CN102579390A - Ibuprofen timing release three-layer tablet drug composition and method for preparing same - Google Patents
Ibuprofen timing release three-layer tablet drug composition and method for preparing same Download PDFInfo
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- CN102579390A CN102579390A CN 201110220132 CN201110220132A CN102579390A CN 102579390 A CN102579390 A CN 102579390A CN 201110220132 CN201110220132 CN 201110220132 CN 201110220132 A CN201110220132 A CN 201110220132A CN 102579390 A CN102579390 A CN 102579390A
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Abstract
The invention relates to the technical field of drug form structures, in particular to an Ibuprofen timing release three-layer tablet drug composition and a method for preparing the same, wherein an Ibuprofen timing release three-layer tablet consists of an Ibuprofen release layer, a coated isolating layer and a coated Ibuprofen release layer, through a large number of tests and prescription screening, the Ibuprofen timing release three-layer tablet is provided for patients, so the domestic blank is filled up, and clinic medicine requirements are satisfied.
Description
Technical field
The present invention relates to a kind of pharmaceutical formulation technical field of structures, be specifically related to ibuprofen delayed release three-layer tablet pharmaceutical composition and preparation method thereof.
Background technology
Pain is a kind of complex physical mental activity, is one of modal symptom clinically.It comprises that noxious stimulation acts on the caused pain of body and feels, and body is to the pain reaction of noxious stimulation.The pain sensation can be used as a kind of warning that body comes to harm, and causes the protective reaction of body series of defence property, is the symbol of danger signal, impels people's urgent action, and hedging goes evil.
Heating is because the heating activator acts on body, and then the generation of giving birth to pyrogen (EP) in causing incorporates brain into and act on thermotaxic centre, more so that the release of the maincenter medium that causes generating heat cause then and the change of set point finally cause heating.Mainly show as body temperature and exceed arm's length standard, or the uncomfortable sensation of own fever of the body.
Ibuprofen is to go on the market in Britain nineteen sixty-eight the earliest, because antipyretic-antalgic aspect evident in efficacy, and toxicity is low, be superior to aspirin and acetaminophen, thereby market enlarges rapidly.Since ibuprofen preferably curative effect with have less untoward reaction, the U.S., Britain ratify to transfer it to nonprescription drugs from prescription drugs in succession.To early 1990s, the sales volume of world market Motrin has broken through 1,000,000,000 dollars of high pointes, is to break through 1,000,000,000 dollars antipyretic analgesic product the earliest.
Good antipyretic-antalgic effect has also driven the exploitation listing of numerous dosage forms; Be peroral dosage form and local form of administration; Like tablet, capsule, dry suspension, granule, drop, effervescent tablet, oral cavity disintegration tablet and ointment, gel, liniment, the injection type list marketing is not arranged as yet.And the injection market of U.S.'s treatment pain reached about 6.79 hundred million dollars in 2008, and this explanation ibuprofen kind also has huge market potential.
Ibuprofen is well-known general medicine kind, and crude drug is cheap, and production cost is very low.Domestic pain market capacity is huge, and ibuprofen is that numerous doctor patients know in addition, and marketing is easy, can predict the exploitation listing of ibuprofen injection, considerable economic benefit and social benefit surely.
Common name: ibuprofen
English name: Ibuprofen
Chemical name: 4-isobutyl group-Alpha-Methyl phenylacetic acid
Structural formula:
Molecular formula: C
13H
18O
2
Molecular weight: 206.28
Pharmacology type: NSAID.
Mechanism of action: the mechanism of ibuprofen antiinflammatory refrigeration function is synthetic relevant with the inhibition prostaglandin.Prostaglandin is a kind of endogenic pyrogen and inflammatory mediator, and ibuprofen is synthetic through suppressing Cycloxygenase (COX) and then suppressing prostaglandin (PG), and inflammatory reaction, heating and the pain that causes is assembled in alleviation because of prostaglandin.
According to the clinical practice needs, consider that ibuprofen should satisfy the release request of different periods, through being test and prescription screening in a large number,, filled up domestic blank for extensive patients provides a kind of ibuprofen delayed release three-layer tablet, satisfy the clinical application demand.
Chinese patent CN200810229131.1 relates to brufen composition; Said composition contains ibuprofen and the vitamin C and the pharmaceutic adjuvant of treating effective dose; Wherein ibuprofen and ascorbic weight ratio are 1: 1-1.4; Preferred 1: 1.2, said composition can effectively reduce mouth and the bottleneck throat burn feeling that ibuprofen produces.
