CN105769797A - Kurarinone osmotic pump controlled release tablets and preparation method thereof - Google Patents
Kurarinone osmotic pump controlled release tablets and preparation method thereof Download PDFInfo
- Publication number
- CN105769797A CN105769797A CN201610141872.9A CN201610141872A CN105769797A CN 105769797 A CN105769797 A CN 105769797A CN 201610141872 A CN201610141872 A CN 201610141872A CN 105769797 A CN105769797 A CN 105769797A
- Authority
- CN
- China
- Prior art keywords
- kushenin
- controlled release
- osmotic pump
- pump controlled
- pellicle
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0004—Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
- A61K36/489—Sophora, e.g. necklacepod or mamani
Landscapes
- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention belongs to the technical field of medicine controlled release preparations, particularly discloses kurarinone osmotic pump controlled release tablets, and further discloses a preparation method of the kurarinone osmotic pump controlled release tablets. The kurarinone osmotic pump controlled release tablets are prepared from kurarinone tablets and protective films outside the tablets, wherein the tablets are prepared from core tablets and semipermeable films outside the core tablets; a medicine release hole is formed in each semipermeable film; the core tablets are prepared from the following raw materials in percentage by weight: 40.00%-60.00% of kurarinone, 15.00%-25.00% of sodium chloride, 20.00%-30.00% of lactose, 2.00%-5.00% of hydroxypropyl methylcellulose, 1.00%-3.50% of polyvinylpyrrolidone and 0.50%-2.00% of magnesium stearate. The kurarinone osmotic pump controlled release tablets provided by the invention can keep favorable zero-order medicine release within 20 hours, the final total release amount exceeds 70%, and part of the final total release amount exceeds 80%, so that the kurarinone osmotic pump controlled release tablets can be clinically used for treating Chronic Hepatitis B.
Description
Technical field
The present invention relates to pharmaceutical controlled release formulation technical field, particularly to a kind of kushenin osmotic pumps
Controlled release tablet, also relates to its preparation method.
Background technology
Kushenin, calls oxymatrine, Fick gunter, derives from Sophora alopecuroide.Sophora alopecuroide is
A kind of cassia leguminous plant being grown in NORTHWEST CHINA area, carries according to Shennong's Herbal, bitter
Bean or pea have heat-clearing, dampness removing, dispel the wind, desinsection, the effect such as removing toxic substances.The effective ingredient of kushenin
For oxymatrine and a small amount of N-Oxysophocarpine.Pharmacology and clinic to kushenin in recent years
Finding in research, it has the multiple pharmacological effect such as antiviral, step-down, anti-arrhythmia cordis, spy
It not that chronic hepatitis is treated achieved with good curative effect, and bad reaction is less.
For the treatment of chronic hepatitis, Western medicine mainly uses interferon medicine medicine similar with nucleosides,
The kushenin of Chinese medicine is considered as to have good hepatitis virus resisting effect and improve liver function effect,
Become the most wide variety of series products at present.For not being resistant to or be unwilling accept to do
Disturb the plain patient treating, having again antiviral indication with ucleosides, use kushenin to combine and exempt from
Epidemic disease regulating drug has preferable curative effect.Oxymatrine was in treatment virus hepatitis side in recent years
The research in face finds, oxymatrine has direct Anti-hepatitis B virus effects, can suppress glue
Former mobility and preventing and treating liver fibrosis, can block liver cell aberrant apoptosis, and oxymatrine is to reality
The property tested Mouse Liver exhaustion has protective effect.The clinical practice of oxymatrine in treating patients with chronic hepatitis hepatitis
Also obtain good efficacy, have the Chronic Hepatitis B that leucocyte and blood platelet reduce, through peroxidating
After Sophorcarpidine Treating, 1/3 patient's leucocyte and platelet recovery are normal, or have and carry in various degree
Height, before finding that Oxymatrine Treating group serotype collagen and hyaluronic acid level are relatively treated simultaneously
All it is decreased significantly, there is while showing oxymatrine in treating patients with chronic hepatitis hepatitis suppression collagen and live
Dynamic degree and fibrosis effect.On the whole, oxymatrine has suppression HCV propagation, resists
Liver fibrosis and the effect of regulation host immune.
The patent application of Publication No. CN 1480137A discloses a kind of kushenin osmotic pumps
Type controlled release preparation and preparation method thereof, said preparation has the controlled-release function of 24 hours, controlled release tablet
It is made up of kushenin, diluent, penetration enhancer, lubricant, adhesive etc., this kushenin
Controlled release tablet every tablet weight is 580mg, owing to kushenin raw material is highly dissoluble, high osmosis
Composition, is not added with stabilizer in side at which, is easy in vitro occur to dash forward in dissolution test
Release phenomenon；The hole knockout simultaneously used on pellicle is mechanical punching, the aperture difference between sheet
Different bigger, it is difficult to accomplish scale production.
The patent application of Publication No. CN 101584676A discloses a kind of Kurarinol slow-release sheet
And preparation method thereof, this sustained release tablets has a slow releasing function of 16 hours, mainly by kushenin,
Lactose, microcrystalline cellulose, PVP K-30 ethanol solution, HPMC, tristearin
Acid magnesium, stomach dissolution type coating coating powder composition, this sustained release tablets discharged about 30% at 0-2 hour,
Release about 60% in 6 hours, release about 80% in 12 hours, release about 90% in 16 hours,
Having certain slow release characteristic, but early stage release is very fast, the stable constant speed failing to realize medicine is released
Putting, i.e. Zero order release feature, patient still needs to one take medicine 2 times.
For these reasons, it is necessary to a kind of kushenin controlled release preparation is provided, makes insoluble drug release steady
Fixed, it is to avoid phenomenon of burst release occurs, and can closely constant speed release medicine, increase release controllability, make
The availability of medicine is higher.
Summary of the invention
The technical problem that present invention mainly solves is to provide a kind of kushenin osmotic pump controlled release tablet,
All keep good zero-order release in 20 hours, final Cumulative release amount all more than 70%, portion
Divide final Cumulative release amount more than 80%, controlling of chronic viral hepatitis type B can be clinically used for
Treat.
Present invention solves the technical problem that to also reside in and a kind of kushenin osmotic pump controlled release tablet is provided
Preparation method.
