CN102258485A - Acetaminophen-contained preparation for injection and applications thereof - Google Patents
Acetaminophen-contained preparation for injection and applications thereof Download PDFInfo
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- CN102258485A CN102258485A CN2011100045475A CN201110004547A CN102258485A CN 102258485 A CN102258485 A CN 102258485A CN 2011100045475 A CN2011100045475 A CN 2011100045475A CN 201110004547 A CN201110004547 A CN 201110004547A CN 102258485 A CN102258485 A CN 102258485A
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Abstract
The invention relates to an acetaminophen-contained preparation for injection and applications thereof. The preparation is a composition for injection, which is prepared by taking acetaminophen as an active medicinal ingredient, and pharmaceutically-acceptable adjuvant. The dosage form comprises a powder injection, large-capacity injection (more than 50ml) and small-capacity injection (below 20ml). The preparation for injection is prepared and developed by taking the acetaminophen as a raw material, adding certain adjuvant with specific type and proportion, and adopting the technical means described in the invention. The preparation for injection is mainly applied in stopping pains and eliminating the fever clinically.
Description
Technical field
The present invention relates to a kind of injection preparation and application thereof that contains acetaminophen, comprise injectable powder, bulk capacity injection (more than the 50ml), small-volume injection (20ml is following).Belong to medical technical field.
Background technology
Pain is human subjective inner sense that the earliest can perception, also is human problem of the most often meeting.But because people are more unilateral to the understanding of pain for a long time, think that pain is the symptom of disease, as long as disease is cured, pain will disappear, so also have numerous patients standing the torment of pain so far.Chronic pain has caused global great attention as a kind of disease, and world's pain conference is confirmed as " human the 5th big vital signs " after breathing, pulse, body temperature and blood pressure with pain.A lot of pathological pains itself are exactly a kind of disease that has a strong impact on patients ' life quality and work quality, people recognize the importance of pain gradually, World Health Organization (WHO) just proposed " chronic pain is a class disease " in 2000, IASP decision is since 2004, will be decided to be " Global day against pain " on October 11 in every year.
Show have 35% people to suffer from chronic pain the America and Europe according to authoritative statistical data, and that China contrasts this numeral is only high not low: the torment that every day, about 5,500,000 people bore the pain in the world, about 57% people lives through headache in various degree among the Chinese city resident.The acute pain that diseases such as some fracture, wound, burn, cancer cause has a strong impact on (comprising sharp pain and angor) the universality difficult problem of patient's life quality especially.
Medical science is paid attention to patient's quality of life more at present, and various diseases is caused that treatment of pain has also expedited the emergence of new analgesic market.According to the prediction of the international consulting firm of IMS, 2005, the global analgesic total market size reached more than 80,000,000,000 dollars.At present, the U.S., Europe and Japan are maximum analgesic market, the whole world, the past over 30 years the analgesic sales volume be in the state that grows steadily always.
China is the consumption big country of analgesic drug product, and dosage is in rising trend every year, also is the big producing country of analgesic drug product simultaneously, and at present, China has become the antipyretic analgesic production and the big export country of Asia maximum, the second in the world.But product is based on acetaminophen, aspirin and dipyrone, and the technological element of a product is not high, and added value is very low, compares with external major company, and the antipyretic analgesic of China still is difficult to it competition mutually in the research and development innovation ability with aspect fresh water (FW) equality is many.
Its chemistry of acetyl aminophenol (Paracetamol) N-(4 hydroxy phenyl) acetamide by name.Be acetophenone amine antipyretic analgesic. by suppressing Cycloxygenase, selectivity suppresses the synthetic of hypothalamus thermotaxic centre prostaglandin, cause peripheral blood vessel expansion, perspire and reach the antipyretic effect, its refrigeration function intensity is similar to aspirin: by suppressing the synthetic of prostaglandin etc. and discharging, improve the pain fault and play analgesic activity, belong to the periphery analgesic, the effect than a little less than the aspirin, only to light, moderate pain is effective.
Summary of the invention
The present invention for a kind of be the injection preparation of active component with the acetaminophen, contain active component acetaminophen and pharmaceutically acceptable pharmaceutic adjuvant.Its dosage form comprises injectable powder, bulk capacity injection (more than the 50ml), small-volume injection (20ml is following).
Described injectable powder, its acetaminophen specification is 500-5000mg, is preferably 1000mg; Bulk capacity injection (more than the 50ml) acetaminophen specification is 0.5%-2%, is preferably 1%; Small-volume injection (20ml is following) specification is 0.5%-10%, is preferably 1%.。
Described pharmaceutically acceptable pharmaceutic adjuvant comprises one or more in pharmaceutical carrier, isoosmotic adjusting agent, pH regulator agent, the antioxidant.
