CN101978955A - Dextral ibuprofen amino acid salt tablets and preparation method thereof - Google Patents
Dextral ibuprofen amino acid salt tablets and preparation method thereof Download PDFInfo
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- CN101978955A CN101978955A CN2010105325124A CN201010532512A CN101978955A CN 101978955 A CN101978955 A CN 101978955A CN 2010105325124 A CN2010105325124 A CN 2010105325124A CN 201010532512 A CN201010532512 A CN 201010532512A CN 101978955 A CN101978955 A CN 101978955A
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Abstract
The invention discloses dextral ibuprofen amino acid salt tablets and a preparation method thereof. The tablets are prepared from the following raw materials in part by weight: 1 part of dextral ibuprofen amino acid salt, 0.2 to 20 parts of diluent (or filler), 0.01 to 1 part of adhesive, 0.01 to 1 part of disintegrating agent, 0.01 to 1 part of flavoring agent and 0.001 to 0.1 part of lubricating agent. Wet granulation, dry granulation and tabletting or direct powder tabletting and tablet coating are adopted in the preparation process of the tablets. Based on the dextral ibuprofen, the specification of the tablets can be 30 to 300 milligrams, preferably 37.5 milligrams or integral multiple of 37.5 milligrams. The dextral ibuprofen amino acid salt serving as an effective ingredient of the tablets has the advantages of quick response, accurate dose, low side effect and small individual difference. The tablets can be prepared into common tablets, chewable tablets, effervescent tablets, soluble tablets, oral fast dissolving tablets, sugar coated tablets, film coated tablets and the like.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, be specifically related to Dexibuprofen amino acid salt tablet and preparation method thereof.
Background technology
Ibuprofen (Ibuprofen), 2-(4-isobutylphenyl) propanoic acid has another name called ibuprofen, and molecular formula is C
13H
18O
2, molecular weight is 206.28.Ibuprofen antiinflammatory, analgesia, refrigeration function are strong, and GI irritation is little, and untoward reaction is few, and better tolerance is an antipyretic analgesic commonly used clinically at present.
Ibuprofen has optical activity, and the activity of (S)-ibuprofen is 160 times of its levo form, is 1.6 times of raceme, racemic modification commonly used clinically at present.Studies show that after racemic ibuprofen entered human body, the part levo form can be converted into d-isomer, conversion ratio is about 18%～32%.Consider from the clinical rational drug use angle,, and might reduce untoward reaction if all give (S)-ibuprofen then help improving curative effect or reduce dosage.And, owing to transforming in vivo, levo form may have interindividual variation, the interindividual variation when the (S)-ibuprofen preparation then helps reducing patient's medication, and it is accurate to help dosage.
But (S)-ibuprofen is the same almost insoluble in water with ibuprofen, and this has brought difficulty not only for the exploitation of solution type preparation, and the more important thing is to influence bioavailability of medicament.The ibuprofen salt for preparing with basic amino acid has good water-solubility, and can significantly improve the infiltration rate of medicine.For example, U.S. Pat 6,342530B1 has mentioned the prescription and the preparation method of Ibuproben-Lysiante parenteral, U.S. Pat 5,463,117 describe the salt for preparing ibuprofen with basic amino acid.
The invention provides a kind of (S)-ibuprofen arginine salt tablet and preparation method thereof, this tablet has the characteristics rapidly that absorb, and can be according to the conversion ratio of levo form in the racemic ibuprofen, appropriate design (S)-ibuprofen content in the tablet, a kind of safer, effective antipyretic-antalgic agent is provided.
Summary of the invention
The object of the present invention is to provide a kind of more safe and effective Dexibuprofen amino acid salt tablet and preparation method thereof.The present invention is that active component prepares tablet with the Dexibuprofen amino acid salt.
Another object of the present invention is to provides a kind of more safe and effective ntipyretic analgesic medicine for the quick antipyretic patient of needs.
