CN107095855A - A kind of Piribedil sustained-release tablet and preparation method thereof - Google Patents
A kind of Piribedil sustained-release tablet and preparation method thereof Download PDFInfo
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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
- A61K9/2004—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
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
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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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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Abstract
The invention belongs to field of pharmaceutical preparations, the invention discloses sustained release tablets of piribedil and preparation method thereof.The sustained release tablets of the present invention include piribedil, hydrophobic framework material, adhesive and lubricant;Wherein, according to mass percent meter, piribedil 10%~40%, hydrophobic framework material 50% ~ 80%, adhesive 1% ~ 5%, lubricant 0.5% ~ 5%;The hydrophobic framework material is the mixture of microcrystalline cellulose, glycerine ester type waxes and fusogen;Described glyceride is one or both of glycerin monostearate or glyceryl palmitostearate;Described wax is one or both of cera alba or palm wax.The sustained release tablets of the present invention include hydrophobic framework material etc., can be very good the release of regulating medicine, can be used for treating Parkinson's, technique is simple, is conducive to expanding production.
Description
Technical field
The present invention relates to a kind of pharmaceutical preparation and preparation method thereof, more particularly to a kind of Piribedil sustained-release tablet and its preparation
Method.
Background technology
Parkinson's (Parkinson's disease, PD) are common central nervous system degenerative diseases, to transport
Dynamic to reduce, muscle rigidity and tremble for cardinal symptom, its pathological change is mainly that black substance and striatal dopaminergic neuron become
Property missing, corpus straitum DA mediators are reduced, and 7EC6 intracellular acidophilia Lewy bodies are formed.The PD incidence of disease increases and increased with the age
Plus, the incidence of disease of more than 50 years old is 0.5%, is within more than 60 years old 1%.China PD patient has 1,700,000, and estimation increases patient newly about every year
100000.After 1960s, western medical treatment PD uses levodopa alternative medicine always, it has now been found that the effect of replacement therapy
It is general to start decline after 3~5 years, and occur with the complication that drug-induced dyskinesia (unusual fluctuation disease) is the form of expression, early stage
Side effect have nausea, apocleisis, dizziness;Long-term taking can cause the last phenomenon of agent, on-off phenomenon and dyskinesia.Piribedil is
A kind of Dopaminergic Agents of French Les Laboratoires servier research and development, chemical entitled 2- (4- piperonyl -1- piperazinyls) pyrimidine.It is made
With mechanism for that can stimulate the D2 acceptors and middle Cerebral cortex in brain nigrostriatum postsynaptic, the D2 and D3 of midbrain marginal convolution path by
Body is there is provided effective DOPA amine effect, in zoopery, and piribedil can stimulate cerebral metabolism, while stimulating cortex electricity hair
It is raw, increase oxygen consumption, improve brain cortex tissue PO2, increase circulating blood volume;In human body, piribedil occur during treating with
" dopaminergic " type stimulates Cerebral cortex electricity to occur, and has clinical effect to the various functions caused by dopamine.Followed for periphery
Ring, this medicine can increase vascular flow amount.Because its selectivity is strong, PD each stage can be used for, security to be good, dosage regimen letter
It is single, therefore be the drug of first choice for treating PD, it has been widely used in the treatment of Parkinson's.
Slowly non-constant velocity discharges medicine in a long time after sustained release tablets refer to orally, is characterized in that medicine temporally changes
Few lasting non-constant velocity release after first many.It will not be as ordinary tablet once to discharging completely in vivo, and such sustained release tablets are just not
Intestines and stomach can be produced with larger stimulation, mainly shielded, more so used in the larger medicine of local excitation.Make medicine blood medicine
Toxicity produced by fluctuation of concentration is minimized, it is possible to reduce medicining times, so as to improve the compliance of patient.
