CN109793780A - It is a kind of for the hypoglycemic substance of type II diabetes, preparation method and applications - Google Patents

It is a kind of for the hypoglycemic substance of type II diabetes, preparation method and applications Download PDF

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Publication number
CN109793780A
CN109793780A CN201711137182.7A CN201711137182A CN109793780A CN 109793780 A CN109793780 A CN 109793780A CN 201711137182 A CN201711137182 A CN 201711137182A CN 109793780 A CN109793780 A CN 109793780A
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hevea brasiliensis
solvent
fatty contents
seed
para ruber
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CN201711137182.7A
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徐爽
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Abstract

The present invention discloses a kind of substance hypoglycemic for type-2 diabetes mellitus and its application.The substance is plantHevea brasiliensisThe fatty contents of the seed of (para ruber) are made with drying the kernel after decladding by the methods of mechanical presses method, extraction method, defibrination water substitution, supercritical extraction.The substance can be applied to drug, health food, in food, for hypoglycemic for type-2 diabetes mellitus.Type-2 diabetes mellitus personage passes through daily to take or the edible drug, health food, food for being added to the substance can obtain good blood sugar decreasing effect, and without side-effects, can be used for a long time.

Description

It is a kind of for the hypoglycemic substance of type II diabetes, preparation method and applications
Technical field
The present invention discloses a kind of for the hypoglycemic substance of type-2 diabetes mellitus and its application, belongs to medicine and field of food.
Background technique
Type-2 diabetes mellitus is also referred to as non-insulin-depending type type-2 diabetes mellitus, its main feature is that human body itself can generate pancreas islet Element, but cell can not react to it, and the effect of insulin is made to have a greatly reduced quality.The disease is mostly fallen ill after 35~40 years old, 90% or more type 2 diabetes patient is accounted for, disease incidence is in increase trend year by year in the world.Type-2 diabetes mellitus has become After cardiovascular disease and tumour, the 3rd threatens the non-communicable diseases of health of people and life.Current treatment method is divided into Two major classes, one is oral hypoglycemic drug, another kind is insulin injection.
Current hypoglycemic medicine includes: (1) biguanides, such as melbine;(2) sulfonylureas, such as Glimepiride, Ge Lieben Urea, gliclazide and gliquidone;(3) thiazolidinediones, such as Rosiglitazone and Pioglitazone;(4) benzoic acid derivative class, Such as Repaglinide and Nateglinide;(5) alpha-glucosidase restrainer, such as acarbose and voglibose.The above medicine Object has different degrees of side effect.
Summary of the invention
The purpose of the present invention is to provide one kind, some is directed to the hypoglycemic object of type 2 diabetes patient in the prior art Matter (Hevea brasiliensisSeed fatty contents) and its in pharmacy and the application in food.The substance isHevea brasiliensisSeed fatty contents, can be applied to drug, health food, in food, be used for type-2 diabetes mellitus Patient is hypoglycemic.Type 2 diabetes patient passes through daily takes or eats the drug, health food, food that are added to the substance It can be obtained good therapeutic effect.
Hevea brasiliensisIt is the plant para ruber general latin name at home and in the world, for standard For the sake of really, the plant is called with the latin name herein.
In order to realize above-mentioned purpose of the invention, the present invention provides the following technical solutions.
Hevea brasiliensisSeed fatty contents, the substance are prepared by any one of following methods.
Mechanical presses method: with freshHevea brasiliensisSeed is raw material, after drying shelling, obtains kernel, plants Benevolence material is heated to 80-100 DEG C before extrusion, then by static squeeze or dynamic screw extrusion, squeezes out Liquid isHevea brasiliensisSeed fatty contents.
Extraction method: with freshHevea brasiliensisSeed is raw material, after drying shelling, obtains kernel, will Kernel carries out extruding, is granulated or rolling embryo with leaching container that is after processing, being put into sealing, and solvent, selected solvent is added For one of soybean extracting solvent no.6,30-90 DEG C of boiling spread of petroleum ether, n-hexane, ether, ethyl acetate, n-butanol, Or wherein several mixture, under the temperature condition and normal pressure lower than solvent boiling point, to material and solvent be stirred with Mixing, or ultrasonication is carried out, it allows material to come into full contact with solvent, staticly settles later, leach solvent, be then higher than At the temperature and vacuum condition of solvent boiling point, solvent is allowed to volatilize, the liquid stayed isHevea brasiliensisKind Sub- fatty contents.
