CN109010293A - A kind of net tablet of nanometer assembling En Gelie and preparation method for diabetes - Google Patents
A kind of net tablet of nanometer assembling En Gelie and preparation method for diabetes Download PDFInfo
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- CN109010293A CN109010293A CN201810965196.6A CN201810965196A CN109010293A CN 109010293 A CN109010293 A CN 109010293A CN 201810965196 A CN201810965196 A CN 201810965196A CN 109010293 A CN109010293 A CN 109010293A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1611—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
Abstract
The present invention relates to a kind of net tablets of nanometer assembling En Gelie and preparation method for diabetes, belong to Remedies for diabetes technical field.The present invention solves the preparation method that technical problem is to provide a kind of nanometer assembling net tablet of En Gelie for diabetes.The preparation method carries out nanometer assembling by carrier of mesoporous silicon oxide by the way that En Gelie is ground to nanoscale with Sodium Hyaluronate only, so that the outer boundary of nanometer En Gelie net nanometer sufficiently demonstrates, dissolution rate increases；And overcome defect easy to reunite after nanosizing；Meanwhile it is net using Sodium Hyaluronate aided nano En Gelie, hydrophily and biocompatibility make nanometer En Gelie be easier to dissolve out only, improve En Gelie net utilization.The method of the present invention is simply at low cost, and the net tablet of the En Gelie being prepared, effective component dissolution rate is fast, and En Gelie net utilization is high.
Description
Technical field
The present invention relates to a kind of net tablets of nanometer assembling En Gelie and preparation method for diabetes, belong to diabetes and control
Treat technical field of pharmaceuticals.
Background technique
Type-2 diabetes mellitus becomes the disease of increased popularity, high-frequency complication (such as diabetes, blindness, kidney failure
Deng) not only influence the quality of life of patient, and it is possible to lead to the shortening in service life.En Gelie is net (empagliflozin)
A kind of white -2(SGLT-2 of oral sodium glucose co-transporter 2) inhibitor.SGLT-2 is mainly responsible for from glomerulus
Glucose is reabsorbed in filtrate and enters the transporter of body circulation, and by inhibiting SGLT-2, En Gelie only reduces kidney is to filtration Portugal
The re-absorption of grape sugar, and the kidney threshold value of glucose is reduced, to increase the excretion of glucose in urine.Suffer from for type-2 diabetes mellitus adult
The glycemic control of person.It is initially researched and developed jointly by Boehringer Ingelheim company and Li Lai company, obtains European Union batch in June, 2014
Standard, in August, 2014 obtain U.S. FDA approval.
En Gelie net chemical name are as follows: (1S) -1,5- dehydration -1-C- [the chloro- 3- of 4- [[4- [[(3S)-tetrahydro -3- furans
Base] oxygroup] phenyl] methyl] phenyl]-D-Glucose alcohol.Targeting, mechanism of action can be played directly against glucose
Independent of B cell function and insulin resistance.Moreover, En Gelie has great advantage in validity and safety only.
But when actually taking, it is dissolved in water since En Gelie is only atomic, so that dissolution rate reduces.And the dissolution of drug
Degree directly affects the absorption of drug, and dissolution rate is low to cause bioavilability low, influences curative effect of medication, the curative effect of drug is caused to pay no attention to
Think and waste, and large dose oral administration drug is easy to produce many adverse reactions.Routine techniques is to improve preparation dissolution rate, can be right
Raw material is micronized.It is desirable that improving result of extraction by further nanosizing, but in fact, the En Gelie after nanometer is net
Easily reunite, and hydrophobic, affects result of extraction instead.
Application No. is 201080015987.4 patents of invention to disclose a kind of method for preparing the net tablet of En Gelie, the hair
It is bright that the partial size of the net raw material of En Gelie is reduced to improve its dissolution rate in vitro by special mechanical crushing or Jet Mill.
But to reach the grain graininess and need to be micronized drug, comparatively laborious in production, production efficiency is low, can not advise greatly
Mould industrial applications.