Matrix tablet is the important set composition of sustained-release preparation, refers to medicine and leads to one or more inert solid framework materials
The tablet that compressing technology is made is crossed, medicine is dispersed in porous or non-porous material, medicine is discharged by various mechanism,
Medicine is set slowly to discharge.During intestines and stomach release, medicine and gastrointestinal mucosa exposure concentration are small, advantageously reduce medicine
Toxic side effect.There is hydrophilic gel matrix material applied to the framework material in sustained-release matrix tablets, erodible framework material is insoluble
Framework material, several classes of mixed matrix material.Wherein hydrogel matrix kind at most, is occupied first of sustained-release and controlled release preparation.It releases the drug
Mechanism is mainly dissolution principle, diffusion principle and corrosion and is combined action principle with diffusion, dissolution.Hydrophilic gel matrix material
Four classes 1. cellulose derivative can be divided(Methylcellulose, hydroxyethyl cellulose, hydroxyethylmethylcellulose, hydroxypropyl cellulose,
Hydroxypropyl methyl cellulose, hydroxymethyl cellulose and sodium cellulose glycolate etc.)2. non-cellulosic polysaccharide(As glucose, shell are more
Sugar and galactolipin etc.)3. natural gum(Pectin, sodium alginate, potassium alginate, agar, pawl ear natural gum and tragacanth etc.)4. ethene
Based polyalcohol or acrylate copolymer etc.(Such as polyvinyl alcohol and poly- hydroxyalkyl vinyl 934).Mixing material matrix sustained release tablet is by medicine
What thing was made after being mutually mixed with insoluble wax and organophilic gel framework material more than above two.Conventional insoluble bone
Frame material has:Ethyl cellulose, polyethylene, polypropylene, glycerolipid, polysiloxanes and polyoxyethylene etc..
Fatty acid glycerine esters include glycerin monostearate, glyceryl palmitostearate, be by long chain fatty acids or
Person's grease and glycerine reaction and be made.It is a kind of non-ionic surfactant.Chinese invention patent application number:
CN201610095100.6 discloses a kind of diclofenac sustained release tablets and preparation method thereof.Wherein glycerin monostearate is made
For adhesive, make Mechanism of Drug Release more reasonable.In sustained release tablets framework material, there is not yet on glycerin monostearate and firmly
The report of resin acid tripalmitin.
Cera alba English name:Bees wax, are the esters formed by the fatty alcohol containing 26 ~ 34 carbon atoms and palmitic acid.
It is common in suppository, Chinese invention patent application number:CN201110208197.4 discloses a kind of containing with reference to estrogen
Composition medicine preparation, wherein beeswax as oil phase one kind.
Brazil wax quality is very rigid, with high gloss, easily emulsifies, and has good Oil keeping.China
Application for a patent for invention number:CN201610877537.5 discloses safe ten thousand rhzomorph granular preparations of a kind of tartaric acid and preparation method thereof,
Palm wax selected from wax is as carrier auxiliary material, and condensation spraying granulation prepares the safe ten thousand rhzomorph granular preparations of tartaric acid.Not yet find
In piribedil sustained-release tablet is made as hydrophobic framework material.
The content of the invention
It is an object of the invention to provide a kind of Piribedil sustained-release tablet, not only delay the rate of release of medicine piribedil,
The release of medicine is more stablized, drug effect is improved, while having good internal in vitro correlation.
To achieve the above object of the invention, the technical scheme is that:A kind of Piribedil sustained-release tablet, including:Pyrrole shellfish
That, hydrophobic framework material, adhesive and lubricant;Wherein, according to mass percent meter, piribedil 10%~40%, hydrophobic bone
Frame material 50% ~ 80%, adhesive 1% ~ 5%, lubricant 0.5% ~ 5%;
The hydrophobic framework material is the mixture of microcrystalline cellulose, glyceride, wax and fusogen;Described glyceride is single hard
One or both of glycerol or glyceryl palmitostearate;Described wax is one kind in cera alba or palm wax
Or two kinds.
It is preferred that hydrophobic framework material melt for glyceryl palmitostearate, microcrystalline cellulose, cera alba, palm wax and rush
The mixture of agent.
Described hydrophobic framework material, according to mass percent meter, the content of each component is:Microcrystalline cellulose 5% ~ 50%,
Glyceride 10% ~ 80%, wax 10% ~ 30%, fusogen 5% ~ 10%.
The preferred component content of the hydrophobic framework material is:Wax and fusogen:Microcrystalline cellulose and glyceride mixture
Mass ratio be 1:3.
Described fusogen is PEG6000Or PEG2000.In above-mentioned technical proposal, described adhesive is polyvinylpyrrolidine
Ketone K-30 ethanol solution.
In above-mentioned technical proposal, the lubricant is one or both of magnesium stearate or silica.