Described isoosmotic adjusting agent can be a sodium chloride, one or more in glucose, glycerol, propylene glycol, mannitol, glucose, sorbitol, dextran, nicotiamide, citric acid, citrate, pantothenic acid and salt thereof, agedoite, aminoacid and the amino acid salts.
Described antioxidant can be sulfurous acid, sulphite, bisulfites, pyrosulfite, thiosulfate, thioglycerol, gallic acid and cysteine hydrochloride, ascorbic acid and salt thereof, thiourea, methionine, one or more in the thiacetic acid..
The preparation technology of lyophilized powder adds the acetaminophen stirring and dissolving for getting part water for injection in the described injectable powder, adds an amount of pharmaceutical carrier, antioxidant and chelating agen, with pH regulator agent adjust pH, add an amount of needle-use activated carbon, medicinal liquid is heated to 50 ℃-70 ℃, stir, behind the filtering decarbonization, add the injection water to total amount, adopt 0.22 μ m microporous filter membrane fine straining again, fill is in glass tube vial, cillin bottle is placed in the freezer dryer lyophilization.
Described bulk capacity injection (more than the 50ml), small-volume injection (20ml is following) preparation technology are for getting part water for injection, add the acetaminophen stirring and dissolving, add an amount of antioxidant and chelating agen, with pH regulator agent adjust pH, add an amount of needle-use activated carbon, medicinal liquid is heated to 50 ℃-70 ℃, stirs, behind the filtering decarbonization, add the injection water to total amount, adopt 0.22 μ m microporous filter membrane fine straining again, fill is in bottle, and sterilization gets final product.
This ejection preparation is mainly used in clinically brings down a fever and various treatment of pain.
The specific embodiment
Come the present invention done further specifying by following example, comprise but be not restricted to following example.
Embodiment 1 acetaminophen freeze-dried powder
Prescription:
Preparation method:
Get water for injection 80L, the acetaminophen stirring and dissolving that adds recipe quantity, the mannitol of adding recipe quantity, cysteine, sodium hydrogen phosphate, with sodium hydroxide solution adjust pH 5.5-6.5, add an amount of needle-use activated carbon by amount of preparation, medicinal liquid is heated to about 50 ℃-60 ℃, stir 20min, behind the filtering decarbonization, add the injection water to total amount, intermediate detects.After the intermediate detection is qualified, adopt 0.22 μ m microporous filter membrane fine straining again, fill places cillin bottle in the freezer dryer lyophilization in cillin bottle.
The lyophilization condition is :-40 ℃ of pre-freezes 4 hours, and the phase I is warming up to-10 ℃, 3 hours time, vacuum drying 22 hours, second stage heats up in 1 hour from-10 ℃～30 ℃, and is incubated 4 hours.
After the lyophilization, press rubber stopper, roll aluminium-plastic cap.
The lyophilization curve is seen accompanying drawing 1
Embodiment 2: the acetaminophen liquid drugs injection
Prescription:
Preparation method:
Get water for injection 80L, add the acetaminophen stirring and dissolving, add the mannitol of recipe quantity, cysteine, sodium hydrogen phosphate, stirring and dissolving, regulating pH value with sodium hydroxide solution is 5.5, add an amount of needle-use activated carbon, medicinal liquid is heated to about 50 ℃-60 ℃, stirs 20min, behind the filtering decarbonization, add the injection water to total amount, intermediate detects.After the intermediate detection is qualified, adopt 0.22 μ m microporous filter membrane fine straining again, fill is in ampoule bottle, and every bottle of 100ml seals, and moist heat sterilization gets final product.
Embodiment 3: the acetaminophen primary infusion
Prescription: every bottle of prescription
Preparation method:
Get water for injection 80L, add the acetaminophen stirring and dissolving, add the mannitol of recipe quantity, cysteine, the sodium hydrogen phosphate stirring and dissolving, regulating pH value with sodium hydroxide solution is 5.5-6.5, adds an amount of needle-use activated carbon, and medicinal liquid is heated to about 50 ℃-60 ℃, stir 20min, behind the filtering decarbonization, add the injection water to total amount, intermediate detects.After the intermediate detection is qualified, adopt 0.22 μ m microporous filter membrane fine straining again, fill is in infusion bottle, and every bottle of 250ml seals, and moist heat sterilization gets final product.
Embodiment 4 acetaminophen freeze-dried powders
Prescription:
Preparation method:
Get water for injection 80L, the acetaminophen stirring and dissolving that adds recipe quantity, the mannitol of adding recipe quantity, cysteine, sodium hydrogen phosphate, with sodium hydroxide solution adjust pH 5.5-6.5, add an amount of needle-use activated carbon by amount of preparation, medicinal liquid is heated to about 50 ℃-60 ℃, stir 20min, behind the filtering decarbonization, add the injection water to total amount, intermediate detects.After the intermediate detection is qualified, adopt 0.22 μ m microporous filter membrane fine straining again, fill places cillin bottle in the freezer dryer lyophilization in cillin bottle.