Supercritical extract: with freshHevea brasiliensisSeed is raw material, after drying shelling, obtains kernel, will After kernel carries out extruding, is granulated or rolls embryo processing, it is put into the supercritical extract container of sealing pressure resistance, solvent titanium dioxide is added Carbon is stirred and mixes with solvent to material, or surpassed under conditions of being more than solvent critical temperature and critical pressure Sonicated allows material to come into full contact with solvent.It staticly settles later, leaches solvent, then at room temperature, reduce pressure Power allows solvent to volatilize, and the liquid stayed isHevea brasiliensisSeed fatty contents.
Invention also provides contain the described of therapeutically effective amountHevea brasiliensisThe fat-soluble portion of seed Divide the pharmaceutical composition with pharmaceutically acceptable carrier.
And health food, by describedHevea brasiliensisSeed fatty contents and health food are common Carrier is formed.
With food, by describedHevea brasiliensisSeed fatty contents and food common carrier are formed.
The present invention also provides describedHevea brasiliensisSeed fatty contents treat II type glycosuria in preparation Application in the drug of patient.
Application as mentioned, wherein describedHevea brasiliensisSeed fatty contents as sole active at Point.
Present invention further provides describedHevea brasiliensisSeed fatty contents treat II in preparation Application in the health food of diabetes mellitus type.
And it is describedHevea brasiliensisFood of the seed fatty contents in preparation type 2 diabetes patient In application.
Application as mentioned, wherein describedHevea brasiliensisSeed fatty contents as sole active at Point.
According to experimental data, compared with the existing drug hypoglycemic for type 2 diabetes patient, the present invention has such as Lower advantage.
1, the present invention provides a kind of completely new, the substance of type-2 diabetes mellitus is treated.
2, safety is good, without side-effects, can be used for a long time.
Specific embodiment
Below by the embodiment of the present invention, property content is described further for the essence of the present invention, but is not limited with this The fixed present invention.
Embodiment 1
Solvent extraction preparationHevea brasiliensisSeed fatty contents, extracting selected solvent is No. 6 solvents.With 100kg is freshHevea brasiliensisSeed is raw material, after drying shelling, prepares kernel 40kg.Then by kernel into After row expanding treatment, it is put into the leaching container of sealing, the solvent of 2 times of weight is added.In 55 DEG C of (being lower than solvent boiling point) conditions Under normal pressure, material is stirred and is mixed with solvent, material is allowed to come into full contact with solvent.It staticly settles, leaches molten later Then agent allows solvent to volatilize, stays 18kg liquid object 120 DEG C (being higher than solvent boiling point temperature) under 100Pa vacuum condition Matter is substance of the invention.
40 type 2 diabetes patients are recruited, are randomly divided into two groups, every group of 20 people.First group (experimental group) the oral present invention Drug made of substance, dose are 5g/ days (with the meter of substance of the present invention in drug);Second group (control group) oral flax Seed oil, oral dose are 5 grams/day.It is detected after 30 days oral.
Testing index is the postprandial two hours blood glucose of patient.The postprandial two hours blood glucose of experimental group from 16.6 before experiment ± 2.2mmol/L, 5.6 ± 1.5mmol/L after being reduced to experiment, difference are extremely significant (P < 0.01);Postprandial two is small before control group experiment When 15.2 ± 2.3mmol/L of blood glucose, 16.2 ± 3.0mmol/L after experiment, experiment front and back no significant difference (P > 0.05).Experiment Group has apparent therapeutic effect compared to the control group, and difference is extremely significant (P < 0.01).
Embodiment 2
The preparation of mechanical presses methodHevea brasiliensisSeed fatty contents, institute's choosing method are static extrusion.With 100kg is freshHevea brasiliensisSeed is raw material, after drying shelling, prepares kernel 40kg.Kernel material is in warm To 80-100 DEG C, then by static extruding, pressure 50MPa, squeezing out 12kg liquid is substance of the invention.
40 type 2 diabetes patients are recruited, are randomly divided into two groups, every group of 20 people.First group (experimental group) the oral present invention Health food made of substance, dose are 10g/ days (with the meter of substance of the present invention in drug);Second group of (control group) mouth Purple Perilla Seed Oil is taken, oral dose is 10 grams/day.It is detected after 30 days oral.
Testing index is patient's glucose in urine.Before experiment, glucose in urine is the positive for experimental group and control group +++.It is real by 30 days After testing, 16 patient's glucoses in urine of experimental group become negative, 4 for it is positive+;20 patients of control group, the still all positives of glucose in urine+ ++.Experimental group has apparent therapeutic effect compared to the control group, and difference is extremely significant (P < 0.01).
Embodiment 3
The preparation of mechanical presses methodHevea brasiliensisSeed fatty contents, institute's choosing method are screw extrusion method.With 100kg is freshHevea brasiliensisSeed is raw material, after drying shelling, prepares kernel 40kg.Kernel material is in warm To 80-100 DEG C, then pass through dynamic screw extrusion, the screw extrusion time is 45 seconds or so, squeezes out 15kg liquid and is Substance of the invention.
