WO2015018128A1 - 一种降血糖的中药制剂及其制备方法 - Google Patents

一种降血糖的中药制剂及其制备方法 Download PDF

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WO2015018128A1
WO2015018128A1 PCT/CN2013/085131 CN2013085131W WO2015018128A1 WO 2015018128 A1 WO2015018128 A1 WO 2015018128A1 CN 2013085131 W CN2013085131 W CN 2013085131W WO 2015018128 A1 WO2015018128 A1 WO 2015018128A1
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preparation
chinese medicine
ginseng
epimedium
wild chrysanthemum
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French (fr)
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袁志贤
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Yuan Zhixian
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/56Materials from animals other than mammals
    • A61K35/62Leeches; Worms, e.g. cestodes, tapeworms, nematodes, roundworms, earth worms, ascarids, filarias, hookworms, trichinella or taenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/23Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A61K36/236Ligusticum (licorice-root)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/25Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax
    • A61K36/258Panax (ginseng)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/28Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/28Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A61K36/287Chrysanthemum, e.g. daisy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/29Berberidaceae (Barberry family), e.g. barberry, cohosh or mayapple
    • A61K36/296Epimedium
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/42Cucurbitaceae (Cucumber family)
    • A61K36/428Trichosanthes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/48Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/488Pueraria (kudzu)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/53Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/539Scutellaria (skullcap)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/81Solanaceae (Potato family), e.g. tobacco, nightshade, tomato, belladonna, capsicum or jimsonweed
    • A61K36/815Lycium (desert-thorn)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/85Verbenaceae (Verbena family)
    • A61K36/855Clerodendrum, e.g. glorybower
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/896Liliaceae (Lily family), e.g. daylily, plantain lily, Hyacinth or narcissus
    • A61K36/8964Anemarrhena
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/896Liliaceae (Lily family), e.g. daylily, plantain lily, Hyacinth or narcissus
    • A61K36/8969Polygonatum (Solomon's seal)
    • AHUMAN NECESSITIES
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    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/898Orchidaceae (Orchid family)
    • A61K36/8988Gastrodia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/899Poaceae or Gramineae (Grass family), e.g. bamboo, corn or sugar cane
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine

Definitions

  • the invention relates to a traditional Chinese medicine preparation for lowering blood sugar, in particular to a formula and a preparation method of the traditional Chinese medicine preparation relating to the blood sugar lowering effect. Background technique
  • the sugar in human blood is called blood sugar. In most cases, it is glucose. Sugar is one of the essential nutrients of the human body. Most of the energy of cells in the human body comes from glucose. People eat cereals, vegetables, etc. After the digestive system is converted into glucose into the blood and transported to the whole body as a source of energy, blood sugar must be maintained at a certain level to maintain the needs of various organs and tissues. Normal people have a fasting blood glucose concentration of 4. 1-6. Ommol/L, and a fasting blood glucose concentration of more than 6. 0 mmol/L is called hyperglycemia. At this time, a part of glucose is excreted in the urine, which is diabetes.
  • Diabetes is a disease that is difficult to cure. Patients need long-term medication and diet control.
  • the common manifestations of diabetes are polyuria, polydipsia, and more food.
  • weight loss and other performance that is, "three more than one less" symptoms, and diabetes is very likely to cause cardiovascular disease, kidney disease, neuropathy and other complications.
  • hypoglycemic drugs only a few drugs such as insulin, and only effective in injection, there is no drug that can completely cure diabetes, and more drugs that lower blood sugar, but also regulate blood sugar, Moreover, these drugs have certain limitations and adverse reactions, which may lead to side effects such as hypoglycemia and lactic acidosis. Therefore, it is imperative to find a safe, effective and no side effects of hypoglycemic drugs.
  • the object of the present invention is to provide a traditional Chinese medicine preparation for preventing and reducing hyperglycemia according to the above-mentioned deficiencies, based on the secret recipe of the ancestors, and in combination with modern Chinese and Western medicine technology, in particular to provide a formula and a preparation method for the preparation of the traditional Chinese medicine.
  • the invention has obvious hypoglycemic effect, is non-toxic, has no side effects, and has stable effects, and the preparation process is simple and easy.
  • the preparation of the invention is composed of pure water, puerarin, wild chrysanthemum, mulberry parasitic, corn mustard, smallpox, scutellaria, yinyanghu, stagnation sylvestris, scutellaria, earthworm, gastrodia elata, medlar, chuanxiong, zhimu, sinensis, a liquid preparation of a composition prepared from ginseng, brown sugar and 65% ethanol solution, wherein the mass ratio of each component is
  • the preferred raw material quality ratio of the present invention is
  • Mulberry parasitic 25g corn must 25g small pollen 20g
  • the preparation method of the above hypoglycemic traditional Chinese medicine preparation comprises the following steps:
  • the powder mixture of pueraria, wild chrysanthemum, mulberry parasitic, corn mustard, trichosanthin, scutellaria, sylvestris, sylvestris sylvestris is added to pure water for three times, the first time added 10 times the amount of water to cook half Hours, add 5 times the amount of water for 20 minutes, add 5 times the amount of water for 10 minutes, then combine the decoction and filter, set aside; 3), the yellow essence, earthworm, gastrodia elata, medlar, Chuanxiong, Zhimu, Rotary flower, ginseng proportioned well, crushed by a pulverizer and passed through a 80 mesh sieve, and then baked at a high temperature of 50-70 ° C Dry, then naturally dry to room temperature for use;
  • step 5 at room temperature, the above step 2) and the decoction obtained in step 4), and added 65% ethanol solution and stirred evenly, forming a Chinese medicine composition solution preparation;
  • the prepared Chinese medicine composition solution preparation can be used for oral administration, and if it can be consumed once in the morning and evening and long-term drinking, the effect is better.
