CN101991540A - Ibuprofen injection and preparation method thereof - Google Patents
Ibuprofen injection and preparation method thereof Download PDFInfo
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- CN101991540A CN101991540A CN2009101020285A CN200910102028A CN101991540A CN 101991540 A CN101991540 A CN 101991540A CN 2009101020285 A CN2009101020285 A CN 2009101020285A CN 200910102028 A CN200910102028 A CN 200910102028A CN 101991540 A CN101991540 A CN 101991540A
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- ibuprofen
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- cyclodextrin
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Abstract
The invention relates to ibuprofen injection and a preparation method thereof. The ibuprofen injection comprises 0.5 to 20 weight percent of ibuprofen, 10 to 60 weight percent of cyclodextrin or cyclodextrin derivatives, 1 to 40 weight percent of water soluble excipient and the balance of water, wherein ibuprofen serves as a main medicament; and the cyclodextrin or cyclodextrin derivatives and the water soluble excipient serve as medicinal auxiliary materials. In the invention, the cyclodextrin or cyclodextrin derivatives represented by hydroxypropyl-beta-cyclodextrin is used to make the ibuprofen, which used to be water insoluble, very water soluble. The stability of the medicament is improved. The clathrate compounds can be made into injection using water as a solvent or power for injection. Thus, it is very convenient to administrate the medicament in clinic and it is easy to control injection volume. Meanwhile, the drawback of the universal adoption of auxiliary materials and solvents for injection, which are very dangerous, such as organic solvents and cosolvents, of the conventional insoluble and soluble medicinal injection is overcome.
Description
Technical field
The present invention relates to field of medicine preparations, relate in particular to a kind of ibuprofen injection and preparation method thereof.
Background technology
Rheumatic arthritis belongs to allergic disease, is one of main performance of rheumatic fever.How with febris acuta and arthralgia onset, typical case's performance is slight or the moderate heating, migratory polyarthritis, the joint of getting involved mostly are big joint such as knee joint, ankle, shoulder, elbow, wrist, commonly are transferred to another joint by a joint; the pathological changes part presents red, swollen, scorching hot, severe pain; part patient also has several joints to fall ill simultaneously, and atypical patient only has arthralgia and do not have other inflammation performances, and acute inflammation generally disappears in 2-4 week; do not stay sequela, but Chang Fanfu shows effect.If active rheumatism influences heart, then myocarditis can take place, even leave over valve disorder.
The analgesia of ibuprofen tool, antiinflammatory, refrigeration function.Its mechanism of action reduces the synthetic of prostaglandin by the inhibition to epoxidase, alleviates the sensitivity of the tissue hyperemia that causes because of prostaglandin, swelling, the reduction peripheral nerve pain sensation thus.It plays refrigeration function by the hypothalamus center of body temperature regulation.Ibuprofen is applicable to: 1, alleviate the acute attack stage of various chronic arthritiss such as rheumatoid arthritis, osteoarthritis, SpA, gouty arthritis, rheumatic arthritis or the arthralgia symptom of persistence, anosis effect because of the treatment and the control course of disease.2, the non-arthrogenous various soft tissue rheumatism pain of treatment are as shoulder pain, tenosynovitis, bursitis, the damaging pain of myalgia and motion back etc.3, acute light, moderate pain as: after operation back, the wound, strain back, primary dysmenorrhea, toothache, headache etc.4, the heating to adult and child has refrigeration function.Its analgesic activity of ibuprofen is stronger, and is stronger 16～32 times than aspirin; Antiinflammatory action a little less than, antipyretic effect similar to aspirin but the effect than more lasting.This product is lighter to the gastrointestinal side effect, and easily tolerance is minimum to gastrointestinal irritation in this type of medicine.
Ibuprofen has the preparation of multiple dosage form and specification at present using, and capsule, sheet, granule, syrup, suspendible, ointment, bolt, liniment, gel etc. are arranged, and is generally oral formulations.But ibuprofen has stronger acid, sheet, granule flavoring commonly used are not thorough, make its mouthfeel poor, in addition, the bioavailability of oral formulations is low, and onset is slow, when the patient can not oral medication, ibuprofen for injection can offer the patient and be used for alleviating pain and heating, and therefore clinical have epochmaking value.