For solving above-mentioned technical problem, the technical solution used in the present invention is: a kind of kushenin oozes
Pump controlled-releasing tablet thoroughly, described kushenin osmotic pump controlled release tablet is by element sheet and is wrapped in described element off-chip
Moisture-proof protective film forms, and described element sheet is by label and the pellicle group being wrapped in outside described label
Become, described pellicle is provided with a release hole；
Described label is made up of the raw material of following weight percent content:
Kushenin 40.00%～60.00%,
Sodium chloride 15.00%～25.00%,
Lactose 20.00%～30.00%,
Hydroxypropyl methyl cellulose 2.00%-5.00%,
Polyvinylpyrrolidone 1.00%～3.50%,
Magnesium stearate 0.50%～2.00%；
The weight of described label is 350.00～450.00mg.
Optionally, the pellicle coating solution of described pellicle is prepared by following weight percent content
Raw material composition:
Cellulose acetate 3.50%～3.80%, PEG-4000 0.25%～0.27%, adjacent benzene
Dicarboxylate 0.35%～0.38%, water 2.18%～2.34%, acetone 93.37%～
93.56%.
Optionally, the moistureproof coating liquid preparing described moisture-proof protective film is contained by following percentage by weight
The raw material composition of amount:
IV acrylic resin 7.0%～8.0%, talcum powder 1.3%～1.5%, magnesium stearate
1.3%～1.5%, absolute ethyl alcohol 89.0%～90.4%.
Preferably, in described kushenin osmotic pump controlled release tablet the content of kushenin be 180～
210mg。
The release hole arranged on described pellicle is formed by laser boring, and pore size is
0.5mm。
Preferably, described label is made up of the raw material of following weight percent content:
Kushenin 50.00%, sodium chloride 20.00%, lactose 24.00%, hydroxypropyl methyl fiber
Element 3.75%, polyvinylpyrrolidone 1.25%, magnesium stearate 1.00%.
It is further preferred that the weight of described label is 400.00mg.
A kind of preparation method of kushenin osmotic pump controlled release tablet, including step:
(1) label is prepared
Form by following weight percent content and weigh raw material:
Kushenin 40.00%～60.00%,
Sodium chloride 15.00%～25.00%,
Lactose 20.00%～30.00%,
Hydroxypropyl methyl cellulose 2.00%-5.00%,
Polyvinylpyrrolidone 1.00%～3.50%,
Magnesium stearate 0.50%～2.00%；
Kushenin crosses 200 mesh sieves, sodium chloride, lactose, hydroxypropyl methyl cellulose, polyethylene
Pyrrolidones, magnesium stearate cross 100 mesh sieves respectively；Kushenin, sodium chloride, lactose, hydroxypropyl
Ylmethyl cellulose, polyvinylpyrrolidone mix, and cross 100 mesh sieve 2 times, after mixing,
Add appropriate anhydrous alcohol for medical use to make wetting agent stirring and make softwood, cross 30 mesh sieves and pelletize,
Obtaining wet granular, described wet granular is placed in 40 DEG C of baking ovens and is dried 5h, with the 20 whole grains of mesh sieve,
It is subsequently adding magnesium stearate lubricant to mix, obtains dry particle, by tabletting machine, pressure
Sheet punch die is the punch die in diameter 10mm aperture, weighs the dry particle of Core formulation amount, presses
Sheet operates, and prepares label, and the weight of described label is 350.00～450.00mg；
(2) pellicle coating
Preparation pellicle coating solution: prepare the pellicle coating solution of pellicle by following weight percent
Form than the raw material of content:
Cellulose acetate 3.50%～3.80%, PEG-4000 0.25%～0.27%, adjacent benzene
Dicarboxylate 0.35%～0.38%, water 2.18%～2.34%, acetone 93.37%～
93.56%；
Pellicle coating operations is carried out in coating pan, and coating process parameters is: EAT
40～45 DEG C, engine speed 8～12r/min, air intake rotating speed 1100r/min, air draft rotating speed 1800
R/min, peristaltic pump rotating speed 8.0～11.0r/min, atomizing pressure 0.1MPa, coating operations completes
After in 40 DEG C of baking ovens place 5h；
(3) laser boring
Using laser-beam drilling machine, punching pore size is 0.5mm；
(4) moisture-proof protective film coating
Preparation moistureproof coating liquid: prepare the moistureproof coating liquid of moisture-proof protective film by following weight percent
Form than the raw material of content:
IV acrylic resin 7.0%～8.0%, talcum powder 1.3%～1.5%, magnesium stearate
1.3%～1.5%, absolute ethyl alcohol 89.0%～90.4%；
Moistureproof coating operation carry out in coating pan, coating process parameters is: EAT 47～
53 DEG C, engine speed 8～12r/min, air intake rotating speed 1100r/min, air draft rotating speed 1800
R/min, peristaltic pump rotating speed 2.0～3.0r/min, atomizing pressure 0.15MPa, coating operations is complete
In 40 DEG C of baking ovens, place 5h after one-tenth, obtain kushenin osmotic pump controlled release tablet.
Preferably, described label is made up of the raw material of following weight percent content:
Kushenin 50.00%, sodium chloride 20.00%, lactose 24.00%, hydroxypropyl methyl fiber
Element 3.75%, polyvinylpyrrolidone 1.25%, magnesium stearate 1.00%.
It is further preferred that the weight of described label is 400.00mg.
In research process, applicant has investigated kushenin osmotic pump controlled-releasing by single factor experiment
In tablet recipe, auxiliary material selects and the key factor such as the selection of ratio, coating solution components and proportioning thereof,
Finally draw compounding rational kushenin osmotic pump controlled-releasing tablet recipe, can make medicine in 24h
Nearly constant release.The invention has the beneficial effects as follows: the kushenin osmotic pump controlled-releasing that the present invention provides
Sheet, after human body provides kushenin, takes, sustainable stably release 20 hours, release per hour
High-volume being about the 4.0%～5.0% of total content, controllability is higher, and availability is higher.At 24h
Interior nearly constant release medicine, by the drug release process of nearly constant speed, suppression collagen is lived in vivo
Dynamic degree and preventing and treating liver fibrosis, thus play the effect of anti-hepatitis B virus, effectively prevent
The peak valley phenomenon of medicine blood concentration, alleviates the toxicity of medicine, decreases the clothes of patient
Medicine number of times, patient only needs the most once, easily takes medicine on time, substantially increases patient's
Compliance, has adapted to the needs of clinical development.
