CN107088199B - Alpha-glucosidase restrainer and its application - Google Patents

Alpha-glucosidase restrainer and its application Download PDF

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Publication number
CN107088199B
CN107088199B CN201710403890.4A CN201710403890A CN107088199B CN 107088199 B CN107088199 B CN 107088199B CN 201710403890 A CN201710403890 A CN 201710403890A CN 107088199 B CN107088199 B CN 107088199B
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parts
drug
diabetes
agent
active ingredient
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CN107088199A (en
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张秀敏
张利平
高志远
李建龙
李楼
霍莉
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Hebei University
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Hebei University
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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
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • 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
    • A61K36/06Fungi, e.g. yeasts
    • A61K36/07Basidiomycota, e.g. Cryptococcus
    • 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
    • A61K36/16Ginkgophyta, e.g. Ginkgoaceae (Ginkgo family)
    • 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
    • A61K36/288Taraxacum (dandelion)
    • 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)
    • A61K36/41Crassulaceae (Stonecrop family)
    • 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
    • A61K36/484Glycyrrhiza (licorice)
    • 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
    • A61K36/535Perilla (beefsteak plant)
    • 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)
    • A61K36/54Lauraceae (Laurel family), e.g. cinnamon or sassafras
    • 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)
    • A61K36/60Moraceae (Mulberry family), e.g. breadfruit or fig
    • A61K36/605Morus (mulberry)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/71Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
    • A61K36/718Coptis (goldthread)
    • 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)
    • A61K36/80Scrophulariaceae (Figwort family)
    • A61K36/804Rehmannia
    • 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)
    • A61K36/899Poaceae or Gramineae (Grass family), e.g. bamboo, corn or sugar cane

Abstract

The invention discloses a kind of α glucosidase inhibitors, including:4 thio 2' BrdUs.The α glucosidase inhibitors are used to prepare the drug or prodrug of prevention type II diabetes.α glucosidase inhibitors provided by the invention can effectively inhibit the activity of α glucuroides, and then effectively reduce type II diabetes people's postprandial blood sugar content.The present invention also provides application α glucosidase inhibitors preparation for preventing the drug of type II diabetes, count in parts by weight, the drug includes:4 thio 5 10 parts of 2' BrdUs, the second 80 90 parts of active ingredient of Chinese herbs.Above-mentioned α glucosidase inhibitors provided by the invention carry out rational proportion with other second active ingredient of Chinese herbs and are prepared into effective blood sugar reducing health drug for preventing type II diabetes, after medication in 12 weeks, it is 42.7% to the cure-remarkable-effectiveness rate of patients with NIDDM, high efficiency is up to 95.2%.

Description

Alpha-glucosidase restrainer and its application
Technical field
The present invention relates to pharmaceutical technology field, more particularly to a kind of alpha-glucosidase restrainer and its application.
Background technology
Diabetes are a kind of endocrine and metabolic disorders diseases being happened in worldwide scope, it is due to human insulin Caused by diacrisis and islet function damage, it is a kind of commonplace chronic disease, is mainly characterized by hyperglycaemia.With cancer Disease, angiocardiopathy are considered as worldwide three big diseases jointly, it is caused by the interaction of the composite factors such as h and E Common disease.Diabetes not only cause hyperglycemia, but also long term hyperglycemia and metabolic disorder etc. are also possible to human body can be caused to be permitted Multigroup diabetic complication knitted with organ, such as diabetic cataract, atherosclerosis, peripheral nerve disease, kidney trouble Change and retinopathy etc..So that the health of people, work and life etc. are subject to very big threat.
Clinically, diabetes are divided into four types, i.e.,:I type glycosuria is divided into according to the dependence situation difference to insulin Sick (dependences), type II diabetes (not depending on), also other specific types and gestational diabetes.
In the past few decades, the quantity of diabetes (DM) people constantly accelerates, and in the case quantity of 2010 The whole world 2.85 hundred million is reached.Wherein in most cases, it is type II diabetes (T2DM)。
The quantity of nearly 3 years diabetes patients is even more sharp increase, according to International Diabetes Federation (IDF) statistics of 2013 Report, whole world maturity-onset diabetes number has 3.82 hundred million, wherein 95% belongs to type II diabetes.
