CN102160855A - Dex-ibuprofen sustained release tablets and preparation method thereof - Google Patents
Dex-ibuprofen sustained release tablets and preparation method thereof Download PDFInfo
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- CN102160855A CN102160855A CN2011100786082A CN201110078608A CN102160855A CN 102160855 A CN102160855 A CN 102160855A CN 2011100786082 A CN2011100786082 A CN 2011100786082A CN 201110078608 A CN201110078608 A CN 201110078608A CN 102160855 A CN102160855 A CN 102160855A
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Abstract
The invention belongs to the technical field of pharmacy, and in particular relates to a prescription and preparation of dex-ibuprofen sustained release tablets. The dex-ibuprofen sustained release tablets are prepared by mixing a quick release part, a sustained release part and magnesium stearate, wherein the quick release part comprises the following components in part by weight: 40 to 80 parts of dex-ibuprofen, 31.0 to 240 parts of starch, 10.0 to 60 parts of hydroxypropylcellulose, and 1.0 to 5.0 parts of 3 mass percent of hydroxypropyl methylcellulose solution; the sustained release part comprises the following components in part by weight: 220 to 260 parts of dex-ibuprofen, 10 to 40 parts of microcrystalline cellulose, 40 to 130 parts of hydroxypropyl methyl cellulose and 2.0 to 8.0 parts of ethyecellulose; and the magnesium stearate accounts for 3.0 to 18.0 weight parts of the total weight. The dex-ibuprofen sustained release tablets prolong the release time of the medicine in vivo, are easily absorbed by a human body, reduce irritation to gastrointestinal tract and improve the bioavailability.
Description
Technical field
The invention belongs to the pharmaceutical technology field, be specifically related to a kind of prescription and preparation of Dexibuprofen sustained-release sheet.
Background technology
Raw material: (S)-ibuprofen
Chemical name: S (+)-2 (4-isobutylphenyl) Propionic acid
English name: Dexibuprofen
Molecular formula: C
13H
18O
2
Molecular weight: 206.28
Structural formula:
(S)-ibuprofen is non-deep and remote body class antibiotic medicine, mainly is to suppress the synthetic of Cycloxygenase and prostaglandin and reach antiinflammatory, analgesic activity, and plays refrigeration function by the hypothalamus center of body temperature regulation.Has application value.
Be used for 1 clinically at present more, alleviate the acute attack stage of various chronic arthritiss such as rheumatoid arthritis, osteoarthritis, SpA, gouty arthritis, rheumatic arthritis or the arthralgia condition of illness of persistence, anosis effect because of the treatment and the control course of disease; 2. treat non-arthrogenous various soft tissue rheumatism pain, as shoulder pain, key vaginitis, bursitis, the damaging pain of myalgia and motion back etc.; 3. acute light, moderate pain as; After operation back, the wound, oldly decrease back, primary dysmenorrhea, toothache, headache etc.; 4. the heating to adult and child has refrigeration function.
At present, the (S)-ibuprofen of listing only has tablet, capsule and suppository, and oral formulations such as tablet and capsule exist and absorb shortcomings such as inhomogeneous, that first pass effect is strong, bioavailability is low, the decrement when being not easy to special disease such as old people is taken.The subject matter of suppository is to use inconvenience, and its suitable crowd only is defined in pediatric patient.There is no any slow releasing preparation and be seen in report.
Summary of the invention
Dosage form at existing medicine absorbs defectives such as inhomogeneous, that first pass effect is strong, bioavailability is low, the invention provides a kind of Dexibuprofen sustained-release sheet, prolong drug release time in vivo, help absorption of human body, minimizing irritates gastrointestinal, improves bioavailability.
1, a kind of Dexibuprofen sustained-release sheet of the present invention is made up of immediate release section, slow-released part and magnesium stearate mixing;
The immediate release section prescription according to the weight portion formulation ratio that accounts for gross weight is:
The slow-released part prescription according to the weight portion formulation ratio that accounts for gross weight is:
The weight portion of the shared gross weight of described magnesium stearate is 3.0 parts-18.0 parts.
Dexibuprofen sustained-release sheet optimum ratio of the present invention is as follows:
The immediate release section prescription according to the weight portion formulation ratio that accounts for gross weight is:
The slow-released part prescription according to the weight portion formulation ratio that accounts for gross weight is:
The weight portion of the shared gross weight of described magnesium stearate is 9.0 parts.
