CN101669903A - Preparation method of ibuprofen aminophenol injection - Google Patents
Preparation method of ibuprofen aminophenol injection Download PDFInfo
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- CN101669903A CN101669903A CN200910093314A CN200910093314A CN101669903A CN 101669903 A CN101669903 A CN 101669903A CN 200910093314 A CN200910093314 A CN 200910093314A CN 200910093314 A CN200910093314 A CN 200910093314A CN 101669903 A CN101669903 A CN 101669903A
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- ibuprofen
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- aminophenol
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- aminoacid
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Abstract
The invention discloses a preparation method of ibuprofen aminophenol injection. After a plenty of experiment researches, the researchers finally find a way to prepare the ibuprofen aminophenol injection. The preparation method comprises the steps of making ibuprofen and aminophenol into a compound, combining with proper accessories and making into injection. By making ibuprofen and aminophenol into a compound, the invention can solve the problem of the inferior water-solubility of the ibuprofen. Making the compound into injection brings convenience to the patient who can not take orally. Theinvention has fast effect and obvious pharmacological action.
Description
Affiliated technical field
The invention belongs to medical technical field, be specifically related to a kind of preparation method of ibuprofen aminophenol injection.
Background technology
Ibuprofen from 1969 after Britain comes out, become one of most widely used medicine in global analgesia field gradually.Originally it mainly is used to treat chronic arthritis with less relatively dosage (1200mg/d), accumulation along with people's clinical experience, maximal dose when ibuprofen is used for the treatment of chronic inflammation disease and severe osteoarthritis constantly increases, and the therapeutic dose when above-mentioned two kinds of diseases are treated with this medicine by the Britain and the U.S. reaches 2400mg/d and 3600mg/d respectively.Meanwhile, (≤1200mg/d) indication is constantly expansion also, and light, moderate pain that multiple disease (comprising headache, heating, dysmenorrhea, musculoskeletal injuries, flu and influenza etc.) causes are its indication for low dose of ibuprofen.
Ibuprofen is an antiinflammatory antipyretic analgesic class OTC product, is one of the most general on-steroidal AID class medicine of clinical use, is widely used for treating rheumatism or rheumatoid disease by numerous doctors, and multiple pain such as articular muscle is felt sorry, headache, dysmenorrhea.But up to the present, most ibuprofen all have only peroral dosage form, and common ibuprofen dosage form has solid dosage formss such as tablet, powder, capsule, and all there are shortcomings such as stripping is slow, absorption is incomplete in above dosage form.When the patient can not oral medication, ibuprofen for injection can offer the patient and be used for alleviating pain and heating.Therefore June in 2009 drugs approved by FDA Cumberland on the 11st pharmaceutical manufacturing the ibuprofen for injection listing, but ibuprofen poorly water-soluble, there is certain difficulty so be made into liquid preparation, research worker of the present invention is discovered by experiment, after earlier ibuprofen and aminoacid being made complex, refabrication becomes injection, significantly increases the water solublity of ibuprofen, has significant antipyretic effect after the animal experiment study demonstration is made injection with this complex.
Summary of the invention
Research worker of the present invention is prepared into complex through lot of experiments earlier with ibuprofen and aminoacid, combines with proper auxiliary materials more afterwards, makes injection; The present invention makes complex with ibuprofen and aminoacid, has solved the shortcoming of ibuprofen poorly water-soluble, again this complex is prepared into injection, can not oral patient be offered convenience, and simultaneously rapid-action, pharmacological action is remarkable.
The object of the present invention is to provide a kind of ibuprofen and amino acid whose complex.
The injection that the object of the present invention is to provide a kind of ibuprofen and amino acid complex to be prepared into.
The object of the present invention is to provide a kind of preparation method of ibuprofen injection.
