CN114099523A - Hypoglycemic drug and preparation method and application thereof - Google Patents
Hypoglycemic drug and preparation method and application thereof Download PDFInfo
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- CN114099523A CN114099523A CN202111514284.2A CN202111514284A CN114099523A CN 114099523 A CN114099523 A CN 114099523A CN 202111514284 A CN202111514284 A CN 202111514284A CN 114099523 A CN114099523 A CN 114099523A
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- Prior art keywords
- leaves
- dihydromyricetin
- trilobatin
- ampelopsis grossedentata
- lithocarpus litseifolius
- Prior art date
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- KQILIWXGGKGKNX-UHFFFAOYSA-N dihydromyricetin Natural products OC1C(=C(Oc2cc(O)cc(O)c12)c3cc(O)c(O)c(O)c3)O KQILIWXGGKGKNX-UHFFFAOYSA-N 0.000 claims abstract description 76
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
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- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K36/18—Magnoliophyta (angiosperms)
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
- C07D311/26—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3
- C07D311/28—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only
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Abstract
The invention discloses a hypoglycemic drug and a preparation method and application thereof, the formula comprises dihydromyricetin and trilobatin, and the weight percentages of the components are as follows: 5-30% of dihydromyricetin and 70-95% of trilobatin; wherein the dihydromyricetin is separated and extracted from the ampelopsis grossedentata leaves, and the dihydromyricetin is purified by using the characteristics of slightly soluble in cold water and easily soluble in hot water in a concentration, crystallization and other modes to obtain the relatively pure dihydromyricetin; the trilobatin is separated and extracted from Lithocarpus litseifolius leaves, and anhydrous ethanol is used as a solvent, so that the activity of the trilobatin can be effectively ensured; the invention fully utilizes the effects that both dihydromyricetin and trilobatin have the blood sugar reducing effect, and the mixing of the two components has the synergistic promotion effect; the hypoglycemic drug prepared by the invention comprises the components of dihydromyricetin and trilobatin, wherein the dihydromyricetin and the trilobatin are both natural products, and the hypoglycemic drug has no toxic or side effect, has good hypoglycemic effect, high medicinal value and market application prospect.
Description
Technical Field
The invention relates to the technical field of medicine preparation, in particular to a hypoglycemic medicine and a preparation method and application thereof.
Background
It is reported that the number of diabetic patients in China reaches 1.29 hundred million, and other people in the early stage of diabetes are about 1.5 hundred million, so that the number of diabetic patients in China increases year by year, and particularly once diabetes is suffered, the diabetes cannot be cured, which is caused by the pathogenesis of the diabetes. Type I diabetes is primarily manifested as irreversible islet failure, while type II diabetes is early, and most likely cured if strictly intervened. Aiming at the hypoglycemic drugs clinically used at present for the type II diabetes, except insulin, the hypoglycemic drugs mainly comprise metformin, repaglinide, acarbose, glimepiride, rosiglitazone, dapagliflozin and the like, and the hypoglycemic drugs are all synthetic drugs, and the proportion of the Chinese patent drugs is less. Most of the medicines are monopolized by foreign resources, and the scale of domestic enterprises is very small. Domestic enterprises have single products and face the edge of elimination. The search and development of natural medicines for reducing blood sugar is very slow.
Lithocarpus litseifolius (Hance) Chun, a plant of the family Fagaceae, the genus Lithocarpus, is rich in vitamins, trace elements (iron, zinc, selenium, calcium, etc.), and various amino acids and flavonoids essential to human body. Modern medical research shows that the important functional components in Lithocarpus litseifolius have the effects of reducing blood sugar, blood fat and blood pressure, resisting inflammation, resisting oxidation, resisting allergy and the like, particularly the trilobatin component has unique effect in preventing and treating diabetes and complications thereof, the trilobatin has obvious inhibition effect on alpha-glucosidase, and is noncompetitive inhibition, and the inhibition effect is not obviously different from acarbose. Therefore, Lithocarpus litseifolius is expected to be a new medicinal material for preventing and treating diabetes. Ampelopsis grossedentata (with the scientific name of Ampelopsis grossedentata (hand. -Mazz.) W.T.Wang) is a common medicinal material for minority people in Yao, Dong, Tujia and the like in China. Modern medicine proves that the ampelopsis grossedentata has various pharmacological activities of oxidation resistance, aging resistance, bacteria resistance, virus resistance, inflammation resistance, pain relief, allergy resistance, leukemia treatment, blood pressure reduction, blood sugar reduction, blood fat reduction, cancer prevention and resistance, liver protection, alcohol effect dispelling and the like, and particularly, the dihydromyricetin serving as an effective component of the ampelopsis grossedentata has better effects of reducing blood sugar and blood fat.