Chinese patent CN200710061682.7 discloses the new pharmaceutical composition of a kind of ibuprofen; Wherein ibuprofen can be the free acid of ibuprofen, the salt of ibuprofen or their combination in any, or the combination of the pseudoephedrine hydrochloride of ibuprofen and medically acceptable dosage.This new compositions has overcome the shortcoming that the existing product bioavailability is low, peak time is long, has improved the curative effect of medicine.
Chinese patent CN200610070783.6 discloses a kind of (s)-ibuprofen granules and method for preparing; It is characterized in that containing in its composition following materials of weight proportions: (S)-ibuprofen 1; Alkaline auxiliary solvent 0-100, filler 0.1-100, binding agent 0.1-12; Correctives 0.01-0.5, lubricant 0.1-2.Its preparation method is each component mixing, granulation, packing.The present invention has overcome ordinary preparations such as traditional oral (S)-ibuprofen tablet, capsule, dispersible tablet, oral administration mixed suspension; Shortcoming such as be difficult for dissolving, absorption difference, bioavailability is low, onset is relatively slow; Be convenient to (S)-ibuprofen dissolving in water rapidly, form transparent and delicious solution, have taking convenience, bioavailability is high, onset is rapid; Carry advantage more easily and compare also to have with the common liq preparation.
Summary of the invention
The object of the invention just is according to existing adjuvant and working condition; Guaranteeing to have lower production cost and simple preparation technology; Be suitable under the prerequisite of large-scale industrial production; Be necessary to work out a kind of suitable prescription and form and preparation technology, can produce ibuprofen delayed release three-layer tablet pharmaceutical composition, make it have good bioavailability and stability of drug products.
The object of the present invention is to provide a kind of ibuprofen delayed release three-layer tablet pharmaceutical composition and preparation method thereof, it can overcome the deficiency of prior art, efficiently solves the problem that ibuprofen regularly discharges.
The purpose of this invention is to provide a kind of ibuprofen delayed release three-layer tablet.
Ibuprofen delayed release three-layer tablet pharmaceutical composition provided by the present invention and preparation method thereof prepares 1000, and compositing formula is following:
The A granule
B granule sealing coat
Ibuprofen delayed release three-layer tablet pharmaceutical composition provided by the present invention and preparation method thereof prepares 1000 method for preparing, following steps:
1) get ibuprofen, the pregelatinized Starch of recipe quantity, mix homogeneously adopts 2.5% methocel solution, and 20 eye mesh screens are granulated, 50 ± 5 ℃ of dryings, and granulate, subsequent use;
2) with 1) middle pregelatinized Starch, carboxymethyl starch sodium, polyvinylpolypyrrolidone, the magnesium stearate that adds the residue recipe quantity, be mixed and made into granule A;
3) with hydroxypropyl cellulose K15M, hydroxypropyl cellulose K4, mannitol, Pulvis Talci, the blue shallow lake mix homogeneously of recipe quantity, adopt 10% polyvidone alcoholic solution, 20 eye mesh screens are granulated, 50 ± 5 ℃ of dryings, and granulate makes granule B;
4) tabletting: be pressed into cylindric three-layer tablet, granule B is in the centre;
5) coating: carriage rotation (hole) the coating machine with particular design, one of three-layer tablet is inserted in this hole, expose portion (containing the sealing coat and the second medicine layer) with 5% cellulose ether methanol solution spray coating, gets not infiltration layer of thickness 0.2mm water.
6) drying promptly gets ibuprofen delayed release three-layer tablet pharmaceutical composition and preparation method thereof.
Ibuprofen delayed release three-layer tablet pharmaceutical composition provided by the present invention and preparation method thereof, ground floor medicine layer is the rapid release effect, second layer medicine layer is a slow release effect, time lag 4.5-5.0 hour in vivo.
Among the present invention,, optimized its recipe quantity, solved it and regularly discharged problem through the screening of tens of times test recipes and the summary of test data, and constant product quality.
The inventor finds through great deal of experimental, when the ibuprofen pharmaceutical compositions is above-mentioned prescription, and described pharmaceutical composition the best in quality, stability is best, and yield rate is high, is prone to industrialized implementation.
Another aspect of the present invention provides the method for preparing of ibuprofen delayed release three-layer tablet of the present invention, and this method is simple, prepared ibuprofen delayed release three-layer tablet good stability.
