CN104323988A - Dexibuprofen pharmaceutical composition for injection - Google Patents
Dexibuprofen pharmaceutical composition for injection Download PDFInfo
- Publication number
- CN104323988A CN104323988A CN201410692234.7A CN201410692234A CN104323988A CN 104323988 A CN104323988 A CN 104323988A CN 201410692234 A CN201410692234 A CN 201410692234A CN 104323988 A CN104323988 A CN 104323988A
- Authority
- CN
- China
- Prior art keywords
- ibuprofen
- trometamol
- injection
- water
- stirred
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a dexibuprofen composition which comprises dexibuprofen and aqueous solution of tromethamine, wherein the concentration of the dexibuprofen is 2-4mg/ml, and the concentration of the tromethamine is 1.0-3.4mg/ml. The dexibuprofen composition can be resistant to high temperature sterilization and is high in process reproducibility.
Description
Technical field
The present invention relates to pharmaceutical field, be specifically related to a kind of Dexibuprofen pharmaceutical composition.
Background technology
Nonsteroidal antiinflammatory drug has good anti inflammation and heat resolution analgesic activity.Ibuprofen is go on the market in Britain nineteen sixty-eight the earliest, evident in efficacy due to antipyretic-antalgic aspect, and toxicity is low, is better than aspirin and acetaminophen, is widely used.Although there are many advantages, one of major defect of ibuprofen is its poorly soluble in water.WO 03/039532 and WO 2005/065674 describes the composition of liquid medicine of ibuprofen, and it comprises for improving the deliquescent aminoacid of ibuprofen, as arginine.Ibuprofen injection is in 2009 in U.S.'s listing, and wherein the concentration of ibuprofen is 100mg/ml, and the mol ratio of cosolvent arginine and ibuprofen is 0.92: 1.Disclosing ibuprofen concentration in ibuprofen injection in DE19912436A is 8mg/ml, and trometamol concentration is 6.04mg/ml, and its sterilization method adopts aseptic filtration, and under pointing out this concentration, compositions is not suitable for high temperature sterilize.For solving high temperature sterilize problem, CN102892410 discloses a kind of low concentration ibuprofen injection, and ibuprofen concentration is 2 ~ 6mg/ml, and trometamol concentration is 1.8 ~ 5.8mg/ml.
(S)-ibuprofen is S-(+)-isomer of ibuprofen, is very easily dissolved in ethanol, acetone, and chloroform and ether are water-soluble hardly.CN102362857A discloses a kind of Dexibuprofen injection, and said preparation is by (S)-ibuprofen, and meglumine, citric acid and trisodium citrate form, and (S)-ibuprofen concentration is 50mg/ml.CN103720647A discloses a kind of Dexibuprofen injection, and (S)-ibuprofen concentration is 100mg/ml, (S)-ibuprofen and arginic mol ratio 1: 0.8 to 1: 1.4, is preferably 1: 1.3.Because arginine can decompose in sterilization process, produce unpredictalbe impurity, we select trometamol and (S)-ibuprofen to combine.
Study favorite outer discovery, when adopting (S)-ibuprofen and trometamol to combine, during trometamol higher concentration, before and after filtering, content declines obviously, and for this reason, we are on prior art basis, provide a kind of preferred (S)-ibuprofen and trometamol compositions.
Summary of the invention
The invention provides a kind of new (S)-ibuprofen compositions.
Technical scheme of the present invention is: (S)-ibuprofen compositions, and it comprises the aqueous solution of (S)-ibuprofen and trometamol, wherein (S)-ibuprofen 2 ~ 4mg/ml, trometamol 1.0 ~ 3.4mg/ml.
(S)-ibuprofen is 2.5 ~ 3.5mg/ml preferably, and trometamol is 1.8 ~ 3.0mg/ml.
More preferably (S)-ibuprofen 2mg/ml, trometamol 1.0 ~ 1.4mg/ml, preferably 1.0 ~ 1.2mg/ml; Or
(S)-ibuprofen 3mg/ml, trometamol 1.5 ~ 2.7mg/ml, preferably 1.5 ~ 1.8mg/ml; Or
(S)-ibuprofen 4mg/ml, trometamol 2.4 ~ 3.4mg/ml, preferably 2.4 ~ 3.0mg/ml.
Above-mentioned (S)-ibuprofen compositions, also comprises pH adjusting agent and osmotic pressure regulator, and described pH adjusting agent is sodium hydroxide, pH scope 6.5 ~ 8.5, and described osmotic pressure regulator is sodium chloride.
The preparation method of described (S)-ibuprofen compositions is:
(1) trometamol and sodium hydroxide (and sodium chloride) are added in water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) active carbon is added, heated and stirred;
(4) filter, water for injection adds to enough, adjust ph;
(5) embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Before and after described (S)-ibuprofen compositions ensure that and filters, content is without significant change, resistant against high temperatures sterilizing.
Detailed description of the invention
Detailed description of the invention is only and further explains and describes the present invention, should not be interpreted as any limitation of the invention.