  • the theoretical basis of the present invention is: Pueraria, a legume plant kudzu, is a common vegetable in some provinces and autonomous regions of southern China, and its taste is sweet and delicious, and is often used as a soup. Its main component is starch, and it also contains about 12% of flavonoids, including soybean (soybean) glutinous rice, soybean aglycone, puerarin and other 10 kinds; and contains carrots, amino acids, coumarins and the like.
  • Pueraria is cool, sweet and pungent. It is a commonly used hurricane solution.
  • Pueraria has a blocking effect on ⁇ receptor and angiotensin II receptor, and its curative effect is superior to previous antihyperglycemic drugs.
  • Puerarin can significantly increase the level of plasma endothelin ( ⁇ ) to return to normal, so puerarin treatment of hyperglycemia
  • One of the mechanisms may be to inhibit the excessive release of ET, promote the endothelial recovery function, and then stimulate the activity of PG12 synthase, significantly increase the production of PG by EC to inhibit platelet aggregation and improve blood circulation. Large doses of puerarin can lower blood sugar and significantly lower serum cholesterol.
  • Wild chrysanthemum the head of the perennial herb of the Compositae, is similar to chrysanthemum. It is wild on the hillside grassland and on the side of the road. Wild chrysanthemum can be widely used for detoxification, treatment of acne swelling, sore throat, red eyes, headache and dizziness. At the same time, it has a good hypoglycemic effect and can be used for adjuvant treatment of hyperglycemia.
  • the single-flavored decoction has a general effect, but it is very effective in combination with other traditional Chinese medicines of the present invention.
  • Mulberry parasitic, bitter taste; sweet; sex, into the liver, kidney can be rheumatism, liver and kidney, nourishing blood, and is mainly used for sputum, blood, nourishment, liver and kidney deficiency caused by weak bones, waist Knee acid soft embolism, also commonly used in the treatment of liver and kidney yin deficiency type hyperglycemia.
  • Corn, corn must be the style and stigma of the gramineous plant, also known as jade, mustard, sweet, flat, stomach, gallbladder, kidney, diuretic, swelling, heat, blood pressure and blood sugar .
  • Trichosanthin sweet and bitter, sour and sour, return to the lung and kidney, have the effect of thirst, benefit the stomach and reduce the fire and dryness.
  • Trichosanthin is often associated with Zhimu, Yam, Ophiopogon japonicus, Scorpion, and Astragalus, and treats yin deficiency type diabetes.
  • Astragalus can clear away heat and detoxification, purging fire and detoxification, its taste bitter cold, effect digestion and accumulation, blood circulation, clearing heat and detoxification, purging fire detoxification, dealing with liver heat and hyperglycemia, clearing dizziness, headache, mouth The effect of bitterness and upset. Whether it is decoction or infusion, it has obvious antihypertensive effect. It is compatible with wild chrysanthemum and medlar to treat neurohypoglycemia and arteriosclerosis and hyperglycemia, which can lower blood sugar, headache, chest tightness and impetuous symptoms. And disappeared.
  • Epimedium alias iron arrow, horn flower, long green grass, born in a damp ravine, hillside forest or bamboo clumps, warm, sweet and fragrant, tonifying kidney, strong bones, rheumatism.
  • soft bones, rheumatism numbness, numbness; menopausal hyperglycemia and other symptoms.
  • the stinky paulownia is also known as Haizhou Changshan, Taishan Red Five Star, Bubble Flower Tong, Star Aniseed Sycamore, Chasing Wind, Back Court Flower, etc. It is pungent, bitter, sweet, cool, into the liver, gallbladder, spleen.
  • Huang Jing also known as tiger ginger, chicken head ginseng. It is a dried rhizome of Liliaceae, such as Huangjing, Huangjing or Duohuahuang. The yellow essence is sweet and flat. Return to the lungs, spleen, kidney. It can nourish the kidneys and lungs. Earth dragon, cold, salty.
  • Gastrodia elata a perennial herb, is distributed in most parts of the country. Its dry tubers, also known as gastrodia elata, are commonly used and more expensive traditional Chinese medicines. They are clinically used for headache, dizziness, limb numbness, convulsions in children, epilepsy, convulsions, tetanus, etc., and can be used for liver and yang. Headache, dizziness and other symptoms.
  • Scorpion return to the liver; kidney; lung.