The kushenin osmotic pump controlled release tablet that the present invention provides, after patient takes, controlled release tablet outer layer
Moisture-proof protective film be disintegrated rapidly in gastric juice, the hydrone in alimentary canal through pellicle enter
Label, makes label progressively dissolve, thus creates permeable pressure head, led to together with medicine by lysate
Release hole on semi-permeable membrane is released and is entered intestines and stomach, owing to kushenin is at enteron aisle different parts
There was no significant difference in absorption in (duodenum, jejunum, ileum and colon), therefore medicine
Can be efficiently absorbed after the nearly constant release of different parts in vivo.
Tests prove that, the kushenin osmotic pump controlled release tablet that the present invention provides is equal in 20 hours
Keeping good zero-order release, final Cumulative release amount is all more than 70%, and part is released by final adding up
High-volume more than 80%, the treatment of chronic viral hepatitis type B can be clinically used for.
Accompanying drawing explanation
Fig. 1 is the structural representation of the kushenin osmotic pump controlled release tablet that embodiment of the present invention 1-6 provides
Figure；
Fig. 2 is the drug release profiles of the kushenin osmotic pump controlled release tablet that embodiment of the present invention 1-6 provides
Comparison diagram；
Fig. 3 is the kushenin osmotic pump controlled release tablet prepared by Core formulation 1-Core formulation 3 respectively
Releasing curve diagram；
Fig. 4 is the kushenin osmotic pump controlled release tablet prepared by Core formulation 4-Core formulation 6 respectively
Releasing curve diagram；
Fig. 5 is the kushenin osmotic pump controlled-releasing prepared by Core formulation 7, Core formulation 8 respectively
The releasing curve diagram of sheet；
Fig. 6 is the kushenin osmotic pump controlled-releasing prepared by Core formulation 9-Core formulation 11 respectively
The releasing curve diagram of sheet；
Fig. 7 is the kushenin osmotic pump controlled-releasing prepared by Core formulation 12-Core formulation 14 respectively
The releasing curve diagram of sheet；
Fig. 8 is to be prepared by pellicle coating fluid prescription 1, pellicle coating fluid prescription 2 respectively
The releasing curve diagram of kushenin osmotic pump controlled release tablet；
Fig. 9 is to be prepared by pellicle coating fluid prescription 3, pellicle coating fluid prescription 4 respectively
The releasing curve diagram of kushenin osmotic pump controlled release tablet；
Figure 10 is to be prepared by pellicle coating fluid prescription 5-pellicle coating fluid prescription 7 respectively
The releasing curve diagram of kushenin osmotic pump controlled release tablet；
After Figure 11 is kushenin osmotic pump controlled release tablet and the moistureproof coating not carrying out moistureproof coating
Kushenin osmotic pump controlled release tablet vitro release comparison diagram.
Detailed description of the invention
Below by specific embodiment, technical scheme is described in detail.
Embodiment 1
As shown in Figure 1, a kind of kushenin osmotic pump controlled release tablet, by element sheet be wrapped in element off-chip
Moisture-proof protective film 4 form, element sheet is by label 2 and the pellicle 3 groups that is wrapped in outside label 2
Become, pellicle 3 is provided with a release hole 1；Release hole 1 is formed by laser boring,
Pore size is 0.5mm.
Label 2 is made up of the raw material of following weight percent content:
Kushenin 40.00%, sodium chloride 21.00%, lactose 30.00%, hydroxypropyl methyl fiber
Element 5.00%, polyvinylpyrrolidone 3.50%, magnesium stearate 0.50%；The weight of label is
450.00mg。
Prepare the pellicle coating solution raw material group by following weight percent content of pellicle 3
Become:
Cellulose acetate 3.50%, PEG-4000 0.25%, diethyl phthalate
0.35%, water 2.34%, acetone 93.56%.
Prepare the moistureproof coating liquid raw material by following weight percent content of moisture-proof protective film 4
Composition:
IV acrylic resin 7.0%, talcum powder 1.3%, magnesium stearate 1.3%, anhydrous second
Alcohol 90.4%.
The preparation method of the present embodiment kushenin osmotic pump controlled release tablet, including step:
(1) label is prepared
Weighing each raw material by above weight percent content composition, kushenin crosses 200 mesh sieves, chlorine
Change sodium, lactose, hydroxypropyl methyl cellulose, polyvinylpyrrolidone, magnesium stearate mistake respectively
100 mesh sieves；Kushenin, sodium chloride, lactose, hydroxypropyl methyl cellulose, polyvinyl pyrrole
Alkanone mixes, and crosses 100 mesh sieve 2 times, after mixing, adds appropriate medicinal anhydrous second
Alcohol is made wetting agent stirring and is made softwood, crosses 30 mesh sieves and pelletizes, obtains wet granular, and wet granular exists
Place in 40 DEG C of baking ovens and be dried 5h, with the 20 whole grains of mesh sieve, be subsequently adding magnesium stearate lubricant
Mixing, obtain dry particle, with tabletting machine, tableting die is diameter 10mm aperture
Punch die, weigh the dry particle of Core formulation amount, carry out sheeting operation, prepare label, label
Weight be 450.00mg；
(2) pellicle coating
Prepare pellicle coating solution according to the composition of the present embodiment pellicle coating solution, then enter
Row enrobing processes, pellicle coating operations is carried out in coating pan, and coating process parameters is: enter
Air temperature 45 DEG C, engine speed 12r/min, air intake rotating speed 1100r/min, air draft rotating speed 1800
R/min, peristaltic pump rotating speed 11.0r/min, atomizing pressure 0.1MPa, coating operations complete after in
5h is placed in 40 DEG C of baking ovens；
(3) laser boring
Using laser-beam drilling machine, punching pore size is 0.5mm；
(4) moisture-proof protective film coating
Prepare moistureproof coating liquid according to the composition of the present embodiment moistureproof coating liquid, then wrap
Clothing operation, moistureproof coating operation is carried out in coating pan, and coating process parameters is: EAT
47 DEG C, engine speed 8r/min, air intake rotating speed 1100r/min, air draft rotating speed 1800r/min,
Peristaltic pump rotating speed 2.0r/min, atomizing pressure 0.15MPa, coating operations complete after in 40 DEG C of bakings
Place 5h in case, obtain kushenin osmotic pump controlled release tablet.
Embodiment 2
As shown in Figure 1, a kind of kushenin osmotic pump controlled release tablet, by element sheet be wrapped in element off-chip
Moisture-proof protective film 4 form, element sheet is by label 2 and the pellicle 3 groups that is wrapped in outside label 2
Become, pellicle 3 is provided with a release hole 1；Release hole 1 is formed by laser boring,
Pore size is 0.5mm.