Application No. is 201410810900.2 patents of invention to disclose net piece of En Gelie and its preparation method and application, institute
Stating the net piece of En Gelie includes: comprising the first component and the second component, wherein described first group be divided into it is net selected from En Gelie, its can
At least one of pharmaceutical salts and its solvate, described second group is divided into microcrystalline cellulose.The invention is fine by control crystallite
Dimension element dissolve out En Gelie can more preferably in the media such as 0.1N hydrochloric acid, water only in a reasonable range, improve its biology benefit
Expenditure and stability.The net tablet formulation of the En Gelie of the invention and preparation process are although simple and easy, but the exhausted great Cheng of its effect
Microcrystalline cellulose is relied on degree, and preparing for microcrystalline cellulose is complex, therefore, the cost of the invention remains unchanged higher and molten
Out-degree is limited, needs further to improve.
Application No. is the patents of invention of 201510932515.X to disclose a kind of net tablet of En Gelie and preparation method thereof, should
Tablet includes: that En Gelie is net, succinic acid, hydroxypropyl-β-cyclodextrin, methacrylic acid, avocado oil, filler, adhesive, disintegration
Agent, lubricant, He Shui.Preparation method is first that En Gelie is net and succinic acid mixes, and avocado oil, grinding, gained mixing is added
Object and hydroxypropyl-β-cyclodextrin, methacrylic acid add in 1/5 parts by weight water, stir, filtering, the net inclusion compound of get En Gelie；So
Adhesive is added in remaining weight part water afterwards, stirs, obtains binder solution；Finally by the net inclusion compound of En Gelie, filler and
Disintegrating agent mixing, be added binder solution granulation, whole grain, drying, be added lubricant, mixing, tabletting to get.The present invention is by grace
For lattice column net system at tablet is further made after inclusion compound, gained tablet quality is stable, has good In Vitro Dissolution behavior, the party
The net piece of En Gelie of method preparation, ingredient complexity type is more, although the net dissolution of En Gelie can be improved, dissolution rate is limited,
It needs further to improve.
Summary of the invention
Reduce only for existing En Gelie and be easy after partial size to reunite, be hydrophobic, influences to dissolve out, the not high defect of dissolution rate,
The present invention provides a kind of net tablet of nanometer assembling En Gelie and preparation method for diabetes.
First technical problem that the present invention solves is to provide a kind of nanometer assembling net tablet of En Gelie for diabetes
Preparation method.
Preparation method of the present invention for the nanometer assembling net tablet of En Gelie of diabetes, which is characterized in that including as follows
Step:
A, it grinds: Sodium Hyaluronate and the net powder of En Gelie 1:5~10 in mass ratio being uniformly mixed, are subsequently placed in grinder
Grinding, is ground to nanoscale, obtains nano powder；
B, self-assembly microspheres are prepared: nano powder being mixed with dispersing agent, distilled water, obtains a nanometer jelly；Using ultrasonic disperse,
Power is 300~500W, and ultrasonic time is 5~15min；Then mesoporous silicon oxide is added, continues 3~5min of ultrasonic disperse,
Spray drying obtains self-assembly microspheres；Wherein, the mass ratio for guaranteeing nano powder and mesoporous silicon oxide is 2~5:1；Dispersing agent
Additional amount is the 5~10% of nano powder weight；
C, tabletting: self-assembly microspheres and filler, disintegrating agent, adhesive and mix lubricant are uniform, it is tabletted, it is used
The net tablet of En Gelie is assembled in the nanometer of diabetes, wherein by weight, 20~40 parts of self-assembly microspheres, filler 50~
200 parts, 5~20 parts of disintegrating agent, 5~20 parts of adhesive, 1~10 part of lubricant.
The method of the present invention is to carry with mesoporous silicon oxide by the way that En Gelie is ground to nanoscale with Sodium Hyaluronate only
Body carries out nanometer assembling, so that the outer boundary of nanometer En Gelie net nanometer sufficiently demonstrates, dissolution rate increases；And it overcomes
Defect easy to reunite after nanosizing；Meanwhile, hydrophily and bio-compatible net using Sodium Hyaluronate aided nano En Gelie
Property make nanometer En Gelie only be easier dissolve out, improve En Gelie net utilization.
