CN1557290A - Compound diclofenac Potassium injection liquid formulation - Google Patents
Compound diclofenac Potassium injection liquid formulation Download PDFInfo
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- CN1557290A CN1557290A CNA2004100139519A CN200410013951A CN1557290A CN 1557290 A CN1557290 A CN 1557290A CN A2004100139519 A CNA2004100139519 A CN A2004100139519A CN 200410013951 A CN200410013951 A CN 200410013951A CN 1557290 A CN1557290 A CN 1557290A
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- diclofenac potassium
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- propylene glycol
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- potassium
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Abstract
The compound diclofanac potassium injection preparation is prepared with diclofanac potassium and Lidocaine hydrochloride as main components as well as supplementary material including polyglycol-400 and propylene glycol as solvent and pH regulator, antixidant, bateria-free injection water, etc. The injection preparation contains diclofanac potassium 10-50 mg/ml, Lidocaine 5-20 mg/ml, polyglycol-400 in 5-30 vol% and propylene glycol in 5-50 vol%. The present invention is used mainly in treating rheumatism, including various kinds of arthritises, and may be also applied clinically in treating acute pain . The addition of Lidocaine hydrochloride can reduce pain and tissue damage in the injected part effectively.
Description
Affiliated technical field
The present invention relates to a kind of compound injection liquid formulation.
Background technology
Diclofenac is the potent non_steroidal anti_inflammatory drug of third generation fenamic acids, by suppressing Cycloxygenase, suppresses the synthetic of the interior prostaglandin of body, thereby blocks the intermediate link of inflammatory reaction process, reaches the purpose of anti-inflammatory analgesic; To rheumatic arthritis, rheumatoid arthritis, degenerative osteoarthritis, gout, periarticular soft tissues inflammation are damaged caused arthralgia and are had the good curing effect.Its curative effect is better than the anti-class medicines of other outer steroidal classes such as indometacin, aspirin, ibuprofen, naproxen, and absorb fast, few side effects, gastrointestinal reaction is lighter than most of nonsteroidal antiinflammatory drugs, better tolerance, dosage is little, and individual variation is little, so be widely used in more than 120 countries and regions, countries in the world at present.With the lidocaine hydrochloride prescription, can improve dissolubility and the stability of diclofenac potassium in solution, also can alleviate local injection liquid pain effectively, therefore, the compound injection liquid formulation of exploitation diclofenac potassium and lidocaine hydrochloride, the effect of pharmacological action can be reached, patient's compliance can be satisfied again.
Summary of the invention:
The present invention provides a kind of practicality for clinical, and the injection formulation of rheumatism treatment reliably cures mainly rheumatism outside inflammation, joint degeneration and the joint of muscle joint, joint capsule, tendon, stndon sheath and lumbar spine.
The present invention is a main component with diclofenac potassium and lidocaine hydrochloride, and being aided with PEG400 and propylene glycol is solvent and other antioxidant, the PH regulator, and sterilizeds water for injection etc. are made injection routinely, make it reach the purpose of anti-inflammatory analgesic; To rheumatic arthritis, rheumatoid arthritis, degenerative osteoarthritis, caused arthralgia such as gout has the good curing effect, can also alleviate local injection pain effectively simultaneously.
The content of diclofenac potassium of the present invention is 10-50mg/ml; The content of the content 5-20mg/ml Polyethylene Glycol of lidocaine hydrochloride is 5%-30% (V/V); The content of propylene glycol is 5%-50% (V/V).
The preferred version of injection of the present invention is: the diclofenac potassium content is 18-48mg/ml, and the content of lidocaine hydrochloride is 8-18mg/ml, and the content of PEG400 is 7.5%-25% (V/V), and the content of propylene glycol is 7.5%-40% (V/V).
Diclofenac potassium belongs to nonsteroidal anti-inflammatory analgetic, the main mechanism of action of well-known outer steroidal class anti-inflammation analgesia medicine is that they can be suppressed at conversion of arachidonic acid and be converted into some invertase that play an important role in the prostatitic process, prostaglandin is a main inflammatory mediator in the body, and it plays important regulatory role in the pathological process of heating and pain.Diclofenac potassium is potent cox-2 inhibitors, and Cycloxygenase is a kind of enzyme in the prostaglandin building-up process, because diclofenac potassium has inhibitory action to this kind of enzyme, and Here it is its mechanism place that plays a role.