Another purpose of the present invention also is to provide the agent of a kind of antipyretic-antalgic safely and effectively for take medicine poor compliance, the relatively poor crowd of swallow such as child, old people, the Dexibuprofen amino acid salt sheet can be prepared into chewable tablet, fuse, oral instant-dissolving tablet as required, etc.
Beneficial effect of the present invention is to use (S)-ibuprofen as active component, not only may improve curative effect, also may reduce patient's taking dose, reduces untoward reaction, improve drug compliance, thereby reach the purpose of rational use of drug.
Aminoacid in active constituents of medicine among the present invention or the raw material Dexibuprofen amino acid salt is basic amino acid, can be arginine, lysinate or histidine, amino acid whose configuration can be a D-aminoacid, also can be L-aminoacid, also can be DL-aminoacid.
The specification of tablet can be 37.5mg, 75mg, 150mg, 225mg, 300mg etc. in (S)-ibuprofen among the present invention.
Tablet among the present invention can be ordinary tablet, chewable tablet, effervescent tablet, fuse, oral instant-dissolving tablet, coated tablet, Film coated tablets etc.
Adjuvant among the present invention adopts tablet adjuvant commonly used, comprises diluent (filler), binding agent, disintegrating agent, wetting agent, lubricant etc.
Supplementary product consumption among the present invention adopts the usual amounts in the tablet manufacture.
The specific embodiment
Embodiment 1 (ordinary tablet adopts wet granulation process)
Prescription:
(S)-ibuprofen arginine salt 138.3g (counting 75g) with (S)-ibuprofen
Starch 80g
Dextrin 40g
Microcrystalline Cellulose 60g
10% starch slurry is an amount of
Magnesium stearate 1.5g (0.5%)
Make 1000 (every contains (S)-ibuprofen 75mg)
Preparation: the (S)-ibuprofen arginine salt is crossed 80 mesh sieves,, add starch slurry and make soft material with starch, dextrin, microcrystalline Cellulose mixing, after the granulation of 20 mesh sieves, wet granular is put 50 ℃ of dryings, and moisture Control is 2%～3%, 14 order granulate, tabletting behind the adding magnesium stearate mixing, promptly.
Embodiment 2 (chewable tablet, fuse, oral instant-dissolving tablet or oral cavity quick disintegrating slice)
Prescription:
(S)-ibuprofen lysinate 256.3g (counting 150g) with (S)-ibuprofen
Sucrose 40g
Mannitol 40g
Sorbitol 20g
5% hydroxypropyl emthylcellulose (HPMC) solution is an amount of
Magnesium stearate 1.9g (0.5%)
Make 1000 (every contains (S)-ibuprofen 150mg)
Preparation: the (S)-ibuprofen arginine salt is crossed 80 mesh sieves, and sucrose, mannitol are crossed 100 mesh sieves, with three's mixing, add 5%HPMC solution and make soft material, after the granulation of 20 mesh sieves, wet granular is put 50 ℃ of dryings, and moisture Control is 2%～3%, 14 order granulate, tabletting behind the adding magnesium stearate mixing, promptly.
Embodiment 3 (effervescent tablet)
Prescription:
(S)-ibuprofen arginine salt 553.3g (counting 300g) with (S)-ibuprofen
Lactose 120g
Citric acid 24g
Sodium bicarbonate 40g
Carboxymethyl starch sodium (CMS-Na) 20g
5% polyvidone (PVP) ethanol solution is an amount of
Magnesium stearate 3.7g (0.5%)
Make 1000 (every contains (S)-ibuprofen 300mg)
Preparation: supplementary material was mixed 100 mesh sieves, behind the mix homogeneously, add the 5%PVP ethanol solution and make soft material, after granulating with 20 mesh sieves, wet granular is put 50 ℃ of dryings, and moisture Control is 2%～3%, 14 order granulate, and tabletting behind the adding magnesium stearate mixing, promptly.
