulated with cyclodextrin and used as a first extract and a residue; Vaccaria segetalis was taken, and the residue and Vaccaria segetalis were extracted with water twice to obtain a second extract; the first extract and the second extract were mixed and concentrated to a clear paste at a concentration temperature of 100° C. The relative density of the clear paste was 1.35, ethanol was added until the alcohol content reached 80%, the mixture was allowed to stand for 24 hours, and the alcohol precipitate was obtained by filtering;
[0095] (3) Take safflower and Corydalis yanhusuo, extract them twice with 8 times and 6 times the volume fraction of 60% ethanol, respectively, for 40 minutes each time, filter, and combine the alcohol extracts;
[0096] (4) combining the alcohol precipitate in step (2) and the alcohol extract in step (3), and concentrating the mixture at a temperature of 100° C. to obtain a Chinese medicine extract;
[0097] (5) Grind musk into fine powder and set aside;
[0098] (6) stirring and dissolving borneol in ethanol at a dissolution temperature of 80° C. to obtain a borneol solution;
[0099] (7) Slowly add borneol solution, volatile oil inclusion compound, musk powder and propylene glycol to the Chinese herbal medicine extract and stir evenly at 80°C.
[0100] Comparative Example 1 A Chinese medicine composition D1# for treating breast hyperplasia
[0101] The difference between Comparative Example 1 and Example 3 is that Comparative Example 1 includes 26 parts of cloves and does not include asarum, and the rest are the same.
[0102] Comparative Example 2 A Chinese medicine composition D2# for treating breast hyperplasia
[0103] The difference between Comparative Example 2 and Example 3 is that Asarum is not included, and the rest are the same.
[0104] Comparative Example 3 A Chinese medicine composition D3# for treating breast hyperplasia
[0105] The difference between Comparative Example 3 and Example 4 is that Comparative Example 3 includes 2 parts of borneol and does not include musk, and the rest are the same.
[0106] Comparative Example 4 A Chinese medicine composition D4# for treating breast hyperplasia
[0107] The difference between Comparative Example 4 and Example 4 is that Comparative Example 4 does not include musk, and the rest is the same.
[0108] Comparative Example 5 A Chinese medicine composition D5# for treating breast hyperplasia
[0109] The difference between Comparative Example 5 and Example 2 is that the extraction time of the volatile oil by water extraction in step (2) of Comparative Example 5 is 10 hours, and the rest are the same.
[0110] Experimental Example 1: Animal Model Experiment on Breast Hyperplasia
[0111] 1.1 Experimental Animals 151 SD rats (SPF grade), female (190-200 g)
[0112] 1.2 Drug testing
[0113] (1) According to the preparation methods of Examples 1 to 8 and Comparative Examples 1 to 4, Chinese medicine compositions 1# to 8# and Chinese medicine compositions D1# to D4# were prepared.
[0114] (2) Preparation of tamoxifen ointment: 1 g of tamoxifen, 48.6 g of polyethylene glycol-4000, 36.4 g of polyethylene glycol-400, and 14 ml of propylene glycol. Dissolve tamoxifen in propylene glycol by ultrasonication, melt polyethylene glycol 4000 by heating, mix with polyethylene glycol 400, stir and add to the propylene glycol solution, stir until cool, and obtain the ointment.
[0115] 1.3 Model establishment and drug administration 151 female SD rats were naturally fed for 7 days to adapt to the environment, and the third pair of breasts were depilated for the experiment. Ten rats were randomly selected as the normal group, and the remaining rats were used to replicate the breast hyperplasia model according to the method of estradiol benzoate combined with progesterone. Reference [Miao Mingsan, Wen Yajuan, Bai Ming, et al. Preparation of animal model of breast hyperplasia (draft) [J]. Chinese Journal of Experimental Traditional Chinese Medicine, 2017 (24): 17-22.], that is, firstly, 0.5 mg / (kg / d) of estradiol benzoate was injected intramuscularly into the hind limbs for 25 consecutive days, and then 4 mg / (kg / d) of progesterone was injected intraperitoneally for 5 consecutive days. After the modeling, the mice showed poor spirits, dull hair, and decreased appetite. One rat was randomly selected to remove the mammary gland, observe the pathological morphology, and determine whether the model was established. The rats after modeling were randomly divided into 14 groups, 10 rats in each group, namely, tamoxifen ointment group, model group, experimental group: Example 1, Example 2, Example 3, Example 4, Example 5, Example 6, Example 7, Example 8, Comparative Example 1, Comparative Example 2, Comparative Example 3, Comparative Example 4. The tamoxifen ointment group was smeared with 0.1 g of tamoxifen ointment on the mammary gland of the rats, and each experimental group was smeared with 0.1 g of the Chinese medicine composition on the mammary gland of the rats, once a day, and the model group and the normal group were not intervened for 20 consecutive days.
