CN102552133A - Middle/long chain triglyceride flurbiprofen axetil injection and preparation method thereof - Google Patents
Middle/long chain triglyceride flurbiprofen axetil injection and preparation method thereof Download PDFInfo
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- CN102552133A CN102552133A CN201010590512XA CN201010590512A CN102552133A CN 102552133 A CN102552133 A CN 102552133A CN 201010590512X A CN201010590512X A CN 201010590512XA CN 201010590512 A CN201010590512 A CN 201010590512A CN 102552133 A CN102552133 A CN 102552133A
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- chain triglycerides
- flurbiprofen
- flurbiprofen axetil
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Abstract
The invention provides anti-inflammatory and analgesic flurbiprofen axetil injection and a preparation method thereof. A mixture of 0.1-10 percent (w/v) of flurbiprofen axetil, 10-20 percent (w/v) of middle chain triglyceride (MCT) and 10-20 percent (w/v) of long chain triglyceride (LCT) is contained in the prescription (wherein the proportion of MCT and LCT is 4:1-1:4). The preparation method comprises the following steps: taking 1-5 percent (w/v) of lecithin as an emulsifying agent, taking 1-5 percent (w/v) of glycerol as an isotonic agent, finally adding disodium hydrogen phosphate, citric acid and water for injection and adjusting the pH value to 4-7 to prepare flurbiprofen axetil fat emulsion injection through colostrums, homogeneity and sterilization. The injection has the beneficial effects that the anti-inflammatory and analgesic effect is taken more quickly; the accumulation of fat of a human body can be reduced, and fatty tissues and liver load can be reduced; and the injection is more suitable for critically ill patients and people with poor liver functions and has lower toxic and side effects.
Description
Technical field
The present invention relates to a kind of anti-inflammatory analgesic Flurbiprofen axetil fat emulsion injection and preparation method thereof; The mixture that contains median chain triglyceride oil (MCT) and long chain triglycerides (LCT) in this injection; Its anti-inflammatory analgesic drug effect onset is rapid, is applicable to the anti-inflammatory analgesic treatment of human body.
Background technology
Flurbiprofen axetil (Furbiprofen axetil) has another name called: triumphant confused, its chemical name is: (±) 2-(2-fluoro-4-xenyl) propanoic acid-1-acetoxyl group ethyl ester, 1992 at first in Japan's listing, goes on the market in China in 2004.The flurbiprofen ester injection is non-steroidal intravenous injection targeting analgesic; Have persistent, advantage that curative effect is clear and definite, and do not have dependency and have the effect of preemptive analgesia, be widely used in clinical at present; Because Flurbiprofen axetil is water insoluble, present dosage form is the Emulsion injection.Japan Patent (JP 1985001122) discloses a kind of technology preparation of Flurbiprofen axetil fat emulsion injection; The Flurbiprofen axetil that wherein contains 1% (w/v), the phosphoric acid of the enuatrol, 0.05% (w/v) of the glycerol, 0.05% (w/v) of the lecithin, 2.25% (w/v) of 10% soybean oil, 1.2% (w/v).After through constantly improving into present prescription promptly: the Flurbiprofen axetil of 1% (w/v), glycerol, 0.05% (w/v) sodium hydrogen phosphate of the lecithin, 2.25% (w/v) of 10% soybean oil, 1.2% (w/v), water for injection are also regulated pH value 4.5-6.5 with citric acid.Though present prescription is extensive use and clinical,, its carrier therefore can increase risk clinically because being long chain triglycerides.For example: the risk that hypertriglyceridemia occurs is bigger, and the metabolic burden of liver fat is heavier, and particularly metabolism exists the patient of obstacle more unfavorable to ester.And median chain triglyceride oil is compared characteristics such as having rapid, the quick digestion of absorption of human body, quick oxidation Decomposition with long chain triglycerides; Consequently median chain triglyceride oil can provide heat energy at any time and be difficult for being stored by human body; But because median chain triglyceride oil does not contain the necessary fatty acid of human body; Generally need and a certain amount of long-chain long chain triglycerides mixing use, this point gets the nod at other drug, for example: parenteral nutrition medicine fat emulsion injection, anesthetics propofol injection etc.The mixture of use median chain triglyceride oil (MCT) and long chain triglycerides (LCT) can effectively reduce the shortcoming (CLINICAL NUTRITION (1989) 8:223-235) of simple use long chain triglycerides as carrier.The present invention just is being based on such consideration a kind of Flurbiprofen axetil fat emulsion injection and preparation method thereof is provided.
