CN104586810B - A kind of slow-releasing acipimox tablet and preparation method thereof - Google Patents
A kind of slow-releasing acipimox tablet and preparation method thereof Download PDFInfo
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- CN104586810B CN104586810B CN201510033991.8A CN201510033991A CN104586810B CN 104586810 B CN104586810 B CN 104586810B CN 201510033991 A CN201510033991 A CN 201510033991A CN 104586810 B CN104586810 B CN 104586810B
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Abstract
The present invention relates to a kind of slow-releasing acipimox tablet, sustained release tablets prepared by the present invention are made up of plain piece and sustained release clothing film, plain piece contains Acipimox, HPMC and microcrystalline cellulose, sustained release coating includes Eurdragit NE 30D, talcum powder, Macrogol 6000 and lauryl sodium sulfate, slow-releasing acipimox tablet drug release prepared by the present invention is steady, organic solvent-free residue problem, it is process is simple, easy to operate, and considerable economic and social benefit can be produced.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, and in particular to a kind of slow-releasing acipimox tablet agent and preparation method thereof.
Background technology
In recent years, with eating habit change, living standard raising, operating pressure increase, hyperlipidemia and hyperproteinemia
Disease patient is more and more, and, patient population increasingly rejuvenation.Hyperlipidemia and hyperproteinemia are one group of clinical common fat
Matter metabolic disorder disease, when the concentration of blood plasma lipide exceedes, normal value is high to turn into hyperlipidemia in limited time, and lipoprotein surpasses in blood plasma
Cross high the prescribing a time limit of normal value and be referred to as hyperlipoprotememia.Epidemiological study shows, plasma low density lipoprotein and extra-low density fat
Increasing for protein level, is the key factor for early starting pulse atherosclerosis and coronary heart disease.Statistical analysis show, serum cholesterol
1% is often reduced, the pathogenetic risk of coronary disease will reduce by 2%.Therefore, rational diet, motion and drug therapy are to hyperlipemia
Disease and patients with hyperlipoproteinemia are very important.
Acipimox is nicotinic acid derivates, and the medicine mainly acts on adipose tissue, discharges free by suppressing adipose tissue
Aliphatic acid, reduces the synthesis of plasma low density lipoprotein and VLDL, so as to reduce plasma low density fat in blood plasma
The level of albumen and VLDL, while reducing dividing for plasma high density lipoprotein level by suppressing hepatic lipase activity
Solution.Clinically, Acipimox can effectively treat increased TG, hypercholesterolemia and high triglyceride merging cholesterol
Mass formed by blood stasis, be it is a kind of safely, effectively, the lipid regulating agent of better tolerance.The medicine oral absorption is rapid, and blood medicine is dense in 2 hours after medication
Degree can peaking, half-life period is shorter.The medicine is not combined with plasma protein, is not metabolized, mainly with original shape through urine ejection.Due to half
Phase of declining is short, not only brings inconvenience to patient, can not meet the needs such as growing life and medicinal application.Therefore by Ah
Former times does not take charge of and develops into sustained release agent.Slow-releasing acipimox tablet can reduce medicining times, reduce side effect, improve the compliance of patient
Property.
Chinese patent CN03130362.5 discloses a kind of delayed releasing Acipimox prepn, in order to be further ensured that length in invention
The effective blood drug concentration of time, improves the compliance of patient, increases the consumption of slow-release material, but the increase of slow-release material is faced
Bed medication brings certain potential safety hazard.
Chinese patent CN02129443.7A discloses a kind of slow-releasing acipimox capsule, and it is by Acipimox, blank pill
Core, sustained release agent, plasticizer, antiplastering aid composition, dissolution rate is preferable, but slow-release time only has 8 hours.
Chinese patent CN103211785A discloses a kind of Acipimox film-controlled slow-release micro pill capsule, discloses capsule core prescription
With sustained release clothing film prescription, said preparation early stage discharges relatively slow, but there is obvious phenomenon of burst release in the later stage, causes the later stage to discharge very fast, releases
Put unstable, and pharmaceutical release time is shorter.
Existing delayed releasing Acipimox prepn, slow-release time is shorter, has significant difference and medicine before and after rate of release
Phenomenon of burst release.
The content of the invention
Disadvantages mentioned above based on prior art, the purpose of the present inventor is intended to obtain that a kind of drug release is steady, the duration is long,
The delayed releasing Acipimox prepn of process is simple.
Hydroxypropyl methyl cellulose containing water-swellable in plain piece of the invention, hydroxypropyl methyl cellulose is after absorbing water
Substantially expansion can play a supporting role, inventor has found, Acipimox does not react with hydroxypropyl methyl cellulose, can be very well
Be attached to above, play the role of hydroxypropyl methyl cellulose, label glomeration in an aqueous medium, by appropriate Ah former times not
Among department's parcel, certain slow releasing function is played, it is to avoid the phenomenon of burst release in medicine later stage, the medicine later stage is steadily discharged.
In the selection of sustained release clothing film, inventor has found, select the polyethylene glycol of appropriate components, talcum powder with
Eurdragit NE30D mix, and gained formulation products have good stability, can long term storage, use dodecyl sulphate
Sodium can further maintain the steady release of medicine as pore-foaming agent.
By above technology, the present invention produce a kind of production efficiency high, drug release steady, process is simple, low cost, without having
The slow-releasing acipimox tablet of machine problem of solvent residual.
The present invention provides a kind of sustained release tablets comprising Acipimox.The content of slow-releasing acipimox tablet of the present invention
It is plain piece, its composition is as follows：
1) plain piece, it is composed of the following components：
Preferably：
2) clothing film is sustained, it is composed of the following components：
Preferably：
Wherein coat weight is the 10-20% of plain piece, it is preferable that coat weight is the 13-17% of plain piece, most preferably
15%.
The present invention additionally provides the preparation method of above-mentioned sustained release tablets simultaneously, comprises the following steps：
(1) Acipimox, microcrystalline cellulose, HPMC are mixed；
(2) add 50% ethanol solution appropriate to gained mixture；
(3) pelletize, dry, obtain dry particl；
(4) dry particl is well mixed, compressing tablet with appropriate silica (weight is the 1% of dry particl)；
(5) Macrogol 6000 and lauryl sodium sulfate are dissolved in the water, add EurdragitNE 30D and talcum
Powder, obtains sustained release coating liquid；
(6) plain piece is coated with coating solution, obtains sustained release tablets；
The content of described silica is the 1% of dry particl.
2 hours releases of the slow-releasing acipimox tablet obtained by the present invention can be efficiently controlled within 30%, larger
Improve to amplitude the slow release effect of medicine.In slow-releasing acipimox tablet preparation method of the present invention, Sustained release coating materials
Solvent need not be made using organic solvent, required equipment is simple, the features such as the method is had economical, safe and environment-friendly.
Specific embodiment
The present invention is further illustrated by the following examples, but these embodiments limit the present invention never in any form.
1st, influences of the Eurdragit NE 30D of different content to sustained drug release effect is explored：
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 150g, HPMC 10g, appropriate silica；
Sustained release coating is constituted：
Eurdragit the NE 30D, talcum powder 18g, polyethylene glycol of five kinds of different amounts of 48g, 60g, 75g, 96g, 105g
600012g, lauryl sodium sulfate 6g, preparation method is：
(1) Acipimox, microcrystalline cellulose, HPMC are mixed；
(2) 50% appropriate amount of ethanol softwood is added to gained mixture；
(3) pelletize, dry, obtain dry particl；
(4) dry particl is well mixed, compressing tablet with silica (weight is the 1% of dry particl)；
(5) Macrogol 6000 and lauryl sodium sulfate are dissolved in the water, add EurdragitNE 30D and talcum
Powder, obtains sustained release coating liquid；
(6) plain piece is coated with coating solution, obtains sustained release tablets；
Coat weight is the 13% of plain piece.
Experimental result is as follows：
Influence of the difference Eurdragit NE 30D consumptions of table 1. to release
From above-mentioned data, Eurdragit NE 30D have large effect, currently preferred content to release
It is 48-96g, most preferably 60g can reach its sustained release and require within this range.
2nd, influence of the sustained release coating weightening to insoluble drug release is explored：
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 150g, HPMC 10g, appropriate silica；
Sustained release coating is constituted：
Eurdragit NE 30D 60g, talcum powder 18g, Macrogol 6000 12g, lauryl sodium sulfate 6g.It is coated
Weightening is respectively 8%, 10%, 13%, 15%, 17%, the 20% of plain piece.Preparation method is with 1.
Experimental result is as follows
Influence of the different coating weight gains of table 2. to release
From above-mentioned data, coating weight gain can reach its sustained release in the range of 10-20% and require, coating weight gain 15%
When, release the drug most stable.
3rd, influence of the HPMC proportion of composing to insoluble drug release is explored：
Embodiment 1
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 150g, HPMC 5.0g, appropriate silica；
Sustained release coating is constituted：
Eurdragit NE 30D 60g, talcum powder 18g, Macrogol 6000 12g, lauryl sodium sulfate 6g, are coated
It is the 15% of plain piece to increase weight, and has following preparation method to be made：
(1) Acipimox, microcrystalline cellulose, HPMC are mixed；
(2) 50% appropriate amount of ethanol softwood is added to gained mixture；
(3) pelletize, dry, obtain dry particl；
(4) dry particl is well mixed, compressing tablet with silica (weight is the 1% of dry particl)；
(5) Macrogol 6000 and lauryl sodium sulfate are dissolved in the water, add EurdragitNE 30D and talcum
Powder, obtains sustained release coating liquid；
(6) plain piece is coated with coating solution, obtains sustained release tablets；
Embodiment 2
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 150g, HPMC 7.0g, appropriate silica；
Sustained release coating is constituted：
Eurdragit NE 30D 60g, talcum powder 18g, Macrogol 6000 12g, lauryl sodium sulfate 6g, are coated
It is the 15% of plain piece to increase weight, and preparation method is with embodiment 1.
Embodiment 3
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 150g, HPMC 10g, appropriate silica；
Sustained release coating is constituted：
Eurdragit NE 30D 60g, talcum powder 18g, Macrogol 6000 12g, lauryl sodium sulfate 6g；It is coated
It is the 15% of plain piece to increase weight, and preparation method is with embodiment 1.
Embodiment 4
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 150g, HPMC 15g, appropriate silica；
Sustained release coating is constituted：
Eurdragit NE 30D 60g, talcum powder 18g, Macrogol 6000 12g, lauryl sodium sulfate 6g, are coated
It is the 15% of plain piece to increase weight, and preparation method is with embodiment 1.
Embodiment 5
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 150g, HPMC 20g, appropriate silica；
Sustained release coating is constituted：
Eurdragit NE 30D 60g, talcum powder 18g, Macrogol 6000 12g, lauryl sodium sulfate 6g, are coated
It is the 15% of plain piece to increase weight, and preparation method is with embodiment 1.
Embodiment 6：
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 100g, HPMC 10g, appropriate silica；
Sustained release coating is constituted：
Eurdragit NE 30D 60g, talcum powder 18g, Macrogol 6000 12g, lauryl sodium sulfate 6g, are coated
It is the 15% of plain piece to increase weight, and preparation method is with embodiment 1.
Embodiment 7：
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 200g, HPMC 10g, appropriate silica；
Sustained release coating is constituted：
Eurdragit NE 30D 60g, talcum powder 18g, Macrogol 6000 12g, lauryl sodium sulfate 6g, are coated
It is the 15% of plain piece to increase weight, and preparation method is with embodiment 1.
Comparative example 1
The prescription of 1000 sustained release tablets
Compressing tablet is carried out using general tabletting method.
Comparative example 2
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 150g, 1% sodium carboxymethylcellulose are appropriate, appropriate silica；
Sustained release coating is constituted：
Eurdragit NE 30D60g, talcum powder 18g, Macrogol 6000 12g, lauryl sodium sulfate 6g are coated and increase
Weight is the 15% of plain piece；
Preparation method is with embodiment 1.
Comparative example 3
Plain piece is constituted：
Acipimox 250g, microcrystalline cellulose 150g, HPMC 30g, appropriate silica；
Sustained release coating is constituted：
Eurdragit NE 30D60g, talcum powder 18g, Macrogol 6000 12g, lauryl sodium sulfate 6g are coated and increase
Weight is the 15% of plain piece；
Preparation method is with embodiment 1.
Comparative example 4
The micropill prescription of Acipimox film-controlled slow-release micro pill capsule is as follows：
First, capsule core prescription (1000)
2nd, it is sustained clothing film prescription
Acipimox is crossed into 60 mesh sieves, and microcrystalline cellulose PH101, lactose are put and be well mixed in wet granulator, 1%
The ethanol solution softwood of sodium carboxymethylcellulose 10%, extrusion spheronization is simultaneously dried in fluid bed, and sieving is taken between 16~30 mesh
Capsule core, be then coated, coating weight gain is 14.8%, will wrap the micropill of extended release coatings in fluid bed, under the conditions of 40 DEG C/2h
Heat treatment, coating micro-pill filling capsule is obtained final product.
Checking embodiment：
Drug release determination：According to dissolution method (two methods of annex XC second of Chinese Pharmacopoeia version in 2010), with 900ml
The hydrochloric acid solution of 0.1mol/L is dissolution medium, and release is surveyed in rotating speed 50rpm, different time sampling, and concrete outcome is shown in Table 3：
The drug release determination result of each embodiment of table 3
As can be seen from Table 3：
The release of embodiment 1-7 can be controlled within 30%, and highest release has reached 99.17%；
Comparative example 1 is matrix sustained release tablet, and basic release in 8 hours is finished；
Comparative example 2 does not contain HPMC, and medicine is not wrapped up, and medicine later stage rate of release is very fast；
The HPMC that comparative example 3 is contained is excessive, and rate of release is excessively slow；
The change of the capsule core prescription of comparative example 4, causes quick release.
Find out from embodiment and comparative example's releasing result, it is of the invention by Acipimox, microcrystalline cellulose, hydroxypropyl
Cellulose not only increases the sustained level of medicine as the key component of capsule core, and drug release process is steady, has obtained preferably
Technique effect.
Claims (5)
1. a kind of slow-releasing acipimox tablet, is made up of plain piece and sustained release clothing film, it is characterised in that the component of plain piece be Ah former times not
Department, microcrystalline cellulose, HPMC and silica, described HPMC can substantially expand after absorbing water
Play a supporting role, in the presence of HPMC, label glomeration in an aqueous medium, by appropriate Acipimox
Among parcel, certain slow releasing function is played；The component for being sustained clothing film is Eurdragit NE 30D, talcum powder, polyethylene glycol
6000 and lauryl sodium sulfate, the component of described plain piece is：
100 parts of Acipimox
HPMC 2-8 parts
Microcrystalline cellulose 40-80 parts
Appropriate silica
Described sustained release clothing film each component is：
4-8 parts of Eurdragit NE 30D
1.5 parts of talcum powder
1 part of Macrogol 6000
Lauryl sodium sulfate 0.1-1 parts
Sustained release clothing film weight is the 10-20% of plain piece；
Described slow-releasing acipimox tablet is prepared by the following method：
(1) Acipimox, microcrystalline cellulose, HPMC are mixed；
(2) add 50% ethanol solution appropriate to gained mixture；
(3) pelletize, dry, obtain dry particl；
(4) dry particl is well mixed with appropriate silica, compressing tablet；
(5) Macrogol 6000 and lauryl sodium sulfate are dissolved in the water, add Eurdragit NE 30D and talcum
Powder, obtains sustained release coating liquid；
(6) plain piece is coated with coating solution, obtains sustained release tablets.
2. the slow-releasing acipimox tablet as described in claim 1, it is characterised in that plain piece each group is divided into：
100 parts of Acipimox
4 parts of HPMC
60 parts of microcrystalline cellulose
Appropriate silica.
3. the slow-releasing acipimox tablet as described in claim 1, it is characterised in that sustained release clothing film each component is：
5 parts of Eurdragit NE 30D
1.5 parts of talcum powder
1 part of Macrogol 6000
0.5 part of lauryl sodium sulfate.
4. the slow-releasing acipimox tablet as described in claim 1, it is characterised in that coat weight is the 13-17% of plain piece.
5. the slow-releasing acipimox tablet as described in claim 1, it is characterised in that coat weight is the 15% of plain piece.
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| CN201510033991.8A CN104586810B (en) | 2015-01-22 | 2015-01-22 | A kind of slow-releasing acipimox tablet and preparation method thereof |
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| CN201510033991.8A CN104586810B (en) | 2015-01-22 | 2015-01-22 | A kind of slow-releasing acipimox tablet and preparation method thereof |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1395928A (en) * | 2002-08-26 | 2003-02-12 | 鲁南制药股份有限公司 | Slow-releasing acipimox tablet |
| CN1486695A (en) * | 2003-07-04 | 2004-04-07 | 天津万斯瑞医药科技有限公司 | Delayed releasing Acipimox prepn |
| CN102188431A (en) * | 2011-05-09 | 2011-09-21 | 浙江九旭药业有限公司 | Doxazosin mesylate sustained-release tablets and preparation method thereof |
-
2015
- 2015-01-22 CN CN201510033991.8A patent/CN104586810B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1395928A (en) * | 2002-08-26 | 2003-02-12 | 鲁南制药股份有限公司 | Slow-releasing acipimox tablet |
| CN1486695A (en) * | 2003-07-04 | 2004-04-07 | 天津万斯瑞医药科技有限公司 | Delayed releasing Acipimox prepn |
| CN102188431A (en) * | 2011-05-09 | 2011-09-21 | 浙江九旭药业有限公司 | Doxazosin mesylate sustained-release tablets and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 星点设计－效应面法优化阿昔莫司控释片处方研究;郝贵周等;《齐鲁药事》;20121231;第31卷(第5期);第258-259、262页 * |
| 阿昔莫司缓释片的体外释放度及释放机制的初步研究;潘卫三等;《中国新药杂志》;20051231;第14卷(第4期);第440-444页 * |
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