Lidocaine hydrochloride belongs to local anesthetic, this medicine is rapid-action, effect is strong and lasting, penetration power is also stronger, and to organizing almost nonirritant, the local vascular dilation effect is not obvious, safety range is bigger, can penetrate mucosa, because this preparation is mainly used in intramuscular injection, this component plays the effect that reduces local pain at prescription.
PEG400 is an ethylene oxide polymer among the present invention, this product is a liquid, can be miscible with water, ethanol, glycerol and propylene glycol etc., belong to solvent for injection relatively more commonly used, this product except as the solvent place, has also played considerable effect aspect sample stability in prescription.
Propylene glycol can increase the stability of the dissolubility and the raising injection of medicine also as solvent for injection in this prescription.
As previously mentioned, compound diclofenac potassium injection has antiinflammatory and analgesic character, can suppress the synthetic of prostaglandin.Be applicable to muscle clinically, disease outside the inflammation of joint, joint capsule, bursa and vertebra and the joint is as soft tissue rheumatism, bursitis, tenosynovitis, sciatica and all kinds of neuritis and neuralgia, the pain that outer rheumatic inflammation causes, various neuralgias, pain after operation and the wound.
The present invention is because with diclofenac potassium, lidocaine hydrochloride and PEG400, propylene glycol organically combines, and makes injection, thereby makes it both have the pharmacological action of anti-inflammatory analgesic, can alleviate local injection pain effectively again, improve the dissolubility and the stability of injection simultaneously again.
Pharmacodynamics test of the present invention studies show that: this product can be obvious to the suppression ratio that rat carrageenan causes after the sufficient sole of the foot swells; The swollen hypertrophy of rat granuloma also had the obvious suppression effect; Dichlorodiphenyl Acetate causes the pain mice and has significant analgesia role.
The present invention is by anaphylaxis, and hemolytic and blood vessel irritation test show: there is not anaphylaxis in compound diclofenac potassium injection, hemolytic and blood vessel irritation.
The present invention passes through the clinical practice to lumbago and skelalgia 7 examples of 50 routine rheumatic arthritis, 12 routine intervertebral disk hernia, 6 routine degeneration gonarthritis, 4 routine ankylosing spondylitiss and other reasons, the result shows, this product is rapid-action, and curative effect is obvious, is a kind of safe non-steroidal anti-inflammatory compound recipe medication.
PH regulator involved in the present invention, antioxidant etc., but the relevant kind that drug of choice allusion quotation textbook and document record are according to the conventional method adjustment.
The specific embodiment
Embodiment one: its prescription is: diclofenac potassium 78.8g, lidocaine hydrochloride 20g, PEG400 are that 300ml, propylene glycol 400ml, sodium sulfite 2g, EDTAlg, 10% sodium hydroxide solution are an amount of, sterilized water for injection adds to 2000ml, make 1000 of 2ml injections, its preparation method is: take by weighing lidocaine hydrochloride with after the low amounts of water dissolving, add propylene glycol and PEG400 again, stir, standby as solution I.Other takes by weighing after diclofenac potassium is dissolved in an amount of about 50 ℃-60 ℃ sterilized water for injection, adds sodium sulfite and EDTA, stirs and also makes the two dissolving, and is standby, as solution II.Solution I is slowly poured in the solution II of not stopping stirring, regulate PH to 7.0-8.5 with 10% sodium hydroxide after, add to the full amount of water for injection, stir, filter, embedding is in the 2ml ampoule bottle, 100 ℃ of flowing steam sterilizations 30 minutes are promptly.
