阅读说明：本技术 治疗痛风及降低尿酸的药物 (Medicine for treating gout and reducing uric acid ) 是由 温先敏 于 2021-03-23 设计创作，主要内容包括：本发明属中药技术领域。本发明所述的治疗痛风及降低尿酸的药物是由木贼提取物和适量的药用辅料制成的药物制剂。所述的提取物为所述木贼通过浸提、加热回流或超临界萃取所获得的提取物,提取物所使用溶剂为60％以上浓度的乙醇或者是丙酮、乙醚、石油醚、氯仿、乙酸乙酯单独或以任何比例相混溶的液体,或者是液态CO-2。本发明的药物制剂包括各种口服、注射、腔道、经皮等不同的给药途径。本发明是以木贼作为单一有效成分,辅以药用辅料制成治疗痛风、降低血尿酸的天然药物。本发明所制成的药物制剂无明显毒副作用及不良反应,为痛风治疗及降低血尿酸提供了安全、快速、有效的药物新产品。其作用优于别嘌醇等常用降尿酸药物,且不良反应少。(The present invention belongs to the field of Chinese medicine technology. The medicament for treating gout and reducing uric acid is a medicinal preparation prepared from equisetum hiemale extract and a proper amount of medicinal auxiliary materials. The extract is obtained by leaching, heating reflux or supercritical extraction of herba Equiseti hiemalis, and the solvent used in the extract is ethanol with concentration of above 60%, or acetone, diethyl ether, petroleum ether, chloroform, ethyl acetate, or liquid CO 2 . The pharmaceutical preparation of the invention comprises various administration routes of oral administration, injection, cavity, transdermal administration and the like. The invention relates to a natural medicine for treating gout and reducing blood uric acid, which is prepared by taking a horsetail as a single effective component and adding a pharmaceutical adjuvant. The medicinal preparation prepared by the invention has no obvious toxic or side effect and adverse reaction, and provides a safe, quick and effective novel medicinal product for treating gout and reducing blood uric acid. The effect is superior to that of common uric acid lowering drugs such as allopurinol and the like, andhas less adverse reaction.)

1. A medicament for treating gout and reducing uric acid is characterized in that the medicament is a medicinal preparation prepared from equisetum hiemale extract and a proper amount of medicinal auxiliary materials.

2. The medicament for treating gout and lowering uric acid as claimed in claim 1, wherein the horsetail is an overground dried part of Equisetum hiemali L; the extract is obtained by leaching, heating reflux or supercritical extraction of herba Equiseti hiemalis, and the solvent used in the extract is ethanol with concentration of above 60%, or acetone, diethyl ether, petroleum ether, chloroform, ethyl acetate, or liquid CO₂。

3. The drug for treating gout and reducing uric acid as claimed in claim 1, wherein the drug preparation is a capsule, a tablet, a capsule, a pill, a mixture, an external liniment, a spray, an injection prepared from the extract raw material and corresponding pharmaceutical excipients by a conventional process.

Technical Field

The present invention belongs to the field of Chinese medicine technology. In particular to a natural medicine for treating gout and reducing uric acid.

Technical Field

Gout is crystal-related arthralgia caused by deposition of mono-sodiuurate (MSU), is directly related to purine metabolic disorder and/or hyperuricemia caused by reduction of uric acid excretion, and belongs to the category of metabolic rheumatalgia. Hyperuricemia is the basis of gout, and the influencing factors causing the hyperuricemia comprise: genetics, high purine diet, obesity, hyperlipidemia, hypertension, diabetes, alcoholism, etc. When the blood uric acid level exceeds the joint mono-natriuretic urate saturation, urate crystals are precipitated and deposited on peripheral joints and peripheral tissues, and severe patients have joint destruction and serious complications of renal function injury.

With the improvement of living standard, gout and hyperuricemia (OHOA) become common frequently-occurring diseases in modern times, and the incidence rate in Europe and America is 1-4%. The disease rate of China is 1-3%, and the disease rate is on the trend of rising year by year, and gout becomes one of the common frequently encountered diseases affecting human health.