  • the scorpion is not greasy, and it has the functions of nourishing yin and tonifying the kidney, benefiting the eyesight, promoting thirst, yin and yang. It is compatible with Schisandra, Polygonatum and Yuanshen. It is suitable for those who are deficient in liver and kidney, and can improve the symptoms of diabetes.
  • Chuanxiong a kind of traditional Chinese medicine plant, is often used for promoting blood circulation, relieving pain and relieving pain. It is mainly cultivated in Sichuan, Yunnan, Guizhou, Guangxi, Hubei and other places.
  • Chuanxiong Xin Wenxiang dry go without keeping, can not only disperse, up to the dome; and into the blood, down to blood. It has a wide-ranging effect on blood stasis, which is suitable for blocking blood stasis and various diseases. It has good qi and pain, and it has good effect. It can cure head wind headache, rheumatism and pain.
  • Chuanxiong was a gas medicine in the blood, and it was said that it had functions such as disintegration, depression, accessibility, and pain relief. Zhimu, this product is the dry rhizome of the monocotyledonous lily family, the effect of clearing heat and purging fire, Shengjin Runzao.
  • Ginseng perennial herb, hi-smooth, humid climate, mostly grown in coniferous and broad-leaved mixed forests or mixed forests with low temperature difference between day and night, 500 ⁇ 1100 meters above sea level. Ginseng can promote the blood sugar lowering of experimental animals, and can reduce the increase of diabetes and blood lipids and weakness symptoms. Clinical reports of ginseng extract have a therapeutic effect on early mild diabetes, which reduces urine sugar and lowers blood glucose by 40 mg. After stopping the drug, the effect can still last for more than 2 weeks.
  • 65% ethanol solution contains alcohol.
  • Liquor is known as "the longest of 100 medicines".
  • the liquor is stable, safe and effective, and because alcohol is a good semi-polar organic solvent, the various active ingredients of traditional Chinese medicine are soluble. Among them, the medicine exerts its effectiveness by means of alcohol and alcohol to help the drug, and improves the therapeutic effect. Diabetes is caused by insufficient insulin secretion and hyperglycemia, and Western medicine currently has no particularly good treatment for diabetes. It is called incurable disease.
  • traditional Chinese medicines have very unique treatments for diabetes. For example, the combination of these drugs has a triple action, which is both a blood glucose inhibitor and an insulin sensitizer, and at the same time enhances insulin receptor function, and the effect is stable.
  • the preparation is safe and has no toxic side effects.
  • the oral liquid of the preparation of the present invention is taken 1 hour after the meal, 3 times a day, 300 ml each time, 1 month is a course of treatment, and two courses are observed as therapeutic effects.
  • the oral liquid of the preparation of the present invention is taken 1 hour after the meal, 3 times a day, 300 ml each time, 1 month is a course of treatment, and two courses are observed as therapeutic effects.
  • the beneficial effects of the present invention are as follows: the preparation prepared by the invention has obvious hypoglycemic effect, is non-toxic, has no side effects, is stable in effect, and has a simple and easy preparation process. Concrete implementation
  • the preparation of the invention is composed of pure water, puerarin, wild chrysanthemum, mulberry parasitic, corn mustard, smallpox, scutellaria, yinyanghu, stagnation sylvestris, scutellaria, earthworm, gastrodia elata, medlar, chuanxiong, zhimu, sinensis,
  • the preparation method of the above hypoglycemic traditional Chinese medicine preparation comprises the following steps:
  • the powder mixture of pueraria, wild chrysanthemum, mulberry parasitic, corn mustard, trichosanthin, scutellaria, sylvestris, sylvestris sylvestris is added to pure water for three times, the first time added 10 times the amount of water to cook half Hours, add 5 times the amount of water for 20 minutes, add 5 times the amount of water for 10 minutes, then combine the decoction and filter, set aside;
  • step 5 at room temperature, the decoction obtained in the above step 2) and step 4) is mixed, and added to a 65% ethanol solution and stirred uniformly to form a formulation of the traditional Chinese medicine composition solution; 6), adding the traditional Chinese medicine composition solution preparation in the above step 5) to brown sugar, and stirring
  • the preparation of the above-mentioned traditional Chinese medicine composition solution can be used for oral administration, and if it can be consumed once in the morning and evening and long-term drinking, the effect is better.
  • the preferred raw material quality of the present invention is (g):
  • the preparation method is as in Example 1.
  • the preferred raw material quality of the present invention is (g):
  • Mulberry parasitic 25g corn must 30g small pollen 25g
  • Rotary flower 25g brown sugar 25g 20 g of a 65% ethanol solution
  • the preparation method is as in Example 1.
  • the preferred raw material quality of the present invention is (g):
  • the preparation method is as in Example 1.
  • the preferred raw material quality of the present invention is (g):
  • the preferred raw material quality of the present invention is (g):
  • the preparation method is as in Example 1.
  • hypoglycemic preparation If the therapeutic effect of the hypoglycemic preparation is not affected, it will fall within the scope of the present invention.

