CN101912360A - Ibuprofen suspension and preparation method thereof - Google Patents
Ibuprofen suspension and preparation method thereof Download PDFInfo
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- CN101912360A CN101912360A CN 201010229657 CN201010229657A CN101912360A CN 101912360 A CN101912360 A CN 101912360A CN 201010229657 CN201010229657 CN 201010229657 CN 201010229657 A CN201010229657 A CN 201010229657A CN 101912360 A CN101912360 A CN 101912360A
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Abstract
The invention relates to an ibuprofen suspension and a preparation method thereof. In the ibuprofen suspension, the grain size of ibuprofen is 12-28 mums, the viscosity is not less than (75*0.4) mpas, the amount of a surfactant is 0.05-1%, and the amount of a pH regulator leads that the pH value of the suspension is 3-6. The ibuprofen suspension is prepared by adopting the preparation method comprising the following steps of: firstly fully homogenizing ibuprofen with a wetting agent and the surfactant by a homogenizer, and then fully and uniformly mixing the ibuprofen with a solution containing other components. The ibuprofen suspension solves the technical problems that the traditional ibuprofen suspension has the common disadvantages of poor stability and uniformity, easy generation of aggregated floating substances, and the like after being placed for a long time.
Description
Technical field
The present invention relates to technical field of medicine, in particular to the preparation method and the application of a kind of novel ibuprofen suspension and this novel ibuprofen suspension.
Background technology
Ibuprofen (Ibuprofen) has another name called the isobutylbenzene propanol, is the nonsteroidal antiinflammatory and analgesic medicine.Its antiinflammatory, analgesia, refrigeration function are respond well, and untoward reaction is less.Extensive use in the world at present becomes one of global best-selling over-the-counter drug and aspirin, acetaminophen and is listed as antipyretic analgesic three big pillar products together.
Ibuprofen goes on the market in Britain early than nineteen sixty-eight, and the manufacturer is a Britain The Boots Co. PLC, and commodity are called Brufen.Go on the market in states such as Germany, France, Italy, Japan, the U.S. again then very soon.Because it has rheumatism and analgesic analgesic curative effect concurrently, and toxicity is low, all is better than aspirin and acetaminophen at aspects such as curative effect and side effect, thereby market enlarges rapidly.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.
The ibuprofen dosage form of China's listing has conventional tablet, capsule, effervescent tablet, oral cavity disintegration tablet, granule, suppository, slow releasing tablet (capsule), chewable tablet, gel, suspension etc.Suspension is compared other dosage forms, has easily characteristics such as swallow, easily divided dose, mouthfeel be better.Because child and infant swallow are poor, body weight difference is big, the medication in children amount difference of all ages and classes section, thereby the medication crowd of this dosage form is primarily aimed in child and infant patient.
Then, there is a problem usually in the suspension dosage form, and promptly after placing after a while, its drug particle is easily assembled, and assembles sedimentation or buoyant phenomenon thereby medicine more or less occurs.This phenomenon occurs in certain, shake up or fully do not shake up, can cause actual dosage more excessive or not enough, thereby drug intoxication or invalid situation occur than expection such as forgetting before taking.For infant, because more responsive to the variation of medication amount, such situation occurs bringing the worse consequence.
Ibuprofen is that a kind of fusing point is low, the medicine of light weight, with other suspension after long-term the placement, what the easy aggregate and precipitate of drug particle was different is, it shows easy floating state in water, so the ibuprofen suspension long-time placement of process usually, and medicine can accumulate in the upper surface of suspension.Though, be uniformly dispersed once more by jolting meeting drug particle.But before the father and mother that may run into carelessness unavoidably take medicine to child, forget to shake up or do not shake up fully.
Ibuprofen suspension is in the existing time in 10 years nearly of China's listing, and ibuprofen suspension is through particle accumulation hydro-planing in various degree occurring after placing for a long time, and it is well stable still to be hard to keep, and this problem is not solved at present yet well.And, do not put down in writing the technology that solves the ibuprofen suspension hydro-planing at present in the prior art.
Therefore, still there is intensive demand in ibuprofen suspension stable, that be not prone to hydro-planing and its production and application.
Summary of the invention
An object of the present invention is to provide a kind of ibuprofen suspension stable, that be not prone to hydro-planing, wherein, the particle diameter of described ibuprofen is between 12～28 μ m; Viscosity is not less than (75 * 0.4) mpas; Dosage of surfactant is 0.05～1%; PH value regulator consumption is to make that the pH value of suspension is between the 3-6.
In embodiment, the particle diameter of described ibuprofen is between 15～25 μ m therein.
In embodiment, the particle diameter of described ibuprofen is between 18～20 μ m therein.
In embodiment, described viscosity is not less than (80 * 0.4) mpas therein.
In embodiment, described surfactant is a Tween 80 therein.
In embodiment, the consumption of described Tween 80 is 0.2% therein.
In embodiment, described pH value regulator is a citric acid therein.
In embodiment, described citric acid consumption is to make that the pH value of described suspension is between the 4-5 therein.
In embodiment, above-mentioned ibuprofen suspension is prepared as follows therein: at first with ibuprofen and wetting agent, surfactant by the abundant homogenize of homogenizer, afterwards again with the abundant mix homogeneously of the solution that contains other composition.
Another purpose of the present invention provides the method for the above-mentioned ibuprofen suspension of preparation, and this method comprises at first passes through the abundant homogenize of homogenizer with ibuprofen and wetting agent, surfactant, afterwards again with the abundant mix homogeneously of the solution that contains other composition.
Another purpose of the present invention provides the method that reduces the ibuprofen suspension hydro-planing, and comprise making suspension have following feature: the particle diameter of ibuprofen is at 12-28 μ m; Viscosity is not less than (75 * 0.4) mpas; Surfactant is a Tween 80, and consumption is 0.05-1%; The pH value regulator is a citric acid, and its consumption is to make that the pH value of suspension is between the 3-6, and by at first ibuprofen and wetting agent, surfactant being passed through the abundant homogenize of homogenizer, prepares with the abundant mix homogeneously of the solution that contains other composition more afterwards.
The particle diameter of ibuprofen of the present invention, 12～28 μ m for example, the particle size distribution range that is meant ibuprofen is between 12～28 μ m.
Described wetting agent can be any suitable wetting agent, for example is selected from glycerol, propylene glycol, Polyethylene Glycol, preferably glycerine, and those of ordinary skills can easily select according to the knowledge of grasping.
The solution of described other compositions also is that those of ordinary skills know, and other compositions comprise for example xanthan gum, sorbitol, sucrose, sodium benzoate, citric acid.
The specific embodiment
Unless definition in addition herein, employed all technology of this paper and scientific terminology have the common implication of understanding of those of ordinary skills.Although those methods and the material similar or of equal value with material to method described herein also can be used in the practice of the present invention, preferable methods and material are still described in this article.In addition, as used herein, term " ", " one " or " a kind of " comprise a plurality of or multiple, point out in addition unless context is clear and definite.Numerical range comprises the numeral that defines this scope.Subhead of the present invention is just to the purpose of setting forth, and is not intended to limit the scope of the invention.
Ibuprofen suspension is placed through long-time usually, and medicine can accumulate in the upper surface of suspension.Though, be uniformly dispersed once more by jolting meeting drug particle.But sometimes run into careless father and mother, can forget before taking medicine to child to shake up, thus cause dosage too actual needs dosage and cause overdose, or be less than the dosage of actual needs and cause invalid.Ibuprofen raw material light weight, if the ibuprofen suspension of the suspension technology of preparing preparation by routine keeps stable not difficult in a short time, but long-term, as 2 years, 3 years or longer time, keeps the uniformity of suspension, is still technical issues that need to address.Cause long-term placement of ibuprofen suspension ibuprofen to occur to assemble buoyant reason generally be because the physicochemical property of medicine, prescription, the drug particle feature, preparation technology's features etc. are relevant.
The present invention has obtained the stable hydro-planing ibuprofen suspension that well, is not prone to by a large amount of tests, found that by the test contrast ibuprofen particle size distribution is at 12 microns-28 microns, have good stability, preferred 15 microns-25 microns, more preferably 18 microns-20 microns.
In addition, be the suspension of main suspending agent with for example xanthan gum, its viscosity is measured by rotary viscosimeter, is not less than (75 * 0.4) mpas, and suspension stability is good, and mouthfeel is good, preferably is not less than (80 * 0.4) mpas, more preferably is not less than (85 * 0.4) mpas.
In addition, pre-preparation stability is ibuprofen suspension well, needs to comprise in the ibuprofen suspension prescription a certain amount of crucial adjuvant, and crucial adjuvant comprises for example Tween 80 of surfactant, and its consumption is 0.05-1% (V/V), preferred 0.2% (V/V); And pH value regulator citric acid for example, its consumption is to make that the pH value of suspension is between the 3-6, and preferred pH value is between the 4-5, and preferred pH value is 4.5.
In addition, preparation technology has an important factor among the role of material impact to stability, the present invention finds can further increase the stability of ibuprofen suspension by being prepared as follows technology, reduce the ibuprofen suspension hydro-planing: at first ibuprofen and wetting agent, surfactant are passed through the abundant homogenize of homogenizer, afterwards again with the abundant mix homogeneously of the solution that contains other composition promptly.
Ibuprofen suspension of the present invention (individually or their combination) under above-mentioned each influence factor, can prepare stability and well, not be prone to the hydro-planing ibuprofen suspension, even through long-time, after placing as 2 years even 3 years, ibuprofen suspension still keeps homodisperse steady statue, the gathering hydro-planing of ibuprofen do not occur.
The present invention is by above-mentioned research, solved that present ibuprofen suspension places for a long time that the ubiquitous stability in back is bad, lack of homogeneity, has been prone to the technical problem of assembling hydro-planing.
Embodiment
Be the illustrative preparation method of ibuprofen suspension of the present invention below.Yet scope of the present invention is not limited to this embodiment.Unless stated otherwise, all commercially available acquisition of all reagent.
Embodiment 1
200ml Tween 80 (0.2%), glycerol 5kg are dissolved in the water of 30kg, add ibuprofen (the about 18 μ m-20 μ m of particle size distribution) 2kg in the whipping process,, obtain the ibuprofen mixed liquor A by high-speed stirred emulsification pretreatment equipment homogenize 5 minutes.
Xanthan gum 0.2kg disperses with the 25kg purified water, and fully swelling after the stirring and dissolving, gets mixed solution B.Sorbitol 5kg, sucrose 10kg, sodium benzoate 0.3kg add purified water 20kg dissolving, get solution C.Solution C is with after B fully mixes, by emulsifying device 5 minutes, and with the mixed liquor A mix homogeneously, obtain mixed liquor D.Anhydrous citric acid 320g after a small amount of purified water dissolving, is added among the mixed liquor D, stirs, and adds purified water to about 100L cumulative volume, and stirs, and promptly gets ibuprofen suspension.
Suspension after testing, viscosity is (85 * 0.4) mpas, pH value is 4.5.
Embodiment 2
50ml Tween 80 (0.05%), glycerol 5kg are dissolved in the water of 30kg, add ibuprofen (the about 12 μ m-28 μ m of particle size distribution) 2kg in the whipping process,, obtain the ibuprofen mixed liquor A by high-speed stirred emulsification pretreatment equipment homogenize 5 minutes.
Xanthan gum 0.18kg disperses with the 25kg purified water, and fully swelling after the stirring and dissolving, gets mixed solution B.Sorbitol 5kg, sucrose 10kg, sodium benzoate 0.3kg add purified water 20kg dissolving, get solution C.Solution C is with after B fully mixes, by emulsifying device 5 minutes, and with the mixed liquor A mix homogeneously, obtain mixed liquor D.Anhydrous citric acid 475g after a small amount of purified water dissolving, is added among the mixed liquor D, stirs, and adds purified water to about 100L cumulative volume, and stirs, and promptly gets ibuprofen suspension.
Suspension after testing, viscosity is (75 * 0.4) mpas, pH value is 3.0.
Embodiment 3
1000ml Tween 80 (1%), glycerol 5kg are dissolved in the water of 30kg, add ibuprofen (the about 15 μ m-25 μ m of particle size distribution) 2kg in the whipping process,, obtain the ibuprofen mixed liquor A by high-speed stirred emulsification pretreatment equipment homogenize 5 minutes.