In view of the above situation, trilobatin in lithocarpus litseifolius and dihydromyricetin in ampelopsis grossedentata both have good blood sugar lowering effects. The invention develops the hypoglycemic drug by taking the components as the basis and utilizing the synergistic effect of the two components, so as to fill the vacancy of the hypoglycemic drug with intellectual property rights in China and fill the vacancy of the purely natural hypoglycemic drug at home and abroad.
Disclosure of Invention
The invention aims to provide a hypoglycemic drug, a preparation method and application thereof, so as to solve the problems in the background technology.
In order to achieve the purpose, the invention provides the following technical scheme: a hypoglycemic drug comprises dihydromyricetin and trilobatin in a formula, wherein the weight percentages of the components are as follows: 5-30% of dihydromyricetin and 70-95% of trilobatin.
Preferably, the dihydromyricetin is separated, extracted and purified from the ampelopsis grossedentata leaves.
Preferably, the trilobatin is separated, extracted and purified from lithocarpus litseifolius leaves.
A preparation method of a hypoglycemic drug comprises the following steps: step one, material pretreatment; step two, preparing dihydromyricetin and trilobatin extract; step three, concentrating, purifying and drying; step four, preparing a formula; step five, sterilizing and packaging;
wherein, the first step comprises the following steps:
1) selecting fresh Ampelopsis grossedentata leaves and Litsea polysachyus leaves for later use;
2) soaking the selected Ampelopsis grossedentata leaves in warm water at 40-50 ℃ for 10-15min, rinsing the soaked Ampelopsis grossedentata leaves in cleaning water for 2-3 times, fishing out the rinsed Ampelopsis grossedentata leaves, placing the rinsed Ampelopsis grossedentata leaves in a stainless steel draining disc for draining, placing the rinsed Lithocarpus litseifolius leaves in an oven for drying, baking at 50-55 ℃ until the leaves can be pinched by hands, crushing and sieving the leaves with a screen of 180 meshes, and placing the obtained Ampelopsis grossedentata leaves granules in a dry place for later use;
3) similarly, washing selected Lithocarpus litseifolius leaves by using clear water, then placing the washed Lithocarpus litseifolius leaves in a clear water pool for rinsing for 2-3 times, then placing the rinsed Lithocarpus litseifolius leaves in an oven for drying, wherein the baking temperature in the oven is 50-55 ℃, when the Lithocarpus litseifolius leaves are baked to be hand-kneadable, then crushing and sieving the Lithocarpus litseifolius leaves with a screen of 180 meshes, and then placing the obtained Lithocarpus litseifolius leaves in a dry place for storage;
wherein in the second step, the following processes are included:
1) transferring the Ampelopsis grossedentata leaf granules obtained in the step one into an extraction kettle, and extracting by adopting an ultrasonic-assisted method to obtain a crude extract of Ampelopsis grossedentata dihydromyricetin;
2) transferring the Lithocarpus litseifolius leaf granules obtained in the first step into an extraction kettle, and extracting with ethanol to obtain Lithocarpus litseifolius leaf glycoside extract;
wherein, the third step comprises the following steps:
1) freezing the crude trilobatin extract obtained in the second step to minus 20 ℃, standing at 0-4 ℃ for 60min, filtering to leave precipitate, dissolving the precipitate in 65 ℃ ethanol, freezing to minus 20 ℃, standing at 0-4 ℃ for 60min, filtering to leave precipitate, and vacuum drying the precipitate to obtain trilobatin powder;
2) the crude extract of the dihydromyricetin obtained in the second step is frozen to minus 10 ℃, then dissolved at 0-4 ℃, filtered to leave a precipitate, the precipitate is dissolved in hot water at 93 ℃, then frozen to minus 10 ℃, then dissolved at 0-4 ℃, filtered to leave a precipitated crystal of the precipitate, and the crystal is subjected to vacuum drying to obtain dihydromyricetin powder;
wherein in the fourth step, the formula comprises dihydromyricetin and trilobatin, and the mass percentages of the components are as follows: 5-30% of dihydromyricetin and 70-95% of trilobatin;
in the fifth step, the mixed powder obtained in the fourth step is sterilized by microwaves, placed on a quality inspection table, detected by an instrument for corresponding indexes, and prepared into a medicament after quality inspection is qualified; then, coding, labeling, boxing, refrigerating and warehousing to obtain the medicament for reducing the blood sugar.