The preparation method of above-mentioned Piribedil sustained-release tablet comprises the following steps:
(1)After batch weighing, piribedil, glyceride, microcrystalline cellulose are mixed, sieved;
(2)Wax and fusogen are mixed, heating melting;
(3)Fused solution is added into step(1)In obtained mixture, plus softwood is made in adhesive;
(4)Above-mentioned softwood is sieved and pelletized, is dried, with sieve whole grain, lubricant is added, is well mixed, tabletting obtains the pyrrole shellfish
Ground that sustained release tablets.
Wherein, step(1)Described sieving was 80 mesh sieves;Step(4)Described sieving was 30 mesh sieves.
Wherein, step(2)Described melting is in 85 DEG C of meltings.
Compared to the prior art, prior art of the invention has advantages below:
1. sustained release purpose is reached using pore-foaming agent more than the method for existing sustained release tablets, but your release has pH quick to pyrrole
Perception, dissolution rate is high in acid condition, and dissolution rate is relatively low in water.Can not reaching pyrrole using pore-foaming agent, your sustained release is imitated
Really.The technical solution adopted in the present invention, without using pore-foaming agent, using tristerin and glyceryl palmitostearate with
Microcrystalline cellulose is engaged, and can be good at solving the problems, such as the sustained release of piribedil.
2. glyceryl palmitostearate, which is used alone, to pelletize, exclusive use microcrystalline cellulose insoluble drug release is too fast,
It is unable to reach slow release effect.Being used in mixed way for glyceryl palmitostearate and microcrystalline cellulose, can be very good regulating medicine
Release.
3. in the prior art, wax is passed through frequently as polishing sugar coated tablet or the film coating as sustained release tablets.The technology of the present invention
Make it as hydrophobic framework material, with glycerolipid pelletizing press sheet after melting, pyrrole that release can be regulated and controled well.
4. sustained release tablets of the present invention are overcome single using the mixed matrix material of medicine and hydrophobic framework material
A kind of material is difficult to regulate and control, and tests release in vitro, shows preferable slow release effect.Meanwhile, sustained release blade technolgy letter of the invention
It is single, be conducive to expanding production.
Brief description of the drawings
Fig. 1 is the contrast releasing curve diagram of embodiment 1-3 middle skeleton pieces.
Fig. 2 is the contrast releasing curve diagram of embodiment 2,4 and 5 middle skeleton pieces.
Fig. 3 be embodiment 2 four kinds of media in elution profiles.
Embodiment
Below will be by the way that the invention will be further described, these descriptions are not to make further to present invention
Limit.It should be understood by those skilled in the art that the equivalent substitution made to present invention, or be correspondingly improved, still fall within this
Within the protection domain of invention.
Embodiment 1:The preparation of Piribedil sustained-release tablet
Weigh 2.5g piribedils, 2.5g glyceryl palmitostearates, 5g microcrystalline celluloses progressively increase method mixing according to equivalent
80 mesh sieves, 2.5g wax-like fused solution are crossed after uniform(0.5g cera albas, 1g palm waxs and 1gPEG6000Plus ethanol is in 85 DEG C of meltings
Dry afterwards and remove ethanol)In the mixture for adding main ingredient and microcrystalline cellulose and glyceryl palmitostearate, with PVPK30's
Ethanol solution(Concentration is 5%wt.)It is used as adhesive(Solution usage 10g)Softwood processed, the granulation of 30 mesh sieves, 60 DEG C of dry 1h, 30 mesh
Sieve after whole grain, add 0.2g magnesium stearates and 0.3g silica, mix, tabletting.
Embodiment 2:The preparation of Piribedil sustained-release tablet
Weigh 2.5g piribedils, 5g glyceryl palmitostearates, 2.5g microcrystalline celluloses progressively increase method mixing according to equivalent
80 mesh sieves, 2.5g wax-like fused solution are crossed after uniform(0.5g cera albas, 1g palm waxs and 1gPEG6000Plus ethanol is in 85 DEG C of meltings
Dry afterwards and remove ethanol)In the mixture for adding main ingredient and microcrystalline cellulose and glyceryl palmitostearate, with PVPK30's
Ethanol solution(Concentration is 5%wt.)It is used as adhesive(Solution usage 10g)Softwood processed, the granulation of 30 mesh sieves, 60 DEG C of dry 1h, 30 mesh
Sieve after whole grain, add 0.2g magnesium stearates and 0.3g silica, mix, tabletting.