Xanthan gum 0.19kg disperses with the 25kg purified water, and fully swelling after the stirring and dissolving, gets mixed solution B.Sorbitol 5kg, sucrose 10kg, sodium benzoate 0.3kg add purified water 20kg dissolving, get solution C.Solution C is with after B fully mixes, by emulsifying device 5 minutes, and with the mixed liquor A mix homogeneously, obtain mixed liquor D.Anhydrous citric acid 65g after a small amount of purified water dissolving, is added among the mixed liquor D, stirs, and adds purified water to about 100L cumulative volume, and stirs, and promptly gets ibuprofen suspension.
Suspension after testing, viscosity is (80 * 0.4) mpas, pH value is 6.0.
The ibuprofen suspension of embodiment 1 to embodiment 3 and the acceleration appearance stability of certain commercially available product ibuprofen suspension test comparing result are as follows:
| The investigation time | Certain commercially available product | Suspension 1 of the present invention | Suspension 2 of the present invention | Suspension 3 of the present invention |
| 30 days | Even suspension | Even suspension, no hydro-planing | Even suspension, no hydro-planing | Even suspension, no hydro-planing |
| June | Ibuprofen is assembles floating trend | Even suspension, no hydro-planing | Even suspension, no hydro-planing | Even suspension, no hydro-planing |
| December | Ibuprofen accumulates in the suspension upper surface, and stratification state appears in suspension | Even suspension, no hydro-planing | Even suspension, no hydro-planing | Even suspension, no hydro-planing |
| 24 months | Ibuprofen accumulates in the suspension upper surface, and the bottom is the settled solution attitude | Even suspension, no hydro-planing | Even suspension, no hydro-planing | Even suspension, no hydro-planing |
Annotate: accelerated stability test condition: 40 ℃ of temperature, relative humidity 60 ± 5%.
As what it will be apparent to those skilled in the art that, can make many modifications and variations of the present invention and do not deviate from its spirit and scope.Specific embodiments described herein only provides in the mode of example, and gamut restriction the present invention of the equivalent that only is awarded together with these claim with claims.
Claims (10)
1. ibuprofen suspension, wherein, the particle diameter of described ibuprofen is between 12～28 μ m; Viscosity is not less than (75 * 0.4) mpas; Dosage of surfactant is 0.05～1%; PH value regulator consumption is to make that the pH value of suspension is between the 3-6.
2. ibuprofen suspension according to claim 1, wherein, the particle diameter of described ibuprofen is between 15～25 μ m.
3. ibuprofen suspension according to claim 2, wherein, the particle diameter of described ibuprofen is between 18～20 μ m.
4. ibuprofen suspension according to claim 1, wherein, described viscosity is not less than (80 * 0.4) mpas.
5. ibuprofen suspension according to claim 1, wherein, described surfactant is a Tween 80.
6. ibuprofen suspension according to claim 5, wherein, the consumption of described Tween 80 is 0.2%.
7. ibuprofen suspension according to claim 1, wherein, described pH value regulator is a citric acid.
8. ibuprofen suspension according to claim 7, wherein, described citric acid consumption is to make that the pH value of described suspension is between the 4-5.
9. according to each described ibuprofen suspension of claim 1-8, wherein, described ibuprofen suspension is prepared as follows: at first with ibuprofen and wetting agent, surfactant by the abundant homogenize of homogenizer, afterwards again with the abundant mix homogeneously of the solution that contains other composition.
10. the method for preparing each described ibuprofen suspension of claim 1-8, this method comprise at first ibuprofen and wetting agent, surfactant by the abundant homogenize of homogenizer, afterwards again with the abundant mix homogeneously of the solution that contains other composition.
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| CN103462889A (en) * | 2013-08-09 | 2013-12-25 | 林凡友 | Ibuprofen suspension and preparation method thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1481235A (en) * | 2000-11-16 | 2004-03-10 | ��������ķ������ | Microgranules based on active principle and method for making same |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1481235A (en) * | 2000-11-16 | 2004-03-10 | ��������ķ������ | Microgranules based on active principle and method for making same |
Non-Patent Citations (1)
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| 《中国药师》 19991231 冯晓东等 布洛芬混悬液的研制及临床疗效观察 第2卷, 第06期 2 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103462889A (en) * | 2013-08-09 | 2013-12-25 | 林凡友 | Ibuprofen suspension and preparation method thereof |
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Application publication date: 20101215 |