Preferably, in the second step, the ultrasonic-assisted method adopts purified water as an extraction solvent, the liquid-material ratio is 25:1, the ultrasonic temperature is 70 ℃, the ultrasonic time is 45min, the ultrasonic power is 240W, the extraction is continuously carried out for 60min, and the extraction is repeated for 3 times.
Preferably, in the second step, the ethanol extraction method comprises adding 3 times volume of anhydrous ethanol (M: V) at 50 deg.C, continuously extracting for 60min with rotary evaporator, and repeating the extraction for 3 times.
Preferably, in the third step, the crystallization temperature is 0-4 ℃, the crystallization time is 10 hours, the drying temperature is 60-70 ℃, and the drying time is 8 hours.
The application of the hypoglycemic drug comprises that the prepared hypoglycemic drug contains dihydromyricetin and trilobatin extracted from Ampelopsis grossedentata leaves and Lithocarpus litseifolius leaves, the dihydromyricetin has the special effect of reducing blood sugar, and the trilobatin has the biological activity of inhibiting the key enzyme alpha-glucosidase of diabetes, so the product has good medicinal value and market application prospect in the aspect of reducing blood sugar.
Compared with the prior art, the invention has the beneficial effects that: according to the invention, the raw materials are extracted from the plants to prepare the hypoglycemic drug, so that the traditional method for preparing the hypoglycemic drug is changed, the naturalness of the product is ensured, and toxic and side effects and adverse reactions are avoided; the anhydrous ethanol is used as a solvent for extracting the trilobatin, so that the activity of the trilobatin can be effectively ensured; the dihydromyricetin is purified by using the characteristics that the dihydromyricetin is slightly soluble in cold water and easily soluble in hot water in a concentration mode, a crystallization mode and the like to obtain the purer dihydromyricetin, so that the quality of the product can be effectively improved. Ensures the treatment effect of the hypoglycemic drug.
Drawings
FIG. 1 is a flow chart of the method of the present invention.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the drawings in the embodiments of the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.
Referring to fig. 1, an embodiment of the present invention:
example 1:
a hypoglycemic drug comprises the following components: the dihydromyricetin and trilobatin comprise the following components in percentage by weight: 5-30% of dihydromyricetin and 70-95% of trilobatin, wherein the dihydromyricetin is separated, extracted and purified from the ampelopsis grossedentata leaves, and the trilobatin is separated, extracted and purified from the lithocarpus litseifolius leaves.