Embodiment 3:The preparation of Piribedil sustained-release tablet(Comparative example)
2.5g piribedils are weighed, 7.5g glyceryl palmitostearates progressively increase after method is well mixed according to equivalent and cross 80 mesh
Sieve, 2.5g wax-like fused solution(0.5g cera albas, 1g palm waxs and 1gPEG6000Plus ethanol is in 85 DEG C of meltings)Add main ingredient with
In the mixture of microcrystalline cellulose and glyceryl palmitostearate, with PVP K30 ethanol solution(Concentration is 5%wt.)As
Adhesive(Solution usage 10g)After softwood processed, the granulation of 30 mesh sieves, 60 DEG C of dry 1h, 30 mesh sieve whole grains, 0.2g magnesium stearates are added
With 0.3g silica, mix, tabletting.
Embodiment 4:The preparation of Piribedil sustained-release tablet(Comparative example)
Weigh 2.5g piribedils, 5g glyceryl palmitostearates, 3.75g microcrystalline celluloses progressively increase method mixing according to equivalent
80 mesh sieves, 1.25g wax-like fused solution are crossed after uniform(0.25g cera albas, 0.5g palm waxs and 0.5gPEG6000Plus ethanol is 85
DEG C melting after dry remove ethanol)In the mixture for adding main ingredient and microcrystalline cellulose and glyceryl palmitostearate, with
PVPK30 ethanol solution(Concentration is 5%wt.)It is used as adhesive(Solution usage 10g)Softwood processed, the granulation of 30 mesh sieves, 60 DEG C are done
After dry 1h, 30 mesh sieve whole grains, 0.2g magnesium stearates and 0.3g silica are added, is mixed, tabletting.
Embodiment 5:The preparation of Piribedil sustained-release tablet(Comparative example)
Weigh 2.5g piribedils, 5g glyceryl palmitostearates, 1.25g microcrystalline celluloses progressively increase method mixing according to equivalent
80 mesh sieves, 3.75g wax-like fused solution are crossed after uniform(0.75g cera albas, 1.5g palm waxs and 1.5gPEG6000Plus ethanol is 85
DEG C melting after dry remove ethanol)In the mixture for adding main ingredient and microcrystalline cellulose and glyceryl palmitostearate, with
PVPK30 ethanol solution(Concentration is 5%wt.)It is used as adhesive(Solution usage 10g)Softwood processed, the granulation of 30 mesh sieves, 60 DEG C are done
After dry 1h, 30 mesh sieve whole grains, 0.2g magnesium stearates and 0.3g silica are added, is mixed, tabletting.
Embodiment 6:Piribedil sustained-release tablet drug release determination
Take the Piribedil sustained-release tablet of the preparation of above-described embodiment 1 ~ 5 and the sustained release tablets of comparative example 1(The Thailand of French Shi Weiya research and development
Shu Da), by Chinese Pharmacopoeia two annex XD the first methods of drug release determination of version in 2010, using the two annex XC dissolutions of version in 2010
Degree determines the device of the second method, and the hydrochloric acid solution 1000mL using pH1.0 is dissolution medium, and rotating speed is 100rmin-1, grasp in accordance with the law
Make.In the separately sampled 2mL of 2h, 4h, 8h, 12h and 24h, while adding equivalent release liquid, and centrifuge immediately, take supernatant, carry out
HPLC is analyzed, and calculates the Cumulative release amount of medicine.
From Fig. 1(Embodiment 1 is to example 3)It can be seen that the ratio of the hydrophilic skeleton material and hydrophobic framework material in its prescription
Difference, its release is different, and the microcrystalline cellulose amount of embodiment 1 is more, and its release is higher, the stearic acid palm of embodiment 3
Acid glyceride is more, and its release is smaller, discharges slower.
From Fig. 2(Embodiment 4 is to example 5), the amount of the fused solution of its wax is different, and the wax-like fused solution of embodiment 4 is less, release
Degree is higher, and the wax-like fused solution of embodiment 5 is more, and its release is substantially reduced.
It can thus be concluded that, when hydrophobic framework material is used in mixed way, uniformity can be overcome poor, the later stage discharges the defect such as very fast.Medicine
Thing release is relatively stablized, and compressibility is preferable.Embodiment 2 is optimal, and it is close to grind release with original.Embodiment 2 is optimal prescription.