[0116] 1.4 Measurement of rat nipple diameter and height The diameter and height of the third pair of rat nipples were measured using a vernier caliper.
[0117] 1.5 Measurement of E2 and P content 48 hours after the last administration, 10 mL of blood was collected from the apex of the rats and centrifuged at 3000 r / min for 30 minutes. The supernatant was placed at 4°C for 2 hours for later use. The levels of E2 and P in the serum of rats in each group were detected according to the detection methods in the instructions of the E2 kit and the P kit.
[0118] 1.6 Statistical methods were performed using SPSS26 software, and measurement data were expressed as mean ± standard deviation. The variance analysis was performed between the groups, with P = 0.05 as the test level.
[0119] 1.7 The nipple diameter and height of rats in each group were compared with those in the normal control group. The nipple diameter and height of rats in the model group were increased compared with those in the normal group (P < 0.05), indicating that the modeling was successful and the mammary glands in the model group were significantly swollen. Compared with the model group, the nipple diameter and height of rats in each experimental group decreased. There were significant differences among the tamoxifen ointment group, Example 1, Example 2, Example 3, Example 4, Example 5, Example 6, Example 7, and Example 8 (P < 0.05), and the nipple diameter and height of rats in Example 4 decreased most significantly. The results are shown in Table 1.
[0120] Table 1 Comparison of nipple diameter and height measurement results of rats in each group with those of the normal control group: **P<0.05 compared with the model group: ## P<0.05
[0121]
[0122] 1.8 Effect on E2 and P Contents According to the detection method in the kit instructions, it was found that compared with the normal control group, the E2 content of the rats in the model group was significantly increased, while the P content was significantly decreased (P < 0.05), indicating that the model was successful; compared with the model group, the E2 content in the serum of the rats in each experimental group was significantly decreased, while the P content was significantly increased. The differences among the tamoxifen ointment group, Example 1, Example 2, Example 3, Example 4, Example 5, Example 6, Example 7, and Example 8 were statistically significant (P < 0.05), indicating that the Chinese medicine composition may treat rats with breast hyperplasia by regulating the levels of E2 and P in serum, and the E2 content of the Chinese medicine composition Example 4 group decreased most significantly, and the P content increased most significantly. The results are shown in Table 2.
[0123] Table 2 Effect of Chinese medicine composition on E2 and P content in rats compared with the normal control group: ** P<0.05 compared with the model group: ## P<0.05
[0124]
[0125] Experimental Example 2: One-time skin irritation test
[0126] 2.1 Experimental Animals 40 rabbits, ordinary grade, weighing 2-3 kg, half male and half female
[0127] 2.2 Experimental Sample Chinese Medicine Compositions According to the preparation methods of Examples 1 to 8 and Comparative Example 5, Chinese medicine compositions 1# to 8# and Chinese medicine composition D5# were prepared.
[0128] 2.3 Experimental method The left and right sides of the same body were compared by self-comparison method. According to the literature [Zheng Yangbin, Liu Ning, Ai Liqi, et al. Evaluation of skin irritation and allergic reaction of commercial anti-inflammatory analgesic ointment [J]. Drug Evaluation, 2021, 18 (7): 3], rabbits were divided into 10 groups [Example 1, Example 2, Example 3, Example 4, Example 5, Example 6, Example 7, Example 8, Comparative Example 5, Negative Control Group], 4 rabbits in each group, and the negative control was absorbent gauze. Before the test, the hair on both sides of the dorsal spine of the test animal was cut off, and the hair removal range was 3cm × 3cm respectively. Gauze of 2.5cm × 2.5cm was taken; about 0.5g of the test substance was added to a 2.5cm × 2.5cm absorbent gauze block. The patch was fixed with a bandage for 0.5h / day, and the other side was used with absorbent gauze as a control for 28 consecutive days. Observe with naked eyes at 1, 24, 48 and 72 hours after the last administration, and record the presence of erythema and edema at the administration site. Calculate the average score of the skin reaction score of each group of test substances and excipients at each observation time point according to Table 3. The average skin irritation test reaction value = (total score of erythema and eschar formation + total score of edema formation) / number of animals in each group. Subtract the average score of the skin reaction score of the excipient from the average score of the skin reaction score of the test substance to obtain the primary irritation index.
[0129] Evaluation of irritation intensity: a score of <0.5 is no irritation, 0.5≤score<3 is mild irritation, 3≤score<6 is moderate irritation, and 6≤score≤8 is strong irritation.
[0130] Table 3 Skin irritation reaction scores
[0131]
[0132] 2.4 Experimental Results The Chinese medicine composition Examples 1, 3-6, and 8 were non-irritating, Examples 2 and 7 were mildly irritating after 72 hours, and Comparative Example 5 began to be mildly irritating after 24 hours and was moderately irritating after 72 hours. The irritation reaction scores are shown in Table 4.