A preparation method of a hypoglycemic drug comprises the following steps: step one, material pretreatment; step two, preparing a dihydromyricetin extracting solution and a trilobatin extracting solution; step three, concentrating, purifying and drying; step four, preparing a formula; step five, sterilizing and packaging;
wherein, the first step comprises the following steps:
1) selecting fresh Ampelopsis grossedentata leaves and Litsea polysachyus leaves for later use;
2) soaking the selected Ampelopsis grossedentata leaves in warm water at 40-50 ℃ for 10-15min, rinsing the soaked Ampelopsis grossedentata leaves in cleaning water for 2-3 times, taking out the rinsed Ampelopsis grossedentata leaves, placing the rinsed Ampelopsis grossedentata leaves in a stainless steel draining disc for draining, placing the drained Ampelopsis grossedentata leaves in an oven for drying, baking the Ampelopsis grossedentata leaves in the oven at 50-55 ℃, kneading the leaves when the leaves are baked to be hand-crushable, crushing and sieving the leaves with a 180-mesh screen, and placing the obtained Ampelopsis grossedentata leaf granules in a dry place for storage;
3) similarly, washing selected Lithocarpus litseifolius leaves by using clear water, then placing the washed Lithocarpus litseifolius leaves in a clear water pool for rinsing for 2-3 times, then placing the Lithocarpus litseifolius leaves after rinsing and draining in an oven for drying, wherein the baking temperature in the oven is 50-55 ℃, when the Lithocarpus litseifolius leaves are baked to be kneaded and crushed by hands, then crushing and sieving the Lithocarpus litseifolius leaves with a screen of 180 meshes, and then placing the obtained Lithocarpus litseifolius leaves granules in a dry place for storage;
wherein in the second step, the following processes are included:
1) transferring the Ampelopsis grossedentata leaf granules obtained in the step one into an extraction kettle, and extracting by adopting an ultrasonic-assisted method to obtain a crude extract of Ampelopsis grossedentata dihydromyricetin;
2) transferring the Lithocarpus litseifolius leaf granules obtained in the first step into an extraction kettle, and extracting with ethanol to obtain Lithocarpus litseifolius leaf glycoside extract;
wherein, the third step comprises the following steps:
1) freezing the crude extract of dihydromyricetin obtained in the second step to minus 10 ℃, then dissolving at 0-4 ℃, filtering to leave precipitate, dissolving the precipitate in hot water at 93 ℃, then freezing to minus 10 ℃, then dissolving at 0-4 ℃, filtering to leave precipitated crystal of the precipitate, and carrying out vacuum drying on the crystal to obtain dihydromyricetin powder;
2) freezing the crude trilobatin extract obtained in the second step to minus 20 ℃, standing at 0-4 ℃ for 60min, filtering to leave precipitate, dissolving the precipitate in 65 ℃ ethanol, freezing to minus 20 ℃, standing at 0-4 ℃ for 60min, filtering to leave precipitate, and vacuum drying the precipitate to obtain trilobatin powder;
wherein in the fourth step, the formula comprises dihydromyricetin and trilobatin, and the mass percentages of the components are as follows: 5% dihydromyricetin and 95% trilobatin;
in the fifth step, the mixed powder obtained in the fourth step is sterilized by microwaves, placed on a quality inspection table, detected by an instrument for corresponding indexes, and prepared into a medicament after quality inspection is qualified; then, coding, labeling, boxing, refrigerating and warehousing to obtain the medicament for reducing the blood sugar.
The application of the hypoglycemic drug comprises that the prepared hypoglycemic drug contains dihydromyricetin and trilobatin extracted from Ampelopsis grossedentata leaves and Lithocarpus litseifolius leaves, the dihydromyricetin has the special effect of reducing blood sugar, and the trilobatin has the biological activity of inhibiting the key enzyme alpha-glucosidase of diabetes, so the product is expected to have good application value and market prospect in the aspect of reducing blood sugar.
Example 2:
a hypoglycemic drug comprises the following components: the dihydromyricetin and trilobatin comprise the following components in percentage by weight: 5-30% of dihydromyricetin and 70-95% of trilobatin, wherein the dihydromyricetin is separated, extracted and purified from the ampelopsis grossedentata leaves, and the trilobatin is separated, extracted and purified from the lithocarpus litseifolius leaves.