Embodiment 7:The preparation of Piribedil sustained-release tablet
Weigh 3.5g piribedils, 0.5g glycerin monostearates, 2.5g microcrystalline celluloses are well mixed according to equivalent method of progressively increasing
80 mesh sieves, 2g wax-like fused solution are crossed afterwards(1.5g cera albas and 0.5gPEG2000Plus ethanol is dried after 85 DEG C of meltings and removes second
Alcohol)In the mixture for adding main ingredient and microcrystalline cellulose and glyceryl palmitostearate, with PVPK30 ethanol solution(Concentration
For 2%wt.)It is used as adhesive(Solution usage 10g)After softwood processed, the granulation of 30 mesh sieves, 60 DEG C of dry 1h, 30 mesh sieve whole grains, add
0.1g magnesium stearates, are mixed, tabletting.
Embodiment 8:The preparation of Piribedil sustained-release tablet
Weigh 3.8g piribedils, 4.8g glyceryl palmitostearates, 0.3g microcrystalline celluloses progressively increase method mixing according to equivalent
80 mesh sieves, 1.5g wax-like fused solution are crossed after uniform(0.6g palm waxs and 0.3gPEG6000Plus ethanol is dried after 85 DEG C of meltings
Remove ethanol)It is molten with PVPK30 ethanol in the mixture for adding main ingredient and microcrystalline cellulose and glyceryl palmitostearate
Liquid(Concentration is 2%wt.)It is used as adhesive(Solution usage 5g)Softwood processed, the granulation of 30 mesh sieves, 60 DEG C of dry 1h, 30 mesh sieve whole grains
Afterwards, 0.05g silica is added, is mixed, tabletting.
Embodiment 9:The preparation of Piribedil sustained-release tablet
4g piribedils are weighed, 0.5g glyceryl palmitostearates, 0.5g glycerin monostearates, 2g microcrystalline celluloses are pressed
Progressively increase according to equivalent after method is well mixed and cross 80 mesh sieves, 1.75g wax-like fused solution(1g cera albas, 0.5g palm waxs and
0.5gPEG6000Plus ethanol is dried after 85 DEG C of meltings and removes ethanol)Add main ingredient and microcrystalline cellulose and stearic acid palmitic acid are sweet
In the mixture of grease, with PVPK30 ethanol solution(Concentration is 5%wt.)It is used as adhesive(Solution usage 10g)Softwood processed,
30 mesh sieves are pelletized, 60 DEG C of dry 1h, after 30 mesh sieve whole grains, add 0.25g magnesium stearates and 0.25g silica, are mixed, pressure
Piece.
Embodiment 10:The preparation of Piribedil sustained-release tablet
Weigh 1g piribedils, 3.5g glyceryl palmitostearates, 3g microcrystalline celluloses are well mixed according to equivalent method of progressively increasing
80 mesh sieves, 1.5g wax-like fused solution are crossed afterwards(0.7g cera albas, 0.3g palm waxs and 0.5gPEG6000Plus ethanol is in 85 DEG C of meltings
Dry afterwards and remove ethanol)In the mixture for adding main ingredient and microcrystalline cellulose and glyceryl palmitostearate, with PVPK30's
Ethanol solution(Concentration is 2%wt.)It is used as adhesive(Solution usage 25g)Softwood processed, the granulation of 30 mesh sieves, 60 DEG C of dry 1h, 30 mesh
Sieve after whole grain, add 0.2g magnesium stearates and 0.3g silica, mix, tabletting.
Claims (10)
1. a kind of Piribedil sustained-release tablet, it is characterised in that the Piribedil sustained-release tablet includes:Piribedil, hydrophobic framework
Material, adhesive and lubricant;Wherein, according to mass percent meter, piribedil 10%~40%, hydrophobic framework material 50% ~
80%, adhesive 1% ~ 5%, lubricant 0.5% ~ 5%;
The hydrophobic framework material is the mixture of microcrystalline cellulose, glyceride, wax and fusogen;Described glyceride is single hard
One or both of glycerol or glyceryl palmitostearate;Described wax is one kind in cera alba or palm wax
Or two kinds.
2. according to the Piribedil sustained-release tablet described in claim 1, it is characterised in that preferred hydrophobic framework material is stearic acid palm fibre
Palmitic acid acid glyceride, microcrystalline cellulose, cera alba, the mixture of palm wax and fusogen.