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Abstract

一种降血糖中药制剂,是由纯净水、葛根、野菊花、桑寄生、玉米须、天花粉、黄苓、淫羊霍、臭梧桐、黄精、地龙、天麻、枸杞子、川芎、知母、旋复花、人参、红糖和65%乙醇溶液经粉碎、煎煮、混合、搅拌等工序制成的液态制剂。该制剂降血糖效果明显,无毒,无副作用,制作工艺简单。

Description

一种降血糖的中药制剂及其制备方法
技术领域
本发明涉及一种降血糖作用的中药制剂,具体的说是涉及这种降 血糖作用的中药制剂的配方及制备方法。 背景技术
人体血液中的糖分称为血糖, 绝大多数情况下都是葡萄糖, 糖分 是人体必不可少的营养之一,人体内各组织细胞活动的能量大部分来 自葡萄糖, 人们摄入的谷物、 蔬菜等, 经过消化系统转化为葡萄糖进 入血液内, 输送到全身的细胞, 作为能量的来源, 所以血糖必须保持 一定的水平才能维持各个器官和组织的需要。正常人在空腹血糖浓度 为 4. 1-6. Ommol/L, 空腹血糖浓度超过 6. 0 mmol/L称为高血糖, 这 时候会有一部分葡萄糖随着尿液排出, 这就是糖尿。
随着人们生活水平的逐步提高, 患有糖尿病的人越来越多, 糖尿 病是一种很难治愈的疾病, 患者需要长期服药和控制饮食, 糖尿病的 常见表现有多尿、 多饮、 多食、 消瘦等表现, 即 "三多一少"症状, 而且糖尿病极易引起心血管病变, 肾脏病变、 神经病变等并发症。
目前, 临床所用的降血糖的药物, 只有胰岛素等为数不多的几种 药物,而且只有注射才有效,还没有一种能够完全治愈糖尿病的药物, 多以降血糖的药物, 也只是调控血糖而已, 况且这些药物都存在一定 的局限性和不良反应, 可能导致低血糖症, 乳酸性酸中毒等副作用。 所以,寻找一种安全、有效、无副作用的降血糖药物,成为当务之急
本发明的目的即在于针对上述不足, 在祖传秘方的基础上, 结合 现代中西医技术, 提供一种预防和降低高血糖的中药制剂, 具体的说 是提供这种中药制剂的配方和制备方法, 本发明降血糖效果明显, 而 且无毒, 无副作用, 效果稳定, 制取工艺简便易行。
本发明的技术方案如下所述:
本发明制剂是由纯净水、 葛根、 野菊花、 桑寄生、 玉米须、 天花 粉、 黄苓、 淫羊霍、 臭梧桐、 黄精、 地龙、 天麻、 枸杞子、 川芎、 知 母、 旋复花、 人参、 红糖和 65%乙醇溶液制备成的组合物液态制剂, 其中各组分的质量配比为
纯净水 4000-8000g 葛根 10-30g 野菊花 20-40g 桑寄生 20-40g 玉米须 25-35g 天花粉 20-30g 黄苓 15-25g 淫羊藿 20-30g 臭梧桐 20-30g 黄精 20-30g 地龙 20-30g 天麻 30-40g 枸杞子 30-40g 川芎 20-30g 知母 20-30g 旋复花 20-35g 人参 10-20g 红糖 20-30g 65%乙醇溶液 30g。
为了获得更好的效果, 本发明可优选的原料质量配比为
纯净水 5000-8000g 葛根 10-20g 野菊花 20-30g 桑寄生 20-30g 玉米须 25-30g 天花粉 20-25g 黄苓 15-20g 淫羊藿 20-25g :梧桐 20-25g 黄精 20-25g 地龙 20-25g 天麻 30-35g 枸杞子 30-35g 川芎 20-25g 知母 20-25g 旋复花 20-30g 人参 10_20g 红糖 20-30g 当然, 为了获得进一步好的效果, 本发明还可优选的原料质量配 纯净水 6000g 葛根 15g 野菊花 25g
桑寄生 25g 玉米须 25g 天花粉 20g
黄芬 15g 淫羊藿 20g
Figure imgf000004_0001
黄精 25g 地龙 20g 天麻 30g
枸杞子 30g 川芎 20g 知母 20g
旋复花 25g 红糖 30g
65%乙醇溶液 20g。
上述降血糖中药制剂的制备方法, 包括如下步骤:
1 )、将葛根、野菊花、桑寄生、玉米须、天花粉、黄苓、淫羊霍、 臭梧桐按比例配好, 经过粉碎机粉碎并过 80目筛, 然后在 50— 70 °C 的高温下烘干, 然后自然晾到室温备用;