A preparation method of a hypoglycemic drug comprises the following steps: step one, material pretreatment; step two, preparing a dihydromyricetin extracting solution and a trilobatin extracting solution; step three, concentrating, purifying and drying; step four, preparing a formula; step five, sterilizing and packaging;
wherein, the first step comprises the following steps:
1) selecting fresh Ampelopsis grossedentata leaves and Litsea polysachyus leaves for later use;
2) soaking the selected Ampelopsis grossedentata leaves in warm water at 40-50 ℃ for 10-15min, rinsing the soaked Ampelopsis grossedentata leaves in cleaning water for 2-3 times, taking out the rinsed Ampelopsis grossedentata leaves, placing the rinsed Ampelopsis grossedentata leaves in a stainless steel draining disc for draining, placing the drained Ampelopsis grossedentata leaves in an oven for drying, baking the Ampelopsis grossedentata leaves in the oven at 50-55 ℃, kneading the leaves when the leaves are baked to be hand-crushable, crushing and sieving the leaves with a 180-mesh screen, and placing the obtained Ampelopsis grossedentata leaf granules in a dry place for storage;
3) similarly, washing selected Lithocarpus litseifolius leaves by using clear water, then placing the washed Lithocarpus litseifolius leaves in a clear water pool for rinsing for 2-3 times, then placing the Lithocarpus litseifolius leaves after rinsing and draining in an oven for drying, wherein the baking temperature in the oven is 50-55 ℃, when the Lithocarpus litseifolius leaves are baked to be kneaded and crushed by hands, then crushing and sieving the Lithocarpus litseifolius leaves with a screen of 180 meshes, and then placing the obtained Lithocarpus litseifolius leaves granules in a dry place for storage;
wherein in the second step, the following processes are included:
1) transferring the Ampelopsis grossedentata leaf granules obtained in the step one into an extraction kettle, and extracting by adopting an ultrasonic-assisted method to obtain a crude extract of Ampelopsis grossedentata dihydromyricetin;
2) transferring the Lithocarpus litseifolius leaf granules obtained in the first step into an extraction kettle, and extracting with ethanol to obtain Lithocarpus litseifolius leaf glycoside extract;
wherein, the third step comprises the following steps:
1) the crude extract of the dihydromyricetin obtained in the second step is frozen to minus 10 ℃, then dissolved at 0-4 ℃, filtered to leave a precipitate, the precipitate is dissolved in hot water at 93 ℃, then frozen to minus 10 ℃, then dissolved at 0-4 ℃, filtered to leave a precipitated crystal of the precipitate, and the crystal is subjected to vacuum drying to obtain dihydromyricetin powder;
2) freezing the crude trilobatin extract obtained in the second step to minus 20 ℃, standing at 0-4 ℃ for 60min, filtering to leave precipitate, dissolving the precipitate in 65 ℃ ethanol, freezing to minus 20 ℃, standing at 0-4 ℃ for 60min, filtering to leave precipitate, and vacuum drying the precipitate to obtain trilobatin powder;
wherein in the fourth step, the formula comprises dihydromyricetin and trilobatin, and the mass percentages of the components are as follows: 30% dihydromyricetin and 70% trilobatin;
in the fifth step, the mixed powder obtained in the fourth step is sterilized by microwaves, placed on a quality inspection table, detected by an instrument for corresponding indexes, and prepared into a medicament after quality inspection is qualified; then, coding, labeling, boxing, refrigerating and warehousing to obtain the medicament for reducing the blood sugar.
The application of the hypoglycemic drug comprises that the prepared hypoglycemic drug contains dihydromyricetin and trilobatin extracted from Ampelopsis grossedentata leaves and Lithocarpus litseifolius leaves, the dihydromyricetin has the special effect of reducing blood sugar, and the trilobatin has the biological activity of inhibiting the key enzyme alpha-glucosidase of diabetes, so the product is expected to have good application value and market prospect in the aspect of reducing blood sugar.
Example 3:
a hypoglycemic drug comprises the following components: the dihydromyricetin and trilobatin comprise the following components in percentage by weight: 5-30% of dihydromyricetin and 70-95% of trilobatin, wherein the dihydromyricetin is separated, extracted and purified from the ampelopsis grossedentata leaves, and the trilobatin is separated, extracted and purified from the lithocarpus litseifolius leaves.
