CN101077343B - Dexibuprofen granule and preparation method thereof - Google Patents
Dexibuprofen granule and preparation method thereof Download PDFInfo
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- CN101077343B CN101077343B CN2006100707836A CN200610070783A CN101077343B CN 101077343 B CN101077343 B CN 101077343B CN 2006100707836 A CN2006100707836 A CN 2006100707836A CN 200610070783 A CN200610070783 A CN 200610070783A CN 101077343 B CN101077343 B CN 101077343B
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Abstract
The present invention discloses one kind of dextro brufen granule and its preparation process, and features that the dextro brufen granule contains dextro brufen 1 weight portions, alkaline cosolvent 0-100 weight portions, stuffing 0.1-100 weight portions, adhesive 0.1-12 weight portions, corrective 0.01-0.5 weight portion, and lubricant 0.1-2 weight portions. Its preparation process includes the steps of mixing, pelletizing and packing. The effervescent dextro brufen tablet is superior to traditional orally taken dextro brufen preparation, can dissolve in water to form tasty solution, and has easy taking, high bioavailability, fast acting and other advantages.
Description
Technical field:
The invention belongs to medical technical field, be specifically related to a kind of (s)-ibuprofen granules and preparation method that is used for the treatment of diseases such as pain that a variety of causes causes, heating.
Background technology
Ibuprofen, promptly 2-(4-isobutyl phenenyl) propanoic acid are NSAID (non-steroidal anti-inflammatory drug) (NSAIDs), are that first is used for the fragrant class medicine in clinical and still widely used so far Lip river in the world, are acknowledged as one of safest medicine among the NSAIDs.Pharmacological action shows its antiinflammatory, analgesia, refrigeration function.Clinical various acute, chronic arthritiss, soft tissue rheumatism disease, tenosynovitis, motional injury and headache, myalgia, dysmenorrhea, pain and the cancerous pain etc. after getting a tooth pulled out of being used for.This medicine is recommended as the first ladder medicine [2] in the medication of analgesia ladder, at home and abroad all records in the pharmacopeia, and be one of essential drugs of China
The stereo selectivity of ibuprofen because racemic modification is lived, its mark sheet is present: left-handed ibuprofen enantiomer must unidirectionally change into its effect of (S)-ibuprofen enantiomer competence exertion in vivo.Experiment showed, that the (S)-ibuprofen enantiomer is the active ingredient in the raceme ibuprofen, the tool pharmacologically active shows upward effect of treatment; And left-handed ibuprofen enantiomer is nonactive composition, and relates to potential toxic action.Owing to use (S)-ibuprofen to overcome ibuprofen some shortcomings aspect use pharmacodynamics and pharmacokinetics, the external existing trend that substitutes the raceme ibuprofen with (S)-ibuprofen.Its clinical meaning is as follows:
1. (S)-ibuprofen is an active single enantiomer of tool medicine generation, so use the (S)-ibuprofen that is lower than raceme ibuprofen dosage can produce pharmacological action equal even strong degree, also produces to a certain degree pharmacological action even be less than 1/2 dosage.
2. (S)-ibuprofen does not need conversion process, and the back obtains sufficiently high blood drug level easily rapidly in the body so enter, and shows rapid-actionly, acts on strong characteristics.
3. (S)-ibuprofen does not disturb body fat tissue biological synthetic, has got rid of the possibility of bringing out the hyperreaction reaction.
4. (S)-ibuprofen has reduced dosage, and not only reduction is brought out the probability of genotoxic potential but also is that the heavy dose of preparation of preparation (as slow releasing agent, controlled release agent etc.) is more favourable.
5. (S)-ibuprofen shows better simply pharmacodynamics and pharmacokinetics characteristics, thereby helps optimization of dosage etc.
(S)-ibuprofen (S)--2-(4-isobutyl phenenyl) propanoic acid are at first developed successfully by Austrian Gebro-Broscheh GmbH company, and commodity were called Seractil through the approval listing in 1994.In June, 1997, the Pelletech company of microsphere technical point company of Switzerland Spirig also succeeded in developing, commodity Soptifen by name and Ultraprofen.The said firm registers its product in the world by its affiliate.Just seeking at present to enter other country, comprising Spain, Hungary etc.In addition, also there is this medicine listing in Denmark Nycomed company, and commodity are called Nyfen.All there are this medicine listing in U.S. Alemarle Corp, France etc., and this medicine crude drug was exclusively succeeded in developing by Hubei Baike Medicine Industrial Co., Ltd. in China and put on market calendar year 2001, and preparation is also listing just successively at home.