2 )、 将上述步骤中葛根、 野菊花、 桑寄生、 玉米须、 天花粉、 黄 苓、 淫羊霍、 臭梧桐的粉末混合物加入纯净水煎煮三次, 第一次加入 10倍量水煎煮半个小时, 第二次加入 5倍量水煎煮 20分钟, 第三次 加入 5倍量水煎煮 10分钟, 然后合并煎液并过滤, 备用; 3)、 将黄精、 地龙、 天麻、 枸杞子、 川芎、 知母、 旋复花、 人参 按比例配好, 经过粉碎机粉碎并过 80目筛, 然后在 50— 70°C的高温 下烘干, 然后自然晾到室温备用;
4)、 将上述黄精、 地龙、 天麻、 枸杞子、 川芎、 知母、 旋复花、 人参的粉末混合物加入 10倍量的纯净水煎煮半个小时, 然后取煎液 并过滤, 备用;
5)、 在室温状态下, 将上述步骤 2 ) 和步骤 4) 中获得的煎液混 合, 并加入 65%乙醇溶液并搅拌均匀, 形成中药组合物溶液制剂;
6)、 将上述步骤 5) 中的中药组合物溶液制剂加入红糖, 并搅拌 5分钟, 即可制得。
制取的上述中药组合物溶液制剂可以用于口服,如果能够早中晚 各饮用一次并长期饮用, 效果更好。 本发明的理论依据在于: 葛根, 为豆科植物野葛, 是中国南方一些省区的一种常食蔬菜, 其味甘凉可口, 常作煲汤之用。 其主要成分是淀粉, 此外还含有约 12%的黄酮类化合物, 包括大豆 (黄豆) 甙、 大豆甙元、 葛根素等 10 余种;并含有胡萝卜甙、氨基酸、香豆素类等。作为中药,葛根性凉, 味甘、 辛, 是常用的祛风解表药, 临床报道用于治疗高血糖伴有颈项 强痛者疗效显着。 最新资料表明, 葛根具有 α 受体和血管紧张素 II 受体亦有阻断作用, 疗效优于以往各类抗高血糖药物。葛根素可使明 显增高的血浆内皮素 (ΕΤ)水平较快恢复正常,故葛根素治疗高血糖病 的机制之一可能在于能抑制 ET过量释放, 促进内皮恢复功能, 进而 兴奋 PG12合成酶活性, 显著增高 EC生成 PG抑制血小板聚集, 起到 改善血液循环的作用。大剂量葛根素能降低血糖, 能明显降低血清胆 固醇。但是单用葛根来降血糖, 结果并不明显, 但是在本发明中和其 他中药配伍来治疗高血糖病, 降糖结果明显, 对高血糖引起的口渴、 恶心、 呕吐等症状有很好的效果。 野菊花, 为菊科多年生草本植物野菊的头状花序, 外形与菊花相 似, 野生于山坡草地、 田边路旁。 野菊花可广泛用于清热解毒, 治疗 疔疮痈肿、 咽喉肿痛、 风火赤眼、 头痛眩晕等病证。 同时又有很好的 降糖作用, 可用于高血糖病的辅助治疗。 单味煎服效果一般, 但是与 本发明其他中药为伍, 则效果非常突出。 桑寄生, 味苦; 甘; 性平, 入肝、 肾经, 可以祛风湿, 补肝肾, 养血安胎, 主要用于痹症血不养筋、 肝肾不足所引起的筋骨萎弱、 腰 膝酸软等症, 亦常用于肝肾阴虚型高血糖病的治疗。 玉米须,玉米须为禾本科植物玉蜀黍的花柱和柱头,又名玉麦须, 性味甘、 平, 归胃、 胆、 肾诸经, 有利尿、 消肿、 清热、 降压降糖之 功效。 主治糖尿病口渴、 多尿者。 天花粉, 性味甘苦酸凉, 归肺肾经, 有生津止渴、 益胃降火润燥 等功效。 我国医书古籍《本经》 曰: 主消渴、 身热、 烦满、 大热, 补 虚安中。 天花粉常与知母、 山药、 麦冬、 枸杞子、 黄芪配伍, 主治阴 虚型糖尿病。 黄苓, 可以清热解湿, 泻火解毒, 其味苦寒, 效用消食化积, 活 血降压, 清热解湿, 泻火解毒, 对付肝经实热的高血糖病, 有清除眩 晕、 头痛、 口苦、 心烦的效用。 无论是煎剂、 浸剂, 均有较明显的降 压效用, 与野菊花、枸杞子等配伍治疗神经性高血糖和动脉硬化高血 糖病, 可使血糖低落, 头痛、 胸闷、 浮躁等症状明显改进和消失。 淫羊藿, 别名铁箭头、 牛角花, 为长绿草木, 生于阴湿的山沟、 山坡杂林或竹丛中, 性温, 味辛甘, 补肾阳, 强筋骨, 祛风湿。 用于 阳痿遗精, 筋骨痿软, 风湿痹痛, 麻木拘挛; 更年期高血糖等症状。 臭梧桐又名海州常山、泰山红五星、泡花桐、八角梧桐、追骨风 、 后庭花等, 性辛、 味苦、 甘, 凉, 入肝经, 胆经, 脾经。 可以治疗风 湿痹痛, 半身不遂, 高血糖病, 偏头痛; 疟疾, 痢疾, 痔疮, 痈疽疮 疥。臭梧桐经高热煎煮后,作用减弱。但是与本发明中其他中药配伍, 则药效不受影响。 黄精, 又名老虎姜、 鸡头参。 为百合科植物滇黄精、 黄精或多花 黄精的干燥根茎, 黄精味甘性平。 归肺, 脾, 肾经。 可以滋肾润肺, 地龙, 性寒, 味咸。 可以清热定惊, 通络、 平喘, 利尿; 用于高 热神昏惊痫抽搐, 关节麻痹, 肢体麻木, 半身不遂, 肺热喘咳, 尿少 水肿, 高血糖症。 