A preparation method of a hypoglycemic drug comprises the following steps: step one, material pretreatment; step two, preparing a dihydromyricetin extracting solution and a trilobatin extracting solution; step three, concentrating, purifying and drying; step four, preparing a formula; step five, sterilizing and packaging;
wherein, the first step comprises the following steps:
1) selecting fresh Ampelopsis grossedentata leaves and Litsea polysachyus leaves for later use;
2) soaking the selected Ampelopsis grossedentata leaves in warm water at 40-50 ℃ for 10-15min, rinsing the soaked Ampelopsis grossedentata leaves in cleaning water for 2-3 times, taking out the rinsed Ampelopsis grossedentata leaves, placing the rinsed Ampelopsis grossedentata leaves in a stainless steel draining disc for draining, placing the drained Ampelopsis grossedentata leaves in an oven for drying, baking the Ampelopsis grossedentata leaves in the oven at 50-55 ℃, kneading the leaves when the leaves are baked to be hand-crushable, crushing and sieving the leaves with a 180-mesh screen, and placing the obtained Ampelopsis grossedentata leaf granules in a dry place for storage;
3) similarly, washing selected Lithocarpus litseifolius leaves by using clear water, then placing the washed Lithocarpus litseifolius leaves in a clear water pool for rinsing for 2-3 times, then placing the Lithocarpus litseifolius leaves after rinsing and draining in an oven for drying, wherein the baking temperature in the oven is 50-55 ℃, when the Lithocarpus litseifolius leaves are baked to be kneaded and crushed by hands, then crushing and sieving the Lithocarpus litseifolius leaves with a screen of 180 meshes, and then placing the obtained Lithocarpus litseifolius leaves granules in a dry place for storage;
wherein in the second step, the following processes are included:
1) transferring the Ampelopsis grossedentata leaf granules obtained in the step one into an extraction kettle, and extracting by adopting an ultrasonic-assisted method to obtain a crude extract of Ampelopsis grossedentata dihydromyricetin;
2) transferring the Lithocarpus litseifolius leaf granules obtained in the first step into an extraction kettle, and extracting with ethanol to obtain Lithocarpus litseifolius leaf glycoside extract;
wherein, the third step comprises the following steps:
1) the crude extract of the dihydromyricetin obtained in the second step is frozen to minus 10 ℃, then dissolved at 0-4 ℃, filtered to leave a precipitate, the precipitate is dissolved in hot water at 93 ℃, then frozen to minus 10 ℃, then dissolved at 0-4 ℃, filtered to leave a precipitated crystal of the precipitate, and the crystal is subjected to vacuum drying to obtain dihydromyricetin powder;
2) freezing the crude trilobatin extract obtained in the second step to minus 20 ℃, standing at 0-4 ℃ for 60min, filtering to leave precipitate, dissolving the precipitate in 65 ℃ ethanol, freezing to minus 20 ℃, standing at 0-4 ℃ for 60min, filtering to leave precipitate, and vacuum drying the precipitate to obtain trilobatin powder;
wherein in the fourth step, the formula comprises dihydromyricetin and trilobatin, and the mass percentages of the components are as follows: 20% dihydromyricetin and 80% trilobatin;
in the fifth step, the mixed powder obtained in the fourth step is sterilized by microwaves, placed on a quality inspection table, detected by an instrument for corresponding indexes, and prepared into a medicament after quality inspection is qualified; then, coding, labeling, boxing, refrigerating and warehousing to obtain the medicament for reducing the blood sugar.
The application of the hypoglycemic drug comprises that the prepared hypoglycemic drug contains dihydromyricetin and trilobatin extracted from Ampelopsis grossedentata leaves and Lithocarpus litseifolius leaves, the dihydromyricetin has the special effect of reducing blood sugar, and the trilobatin has the biological activity of inhibiting the key enzyme alpha-glucosidase of diabetes, so the product is expected to have good application value and market prospect in the aspect of reducing blood sugar.