The invention of ibuprofen injection is mainly used in inpatient releasing pain that can not be oral and brings down a fever.The commercially available injection that eases the pain only has opioid drug morphine and Pethidine and non-steroid antiinflammatory drug ketone to cough up sweet smell at present.Opioid drug can cause calmness, feels sick, vomiting, cognitive impairment and inhibition are breathed.Ketone is coughed up sweet smell the increase danger of bleeding, gastrointestinal tract and kidney complication.Ibuprofen is a white crystalline powder, and foreign odor is arranged, and is tasteless.Water insoluble, be soluble in ethanol, ether, chloroform and acetone, be soluble in sodium hydroxide and sodium carbonate liquor.Domestic no injection listing.
Summary of the invention
The object of the present invention is to provide a kind of rapid-action, bioavailability is high, side effect is little ibuprofen injection.
Another object of the present invention is to provide a kind of preparation method of ibuprofen injection.
In order to realize the foregoing invention purpose, the present invention adopts following technical scheme:
A kind of ibuprofen injection, comprise principal agent ibuprofen and pharmaceutically acceptable auxiliaries, described pharmaceutically acceptable auxiliaries comprises cyclodextrin or cyclodextrin derivative, water soluble excipient, each constituent content is ibuprofen 1%～20%, cyclodextrin or cyclodextrin derivant 10%～60% by weight percentage, water soluble excipient 1%～40% remains and is water.
Described cyclodextrin or cyclodextrin derivant are alpha-cyclodextrin, beta-schardinger dextrin-, gamma-cyclodextrin, alpha-cyclodextrin derivant, beta-cyclodextrin derivative, gamma-cyclodextrin derivant, preferred HP-.
Described water soluble excipient is one or more mixture of ethanol, Polyethylene Glycol, mannitol, lactose, glucose, xylitol, sorbitol and maltose alcohol.
The present invention can also comprise bronsted lowry acids and bases bronsted lowry.
Described acid is one or more mixture in hydrochloric acid, citric acid, tartaric acid, acetic acid, phosphoric acid, the maleic acid.
Described alkali is one or more mixture in sodium carbonate, sodium bicarbonate, sodium hydroxide, the sodium citrate.
Described injection is injection or sterile injection powder.
The preparation ibuprofen injection: at first cyclodextrin or cyclodextrin derivant are dissolved in water for injection, add ibuprofen then and stir, ultrasonic after stirring, obtain the ibuprofen inclusion complex in solution; Add other adjuvants again, PH is adjusted to about 6, filtration sterilization promptly.
Preparation ibuprofen sterile injection powder: at first cyclodextrin or cyclodextrin derivant are dissolved in water for injection, add ibuprofen then and stir, ultrasonic after stirring, obtain the ibuprofen inclusion complex in solution; Add other adjuvants again, PH is adjusted to about 6, filtration sterilization obtains the ibuprofen sterile injection powder through lyophilization.
Ibuprofen injection of the present invention has solved problems such as the onset that Motrin exists in the background technology is slow, bioavailability is low, side effect is big, and a kind of rapid-action, bioavailability is high, side effect is little ibuprofen injection is provided.It is the cyclodextrin or the derivant of representative with the HP-that the present invention has adopted, and insoluble to become water solublity fabulous by water to make ibuprofen.And stability of drug is improved.It is the injection of solvent that these clathrates both can be made into water, also can be made into sterile injection powder.Greatly facilitate clinical administration, dosage is controlled easily, has overcome simultaneously to have organic solvent and dangerous higher injection supplementary material and the solvents such as cosolvent, solubilizing agent that generally adopt in insoluble and the insoluble drug injection now.
The specific embodiment
The present invention will be further described below by specific embodiment, but the present invention is not limited by embodiment.
Embodiment 1: present embodiment preparation 250 ibuprofen injections (specification is 30mg/ml), adopt following prescription:
The name of material inventory
Ibuprofen 75g
HP-1000ml
Hydrochloric acid 100ml
PEG400 100ml
Sodium hydroxide is an amount of
Water for injection adds to 2500ml
Make 250
Preparation method: get HP-and place water for injection, after the dissolving, adding ibuprofen, it is ultrasonic to stir the back, obtain the ibuprofen inclusion complex in solution, add hydrochloric acid, Polyethylene Glycol to the ibuprofen inclusion complex in solution again, solution PH is adjusted to about 6 with sodium hydroxide, filter the back sterilization, obtain ibuprofen injection.