Label 2 is made up of the raw material of following weight percent content:
Kushenin 40.00%, sodium chloride 25.00%, lactose 26.00%, hydroxypropyl methyl fiber
Element 4.75%, polyvinylpyrrolidone 2.75%, magnesium stearate 1.50%；The weight of label is
450.00mg。
Prepare the pellicle coating solution raw material group by following weight percent content of pellicle 3
Become:
Cellulose acetate 3.50%, PEG-4000 0.25%, diethyl phthalate
0.35%, water 2.34%, acetone 93.56%.
Prepare the moistureproof coating liquid raw material by following weight percent content of moisture-proof protective film 4
Composition:
IV acrylic resin 7.0%, talcum powder 1.3%, magnesium stearate 1.3%, anhydrous second
Alcohol 90.4%.
Embodiment 3
As shown in Figure 1, a kind of kushenin osmotic pump controlled release tablet, by element sheet be wrapped in element off-chip
Moisture-proof protective film 4 form, element sheet is by label 2 and the pellicle 3 groups that is wrapped in outside label 2
Become, pellicle 3 is provided with a release hole 1；Release hole 1 is formed by laser boring,
Pore size is 0.5mm.
Label 2 is made up of the raw material of following weight percent content:
Kushenin 60.00%, sodium chloride 15.00%, lactose 20.00%, hydroxypropyl methyl fiber
Element 2.75%, polyvinylpyrrolidone 1.25%, magnesium stearate 1.00%；The weight of label is
350.00mg。
Prepare the pellicle coating solution raw material group by following weight percent content of pellicle 3
Become:
Cellulose acetate 3.80%, PEG-4000 0.27%, diethyl phthalate
0.38%, water 2.18%, acetone 93.37%.
Prepare the moistureproof coating liquid raw material by following weight percent content of moisture-proof protective film 4
Composition:
IV acrylic resin 8.0%, talcum powder 1.5%, magnesium stearate 1.5%, anhydrous second
Alcohol 89.0%.
Embodiment 4
As shown in Figure 1, a kind of kushenin osmotic pump controlled release tablet, by element sheet be wrapped in element off-chip
Moisture-proof protective film 4 form, element sheet is by label 2 and the pellicle 3 groups that is wrapped in outside label 2
Become, pellicle 3 is provided with a release hole 1；Release hole 1 is formed by laser boring,
Pore size is 0.5mm.
Label 2 is made up of the raw material of following weight percent content:
Kushenin 60.00%, sodium chloride 15.00%, lactose 20.00%, hydroxypropyl methyl fiber
Element 2.00%, polyvinylpyrrolidone 1.00%, magnesium stearate 2.00%；The weight of label is
350.00mg。
Prepare the pellicle coating solution raw material group by following weight percent content of pellicle 3
Become:
Cellulose acetate 3.80%, PEG-4000 0.27%, diethyl phthalate
0.38%, water 2.18%, acetone 93.37%.
Prepare the moistureproof coating liquid raw material by following weight percent content of moisture-proof protective film 4
Composition:
IV acrylic resin 8.0%, talcum powder 1.5%, magnesium stearate 1.5%, anhydrous second
Alcohol 89.0%.
Embodiment 5
As shown in Figure 1, a kind of kushenin osmotic pump controlled release tablet, by element sheet be wrapped in element off-chip
Moisture-proof protective film 4 form, element sheet is by label 2 and the pellicle 3 groups that is wrapped in outside label 2
Become, pellicle 3 is provided with a release hole 1；Release hole 1 is formed by laser boring,
Pore size is 0.5mm.
Label 2 is made up of the raw material of following weight percent content:
Kushenin 50.00%, sodium chloride 20.00%, lactose 24.00%, hydroxypropyl methyl fiber
Element 3.75%, polyvinylpyrrolidone 1.25%, magnesium stearate 1.00%；The weight of label is
400.00mg。
Prepare the pellicle coating solution raw material group by following weight percent content of pellicle 3
Become:
Cellulose acetate 3.60%, PEG-4000 0.26%, diethyl phthalate
0.36%, water 2.23%, acetone 93.55%.
Prepare the moistureproof coating liquid raw material by following weight percent content of moisture-proof protective film 4
Composition:
IV acrylic resin 7.5%, talcum powder 1.4%, magnesium stearate 1.4%, anhydrous second
Alcohol 89.7%.
Embodiment 6
As shown in Figure 1, a kind of kushenin osmotic pump controlled release tablet, by element sheet be wrapped in element off-chip
Moisture-proof protective film 4 form, element sheet is by label 2 and the pellicle 3 groups that is wrapped in outside label 2
Become, pellicle 3 is provided with a release hole 1；Release hole 1 is formed by laser boring,
Pore size is 0.5mm.
Label 2 is made up of the raw material of following weight percent content:
Kushenin 50.00%, sodium chloride 18.00%, lactose 27.00%, hydroxypropyl methyl fiber
Element 2.50%, polyvinylpyrrolidone 1.50%, magnesium stearate 1.00%；The weight of label is
400.00mg。
Prepare the pellicle coating solution raw material group by following weight percent content of pellicle 3
Become:
Cellulose acetate 3.60%, PEG-4000 0.26%, diethyl phthalate
0.36%, water 2.23%, acetone 93.55%.
Prepare the moistureproof coating liquid raw material by following weight percent content of moisture-proof protective film 4
Composition:
IV acrylic resin 7.5%, talcum powder 1.4%, magnesium stearate 1.4%, anhydrous second
Alcohol 89.7%.
The preparation method of the kushenin osmotic pump controlled release tablet that embodiment 2-embodiment 6 provides can be joined
Carrying out according to embodiment 1, wherein parameter EAT, engine speed, peristaltic pump rotating speed can wanted
It is adjusted in the range of asking selecting, all can implement.
Test example
1, the kushenin osmotic pump controlled release tablet effect test that embodiment 1-6 provides
The kushenin osmotic pump controlled release tablet providing embodiment of the present invention 1-6 has carried out insoluble drug release
Test, the curve comparison figure obtained is as shown in Figure 2.As seen from Figure 2, each embodiment is bitter
Ginseng element osmotic pump controlled release tablet all kept good zero-order release in 20 hours, and final adding up is released
The most all more than 70%, embodiment 5, embodiment 6 final Cumulative release amount more than 80%.