The existing medicines for treating gout mainly comprise two types: 1. the medicine for treating pain and inflammatory reaction during gout attack, and the main treating medicine during gout attack is colchicine, indometacin and other non-steroidal anti-inflammatory medicines, glucocorticoid and the like. 2. The medicine for reducing uric acid comprises febuxostat for inhibiting uric acid generation, allopurinol, benzbromarone for promoting uric acid excretion and the like. The medicines have toxic and side effects and adverse reactions of different degrees, such as severe gastrointestinal reaction, liver and kidney function damage, bone marrow suppression, rash and the like. Therefore, the search and development of safe and effective gout treatment/uric acid reduction medicines from natural plant medicines and traditional Chinese medicines has great social and economic values and significance.

Chinese patent application No. 201911152871.4 discloses a Zhuang nationality medicine preparation for preventing and treating hyperuricemia, which is prepared from the following raw materials in parts by weight: 10-20 parts of selaginella doederleinii, 5-15 parts of berchemia lineate, 5-15 parts of small-leaf golden flower, 20-40 parts of horsetail, 20-40 parts of lalang grass rhizome, 10-20 parts of desmodium styracifolium, 10-20 parts of motherwort, 5-15 parts of glabrous greenbrier rhizome, 5-15 parts of sappan wood, 5-15 parts of desmodium triquetrum, 5-15 parts of Japanese ardisia herb and 2-10 parts of liquorice. The Zhuang medicine preparation improves the current clinical treatment dilemma of hyperuricemia, has the treatment effects of clearing heat, promoting urination, reducing blood uric acid, protecting the kidney and the like, can obviously improve the glomerular filtration rate and promote the excretion of uric acid, and has obvious curative effect advantage and relatively low price.

Chinese patent application No. 201611211559.4 discloses a Chinese medicament for treating hyperuricemia, which comprises the following Chinese medicinal raw materials in part by weight: 9-15 parts of tea, 15-30 parts of plantain herb, 30-60 parts of cortex acanthopanacis, 6-60 parts of radix hemerocallis, 9-15 parts of filliform cassytha herb, 15-30 parts of common scouring rush herb and 15-60 parts of lygodium japonicum. The invention has the functions of promoting urination and removing acid, improving enzymes, reducing the production of endogenous uric acid to effectively prevent and reduce hyperuricemia and improve the sub-health state of the people, has good clinical practice effect, is non-toxic and safe, and is convenient for frequent health care application.

The two patent applications are both a prescription compatible with traditional Chinese medicines with the functions of clearing heat and promoting urination, and the medicine is prepared by extracting active ingredients with high-polarity solvents such as water or acid. The two patent applications are compound compositions, the effective components of which are unclear, but the effective components are water-soluble components for preventing and treating hyperuricemia.

The main functions of the horsetail in the formula are clearing heat, and relieving pain and diminishing inflammation. The water/acid extraction product is mainly acid substances, such as ferulic acid, caffeic acid and the like, wherein the ferulic acid has the functions of easing pain, resisting platelet aggregation, resisting thrombus and the like, and the caffeic acid has the antibacterial function.

Disclosure of Invention

The invention aims to provide a medicament for treating gout and reducing uric acid by taking a equisetum hiemale extract as a single effective component.

The medicament for treating gout and reducing uric acid is a medicinal preparation prepared from equisetum hiemale extract and a proper amount of medicinal auxiliary materials.

The horsetail of the present invention is the above-ground dried part of Equisetum hiemali l. The extract is obtained by leaching, heating reflux or supercritical extraction of herba Equiseti hiemalis, and the solvent used in the extract is ethanol with concentration of above 60%, or acetone, diethyl ether, petroleum ether, chloroform, ethyl acetate, or liquid CO₂。

The horsetail extract mainly refers to fat-soluble extract and volatile oil of horsetail, and the components of the horsetail extract include but are not limited to ethyl palmitate, glutaric acid formic acid, 2 methoxy 3-1 methyl ethyl) pyrazine, pentadecane, 9 octyl heptadecane and the like. Can be used for treating gout and reducing uric acid.