Comparative example 1
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide are added in 80% water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.5% active carbon (w/v) is added, heated and stirred;
(4) filter, water for injection adds to enough, measures pH6.7;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Comparative example 2
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide are added in 80% water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.5% active carbon (w/v) is added, heated and stirred;
(4) filter, water for injection adds to enough, measures pH6.7;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Embodiment 1
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide are added in water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.5% active carbon (w/v) is added, heated and stirred;
(4) filter, water for injection adds to enough, measures pH6.6; ;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Embodiment 2
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide are added in water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.5% active carbon (w/v) is added, heated and stirred;
(4) filter, water for injection adds to enough, measures pH6.8; ;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Embodiment 3
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide are added in water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.5% active carbon (w/v) is added, heated and stirred;
(4) filter, water for injection adds to enough, measures pH6.7;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Embodiment 4
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide are added in water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.5% active carbon (w/v) is added, heated and stirred;
(4) filter, water for injection adds to enough, measures pH6.6;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Embodiment 5
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide are added in water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.5% active carbon (w/v) is added, heated and stirred;
(4) filter, water for injection adds to enough, measures pH6.7;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Embodiment 6
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide are added in water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.5% active carbon (w/v) is added, heated and stirred;
(4) filter, water for injection adds to enough, measures pH6.7;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Testing example 1
(S)-ibuprofen assay (HPLC method)
Result shows, comparative example 1 and comparative example 2 trometamol consumption too high, in filter process, (S)-ibuprofen content significantly declines.
Embodiment 7
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide, sodium chloride are added in water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.1% active carbon (w/v) is added, heated and stirred;
(4) filter (after filtering, content declines 0.4%), water for injection adds to enough, pH7.3;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Embodiment 8
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide, sodium chloride are added in water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.1% active carbon (w/v) is added, heated and stirred;
(4) filter (after filtering, content declines 0.3%), water for injection adds to enough, measures pH8.5;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
Embodiment 9
Prescription:
Preparation method:
(1) trometamol and sodium hydroxide, sodium chloride are added in water for injection;
(2) add (S)-ibuprofen, be stirred to dissolving;
(3) liquid volume 0.1% active carbon (w/v) is added, heated and stirred;
(4) filter (after filtering, content declines 0.5%), water for injection adds to enough, measures pH7.8;
(5) vial embedding, sterilizing (121 DEG C, F0 > 12), to obtain final product.
More than describe the preferred embodiment of the present invention in detail; but; the present invention is not limited to the detail in above-mentioned embodiment; within the scope of technical conceive of the present invention; can carry out simply multiple to technical scheme of the present invention. modification; these simple variant all belong to protection scope of the present invention, as (S)-ibuprofen can replace to (S)-ibuprofen sodium salt by grade mole.
It should be noted that in addition, each concrete technical characteristic described in above-mentioned detailed description of the invention, in reconcilable situation, can be combined by any suitable mode, in order to avoid unnecessary repetition, the present invention illustrates no longer separately to various possible compound mode.
In addition, also can carry out combination in any between various different embodiment of the present invention, as long as it is without prejudice to thought of the present invention, it should be considered as content disclosed in this invention equally.
Claims (10)
1. a (S)-ibuprofen compositions, it comprises the aqueous solution of (S)-ibuprofen and trometamol, it is characterized in that, (S)-ibuprofen is 2 ~ 4mg/ml, and trometamol is 1.0 ~ 3.4mg/ml.
2. (S)-ibuprofen compositions according to claim 1, is characterized in that, (S)-ibuprofen is 2.5 ~ 3.5mg/ml, and trometamol is 1.8 ~ 3.0mg/ml.
3. (S)-ibuprofen compositions according to claim 1, is characterized in that, (S)-ibuprofen is 2mg/ml, and trometamol is 1.0 ~ 1.4mg/ml.
4. (S)-ibuprofen compositions according to claim 3, is characterized in that, trometamol is 1.0 ~ 1.2mg/ml.
5. (S)-ibuprofen compositions according to claim 1, is characterized in that, (S)-ibuprofen is 3mg/ml, and trometamol is 1.5 ~ 2.7mg/ml.
6. (S)-ibuprofen compositions according to claim 5, is characterized in that, trometamol is 1.5 ~ 1.8mg/ml.
7. (S)-ibuprofen compositions according to claim 1, is characterized in that, (S)-ibuprofen is 4mg/ml, and trometamol is 2.4 ~ 3.4mg/ml.
8. (S)-ibuprofen compositions according to claim 7, is characterized in that, trometamol is 2.4 ~ 3.0mg/ml.
9., according to the arbitrary described (S)-ibuprofen compositions of claim 1 to 8, it is characterized in that, containing pH adjusting agent.
