CN100596276C - Vinpocetine sustained-release capsules and preparation method thereof - Google Patents
Vinpocetine sustained-release capsules and preparation method thereof Download PDFInfo
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- CN100596276C CN100596276C CN200510006685A CN200510006685A CN100596276C CN 100596276 C CN100596276 C CN 100596276C CN 200510006685 A CN200510006685 A CN 200510006685A CN 200510006685 A CN200510006685 A CN 200510006685A CN 100596276 C CN100596276 C CN 100596276C
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Abstract
The present invention provides one kind of slow-released vincamine capsule and its preparation process. The slow-released vincamine capsule contains slow-released vincamine micro pills comprising blank micro pill, active medicine layer and releasing coating. The slow-released vincamine capsule may have different micro pill combination for ideal slow-release speed for the patient to take 1-2 timesa day. Compared with other vincamine preparations, the preparation of the present invention has the advantages of smooth blood medicine concentration, long maintenance time, less toxic side effect, high patient dependence in taking medicine, etc.
Description
Technical field
The invention belongs to pharmaceutical preparation, relate to a kind of slow releasing capsule dosage form of cerebral vasodilator, be specifically related to slow releasing capsule of vinpocetine and preparation method thereof.
Background technology
Vinpocetine (Vinpocetine, chemical name are ethyl apo-vincamine-22-acetate) is a cerebral vasodilator, can suppress phosphodiesterase activity, increase the effect of the courier c-GMP of vascular smooth muscle relaxation, optionally the cerebral blood flow increasing amount can also suppress platelet aggregation in addition, reduce human blood viscosity, strengthen red blood cell deformation power, improve blood fluidity and microcirculation, promote the cerebral tissue ingestion of glucose, increase the brain oxygen consumption, improve the brain metabolism.This product can reach the blood drug level peak value in oral 1 hour, about 2～4 hours of half-life.Be used to improve multiple nerve or mental symptom due to cerebral hemorrhage, cerebral infarction sequela and the cerebral arteriosclerosis clinically, dizzy, nose heave, headache, hypomnesis, action obstacle, lassitude, depression, insomnia, numb limbs and tense tendons and aphasis etc.Because this type of patient mostly is the gerontal patient, handicapped, intellectual deterioration, but need take medicine for a long time, this product ordinary preparation needed clothes 3 times in one day, and this brings inconvenience to them.The dosage form that present this product is at home and abroad gone on the market has only tablet, injection and transfusion etc.Be made into 1～2 time on the one slow releasing capsule, can reduce patient's medicining times, long time provides steadily effectively blood drug level, reduces toxic and side effects, thereby improves the compliance that the patient takes medicine greatly.Far and away, in aged tendency of population more and more serious today, the appearance of slow-released vincamine capsule will bring glad tidings for more gerontal patient.
Summary of the invention
The objective of the invention is provides a kind of slow-released vincamine capsule and preparation method thereof in order to overcome above-mentioned the deficiencies in the prior art.It only needed take medicine in one 1～2 time, just can keep 12～24 hours increase brain blood and supply, improve the metabolic curative effect of brain, overcome this product ordinary preparation and needed day clothes 3 times, and the back blood concentration fluctuation of taking medicine is big, short treating period, the shortcoming that toxic and side effects is big is for extensive patients is brought more fine curative effect, more convenient.
Preparation of the present invention is a slow releasing capsule, includes 5～30mg vinpocetine slow-release micro-pill (piller), and this micropill (piller) is made up of celphere, active medicine layer and sustained-release coating layer, and further, the present invention's prescription is made up of following component by weight percentage:
(1) celphere: 5～50%
(2) active medicine layer:
Vinpocetine 1～50%
Organic acid 1～50%
Filler 5～70%
Binding agent 0.1～8%
(3) sustained-release coating layer:
Slow-release material 5～20%
Porogen 0～5%
Plasticizer 0～5%
Antiplastering aid 0.5～20%
Opacifier 0～5%
Above each component consumption sum is 100%.