The most sustainable stably release 20 hours after taking, per hour burst size be about total content 4.0%～
5.0%, controllability is higher, and availability is higher.
The kushenin osmotic pump controlled release tablet that embodiment of the present invention 1-6 provides complies fully with quality control
Requirement, its vitro release measures with reference to drug release determination method (Chinese Pharmacopoeia version two in 2010
Portion's annex XD the first method) and dissolution method (Chinese Pharmacopoeia two annex of version in 2010
XC the first method) it is measured, it is desirable within 2 hours, release is 5%～15%, release in 6 hours
Degree is 20%～30%, and within 12 hours, release is 45%～65%, and within 20 hours, release is
70%～85%, within 24 hours, release must not be less than 80%.
By the drug release process of nearly constant speed, suppression collagen mobility and preventing and treating liver are fine in vivo
Dimensionization, thus play the effect of anti-hepatitis B virus, effectively prevent medicine blood concentration
Peak valley phenomenon, alleviates the toxicity of medicine, decreases the medicining times of patient, and patient is only
Need the most once, easily take medicine on time, substantially increase the compliance of patient, adapt to
The needs of clinical development.
2, Core formulation, pellicle coating fluid prescription and the test of moistureproof coating liquid prescription screening
2.1 Core formulation screenings
Firstly the need of explanation, in Core formulation screening process, pellicle coating fluid prescription is:
Cellulose acetate 3.50%, PEG-4000 0.25%, diethyl phthalate 0.35%,
Water 2.34%, acetone 93.56%；Moistureproof coating liquid prescription is: IV acrylic resin 7.5%,
Talcum powder 1.4%, magnesium stearate 1.4%, absolute ethyl alcohol 89.7%；More than it is weight percent
Compare content.
All with final accumulative releasing degree and the linear analogue coefficients R of In-vitro release curves2For investigating
Target.
2.1.1 the screening of osmotically active composition in label
In Core formulation, individually select lactose, mannitol, sodium chloride, select hydroxypropyl
Methylcellulose (HPMC-K4M), as retarding agent, selects magnesium stearate as lubricant
Carrying out pelletizing press sheet, concrete prescription is shown in Table 1.Prepared by Core formulation 1-Core formulation 3 respectively
Kushenin osmotic pump controlled release tablet release profiles as shown in Figure 3.
Table 1 Core formulation 1-3
| Supplementary material title | Prescription 1/mg | Prescription 2/mg | Prescription 3/mg |
| Kushenin | 200 | 200 | 200 |
| Sodium chloride | 180 | - | - |
| Lactose | - | 180 | - |
| Mannitol | - | - | 180 |
| HPMC-K4M | 16 | 16 | 16 |
| Magnesium stearate | 4 | 4 | 4 |
| Add up to | 400 | 400 | 400 |
Release result according to Fig. 3, selecting sodium chloride, lactose is osmotic pumps active component
Kushenin osmotic pump controlled release tablet release profiles basically identical, and select mannitol be osmotic pumps live
Property composition the release of kushenin osmotic pump controlled release tablet very fast, 12h has discharged completely, in order to adjust
Compressing tablet loading and hardness level, may select sodium chloride with lactose with the use of debugging.
2.1.2 osmotically active composition sodium chloride and the screening of galactose ratio in label
By consulting data of literatures, it is prepared as oozing of osmotic pump controlled release tablet at ease of solubility composition
Active component content should be the 35%～55% of label gross weight thoroughly, and the infiltration of this Formulation is lived
Property composition total amount is as the criterion with 45% (180mg), carries out examining of sodium chloride and lactose different proportion
Examining, concrete prescription is shown in Table 2.The kushenin prepared by Core formulation 4-Core formulation 6 respectively oozes
The release profiles of pump controlled-releasing tablet is as shown in Figure 4 thoroughly.
Table 2 Core formulation 4-6
| Supplementary material title | Prescription 4/mg | Prescription 5/mg | Prescription 6/mg |
| Kushenin | 200 | 200 | 200 |
| Sodium chloride | 60 | 90 | 120 |
| Lactose | 120 | 90 | 60 |
| HPMC-K4M | 16 | 16 | 16 |
| Magnesium stearate | 4 | 4 | 4 |
| Add up to | 400 | 400 | 400 |
Release result according to Fig. 4, when in prescription 4, lactose and sodium chloride ratio are 2: 1,
Release is linear preferably, but release is the most on the low side compared with latter two prescription, but still at tolerance interval
Interior (more than 80%)；And when in prescription 6, the ratio of lactose and sodium chloride is 1: 2, release
Preferably, the linearly dependent coefficient R but in 24h2The most not ideal；Comparatively speaking, breast is worked as
Sugar with sodium chloride ratio be 1: 1 time, release with linearly all meet expection.Therefore, sodium chloride
And the proportion of lactose should be chosen as between 1: 1～1: 2.
2.1.3 the screening of retarding agent composition in label
Select hydroxypropyl methyl cellulose (HPMC-K4M) and polyvinylpyrrolidone respectively
(PVP-K30), selecting sodium chloride (18.0%), lactose (27.0%) is osmotically active composition,
Selecting magnesium stearate to carry out pelletizing press sheet as lubricant, concrete prescription is shown in Table 3.Respectively by sheet
The release profiles such as Fig. 5 of the kushenin osmotic pump controlled release tablet that core prescription 7, Core formulation 8 prepare
Shown in.
Table 3 Core formulation 7-8
Release result according to Fig. 5, selects HPMC-K4M as the prescription of retarding agent
Overall release is less than the latter, and the hardness when compressing tablet is less than normal, is susceptible to capping phenomenon, but
Its linearly dependent coefficient R2It is 0.9867, the most preferably；And select PVP-K30 as retardance
The overall release of prescription of agent be higher than the former, but in vitro dissolution test time be found to have at part
Square piece there occurs prominent releasing at 6h, thus improves overall accumulative releasing degree；Through consulting relevant literary composition
Offering, ease of solubility main ingredient is easier to when making sustained-release preparation phenomenon of burst release.Examination through us
Test research to find, add appropriate HPMC-K4M and can effectively prevent prescription from dashing forward as retarding agent
Release, although and PVP-K30 retardation is weak compared with HPMC-K4M, but have in pelletization
Effect act as the effect of adhesive, and therefore both are indispensable.Further, also can suitably adjust
Both ratios of examination are investigated.