天麻, 为多年生草本植物, 分布于全国大部分地区。 其干燥块茎 亦称天麻, 是一味常用而较名贵的中药, 临床多用于头痛眩晕、 肢体 麻木、 小儿惊风、 癫痫、 抽搐、 破伤风等症, 可以平肝熄火, 适用于 肝阳上亢所致的头痛、 眩晕等症。 枸杞子, 归肝经; 肾经; 肺经。 枸杞子补而不腻, 有滋阴补肾、 益精明目、 生津止渴、 阴阳并补之功。 配伍五味子、 黄精、 元参, 适 用于偏于肝肾不足者, 可改善消渴症状。 川芎, 一种中药植物, 常用于活血行气, 祛风止痛, 主要栽培于 四川、 云南、 贵州、 广西、 湖北等地。 川芎辛温香燥, 走而不守, 既 能行散, 上行可达巅顶; 又入血分, 下行可达血海。 活血祛瘀作用广 泛, 适宜瘀血阻滞各种病症; 祛风止痛, 效用甚佳, 可治头风头痛、 风湿痹痛等症。 昔人谓川芎为血中之气药, 殆言其寓辛散、 解郁、 通 达、 止痛等功能。 知母,该品为单子叶植物百合科知母的干燥根茎,功效清热泻火, 生津润燥。 清热泻火, 生津润燥。 用于外感热病, 高热烦渴, 肺热燥 咳, 骨蒸潮热, 内热消渴, 肠燥便秘。 旋复花, 又名驴儿草、 百叶草。 多年生草本, 茎具纵棱, 绿色或 微带紫红色。 叶互生, 椭圆形、 椭圆状披针形或窄长椭圆形。 头状花 序少数或多数, 顶生, 呈伞房状排列, 旋复花咸、 温、 有小毒, 用于 消痰, 下气, 软坚, 行水。 人参, 多年生草本植物, 喜阴凉、 湿润的气候, 多生长于昼夜温 差小的海拔 500〜1100米山地缓坡或斜坡地的针阔混交林或杂木林 中。人参可促进实验动物血糖降低, 并可降低糖尿性血脂升高及无力 症状。临床报道人参浸膏对早期轻症糖尿病有治疗效果,使尿糖减少, 血糖降低 40毫克, 停药后疗效仍可持续 2周以上。
65%乙醇溶液含酒精,白酒素有"百药之长"之称,白酒性质稳定、 安全有效, 而且因为酒精是一种良好的半极性有机溶剂, 中药的各种 有效成分都易溶于其中, 药借酒力、 酒助药势而充分发挥其效力, 提 高治疗效果。 糖尿病是由于胰岛素分泌不足导致血糖过高代谢障碍,西医目前 对糖尿病没有特别好的治疗办法, 称之为不治之症。而我国传统中药 对糖尿病有非常独到的治疗方法,例如本发明这些药物配合使用具有 三重作用, 既是血糖抑制剂, 又是胰岛素增敏剂, 同时又增强胰岛素 受体功能, 而且效果稳定, 本发明的制剂安全无毒副作用, 适合长期 服用, 无需节食, 不忌口, 无需服用其它降糖药物, 单独服用即可, 可以有效保卫胰岛, 降低血糖, 提高免疫, 目前西药也治疗高血糖, 其实仅仅是调控血糖,不能从人体机能的调理入手,而中药作用缓和, 稳定血糖效果较好, 本发明尤其适用于早期、 中老年高血糖患者。 临床实验 1:
1 )、观察时间:在本发明技术方案未曾披露的情况下,选择 2013 年 1月到 2013年 3月的 3个月时间。
2 )、 观察对象: 在广东省深圳市中医院选择 10例糖尿病病例: 男 5例, 女 5例; 年龄: 45— 55岁 5例, 55— 75岁 5例; 职业: 民 营企业主 5例, 退休人员 5例。病程:清晨空腹血糖浓度不低于 11. 6 匪 ol/L, 尿多, 皮肤干燥, 脱水、 口渴、 恶心、 呕吐等明显症状。
3 )、 使用方法: 将本发明制剂口服液在餐后 1小时服用, 每日 3 次, 每次 300ml, 1个月为 1疗程, 两个疗程作为疗效观察。
4)、 观察效果:
在连续服用两个疗程后, 空腹测量血糖, 其中 4例患者降至不高 于 9. Ommol/L, 3例降至不高于 8. Ommol/L, 3例降至不高于 8. 5mmol/L。 停药 7天后观察, 没有明显反弹迹象, 血糖平稳, 尿量减少, 皮肤干 燥改善, 恶心、 呕吐等症状不明显。
临床实验 2:
1 )、观察时间: 在本发明技术方案未曾披露的情况下, 选择 2013 年 4月到 2013年 6月的 3个月时间。
2 )、 观察对象: 在广东省深圳市福田区中医院选择 10例病例: 男 6例, 女 4例; 年龄: 55— 65岁 5例, 65— 75岁 5例; 职业: 曾 担任岗位领导的糖尿病型公务员 5例, 糖尿病普通退休公务员 5例。 病程: 清晨空腹血糖浓度不低于 12. 5 mmol/L, 尿多, 皮肤干燥, 脱 水、 口渴、 恶心、 呕吐等明显症状。