Embodiment 4 (ordinary tablet adopts dry granulation method or direct powder compression)
Prescription:
(S)-ibuprofen lysinate 128.2g (counting 75g) with (S)-ibuprofen
Pregelatinized Starch 80g
Microcrystalline Cellulose (MCC) 80g
Pulvis Talci 15g (5%)
Make 1000 (every contains (S)-ibuprofen 75mg)
Preparation: supplementary material is crossed 100 mesh sieves respectively, mixing, briquetting, pulverizing, 16 order granulate add the Pulvis Talci mixing, and the dry granulation tabletting perhaps adopts direct powder compression, promptly.
Embodiment 5 (Film coated tablets)
Prescription:
(S)-ibuprofen arginine salt 276.7g (counting 150g) with (S)-ibuprofen
Starch 40g
Sucrose 20g
Dextrin 40g
5% sodium carboxymethyl cellulose (CMC-Na) solution is an amount of
Magnesium stearate 1.9g (0.5%)
12%HPMC (coating solution) is an amount of
Make 1000 (every contains (S)-ibuprofen 150mg)
Preparation: the (S)-ibuprofen arginine salt is crossed 80 mesh sieves, with starch (20g), sucrose, dextrin mixing, add 5%CMC-Na solution and make soft material, after the granulation of 20 mesh sieves, wet granular is put 50 ℃ of dryings, and moisture Control is 2%～3%, 14 order granulate, tabletting behind adding magnesium stearate, remaining starch (20g) mixing gets plain sheet; With turnadle pan coating or fluidized coating method coating, promptly.
Claims (10)
1. Dexibuprofen amino acid salt tablet, its active component is a Dexibuprofen amino acid salt, is made by the raw material of following weight portion:
1 part of Dexibuprofen amino acid salt
0.2～20 part of diluent (or filler)
0.01～1 part of binding agent
0.01～1 part of disintegrating agent
0.01～1 part of correctives
0.001～0.1 part of lubricant
2. Dexibuprofen amino acid salt tablet as claimed in claim 1, wherein aminoacid is basic amino acid, can be arginine, lysinate or histidine.
3. Dexibuprofen amino acid salt tablet as claimed in claim 1, wherein amino acid whose configuration can be a D-aminoacid, can be L-aminoacid, also can be DL-aminoacid.
4. Dexibuprofen amino acid tablet as claimed in claim 1 can be ordinary tablet, chewable tablet, effervescent tablet, fuse, oral instant-dissolving tablet or oral cavity quick disintegrating slice etc., also can be made into coated tablet, Film coated tablets, enteric coatel tablets.
5. Dexibuprofen amino acid salt tablet as claimed in claim 1, wherein said filler (diluent) is selected any one or a few in starch, pregelatinized Starch, sucrose, dextrin, microcrystalline Cellulose, lactose, mannitol, sorbitol, glucose, the fructose for use; Wherein binding agent is selected any one or a few in 5%～20% starch slurry, polyvidone, sucrose, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, microcrystalline Cellulose, the Polyethylene Glycol for use; Wherein disintegrating agent is selected any one or a few in dried starch, microcrystalline Cellulose, effervescent Acid-Base system, polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose, the carboxymethyl starch sodium for use; Wherein correctives is selected any one or a few in sucrose, mannitol, sorbitol, aspartame, steviosin, the edible or medicinal essence for use; Wherein lubricant is selected any one or a few of magnesium stearate, Pulvis Talci, micropowder silica gel, Polyethylene Glycol for use; Can add that food coloring carmine, lemon yellow, amaranth, Fructus Litchi are red, Rhizoma Dioscoreae any one or a few in purple.
6. the preparation method of Dexibuprofen amino acid salt tablet may further comprise the steps:
With Dexibuprofen amino acid salt, filler (diluent), disintegrating agent mixing, can adopt equivalent incremental method (facing-up method) with the pressed powder mix homogeneously, with binding agent system soft material, after granulating 60 ℃ of dryings, granulate adds lubricant, disintegrating agent, food coloring or essence, mixing, tabletting promptly gets the Dexibuprofen amino acid salt sheet.
7. method as claimed in claim 6, wherein baking temperature is 40 ℃～90 ℃, preferred 60 ℃～80 ℃; Be 1～3 hour drying time.
