CN106137984A - A kind of nefopam hydrochloride injection and preparation method thereof - Google Patents
A kind of nefopam hydrochloride injection and preparation method thereof Download PDFInfo
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- CN106137984A CN106137984A CN201610626672.2A CN201610626672A CN106137984A CN 106137984 A CN106137984 A CN 106137984A CN 201610626672 A CN201610626672 A CN 201610626672A CN 106137984 A CN106137984 A CN 106137984A
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- injection
- water
- nefopam hydrochloride
- nefopam
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Dermatology (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of nefopam hydrochloride injection, by following parts by weight acquirement raw material: nefopam hydrochloride 10 50 parts, composite phosphate 0.109 0.75 parts, medicinal charcoal 12 parts, water for injection 1000ml.Advantages of the present invention has: good stability, and safety coefficient is high, and toxic and side effects is little, little by surrounding environment influence.The present invention is widely used in pharmaceuticals industry.
Description
Technical field
The present invention relates to technical field of medicine, particularly to a kind of nefopam hydrochloride injection and preparation method thereof.
Background technology
Nefopam hydrochloride injection (Nefopam Hydrochloride InjECTion), for colourless clear liquid.Main
Want the composition to be: nefopam hydrochloride, chemical name: 5-methyl isophthalic acid-phenyl-3,4,5,6-tetrahydrochysene-1 H-2,5-paroxazine and pungent because of
Hydrochlorate, molecular formula: C17H19NO HCl, molecular weight: 289.80.
Indication: for postoperative analgesia, cancer pain, acute trauma pain, also for acute gastritis, ascariasis of biliary tract, urine output
The visceral smooth muscle angor such as pipe calculus, the anesthesia adjuvant drug such as local anesthesia, needle anaesthesia.Pharmacological toxicology: this product is a kind of novel
Non-narcotic analgesics, has slight antipyretic and Muscle relaxation concurrently.Chemical constitution belongs to cyclisation o-methyl-diphenhydramine.So not
There is the characteristic of NSAID (non-steroidal anti-inflammatory drug), the most non-opioid receptor agonist.Effectively, intramuscular injection this product 20mg is suitable for centering, severe pain
12mg morphine effect.Lighter to respiration inhibition effect.To blood circulation unrestraint effect.Without tolerance and dependency.
Existing nefopam hydrochloride injection technology of preparing, or configuration during there are related substance increase or transport,
, all there is product in production, storage, transportation by environment in relevant grade affected by environment rising etc. problem during storage
Impact, has the problem such as related substance increase, quality instability.It is intended to improve stability and the safety of nefopam hydrochloride injection,
Guarantee the drug safety of patient.
Summary of the invention
It is an object of the invention to provide a kind of good stability, safety coefficient is high, toxic and side effects is little, little by surrounding environment influence
Nefopam hydrochloride injection and preparation method thereof.
Technical scheme is as follows: a kind of nefopam hydrochloride injection, by following parts by weight acquirement raw material: hydrochloric acid
Nefopam 10-50 part, composite phosphate 0.109-0.75 part, medicinal charcoal 1-2 part, water for injection 1000ml.
Further, described composite phosphate is made up of sodium dihydrogen phosphate and disodium hydrogen phosphate, and sodium dihydrogen phosphate: phosphorus
Acid disodium hydrogen is 14.8-15.4.
The preparation method of a kind of nefopam hydrochloride injection, comprises the following steps:
(1) by above-mentioned parts by weight acquirement raw material: nefopam hydrochloride, composite phosphate, medicinal charcoal, water for injection；
(2) take in 2/3 addition preparing tank of water for injection, control water temperature less than 40 DEG C；
(3) in the water for injection that step (2) obtains, it is slowly added to composite phosphate, nitrogen charging in tank, and stir 10 minutes and make
It is completely dissolved；
(4) in the solution of step (3) gained, add nefopam hydrochloride, stir 15 minutes；
(5) regulating step (4) obtains the pH value of solution is 4.9-5.1；
(6) in the solution that step (5) obtains, benefit water for injection, to full dose, adds medicinal charcoal 0.01%, and stirring and adsorbing 15-30 is divided
Clock；
(7) solution step (6) obtained is through twin-stage 0.22 micrometer Millipore filter membrane aseptic filtration, and nitrogen charging embedding, 121 DEG C of sterilizings
15 minutes；
(8) medicinal liquid packaging step (7) obtained, i.e. can get finished product salt acid nefopam injection.
Further, the present invention can make the product of different size, such as: 1ml:20mg, 2ml:20mg, 2ml:50mg,
2ml:100mg etc., preferably specification are 1ml:20mg, 2ml:20mg.
The invention have the advantage that good stability, safety coefficient is high, and toxic and side effects is little, little by surrounding environment influence.
