CN101978955A - Dexibuprofen amino acid salt tablet and preparation method thereof - Google Patents
Dexibuprofen amino acid salt tablet 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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- amino acid
- tablet
- tablets
- acid salt
- dexibuprofen
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- -1 Dexibuprofen amino acid salt Chemical class 0.000 title claims abstract description 22
- 238000002360 preparation method Methods 0.000 title claims abstract description 18
- 229960003428 dexibuprofen Drugs 0.000 title claims description 18
- 239000003826 tablet Substances 0.000 claims abstract description 40
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 6
- 239000007910 chewable tablet Substances 0.000 claims abstract description 5
- 239000000945 filler Substances 0.000 claims abstract description 5
- 239000000314 lubricant Substances 0.000 claims abstract description 5
- 239000003085 diluting agent Substances 0.000 claims abstract description 4
- 238000007908 dry granulation Methods 0.000 claims abstract description 4
- 239000007938 effervescent tablet Substances 0.000 claims abstract description 4
- 239000007941 film coated tablet Substances 0.000 claims abstract description 4
- 239000002994 raw material Substances 0.000 claims abstract description 3
- 238000005550 wet granulation Methods 0.000 claims abstract description 3
- 239000000796 flavoring agent Substances 0.000 claims abstract 3
- 239000000843 powder Substances 0.000 claims abstract 3
- 239000000853 adhesive Substances 0.000 claims abstract 2
- 230000001070 adhesive effect Effects 0.000 claims abstract 2
- 239000008298 dragée Substances 0.000 claims abstract 2
- 235000013355 food flavoring agent Nutrition 0.000 claims abstract 2
- 239000007940 sugar coated tablet Substances 0.000 claims abstract 2
- HEFNNWSXXWATRW-JTQLQIEISA-N dexibuprofen Chemical compound CC(C)CC1=CC=C([C@H](C)C(O)=O)C=C1 HEFNNWSXXWATRW-JTQLQIEISA-N 0.000 claims description 26
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 18
- 229920002472 Starch Polymers 0.000 claims description 12
- 239000008107 starch Substances 0.000 claims description 12
- 235000019698 starch Nutrition 0.000 claims description 12
- 239000004475 Arginine Substances 0.000 claims description 9
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 9
- 235000019359 magnesium stearate Nutrition 0.000 claims description 9
- 150000001413 amino acids Chemical class 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 7
- 229930006000 Sucrose Natural products 0.000 claims description 7
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 7
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 7
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 7
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 7
- 239000005720 sucrose Substances 0.000 claims description 7
- 238000001035 drying Methods 0.000 claims description 6
- 239000008187 granular material Substances 0.000 claims description 6
- 229920001353 Dextrin Polymers 0.000 claims description 5
- 239000004375 Dextrin Substances 0.000 claims description 5
- 235000019425 dextrin Nutrition 0.000 claims description 5
- 239000011734 sodium Substances 0.000 claims description 5
- 239000007779 soft material Substances 0.000 claims description 5
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- 229940068682 chewable tablet Drugs 0.000 claims description 4
- 239000000594 mannitol Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 4
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 3
- 239000011230 binding agent Substances 0.000 claims description 3
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims description 3
- 239000000203 mixture Substances 0.000 claims description 3
- 210000000214 mouth Anatomy 0.000 claims description 3
- 239000002002 slurry Substances 0.000 claims description 3
- 239000000600 sorbitol Substances 0.000 claims description 3
- 235000010356 sorbitol Nutrition 0.000 claims description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims description 2
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 2
- 229920000881 Modified starch Polymers 0.000 claims description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 2
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims description 2
- 239000008101 lactose Substances 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 239000007884 disintegrant Substances 0.000 claims 2
- 239000000576 food coloring agent Substances 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 240000001592 Amaranthus caudatus Species 0.000 claims 1
- 235000009328 Amaranthus caudatus Nutrition 0.000 claims 1
- 108010011485 Aspartame Proteins 0.000 claims 1
- 235000005979 Citrus limon Nutrition 0.000 claims 1
- 244000131522 Citrus pyriformis Species 0.000 claims 1
- 150000008574 D-amino acids Chemical class 0.000 claims 1
- 239000005715 Fructose Substances 0.000 claims 1