Summary of the invention
The present invention is directed to the defective of existing Flurbiprofen axetil fat emulsion injection; With the long chain triglycerides in the former injection with in a certain proportion of/long chain triglycerides replace processing in/long-chain (C6-C24) Flurbiprofen axetil fat emulsion injection, thereby reach the therapeutic effect of anti-inflammatory analgesic.Its drug effect is rapid-action, toxic side effects is low, is applicable to that the critical patient uses.
In a kind of/long chain triglycerides flurbiprofen ester injection, its composition weight volume ratio (W/V) as follows:
Flurbiprofen axetil 0.1%～10%
In/long chain triglycerides mixture 10%～20%
(wherein the w/v of median chain triglyceride oil and long chain triglycerides is 4: 1～1: 4) lecithin 1%～5%
Glycerol 1%～5%
Sodium dihydrogen phosphate 0.05%～0.1%
All the other are water for injection,
In the said medicine component, add water for injection, and regulate PH to 4.0～7.0 with citric acid.
The preferred proportioning of the present invention (W/V) is:
Flurbiprofen axetil 1%
Median chain triglyceride oil 5%
Long chain triglycerides 5%
Lecithin 1.2%
Glycerol 2.25%
Sodium hydrogen phosphate 0.05%
All the other are water for injection,
Regulate PH to 4.5～6.5 with citric acid.
Described long chain triglycerides can replace with soybean oil; This injectable drug is used for the anti-inflammatory analgesic treatment of human body.
The method for preparing of injection of the present invention is:
By said ratio; Flurbiprofen axetil, median chain triglyceride oil, long chain triglycerides, lecithin are mixed; High-speed stirred forms solution under 40 ℃～75 ℃ temperature; And same sodium hydrogen phosphate, glycerol, aqueous solution for injection with citric acid regulator solution pH value to 4～7, form colostrum through homogenizer 20 ℃～40 ℃ mixing then; The continuous high pressure of colostrum (pressure 500kg/cm
2-700kg/cm
2) homogenizing 4～7 times, again through irritate, envelope and 115 ℃ of sterilizations 30 minutes, make injection of the present invention.
Described long chain triglycerides can replace with soybean oil.This injectable drug is used for the anti-inflammatory analgesic treatment of human body.
Beneficial effect of the present invention:
Compare with existing Flurbiprofen axetil fat emulsion injection; These article anti-inflammatory analgesic drug effect is remarkable, and it is rapider to have an onset, can reduce body fat accumulation, reduce fatty tissue and liver load; Be applicable to critical patient and hepatic disfunction person's use more, and have lower toxic and side effects.
The specific embodiment
Through embodiment the present invention is explained below, but be not limited to following examples embodiment 1
The preparation injection
Proportioning:
| Flurbiprofen axetil | 100g |
| Long chain triglycerides | 500g |
| Median chain triglyceride oil | 500g |
| Lecithin | 120g |
| Glycerol | 225g |
| Sodium hydrogen phosphate | 5g |
| Water for injection | Add to 10000ml |
| Citric acid | Regulate pH 4.0～7.0 |
Preparation process: by the accurate weighing material of above proportioning; Flurbiprofen axetil, median chain triglyceride oil, long chain triglycerides, lecithin are blended in 40 ℃ of-75 ℃ of high-speed stirred form solution; And same sodium dihydrogen phosphate, glycerol, aqueous solution for injection be 20 ℃ of-40 ℃ of mixing, and regulate PH4.5 with citric acid and form colostrum through homogenizer then.(the continuous high pressure of colostrum keep-ups pressure 500kg/cm
2-600kg/cm
2) homogenizing 5 times, through irritate, envelope and 115 ℃ of sterilizations 30 minutes.