Preparation of the present invention can adopt centrifugal coating pelletizing machine, High Speed Stirring Machine, extrudes spheronizator, fluidized bed coating granulator, atresia or the preparation of porose efficient film coating pan.Concrete preparation method is as described below:
Wrap vinpocetine active medicine layer with binding agent on celphere, or vinpocetine active medicine layer is made into suspension, spray is wrapped on the celphere, and 40～70 ℃ of dryings get the vinpocetine pill; Wrap sustained-release coating layer again,,, get the vinpocetine slow-release pill in 40～50 ℃ of dryings according to the consumption of drug releasing rate control coating solution; The piller that also one or more can be had different drug release rates is mixed in proportion to obtain to have the vinpocetine slow-release pill of desirable drug release rate; Incapsulate by standard quantity, promptly get slow-released vincamine capsule.
Principal agent is selected vinpocetine for use in the slow releasing capsule of the present invention, and the optimum content of vinpocetine is 15mg in the described capsule.
Slow releasing capsule empty ball core of the present invention is made up of sucrose and starch, also can be made up of microcrystalline Cellulose, and the size of celphere is 0.30～1.00mm, preferred 0.40～0.60mm.
The active medicine layer is made up of vinpocetine, organic acid, filler, binding agent in the slow releasing capsule of the present invention.
Organic acid can be selected citric acid, tartaric acid, malic acid, fumaric acid, adipic acid, succinic acid or maleic acid in the slow releasing capsule of the present invention, optimization citric acid, tartaric acid.
Filler can be selected a kind of in starch, microcrystalline Cellulose, sucrose, lactose, pregelatinized Starch, mannitol, sorbitol, polyoxyethylene sorbitan monoleate, sodium lauryl sulphate, micropowder silica gel, the Pulvis Talci or their mixture in the slow releasing capsule of the present invention.
Binding agent can be selected polyvinylpyrrolidone, hypromellose, sucrose solution, various organic acid soln, water, ethanol etc. in the slow releasing capsule of the present invention.
Sustained-release coating layer is made up of slow-release material, porogen, plasticizer, antiplastering aid and opacifier in the slow releasing capsule of the present invention.
In the slow releasing capsule of the present invention slow-release material can select ethyl cellulose (EC,
), one of hypromellose (HPMC), acrylic resin (Eudragit RS100, Eudragit RL100, Eudragit RS30D, Eudragit RL30D, EudragitRS PO, Eudragit RL PO, Eudragit NE30D, Eudragit L100-55, Eudragit L30D-55, EudragitL100, Eudragit S100) or their mixture.
Porogen can be selected hypromellose (HPMC), polyethylene glycol 6000 (PEG6000), polyvinylpyrrolidone (PVP) in the slow releasing capsule of the present invention.
Plasticizer can be selected polyethylene glycol 6000 (PEG6000), triethyl citrate, dibutyl sebacate in the slow releasing capsule of the present invention.
Antiplastering aid can be selected Pulvis Talci, Stepanol MG etc. in the slow releasing capsule of the present invention.
Opacifier can be selected titanium dioxide etc. in the slow releasing capsule of the present invention.
The present invention is as cerebral vasodilator; the energy selectivity improves the blood circulation of brain, promotes the energy metabolism of brain, regulates the neurotransmitter systemic-function; many-sided protection brain is avoided anoxybiotic infringement; only need take medicine 1～2 time in 1st, just can continue to bring into play curative effect 12～24 hours, toxic and side effects is low; taking convenience; be particularly suitable for the treatment of cardiovascular and cerebrovascular disease, the brain diseases due to the aging is also had significant curative effect, solved the deficiencies in the prior art.
The specific embodiment
Embodiment 1:
Pharmaceutical formulation of the present invention is made up of following component:
(1) celphere:
Sucrose starch ball core 30.0g
(2) active medicine layer:
Vinpocetine 15.0g
Citric acid 45.0g
Starch 100.0g
Micropowder silica gel 1.4g
Ethanol is an amount of
(3) sustained-release coating layer:
Eudragit?L100 25.0g
Triethyl citrate 2.7g
Pulvis Talci 14.0g
Titanium dioxide 4.5g
Ethanol is to 410.0g
Make 1000 altogether
Preparation process:
(1) in centrifugal coating pelletizing machine, be binding agent with the alcoholic solution, on celphere, wrap the vinpocetine active medicine layer of forming by vinpocetine, citric acid, starch, micropowder silica gel, 60 ℃ of dryings get the vinpocetine pill;
(2) in centrifugal coating pelletizing machine, on the vinpocetine pill, wrap the sustained-release coating layer coating solution,,, promptly get the vinpocetine slow-release pill through 40～50 ℃ of dry about 2h according to the consumption of drug releasing rate control coating solution;
(3) incapsulate by standard quantity, promptly get slow-released vincamine capsule.
Embodiment 2:
(1) celphere:
Microcrystalline Cellulose ball core 15.0g
(2) active medicine layer:
Vinpocetine 30.0g
Citric acid 15.0g
Mannitol 10.0g
Sodium lauryl sulphate 1.4g
The 2%PVP alcoholic solution is an amount of
(3) sustained-release coating layer:
Ethyl cellulose 7.0g
PVP 0.7g
Pulvis Talci 7.0g
Ethanol is to 140ml
Make 1000 altogether
Preparation process:
(1) in the fluidized bed coating comminutor, be binding agent with the alcoholic solution of 2%PVP, on celphere, wrap vinpocetine active medicine layer, 60 ℃ of dryings, the vinpocetine pill;
(2) in the fluidized bed coating comminutor, on the vinpocetine pill, wrap the sustained-release coating layer coating solution, the consumption according to drug releasing rate control coating solution through 40 ℃ of dry 2h, promptly gets the vinpocetine slow-release pill;
(3) incapsulate by standard quantity, promptly get slow-released vincamine capsule.
Embodiment 3:
(1) celphere:
Sucrose starch ball core 50.0g
(2) active medicine layer:
Vinpocetine 7.5g
Tartaric acid 52.5g
Lactose 50.0g
50% alcoholic solution of 2%HPMC is an amount of
(3) sustained-release coating layer:
Eudragit?RS?30D 12.5g
Eudragit?RL?30D 12.5g
Dibutyl sebacate 0.8g
Pulvis Talci 4.2g
Water 25.0g
Make 1000 altogether
Preparation process:
(1) in the fluidized bed coating comminutor, with 50% alcoholic solution of 2%HPMC vinpocetine active medicine layer is made into suspension, spray is wrapped on the celphere, 60 ℃ of dryings, the vinpocetine pill;
(2) in the fluidized bed coating comminutor, on the vinpocetine pill, wrap the sustained-release coating layer coating solution, the consumption according to drug releasing rate control coating solution through 40 ℃ of dry 2h, promptly gets the vinpocetine slow-release pill;
(3) incapsulate by standard quantity, promptly get slow-released vincamine capsule.
Embodiment 4:
(2) celphere:
Sucrose starch ball core 30.0g
(2) active medicine layer:
Vinpocetine 15.0g
Citric acid 15.0g
Starch 50.0g
50% sucrose solution is an amount of
(3) sustained-release coating layer:
Eudragit?NE?30D 48.3g
Pulvis Talci 14.5g
Water 53.0g
Make 1000 altogether
Preparation process:
(1) in centrifugal coating pelletizing machine, be binding agent with 50% sucrose solution, wrap vinpocetine active medicine layer on celphere, 60 ℃ of dryings get the vinpocetine pill;
(2) in the fluidized bed coating comminutor, on the vinpocetine pill, wrap the sustained-release coating layer coating solution, through 40 ℃ of dry 2h, promptly get the vinpocetine slow-release pill;
(3) two kinds of micropills that will have different drug release rates are mixed in proportion the vinpocetine slow-release pill that obtains desirable drug release rate;
(4) incapsulate by standard quantity, promptly get slow-released vincamine capsule.
Through investigating, the release in vitro degree of the foregoing description gained slow-released vincamine capsule is: 1h:10～40%; 4h:40～80%; 12h: 〉=70%.
Claims (4)
1, a kind of slow-released vincamine capsule is characterized in that: this capsule 's content is the vinpocetine slow-release pill, and this piller is made up of celphere, active medicine layer and sustained-release coating layer, and per 1000 capsules are made up of following component:
(1) celphere: be sucrose starch ball core 30.0g
(2) active medicine layer:
Vinpocetine 15.0g
Citric acid 45.0g
Starch 100.0g
Micropowder silica gel 1.4g
Ethanol is an amount of
(3) sustained-release coating layer:
The strange L100 25.0g of acrylic resin You Te
Triethyl citrate 2.7g
Pulvis Talci 14.0g
Titanium dioxide 4.5g
Ethanol is to 410.0g.