Embodiment 2: present embodiment preparation 250 ibuprofen sterile injection powders (specification is 300mg), adopt following prescription:
The name of material inventory
Ibuprofen 75g
HP-1000ml
Citric acid 150ml
Mannitol 100ml
Sodium bicarbonate is an amount of
Water for injection adds to 2500ml
Make 250
Preparation method: get HP-and place water for injection, after the dissolving, adding ibuprofen, it is ultrasonic to stir the back, obtain the ibuprofen inclusion complex in solution, add mannitol, citric acid to the ibuprofen inclusion complex in solution again, with sodium bicarbonate solution PH is adjusted to about 6 then, filter the back sterilization, obtain the ibuprofen sterile injection powder through lyophilization.
The ibuprofen sterile injection powder that the present invention makes, have the good characteristics of dissolubility, stability of drug is improved, overcome the organic solvent and dangerous higher injection supplementary material and the solvents such as cosolvent, solubilizing agent that generally adopt in the existing insoluble and insoluble drug injection, and advantage rapid-action, that bioavailability is high, side effect is little.
Embodiment 3: present embodiment preparation 250 ibuprofen sterile injection powders (specification is 200mg), adopt following prescription:
The name of material inventory
Ibuprofen 50g
HP-1000ml
Maleic acid 150ml
Glucose 100ml
Sodium citrate is an amount of
Water for injection adds to 2500ml
Make 250
Preparation method: get HP-and place water for injection, after the dissolving, adding ibuprofen, it is ultrasonic to stir the back, obtain the ibuprofen inclusion complex in solution, add glucose, maleic acid to the ibuprofen inclusion complex in solution again, with sodium citrate solution PH is adjusted to about 6 then, filter the back sterilization, obtain the ibuprofen sterile injection powder through lyophilization.
Embodiment 4: present embodiment preparation 250 ibuprofen injections (specification is 20mg/ml), adopt following prescription:
The name of material inventory
Ibuprofen 50g
Alpha-cyclodextrin 1000ml
Tartaric acid 100ml
PEG400 100ml
Sodium carbonate is an amount of
Water for injection adds to 2500ml
Make 250
Preparation method: get alpha-cyclodextrin and place water for injection, after the dissolving, adding ibuprofen, it is ultrasonic to stir the back, obtain the ibuprofen inclusion complex in solution, add tartaric acid, Polyethylene Glycol to the ibuprofen inclusion complex in solution again, solution PH is adjusted to about 6 with sodium carbonate, filter the back sterilization, obtain ibuprofen injection.
Claims (9)
1. ibuprofen injection, it is characterized in that comprising principal agent ibuprofen and pharmaceutically acceptable auxiliaries, described pharmaceutically acceptable auxiliaries comprises cyclodextrin or cyclodextrin derivative, water soluble excipient, each constituent content is ibuprofen 0.5%～20%, cyclodextrin or cyclodextrin derivant 10%～60% by weight percentage, water soluble excipient 1%～40% remains and is water.
2. a kind of ibuprofen injection according to claim 1, it is characterized in that described cyclodextrin or cyclodextrin derivant are alpha-cyclodextrin, beta-schardinger dextrin-, gamma-cyclodextrin, alpha-cyclodextrin derivant, beta-cyclodextrin derivative, gamma-cyclodextrin derivant, preferred HP-.
3. a kind of ibuprofen injection according to claim 1 is characterized in that described water soluble excipient is one or more mixture of ethanol, Polyethylene Glycol, mannitol, lactose, glucose, xylitol, sorbitol and maltose alcohol.
4. a kind of ibuprofen injection according to claim 1 is characterized in that also comprising bronsted lowry acids and bases bronsted lowry.
5. a kind of ibuprofen injection according to claim 4 is characterized in that described acid is one or more mixture in hydrochloric acid, citric acid, tartaric acid, acetic acid, phosphoric acid, the maleic acid.