The hypoglycemic agents obtained in the above examples 1, 2 and 3, as well as single dihydromyricetin and single trilobatin are subjected to function detection to investigate whether the agent has the function of controlling the blood sugar of mice in a diabetes model; taking 100 mice, half of each male and female, wherein 16 mice are normal groups, after feeding 84 mice for 42 days by adopting high-fat diet, carrying out intraperitoneal injection of 0.035g/kg Streptozotocin (STZ) to establish a type II diabetes mouse model, selecting 80 mice successfully modeled, randomly dividing the mice into 5 groups, wherein 16 mice in each group are divided into a normal saline group, a drug group (products of examples 1, 2 and 3, and dihydromyricetin and trilobatin respectively become a drug group 1, a drug group 2, a drug group 3, a dihydromyricetin group and a trilobatin group) and a repaglinide group according to the correspondence of gavage normal saline, hypoglycemic drug dissolved solution and repaglinide; after 56 days of intragastric administration, the mice of each group were tested for changes in Fasting Plasma Glucose (FPG) and glycated hemoglobin (HbA1 c). As a result, the FPG and HbA1c levels were significantly increased in the remaining 3 groups (saline group, drug group, repaglinide group) compared to the normal group (P < 0.05); however, compared with the normal saline group, the FPG and HbA1c levels of the drug group 1, the drug group 2, the drug group 3 and the repaglinide group are significantly reduced (P <0.05), while compared with the normal saline group, the water levels of the dihydromyricetin group and the trilobatin group FPG and HbA1c in the drug group are reduced on average, but the difference does not reach a significant level (P > 0.05); the hypoglycemic drug can effectively control the blood sugar of the diabetic rat, and the dihydromyricetin and the trilobatin have good synergistic effect together.
Based on the above, the invention has the advantages that the dihydromyricetin and trilobatin extracted from Ampelopsis grossedentata leaves and Lithocarpus litseifolius leaves are used as raw materials for preparing the hypoglycemic drug, and the dihydromyricetin is purified by using the characteristics that the dihydromyricetin is slightly soluble in cold water and easily soluble in hot water in a concentration and crystallization manner, so that the purer dihydromyricetin is obtained, and the quality of the product can be effectively improved; the treatment effect of the hypoglycemic drug is ensured, the absolute ethyl alcohol is used as a solvent for extracting the trilobatin, the activity of the trilobatin can be effectively ensured, and meanwhile, the adopted raw materials are all obtained from pure natural plants, so that the traditional method for preparing the hypoglycemic drug is changed, the naturalness of the product is ensured, and toxic and side effects and adverse reactions are avoided.
It will be evident to those skilled in the art that the invention is not limited to the details of the foregoing illustrative examples and that the present invention may be embodied in other specific forms without departing from the spirit or essential characteristics thereof, particularly as long as many Ampelopsis plants contain higher dihydromyricetin and many Lithocarpus polystachyus (wall. ex A. DC.) Rehder medicinal materials also contain higher amounts of trilobatin. The present embodiments are therefore to be considered in all respects as illustrative and not restrictive, the scope of the invention being indicated by the appended claims rather than by the foregoing description, and all changes which come within the meaning and range of equivalency of the claims are therefore intended to be embraced therein. Any reference sign in a claim should not be construed as limiting the claim concerned.
Claims (9)
1. A hypoglycemic drug comprises the following components: dihydromyricetin and trilobatin, characterized in that: the weight percentages of the components are respectively as follows: 5-30% of dihydromyricetin and 70-95% of trilobatin.
2. The hypoglycemic agent according to claim 1, wherein: the dihydromyricetin is separated, extracted and purified from the ampelopsis grossedentata leaves.
3. The hypoglycemic agent according to claim 1, wherein: the trilobatin is separated, extracted and purified from Lithocarpus litseifolius leaves.