The method for preparing Dexibuprofen sustained-release sheet of the present invention, step is:
(1) preparation of slow-released part
Get (S)-ibuprofen, microcrystalline Cellulose, hydroxypropyl emthylcellulose according to the described formulation ratio mixing of claim 1, sieve with 80 orders; Alcoholic solution with ethyl cellulose and hydroxypropyl methylcellulose mixtures is made soft material with said mixture; After secondary is crossed 30 mesh sieves; Dry 12h down for 40 ℃;
(2) preparation of immediate release section
Mix according to the described formulation ratio of claim 1, dry behind 30 mesh sieves excessively;
(3) preparation of slow releasing tablet
After above two kinds of granules mixing, by 30 mesh sieve granulate; The magnesium stearate mixing that adds the described weight portion of claim 1; Last tabletting gets the Dexibuprofen sustained-release sheet.
Advantage of the present invention is: Dexibuprofen sustained-release sheet provided by the invention, prolong drug release time in vivo help absorption of human body, and improve bioavailability.The release in vitro degree first hour was 15%---35%, and second hour is 30%---55%, and the 4th hour is 50%---75%, and the 7th hour is 65%---90%, and the tenth hour is more than 85%. the pharmacokinetics of dog oral administration shows:
The specific embodiment
The present invention is further illustrated according to specific embodiment below, but do not mean that restriction protection scope of the present invention.
One, prescription
Two, prescription foundation
1, (S)-ibuprofen dosage
With reference to the dosage of ibuprofen in the ibuprofen modified release capsule and decide.
2, the selection of adjuvant and consumption thereof
The guiding theory of this sustained-release tablet recipe design, it is very fast to be to make the (S)-ibuprofen onset to produce, and clinical effectiveness is stronger, and release continues longer.Therefore, each composition reference literature of will writing out a prescription is earlier made rapid release and two kinds of granules of slow release respectively; And then mix; Carry out tabletting at last.By prerun, 26 prescriptions of preliminary examination, screening different auxiliary material and consumption and pressure are index with the cumulative in vitro release, selected proper supplementary material, consumption and pressure.Now selecting 7 prescriptions is summarized as follows:
The composition (g) of table 1, seven different prescriptions
No. 6 and No. 7 different pressures of writing out a prescription together of notes *
1-5 number is 200 recipe quantity; 6, No. 7 is 400 recipe quantity.
The cumulative release degree (%) of table 2, seven different prescription slow releasing tablet
(assay method is seen data NO.7)
Comprehensive above-mentioned The selection result is chosen the hydroxypropyl emthylcellulose and the ethyl cellulose of proper proportion macromolecular material and is made the purpose that matrix sustained release tablet can reach the slow release (S)-ibuprofen and prolong drug effect.The result of the cumulative release degree of eight prescriptions shows that No. eight prescription wherein is fit to and satisfies the clinical treatment requirement, is more excellent scheme.
Three, preparation technology
(1) preparation of slow-releasing granules
Get (S)-ibuprofen, microcrystalline Cellulose, hydroxypropyl emthylcellulose and mix, sieve with 80 orders according to above-mentioned formulation ratio; Alcoholic solution with ethyl cellulose and hydroxypropyl methylcellulose mixtures is made soft material with said mixture; After secondary is crossed 30 mesh sieves; Dry 12h down for 40 ℃;
(2) preparation of immediate-release granules
Above-mentioned formulation ratio mixes, and dries behind 30 mesh sieves excessively;
(3) preparation of slow releasing tablet
After above two kinds of granules mixing, by 30 mesh sieve granulate; Add the magnesium stearate mixing; Last tabletting gets the Dexibuprofen sustained-release sheet.
Four, the effect of adjuvant in prescription
The starch disintegrating agent;
The microcrystalline Cellulose disintegrating agent;
Ethyl cellulose blocker binding agent;
The hydroxypropyl cellulose binding agent;
Hydroxypropyl emthylcellulose binding agent blocker;
Magnesium;
Five, adjuvant source and quality standard
Starch: Fructus Vitis viniferae sugar refinery, Hunan, Chinese Pharmacopoeia;
Microcrystalline Cellulose: Shanghai pharmaceutic adjuvant factory, Q/WS-1133-82 difficult to understand;
Ethyl cellulose: Britain blocks happy Kanggong department, American Pharmacopeia;
Hydroxypropyl emthylcellulose: Britain blocks happy Kanggong department, American Pharmacopeia;
Hydroxypropyl cellulose: Shenyang No. 1 Pharmaceutical Factory, Chinese Pharmacopoeia.
Six, documents and materials
Luo Mingsheng etc., pharmaceutical necessities complete works, 1993.3, P648,743,806.