Embodiment 2
Proportioning:
| Flurbiprofen axetil | 200g |
| Long chain triglycerides | 1000g |
| Median chain triglyceride oil | 1000g |
| Lecithin | 120g |
| Glycerol | 250g |
| Sodium hydrogen phosphate | 10g |
| Water for injection | Add to 10000ml |
| Citric acid | Regulate pH 4.0～7.0 |
Preparation process: by the accurate weighing material of above proportioning; Flurbiprofen axetil, median chain triglyceride oil, long chain triglycerides, lecithin are blended in 40 ℃ of-75 ℃ of high-speed stirred form solution; And same sodium dihydrogen phosphate, glycerol, aqueous solution for injection be 20 ℃ of-40 ℃ of mixing, and regulate PH6.0 with citric acid and form colostrum through homogenizer then.(the continuous high pressure of colostrum keep-ups pressure 600kg/cm
2-700kg/cm
2) homogenizing 7 times, through irritate, envelope and 121 ℃ of sterilizations 12 minutes.
Embodiment 3
Proportioning:
| Flurbiprofen axetil | 200g |
| Long chain triglycerides | 800g |
| Median chain triglyceride oil | 1200g |
| Lecithin | 120g |
| Glycerol | 250g |
| Sodium hydrogen phosphate | 10g |
| Water for injection | Add to 10000ml |
| Citric acid | Regulate pH 4.0～7.0 |
Preparation process: by the accurate weighing material of above proportioning; Flurbiprofen axetil, median chain triglyceride oil, long chain triglycerides, lecithin are blended in 40 ℃ of-75 ℃ of high-speed stirred form solution; And same sodium dihydrogen phosphate, glycerol, aqueous solution for injection be 20 ℃ of-40 ℃ of mixing, and regulate PH5.5 with citric acid and form colostrum through homogenizer then.(the continuous high pressure of colostrum keep-ups pressure 600kg/cm
2-700kg/cm
2) homogenizing 7 times, through irritate, envelope and 115 ℃ of sterilizations 30 minutes.
Claims (5)
1. in one kind/and long chain triglycerides flurbiprofen ester injection, W/V is following for its composition weight volume ratio:
Flurbiprofen axetil 0.1%～10%
In/mixture 10%～20% of long chain triglycerides
In said mixture, the w/v W/V of median chain triglyceride oil and long chain triglycerides is 4: 1～1: 4
Lecithin 1%～5%
Glycerol 1%～5%
Sodium hydrogen phosphate 0.05%～0.1%
All the other are water for injection,
In the said medicine component, add water for injection, and regulate PH to 4.0～7.0 with citric acid.
2. in according to claim 1/and the long chain triglycerides injection, its composition weight volume ratio W/V is:
Flurbiprofen axetil 1%
Median chain triglyceride oil 5%
Long chain triglycerides 5%
Lecithin 1.2%
Glycerol 2.25%
Sodium hydrogen phosphate 0.05%
All the other are water for injection,
Regulate PH to 4.5～6.5 with citric acid.
3. in one kind/method for preparing of long chain triglycerides flurbiprofen ester injection is: by said ratio; Flurbiprofen axetil, median chain triglyceride oil, long chain triglycerides, lecithin are mixed; High-speed stirred forms solution under 40 ℃～75 ℃ temperature; And same sodium hydrogen phosphate, glycerol, aqueous solution for injection be 20 ℃～40 ℃ mixing, with citric acid regulator solution pH value to 4～7, after form colostrum through homogenizer; The continuous high pressure homogenize of colostrum 4～7 times is through irritating, seal and sterilizing 30 minutes at 115 ℃.