4. A preparation method of a hypoglycemic drug comprises the following steps: step one, material pretreatment; step two, preparing a dihydromyricetin extracting solution and a trilobatin extracting solution; step three, concentrating, purifying and drying; step four, preparing a formula; step five, sterilizing and packaging; the method is characterized in that:
wherein, the first step comprises the following steps:
1) selecting fresh Ampelopsis grossedentata leaves and Litsea pungens leaves for later use;
2) soaking the selected Ampelopsis grossedentata leaves in warm water at 40-50 ℃ for 10-15min, rinsing the soaked Ampelopsis grossedentata leaves in cleaning water for 2-3 times, taking out the rinsed Ampelopsis grossedentata leaves, placing the rinsed Ampelopsis grossedentata leaves in a stainless steel draining disc for draining, placing the drained Ampelopsis grossedentata leaves in an oven for drying, baking the Ampelopsis grossedentata leaves in the oven at 50-55 ℃, kneading the leaves when the leaves are baked to be hand-crushable, crushing and sieving the leaves with a 180-mesh screen, and placing the obtained Ampelopsis grossedentata leaf granules in a dry place for storage;
3) similarly, washing selected Lithocarpus litseifolius leaves by using clear water, then placing the washed Lithocarpus litseifolius leaves in a clear water pool for rinsing for 2-3 times, then placing the Lithocarpus litseifolius leaves after rinsing and draining in an oven for drying, wherein the baking temperature in the oven is 50-55 ℃, when the Lithocarpus litseifolius leaves are baked to be kneaded and crushed by hands, then crushing and sieving the Lithocarpus litseifolius leaves with a screen of 180 meshes, and then placing the obtained Lithocarpus litseifolius leaves granules in a dry place for storage;
wherein in the second step, the following processes are included:
1) transferring the Ampelopsis grossedentata leaf granules obtained in the step one into an extraction kettle, and extracting by adopting an ultrasonic-assisted method to obtain a crude extract of Ampelopsis grossedentata dihydromyricetin;
2) transferring the Lithocarpus litseifolius leaf granules obtained in the first step into an extraction kettle, and extracting by using edible ethanol to obtain a Lithocarpus litseifolius triloba glycoside crude extract;
wherein, the third step comprises the following steps:
1) the crude extract of the dihydromyricetin obtained in the second step is frozen to minus 10 ℃, then dissolved at 0-4 ℃, filtered to leave a precipitate, the precipitate is dissolved in hot water at 93 ℃, then frozen to minus 10 ℃, then dissolved at 0-4 ℃, filtered to leave a precipitated crystal of the precipitate, and the crystal is subjected to vacuum drying to obtain dihydromyricetin powder;
2) freezing the crude trilobatin extract obtained in the second step to minus 20 ℃, standing at 0-4 ℃ for 60min, filtering to leave precipitate, dissolving the precipitate in 65 ℃ ethanol, freezing to minus 20 ℃, standing at 0-4 ℃ for 60min, filtering to leave precipitate, and vacuum drying the precipitate to obtain trilobatin powder;
wherein in the fourth step, the formula comprises dihydromyricetin and trilobatin, and the mass percentages of the components are as follows: 5-30% of dihydromyricetin and 70-95% of trilobatin;
in the fifth step, the mixed powder obtained in the fourth step is sterilized by microwaves, placed on a quality inspection table, detected by an instrument for corresponding indexes, and prepared into a medicament after quality inspection is qualified; then, coding, labeling, boxing, refrigerating and warehousing to obtain the medicament for reducing the blood sugar.
5. The process according to claim 4 for producing a hypoglycemic agent, which comprises: in the second step, the ultrasonic auxiliary method adopts purified water as an extraction solvent, the liquid-material ratio is 25:1, the ultrasonic temperature is 70 ℃, the ultrasonic time is 45min, the ultrasonic power is 240W, the extraction is continuously carried out for 60min, and the extraction is repeated for 3 times.
6. The process according to claim 4 for producing a hypoglycemic agent, which comprises: in the second step, 3 times of volume of absolute ethyl alcohol (M: V) is added into the ethanol extraction method, the extraction temperature is 50 ℃, a rotary evaporator is used for continuous extraction for 60min, and the extraction is repeated for 3 times.
7. The process according to claim 4 for producing a hypoglycemic agent, which comprises: in the third step, the weight ratio of the total weight of the selected ethanol to the stock solution is 15: 1, and the concentration of the ethanol is 95%.
8. The process according to claim 4 for producing a hypoglycemic agent, which comprises: in the third step, the crystallization temperature is 0-4 ℃, the crystallization time is 10h, the drying temperature is 60-70 ℃, and the drying time is 8 h.
9. The application of the hypoglycemic drug comprises that the prepared hypoglycemic drug contains dihydromyricetin and trilobatin extracted from Ampelopsis grossedentata leaves and Lithocarpus litseifolius leaves, the dihydromyricetin has the special effect of reducing blood sugar, and the trilobatin has the biological activity of inhibiting the key enzyme alpha-glucosidase of diabetes, so the product has good medicinal value and market application prospect in the aspect of reducing blood sugar.
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| CN110143988A (en) * | 2019-05-08 | 2019-08-20 | 湖南医药学院 | A kind of extracting method of trifloroside |
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