Though (S)-ibuprofen has overcome shortcomings such as the side effect of ibuprofen aspect use pharmacodynamics and pharmacokinetics is big, dosage is big, but its dissolubility in water is constant substantially, be difficult for making the dissolved liquid dosage form of energy, existing dosage form still is ordinary preparations such as tablet, capsule, dispersible tablet, oral administration mixed suspension, (NSAIDs) is the same with other NSAID (non-steroidal anti-inflammatory drug), absorption difference, bioavailability is low, onset is relatively slow, and the patient of child, old people and the solid preparation of can not swallowing is made troubles.
Summary of the invention
Purpose of the present invention exists for solving (S)-ibuprofen oral formulations of the prior art: in water, is difficult for making dissolved liquid dosage form of energy and insoluble drug and is difficult for the particulate shortcoming of preparation, and a kind of (s)-ibuprofen granules and the preparation method that propose.
The present invention solves the technical scheme that the prior art problem adopted:
A kind of (s)-ibuprofen granules and preparation method, described granule contains principal agent (S)-ibuprofen, filler, correctives, binding agent, and described (s)-ibuprofen granules is characterized in that wherein the weight proportion of each component is:
(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.
Described (s)-ibuprofen granules, wherein the alkaline auxiliary solvent can adopt: any in arginine, D-arginine, DL-arginine and salt or lysine, D-lysine, DL-lysine and the salt thereof, and described filler can adopt: any of lactose, glucose, sucrose, mannitol, fructose, dextrin; Described correctives can adopt: any of stevioside and spice.
Can also add an amount of polyvinylpyrrolidone PVP or Polyethylene Glycol among the present invention and disperse enclose to prolong the holding time of product to stop the medicine moisture absorption, also can adopt the starch slurry of suitable concentration, other suitable binding agents such as ethanol water that hydroxypropyl methyl fiber is given birth to plain ethanol water, Polyethylene Glycol PEG ethanol water, suitable concentration.
(s)-ibuprofen granules of the present invention adopts following prepared:
With the (S)-ibuprofen of recipe quantity, arginine (or lysine, DL-lysine, D-lysine, L-lysine) or its salt, lactose or (glucose, sucrose, mannitol, fructose, dextrin) and an amount of correctives stevioside and spice are pulverized mutual mixing; With the polyvinylpyrrolidone PVP of suitable concentration (or other suitable binding agents such as ethanol water of the ethanol water of starch slurry, the fine vitamin of methyl, Polyethylene Glycol PEG ethanol water, suitable concentration) is that binding agent is made soft material, granulation, drying, granulate, packing.
The preparation method of described (s)-ibuprofen granules, a. crosses 40-80 mesh sieves respectively with principal agent (S)-ibuprofen, alkaline auxiliary solvent, filler component; B. after percentage by weight is weighed respectively with said components, mix homogeneously; C. adopt system soft materials such as 30%-99% ethanol water; D. adopting 18 order nylon screens granulation back again is to carry out dried below 35-40 ℃ in temperature; E. adopt 16 order galvanized iron screen cloth granulate, re-use 50 order nylon screens and remove fine powder; F. qualified through chemically examining, be packaged into bag.
The invention has the advantages that: the (s)-ibuprofen granules employing can increase the deliquescent arginine of (S)-ibuprofen, D-arginine, DL-arginine and salt or lysine, D-lysine, DL-lysine and salt thereof are cosolvent, it can make principal agent be dissolved in the solution rapidly, compare with plain particles agent, tablet, dispersible tablet, capsule, the oral administration mixed suspension of same dosage, (s)-ibuprofen granules has taking convenience, absorption is fast, bioavailability is high, onset is rapid, good effect; Can make contain (S)-ibuprofen granule rapidly with the transparent and delicious solution of water reaction formation, carry advantage more easily and compare also to have with the common liq preparation.The invention provides a kind of preparation method that contains (S)-ibuprofen, preparation method is simple and reliable, and cost is low.