The present invention is achieved by the following technical solutions:
The preparation method of ibuprofen of the present invention and amino acid complex:
Ibuprofen and amino acid whose weight part ratio are: 1: 1
Take by weighing weight part ratio respectively and be 1: 1 aminoacid and ibuprofen.Earlier aminoacid is placed the 100mL measuring bottle, adding the 30mL distilled water is stirred to molten entirely under room temperature, again ibuprofen is slowly added after with anhydrous alcohol solution and stir 0.5-2h after adding distil water be settled to scale, constant temperature is added a cover for 25 ℃ and is stirred 10-14h, after the solution clarification, uncaps and continues to stir 2-4h, wave diffusing ethanol, reaction finishes and promptly gets the ibuprofen amino acid complex solution, and this solution contains ibuprofen 100mg/mL, and pH is 7.2-7.5.Ibuprofen amino acid complex solution rotary evaporation under room temperature is got light yellow crystalline powder except that desolvating, promptly get the ibuprofen amino acid complex.
Aminoacid of the present invention can be tyrosine, lysine, agedoite, glutamine, a kind of in the serine.
Ibuprofen liquid preparation preparation method of the present invention:
Earlier that ampoule bottle washing sterilization back is standby, take by weighing ibuprofen amino acid complex, buffer solution and join in 80% the water for injection, stirring and dissolving transfers pH between 5.0-6.0, adds the activated carbon chamber relaxing the bowels with purgatives of warm nature absorption 30 minutes of 0.1% (w/v), decarbonization filtering.Gained filtrate is tested, with the semi-finished product medicinal liquid dilution content to 100% that is up to the standards.Behind 0.22 μ m filtering with microporous membrane, fill is sealed in ampoule.115 ℃ of 30min that sterilize down.Leak detection, lamp inspection, packing is examined qualified back entirely and is stored.
The specific embodiment
Embodiment 1
Take by weighing tyrosine and the ibuprofen of 10g respectively.Earlier tyrosine is placed the 100mL measuring bottle, adding the 30mL distilled water is stirred to molten entirely under room temperature, again ibuprofen is slowly added after with anhydrous alcohol solution and stir 0.5h after adding distil water be settled to scale, constant temperature is added a cover for 25 ℃ and is stirred 10h, after the solution clarification, uncap and continue to stir 2h, wave diffusing ethanol, reaction finishes and promptly gets ibuprofen tyrosine complex solution, pH is 7.2, ibuprofen tyrosine complex solution rotary evaporation under room temperature is got light yellow crystalline powder except that desolvating, promptly get ibuprofen tyrosine complex.
Earlier that ampoule bottle washing sterilization back is standby, take by weighing ibuprofen tyrosine complex, buffer solution and join in 80% the water for injection, stirring and dissolving transfers pH between 5.0-7.0, adds the active carbon 60-70 ℃ of absorption 30 minutes of 0.1% (w/v), decarbonization filtering.Gained filtrate is tested, with the semi-finished product medicinal liquid dilution content to 100% that is up to the standards.Behind 0.22 μ m filtering with microporous membrane, fill is sealed in ampoule.115 ℃ of 30min that sterilize down.Leak detection, lamp inspection, packing is examined qualified back entirely and is stored.
Embodiment 2
Take by weighing 8g lysine and ibuprofen respectively.Earlier lysine is placed the 100mL measuring bottle, adding the 30mL distilled water is stirred to molten entirely under room temperature, again ibuprofen is slowly added after with anhydrous alcohol solution and stir 2h after adding distil water be settled to scale, constant temperature is added a cover for 25 ℃ and is stirred 14h, after the solution clarification, uncap and continue to stir 4h, wave diffusing ethanol, reaction finishes and promptly gets the ibuprofen lysinate complex solution, and pH is 7.5.Ibuprofen lysinate complex solution rotary evaporation under room temperature is got light yellow crystalline powder except that desolvating, promptly get the ibuprofen lysinate complex.