The pathogenesis of type II diabetes is extremely complex, and Western medicine is directed to different diseased mechanism, and action target spot is more clear Chu, effect are stronger.But patients with NIDDM is the entirety of an organic connections, many metabolism of diabetic's body Link exists simultaneously imbalance, acts on a certain target drug merely and is difficult to play optimum therapeuticing effect, brings side effect also opposite Substantially, primary failure, secondary failure problem are also more serious.Application has whole if we are in type II diabetes early stage It adjusts and Mutiple Targets medicine certainly will improve therapeutic effect, symptom management development and the generation for reducing complication.Therefore, study The drug that integrally-regulated, Mutiple Targets are treated and side effect is low has become a direction of type II diabetes drug research.
The content of the invention
It is an object of the invention to solve at least the above, and provide the advantages of at least will be described later.
It is a still further object of the present invention to provide a kind of new alpha-glucosidase restrainer, can effectively inhibit α- The activity of glucuroide, and then effectively reduce type II diabetes people's postprandial blood sugar content.
It is a still further object of the present invention to provide a kind of application of alpha-glucosidase restrainer, by itself and others second Active ingredient of Chinese herbs carries out the blood sugar reducing health drug that rational proportion is prepared into effectively prevention type II diabetes.
In order to realize these purposes and further advantage according to the present invention, a kind of alpha-glucosidase restrainer is provided, Including:
Thio -2'- the BrdUs of 4-, structural formula are
Preferably, the drug or prodrug of prevention type II diabetes are used to prepare.
Application of the alpha-glucosidase restrainer as described above in the drug for preventing type II diabetes is prepared.
It is a kind of that alpha-glucosidase restrainer as described above is applied to prepare to prevent the drug of type II diabetes, by weight Number meter is measured, the drug includes:5-10 parts of 4- thio -2'- BrdUs, the second 80-90 parts of active ingredient of Chinese herbs.
Preferably, count in parts by weight, the drug includes:5-10 parts of 4- thio -2'- BrdUs, the second Chinese medicine 80-90 parts of active ingredient.
Preferably, count in parts by weight, second active ingredient of Chinese herbs for 10-15 parts of Radix Glycyrrhizae, 13-17 parts of rhizoma anemarrhenae, 22-27 parts of mulberry leaf, 3-8 parts of pueraria lobata, 13-15 parts of corn stigma, 5-9 parts of the coptis, 14-19 parts of Radix Rehmanniae, 4-8 parts of Chinese cassia tree, Inonotus obliquus 2-4 parts, 28-32 parts of dandelion, 7-12 part of grass of march, 1-3 parts of ginkgo leaf, 2-5 parts of purple perilla, 2-7 parts of bidens pilosa, it is purple to carry on the back day 13-16 parts of certain herbaceous plants with big flowers, the mixture for the extract that 6-10 parts and small winged lotus 2-4 parts of aizoon stonecrop.
Preferably, count in parts by weight, second active ingredient of Chinese herbs for 13-15 parts of Radix Glycyrrhizae, 15-17 parts of rhizoma anemarrhenae, 22-23 parts of mulberry leaf, 3-4 parts of pueraria lobata, 13-15 parts of corn stigma, 5-6 parts of the coptis, 14-16 parts of Radix Rehmanniae, 4-5 parts of Chinese cassia tree, Inonotus obliquus 2 Part, 28-29 parts of dandelion, 7-9 parts of grass of march, 1-2 parts of ginkgo leaf, 2-3 parts of purple perilla, 2-4 parts of bidens pilosa, Gynura bicolor 13 Part, the mixture for the extract that 6-8 parts and small winged lotus 2-4 parts of aizoon stonecrop.
Preferably, count, count in parts by weight in parts by weight, second active ingredient of Chinese herbs is 15 parts of Radix Glycyrrhizae, knows 17 parts female, 22 parts of mulberry leaf, 3 parts of pueraria lobata, 15 parts of corn stigma, 6 parts of the coptis, 16 parts of Radix Rehmanniae, 4 parts of Chinese cassia tree, 2 parts of Inonotus obliquus, Pu Gong 28 parts of English, 7 parts of march grass, 2 parts of ginkgo leaf, 2 parts of purple perilla, 4 parts of bidens pilosa, 13 parts of Gynura bicolor, 8 parts of aizoon stonecrop and small Fly the mixture of the extract of 2 parts of lotus.