3. according to the Piribedil sustained-release tablet described in claim 1, it is characterised in that the hydrophobic framework material is according to quality percentage
Than meter, the content of each component is:Microcrystalline cellulose 5% ~ 50%, glyceride 10% ~ 80%, wax 10% ~ 30%, fusogen 5% ~ 10%.
4. according to the Piribedil sustained-release tablet described in claim 3, it is characterised in that the preferred component of the hydrophobic framework material contains
Measure and be:Wax and fusogen:The mass ratio of microcrystalline cellulose and glyceride is 1:3.
5. Piribedil sustained-release tablet according to claim 1, it is characterised in that described fusogen is PEG6000Or
PEG2000。
6. Piribedil sustained-release tablet according to claim 1, it is characterised in that described adhesive is polyvinylpyrrolidine
Ketone K-30 ethanol solution.
7. Piribedil sustained-release tablet according to claim 1, it is characterised in that the lubricant is magnesium stearate or dioxy
One or both of SiClx.
8. the preparation method of the Piribedil sustained-release tablet described in a kind of claim 1, it is characterised in that comprise the following steps:
1)After batch weighing, piribedil, glyceride, microcrystalline cellulose are mixed, sieved;
2)Wax and fusogen are mixed, plus ethanol heating melting;
3)Fused solution is added into step(1)In obtained mixture, then add adhesive that softwood is made;
4)Above-mentioned softwood is sieved and pelletized, is dried, with sieve whole grain, lubricant is added, is well mixed, tabletting obtains the pyrrole shellfish
Ground that sustained release tablets.
9. method according to claim 8, it is characterised in that step(1)Described sieving was 80 mesh sieves;Step(4)
Described sieving was 30 mesh sieves.
10. method according to claim 8, it is characterised in that step(2)Described melting is in 85 DEG C of meltings.
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107982233A (en) * | 2017-12-06 | 2018-05-04 | 佛山市弘泰药物研发有限公司 | A kind of pomalidomide sustained release tablets and preparation method thereof |
CN107982234A (en) * | 2017-12-08 | 2018-05-04 | 佛山市弘泰药物研发有限公司 | A kind of Etoricoxib sustained release tablets and preparation method thereof |
CN107998093A (en) * | 2017-12-17 | 2018-05-08 | 佛山市弘泰药物研发有限公司 | A kind of Lurasidone HCl sustained release tablets and preparation method thereof |
CN108014082A (en) * | 2017-12-19 | 2018-05-11 | 佛山市弘泰药物研发有限公司 | A kind of dronedarone hydrochloride sustained release tablets and preparation method thereof |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102240272A (en) * | 2010-05-13 | 2011-11-16 | 丽珠医药集团股份有限公司 | Potassium citrate sustained release tablet and preparation method thereof |
CN104721161A (en) * | 2015-03-31 | 2015-06-24 | 苏州弘森药业有限公司 | Piribedil sustained-release tablet and preparation method thereof |
-
2017
- 2017-06-27 CN CN201710503569.3A patent/CN107095855B/en active Active
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102240272A (en) * | 2010-05-13 | 2011-11-16 | 丽珠医药集团股份有限公司 | Potassium citrate sustained release tablet and preparation method thereof |
CN104721161A (en) * | 2015-03-31 | 2015-06-24 | 苏州弘森药业有限公司 | Piribedil sustained-release tablet and preparation method thereof |
Non-Patent Citations (1)
Title |
---|
许谙等: ""熔融制粒法制备盐酸二甲双胍缓释片", 《中国现代应用药学》 * |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107982233A (en) * | 2017-12-06 | 2018-05-04 | 佛山市弘泰药物研发有限公司 | A kind of pomalidomide sustained release tablets and preparation method thereof |
CN107982234A (en) * | 2017-12-08 | 2018-05-04 | 佛山市弘泰药物研发有限公司 | A kind of Etoricoxib sustained release tablets and preparation method thereof |
CN107998093A (en) * | 2017-12-17 | 2018-05-08 | 佛山市弘泰药物研发有限公司 | A kind of Lurasidone HCl sustained release tablets and preparation method thereof |
CN108014082A (en) * | 2017-12-19 | 2018-05-11 | 佛山市弘泰药物研发有限公司 | A kind of dronedarone hydrochloride sustained release tablets and preparation method thereof |
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