A step is mainly that En Gelie is worn into the process of nano powder only, wherein needs to be added a certain proportion of hyaluronic acid
Sodium.Sodium Hyaluronate is the substance extracted from cockscomb, can also be fermented and is made by Lactococcus, for white or off-white color particle
Or powder, odorless, when dry, nitrogen content is 2.8~4.0%, and glucuronic acid content is 37.0~51.0%.Sodium Hyaluronate is wide
The general physiological activator for being present in animal and human body, in application on human skin, synovium of joint liquid, umbilical cord, aqueous humor and vitreum
It is distributed.Molecular weight is 500000~730000 dalton, and inventor is the study found that a certain amount of Sodium Hyaluronate can assist
Nanometer En Gelie is net, and the hydrophily and biocompatibility of Sodium Hyaluronate complement each other only with En Gelie, are not influencing grace lattice
Under the premise of arranging net drug effect, nanometer En Gelie is enabled to be easier to dissolve out only, to improve En Gelie net utilization.
Preferably, in a step, hyaluronic acid and the net powder of En Gelie 1:8 in mass ratio mixing.
The grinding of a step can use the prior art, in order to improve the net dissolution of En Gelie, while reduce to greatest extent
Grind cost, it is preferred that the granularity of the nano powder after grinding is 5~400nm.
B step is the process of self assembly, and nano powder is mixed with dispersing agent, distilled water, obtains a nanometer jelly；Using super
Sound dispersion, power are 300~500W, and ultrasonic time is 5~15min；Then mesoporous silicon oxide is added, continues ultrasonic disperse 3
~5min, spray drying obtain self-assembly microspheres.The step mainly uses mesoporous silicon oxide to carry out self assembly for carrier.
Mesoporous silicon oxide is a kind of common porous silica silicon materials, currently, common meso-porous titanium dioxide in the market
Silicon materials are mainly by MCM-n series, SBA series, KIT series, MSU series etc..Since mesoporous silicon oxide has in certain model
Enclose the uniform mesoporous pore size of interior continuously adjustable, the channel of rule, stable skeleton structure, the surfaces externally and internally for being easy to modify and nothing
Therefore the features such as physiological-toxicity, is commonly used for the carrier of drug.The present invention also uses mesoporous silicon oxide to carry out as carrier from group
Dress increases dissolution rate so that the outer boundary of nanometer En Gelie net nanometer sufficiently demonstrates, and can overcome after nanosizing easily
The defect of reunion.
Wherein, the amount of mesoporous silicon oxide has a certain impact to self assembly, it is preferred that in b step, nano powder with it is mesoporous
The mass ratio of silica is 4:1；The additional amount of dispersing agent is the 8% of nano powder weight.
Preferably, in b step, the power of ultrasonic disperse is 400W, and ultrasonic time is added mesoporous after being 10min
Silica.
Dispersing agent is one kind in the molecule while having lipophilic and two kinds of opposite natures of hydrophily interfacial agent.It can
Those are poorly soluble in the inorganic of liquid, the solid and liquid particles of organic pigment for uniform dispersion, while can also prevent particle
Sedimentation and cohesion, amphipathic reagent needed for forming stable suspension.It is only and saturating that the present invention disperses En Gelie using dispersing agent
Bright matter acid sodium.Dispersing agent commonly used in the art is suitable for the present invention.Preferably, in b step, the dispersing agent is dodecyl
Sodium sulphate.
Step c is the process of tabletting, and self-assembly microspheres and filler, disintegrating agent, adhesive and mix lubricant are uniform,
It is tabletted.
Preferably, in step c, by weight, 30 parts of self-assembly microspheres, 100 parts of filler, disintegrating agent 12
Part, 10 parts of adhesive, 6 parts of lubricant.
Wherein, filler, disintegrating agent, lubricant and adhesive are common pharmaceutic adjuvant.
Filler also known as filler, compound, filler.Material performance can be improved by being added in material, or can increase-volume, increasing
Weight, reduces the solid matter of the cost of material.The main function of filler of the invention is the weight or body for filling tablet
Product, consequently facilitating tabletting.Common filler has starch, carbohydrate, cellulose family and inorganic salts etc..Preferably, described to fill out
Filling agent is selected from least one of starch, mannitol, sorbierite, talcum powder, calcium phosphate.
Disintegrating agent, which refers to, can make tablet split the substance for being broken into fine particle rapidly in gastro-intestinal Fluid, to keep functional component fast
Speed dissolves and absorbs, and plays a role.This substance mostly has good water imbibition and dilatancy, to realize the disintegration of tablet.