Preferably, the dosage form of the drug is selected from through gastrointestinal administration dosage form or injecting medicine-feeding form.
Preferably, the drug is further included is mixed with pharmaceutically acceptable auxiliary material.
Preferably, the auxiliary material be selected from solvent, propellant, solubilizer, cosolvent, emulsifier, binder, disintegrant, Filler, lubricant, wetting agent, osmotic pressure regulator, stabilizer, glidant, corrigent, preservative, suspending agent, coating material Material, aromatic, anti-binder, integrated agent, penetration enhancer, pH adjusting agent, buffer, plasticizer, surfactant, foaming Agent, antifoaming agent, thickener, inclusion agents, moisturizer, absorbent, diluent, flocculant and deflocculant, filter aid, release retardance Any one or a few in agent.
Alpha-glucosidase (EC 3.2.1.20;α-glucosidase) it is a kind of be located in small intestinal mucosa cell brush border Glucosides metabolic enzyme, be it is a kind of can be from the total of the enzyme of the non-reducing end catalysis hydrolyzation of glucose base containing α-glycosidic bond substrate Claim.
The experience such as polysaccharide by alpha-glucosidase etc. are decomposed into monose after digesting step by step, are eventually become after being absorbed into blood Blood glucose.Diabetes often show postprandial hyperglycemia in pathogenic process, and for patients with NIDDM, control is postprandial Blood glucose is extremely important, and alpha-glucosidase becomes regulation and control postprandial blood sugar medicine as the key enzyme for adjusting food source blood glucose The effect target enzyme of object.
Alpha-glucosidase restrainer acts on alpha-glucosidase, inhibits its activity, hinders point of carbohydrate Solution, influences the generation and absorption of glucose, finally reduces postprandial blood sugar, therefore as a line for the treatment of type II diabetes now Oral hypoglycemic drug plays crucial effect in the metabolic process of body.
The present invention includes at least following advantageous effect:
New alpha-glucosidase restrainer provided by the invention can effectively inhibit the work of alpha-glucosidase Property, and then effectively reduce type II diabetes people's postprandial blood sugar content;Itself and other second active ingredient of Chinese herbs are carried out rationally Proportioning is prepared into the blood sugar reducing health drug of effectively prevention type II diabetes;
The present invention under guidance of traditional Chinese medicine theory, as the second active ingredient of Chinese herbs, match somebody with somebody preferably several Chinese medicines by the science of being subject to 5, make, each drug is made to cooperate, is learnt from other's strong points to offset one's weaknesses, act synergistically, all medicines share treats both principal and secondary aspect of disease, heightens the effect of a treatment;
Chinese medicine material small toxicity used in the present invention, overcome other hypoglycemic medicines particularly Western medicine toxic side effect and its After long-time service Western medicine the shortcomings that damage to liver kidney;
The drug of prevention type II diabetes through zoopery and the clinical verification present invention can make patients with NIDDM empty Abdomen blood glucose and it is postprandial 2 it is small when blood glucose reduce, and it is longer to hold time, while also make hyperlipidemia person's cholesterol and triglycerides drop It is low, it is evident in efficacy;
Scientific formula, raw material are easy to get, and generation technique is advanced, simple and easy to do, workable, moderate product price, are suitble to Preparation of industrialization;It can be according to the effective ingredient, property and formulation requirements of each Chinese medicine, using water extraction, physics in preparation process Sterilizing methods, thus product active constituent content is high, stablizes, and is unlikely to deteriorate, is conducive to preserve for a long time;
In conclusion new alpha-glucosidase restrainer provided by the invention can effectively inhibit alpha-glucosidase Activity, itself and other second active ingredient of Chinese herbs are subjected to the hypoglycemic that rational proportions are prepared into effectively prevention type II diabetes Health medicine;And the medicament composing prescription is reasonable, safe to use, evident in efficacy, Small side effects, moderate cost, easy to make, medicine source is rich Rich, convenient to take, raw material is easy to get, and generation technique is advanced, workable.
Part is illustrated to embody by further advantage, target and the feature of the present invention by following, and part will also be by this The research and practice of invention and be understood by the person skilled in the art.
Specific embodiment
With reference to embodiment, the present invention is described in further detail, to make those skilled in the art with reference to specification Word can be implemented according to this.
It should be appreciated that such as " having ", "comprising" and " comprising " term used herein do not allot one or more The presence or addition of a other elements or its combination.
The present invention provides a kind of alpha-glucosidase restrainer, including:
Thio -2'- the BrdUs of 4-, structural formula areExperiment proves that thio -2'- the deoxidations of 4- Uridine is up to 58.41% to the inhibitory activity of alpha-glucosidase.
In one preferred embodiment, the drug or prodrug of prevention type II diabetes are used to prepare.
Application of the alpha-glucosidase restrainer as described above in the drug for preventing type II diabetes is prepared.
It is a kind of that alpha-glucosidase restrainer as described above is applied to prepare to prevent the drug of type II diabetes, by weight Number meter is measured, the drug includes:5-10 parts of 4- thio -2'- BrdUs, the second 80-90 parts of active ingredient of Chinese herbs.
It in one preferred embodiment, counts in parts by weight, the drug includes:5-10 parts of 4- thio -2'- BrdUs, the Two 80-90 parts of active ingredient of Chinese herbs.
It in one preferred embodiment, counts in parts by weight, second active ingredient of Chinese herbs is 10-15 parts of Radix Glycyrrhizae, rhizoma anemarrhenae 13- 17 parts, 22-27 parts of mulberry leaf, 3-8 parts of pueraria lobata, 13-15 parts of corn stigma, 5-9 parts of the coptis, 14-19 parts of Radix Rehmanniae, 4-8 parts of Chinese cassia tree, birch it is brown 2-4 parts of pore fungi, 28-32 parts of dandelion, 7-12 parts of grass of march, 1-3 parts of ginkgo leaf, 2-5 parts of purple perilla, 2-7 parts of bidens pilosa are purple Carry on the back 13-16 parts of semiaquilegia adoxoides, the mixture for the extract that 6-10 parts and small winged lotus 2-4 parts of aizoon stonecrop.
It in one preferred embodiment, counts in parts by weight, second active ingredient of Chinese herbs is 13-15 parts of Radix Glycyrrhizae, rhizoma anemarrhenae 15- 17 parts, 22-23 parts of mulberry leaf, 3-4 parts of pueraria lobata, 13-15 parts of corn stigma, 5-6 parts of the coptis, 14-16 parts of Radix Rehmanniae, 4-5 parts of Chinese cassia tree, birch it is brown 2 parts of pore fungi, 28-29 parts of dandelion, 7-9 parts of grass of march, 1-2 parts of ginkgo leaf, 2-3 parts of purple perilla, 2-4 parts of bidens pilosa, the purple back of the body 13 parts of semiaquilegia adoxoides, the mixture for the extract that 6-8 parts and small winged lotus 2-4 parts of aizoon stonecrop.
It in one preferred embodiment, counts, counts in parts by weight in parts by weight, second active ingredient of Chinese herbs is Radix Glycyrrhizae 15 Part, 17 parts of rhizoma anemarrhenae, 22 parts of mulberry leaf, 3 parts of pueraria lobata, 15 parts of corn stigma, 6 parts of the coptis, 16 parts of Radix Rehmanniae, 4 parts of Chinese cassia tree, 2 parts of Inonotus obliquus, 28 parts of dandelion, 7 parts of march grass, 2 parts of ginkgo leaf, 2 parts of purple perilla, 4 parts of bidens pilosa, 13 parts of Gynura bicolor, 8 parts of aizoon stonecrop With the mixture of the extract of small winged 2 parts of lotus.
In one preferred embodiment, the dosage form of the drug is selected from through gastrointestinal administration dosage form or injecting medicine-feeding form.
In one preferred embodiment, the drug is further included to be mixed with pharmaceutically acceptable auxiliary material.
In one preferred embodiment, the auxiliary material is selected from solvent, propellant, solubilizer, cosolvent, emulsifier, binder, collapses Solve agent, filler, lubricant, wetting agent, osmotic pressure regulator, stabilizer, glidant, corrigent, preservative, suspending agent, bag Clothing material, aromatic, anti-binder, integrated agent, penetration enhancer, pH adjusting agent, buffer, plasticizer, surfactant, Foaming agent, antifoaming agent, thickener, inclusion agents, moisturizer, absorbent, diluent, flocculant and deflocculant, filter aid, release Any one or a few in retarding agent.
Embodiment 1
It prepares to prevent the drug of type II diabetes using alpha-glucosidase restrainer, count in parts by weight, it is described Drug includes:5 parts of the thio -2'- BrdUs of 4-, the second 80 parts of active ingredient of Chinese herbs;It wherein counts in parts by weight, 80 part second Active ingredient of Chinese herbs for 10 parts of Radix Glycyrrhizae, 13 parts of rhizoma anemarrhenae, 22 parts of mulberry leaf, 3 parts of pueraria lobata, 13 parts of corn stigma, 5 parts of the coptis, 14 parts of Radix Rehmanniae, 4 parts of Chinese cassia tree, 2 parts of Inonotus obliquus, 28 parts of dandelion, 7 parts of march grass, 1 part of ginkgo leaf, 2 parts of purple perilla, 2 parts of bidens pilosa, the purple back of the body The mixture of the extract of 13 parts of semiaquilegia adoxoides, 6 parts of aizoon stonecrop and small winged 2 parts of lotus.
According to said medicine formula preparation piece agent person's capsule, the thio -2'- BrdUs of 4- contains in tablet or capsule It measures as 5-6mg/g, the content of the second active ingredient of Chinese herbs is 80-83mg/g.
Embodiment 2
It prepares to prevent the drug of type II diabetes using alpha-glucosidase restrainer, count in parts by weight, it is described Drug includes:7 parts of the thio -2'- BrdUs of 4-, the second 84 parts of active ingredient of Chinese herbs;It wherein counts in parts by weight, 84 part second Active ingredient of Chinese herbs for 14 parts of Radix Glycyrrhizae, 16 parts of rhizoma anemarrhenae, 23 parts of mulberry leaf, 4 parts of pueraria lobata, 15 parts of corn stigma, 5 parts of the coptis, 14 parts of Radix Rehmanniae, 5 parts of Chinese cassia tree, 2 parts of Inonotus obliquus, 28 parts of dandelion, 7 parts of march grass, 2 parts of ginkgo leaf, 2 parts of purple perilla, 2 parts of bidens pilosa, the purple back of the body The mixture of the extract of 13 parts of semiaquilegia adoxoides, 7 parts of aizoon stonecrop and small winged 3 parts of lotus.
The piece agent either thio -2'- BrdUs of 4- in capsule tablet or capsule are prepared according to said medicine formula Content is 6-7mg/g, and the content of the second active ingredient of Chinese herbs is 83-85mg/g.
Embodiment 3
It prepares to prevent the drug of type II diabetes using alpha-glucosidase restrainer, count in parts by weight, it is described Drug includes:10 parts of the thio -2'- BrdUs of 4-, the second 90 parts of active ingredient of Chinese herbs;It wherein counts in parts by weight, 90 part Two active ingredient of Chinese herbs are 15 parts of Radix Glycyrrhizae, 17 parts of rhizoma anemarrhenae, 22 parts of mulberry leaf, 3 parts of pueraria lobata, 15 parts of corn stigma, 6 parts of the coptis, Radix Rehmanniae 16 Part, 4 parts of Chinese cassia tree, 2 parts of Inonotus obliquus, 28 parts of dandelion, 7 parts of march grass, 2 parts of ginkgo leaf, 2 parts of purple perilla, 4 parts of bidens pilosa, The mixture of the extract of 13 parts of Gynura bicolor, 8 parts of aizoon stonecrop and small winged 2 parts of lotus.
The piece agent either thio -2'- BrdUs of 4- in capsule tablet or capsule are prepared according to said medicine formula Content is 10mg/g, and the content of the second active ingredient of Chinese herbs is 90mg/g.