Detailed description of the invention
Content described in this specification embodiment is only the citing of the way of realization to inventive concept, the protection of the present invention
Scope is not construed as being only limitted to the concrete form that embodiment is stated, protection scope of the present invention is also and in art technology
Personnel according to inventive concept it is conceivable that equivalent technologies means.
Embodiment one
A kind of nefopam hydrochloride injection, by following parts by weight acquirement raw material: nefopam hydrochloride 10 parts, composite phosphate
0.109 part, medicinal charcoal 1 part, water for injection 1000ml, wherein, composite phosphate is by sodium dihydrogen phosphate and disodium hydrogen phosphate group
Become, and sodium dihydrogen phosphate: disodium hydrogen phosphate is 14.8.
The preparation method of a kind of nefopam hydrochloride injection, comprises the following steps:
(1) by above-mentioned parts by weight acquirement raw material: nefopam hydrochloride, composite phosphate, medicinal charcoal, water for injection；
(2) take in 2/3 addition preparing tank of water for injection, control water temperature less than 40 DEG C；
(3) in the water for injection that step (2) obtains, it is slowly added to composite phosphate, nitrogen charging in tank, and stir 10 minutes and make
It is completely dissolved；
(4) in the solution of step (3) gained, add nefopam hydrochloride, stir 15 minutes；
(5) regulating step (4) obtains the pH value of solution is 5；
(6) in the solution that step (5) obtains, water for injection is mended to full dose, addition medicinal charcoal 0.01%, stirring and adsorbing 20 minutes；
(7) solution step (6) obtained is through twin-stage 0.22 micrometer Millipore filter membrane aseptic filtration, and nitrogen charging embedding, 121 DEG C of sterilizings
15 minutes；
(8) medicinal liquid packaging step (7) obtained, i.e. can get finished product salt acid nefopam injection.
Preferably specification is 1ml:20mg, 2ml:20mg.
Embodiment two
A kind of nefopam hydrochloride injection, by following parts by weight acquirement raw material: nefopam hydrochloride 30 parts, composite phosphate
0.5 part, medicinal charcoal 2 parts, water for injection 1000ml, wherein, composite phosphate is made up of sodium dihydrogen phosphate and disodium hydrogen phosphate,
And sodium dihydrogen phosphate: disodium hydrogen phosphate is 15.
The preparation method of a kind of nefopam hydrochloride injection, comprises the following steps:
(1) by above-mentioned parts by weight acquirement raw material: nefopam hydrochloride, composite phosphate, medicinal charcoal, water for injection；
(2) take in 2/3 addition preparing tank of water for injection, control water temperature less than 40 DEG C；
(3) in the water for injection that step (2) obtains, it is slowly added to composite phosphate, nitrogen charging in tank, and stir 10 minutes and make
It is completely dissolved；
(4) in the solution of step (3) gained, add nefopam hydrochloride, stir 15 minutes；
(5) regulating step (4) obtains the pH value of solution is 5；
(6) in the solution that step (5) obtains, water for injection is mended to full dose, addition medicinal charcoal 0.01%, stirring and adsorbing 25 minutes；
(7) solution step (6) obtained is through twin-stage 0.22 micrometer Millipore filter membrane aseptic filtration, and nitrogen charging embedding, 121 DEG C of sterilizings
15 minutes；
(8) medicinal liquid packaging step (7) obtained, i.e. can get finished product salt acid nefopam injection.
Preferably specification is 1ml:20mg, 2ml:20mg.
Embodiment three
A kind of nefopam hydrochloride injection, by following parts by weight acquirement raw material: nefopam hydrochloride 50 parts, composite phosphate
0.75 part, medicinal charcoal 2 parts, water for injection 1000ml, wherein, composite phosphate is by sodium dihydrogen phosphate and disodium hydrogen phosphate group
Become, and sodium dihydrogen phosphate: disodium hydrogen phosphate is 15.4.
The preparation method of a kind of nefopam hydrochloride injection, comprises the following steps:
(1) by above-mentioned parts by weight acquirement raw material: nefopam hydrochloride, composite phosphate, medicinal charcoal, water for injection；
(2) take in 2/3 addition preparing tank of water for injection, control water temperature less than 40 DEG C；
(3) in the water for injection that step (2) obtains, it is slowly added to composite phosphate, nitrogen charging in tank, and stir 10 minutes and make
It is completely dissolved；
(4) in the solution of step (3) gained, add nefopam hydrochloride, stir 15 minutes；
(5) regulating step (4) obtains the pH value of solution is 5；
(6) in the solution that step (5) obtains, water for injection is mended to full dose, addition medicinal charcoal 0.01%, stirring and adsorbing 30 minutes；
(7) solution step (6) obtained is through twin-stage 0.22 micrometer Millipore filter membrane aseptic filtration, and nitrogen charging embedding, 121 DEG C of sterilizings
15 minutes；
(8) medicinal liquid packaging step (7) obtained, i.e. can get finished product salt acid nefopam injection.