The medicinal preparation comprises various medicinal preparations with different administration routes of oral administration, injection, cavity, percutaneous administration and the like, and can be capsules, tablets, capsules, pills, mixtures, external liniments, sprays, injections and the like which are prepared from the extract raw materials and corresponding medicinal auxiliary materials according to a conventional process.

The Equisetum hiemali L is a dried overground part of Equisetum hiemali of family equisetaceae, and the Chinese pharmacopoeia 2020 edition records the functional main treatment as follows: dispel wind-heat and remove nebula, it is indicated for blood-shot eyes due to wind-heat, lacrimation in the wind, nebula produced by eyes. All the generations of herbal medicine take herba Equiseti hiemalis as the essential herb of the ophthalmology, which is mainly used for treating eye diseases and nebula, and also has the functions of expelling pathogenic factors from muscles, arresting bleeding, benefiting liver and kidney, removing rheumatism, treating intestinal wind, stopping dysentery, etc.

The extracted components of lipids, volatile oil and the like in the horsetail medicinal material with low solubility in water have the effect of reducing uric acid. The components have low solubility in water, and can be extracted by extraction with medium or low polar organic solvent such as high concentration ethanol, n-butanol, chloroform, acetone, ethyl acetate, diethyl ether, petroleum ether, etc., heating reflux, supercritical extraction, etc.

The leaching, heating reflux and supercritical extraction are all the prior art.

The invention provides a novel application of horsetail and an extract, and the horsetail is used as a single effective component and is supplemented with pharmaceutical excipients to prepare a natural medicine for treating gout and reducing blood uric acid. The medicinal preparation prepared by the invention has no obvious toxic or side effect and adverse reaction after toxicity experiments and clinical application, and provides a safe, quick and effective novel medicinal product for treating gout and reducing blood uric acid. The effect of the medicine is superior to that of common uric acid lowering medicines such as allopurinol and the like, and the adverse reaction is less.

The invention relates to a drug safety test.

First, acute toxicity test

1. Materials and methods

1.1.1 animals: 30 Kunming seeds, weight 17.6-22.3g, female and male half.

1.1.2 tested medicine and its preparation, the equisetum hiemale capsule of example 1, offered by famous pharmaceutical industry limited of Yunnan, the specification is 0.5 g/grain, take 40 capsules, remove the shell, add 2% carboxymethyl cellulose sodium and add water to make into viscous pasty suspension, the final concentration is 38%, the highest concentration of the tested medicine.

1.2 test methods

According to the research guidelines of new traditional Chinese medicines, 40g/kg of the tested medicine (the maximum concentration and the maximum volume of the suspension) is pre-tested in a laboratory at the room temperature of 20 ℃, the toxic reaction and death condition of the mice are observed for one week, and the LD50 value cannot be measured, so the maximum tolerance test is selected.

Selecting 20 healthy qualified clean-grade Kunming mice with half each male and female, performing intragastric administration on the test drug suspension for 3 times in 24H, wherein the administration volume is 0.2ML/10g of body weight, then freely drinking water and foraging, observing for one week, and recording the situations of diet, body weight, body position, respiratory turning over and reflecting and the like of the mice.

1.3 test results.

None of the mice died within 1 week of the gastric lavage of the test drug suspension, and there was no abnormal change in food intake and water intake, and the results are shown in table 1.

TABLE 1 mice drench horsetail capsule and result (x + -s)

Within 7 days of observation, mice taking the medicine have no death and obvious abnormal phenomena, and each animal is planed through a cervical vertebra dislocation part and is compared with normal mice: under the condition of naked sleep, no abnormal condition is found in heart, liver, spleen, lung, kidney and brain.

The conclusion of the test is as follows: the maximum concentration and the maximum volume of the tested drug of the mouse gavage horsetail are 21.6g/kg of body weight, which are 288 times of the dosage of the drug taken by a human body, and no toxic reaction is seen.

Second, observation of gout clinical case by using equisetum capsules

1. Data and method

1.1 diagnostic criteria

1.1.1 the diagnostic criteria established by the American society for rheumatism are used.