3 )、 使用方法: 将本发明制剂口服液在餐后 1小时服用, 每日 3 次, 每次 300ml, 1个月为 1疗程, 两个疗程作为疗效观察。
4)、 观察效果:
在连续服用两个疗程后, 空腹测量血糖, 其中 2例患者降至不高 于 9. Ommol/L, 3例降至不高于 8. Ommol/L, 5例降至不高于 8. 5mmol/L。 停药 7天后观察, 没有明显反弹迹象, 血糖平稳, 尿量减少, 皮肤干 燥改善, 恶心、 呕吐等症状减退。
结合以上临床数据及本发明的理论依据,可见本发明有益效果在 于, 本发明制成的制剂, 降血糖效果明显, 而且无毒, 无副作用, 效 果稳定, 制取工艺简便易行。 具体实舫式
下面结合实施例对本发明详细加以说明:
实施例 1:
本发明制剂是由纯净水、 葛根、 野菊花、 桑寄生、 玉米须、 天花 粉、 黄苓、 淫羊霍、 臭梧桐、 黄精、 地龙、 天麻、 枸杞子、 川芎、 知 母、 旋复花、 人参、 红糖和 65%乙醇溶液制备成的组合物液态制剂, 其中各组分的质量配比为:
纯净水 4000g 葛根 10g 野菊花 20g 桑寄生 20g 玉米须 25g 天花粉 20g 黄芬 15g 淫羊藿 20g
Figure imgf000012_0001
黄精 20g 地龙 20g 天麻 30g
枸杞子 30g 川芎 20g 知母 20g
旋复花 20g 人参 lOg 红糖 20g
65%乙醇溶液 15gc
上述降血糖中药制剂的制备方法, 包括如下步骤:
1 )、将葛根、野菊花、桑寄生、玉米须、天花粉、黄苓、淫羊霍、 臭梧桐按比例配好, 经过粉碎机粉碎并过 80目筛, 然后在 50— 70°C 的高温下烘干, 然后自然晾到室温备用;
2 )、 将上述步骤中葛根、 野菊花、 桑寄生、 玉米须、 天花粉、 黄 苓、 淫羊霍、 臭梧桐的粉末混合物加入纯净水煎煮三次, 第一次加入 10倍量水煎煮半个小时, 第二次加入 5倍量水煎煮 20分钟, 第三次 加入 5倍量水煎煮 10分钟, 然后合并煎液并过滤, 备用;
3 )、 将黄精、 地龙、 天麻、 枸杞子、 川芎、 知母、 旋复花、 人参 按比例配好, 经过粉碎机粉碎并过 80目筛, 然后在 50— 70°C的高温 下烘干, 然后自然晾到室温备用;
4 )、 将上述黄精、 地龙、 天麻、 枸杞子、 川芎、 知母、 旋复花、 人参的粉末混合物加入 10倍量的纯净水煎煮半个小时, 然后取煎液 并过滤, 备用;
5 )、 在室温状态下, 将上述步骤 2 ) 和步骤 4) 中获得的煎液混 合, 并加入 65%乙醇溶液并搅拌均匀, 形成中药组合物溶液制剂; 6)、 将上述步骤 5 ) 中的中药组合物溶液制剂加入红糖, 并搅拌
5分钟, 即可制得。
制取的上述中药组合物溶液制剂可以用于口服,如果能够早中晚 各饮用一次并长期饮用, 效果更好。
实施例 2:
本发明还可优选的原料质量为 (克):
纯净水 8000g 葛根 30g 野菊花 40g
桑寄生 40g 玉米须 35g 天花粉 30g
黄苓 25g 淫羊藿 30g 臭梧桐 30g
黄精 30g 地龙 30g 天麻 40g
枸杞子 40g 川芎 30g 知母 30g
旋复花 35g 红糖 30g
65%乙醇溶液 15g。
制备方法如实施例 1。
实施例 3:
本发明还可优选的原料质量为 (克):
纯净水 5000g 葛根 15g 野菊花 25g
桑寄生 25g 玉米须 30g 天花粉 25g
黄苓 20g 淫羊藿 25g 臭梧桐 25g
黄精 25g 地龙 25g 天麻 35g
枸杞子 35g 川芎 25g 知母 25g
旋复花 25g 红糖 25g 65%乙醇溶液 20g。
制备方法如实施例 1。
实施例 4:
本发明还可优选的原料质量为 (克):
纯净水 6000g 葛根 20g 野菊花 30g 桑寄生 30g 玉米须 35g 天花粉 30g 黄苓 25g 淫羊藿 30g
Figure imgf000014_0001
黄精 30g 地龙 30g 天麻 35g 枸杞子 35g 川芎 30g 知母 30g 旋复花 30g 红糖 30g
65%乙醇溶液 25g。
制备方法如实施例 1。
实施例 5:
本发明还可优选的原料质量为 (克):
纯净水 7000g 葛根 10g 野菊花 20g 桑寄生 20g 玉米须 25g 天花粉 20g 黄苓 25g 淫羊藿 30g 臭梧桐 30g 黄精 30g 地龙 30g 天麻 30g 枸杞子 30g 川芎 20g 知母 20g 旋复花 35g 人参 20g 红糖 20g