Claims (3)
1. a Dexibuprofen sustained-release sheet is characterized in that, is mixed by immediate release section, slow-released part and magnesium stearate and forms;
The immediate release section prescription according to the weight portion formulation ratio that accounts for gross weight is:
The slow-released part prescription according to the weight portion formulation ratio that accounts for gross weight is:
The weight portion of the shared gross weight of described magnesium stearate is 3.0 parts-18.0 parts.
2. according to the described Dexibuprofen sustained-release sheet of claim 1, it is characterized in that the immediate release section prescription according to the weight portion formulation ratio that accounts for gross weight is:
The slow-released part prescription according to the weight portion formulation ratio that accounts for gross weight is:
The weight portion of the shared gross weight of described magnesium stearate is 9.0 parts.
3. prepare the method for the described Dexibuprofen sustained-release sheet of claim 1, it is characterized in that, step is:
(1) preparation of slow-released part
Get (S)-ibuprofen, microcrystalline Cellulose, hydroxypropyl emthylcellulose according to the described formulation ratio mixing of claim 1, sieve with 80 orders; Alcoholic solution with ethyl cellulose and hydroxypropyl methylcellulose mixtures is made soft material with said mixture; After secondary is crossed 30 mesh sieves; Dry 12h down for 40 ℃;
(2) preparation of immediate release section
Mix according to the described formulation ratio of claim 1, dry behind 30 mesh sieves excessively;
(3) preparation of slow releasing tablet
After above two kinds of granules mixing, by 30 mesh sieve granulate; The magnesium stearate mixing that adds the described weight portion of claim 1; Last tabletting gets the Dexibuprofen sustained-release sheet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011100786082A CN102160855B (en) | 2011-03-30 | 2011-03-30 | Dex-ibuprofen sustained release tablets and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN2011100786082A CN102160855B (en) | 2011-03-30 | 2011-03-30 | Dex-ibuprofen sustained release tablets and preparation method thereof |
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| CN102160855A true CN102160855A (en) | 2011-08-24 |
| CN102160855B CN102160855B (en) | 2013-01-23 |
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| CN2011100786082A Expired - Fee Related CN102160855B (en) | 2011-03-30 | 2011-03-30 | Dex-ibuprofen sustained release tablets and preparation method thereof |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013154512A1 (en) * | 2012-04-13 | 2013-10-17 | Mahmut Bilgic | Pharmaceutical formulations comprising dexibuprofen |
| CN103417505A (en) * | 2012-05-24 | 2013-12-04 | 中国科学院上海药物研究所 | Huperzine A controlled release preparation having biphasic release behavior, and preparation method thereof |
| CN105579033A (en) * | 2013-09-27 | 2016-05-11 | 强生消费者公司 | Compression coated pulsatile release compositions |
| 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 |
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| CN1972666A (en) * | 2003-09-26 | 2007-05-30 | 阿尔扎公司 | OROS push-stick for controlled delivery of active agents |
| CN101073563A (en) * | 2007-02-07 | 2007-11-21 | 西安利君制药有限责任公司 | Chiral composition containing dextrothyroxine buprofenli and levomethadyl cysteliqin and its double slow-releasing tablet |
| CN101784262A (en) * | 2007-08-15 | 2010-07-21 | 麦克内尔-Ppc股份有限公司 | Immediate release and sustained release ibuprofen dosing regiment |
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2011
- 2011-03-30 CN CN2011100786082A patent/CN102160855B/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1972666A (en) * | 2003-09-26 | 2007-05-30 | 阿尔扎公司 | OROS push-stick for controlled delivery of active agents |
| CN101073563A (en) * | 2007-02-07 | 2007-11-21 | 西安利君制药有限责任公司 | Chiral composition containing dextrothyroxine buprofenli and levomethadyl cysteliqin and its double slow-releasing tablet |
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| 《沈阳药科大学学报》 19960131 牟晓虹等 布洛芬缓释片的制备及工艺研究 第5-8页，第40页 1-3 , * |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013154512A1 (en) * | 2012-04-13 | 2013-10-17 | Mahmut Bilgic | Pharmaceutical formulations comprising dexibuprofen |
| CN103417505A (en) * | 2012-05-24 | 2013-12-04 | 中国科学院上海药物研究所 | Huperzine A controlled release preparation having biphasic release behavior, and preparation method thereof |
| CN105579033A (en) * | 2013-09-27 | 2016-05-11 | 强生消费者公司 | Compression coated pulsatile release compositions |
| 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 |
| 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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| CN102160855B (en) | 2013-01-23 |
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