Preferably specification is 1ml:20mg, 2ml:20mg.
Claims (3)
1. a nefopam hydrochloride injection, by following parts by weight acquirement raw material: nefopam hydrochloride 10-50 part, compound phosphorus
Hydrochlorate 0.109-0.75 part, medicinal charcoal 1-2 part, water for injection 1000ml.
A kind of nefopam hydrochloride injection the most according to claim 1, it is characterised in that: described composite phosphate is by phosphorus
Acid dihydride sodium and disodium hydrogen phosphate composition, and sodium dihydrogen phosphate: disodium hydrogen phosphate is 14.8-15.4.
A kind of nefopam hydrochloride injection the most according to claim 1, it is characterised in that: a kind of nefopam hydrochloride injection
Preparation method, comprise the following steps:
(1) raw material is obtained by weight: nefopam hydrochloride 10-50 part, composite phosphate 0.109-0.75 part, medicinal charcoal 1-
2 parts, water for injection 1000ml；
(2) take in 2/3 addition preparing tank of water for injection, control water temperature less than 40 DEG C；
(3) in the water for injection that step (2) obtains, it is slowly added to composite phosphate, nitrogen charging in tank, and stir 10 minutes and make
It is completely dissolved；
(4) in the solution of step (3) gained, add nefopam hydrochloride, stir 15 minutes；
(5) regulating step (4) obtains the pH value of solution is 4.9-5.1；
(6) in the solution that step (5) obtains, benefit water for injection, to full dose, adds medicinal charcoal 0.01%, and stirring and adsorbing 15-30 is divided
Clock；
(7) solution step (6) obtained is through twin-stage 0.22 micrometer Millipore filter membrane aseptic filtration, and nitrogen charging embedding, 121 DEG C of sterilizings
15 minutes；
(8) medicinal liquid packaging step (7) obtained, i.e. can get finished product salt acid nefopam injection.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610626672.2A CN106137984A (en) | 2016-08-03 | 2016-08-03 | A kind of nefopam hydrochloride injection and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610626672.2A CN106137984A (en) | 2016-08-03 | 2016-08-03 | A kind of nefopam hydrochloride injection and preparation method thereof |
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| CN106137984A true CN106137984A (en) | 2016-11-23 |
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| CN201610626672.2A Pending CN106137984A (en) | 2016-08-03 | 2016-08-03 | A kind of nefopam hydrochloride injection and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3679927A1 (en) * | 2019-01-14 | 2020-07-15 | APTYS Pharmaceuticals SAS | A method of manufacturing a pharmaceutical composition comprising nefopam and acetaminophen, and the pharmaceutical composition obtained thereby |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101125126A (en) * | 2006-08-16 | 2008-02-20 | 丛繁滋 | Method for preparing medical freeze-dried powder (injection) preparation |
| CN102085196A (en) * | 2009-12-08 | 2011-06-08 | 北京科信必成医药科技发展有限公司 | Nefopam hydrochloride bilayer slow-release tablet and preparation method thereof |
| CN102397261A (en) * | 2011-07-20 | 2012-04-04 | 吉林敖东集团大连药业股份有限公司 | Nefopam hydrochloride pharmaceutical composition and preparation method thereof |
-
2016
- 2016-08-03 CN CN201610626672.2A patent/CN106137984A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101125126A (en) * | 2006-08-16 | 2008-02-20 | 丛繁滋 | Method for preparing medical freeze-dried powder (injection) preparation |
| CN102085196A (en) * | 2009-12-08 | 2011-06-08 | 北京科信必成医药科技发展有限公司 | Nefopam hydrochloride bilayer slow-release tablet and preparation method thereof |
| CN102397261A (en) * | 2011-07-20 | 2012-04-04 | 吉林敖东集团大连药业股份有限公司 | Nefopam hydrochloride pharmaceutical composition and preparation method thereof |
Non-Patent Citations (3)
| Title |
|---|
| 国家药典委员会编: "《中华人民共和国药典2010年版二部》", 31 January 2010, 中国医药科技出版社 * |
| 百度文库: "注射用药用辅料", 《百度文库HTTPS://WENKU.BAIDU.COM/VIEW/AB14AF0590C69EC3D5BB75AC.HTML?FROM=SEARCH》 * |
| 郭慧玲等主编: "《药剂学》", 28 February 2014, 中山大学出版社 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3679927A1 (en) * | 2019-01-14 | 2020-07-15 | APTYS Pharmaceuticals SAS | A method of manufacturing a pharmaceutical composition comprising nefopam and acetaminophen, and the pharmaceutical composition obtained thereby |
| WO2020148219A1 (en) * | 2019-01-14 | 2020-07-23 | Aptys Pharmaceuticals Sas | A method of manufacturing a pharmaceutical composition comprising nefopam and acetaminophen, and the pharmaceutical composition obtained thereby |
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Application publication date: 20161123 |