6. a kind of ibuprofen injection according to claim 4 is characterized in that described alkali is one or more mixture in sodium carbonate, sodium bicarbonate, sodium hydroxide, the sodium citrate.
7. according to the described a kind of ibuprofen injection of claim 1～6, it is characterized in that described injection is injection or sterile injection powder.
8. the preparation method of a kind of ibuprofen injection according to claim 7, it is characterized in that preparing ibuprofen injection: at first cyclodextrin or cyclodextrin derivant are dissolved in water for injection, add ibuprofen then and stir, ultrasonic after stirring, obtain the ibuprofen inclusion complex in solution; Add other adjuvants again, PH is adjusted to about 6, filtration sterilization promptly.
9. the preparation method of a kind of ibuprofen injection according to claim 7, it is characterized in that preparing the ibuprofen sterile injection powder: at first cyclodextrin or cyclodextrin derivant are dissolved in water for injection, add ibuprofen then and stir, ultrasonic after stirring, obtain the ibuprofen inclusion complex in solution; Add other adjuvants again, PH is adjusted to about 6, filtration sterilization obtains the ibuprofen sterile injection powder through lyophilization.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2009101020285A CN101991540A (en) | 2009-08-27 | 2009-08-27 | Ibuprofen injection and preparation method thereof |
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|---|---|---|---|
| CN2009101020285A CN101991540A (en) | 2009-08-27 | 2009-08-27 | Ibuprofen injection and preparation method thereof |
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| CN101991540A true CN101991540A (en) | 2011-03-30 |
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| CN2009101020285A Pending CN101991540A (en) | 2009-08-27 | 2009-08-27 | Ibuprofen injection and preparation method thereof |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110283259A (en) * | 2019-07-03 | 2019-09-27 | 宁夏医科大学 | A kind of antipyretic-antalgic brufen-the first face of beta-cyclodextrin derivative and preparation method thereof |
| CN113318235A (en) * | 2021-06-15 | 2021-08-31 | 北京农学院 | Chitosan nanoparticles and preparation method thereof |
| CN113616813A (en) * | 2021-10-11 | 2021-11-09 | 奥信阳光(北京)药业科技有限公司 | Inclusion compound of ibuprofen and gallic acid modified sulfobutyl betacyclodextrin sodium |
| CN114588107A (en) * | 2022-04-06 | 2022-06-07 | 河北一品生物医药有限公司 | Ibuprofen lysine salt injection and preparation method thereof |
| CN115919846A (en) * | 2022-12-31 | 2023-04-07 | 江西益昕葆生物科技有限公司 | Carprofen clathrate compound, and preparation method and application thereof |
| GR1010769B (en) * | 2023-07-27 | 2024-09-18 | Ιουλια Κλεωνος Τσετη | Ibuprofen aqueous solution for intravenous administration |
-
2009
- 2009-08-27 CN CN2009101020285A patent/CN101991540A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110283259A (en) * | 2019-07-03 | 2019-09-27 | 宁夏医科大学 | A kind of antipyretic-antalgic brufen-the first face of beta-cyclodextrin derivative and preparation method thereof |
| CN113318235A (en) * | 2021-06-15 | 2021-08-31 | 北京农学院 | Chitosan nanoparticles and preparation method thereof |
| CN113616813A (en) * | 2021-10-11 | 2021-11-09 | 奥信阳光(北京)药业科技有限公司 | Inclusion compound of ibuprofen and gallic acid modified sulfobutyl betacyclodextrin sodium |
| CN114588107A (en) * | 2022-04-06 | 2022-06-07 | 河北一品生物医药有限公司 | Ibuprofen lysine salt injection and preparation method thereof |
| CN115919846A (en) * | 2022-12-31 | 2023-04-07 | 江西益昕葆生物科技有限公司 | Carprofen clathrate compound, and preparation method and application thereof |
| GR1010769B (en) * | 2023-07-27 | 2024-09-18 | Ιουλια Κλεωνος Τσετη | Ibuprofen aqueous solution for intravenous administration |
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| C57 | Notification of unclear or unknown address | ||
| DD01 | Delivery of document by public notice |
Addressee: Zhu Xulei Document name: Notification of Passing Preliminary Examination of the Application for Invention |
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20110330 |