8. method as claimed in claim 6 adopts wet granulation in the preparation process, dry granulation, tabletting, perhaps direct powder compression.
9. method as claimed in claim 6 can be given tablet sugar coating, film-coat or enteric coating in preparation process, method is a method commonly used in the pharmaceutical field.
10. tablet as claimed in claim 1 wherein comprises the (S)-ibuprofen that is equivalent to 30mg～300mg, preferably comprises the (S)-ibuprofen that is equivalent to 37.5mg or 37.5mg integral multiple.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2010105325124A CN101978955A (en) | 2010-11-05 | 2010-11-05 | Dextral ibuprofen amino acid salt tablets and preparation method thereof |
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| CN2010105325124A CN101978955A (en) | 2010-11-05 | 2010-11-05 | Dextral ibuprofen amino acid salt tablets and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013004123A1 (en) * | 2011-07-01 | 2013-01-10 | Sino-American Tianjin Smithkline And French Lab., Ltd | Ibuprofen chewable tablet |
| CN107550895A (en) * | 2016-06-30 | 2018-01-09 | 康普药业股份有限公司 | A kind of R-gene preparation |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0346006A1 (en) * | 1988-06-09 | 1989-12-13 | Reckitt And Colman Products Limited | Pharmaceutical compositions containing ibuprofen-cyclodextrin complexes |
| EP0424028A2 (en) * | 1989-10-17 | 1991-04-24 | Merck & Co. Inc. | S(+)-ibuprofen-L-amino acid and S(+)-ibuprofen-D-amino acid as onset hastened enhanced analgesics |
| US5510385A (en) * | 1993-06-21 | 1996-04-23 | Zambon Group S.P.A. | Pharmaceutical compositions containing the salts of S(+)-2-(4-isobutylphenyl)propionic acid with basic aminoacids |
| CN101265178A (en) * | 2008-04-25 | 2008-09-17 | 北京阜康仁生物制药科技有限公司 | Amino acid salt of (S)-ibuprofen and medicinal composition thereof |
| CN101390844A (en) * | 2007-09-23 | 2009-03-25 | 天津医科大学 | Arginine ibuprofen tablet and preparation method thereof |
-
2010
- 2010-11-05 CN CN2010105325124A patent/CN101978955A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0346006A1 (en) * | 1988-06-09 | 1989-12-13 | Reckitt And Colman Products Limited | Pharmaceutical compositions containing ibuprofen-cyclodextrin complexes |
| EP0424028A2 (en) * | 1989-10-17 | 1991-04-24 | Merck & Co. Inc. | S(+)-ibuprofen-L-amino acid and S(+)-ibuprofen-D-amino acid as onset hastened enhanced analgesics |
| US5510385A (en) * | 1993-06-21 | 1996-04-23 | Zambon Group S.P.A. | Pharmaceutical compositions containing the salts of S(+)-2-(4-isobutylphenyl)propionic acid with basic aminoacids |
| CN101390844A (en) * | 2007-09-23 | 2009-03-25 | 天津医科大学 | Arginine ibuprofen tablet and preparation method thereof |
| CN101265178A (en) * | 2008-04-25 | 2008-09-17 | 北京阜康仁生物制药科技有限公司 | Amino acid salt of (S)-ibuprofen and medicinal composition thereof |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013004123A1 (en) * | 2011-07-01 | 2013-01-10 | Sino-American Tianjin Smithkline And French Lab., Ltd | Ibuprofen chewable tablet |
| AP3309A (en) * | 2011-07-01 | 2015-06-30 | Sino American Tianjin Smithkline And French Lab Ltd | Ibuprofen chewable tablet |
| RU2567050C2 (en) * | 2011-07-01 | 2015-10-27 | Сино-Американ Тяньцзинь Смитклайн Энд Френч Лаб., Лтд | Ibuprofene chewing tablet |
| CN107550895A (en) * | 2016-06-30 | 2018-01-09 | 康普药业股份有限公司 | A kind of R-gene preparation |
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Application publication date: 20110223 |