The lyophilization condition is :-40 ℃ of pre-freezes 4 hours, and the phase I is warming up to-10 ℃, 3 hours time, vacuum drying 22 hours, second stage heats up in 1 hour from-10 ℃～30 ℃, and is incubated 4 hours.
After the lyophilization, press rubber stopper, roll aluminium-plastic cap.
The lyophilization curve is seen accompanying drawing 1
Embodiment 5: the acetaminophen liquid drugs injection
Prescription:
Preparation method:
Get water for injection 80L, add the acetaminophen stirring and dissolving, add the mannitol of recipe quantity, cysteine, sodium hydrogen phosphate, stirring and dissolving, regulating pH value with sodium hydroxide solution is 5.5, add an amount of needle-use activated carbon, medicinal liquid is heated to about 50 ℃-60 ℃, stirs 20min, behind the filtering decarbonization, add the injection water to total amount, intermediate detects.After the intermediate detection is qualified, adopt 0.22 μ m microporous filter membrane fine straining again, fill is in ampoule bottle, and every bottle of 100ml seals, and moist heat sterilization gets final product.
Embodiment 6: the acetaminophen primary infusion
Prescription: every bottle of prescription
Preparation method:
Get water for injection 80L, add the acetaminophen stirring and dissolving, add the mannitol of recipe quantity, cysteine, the sodium hydrogen phosphate stirring and dissolving, regulating pH value with sodium hydroxide solution is 5.5-6.5, adds an amount of needle-use activated carbon, and medicinal liquid is heated to about 50 ℃-60 ℃, stir 20min, behind the filtering decarbonization, add the injection water to total amount, intermediate detects.After the intermediate detection is qualified, adopt 0.22 μ m microporous filter membrane fine straining again, fill is in infusion bottle, and every bottle of 250ml seals, and moist heat sterilization gets final product.
Embodiment 7
Pharmacological evaluation 1: analgesic activity
Get 30 of kunming mices, male and female half and half, body weight 18-22g.Be divided into 3 groups at random, be respectively blank group, diclofenac group, the acetaminophen group, 10 mices of each dosage group are packed mice in the cage into, and the Mus tail places on the heat radiation whipping instrument, the light beam direct projection is in Mus tail 1/3 place, reaction appears in mice behind about 3s, and promptly whipping or turn around causes that with radiant heat whipping reaction required time is the threshold of pain.At first measure the basic threshold of pain of each group.Respectively to mouse subcutaneous injection be subjected to examination give positive drug, measure the mice threshold of pain behind the 30min thereafter.The result shows, with respect to matched group, and all the improve analgesic activity of the threshold of pain of each treatment group, wherein the acetaminophen group is better than diclofenac drug administration by injection effect.Illustrate that injection gives acetaminophen and has analgesic activity preferably, the results are shown in Table 1
Table 1 is respectively organized the threshold of pain, mice administration front and back situation of change
Embodiment 8:
Pharmacological evaluation 2: refrigeration function
Get some of sD rats, body weight (150 ± 20) g.Choose 30 of the rat of body temperature in 36.6 ℃～38.3 ℃, male and female half and half are divided into 3 groups at random, 10 every group, are respectively blank group, diclofenac group, the acetaminophen group.1 subcutaneous injection administration in 1 day, continuous 3d, fasting 12h before experiment, freely drink water, the same day was surveyed body temperature 2 times in experiment, every 2h 1 time, after the last administration at once in rat back subcutaneous injection dry yeast (15%) suspension 10mL/kg, then in 2,6,10h measures anus temperature value, comparison between organizing.The result shows that with respect to matched group, each treatment group all has certain refrigeration function, and wherein the acetaminophen group is better than diclofenac drug administration by injection effect.Illustrate that injection gives acetaminophen and has the better antipyretic effect.The results are shown in Table 2
Table 2 pair dry yeast causes the influence of rat fever
Claims (9)
1. one kind is the injection preparation of active component with the acetaminophen, it is characterized in that containing active component acetaminophen and pharmaceutically acceptable pharmaceutic adjuvant.
2. according to the described injection preparation of claim 1, its dosage form comprises injectable powder, bulk capacity injection (more than the 50ml), small-volume injection (20ml is following).
3. injectable powder according to claim 2, its acetaminophen specification is 500-5000mg, is preferably 1000mg; Bulk capacity injection (more than the 50ml) acetaminophen specification is 0.5%-2%, is preferably 1%; Small-volume injection (20ml is following) specification is 0.5%-10%, is preferably 1%.