Embodiment two: its prescription is: diclofenac potassium 78.8g, lidocaine hydrochloride 20g, PEG400 is 350ml, propylene glycol 350ml, sodium pyrosulfite 2g, EDTA0.2g, 10% sodium hydroxide solution is an amount of, and sterilized water for injection adds to 2000ml, makes 1000 of 2ml injections, its preparation method is: take by weighing hydrochloric acid Li Kaduoyin with after the low amounts of water dissolving, add propylene glycol and PEG400, stir, it is an amount of to add 10% sodium hydroxide solution again, regulate about pH value to 7.0, as solution I.Other takes by weighing after diclofenac potassium is dissolved in an amount of about 50-60 ℃ sterilized water for injection, adds sodium pyrosulfite and EDTA, stirs and also makes the two dissolving, and is standby, as solution II.Solution I is slowly poured in the solution II of not stopping stirring, and the sodium hydroxide solution of reuse 10% is regulated the pH value of whole solution to 7.0-8.5, adds to the full amount of water for injection, and stirs, and filters embedding in the 2ml ampoule bottle, and 100 ℃ of flowing steam sterilizations 30 minutes promptly.
Claims (3)
1, a kind of compound diclofenac potassium injection formulation is a Main Ingredients and Appearance with diclofenac potassium and lidocaine hydrochloride, and auxilliary is that PEG400 and propylene glycol are solvent and PH regulator, antioxidant, sterilized water for injection etc., the injection dosage form of making.
2, compound diclofenac potassium injection formulation according to claim 1, the content that it is characterized in that diclofenac potassium is 10-50mg/ml, the content of lignocaine is 5-20mg/ml, and the content of PEG400 is that the content of 5%-30% (V/V) and propylene glycol is 5-50% (V/V).
3, compound diclofenac potassium injection formulation according to claim 2, it is characterized in that the diclofenac potassium content is 8-48mg/ml, lidocaine hydrochloride 8-18mg/ml, PEG400 content are that the content of 7.5%-25% (V/V) and propylene glycol is 7.5-40% (V/V).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100139519A CN1557290A (en) | 2004-01-19 | 2004-01-19 | Compound diclofenac Potassium injection liquid formulation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100139519A CN1557290A (en) | 2004-01-19 | 2004-01-19 | Compound diclofenac Potassium injection liquid formulation |
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| CN1557290A true CN1557290A (en) | 2004-12-29 |
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| CNA2004100139519A Pending CN1557290A (en) | 2004-01-19 | 2004-01-19 | Compound diclofenac Potassium injection liquid formulation |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101485650B (en) * | 2009-02-19 | 2013-07-17 | 辰欣药业股份有限公司 | Diclofenac sodium and lidocaine hydrochloride injection and preparation method thereof |
| US8809393B2 (en) | 2005-02-01 | 2014-08-19 | Troikaa Pharmaceuticals Ltd | Injectable preparations of diclofenac and its pharmaceutically acceptable salts |
| CN105663105A (en) * | 2016-01-15 | 2016-06-15 | 广州一品红制药有限公司 | Diclofenac sodium-lidocaine compound injection |
| WO2021009525A1 (en) * | 2019-07-18 | 2021-01-21 | Lovasz Sandor | Medicinal and/or pharmaceutical compositions for intravesical instillation, preparation and use thereof |
| US11406612B2 (en) | 2018-02-26 | 2022-08-09 | Rensselaer Polytechnic Institute | Method of treatment via intra-articular application of potassium |
-
2004
- 2004-01-19 CN CNA2004100139519A patent/CN1557290A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8809393B2 (en) | 2005-02-01 | 2014-08-19 | Troikaa Pharmaceuticals Ltd | Injectable preparations of diclofenac and its pharmaceutically acceptable salts |
| CN101485650B (en) * | 2009-02-19 | 2013-07-17 | 辰欣药业股份有限公司 | Diclofenac sodium and lidocaine hydrochloride injection and preparation method thereof |
| CN105663105A (en) * | 2016-01-15 | 2016-06-15 | 广州一品红制药有限公司 | Diclofenac sodium-lidocaine compound injection |
| CN105663105B (en) * | 2016-01-15 | 2017-03-22 | 广州一品红制药有限公司 | Diclofenac sodium-lidocaine compound injection composite and preparation method thereof |
| US11406612B2 (en) | 2018-02-26 | 2022-08-09 | Rensselaer Polytechnic Institute | Method of treatment via intra-articular application of potassium |
| WO2021009525A1 (en) * | 2019-07-18 | 2021-01-21 | Lovasz Sandor | Medicinal and/or pharmaceutical compositions for intravesical instillation, preparation and use thereof |
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