It, all should be added with disintegrating agent in general tablet other than the tablet of sustained release tablets and certain specific uses.Disintegration of the invention
The effect of agent is to eliminate the binding force generated by adhesive or high compression, so that tablet be made to disintegrate in water.It is preferred that
, the disintegrating agent is at least one of croscarmellose sodium, crospovidone.
Adhesive is the sticking substance of tool, and several isolated materials can link together by its viscosity.Preferably,
Described adhesive is at least one of dextrin, lactose.
Lubricant is to drop the frictional resistance of low friction pair, slow down its lubricant medium worn.Preferably, the lubricant
For at least one of magnesium stearate, calcium stearate, zinc stearate, stearic acid, polyethylene glycol.
Second technical problem that the present invention solves is to provide a kind of net tablet of En Gelie.
The net tablet of En Gelie of the present invention, is prepared using the above method, which uses Sodium Hyaluronate aided nano
En Gelie is net, carries out nanometer assembling by carrier of mesoporous silicon oxide, then be aided with filler, disintegrating agent, adhesive etc. and be pressed into
Tablet improves En Gelie net utilization to increase the net dissolution rate of En Gelie.
Compared with prior art, the invention has the following beneficial effects:
The method of the present invention, by the way that En Gelie is ground to nanoscale with Sodium Hyaluronate only, using mesoporous silicon oxide as carrier into
The assembling of row nanometer, so that the outer boundary of nanometer En Gelie net nanometer sufficiently demonstrates, dissolution rate increases；And overcome nanometer
Defect easy to reunite after change；Meanwhile it is net using Sodium Hyaluronate aided nano En Gelie, hydrophily and biocompatibility make
It obtains nanometer En Gelie to be easier to dissolve out only, to improve En Gelie net utilization.
The method of the present invention is simply at low cost, and the net tablet of the En Gelie being prepared, effective component dissolution rate is fast, En Ge
Column net utilization is high.
Specific embodiment
In the following, the present invention will be further described in detail by way of specific embodiments, but this should not be interpreted as to the present invention
Range be only limitted to example below.Without departing from the idea of the above method of the present invention, according to ordinary skill
The various replacements or change that knowledge and customary means are made, should be included in the scope of the present invention.
Embodiment 1
A kind of nanometer assembling net tablet of En Gelie for diabetes, is prepared with the following method:
A, it grinds: Sodium Hyaluronate and the net powder of En Gelie 1:5 in mass ratio being uniformly mixed, is subsequently placed in grinder and grinds
Mill, is ground to nanoscale, obtains nano powder；Guarantee the granularity of nano powder between 5~400nm.
B, self-assembly microspheres are prepared: nano powder being mixed with dispersing agent lauryl sodium sulfate, distilled water, obtains nanometre glue
Shape object；Using ultrasonic disperse, power 300W, ultrasonic time 15min；Then mesoporous silicon oxide is added, continues ultrasound point
5min is dissipated, spray drying obtains self-assembly microspheres；Wherein, the mass ratio for guaranteeing nano powder and mesoporous silicon oxide is 2:1；Dispersion
The additional amount of agent lauryl sodium sulfate is the 10% of nano powder weight.
C, tabletting: self-assembly microspheres and filler, disintegrating agent, adhesive and mix lubricant are uniform, it is tabletted, it obtains
The net tablet of En Gelie is assembled to the nanometer for diabetes, wherein by weight, 20 parts of self-assembly microspheres, 50 parts of filler,
5 parts of disintegrating agent, 5 parts of adhesive, 10 parts of lubricant；Wherein, the filler is selected from starch；The disintegrating agent is crosslinking carboxylic first
Base sodium cellulosate；Described adhesive is dextrin；The lubricant is magnesium stearate.
According to 2010 editions Chinese Pharmacopoeias, two defined methods, takes this to be used for the nanometer of diabetes and assemble the net tablet of En Gelie
It 6, is placed in 250mL beaker, about 20 DEG C of water 100mL is added, concussion measures the dispersion time limit, and the result is shown in tables 1.
According to 2010 editions Chinese Pharmacopoeias, two defined dissolution methods, the nanometer assembling grace for diabetes is carried out
Lattice arrange the dissolution determination experiment of net tablet, measure every the amount of dissolution using ultraviolet-visible spectrophotometry, calculate its dissolution rate,
It the results are shown in Table 2.
Embodiment 2
A kind of nanometer assembling net tablet of En Gelie for diabetes, is prepared with the following method:
A, it grinds: Sodium Hyaluronate and the net powder of En Gelie 1:10 in mass ratio being uniformly mixed, is subsequently placed in grinder and grinds
Mill, is ground to nanoscale, obtains nano powder；Guarantee the granularity of nano powder between 5~400nm.
B, self-assembly microspheres are prepared: nano powder being mixed with dispersing agent lauryl sodium sulfate, distilled water, obtains nanometre glue
Shape object；Using ultrasonic disperse, power 500W, ultrasonic time 5min；Then mesoporous silicon oxide is added, continues ultrasound point
3min is dissipated, spray drying obtains self-assembly microspheres；Wherein, the mass ratio for guaranteeing nano powder and mesoporous silicon oxide is 5:1；Dispersion
The additional amount of agent lauryl sodium sulfate is the 5% of nano powder weight.
C, tabletting: self-assembly microspheres and filler, disintegrating agent, adhesive and mix lubricant are uniform, it is tabletted, it obtains
The net tablet of En Gelie is assembled to the nanometer for diabetes, wherein by weight, 40 parts of self-assembly microspheres, filler 200
Part, 20 parts of disintegrating agent, 20 parts of adhesive, 1 part of lubricant；Wherein, the filler is selected from mannitol；The disintegrating agent is to hand over
Join in povidone；Described adhesive is lactose；The lubricant is calcium stearate.
According to 2010 editions Chinese Pharmacopoeias, two defined methods, takes this to be used for the nanometer of diabetes and assemble the net tablet of En Gelie
It 6, is placed in 250mL beaker, about 20 DEG C of water 100mL is added, concussion measures the dispersion time limit, and the result is shown in tables 1.
According to 2010 editions Chinese Pharmacopoeias, two defined dissolution methods, the nanometer assembling grace for diabetes is carried out
Lattice arrange the dissolution determination experiment of net tablet, measure every the amount of dissolution using ultraviolet-visible spectrophotometry, calculate its dissolution rate,
It the results are shown in Table 2.
Embodiment 3
A kind of nanometer assembling net tablet of En Gelie for diabetes, is prepared with the following method:
A, it grinds: Sodium Hyaluronate and the net powder of En Gelie 1:6 in mass ratio being uniformly mixed, is subsequently placed in grinder and grinds
Mill, is ground to nanoscale, obtains nano powder.
B, self-assembly microspheres are prepared: nano powder being mixed with dispersing agent lauryl sodium sulfate, distilled water, obtains nanometre glue
Shape object；Using ultrasonic disperse, power 250W, ultrasonic time 8min；Then mesoporous silicon oxide is added, continues ultrasound point
4min is dissipated, spray drying obtains self-assembly microspheres；Wherein, the mass ratio for guaranteeing nano powder and mesoporous silicon oxide is 4:1；Dispersion
The additional amount of agent lauryl sodium sulfate is the 6% of nano powder weight.
C, tabletting: self-assembly microspheres and filler, disintegrating agent, adhesive and mix lubricant are uniform, it is tabletted, it obtains
The net tablet of En Gelie is assembled to the nanometer for diabetes, wherein by weight, 25 parts of self-assembly microspheres, 80 parts of filler,
8 parts of disintegrating agent, 14 parts of adhesive, 8 parts of lubricant；Wherein, the filler is selected from sorbierite；The disintegrating agent is crosslinking carboxylic
Sodium carboxymethylcellulose pyce；Described adhesive is dextrin；The lubricant is magnesium stearate.
According to 2010 editions Chinese Pharmacopoeias, two defined methods, takes this to be used for the nanometer of diabetes and assemble the net tablet of En Gelie
It 6, is placed in 250mL beaker, about 20 DEG C of water 100mL is added, concussion measures the dispersion time limit, and the result is shown in tables 1.
According to 2010 editions Chinese Pharmacopoeias, two defined dissolution methods, the nanometer assembling grace for diabetes is carried out
Lattice arrange the dissolution determination experiment of net tablet, measure every the amount of dissolution using ultraviolet-visible spectrophotometry, calculate its dissolution rate,
It the results are shown in Table 2.
Embodiment 4
A kind of nanometer assembling net tablet of En Gelie for diabetes, is prepared with the following method:
A, it grinds: Sodium Hyaluronate and the net powder of En Gelie 1:9 in mass ratio being uniformly mixed, is subsequently placed in grinder and grinds
Mill, is ground to nanoscale, obtains nano powder；Guarantee the granularity of nano powder between 5~400nm.
B, self-assembly microspheres are prepared: nano powder being mixed with dispersing agent lauryl sodium sulfate, distilled water, obtains nanometre glue
Shape object；Using ultrasonic disperse, power 350W, ultrasonic time 11min；Then mesoporous silicon oxide is added, continues ultrasound point
4min is dissipated, spray drying obtains self-assembly microspheres；Wherein, the mass ratio for guaranteeing nano powder and mesoporous silicon oxide is 2.5:1；Point
The additional amount of powder lauryl sodium sulfate is the 9% of nano powder weight.
C, tabletting: self-assembly microspheres and filler, disintegrating agent, adhesive and mix lubricant are uniform, it is tabletted, it obtains
The net tablet of En Gelie is assembled to the nanometer for diabetes, wherein by weight, 35 parts of self-assembly microspheres, filler 180
Part, 18 parts of disintegrating agent, 8 parts of adhesive, 3 parts of lubricant；Wherein, the filler is to select talcum powder；The disintegrating agent is crosslinking
Sodium carboxymethylcellulose；Described adhesive is dextrin；The lubricant is stearic acid.
According to 2010 editions Chinese Pharmacopoeias, two defined methods, takes this to be used for the nanometer of diabetes and assemble the net tablet of En Gelie
It 6, is placed in 250mL beaker, about 20 DEG C of water 100mL is added, concussion measures the dispersion time limit, and the result is shown in tables 1.
According to 2010 editions Chinese Pharmacopoeias, two defined dissolution methods, the nanometer assembling grace for diabetes is carried out
Lattice arrange the dissolution determination experiment of net tablet, measure every the amount of dissolution using ultraviolet-visible spectrophotometry, calculate its dissolution rate,
It the results are shown in Table 2.
Embodiment 5
A kind of nanometer assembling net tablet of En Gelie for diabetes, is prepared with the following method:
A, it grinds: Sodium Hyaluronate and the net powder of En Gelie 1:7 in mass ratio being uniformly mixed, is subsequently placed in grinder and grinds
Mill, is ground to nanoscale, obtains nano powder.
B, self-assembly microspheres are prepared: nano powder being mixed with dispersing agent lauryl sodium sulfate, distilled water, obtains nanometre glue
Shape object；Using ultrasonic disperse, power 400W, ultrasonic time 12min；Then mesoporous silicon oxide is added, continues ultrasound point
4min is dissipated, spray drying obtains self-assembly microspheres；Wherein, the mass ratio for guaranteeing nano powder and mesoporous silicon oxide is 3.5:1；Point
The additional amount of powder lauryl sodium sulfate is the 7% of nano powder weight.
C, tabletting: self-assembly microspheres and filler, disintegrating agent, adhesive and mix lubricant are uniform, it is tabletted, it obtains
The net tablet of En Gelie is assembled to the nanometer for diabetes, wherein by weight, 28 parts of self-assembly microspheres, filler 120
Part, 12 parts of disintegrating agent, 14 parts of adhesive, 6 parts of lubricant；Wherein, the filler is selected from calcium phosphate；The disintegrating agent is to hand over
Join sodium carboxymethylcellulose；Described adhesive is dextrin；The lubricant is polyethylene glycol.
According to 2010 editions Chinese Pharmacopoeias, two defined methods, takes this to be used for the nanometer of diabetes and assemble the net tablet of En Gelie
It 6, is placed in 250mL beaker, about 20 DEG C of water 100mL is added, concussion measures the dispersion time limit, and the result is shown in tables 1.
According to 2010 editions Chinese Pharmacopoeias, two defined dissolution methods, the nanometer assembling grace for diabetes is carried out
Lattice arrange the dissolution determination experiment of net tablet, measure every the amount of dissolution using ultraviolet-visible spectrophotometry, calculate its dissolution rate,
It the results are shown in Table 2.
Embodiment 6
A kind of nanometer assembling net tablet of En Gelie for diabetes, is prepared with the following method:
A, it grinds: Sodium Hyaluronate and the net powder of En Gelie 1:8 in mass ratio being uniformly mixed, is subsequently placed in grinder and grinds
Mill, is ground to nanoscale, obtains nano powder；Guarantee the granularity of nano powder between 5~400nm.
B, self-assembly microspheres are prepared: nano powder being mixed with dispersing agent lauryl sodium sulfate, distilled water, obtains nanometre glue
Shape object；Using ultrasonic disperse, power 400W, ultrasonic time 10min；Then mesoporous silicon oxide is added, continues ultrasound point
4min is dissipated, spray drying obtains self-assembly microspheres；Wherein, the mass ratio for guaranteeing nano powder and mesoporous silicon oxide is 4:1；Dispersion
The additional amount of agent lauryl sodium sulfate is the 8% of nano powder weight.
C, tabletting: self-assembly microspheres and filler, disintegrating agent, adhesive and mix lubricant are uniform, it is tabletted, it obtains
The net tablet of En Gelie is assembled to the nanometer for diabetes, wherein by weight, 30 parts of self-assembly microspheres, filler 100
Part, 12 parts of disintegrating agent, 10 parts of adhesive, 6 parts of lubricant；Wherein, the filler is selected from starch；The disintegrating agent is crosslinking
Sodium carboxymethylcellulose；Described adhesive is dextrin；The lubricant is magnesium stearate.
According to 2010 editions Chinese Pharmacopoeias, two defined methods, takes this to be used for the nanometer of diabetes and assemble the net tablet of En Gelie
It 6, is placed in 250mL beaker, about 20 DEG C of water 100mL is added, concussion measures the dispersion time limit, and the result is shown in tables 1.
According to 2010 editions Chinese Pharmacopoeias, two defined dissolution methods, the nanometer assembling grace for diabetes is carried out
Lattice arrange the dissolution determination experiment of net tablet, measure every the amount of dissolution using ultraviolet-visible spectrophotometry, calculate its dissolution rate,
It the results are shown in Table 2.
Comparative example 1
A kind of nanometer assembling net tablet of En Gelie for diabetes, is prepared with the following method:
A, it grinds: the net powder of En Gelie being placed in grinder and is ground, nanoscale is ground to, obtains nano powder；Guarantee nano powder
Granularity between 5~400nm.
B, self-assembly microspheres are prepared: nano powder being mixed with dispersing agent lauryl sodium sulfate, distilled water, obtains nanometre glue
Shape object；Using ultrasonic disperse, power 400W, ultrasonic time 10min；Then mesoporous silicon oxide is added, continues ultrasound point
4min is dissipated, spray drying obtains self-assembly microspheres；Wherein, the mass ratio for guaranteeing nano powder and mesoporous silicon oxide is 4:1；Dispersion
The additional amount of agent lauryl sodium sulfate is the 8% of nano powder weight.
C, tabletting: self-assembly microspheres and filler, disintegrating agent, adhesive and mix lubricant are uniform, it is tabletted, it obtains
The net tablet of En Gelie is assembled to the nanometer for diabetes, wherein by weight, 30 parts of self-assembly microspheres, filler 100
Part, 12 parts of disintegrating agent, 10 parts of adhesive, 6 parts of lubricant；Wherein, the filler is selected from starch；The disintegrating agent is crosslinking
Sodium carboxymethylcellulose；Described adhesive is dextrin；The lubricant is magnesium stearate.
Comparative example 1 is to assist the net grinding distribution of En Gelie using Sodium Hyaluronate, influences dissolution efficiency.
According to 2010 editions Chinese Pharmacopoeias, two defined methods, takes this to be used for the nanometer of diabetes and assemble the net tablet of En Gelie
It 6, is placed in 250mL beaker, about 20 DEG C of water 100mL is added, concussion measures the dispersion time limit, and the result is shown in tables 1.
According to 2010 editions Chinese Pharmacopoeias, two defined dissolution methods, the nanometer assembling grace for diabetes is carried out
Lattice arrange the dissolution determination experiment of net tablet, measure every the amount of dissolution using ultraviolet-visible spectrophotometry, calculate its dissolution rate,
It the results are shown in Table 2.
Table 1
Table 2
Claims (9)
1. a kind of preparation method of the nanometer assembling net tablet of En Gelie for diabetes, which comprises the steps of:
A, it grinds: Sodium Hyaluronate and the net powder of En Gelie 1:5~10 in mass ratio being uniformly mixed, are subsequently placed in grinder
Grinding, is ground to nanoscale, obtains nano powder；
B, self-assembly microspheres are prepared: nano powder being mixed with dispersing agent, distilled water, obtains a nanometer jelly；Using ultrasonic disperse,
Power is 300~500W, and ultrasonic time is 5~15min；Then mesoporous silicon oxide is added, continues 3~5min of ultrasonic disperse,
Spray drying obtains self-assembly microspheres；Wherein, the mass ratio for guaranteeing nano powder and mesoporous silicon oxide is 2~5:1；Dispersing agent
Additional amount is the 5~10% of nano powder weight；
C, tabletting: self-assembly microspheres and filler, disintegrating agent, adhesive and mix lubricant are uniform, it is tabletted, it is used
The net tablet of En Gelie is assembled in the nanometer of diabetes, wherein by weight, 20~40 parts of self-assembly microspheres, filler 50~
200 parts, 5~20 parts of disintegrating agent, 5~20 parts of adhesive, 1~10 part of lubricant.
2. the preparation method of the nanometer assembling net tablet of En Gelie according to claim 1 for diabetes, feature exist
In: in a step, hyaluronic acid and the net powder of En Gelie 1:8 in mass ratio mixing.
3. the preparation method of the nanometer assembling net tablet of En Gelie according to claim 1 for diabetes, feature exist
In: in a step, the granularity of nano powder is 5~400nm.
4. the preparation method of the nanometer assembling net tablet of En Gelie according to claim 1 for diabetes, feature exist
In: in b step, the mass ratio of nano powder and mesoporous silicon oxide is 4:1；The additional amount of dispersing agent is the 8% of nano powder weight.
5. the preparation method of the nanometer assembling net tablet of En Gelie according to claim 1 for diabetes, feature exist
In: in b step, the power of ultrasonic disperse is 400W, and mesoporous silicon oxide is added after being 10min in ultrasonic time.
6. the preparation method of the nanometer assembling net tablet of En Gelie according to claim 1 for diabetes, feature exist
In: in b step, the dispersing agent is lauryl sodium sulfate.
7. the preparation method of the nanometer assembling net tablet of En Gelie according to claim 1 for diabetes, feature exist
In: in step c, by weight, and 30 parts of self-assembly microspheres, 100 parts of filler, 12 parts of disintegrating agent, 10 parts of adhesive, lubricant
6 parts.
8. the preparation method of the nanometer assembling net tablet of En Gelie according to claim 1 for diabetes, feature exist
In: in step c, the filler is selected from least one of starch, mannitol, sorbierite, talcum powder, calcium phosphate；It is described
Disintegrating agent is at least one of croscarmellose sodium, crospovidone；Described adhesive be dextrin, in lactose extremely
Few one kind；The lubricant is at least one of magnesium stearate, calcium stearate, zinc stearate, stearic acid, polyethylene glycol.
9. the preparation method preparation of the nanometer assembling net tablet of En Gelie according to any one of claims 1 to 8 for diabetes
The net tablet of obtained En Gelie.
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| CN111588713A (en) * | 2020-06-22 | 2020-08-28 | 广州市力鑫药业有限公司 | A Chinese medicinal composition for treating diabetes, and its preparation method |
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| CN111588713A (en) * | 2020-06-22 | 2020-08-28 | 广州市力鑫药业有限公司 | A Chinese medicinal composition for treating diabetes, and its preparation method |
| WO2021258851A1 (en) * | 2020-06-22 | 2021-12-30 | 广州市力鑫药业有限公司 | Pharmaceutical composition for treating diabetes and preparation method therefor |
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