10., according to the arbitrary described (S)-ibuprofen compositions of claim 1 to 8, it is characterized in that, containing isoosmotic adjusting agent.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410692234.7A CN104323988A (en) | 2014-11-27 | 2014-11-27 | Dexibuprofen pharmaceutical composition for injection |
| PCT/CN2015/075844 WO2016082413A1 (en) | 2014-11-27 | 2015-04-03 | Dexibuprofen pharmaceutical composition for injection and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410692234.7A CN104323988A (en) | 2014-11-27 | 2014-11-27 | Dexibuprofen pharmaceutical composition for injection |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104323988A true CN104323988A (en) | 2015-02-04 |
Family
ID=52398897
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410692234.7A Pending CN104323988A (en) | 2014-11-27 | 2014-11-27 | Dexibuprofen pharmaceutical composition for injection |
Country Status (2)
| Country | Link |
|---|---|
| CN (1) | CN104323988A (en) |
| WO (1) | WO2016082413A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016082413A1 (en) * | 2014-11-27 | 2016-06-02 | 北京蓝丹医药科技有限公司 | Dexibuprofen pharmaceutical composition for injection and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19912436A1 (en) * | 1999-03-19 | 2000-09-21 | Merckle Gmbh | Ibuprofen solution |
| CN101069681A (en) * | 2006-05-10 | 2007-11-14 | 汪洪湖 | Injection containing burufen |
| CN102892410A (en) * | 2010-05-18 | 2013-01-23 | 西班牙制药公司 | Pharmaceutical composition of ibuprofen for injection |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101978945B (en) * | 2010-10-25 | 2016-03-30 | 北京世纪博康医药科技有限公司 | A kind of ibuprofen medicinal composition |
| CN102381986A (en) * | 2011-07-25 | 2012-03-21 | 南京特丰药业股份有限公司 | Preparation methods of S-(+)-ibuprofen tromethamine salt and oral solution thereof |
| CN104323988A (en) * | 2014-11-27 | 2015-02-04 | 北京蓝丹医药科技有限公司 | Dexibuprofen pharmaceutical composition for injection |
-
2014
- 2014-11-27 CN CN201410692234.7A patent/CN104323988A/en active Pending
-
2015
- 2015-04-03 WO PCT/CN2015/075844 patent/WO2016082413A1/en active Application Filing
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19912436A1 (en) * | 1999-03-19 | 2000-09-21 | Merckle Gmbh | Ibuprofen solution |
| CN101069681A (en) * | 2006-05-10 | 2007-11-14 | 汪洪湖 | Injection containing burufen |
| CN102892410A (en) * | 2010-05-18 | 2013-01-23 | 西班牙制药公司 | Pharmaceutical composition of ibuprofen for injection |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016082413A1 (en) * | 2014-11-27 | 2016-06-02 | 北京蓝丹医药科技有限公司 | Dexibuprofen pharmaceutical composition for injection and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2016082413A1 (en) | 2016-06-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TWI692364B (en) | Ophthalmic solution containing diquafosol | |
| KR20150131230A (en) | Method for treatment of parkinson's disease | |
| WO2013089394A3 (en) | Composition of an aqueous solution of polymeric nanoparticles and method for preparing same | |
| JP6892494B2 (en) | Aqueous formulation containing paracetamol and ibuprofen | |
| CN101810569B (en) | Enrofloxacin injection liquid and preparation method thereof | |
| CN106466475B (en) | Composite formed by combining antibacterial peptide and polymer, preparation method and application thereof | |
| Siddiqui et al. | Synthesis and sensitive detection of doxycycline with sodium bis 2-ethylhexylsulfosuccinate based silver nanoparticle | |
| JP2018521007A5 (en) | ||
| JP6018048B2 (en) | Ibuprofen pharmaceutical composition for injection | |
| JP2018523694A (en) | Liquid formulation containing picosulfate and magnesium citrate | |
| JP2007055992A5 (en) | ||
| CN104323988A (en) | Dexibuprofen pharmaceutical composition for injection | |
| WO2013018050A3 (en) | Dissolution enhanced controlled drug delivery system for poorly water soluble drugs | |
| JP6549428B2 (en) | Oral composition | |
| CN103948914A (en) | Method for preparing drug-loadable low-molecular-weight water-soluble chitosan nano-particle | |
| CN105435221B (en) | Pharmaceutical composition of humanized antibody for vascular endothelial growth factor | |
| JP3658878B2 (en) | Oral solution | |
| KR101728799B1 (en) | Injections and its preparation method for producing a homogeneous solution was formed by solubilizing poorly soluble active pharmaceutical ingredient | |
| JP5535900B2 (en) | Gatifloxacin-containing aqueous solution, method for producing the same, and method for inhibiting precipitation of the aqueous solution at low temperature storage and freezing and thawing | |
| WO2010068181A8 (en) | 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6)1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene citrate salt | |
| TWI316403B (en) | Glycyrrhizin containing pharmaceutical composition | |
| WO2004093867A3 (en) | Phenolic acid salts of gabapentin in liquid and/or semi-solid dosage forms and methods of use | |
| WO2014045307A3 (en) | Pharmaceutical composition | |
| JP2012501331A (en) | Camphosfamide formulation and method for producing the same | |
| JP2008120795A (en) | Liquid formulation applicable to mucosa |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20150204 |
|
| RJ01 | Rejection of invention patent application after publication |