2.1.4 retarding agent composition HPMC-K4M and the screening of PVP-K30 ratio in label
By consulting data of literatures, it is prepared as the resistance of osmotic pump controlled release tablet at ease of solubility composition
Stagnant stabiliser content should be less than the 10% of label gross weight, the retarding agent total amount of this Formulation
It is as the criterion with 4% (16mg), carries out the investigation of HPMC-K4M Yu PVP-K30 different proportion,
Concrete prescription is shown in Table 4.The kushenin infiltration prepared by Core formulation 9-Core formulation 11 respectively
The release profiles of pump controlled-releasing tablet is as shown in Figure 6.
Table 4 Core formulation 9-11
Release result according to Fig. 6, prescription 9 and the release profiles basic of prescription 10
Cause, its release and linearly dependent coefficient R2Also in desired extent, but prescription 11 then occurs
Phenomenon of burst release, therefore to present local release too high and discharge at 20h for its release profiles
Phenomenon completely.It follows that the ratio of HPMC-K4M Yu PVP-K30 in Core formulation
Should control in the range of 5: 3～3: 1.
2.1.5 the screening of lubricant in label
Core formulation is selected respectively magnesium stearate, silica, talcum powder as lubricant,
Selecting sodium chloride (18.0%), lactose (27.0%) is osmotically active composition, selects HPMC-K4M
(3.75%), polyvinylpyrrolidone PVP-K30 (1.25%) be adhesive, concrete prescription
It is shown in Table 5.The kushenin osmotic pump controlled release tablet prepared by Core formulation 12-Core formulation 14 respectively
Release profiles as shown in Figure 7.
Table 5 Core formulation 12-14
Release result according to Fig. 7, selects the kushenin osmotic pumps of three kinds of lubricants respectively
The release profiles of controlled release tablet is essentially identical, measures its angle of repose also without significant difference after total mixed,
In order to save production cost, select magnesium stearate as lubricant.
2.2 pellicle coating fluid prescription screenings
Firstly the need of explanation, in pellicle coating fluid prescription screening process, Core formulation is:
Kushenin 49.00%, sodium chloride 18.00%, lactose 27.00%, hydroxypropyl methyl cellulose
3.75%, polyvinylpyrrolidone 1.25%, magnesium stearate 1.00%, be more than weight hundred
Proportion by subtraction content；The weight of label is 400.00mg.Moistureproof coating liquid prescription is: No. IV third
Olefin(e) acid resin 7.5%, talcum powder 1.4%, magnesium stearate 1.4%, absolute ethyl alcohol 89.7%.
All with final accumulative releasing degree and the linear analogue coefficients R of In-vitro release curves2For investigating
Target.
2.2.1 the screening of pore-foaming agent in pellicle coating solution
In pellicle coating solution, pore-foaming agent is selected PEG-4000 (PEG 1500) respectively, is gathered
Ethylene glycol-4000 (PEG 4000), is filmogen with cellulose acetate (CA), and adds
Entering plasticizer phthalic acid diethylester (DEP), concrete prescription is shown in Table 6.Respectively by pellicle
Releasing of the kushenin osmotic pump controlled release tablet that coating fluid prescription 1, pellicle coating fluid prescription 2 prepare
Put curve as shown in Figure 8.
Table 6 pellicle coating fluid prescription 1-2
| Supplementary material title | Prescription 1 | Prescription 2 |
| CA | 22.9g | 22.9g |
| PEG 4000 | 2.80g | - |
| PEG 1500 | - | 2.80g |
| DEP | 2.29g | 2.29g |
| Acetone | 750mL | 750mL |
| Water | 10mL | 10mL |
Release result according to Fig. 8, selects PEG 4000 to carry out film bag for pore-foaming agent
The overall release of prescription of clothing is higher than the latter, it may be possible to it has more preferable hydrophilic interaction, causes
Hole effect is more preferable, and PEG 1500 in use finds that it easily softens, during weighing
Inconvenience, thus select PEG 4000 as pore-foaming agent.
2.2.2 the screening of plasticizer in pellicle coating solution
In this screening pellicle coating fluid prescription, one is added diethyl phthalate
(DEP), another is then without DEP, and both of which cellulose acetate (CA) is film forming
Material, adds pore-foaming agent PEG 4000, and concrete prescription is shown in Table 7.Respectively by pellicle coating solution
The release profiles of the kushenin osmotic pump controlled release tablet that prescription 3, pellicle coating fluid prescription 4 prepare
As shown in Figure 9.
Table 7 pellicle coating fluid prescription 3-4
| Supplementary material title | Prescription 3 | Prescription 4 |
| CA | 22.9g | 22.9g |
| PEG 4000 | 2.80g | 2.80g |
| DEP | 2.29g | - |
| Acetone | 750mL | 750mL |
| Water | 10mL | 10mL |
Release result according to Fig. 9, adds plasticizer DEP's in pellicle coating solution
Prescription discharges linear R2It is 0.9784, and the prescription release being not added with plasticizer DEP is linear
R2It is 0.9217, release can be effectively improved after therefore adding plasticizer linear so that it is release more connects
Nearly Zero order release, therefore selects in pellicle coating fluid prescription to add a small amount of DEP as plasticising
Agent.
2.2.3 the screening of pore-foaming agent consumption in pellicle coating solution
By inquiry pertinent literature, the pore-foaming agent common dose solids content percentage in film coating
Ratio is 6.0%～20.0% (being converted into total content percentage about 0.20%～0.60%).This sieve
Choosing selects solids content percentage 6.0%, 10.0% and 15.0% to carry out film coating (folding respectively
Synthesis total content percentage is respectively 0.20%, 0.25% and 0.30%), use cellulose acetate
(CA) it is filmogen, and adds plasticizer phthalic acid diethylester (DEP), specifically
Prescription is shown in Table 8.Prepared by pellicle coating fluid prescription 5-pellicle coating fluid prescription 7 respectively
The release profiles of kushenin osmotic pump controlled release tablet is as shown in Figure 10.