[0133] Table 4 Skin irritation reaction scores of Chinese medicine compositions
[0134]
[0135] The above is only the embodiment of the present application, and the protection scope of the present application is not limited by these specific embodiments, but is determined by the claims of the present application. For those skilled in the art, the present application can have various changes and variations. Any modification, equivalent replacement, improvement, etc. made within the technical ideas and principles of the present application should be included in the protection scope of the present application.
Claims
1. A Chinese medicine composition for treating breast hyperplasia, characterized in that: Calculated by weight, the composition includes: 10-30 parts of cloves, 5-20 parts of asarum, 5-20 parts of Corydalis yanhusuo, 10-30 parts of safflower, 10-30 parts of fenugreek, 0.1-2 parts of musk and 0.2-1.8 parts of borneol.
2. The Chinese medicine composition according to claim 1, characterized in that: Calculated by weight, the composition includes: 15-25 parts of cloves, 6-15 parts of asarum, 6-15 parts of Corydalis yanhusuo, 13-25 parts of safflower, 15-30 parts of fenugreek, 0.2-1.8 parts of musk and 0.3-1.6 parts of borneol.
3. The Chinese medicine composition according to claim 1, characterized in that According to weight parts, it includes: 18 parts of cloves, 8 parts of asarum, 8 parts of yanhusuo, 15 parts of safflower, 18 parts of fenugreek, 0.5 parts of musk and 0.5 parts of borneol; Or, 20 parts of cloves, 10 parts of asarum, 10 parts of Corydalis yanhusuo, 20 parts of safflower, 20 parts of fenugreek, 1 part of musk and 1 part of borneol; Or, 22 parts of cloves, 8 parts of asarum, 12 parts of Corydalis yanhusuo, 18 parts of safflower, 24 parts of fenugreek, 1.4 parts of musk and 1.2 parts of borneol; Or, 24 parts of cloves, 13 parts of asarum, 14 parts of Corydalis yanhusuo, 25 parts of safflower, 28 parts of fenugreek, 1.6 parts of musk and 1.5 parts of borneol.
4. A method for preparing a Chinese medicine composition for treating breast hyperplasia according to any one of claims 1 to 3, characterized in that: The following steps are involved: (1) Weighing Chinese medicinal materials according to weight; (2) Clove and asarum are crushed, soaked in water, extracted with water to obtain volatile oil, and then encapsulated with cyclodextrin to obtain a volatile oil inclusion compound for later use; the first extract and the residue are reserved; Vaccaria segetalis is taken, and the residue and Vaccaria segetalis are extracted with water to obtain a second extract; the first extract and the second extract are mixed and concentrated to a clear paste, ethanol is added, allowed to stand, and filtered to obtain an alcohol precipitate; (3) extracting safflower and corydalis with ethanol respectively, filtering and combining the ethanol extracts; (4) combining the alcohol precipitate in step (2) and the alcohol extract in step (3), and concentrating them to obtain a Chinese medicine extract; (5) Grind musk into fine powder and set aside; (6) stirring and dissolving borneol in a solvent to obtain a borneol solution; (7) Slowly add borneol solution, volatile oil inclusion compound, musk powder and auxiliary materials to the Chinese herbal medicine extract and stir evenly.
5. The preparation method according to claim 4, characterized in that: The extraction time of the volatile oil by water extraction in step (2) does not exceed 8 hours.
6. The preparation method according to claim 5, characterized in that: The extraction time of the volatile oil by water extraction in step (2) is 2 to 8 hours.
7. The preparation method according to claim 4, characterized in that: The solvent in step (6) includes ethanol, propylene glycol or isopropyl myristate; The auxiliary materials in step (7) are auxiliary materials that assist the components in being mixed and dispersed uniformly, and include: one or more of propylene glycol, glycerol, liquid paraffin, Tween 80 or Span 80.
8. The preparation method according to claim 4, characterized in that: The relative density of the clear paste in step (2) is 1.05-1.35; In step (2), ethanol is added until the alcohol content reaches 50% to 80%; The dissolution temperature of borneol in step (6) is 40 to 80° C.; The stirring temperature in step (7) is 40 to 80° C.; The concentration temperature in step (2) and step (4) is 50 to 100°C.
9. A Chinese medicine composition for external use for treating breast hyperplasia, characterized in that: The traditional Chinese medicine composition external preparation contains the traditional Chinese medicine composition according to any one of claims 1 to 3.
10. The external preparation of Chinese medicine composition according to claim 9, characterized in that: The external preparation of the traditional Chinese medicine composition includes ointment, liniment, cream, paint, gel, film coating, gel patch or lotion.