Embodiment 4
It prepares to prevent the drug of type II diabetes using alpha-glucosidase restrainer, count in parts by weight, it is described Drug includes:8 parts of the thio -2'- BrdUs of 4-, the second 88 parts of active ingredient of Chinese herbs;It wherein counts in parts by weight, 88 part second Active ingredient of Chinese herbs for 15 parts of Radix Glycyrrhizae, 17 parts of rhizoma anemarrhenae, 23 parts of mulberry leaf, 4 parts of pueraria lobata, 15 parts of corn stigma, 6 parts of the coptis, 16 parts of Radix Rehmanniae, 5 parts of Chinese cassia tree, 2 parts of Inonotus obliquus, 29 parts of dandelion, 9 parts of march grass, 2 parts of ginkgo leaf, 3 parts of purple perilla, 4 parts of bidens pilosa, the purple back of the body The mixture of the extract of 13 parts of semiaquilegia adoxoides, 8 parts of aizoon stonecrop and small winged 4 parts of lotus.
The piece agent either thio -2'- BrdUs of 4- in capsule tablet or capsule are prepared according to said medicine formula Content is 10mg/g, and the content of the second active ingredient of Chinese herbs is 90mg/g.
First, case standard is selected:
1. meet type II diabetes diagnostic criteria and TCM syndrome diagnostic criteria person.
2. between 18~70 years old age, male or female.
3. after the introduction period, blood glucose still reaches following standard:Fasting blood-glucose >=7.0mmol/L, and≤13.9mmol/L And (or) it is postprandial 2 it is small when blood glucose >=11.1mmol/L, and≤16.6mmol/L.And under conditions of blood glucose meets inclusion criteria, Glycosylated hemoglobin person between 6.5% to 10.0%.
2nd, diagnostic criteria:
All have 1~3 case standard, and meets type II diabetes diagnostic criteria and TCM syndrome diagnostic criteria person, warp Blood glucose assessment can be diagnosed as patients with NIDDM;And it is treated to the drug of embodiment 1-4 in the present invention.
3rd, therapeutic scheme:
4 groups of experimental groups are set in the treatment, and 4 groups of experimental groups are the tablet or capsule prepared according to above-described embodiment 1-4, often Day is 3 times oral, 2 tablets each time, 12 weeks statistics curative effects;
Control group contains only the second active ingredient of Chinese herbs of the present invention in control group drug, daily 3 times oral, and every time 2 Grain, 12 weeks statistics curative effects are simultaneously compared with this experimental group;
Control group is identical with experimental group dosage form, and dosage used in the second active ingredient of Chinese herbs is identical
4th, efficacy assessment standard
(1) it is effective:Decline more than 40% before fasting blood-glucose is relatively treated after treatment or be down to normal level (6.1mmol/L).
(2) effectively:Decline more than 20%, but not up to effective standard before fasting blood-glucose is relatively treated after treatment.
(3) it is invalid:Blood glucose, which declines, is not up to above-mentioned standard.
5th, statistical procedures:
Test group 1 100 is fully recovered 15, effective 20, effective 56, no effect 9, and cure-remarkable-effectiveness rate 35% is efficient 91%;
Test group 2 158 is fully recovered 18, effective 31, effective 95, invalid 14, and cure-remarkable-effectiveness rate 31% is efficient 92%;
Test group 3 124 is fully recovered 25, effective 28, effective 65, invalid 6, and cure-remarkable-effectiveness rate 42.7% is efficient 95.2%;
Test group 4 118 is fully recovered 18, effective 22, effective 66, invalid 12, and cure-remarkable-effectiveness rate 33.8% is efficient 90%;
Control group 114 is fully recovered 10, effective 21, effective 55, invalid 28, and cure-remarkable-effectiveness rate 27.1% is efficient 75.4%;Significantly (P < 0.05), the results show test group is treated for Integrated comparative, cure-remarkable-effectiveness rate, efficient comparing difference between two groups of groups Improve tcm syndrome curative effect and be better than control group.
Note:Cure-remarkable-effectiveness rate=(clinic control recovery from illness+effective)/total number of cases × 100%, efficient=(clinic control recovery from illness+aobvious Effect+effectively) × 100%
Although the embodiments of the present invention have been disclosed as above, but its be not restricted in specification and embodiment it is listed With it can be fully applied to various fields suitable for the present invention, for those skilled in the art, can be easily Realize other modification, therefore without departing from the general concept defined in the claims and the equivalent scope, it is of the invention and unlimited In specific details and shown here as the embodiment with description.