Acute arthritis occurs more than 1 time, and the peak of the attack is reached within 1 day.

② acute arthritis is limited to individual joints.

And the whole joint is dark red.

And fourthly, swelling and pain of the first toe joint.

Acute attack of unilateral toe arthritis.

Sixthly, there is tophus.

And hyperuricemia.

And eighty percent of asymmetric arthritis.

And ninthly, the attack can be automatically stopped.

More than three of them can be used for accurate diagnosis.

1.1.2 hyperuricemia gout patients who met the diagnosis standard 90, 25-68 years old, 56 men, 34 women, randomly divided into 3 groups, and placebo (0.5 g/capsule starch) was given 2 capsules/time and 3 capsules/day for the placebo group. Control group: allopurinol was administered at 100 mg/time, 300 mg/day. Treatment groups: the horsetail capsule of example 1 was administered 2 capsules/time, 3 capsules/day. Uric acid and symptom improvement of the patients after 20 days were observed and statistically analyzed.

1.1.3 uric acid lowering test results

TABLE 2 comparison of blood uric acid before and after treatment

P < 0.05 compared to control; in comparison with the set of models,^▲P＜0.01。

the test result shows that the fat-soluble extract of the equisetum hiemale has the function of reducing the uric acid, has quick action and no obvious adverse reaction, and has better prospect for developing new drugs.

1.1.4 improvement of gout symptoms in patients

TABLE 3 improvement of gout symptoms before and after treatment

Note: the symptoms of the patient such as arthralgia, red swelling and the like and the joint movement are not obviously improved to be ineffective; the patient is effective in substantially eliminating or eliminating symptoms such as arthralgia, redness and swelling, etc., and effective in slightly limiting or not limiting joint movement.

The experimental results show that the equisetum hiemale extract can effectively improve symptoms of arthralgia, red swelling and the like of gout patients, eliminates the condition of limited joint movement of the patients, and has a pharmacological effect of treating gout.

Detailed Description

The present invention is illustrated and described in detail by the following examples, which include but are not limited to these examples.

The medicament for treating gout and reducing uric acid is a medicinal preparation prepared from equisetum hiemale extract and a proper amount of medicinal auxiliary materials. As the invention adopts single active ingredients, the active ingredients and the pharmaceutic adjuvant can be in conventional proportion.

Example 1: equisetum capsules

The formula is as follows: 1000 parts of horsetail and 100 parts of starch.

The preparation method comprises the following steps: crushing 1000 parts of equisetum hiemale into coarse powder, performing hot reflux extraction twice with 60% ethanol, extracting for 3 hours with 3 times of 60% ethanol solvent for the first time, extracting for 1 hour with 2 times of 60% ethanol solvent for the second time, combining the extracting solutions, recovering ethanol, and concentrating into thick paste for later use. Drying at 55-65 deg.C, pulverizing into fine powder, mixing with 100 parts of starch, and encapsulating.

Example 2: equisetum injection

The formula is as follows: 1000 parts of equisetum, 10ML benzyl alcohol and 8 parts of sodium chloride

The preparation method comprises the following steps: pulverizing 1000 parts of herba Equiseti hiemalis into coarse powder, leaching with acetone at room temperature for 2 times, the first time for 48 hr, the second time for 40 hr, mixing the leaching solutions, recovering acetone, concentrating to obtain soft extract, adding benzyl alcohol and sodium chloride, stirring for dissolving, adding water for injection to 1000ML, filtering with G4 remelting glass funnel, packaging in 2ML Ampere bottle, and sterilizing at 100 deg.C for 30 min.

Example 3: equisetum particles

The formula is as follows: 1000 parts of horsetail, 100 parts of starch, 10 parts of dextrin and 20 parts of lactose.

The preparation method comprises the following steps: extracting herba Equiseti hiemalis 1000 parts with petroleum ether and diethyl ether mixture (3:1) at room temperature for 2 times, 40 hr for the first time and 35 hr for the second time, mixing the extractive solutions, recovering organic solvent, concentrating to obtain soft extract, mixing with starch, dextrin and lactose, granulating, and drying at 60-70 deg.C.