The specific embodiment
Below in conjunction with specific embodiment ibuprofen delayed release three-layer tablet pharmaceutical composition of the present invention and preparation method thereof structure is specified to help understanding content of the present invention.
Embodiment 1
Prepare 1000 ibuprofen delayed release three-layer tablets, compositing formula is following:
The A granule
During making:
1) get ibuprofen, the pregelatinized Starch of recipe quantity, mix homogeneously adopts 2.5% methocel solution, and 20 eye mesh screens are granulated, 50 ± 5 ℃ of dryings, and granulate, subsequent use;
2) with 1) middle pregelatinized Starch, carboxymethyl starch sodium, polyvinylpolypyrrolidone, the magnesium stearate that adds the residue recipe quantity, be mixed and made into granule A;
3) with hydroxypropyl cellulose K15M, hydroxypropyl cellulose K4, mannitol, Pulvis Talci, the blue shallow lake mix homogeneously of recipe quantity, adopt 10% polyvidone alcoholic solution, 20 eye mesh screens are granulated, 50 ± 5 ℃ of dryings, and granulate makes granule B;
4) tabletting: be pressed into cylindric three-layer tablet, granule B is in the centre;
5) coating: carriage rotation (hole) the coating machine with particular design, one of three-layer tablet is inserted in this hole, expose portion (containing the sealing coat and the second medicine layer) with 5% cellulose ether methanol solution spray coating, gets not infiltration layer of thickness 0.2mm water.
6) drying promptly gets ibuprofen delayed release three-layer tablet pharmaceutical composition and preparation method thereof.
Embodiment 2
Simulate big production scale,, amplify and produce 3 batches with 30,000 every batch.
Through evidence: product formulation and technology simple possible.Be packaged in 40 ℃ ± 2 ℃ through three batches of products with listing, the accelerated test condition held 6 months of relative humidity 75% ± 5% and long term test condition were placed 6 months, and the result shows, the more stable accords with production requirement of quality.
Test Example 1
Get embodiment 1, the embodiment 2 fragrant delayed release three-layer tablet in Lip river of 4 batches of different batches altogether, investigate its release degree, see the following form:
Can know by above result of the test: the fragrant delayed release three-layer tablet in Lip river, ibuprofen steadily slowly discharges, and effectively guarantees clinical demand, and batch differences is little, steady quality.
Claims (2)
1. an ibuprofen delayed release three-layer tablet is characterized in that, its described ibuprofen delayed release three-layer tablet, and per 1000 its prescriptions consist of:
The A granule
B granule sealing coat
2. the method for preparing of ibuprofen delayed release three-layer tablet according to claim 1 is characterized in that this method comprises the steps:
1) get ibuprofen, the pregelatinized Starch of recipe quantity, mix homogeneously adopts 2.5% methocel solution, and 20 eye mesh screens are granulated, 50 ± 5 ℃ of dryings, and granulate, subsequent use;
2) with 1) middle pregelatinized Starch, carboxymethyl starch sodium, polyvinylpolypyrrolidone, the magnesium stearate that adds the residue recipe quantity, be mixed and made into granule A;
3) with hydroxypropyl cellulose K15M, hydroxypropyl cellulose K4, mannitol, Pulvis Talci, the blue shallow lake mix homogeneously of recipe quantity, adopt 10% polyvidone alcoholic solution, 20 eye mesh screens are granulated, 50 ± 5 ℃ of dryings, and granulate makes granule B;
4) tabletting: be pressed into cylindric three-layer tablet, granule B is in the centre;
5) coating: carriage rotation (hole) the coating machine with particular design, one of three-layer tablet is inserted in this hole, expose portion (containing the sealing coat and the second medicine layer) with 5% cellulose ether methanol solution spray coating, gets not infiltration layer of thickness 0.2mm water;
6) drying promptly gets ibuprofen delayed release three-layer tablet.