Table 8 pellicle coating fluid prescription 5-7
| Supplementary material title | Prescription 5 | Prescription 6 | Prescription 7 |
| CA | 24.02g | 22.91g | 22.51g |
| PEG 4000 | 1.68g | 2.80g | 4.20g |
| DEP | 2.29g | 2.29g | 2.29g |
| Acetone | 750mL | 750mL | 750mL |
| Water | 10mL | 10mL | 10mL |
Release result according to Figure 10, pore-foaming agent PEG 4000 in pellicle coating solution
Solids content percentage vitro release is had large effect, when consolidating of PEG 4000
When body burden percentage is 6%, overall release is significantly lower than the former, contains mainly due to it
Measuring relatively low, pore effect is on the weak side；And when the solids content percentage of PEG 4000 is 15%,
Overall release is fast, and 12～16h discharge completely the most substantially, it is impossible to reach 24h Zero order release
Effect；Comparatively speaking, when the solids content percentage of PEG 4000 is 10%, totally
Discharge preferable with release.Therefore by comparing, the solids content hundred of EG 4000 is selected
Proportion by subtraction be 10% (be converted into total content percentage and be about 0.25%) be preferable.
2.3 moistureproof coating liquid prescription screenings
Moistureproof coating liquid prescription is selected: IV acrylic resin 7.0%～8.0%, talcum powder
1.3%～1.5%, magnesium stearate 1.3%～1.5%, absolute ethyl alcohol 89.0%～90.4%；Coating
Parameter is: EAT 47～53 DEG C, engine speed 8～12r/min, air intake rotating speed 1100
R/min, air draft rotating speed 1800r/min, peristaltic pump rotating speed 2.0～3.0r/min, atomizing pressure
0.15MPa, through actual coating operations, observes finished product sheet, and its surface color is uniform,
There is preferable moisture proof performance, carry out vitro release pair with the prescription not carrying out moistureproof coating
Ratio, its release profiles comparison diagram is as shown in Figure 11.
Release result according to Figure 11, after moistureproof coating, the external of kushenin controlled release tablet is released
Putting curve not to be affected, two release profiles keep consistent substantially, and this moistureproof coating is described
Place can make tablet appearance keep attractive in appearance, has humidity resistance concurrently and does not affect its release.
This kushenin osmotic pump controlled release tablet is by wrapping up one layer of pellicle in advance outside drug core
Coatings, and in pellicle coatings, carry out laser boring, on film-coating, finally wrap up one
Layer moistureproof coating layer, thus prevent label moisture absorption to lose efficacy.After the entrance of this controlled release tablet is internal, first
First moistureproof coating layer is directly dissolved and digests, body fluid by the film-coated aperture of pellicle with
And pellicle enters label, the sodium chloride in label is fabulous with lactose water solubility, so that in sheet
Osmotic pressure apparently higher than off-chip, motive force produced by this permeable pressure head allows medicament to hold
Continue and stably discharge from aperture, by the auxiliary material proportion in single factor exploration prescription, bag
The key factors such as the proportioning of clothing liquid, finally can make medicine nearly constant release in 24h.
The above-mentioned description to embodiment is for the ease of those skilled in the art's energy
Enough understanding and application this case technology, those skilled in the art obviously can be easily to these embodiments
Make various amendment, and General Principle described herein be applied in other embodiments without
Through performing creative labour.Therefore, this case is not limited to above example, those skilled in the art
Member should be in the protection of this case according to the announcement of this case, the improvement made for this case and amendment
In the range of.
Claims (10)
1. a kushenin osmotic pump controlled release tablet, it is characterised in that described kushenin osmotic pumps
Controlled release tablet is made up of element sheet and the moisture-proof protective film being wrapped in described element off-chip, and described element sheet is by sheet
Core and the pellicle composition being wrapped in outside described label, described pellicle is provided with a release
Hole；
Described label is made up of the raw material of following weight percent content:
Kushenin 40.00%～60.00%,
Sodium chloride 15.00%～25.00%,
Lactose 20.00%～30.00%,
Hydroxypropyl methyl cellulose 2.00%-5.00%,
Polyvinylpyrrolidone 1.00%～3.50%,
Magnesium stearate 0.50%～2.00%；
The weight of described label is 350.00～450.00mg.
Kushenin osmotic pump controlled release tablet the most according to claim 1, it is characterised in that
The pellicle coating solution preparing described pellicle is made up of the raw material of following weight percent content:
Cellulose acetate 3.50%～3.80%, PEG-4000 0.25%～0.27%, adjacent benzene
Dicarboxylate 0.35%～0.38%, water 2.18%～2.34%, acetone 93.37%～
93.56%.
Kushenin osmotic pump controlled release tablet the most according to claim 1 and 2, its feature exists
In, prepare the moistureproof coating liquid raw material by following weight percent content of described moisture-proof protective film
Composition:
IV acrylic resin 7.0%～8.0%, talcum powder 1.3%～1.5%, magnesium stearate
1.3%～1.5%, absolute ethyl alcohol 89.0%～90.4%.
Kushenin osmotic pump controlled release tablet the most according to claim 3, it is characterised in that
In described kushenin osmotic pump controlled release tablet, the content of kushenin is 180～210mg.
Kushenin osmotic pump controlled release tablet the most according to claim 4, it is characterised in that
The release hole arranged on described pellicle is formed by laser boring, and pore size is 0.5mm.
Kushenin osmotic pump controlled release tablet the most according to claim 5, it is characterised in that
Described label is made up of the raw material of following weight percent content:
Kushenin 50.00%, sodium chloride 20.00%, lactose 24.00%, hydroxypropyl methyl fiber
Element 3.75%, polyvinylpyrrolidone 1.25%, magnesium stearate 1.00%.
Kushenin osmotic pump controlled release tablet the most according to claim 6, it is characterised in that
The weight of described label is 400.00mg.