4. in according to claim 1/and long chain triglycerides flurbiprofen ester injection, it is characterized in that long chain triglycerides replaces with soybean oil.
5. in according to claim 1/and long chain triglycerides flurbiprofen ester injection, it is characterized in that this injection is used for the anti-inflammatory analgesic treatment of human body.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201010590512XA CN102552133A (en) | 2010-12-15 | 2010-12-15 | Middle/long chain triglyceride flurbiprofen axetil injection and preparation method thereof |
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|---|---|---|---|
| CN201010590512XA CN102552133A (en) | 2010-12-15 | 2010-12-15 | Middle/long chain triglyceride flurbiprofen axetil injection and preparation method thereof |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103393631A (en) * | 2013-08-22 | 2013-11-20 | 北京蓝丹医药科技有限公司 | Flurbiprofen axetil pharmaceutical composition |
| CN104434783A (en) * | 2014-11-13 | 2015-03-25 | 广东嘉博制药有限公司 | Diazepam medium/long-chain fat emulsion preparation and preparation method thereof |
| CN104706575A (en) * | 2013-12-16 | 2015-06-17 | 天津迈迪瑞康生物医药科技有限公司 | Flurbiprofen axetil fat emulsion concentrate and preparation method and use thereof |
| CN104784115A (en) * | 2014-01-20 | 2015-07-22 | 华东理工大学 | Flurbiprofen axetil microsphere injection and preparation method thereof |
| CN108143715A (en) * | 2016-12-02 | 2018-06-12 | 北京普德康利医药科技发展有限公司 | A kind of florfenicol residues |
| CN109793713A (en) * | 2019-03-26 | 2019-05-24 | 李世系 | A kind of pharmaceutical composition and its injection preparation method and application of the short-acting hypnotic calmness for anesthesia |
| CN110237359A (en) * | 2019-06-28 | 2019-09-17 | 广东嘉博制药有限公司 | A kind of pre- encapsulating ejection preparation of emulsion injection and preparation method thereof |
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| CN1846776A (en) * | 2005-04-12 | 2006-10-18 | 天津天士力制药股份有限公司 | Injection of long-chain fat from zedoary oil and its prepn process |
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103393631A (en) * | 2013-08-22 | 2013-11-20 | 北京蓝丹医药科技有限公司 | Flurbiprofen axetil pharmaceutical composition |
| CN103393631B (en) * | 2013-08-22 | 2015-04-08 | 北京蓝丹医药科技有限公司 | Flurbiprofen axetil pharmaceutical composition |
| CN104706575A (en) * | 2013-12-16 | 2015-06-17 | 天津迈迪瑞康生物医药科技有限公司 | Flurbiprofen axetil fat emulsion concentrate and preparation method and use thereof |
| CN104784115A (en) * | 2014-01-20 | 2015-07-22 | 华东理工大学 | Flurbiprofen axetil microsphere injection and preparation method thereof |
| CN104434783A (en) * | 2014-11-13 | 2015-03-25 | 广东嘉博制药有限公司 | Diazepam medium/long-chain fat emulsion preparation and preparation method thereof |
| CN108143715A (en) * | 2016-12-02 | 2018-06-12 | 北京普德康利医药科技发展有限公司 | A kind of florfenicol residues |
| CN109793713A (en) * | 2019-03-26 | 2019-05-24 | 李世系 | A kind of pharmaceutical composition and its injection preparation method and application of the short-acting hypnotic calmness for anesthesia |
| CN110237359A (en) * | 2019-06-28 | 2019-09-17 | 广东嘉博制药有限公司 | A kind of pre- encapsulating ejection preparation of emulsion injection and preparation method thereof |
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Application publication date: 20120711 |