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|---|---|---|---|
| CN 201110220132 CN102579390A (en) | 2011-08-03 | 2011-08-03 | Ibuprofen timing release three-layer tablet drug composition and method for preparing same |
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| CN 201110220132 CN102579390A (en) | 2011-08-03 | 2011-08-03 | Ibuprofen timing release three-layer tablet drug composition and method for preparing same |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105935445A (en) * | 2016-03-28 | 2016-09-14 | 赤峰赛林泰药业有限公司 | 2-(-4-isobutylphenyl)propionic acid dextrogyre-containing pharmaceutical composition and preparation method thereof |
| CN110037994A (en) * | 2019-05-24 | 2019-07-23 | 中国药科大学 | A kind of brufen quick-release and slow-release double-layer tablets and preparation method thereof |
| GB2585414A (en) * | 2019-02-22 | 2021-01-13 | Catalent Uk Swindon Zydis Ltd | Minimizing agglomeration, aeration, and preserving the coating of pharmaceutical compositions comprising ibuprofen |
| US11026892B2 (en) | 2019-02-22 | 2021-06-08 | Catalent U.K. Swindon Zydis Limited | Minimizing agglomeration of drug particle coating material during storage to stabilize disintegration times of pharmaceutical products |
| US11185508B2 (en) | 2019-02-22 | 2021-11-30 | Catalent U.K. Swindon Zydis Limited | Preserving functionally-coated API particles produced by solventless mixing processes in aqueous suspension |
-
2011
- 2011-08-03 CN CN 201110220132 patent/CN102579390A/en active Pending
Cited By (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105935445A (en) * | 2016-03-28 | 2016-09-14 | 赤峰赛林泰药业有限公司 | 2-(-4-isobutylphenyl)propionic acid dextrogyre-containing pharmaceutical composition and preparation method thereof |
| CN105935445B (en) * | 2016-03-28 | 2019-02-01 | 赤峰赛林泰药业有限公司 | Pharmaceutical composition and preparation method thereof containing 2- (- 4- isobutyl phenenyl) propionic acid dextrogyre |
| US11141380B2 (en) | 2019-02-22 | 2021-10-12 | Catalent U.K. Swindon Zydis Limited | Minimizing agglomeration of drug particle coating material during storage to stabilize disintegration times of pharmaceutical products |
| GB2585414A (en) * | 2019-02-22 | 2021-01-13 | Catalent Uk Swindon Zydis Ltd | Minimizing agglomeration, aeration, and preserving the coating of pharmaceutical compositions comprising ibuprofen |
| US11026892B2 (en) | 2019-02-22 | 2021-06-08 | Catalent U.K. Swindon Zydis Limited | Minimizing agglomeration of drug particle coating material during storage to stabilize disintegration times of pharmaceutical products |
| US11077067B2 (en) | 2019-02-22 | 2021-08-03 | Catalent U.K. Swindon Zydis Limited | Minimizing agglomeration, aeration, and preserving the coating of pharmaceutical compositions comprising ibuprofen |
| US11166919B2 (en) | 2019-02-22 | 2021-11-09 | Catalent U.K. Swindon Zydis Limited | Minimizing agglomeration, aeration, and preserving the coating of pharmaceutical compositions comprising ibuprofen |
| US11185508B2 (en) | 2019-02-22 | 2021-11-30 | Catalent U.K. Swindon Zydis Limited | Preserving functionally-coated API particles produced by solventless mixing processes in aqueous suspension |
| GB2597577A (en) * | 2019-02-22 | 2022-02-02 | Catalent Uk Swindon Zydis Ltd | Minimizing agglomeration, aeration, and preserving the coating of pharmaceutical compositions comprising ibuprofen |
| GB2585414B (en) * | 2019-02-22 | 2023-06-14 | Catalent Uk Swindon Zydis Ltd | Minimizing agglomeration, aeration, and preserving the coating of pharmaceutical compositions comprising ibuprofen |
| GB2597577B (en) * | 2019-02-22 | 2023-09-20 | Catalent Uk Swindon Zydis Ltd | Minimizing agglomeration, aeration, and preserving the coating of pharmaceutical compositions comprising ibuprofen |
| US11779540B2 (en) | 2019-02-22 | 2023-10-10 | Catalent U.K. Swindon Zydis Limited | Minimizing agglomeration of drug particle coating material during storage to stabilize disintegration times of pharmaceutical products |
| US11931464B2 (en) | 2019-02-22 | 2024-03-19 | Catalent U.K. Swindon Zydis Limited | Minimizing agglomeration, aeration, and preserving the coating of pharmaceutical compositions comprising ibuprofen |
| CN110037994A (en) * | 2019-05-24 | 2019-07-23 | 中国药科大学 | A kind of brufen quick-release and slow-release double-layer tablets and preparation method thereof |
| CN110037994B (en) * | 2019-05-24 | 2022-04-12 | 中国药科大学 | Ibuprofen quick-release and slow-release double-layer tablet and preparation method thereof |
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Application publication date: 20120718 |