8. the preparation method of a kushenin osmotic pump controlled release tablet, it is characterised in that include step
Rapid:
(1) label is prepared
Form by following weight percent content and weigh raw material:
Kushenin 40.00%～60.00%,
Sodium chloride 15.00%～25.00%,
Lactose 20.00%～30.00%,
Hydroxypropyl methyl cellulose 2.00%-5.00%,
Polyvinylpyrrolidone 1.00%～3.50%,
Magnesium stearate 0.50%～2.00%；
Kushenin crosses 200 mesh sieves, sodium chloride, lactose, hydroxypropyl methyl cellulose, polyethylene
Pyrrolidones, magnesium stearate cross 100 mesh sieves respectively；Kushenin, sodium chloride, lactose, hydroxypropyl
Ylmethyl cellulose, polyvinylpyrrolidone mix, and cross 100 mesh sieve 2 times, after mixing,
Add anhydrous alcohol for medical use to make wetting agent stirring and make softwood, cross 30 mesh sieves and pelletize, obtain
Wet granular, described wet granular is placed in 40 DEG C of baking ovens and is dried 5h, with the 20 whole grains of mesh sieve, so
Rear addition magnesium stearate lubricant mixes, and with tabletting machine after mixing, tableting die is
The punch die in diameter 10mm aperture, prepare label, the weight of described label be 350.00～
450.00mg；
(2) pellicle coating
Preparation pellicle coating solution: prepare the pellicle coating solution of pellicle by following weight percent
Form than the raw material of content:
Cellulose acetate 3.50%～3.80%, PEG-4000 0.25%～0.27%, adjacent benzene
Dicarboxylate 0.35%～0.38%, water 2.18%～2.34%, acetone 93.37%～
93.56%；
Pellicle coating operations is carried out in coating pan, and coating process parameters is: EAT
40～45 DEG C, engine speed 8～12r/min, air intake rotating speed 1100r/min, air draft rotating speed 1800
R/min, peristaltic pump rotating speed 8.0～11.0r/min, atomizing pressure 0.1MPa, coating operations completes
After in 40 DEG C of baking ovens place 5h；
(3) laser boring
Using laser-beam drilling machine, punching pore size is 0.5mm；
(4) moisture-proof protective film coating
Preparation moistureproof coating liquid: prepare the moistureproof coating liquid of moisture-proof protective film by following weight percent
Form than the raw material of content:
IV acrylic resin 7.0%～8.0%, talcum powder 1.3%～1.5%, magnesium stearate
1.3%～1.5%, absolute ethyl alcohol 89.0%～90.4%；
Moistureproof coating operation carry out in coating pan, coating process parameters is: EAT 47～
53 DEG C, engine speed 8～12r/min, air intake rotating speed 1100r/min, air draft rotating speed 1800
R/min, peristaltic pump rotating speed 2.0～3.0r/min, atomizing pressure 0.15MPa, coating operations is complete
In 40 DEG C of baking ovens, place 5h after one-tenth, obtain kushenin osmotic pump controlled release tablet.
The preparation method of kushenin osmotic pump controlled release tablet the most according to claim 8, its
Being characterised by, described label is made up of the raw material of following weight percent content:
Kushenin 50.00%, sodium chloride 20.00%, lactose 24.00%, hydroxypropyl methyl fiber
Element 3.75%, polyvinylpyrrolidone 1.25%, magnesium stearate 1.00%.
The preparation method of kushenin osmotic pump controlled release tablet the most according to claim 9, its
Being characterised by, the weight of described label is 400.00mg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610141872.9A CN105769797B (en) | 2016-03-11 | 2016-03-11 | A kind of kushenin osmotic pump controlled release tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610141872.9A CN105769797B (en) | 2016-03-11 | 2016-03-11 | A kind of kushenin osmotic pump controlled release tablet and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105769797A true CN105769797A (en) | 2016-07-20 |
| CN105769797B CN105769797B (en) | 2018-10-02 |
Family
ID=56393492
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610141872.9A Active CN105769797B (en) | 2016-03-11 | 2016-03-11 | A kind of kushenin osmotic pump controlled release tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105769797B (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1480137A (en) * | 2003-07-04 | 2004-03-10 | 沈阳药科大学 | Osmotic pump type controlled release preparation of kurarinone and its preparing method |
-
2016
- 2016-03-11 CN CN201610141872.9A patent/CN105769797B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1480137A (en) * | 2003-07-04 | 2004-03-10 | 沈阳药科大学 | Osmotic pump type controlled release preparation of kurarinone and its preparing method |
Non-Patent Citations (2)
| Title |
|---|
| 吴晓丽等: "苦参素微孔渗透泵片的研制", 《中国药科大学学报》 * |
| 庞大海等: "苦参素渗透泵控释片的制备及释药影响因素考察", 《中国药剂学杂志》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN105769797B (en) | 2018-10-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN101579325B (en) | Metformin hydrochloride controlled-release tablet and preparation method thereof | |
| CN106924208A (en) | A kind of compound Dapagliflozin Metformin Extended-release Tablets and preparation method thereof | |
| CN107595795A (en) | A kind of Metoprolol succinate sustained-release tablets and preparation method thereof | |
| CN104688700B (en) | A kind of tenofovir disoproxil fumarate piece and preparation method thereof for being easy to dissolve out | |
| CN109875972B (en) | Olmesartan medoxomil and amlodipine pharmaceutical composition | |
| CN104000796A (en) | Coating auxiliary materials, preparation method and coating method for Chinese herb extract preparations | |
| CN105456223A (en) | Mesalazine sustained-release pellets, preparation method thereof and mesalazine sustained-release capsule | |
| CN109568284B (en) | Tenofovir alafenamide enteric-coated tablet and preparation method thereof | |
| CN104800184B (en) | The smooth sustained release agent pieces of butanedioic acid furan Luo Qu | |
| CN104873473A (en) | Potassium chloride sustained-release tablet and preparation method thereof | |
| CN106667936A (en) | Sofosbuvir tablet and preparation method thereof | |
| CN105878256A (en) | Controlled-release preparation containing metformin hydrochloride and glimepiride and preparation method of controlled-release preparation | |
| CN101708169A (en) | Colonic targeting administration preparation containing active substance of paeonol and preparation method thereof | |
| CN102727447A (en) | Florfenicol controlled release preparation and preparation method thereof | |
| CN106138104A (en) | Valid target of periplaneta americana colon tablet and preparation method thereof | |
| CN105769797A (en) | Kurarinone osmotic pump controlled release tablets and preparation method thereof | |
| CN107982240B (en) | Potassium sodium dehydroandroan drographolide succinate enteric coated granules capable of being accurately dissolved out and preparation method thereof | |
| CN105616376B (en) | Composition and preparation method containing magnesium isoglycyrrhetate medicine | |
| CN109758431A (en) | A kind of metformin hydrochloride tablet and preparation method thereof | |
| KR20230086370A (en) | Pharmaceutical combination comprising dapagliflozin and pioglitazone and preparing method thereof | |
| CN104606162B (en) | A kind of body of Pramipexole dihydrochloride slow releasing preparation and preparation method thereof | |
| CN106806353A (en) | Ailamode spansule and preparation method thereof | |
| CN104546771A (en) | Metroprolol succinate containing tablet and preparation method thereof | |
| CN103550182A (en) | Enteric-coated sustained release composition | |
| CN103211999A (en) | Controlled-release pellet for treating acute and chronic hepatitis and preparation method and application thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |