CN101204380A - Sustained-release coated pellets for 24 hours - Google Patents
Sustained-release coated pellets for 24 hours Download PDFInfo
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- CN101204380A CN101204380A CN 200610165403 CN200610165403A CN101204380A CN 101204380 A CN101204380 A CN 101204380A CN 200610165403 CN200610165403 CN 200610165403 CN 200610165403 A CN200610165403 A CN 200610165403A CN 101204380 A CN101204380 A CN 101204380A
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- ball core
- hypromellose
- coated pellets
- piller
- acrylic acid
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Abstract
The invention discloses a controlled-release coating pellet that lasts for 24 hours. The coating pellet, which is composed of a pellet core containing venlafaxine hydrochloride, microcrystalline cellulose and hydroxypropyl methylcellulose, an isolated layer and a controlled-release layer, is mainly used for curing diseases such as depression, anxiety, and panic, etc.
Description
Technical field
The present invention relates to a kind of sustained release coating piller that can continue release in 24 hours, particularly a kind of sustained release coating piller that contains VENLAFAXINE HCL.
Background technology
Venlafaxine (Venlafaxine), it is a kind of novel antidepressant with unique chemical constitution and neuropharmacology effect, it also is a kind of effective antianxiety drugs, venlafaxine is applied with the form of hydrochlorate, its chemistry (±)-1-[2-(2-methylamino) by name-1-(4-anisyl) ethyl] the Hexalin hydrochlorate, he brings into play antidepressant effect by the reuptake of retardance NE and two kinds of mediators of 5-HT, result of study shows venlafaxine and Clomipramine, amitriptyline, the Sertraline therapeutic equivalence, be better than maprotiline, and side reaction is far below above-mentioned all medicines, and rapid-action.At present adult's consumption of VENLAFAXINE HCL tablet is 350mg/ days, and natural gift are taken for 2 to 3 times, repeatedly during medication, easily causes feeling sick, drowsiness.
Chinese patent CN97109594 discloses the slow releasing preparation of the capsulated VENLAFAXINE HCL of a kind of usefulness, it comprises bead and the hard gelatin capsule that contains effective therapeutic dose, this bead is made up of VENLAFAXINE HCL, microcrystalline Cellulose and hypromellose, with one deck coating solution (ethyl cellulose and hypromellose mixture) coating; Because the fine little element of ethyl has easily right, zest, so when big production, if adopt common coating pan coating, then exist the danger of blast, the dust that produces in operating process produces strong impulse to the eyes of human body; The coating solution that adopts in this patent is dichloromethane and absolute methanol simultaneously, has the shortcoming of the higher and organic solvent residual of cost.
The present invention is based on above-mentioned shortcoming, invented the venlafaxine hydrochloride sustained-release capsule of a kind of easy operating, organic solvent-free residue problem.
Summary of the invention
The object of the invention provides a kind of sustained release coating piller of stable, easy operating, and this coated pellets is made up of ball core, sealing coat and the slow release layer of hydrochloric venlafaxine, microcrystalline Cellulose and hypromellose.
The applicant finds on the bases of a large amount of tests, and respectively to ball core bag sealing coat and slow release layer, when reaching same effect, easy operating, organic solvent-free are residual.
As suitable sustained release coating piller provided by the present invention, contain ball core, sealing coat and slow release layer by hydrochloric venlafaxine, microcrystalline Cellulose and hypromellose.
As suitable sealing coat provided by the present invention, containing weight is the hypromellose of 3%~10% (the ball core of double-layer coatings is the basis).
As suitable sealing coat provided by the present invention, containing weight is the hypromellose of 5%~7% (the ball core of double-layer coatings is the basis).
As suitable slow release layer provided by the present invention, containing weight is 5%~15% (based on the piller of ground floor coating) acrylic acid resinae
As suitable acrylic acid resinae provided by the present invention, containing weight is acrylic acid ethyl ester/methyl methacrylate polymer, the acrylic acid ethyl ester/methyl methacrylate/methyl-prop diluted acid chlorination trimethylamine groups polymerizable methacrylate thing of 7%~10% (based on the piller of ground floor coating).
Specific embodiment
The present invention is described in further detail below in conjunction with embodiment, but not only be confined to following embodiment.
Embodiment 1:
Preparation technology:
1. take by weighing VENLAFAXINE HCL, hypromellose, the microcrystalline Cellulose mix homogeneously of recipe quantity, it is an amount of to add water, and the system soft material adopts and extrudes spheronizator extruding balling-up, gets the ball core;
2. use coating solution that forms by hypromellose and the coating solution that forms by acrylic acid resin RS100, acrylic acid resin RL100 that the ball core is wrapped sealing coat and slow release layer respectively, promptly get the sustained release coating piller.
Embodiment 2:
Preparation technology:
1. take by weighing VENLAFAXINE HCL, hypromellose, the microcrystalline Cellulose mix homogeneously of recipe quantity, it is an amount of to add water, and the system soft material adopts and extrudes spheronizator extruding balling-up, gets the ball core;
2. use coating solution that forms by hypromellose and the coating solution that forms by acrylic acid resin NE30D that the ball core is wrapped sealing coat and slow release layer respectively, promptly get the sustained release coating piller.
Embodiment 3:
Preparation technology:
1. take by weighing VENLAFAXINE HCL, hypromellose, the microcrystalline Cellulose mix homogeneously of recipe quantity, it is an amount of to add water, and the system soft material adopts and extrudes spheronizator extruding balling-up, gets the ball core;
2. use coating solution that forms by hypromellose and the coating solution that forms by acrylic acid resin RSl00, acrylic acid resin RLl00 that the ball core is wrapped sealing coat and slow release layer respectively, promptly get the sustained release coating piller.
Embodiment 4:
Preparation technology:
1. take by weighing VENLAFAXINE HCL, hypromellose, the microcrystalline Cellulose mix homogeneously of recipe quantity, it is an amount of to add water, and the system soft material adopts and extrudes spheronizator extruding balling-up, gets the ball core;
2. use coating solution that forms by hypromellose and the coating solution that forms by acrylic acid resin RS30D, acrylic acid resin RL30D that the ball core is wrapped sealing coat and slow release layer respectively, promptly get the sustained release coating piller.
Embodiment 1 drug release determination result:
Embodiment 1 drug release determination result:
Meet the requirement of the relevant release of the national drug standards.
Claims (5)
1. sustained release coating piller that can 24 hours continues to discharge, the ball core contains VENLAFAXINE HCL, microcrystalline Cellulose and hypromellose, and it is levied and is that the ball core wraps sealing coat and slow release layer respectively.
2. coated pellets according to claim 1 is characterized in that described sealing coat comprises the hypromellose that weight is 3%~10% (the ball core of double-layer coatings is the basis).
3. coated pellets according to claim 1 and 2 is characterized in that described sealing coat comprises the hypromellose that weight is 5%~7% (based on the ball core of double-layer coatings).
4. coated pellets according to claim 1 is characterized in that it is 5%~15% (based on the piller of ground floor coating) acrylic acid resinae that described slow release layer comprises weight.
5. according to claim 1 or 4 described coated pellets, it is characterized in that described crylic acid resin comprises acrylic acid ethyl ester/methyl methacrylate polymer, the acrylic acid ethyl ester/methyl methacrylate/methyl-prop diluted acid chlorination trimethylamine groups polymerizable methacrylate thing that weight is 7%~10% (based on the piller of ground floor coating).
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN 200610165403 CN101204380A (en) | 2006-12-19 | 2006-12-19 | Sustained-release coated pellets for 24 hours |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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CN 200610165403 CN101204380A (en) | 2006-12-19 | 2006-12-19 | Sustained-release coated pellets for 24 hours |
Publications (1)
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CN101204380A true CN101204380A (en) | 2008-06-25 |
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Family Applications (1)
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CN 200610165403 Pending CN101204380A (en) | 2006-12-19 | 2006-12-19 | Sustained-release coated pellets for 24 hours |
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102085197A (en) * | 2010-12-14 | 2011-06-08 | 北京万生药业有限责任公司 | Venlafaxine slow-release preparation and preparation method thereof |
CN102293737A (en) * | 2011-09-14 | 2011-12-28 | 北京德众万全药物技术开发有限公司 | Sustained release preparation of Venlafaxine |
CN102772390A (en) * | 2012-08-16 | 2012-11-14 | 河南新帅克制药股份有限公司 | Venlafaxine hydrochloride sustained release capsule and preparation method thereof |
CN103006618A (en) * | 2012-12-14 | 2013-04-03 | 中国药科大学 | Anti-depression slow-release capsule |
CN103893151A (en) * | 2012-12-31 | 2014-07-02 | 石药集团中奇制药技术(石家庄)有限公司 | Venlafaxine hydrochloride sustained release capsule and preparation method thereof |
-
2006
- 2006-12-19 CN CN 200610165403 patent/CN101204380A/en active Pending
Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102085197A (en) * | 2010-12-14 | 2011-06-08 | 北京万生药业有限责任公司 | Venlafaxine slow-release preparation and preparation method thereof |
CN102085197B (en) * | 2010-12-14 | 2013-08-14 | 北京万生药业有限责任公司 | Venlafaxine slow-release preparation and preparation method thereof |
CN102293737A (en) * | 2011-09-14 | 2011-12-28 | 北京德众万全药物技术开发有限公司 | Sustained release preparation of Venlafaxine |
CN102772390A (en) * | 2012-08-16 | 2012-11-14 | 河南新帅克制药股份有限公司 | Venlafaxine hydrochloride sustained release capsule and preparation method thereof |
CN102772390B (en) * | 2012-08-16 | 2014-01-08 | 乐普药业股份有限公司 | Venlafaxine hydrochloride sustained release capsule and preparation method thereof |
CN103006618A (en) * | 2012-12-14 | 2013-04-03 | 中国药科大学 | Anti-depression slow-release capsule |
CN103893151A (en) * | 2012-12-31 | 2014-07-02 | 石药集团中奇制药技术(石家庄)有限公司 | Venlafaxine hydrochloride sustained release capsule and preparation method thereof |
CN103893151B (en) * | 2012-12-31 | 2018-04-27 | 石药集团中奇制药技术(石家庄)有限公司 | A kind of venlafaxine hydrochloride slow-release capsule and preparation method thereof |
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PB01 | Publication | ||
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Open date: 20080625 |