Earlier that ampoule bottle washing sterilization back is standby, take by weighing ibuprofen lysinate complex, buffer solution and join in 80% the water for injection, stirring and dissolving transfers pH between 5.0-7.0, adds the active carbon 60-70 ℃ of absorption 30 minutes of 0.1% (w/v), decarbonization filtering.Gained filtrate is tested, with the semi-finished product medicinal liquid dilution content to 100% that is up to the standards.Behind 0.22 μ m filtering with microporous membrane, fill is sealed in ampoule.115 ℃ of 30min that sterilize down.Leak detection, lamp inspection, packing is examined qualified back entirely and is stored.
Embodiment 3
Take by weighing agedoite and the ibuprofen of 12g respectively.Earlier agedoite is placed the 100mL measuring bottle, adding the 30mL distilled water is stirred to molten entirely under room temperature, again ibuprofen is slowly added after with anhydrous alcohol solution and stir 1h after adding distil water be settled to scale, constant temperature is added a cover for 25 ℃ and is stirred 12h, after the solution clarification, uncap and continue to stir 3h, wave diffusing ethanol, reaction finishes and promptly gets ibuprofen agedoite complex solution, and pH is 7.4.Ibuprofen agedoite complex solution rotary evaporation under room temperature is got light yellow crystalline powder except that desolvating, promptly get ibuprofen agedoite complex.
Earlier that ampoule bottle washing sterilization back is standby, take by weighing ibuprofen agedoite complex, buffer solution and join in 80% the water for injection, stirring and dissolving transfers pH between 5.0-7.0, adds the active carbon 60-70 ℃ of absorption 30 minutes of 0.1% (w/v), decarbonization filtering.Gained filtrate is tested, with the semi-finished product medicinal liquid dilution content to 100% that is up to the standards.Behind 0.22 μ m filtering with microporous membrane, fill is sealed in ampoule.115 ℃ of 30min that sterilize down.Leak detection, lamp inspection, packing is examined qualified back entirely and is stored.
Embodiment 4
Take by weighing 9g glutamine and ibuprofen respectively.Earlier glutamine is placed the 100mL measuring bottle, adding the 30mL distilled water is stirred to molten entirely under room temperature, again ibuprofen is slowly added after with anhydrous alcohol solution and stir 0.5-2h after adding distil water be settled to scale, constant temperature is added a cover for 25 ℃ and is stirred 10-14h, after the solution clarification, uncap and continue to stir 2.5h, wave diffusing ethanol, reaction finishes and promptly gets ibuprofen glutamine complex solution, and pH is 7.3.Ibuprofen glutamine complex solution rotary evaporation under room temperature is got light yellow crystalline powder except that desolvating, promptly get ibuprofen glutamine complex.
Earlier that ampoule bottle washing sterilization back is standby, take by weighing ibuprofen glutamine complex, buffer solution and join in 80% the water for injection, stirring and dissolving transfers pH between 5.5-6.0, adds the active carbon 60-70 ℃ of absorption 30 minutes of 0.1% (w/v), decarbonization filtering.Gained filtrate is tested, with the semi-finished product medicinal liquid dilution content to 100% that is up to the standards.Behind 0.22 μ m filtering with microporous membrane, fill is sealed in ampoule.115 ℃ of 30min that sterilize down.Leak detection, lamp inspection, packing is examined qualified back entirely and is stored.
Embodiment 5
Take by weighing 9g serine and ibuprofen respectively.Earlier serine is placed the 100mL measuring bottle, adding the 30mL distilled water is stirred to molten entirely under room temperature, again ibuprofen is slowly added after with anhydrous alcohol solution and stir 0.5-2h after adding distil water be settled to scale, constant temperature is added a cover for 25 ℃ and is stirred 10-14h, after the solution clarification, uncap and continue to stir 2.5h, wave diffusing ethanol, reaction finishes and promptly gets ibuprofen serine complex solution, and pH is 7.3.Ibuprofen serine complex solution rotary evaporation under room temperature is got light yellow crystalline powder except that desolvating, promptly get ibuprofen serine complex.