4. injectable powder according to claim 2, bulk capacity injection (more than the 50ml), small-volume injection (20ml is following) is characterized in that described pharmaceutically acceptable pharmaceutic adjuvant comprises one or more in pharmaceutical carrier, isoosmotic adjusting agent, pH regulator agent, the antioxidant.
5. preparation according to claim 4, it is characterized in that, described isoosmotic adjusting agent can be a sodium chloride, one or more in glucose, glycerol, propylene glycol, mannitol, glucose, sorbitol, dextran, nicotiamide, citric acid, citrate, pantothenic acid and salt thereof, agedoite, aminoacid and the amino acid salts.
6. preparation according to claim 4, it is characterized in that, described antioxidant can be sulfurous acid, sulphite, bisulfites, pyrosulfite, thiosulfate, thioglycerol, gallic acid and cysteine hydrochloride, ascorbic acid and salt thereof, thiourea, methionine, one or more in the thiacetic acid..
7. injectable powder preparation according to claim 2, it is characterized in that, the preparation technology of lyophilized powder is for getting part water for injection in the described injectable powder, add the acetaminophen stirring and dissolving, add an amount of pharmaceutical carrier, antioxidant and chelating agen, with pH regulator agent adjust pH, add an amount of needle-use activated carbon, medicinal liquid is heated to 50 ℃-70 ℃, stir, behind the filtering decarbonization, add the injection water to total amount, adopt 0.22 μ m microporous filter membrane fine straining again, fill is in glass tube vial, cillin bottle is placed in the freezer dryer lyophilization.
8. preparation according to claim 2, it is characterized in that, described bulk capacity injection (more than the 50ml), small-volume injection (20ml is following) preparation technology are for getting part water for injection, add the acetaminophen stirring and dissolving, add an amount of antioxidant and chelating agen, with pH regulator agent adjust pH, add an amount of needle-use activated carbon, medicinal liquid is heated to 50 ℃-70 ℃, stirs, behind the filtering decarbonization, add the injection water to total amount, adopt 0.22 μ m microporous filter membrane fine straining again, fill is in bottle, and sterilization gets final product.
9. preparation according to claim 2 is characterized in that, this ejection preparation is mainly used in clinically brings down a fever and various treatment of pain.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011100045475A CN102258485A (en) | 2011-01-11 | 2011-01-11 | Acetaminophen-contained preparation for injection and applications thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN2011100045475A CN102258485A (en) | 2011-01-11 | 2011-01-11 | Acetaminophen-contained preparation for injection and applications thereof |
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| CN102258485A true CN102258485A (en) | 2011-11-30 |
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| CN2011100045475A Pending CN102258485A (en) | 2011-01-11 | 2011-01-11 | Acetaminophen-contained preparation for injection and applications thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107205924A (en) * | 2014-12-20 | 2017-09-26 | 特罗伊卡药品有限公司 | The injectable formulation of paracetamol |
| CN107616965A (en) * | 2017-09-27 | 2018-01-23 | 四川科伦药业股份有限公司 | Paracetamol high-capacity injection and preparation method thereof |
| CN116172945A (en) * | 2022-07-26 | 2023-05-30 | 华润三九（南昌）药业有限公司 | A kind of preparation method of acetaminophen oral solution |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1311672A (en) * | 1998-07-31 | 2001-09-05 | 方济各安吉利克化学联合股份有限公司 | Pharmaceutical composition for injection based on paracetamol |
| CN1548038A (en) * | 2003-05-22 | 2004-11-24 | 孙明杰 | New acetaminophen prepn |
| CN101366695A (en) * | 2008-10-16 | 2009-02-18 | 江苏四环生物股份有限公司 | Tylenol injection and preparation method thereof |
-
2011
- 2011-01-11 CN CN2011100045475A patent/CN102258485A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1311672A (en) * | 1998-07-31 | 2001-09-05 | 方济各安吉利克化学联合股份有限公司 | Pharmaceutical composition for injection based on paracetamol |
| CN1548038A (en) * | 2003-05-22 | 2004-11-24 | 孙明杰 | New acetaminophen prepn |
| CN101366695A (en) * | 2008-10-16 | 2009-02-18 | 江苏四环生物股份有限公司 | Tylenol injection and preparation method thereof |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107205924A (en) * | 2014-12-20 | 2017-09-26 | 特罗伊卡药品有限公司 | The injectable formulation of paracetamol |
| CN107616965A (en) * | 2017-09-27 | 2018-01-23 | 四川科伦药业股份有限公司 | Paracetamol high-capacity injection and preparation method thereof |
| CN116172945A (en) * | 2022-07-26 | 2023-05-30 | 华润三九（南昌）药业有限公司 | A kind of preparation method of acetaminophen oral solution |
| CN116172945B (en) * | 2022-07-26 | 2025-02-14 | 华润三九（南昌）药业有限公司 | A preparation method of acetaminophen oral solution |
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Application publication date: 20111130 |