The specific embodiment
Embodiment 1:
Prescription: (S)-ibuprofen 200
Arginine 385
Lactose 785
Polyethylene Glycol PEG 100
Lubricant is an amount of
Stevioside and spice are an amount of
Ethanol or water are an amount of
Technology: with above-mentioned supplementary material pulverizing, mixing, granulation, packing.
Embodiment 2:
Prescription: (S)-ibuprofen 200
Arginine monohydrochloride 385
Sucrose 785
Polyvinylpyrrolidone PVP 100
Lubricant is an amount of
Stevioside and spice are an amount of
Ethanol or water are an amount of
Technology: with above-mentioned supplementary material pulverizing, mixing, granulation, packing.
Embodiment 3:
Prescription: (S)-ibuprofen 200
Lysine 385
Lactose and sucrose mixture 675
Polyvinylpyrrolidone PVP 80
Lubricant is an amount of
Stevioside and spice are an amount of
Ethanol or water are an amount of
Technology: with above-mentioned supplementary material pulverizing, mixing, granulation, packing.
Embodiment 4:
Prescription: (S)-ibuprofen 200
Lysine 385
Lactose 785
Polyvinylpyrrolidone PVP 200
Lubricant is an amount of
Stevioside and spice are an amount of
Ethanol or water are an amount of
Technology: with above-mentioned supplementary material pulverizing, mixing, granulation, packing.
Claims (4)
1. (s)-ibuprofen granules, it is made by following materials of weight proportions:
(S)-ibuprofen 200
Arginine 385
Lactose 785
Polyethylene Glycol PEG 100
Lubricant is an amount of
Stevioside and spice are an amount of
Ethanol or water are an amount of
Its preparation method is as follows:
(1) principal agent (S)-ibuprofen, alkaline auxiliary solvent arginine, lactose are crossed the 40-80 mesh sieve respectively;
(2) said components is weighed according to percentage by weight respectively after, mix homogeneously;
(3) the ethanol water system soft material of employing 30%-99%;
(4) adopting 18 order nylon screens granulation back again is to carry out dried below 35-40 ℃ in temperature;
(5) adopt 16 order galvanized iron screen cloth granulate, re-use 50 order nylon screens and remove fine powder;
(6) qualified through chemically examining, be packaged into bag.
2. (s)-ibuprofen granules, it is made by following materials of weight proportions:
(S)-ibuprofen 200
Arginine monohydrochloride 385
Sucrose 785
Polyvinylpyrrolidone PVP 100
Lubricant is an amount of
Stevioside and spice are an amount of
Ethanol or water are an amount of
Its preparation method is as follows:
(1) principal agent (S)-ibuprofen, alkaline auxiliary solvent arginine monohydrochloride, sucrose are crossed the 40-80 mesh sieve respectively;
(2) said components is weighed according to percentage by weight respectively after, mix homogeneously;
(3) the ethanol water system soft material of employing 30%-99%;
(4) adopting 18 order nylon screens granulation back again is to carry out dried below 35-40 ℃ in temperature;
(5) adopt 16 order galvanized iron screen cloth granulate, re-use 50 order nylon screens and remove fine powder;
(6) qualified through chemically examining, be packaged into bag.
3. (s)-ibuprofen granules, it is made by following materials of weight proportions:
(S)-ibuprofen 200
Lysine 385
Lactose and sucrose mixture 675
Polyvinylpyrrolidone PVP 80
Lubricant is an amount of
Stevioside and spice are an amount of
Ethanol or water are an amount of
Its preparation method is as follows:
(1) principal agent (S)-ibuprofen, alkaline auxiliary solvent lysine, sucrose and milk-sugar mixture are crossed the 40-80 mesh sieve respectively;
(2) said components is weighed according to percentage by weight respectively after, mix homogeneously;
(3) the ethanol water system soft material of employing 30%-99%;
(4) adopting 18 order nylon screens granulation back again is to carry out dried below 35-40 ℃ in temperature;
(5) adopt 16 order galvanized iron screen cloth granulate, re-use 50 order nylon screens and remove fine powder;
(6) qualified through chemically examining, be packaged into bag.
4. (s)-ibuprofen granules, it is made by following materials of weight proportions:
(S)-ibuprofen 200
Lysine 385
Lactose 785
Polyvinylpyrrolidone PVP 200
Lubricant is an amount of
Stevioside and spice are an amount of
Ethanol or water are an amount of
Its preparation method is as follows:
(1) principal agent (S)-ibuprofen, alkaline auxiliary solvent lysine, lactose are crossed the 40-80 mesh sieve respectively;
(2) said components is weighed according to percentage by weight respectively after, mix homogeneously;
(3) the ethanol water system soft material of employing 30%-99%;
(4) adopting 18 order nylon screens granulation back again is to carry out dried below 35-40 ℃ in temperature;
(5) adopt 16 order galvanized iron screen cloth granulate, re-use 50 order nylon screens and remove fine powder;
(6) qualified through chemically examining, be packaged into bag.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN2006100707836A CN101077343B (en) | 2006-12-12 | 2006-12-12 | Dexibuprofen granule and preparation method thereof |
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| CN2006100707836A CN101077343B (en) | 2006-12-12 | 2006-12-12 | Dexibuprofen granule and preparation method thereof |
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| CN101077343A CN101077343A (en) | 2007-11-28 |
| CN101077343B true CN101077343B (en) | 2010-06-30 |
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| CN2006100707836A Expired - Fee Related CN101077343B (en) | 2006-12-12 | 2006-12-12 | Dexibuprofen granule and preparation method thereof |
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Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101829064B (en) * | 2010-04-27 | 2012-04-25 | 海南新中正制药有限公司 | Dexibuprofen granule and preparation method thereof |
| CN101856331B (en) * | 2010-05-20 | 2012-07-04 | 海南新中正制药有限公司 | Arginine (s)-ibuprofen granules and preparation method thereof |
| CN102389401B (en) * | 2011-11-22 | 2013-05-22 | 陆荣政 | Dexibuprofen particles and preparation method thereof |
| CN103156812A (en) * | 2011-12-08 | 2013-06-19 | 杭州赛利药物研究所有限公司 | Dextrorotation ibuprofen dried suspension and preparation method thereof |
| CN104771365A (en) * | 2015-04-20 | 2015-07-15 | 程伟智 | Dexibuprofen dry suspension agent and preparation method thereof |
| CN110123769B (en) * | 2019-05-24 | 2021-02-19 | 北京悦康科创医药科技股份有限公司 | Ibuprofen sustained-release pellet and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1155417A (en) * | 1995-06-13 | 1997-07-30 | 美国家用产品公司 | Oral formulations of S(+)-ibuprofen |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1155417A (en) * | 1995-06-13 | 1997-07-30 | 美国家用产品公司 | Oral formulations of S(+)-ibuprofen |
Non-Patent Citations (6)
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| 张其楷.可溶性布洛芬新口服剂型的活性和药动学.国外医学.药学分册19 5.1992,19(5),316-317. |
| 张其楷.可溶性布洛芬新口服剂型的活性和药动学.国外医学.药学分册19 5.1992,19(5),316-317. * |
| 徐东.布洛芬新型口服制剂.国外医药－合成药、生化药、制剂分册15 3.1994,15(3),167-168. |
| 徐东.布洛芬新型口服制剂.国外医药-合成药、生化药、制剂分册15 3.1994,15(3),167-168. * |
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Effective date of registration: 20071109 Address after: 233000 Anhui city of Bengbu Province Institute of Road No. 6 Building 1 unit Arcadia No. 10 Applicant after: Wang Yang Address before: No. 1, building 505, Xiyuan District, Hongqi Road two, Anhui, Bengbu Applicant before: Wang Honghu |
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Effective date of registration: 20090116 Address after: Postcode 2001, Tu Shan Road, Bengbu, Anhui: 233000 Applicant after: Anhui BBCA Pharmaceutical Co., Ltd. Address before: Anhui city of Bengbu Province Institute of Road No. 6 Arcadia Building 1 Unit No. 10 post encoding: 233000 Applicant before: Wang Yang |
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Owner name: BENGBU FENGYUAN TUSHAN PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: WANG YANG Effective date: 20090116 |
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