Earlier that ampoule bottle washing sterilization back is standby, take by weighing ibuprofen serine complex, buffer solution and join in 80% the water for injection, stirring and dissolving transfers pH between 5.5-6.5, adds the active carbon 60-70 ℃ of absorption 30 minutes of 0.1% (w/v), decarbonization filtering.Gained filtrate is tested, with the semi-finished product medicinal liquid dilution content to 100% that is up to the standards.Behind 0.22 μ m filtering with microporous membrane, fill is sealed in ampoule.115 ℃ of 30min that sterilize down.Leak detection, lamp inspection, packing is examined qualified back entirely and is stored.
Claims (4)
1. an ibuprofen aminophenol injection is characterized in that this injection is to make complex earlier by ibuprofen and aminoacid, makes injection again.
2. ibuprofen aminophenol injection is characterized in that ibuprofen and aminoacid weight part ratio are 1: 1 in this injection.
3. a kind of ibuprofen aminophenol injection as claimed in claim 1 is characterized in that the preparation method step of this injection is as follows:
Take by weighing weight part ratio respectively and be 1: 1 aminoacid and ibuprofen, earlier aminoacid is placed the 100mL measuring bottle, add the 30mL distilled water under room temperature, be stirred to molten entirely, again ibuprofen is slowly added after with anhydrous alcohol solution and stir 0.5-2h after adding distil water be settled to scale, constant temperature is added a cover for 25 ℃ and is stirred 10-14h, after the solution clarification, uncap and continue to stir 2-4h, wave diffusing ethanol, reaction finishes and promptly gets the ibuprofen amino acid complex solution, this solution contains ibuprofen 100mg/mL, and pH is 7.2-7.5; Ibuprofen amino acid complex solution rotary evaporation under room temperature is got light yellow crystalline powder except that desolvating, promptly get the ibuprofen amino acid complex;
Earlier that ampoule bottle washing sterilization back is standby, take by weighing ibuprofen amino acid complex, buffer solution and join in 80% the water for injection, stirring and dissolving transfers pH between 5.0-6.0, adds the activated carbon chamber relaxing the bowels with purgatives of warm nature absorption 30 minutes of 0.1% (w/v), decarbonization filtering; Gained filtrate is tested, with the semi-finished product medicinal liquid dilution content to 100% that is up to the standards; Behind 0.22 μ m filtering with microporous membrane, fill is sealed in ampoule; 115 ℃ of 30min that sterilize down; Leak detection, lamp inspection, packing is examined qualified back entirely and is stored.
4. ibuprofen aminophenol injection is characterized in that the aminoacid described in this injection can be tyrosine, lysine, agedoite, glutamine, a kind of in the serine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200910093314A CN101669903A (en) | 2009-09-27 | 2009-09-27 | Preparation method of ibuprofen aminophenol injection |
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| CN200910093314A CN101669903A (en) | 2009-09-27 | 2009-09-27 | Preparation method of ibuprofen aminophenol injection |
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| CN101669903A true CN101669903A (en) | 2010-03-17 |
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| CN200910093314A Pending CN101669903A (en) | 2009-09-27 | 2009-09-27 | Preparation method of ibuprofen aminophenol injection |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101885680A (en) * | 2010-07-26 | 2010-11-17 | 石家庄中硕药业集团有限公司 | Method for refining ibuprofen for injection |
| CN102138893A (en) * | 2011-03-21 | 2011-08-03 | 陕西宏府怡悦制药有限公司 | Preparation process and use of sodium lysinrofen chloride injection |
-
2009
- 2009-09-27 CN CN200910093314A patent/CN101669903A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101885680A (en) * | 2010-07-26 | 2010-11-17 | 石家庄中硕药业集团有限公司 | Method for refining ibuprofen for injection |
| CN101885680B (en) * | 2010-07-26 | 2012-12-19 | 石家庄中硕药业集团有限公司 | Method for refining ibuprofen for injection |
| CN102138893A (en) * | 2011-03-21 | 2011-08-03 | 陕西宏府怡悦制药有限公司 | Preparation process and use of sodium lysinrofen chloride injection |
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Application publication date: 20100317 |
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