65%乙醇溶液 30gc
制备方法如实施例 1。 实施例 6:
本发明还可优选的原料质量为 (克):
纯净水 4500g 葛根 12g 野菊花 28g
桑寄生 28 玉米须 28g 天花粉 26g
黄苓 18g 淫羊藿 22g 臭梧桐 22g
黄精 22g 地龙 22g 天麻 38g
枸杞子 38g 川芎 21g 知母 21g
旋复花 23g 人参 12g 红糖 28g
65%乙醇溶液 18g。
制备方法如实施例 1。
上述实施例仅是本发明众多实施方式的几种,如将各配方按技术方案
I大或减小药量, 制得的这种降血糖制剂疗效并不受影响, 也将落在本发明的权利保护范围之内。

Claims

权利要求书
1、 一种降血糖中药制剂的配方, 其特征在于, 本发明制剂是由 纯净水、 葛根、 野菊花、 桑寄生、 玉米须、 天花粉、 黄苓、 淫羊霍、 臭梧桐、 黄精、 地龙、 天麻、 枸杞子、 川芎、 知母、 旋复花、 人参、 红糖和 65%乙醇溶液制备成的组合物液态制剂, 其中各组分的质量配 比为:
纯净水 4000-8000g 葛根 10-30g 野菊花 20-40g 桑寄生 20-40g 玉米须 25-35g 天花粉 20-30g 黄苓 15-25g 淫羊藿 20-30g 臭梧桐 20-30g 黄精 20-30g 地龙 20-30g 天麻 30-40g 枸杞子 30-40g 川芎 20-30g 知母 20-30g 旋复花 20-35g 人参 10-20g 红糖 20-30g
65%乙醇溶液 15-30g。
2、 根据权利要求 1所述的降血糖中药制剂的配方, 其特征还在 于, 其中各组分的质量配比为:
纯净水 5000-8000g 葛根 10-20g 野菊花 20-30g 桑寄生 20-30g 玉米须 25-30g 天花粉 20-25g 黄苓 15-20g 淫羊藿 20-25g 臭梧桐 20-25g 黄精 20-25g 地龙 20-25g 天麻 30-35g 枸杞子 30-35g 川芎 20_25g 知母 20-25g 旋复花 20-30g 人参 10_20g 红糖 20-30g
65%乙醇溶液 15-25g (
3、 根据权利要求 1或 2所述的降血糖中药制剂的配方, 其特征 还在于, 其中各组分的质量配比为:
纯净水 6000g 葛根 15g 野菊花 25g
桑寄生 25g 玉米须 25g 天花粉 20g
黄苓 15g 淫羊藿 20g 臭梧桐 20g
黄精 25g 地龙 20g 天麻 30g
枸杞子 30g 川芎 20g 知母 20g
旋复花 25g 人参 15g 红糖 30g
65%乙醇溶液 20go
4、 一种降血糖中药制剂的制备方法, 其特征在于, 其包括如下 步骤:
1 )、将葛根、野菊花、桑寄生、玉米须、天花粉、黄苓、淫羊霍、 臭梧桐按比例配好, 经过粉碎机粉碎并过 80目筛, 然后在 50— 70°C 的高温下烘干, 然后自然晾到室温备用;
2 )、 将上述步骤中葛根、 野菊花、 桑寄生、 玉米须、 天花粉、 黄 苓、 淫羊霍、 臭梧桐的粉末混合物加入纯净水煎煮三次, 第一次加入 10倍量水煎煮半个小时, 第二次加入 5倍量水煎煮 20分钟, 第三次 加入 5倍量水煎煮 10分钟, 然后合并煎液并过滤, 备用;
3 )、 将黄精、 地龙、 天麻、 枸杞子、 川芎、 知母、 旋复花、 人参 按比例配好, 经过粉碎机粉碎并过 80目筛, 然后在 50— 70°C的高温 下烘干, 然后自然晾到室温备用;
4 )、 将上述黄精、 地龙、 天麻、 枸杞子、 川芎、 知母、 旋复花、 人参的粉末混合物加入 10倍量的纯净水煎煮半个小时, 然后取煎液 并过滤, 备用;
5)、 在室温状态下, 将上述步骤 2 ) 和步骤 4) 中获得的煎液混 合, 并加入 65%乙醇溶液并搅拌均匀, 形成中药组合物溶液制剂; 6 )、 将上述步骤 5 ) 中的中药组合物溶液制剂加入红糖, 并搅拌 5分 钟, 即可制得, 制取的上述中药组合物溶液制剂可以用于口服, 如果 能够早中晚各饮用一次并长期饮用, 效果更好。
PCT/CN2013/085131 2013-08-09 2013-10-12 一种降血糖的中药制剂及其制备方法 WO2015018128A1 (zh)

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