2, a kind of slow-released vincamine capsule is characterized in that: this capsule 's content is the vinpocetine slow-release pill, and this piller is made up of celphere, active medicine layer and sustained-release coating layer, and per 1000 capsules are made up of following component:
(1) celphere: be microcrystalline Cellulose ball core 15.0g
(2) active medicine layer:
Vinpocetine 30.0g
Citric acid 15.0g
Mannitol 10.0g
Sodium lauryl sulphate 1.4g
2% polyvinylpyrrolidone alcoholic solution is an amount of
(3) sustained-release coating layer:
Ethyl cellulose 7.0g
Polyvinylpyrrolidone 0.7g
Pulvis Talci 7.0g
Ethanol is to 140ml.
3, a kind of slow-released vincamine capsule is characterized in that: this capsule 's content is the vinpocetine slow-release pill, and this piller is made up of celphere, active medicine layer and sustained-release coating layer, and per 1000 capsules are made up of following component:
(1) celphere: be sucrose starch ball core 50.0g
(2) active medicine layer:
Vinpocetine 7.5g
Tartaric acid 52.5g
Lactose 50.0g
50% alcoholic solution of 2% hypromellose is an amount of
(3) sustained-release coating layer:
The strange RS30D 12.5g of acrylic resin You Te
The strange RL30D 12.5g of acrylic resin You Te
Dibutyl sebacate 0.8g
Pulvis Talci 4.2g
Water 25.0g.
4, a kind of slow-released vincamine capsule is characterized in that: this capsule 's content is the vinpocetine slow-release pill, and this piller is made up of celphere, active medicine layer and sustained-release coating layer, and per 1000 capsules are made up of following component:
(1) celphere: be sucrose starch ball core 30.0g
(2) active medicine layer:
Vinpocetine 15.0g
Citric acid 15.0g
Starch 50.0g
50% sucrose solution is an amount of
(3) sustained-release coating layer:
The strange NE 30D of acrylic resin You Te 48.3g
Pulvis Talci 14.5g
Water 53.0g.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200510006685A CN100596276C (en) | 2005-01-26 | 2005-01-26 | Vinpocetine sustained-release capsules and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200510006685A CN100596276C (en) | 2005-01-26 | 2005-01-26 | Vinpocetine sustained-release capsules and preparation method thereof |
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| CN1810242A CN1810242A (en) | 2006-08-02 |
| CN100596276C true CN100596276C (en) | 2010-03-31 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4061369A1 (en) | 2019-11-19 | 2022-09-28 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | A pharmaceutical form comprising acidic substance |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102274520A (en) * | 2011-07-07 | 2011-12-14 | 程雪翔 | Coating composition and coating method |
| CN102657615A (en) * | 2012-05-02 | 2012-09-12 | 上海智同医药科技有限公司 | Vincamine sustained-release pellet preparation and preparation method thereof |
| CN105395519B (en) * | 2015-12-07 | 2018-06-01 | 青岛正大海尔制药有限公司 | A kind of Topiroxostat spansule and preparation method thereof |
-
2005
- 2005-01-26 CN CN200510006685A patent/CN100596276C/en not_active Expired - Fee Related
Non-Patent Citations (4)
| Title |
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| 微丸的成型性研究进展. 汪芸等.江西中医学院学报，第14卷第1期. 2002 * |
| 长春西汀凝胶骨架片中枸橼酸和介质pH值对药物释放的影响. 聂淑芳等.中国药学杂志，第39卷第6期. 2004 * |
| 长春西汀包合物及其缓释制剂的设计与评价. 聂淑芳.中国博士学位论文全文数据库 医药卫生科技辑，第3期. 2004 * |
| 长春西汀透皮给药系统的设计与评价. 李华.中国博士学位论文全文数据库 医药卫生科技，第3期. 2004 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4061369A1 (en) | 2019-11-19 | 2022-09-28 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | A pharmaceutical form comprising acidic substance |
| EP4061369A4 (en) * | 2019-11-19 | 2024-04-10 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | A pharmaceutical form comprising acidic substance |
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| Publication number | Publication date |
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| CN1810242A (en) | 2006-08-02 |
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