- 229930091371 Fructose Natural products 0.000 claims 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 150000008575 L-amino acids Chemical class 0.000 claims 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical class NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- 244000183278 Nephelium litchi Species 0.000 claims 1
- 235000015742 Nephelium litchi Nutrition 0.000 claims 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 1
- 244000061456 Solanum tuberosum Species 0.000 claims 1
- 235000002595 Solanum tuberosum Nutrition 0.000 claims 1
- 244000228451 Stevia rebaudiana Species 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000003513 alkali Substances 0.000 claims 1
- 235000012735 amaranth Nutrition 0.000 claims 1
- 239000004178 amaranth Substances 0.000 claims 1
- 239000000605 aspartame Substances 0.000 claims 1
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims 1
- 235000010357 aspartame Nutrition 0.000 claims 1
- 229960003438 aspartame Drugs 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 235000012730 carminic acid Nutrition 0.000 claims 1
- 238000013329 compounding Methods 0.000 claims 1
- 229960000913 crospovidone Drugs 0.000 claims 1
- 239000002662 enteric coated tablet Substances 0.000 claims 1
- 239000002702 enteric coating Substances 0.000 claims 1
- 238000009505 enteric coating Methods 0.000 claims 1
- 239000000686 essence Substances 0.000 claims 1
- 239000000835 fiber Substances 0.000 claims 1
- 238000009501 film coating Methods 0.000 claims 1
- 239000007888 film coating Substances 0.000 claims 1
- 235000019634 flavors Nutrition 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 1
- 229940069328 povidone Drugs 0.000 claims 1
- HELXLJCILKEWJH-NCGAPWICSA-N rebaudioside A Chemical compound O([C@H]1[C@H](O)[C@@H](CO)O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O HELXLJCILKEWJH-NCGAPWICSA-N 0.000 claims 1
- 239000000741 silica gel Substances 0.000 claims 1
- 229910002027 silica gel Inorganic materials 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 241000894007 species Species 0.000 claims 1
- 238000009495 sugar coating Methods 0.000 claims 1
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 abstract description 12
- 229960001680 ibuprofen Drugs 0.000 abstract description 11
- 230000000694 effects Effects 0.000 abstract description 4
- 239000004615 ingredient Substances 0.000 abstract 1
- 239000007944 soluble tablet Substances 0.000 abstract 1
- 238000009492 tablet coating Methods 0.000 abstract 1
- 239000002700 tablet coating Substances 0.000 abstract 1
- 235000001014 amino acid Nutrition 0.000 description 11
- 239000003814 drug Substances 0.000 description 9
- 238000002156 mixing Methods 0.000 description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- 238000006243 chemical reaction Methods 0.000 description 5
- 206010013786 Dry skin Diseases 0.000 description 4
- 238000000576 coating method Methods 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 239000011248 coating agent Substances 0.000 description 3
- 238000005469 granulation Methods 0.000 description 3
- 230000003179 granulation Effects 0.000 description 3
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
- IHHXIUAEPKVVII-PTKYJSHISA-N [(5s)-5-amino-5-carboxypentyl]azanium;(2s)-2-[4-(2-methylpropyl)phenyl]propanoate Chemical compound NCCCC[C@H](N)C(O)=O.CC(C)CC1=CC=C([C@H](C)C(O)=O)C=C1 IHHXIUAEPKVVII-PTKYJSHISA-N 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 238000009702 powder compression Methods 0.000 description 2
- 206010070840 Gastrointestinal tract irritation Diseases 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000001754 anti-pyretic effect Effects 0.000 description 1
- 239000002221 antipyretic Substances 0.000 description 1
- 239000003907 antipyretic analgesic agent Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 229940082159 ibuprofen 300 mg Drugs 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000008595 infiltration Effects 0.000 description 1
- 238000001764 infiltration Methods 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-M lysinate Chemical compound NCCCCC(N)C([O-])=O KDXKERNSBIXSRK-UHFFFAOYSA-M 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
- 238000005057 refrigeration Methods 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 230000001131 transforming effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
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)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010105325124A CN101978955A (en) | 2010-11-05 | 2010-11-05 | Dexibuprofen amino acid salt tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010105325124A CN101978955A (en) | 2010-11-05 | 2010-11-05 | Dexibuprofen amino acid salt tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101978955A true CN101978955A (en) | 2011-02-23 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010105325124A Pending CN101978955A (en) | 2010-11-05 | 2010-11-05 | Dexibuprofen amino acid salt tablet and preparation method thereof |
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| Country | Link |
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| CN (1) | CN101978955A (en) |
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 |