A pair the age 64 years old, finds blood glucose rise 20 years with ovum same sex female twin, is after diagnosing type-2 diabetes mellitus.Two people Usually be subcutaneously injected insulin glargine 32IU/ days, oral administration of metformin 15mg/ days, can by glycemic control normal range (NR) it It is interior.
First (elder sister) in twins eat it is disclosed by the invention for food made of the hypoglycemic substance of type-2 diabetes mellitus, Amount is 20 grams/day (in terms of for the hypoglycemic substance of type-2 diabetes mellitus);Second (elder sister) edible corn plumule in twins Food made of oil, amount are 10 grams/day (in terms of maize germ oil).
In 10 days, insulin glargine is gradually kept to 16IU/ days by first, and melbine is gradually kept to 5mg/ days, blood glucose base Originally it remains unchanged, still in the normal range.
In 30 days, it is more than normal that second, which attempts to reduce the dosage of insulin glargine and melbine, but blood glucose rises immediately It is horizontal.Second finally subtracts medicine failure.
Embodiment 4
Solvent extraction preparationHevea brasiliensisSeed fatty contents, extracting selected solvent is No. 6 solvents.With 100kg is freshHevea brasiliensisSeed is raw material, after drying shelling, prepares kernel 40kg.Then by kernel into After row expanding treatment, it is put into the leaching container of sealing, the solvent of 2 times of weight is added.In 55 DEG C of (being lower than solvent boiling point) conditions Under normal pressure, material is stirred and is mixed with solvent, material is allowed to come into full contact with solvent.It staticly settles, leaches molten later Then agent allows solvent to volatilize, stays 18kg liquid object 120 DEG C (being higher than solvent boiling point temperature) under 100Pa vacuum condition Matter is substance of the invention.
A pair the age 68 years old, finds blood glucose rise 30 years with ovum same sex male twin, is after diagnosing type-2 diabetes mellitus.Two people Usually subcutaneous injection insulin glargine 38IU/ days, oral administration of metformin 15mg/ days, but poor blood glucose control.Two people usually on an empty stomach Blood glucose 8-11mmol/L, postprandial blood sugar 19-23mmol/L, glucose in urine +++, there are the complication such as type-2 diabetes mellitus foot.
First (elder brother) in twins eat it is disclosed by the invention for food made of the hypoglycemic substance of type-2 diabetes mellitus, Amount is 30 grams/day (in terms of for the hypoglycemic substance of type-2 diabetes mellitus);Second (elder sister) in twins eats olive oil system At food, amount be 30 grams/day (in terms of olive oil).
After 15 days, first blood glucose level enters normal range (NR), i.e. fasting blood-glucose 5.5-6.3mmol/L, postprandial blood sugar 8- 11mmol/L, glucose in urine become negative;After 30 days, said medicine halves, and blood glucose is still normal;Type-2 diabetes mellitus is controlled enough after 3 months More.
15 days, 30 days and after 3 months, the blood glucose level of second did not change, and still above normal level, medication can not Decrement, type-2 diabetes mellitus have no improvement enough.
Embodiment 5
Supercritical extraction preparationHevea brasiliensisSeed fatty contents, selected solvent are carbon dioxide.With 100kg is freshHevea brasiliensisSeed is raw material, after drying shelling, prepares kernel 40kg.Kernel is made After grain processing, it is put into the supercritical extract container of sealing pressure resistance, solvent is added, solvent quality is 2 times of quality of material.35 DEG C, 10MPa(is more than the critical-temperature and critical pressure of solvent) under conditions of, material is stirred and is mixed with solvent, is allowed Material comes into full contact with solvent.It staticly settles later, leaches solvent, then under room temperature at 25 DEG C, reduce pressure to normal pressure (0.1MPa), allows solvent to volatilize, and staying 18kg liquid is substance of the invention.
A pair the age 40 years old, closely finds blood glucose rise with ovum same sex male twin in two years, is after diagnosing type-2 diabetes mellitus. Two people remain normal per average daily injection insulin glargine 15IU, blood glucose substantially.
First (younger brother) in twins eat it is disclosed by the invention for food made of the hypoglycemic substance of type-2 diabetes mellitus, Amount is 15 grams/day (in terms of for the hypoglycemic substance of type-2 diabetes mellitus);Second (elder brother) edible squash seed oil in twins Manufactured food, amount are 15 grams/day (in terms of pumpkin seed oil).
In 15 days, insulin usage amount is gradually down to zero according to blood glucose level by nail root;Persistently eat needle disclosed by the invention To food half a year made of the hypoglycemic substance of type-2 diabetes mellitus, blood glucose still keeps normal.
In half a year, second attempts to reduce insulin usage amount, but blood glucose increases immediately, subtracts medicine failure.
Embodiment 6:
It is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed fatty contents, by the part Excipient, pelletizing press sheet is added with the ratio of excipient weight ratio 1:1 or 1:2.Tablet can be used as drug, health food or Food.
Embodiment 7:
It is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed fatty contents, by the part, It is wrapped in soft capsule material, routinely soft capsule is made in capsule preparations method.Soft capsule can be used as drug, health food or Person's food.
Embodiment 8:
It is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed fatty contents, with the part, In addition emulsifier, osmotic pressure regulator and water obtain emulsion for injection by high-pressure homogeneous emulsification.
Embodiment 9:
It is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed fatty contents, by the part, Tablet is made as follows again:
Tablet:Hevea brasiliensisSeed fatty contents 100mg
Appropriate starch
Appropriate corn pulp
Magnesium Stearate proper quantity
Preparation method: willHevea brasiliensisSeed fatty contents are mixed with auxiliary agent, sieving, in suitable container Uniformly mixing, obtained granulating mixture tabletting.
Embodiment 10:
It is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed fatty contents, by the part, Soft capsule is made as follows again:
Soft capsule:Hevea brasiliensisSeed fatty contents 1000mg
Appropriate gelatin
Appropriate glycerol
Appropriate amount of water
Preparation method: gelatin, glycerol, which are put into distilled water, to impregnate makes gelatin expansion, softening, is then uniformly mixed, obtains Capsule material glue.Prepared capsule material glue is taken out, is coated in flat plate surface, keeps thickness uniform, then with 90 DEG C or so Temperature heating, evaporates surface moisture, becomes the cushion compound for having certain toughness, having certain elasticity.Finally with pelleting mold or Automatic rotation rolling capsule machine, willHevea brasiliensisSeed fatty contents (1000mg) are fitted into soft capsule skin, production Soft capsule out.
Embodiment 11:
It is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed fatty contents, by the part, Emulsion for injection is made as follows again:
Emulsion for injection:Hevea brasiliensisSeed fatty contents 200g
Appropriate lecithin
Appropriate glycerol
Appropriate sodium chloride
Appropriate amount of water
Preparation method:, will according to formulaHevea brasiliensisSeed fatty contents, lecithin, glycerol mixing add water To 1000mL, add appropriate sodium chloride adjustment osmotic pressure, high-pressure homogeneous emulsification, 121 DEG C of sterilizings are down to room temperature to get newborn to injection Agent.
Embodiment 12:
Tablet: it is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed fatty contents 10mg, Lactose 180mg, starch 55mg, magnesium stearate 5mg;
Preparation method: it will be made of the invention by the method in embodiment 1-5Hevea brasiliensisThe fat-soluble portion of seed Divide, newborn sugar and starch mixing, uniformly moistened with water, the mixture after moistening is sieved and is dried, re-sieving, stearic acid is added Magnesium, then by mixture tabletting, every slice weight 250mg is of the inventionHevea brasiliensisSeed fatty contents content For 10mg.
Embodiment 13:
Capsule: it is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed fatty contents 2000g, gelatin 1000g, glycerol 500g, water 1000g;
Preparation method: by gelatin 1000g, glycerol 500g, being put into 1000g water to impregnate makes gelatin expansion, softening, and then stirring is mixed It closes uniformly, obtains capsule material glue.Prepared capsule material glue is taken out, is coated in flat plate surface, keeps thickness uniform, then uses 90 DEG C or so of temperature heating, evaporates surface moisture, becomes the cushion compound for having certain toughness, having certain elasticity.Finally with pressure Ball mold rotates rolling capsule machine automatically, willHevea brasiliensisSeed fatty contents 1000mg is packed into soft capsule skin In, soft capsule is made.Every soft capsule weighs 1.4g, of the inventionHevea brasiliensisSeed fatty contents content is 1000mg。
Embodiment 14:
Emulsion for injection: it is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed fatty contents 200g, glycerol 25g, lecithin 12g, water 1000g, sodium chloride 1g;
Preparation method: accurate weighing is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed rouge Insoluble portion 200g, glycerol 25g, lecithin 12g, mixing, add water to 1000mL, add sodium chloride, by osmotic pressure adjust to 350mosm/kg H2O.High-pressure homogeneous emulsification obtains emulsion, and 121 DEG C of sterilizings are down to room temperature, are aseptically filled to It is encapsulated in the sterile glass vials of 250mL.Every bottle of emulsion for injection specification is 250mL, of the inventionHevea brasiliensisKind Sub- fatty contents content is 50g.
Embodiment 15:
Food: it is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed fatty contents, pressing should Part reconciles with oil with common edible, is directly becoming food (edible oil);
Preparation method: 10kg is made of the invention by the method in embodiment 1-5Hevea brasiliensisSeed is fat-soluble Part is added in 10kg soybean oil, obtains 20kg blending edible oil.By the filling vial at 500g of blending edible oil, originally InventionHevea brasiliensisSeed fatty contents content is 250g.