Claims (6)

1. a kind of drug for preventing type II diabetes, which is characterized in that count in parts by weight, the drug includes:4- is thio- 5-10 parts of 2'- BrdUs, the second 80-90 parts of active ingredient of Chinese herbs;It counts in parts by weight, second active ingredient of Chinese herbs is 10-15 parts of Radix Glycyrrhizae, 13-17 parts of rhizoma anemarrhenae, 22-27 parts of mulberry leaf, 3-8 parts of pueraria lobata, 13-15 parts of corn stigma, 5-9 parts of the coptis, Radix Rehmanniae 14- 19 parts, 4-8 parts of Chinese cassia tree, 2-4 parts of Inonotus obliquus, 28-32 parts of dandelion, march 7-12 parts of grass, 1-3 parts of ginkgo leaf, purple perilla 2-5 Part, 2-7 parts of bidens pilosa, 13-16 parts of Gynura bicolor, the mixing for the extract that 6-10 parts and small winged lotus 2-4 parts of aizoon stonecrop Object.
2. the drug of prevention type II diabetes as described in claim 1, which is characterized in that count in parts by weight, described second Active ingredient of Chinese herbs is 13-15 parts of Radix Glycyrrhizae, 15-17 parts of rhizoma anemarrhenae, 22-23 parts of mulberry leaf, 3-4 parts of pueraria lobata, 13-15 parts of corn stigma, Huang 5-6 parts of company, 14-16 parts of Radix Rehmanniae, 4-5 parts of Chinese cassia tree, 2 parts of Inonotus obliquus, 28-29 parts of dandelion, 7-9 parts of grass of march, ginkgo leaf 1-2 Part, 2-3 parts of purple perilla, 2-4 parts of bidens pilosa, 13 parts of Gynura bicolor, the extract that 6-8 parts and small winged lotus 2-4 parts of aizoon stonecrop Mixture.
3. the drug of prevention type II diabetes as described in claim 1, which is characterized in that count in parts by weight, by weight Number meter, second active ingredient of Chinese herbs are 15 parts of Radix Glycyrrhizae, 17 parts of rhizoma anemarrhenae, 22 parts of mulberry leaf, 3 parts of pueraria lobata, 15 parts of corn stigma, the coptis 6 parts, 16 parts of Radix Rehmanniae, 4 parts of Chinese cassia tree, 2 parts of Inonotus obliquus, 28 parts of dandelion, march grass 7 parts, 2 parts of ginkgo leaf, 2 parts of purple perilla, three leaves The mixture of the extract of 4 parts of beggar-ticks, 13 parts of Gynura bicolor, 8 parts of aizoon stonecrop and small winged 2 parts of lotus.
4. the drug of the prevention type II diabetes as any one of claim 1-3, which is characterized in that the agent of the drug Type is selected from through gastrointestinal administration dosage form or injecting medicine-feeding form.
5. as claimed in claim 4 prevention type II diabetes drug, which is characterized in that the drug further include with pharmaceutically Acceptable auxiliary material is mixed.
6. the drug of prevention type II diabetes as claimed in claim 5, which is characterized in that the auxiliary material is selected from solvent, casts Agent, solubilizer, cosolvent, emulsifier, binder, disintegrant, filler, lubricant, wetting agent, osmotic pressure regulator, stabilization Agent, glidant, corrigent, preservative, suspending agent, coating material, aromatic, anti-binder, integrated agent, penetration enhancer, pH Be worth conditioning agent, buffer, plasticizer, surfactant, foaming agent, antifoaming agent, thickener, inclusion agents, moisturizer, absorbent, Diluent, flocculant and deflocculant, filter aid, release retarding agent in any one or a few.
CN201710403890.4A 2017-06-01 2017-06-01 Alpha-glucosidase restrainer and its application Expired - Fee Related CN107088199B (en)

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US3163639A (en) * 1962-01-24 1964-12-29 Burroughs Wellcome Co 4-thio-2'-deoxyuridine
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US3163639A (en) * 1962-01-24 1964-12-29 Burroughs Wellcome Co 4-thio-2'-deoxyuridine
CN102675389A (en) * 2011-03-08 2012-09-19 大连大学 5-iodine-4-sulfur-2'-deoxyuridine, and derivatives and synthetic method thereof
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