Claims (10)

1. plantHevea brasiliensis(para ruber) seed fatty contents, it is characterised in that the substance is by following Any one of method is prepared:
Mechanical presses method: with freshHevea brasiliensis(para ruber) seed is that raw material obtains after drying shelling Kernel, kernel material are heated to 80-100 DEG C before extrusion, then squeeze by static squeeze, or dynamic spiral Pressure, squeezing out liquid isHevea brasiliensis(para ruber) seed fatty contents;
Extraction method: with freshHevea brasiliensis(para ruber) seed is that raw material obtains after drying shelling Kernel is carried out extruding, is granulated or rolling embryo with leaching container that is after processing, being put into sealing, solvent is added by kernel, selected Solvent be soybean extracting solvent no.6,30-90 DEG C of boiling spread of petroleum ether, n-hexane, ether, ethyl acetate, in n-butanol One kind, or wherein several mixtures stir material and solvent under the temperature condition and normal pressure lower than solvent boiling point It mixes and mixes, or carry out ultrasonication, allow material to come into full contact with solvent, staticly settle later, leach solvent, then exist Higher than at the temperature and vacuum condition of solvent boiling point, solvent is allowed to volatilize, the liquid stayed isHevea brasiliensis(para ruber) seed fatty contents;
Supercritical extract: with freshHevea brasiliensis(para ruber) seed is that raw material obtains after drying shelling Kernel is put into the supercritical extract container of sealing pressure resistance, is added molten after kernel is carried out extruding, be granulated or rolls embryo processing Agent carbon dioxide is stirred and mixes with solvent to material under conditions of being more than solvent critical temperature and critical pressure, or Person carries out ultrasonication, allows material to come into full contact with solvent, staticly settles later, leaches solvent, then at room temperature, Reduce pressure, allows solvent to volatilize, the liquid stayed isHevea brasiliensis(para ruber) seed liposoluble Property part.
2. containing the described in claim 1 of therapeutically effective amountHevea brasiliensis(para ruber) seed is fat-soluble The pharmaceutical composition of part and pharmaceutically acceptable carrier.
3. health food, by described in claim 1Hevea brasiliensis(para ruber) seed fatty contents It is formed with health food common carrier.
4. food, by described in claim 1Hevea brasiliensis(para ruber) seed fatty contents and food Product common carrier is formed.
5. described in claim 1Hevea brasiliensis(para ruber) seed fatty contents treat II in preparation Application in the drug of patients with type Ⅰ DM.
6. application as claimed in claim 5, which is characterized in that describedHevea brasiliensis(para ruber) Seed fatty contents are as the sole active agent in drug.
7. described in claim 1Hevea brasiliensis(para ruber) seed fatty contents treat II in preparation Application in the health food of patients with type Ⅰ DM.
8. application as claimed in claim 7, which is characterized in that describedHevea brasiliensis(para ruber) Seed fatty contents are as sole active agent.
9. described in claim 1Hevea brasiliensis(para ruber) seed fatty contents are in preparation II type sugar Urinate the application in the food of patient.
10. application as claimed in claim 9, which is characterized in that describedHevea brasiliensis(Hevea rubber Tree) seed fatty contents are as sole active agent.
CN201711137182.7A 2017-11-16 2017-11-16 It is a kind of for the hypoglycemic substance of type II diabetes, preparation method and applications Pending CN109793780A (en)

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CN109793787A (en) * 2017-11-16 2019-05-24 徐爽 It is a kind of for the hypoglycemic substance of Gestational hyperglycemia, preparation method and applications

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Application publication date: 20190524