CN106109402A - A kind of levetiracetam injection - Google Patents
A kind of levetiracetam injection Download PDFInfo
- Publication number
- CN106109402A CN106109402A CN201610568954.1A CN201610568954A CN106109402A CN 106109402 A CN106109402 A CN 106109402A CN 201610568954 A CN201610568954 A CN 201610568954A CN 106109402 A CN106109402 A CN 106109402A
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- CN
- China
- Prior art keywords
- levetiracetam
- injection
- tartaric acid
- mixture
- alkaline matter
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
-
- 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
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- 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
-
- 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
Abstract
The present invention relates to a kind of levetiracetam injection, described levetiracetam injection is mainly made up of the component of following weight portion: levetiracetam 40 60 parts, acidic materials 0.5 0.7 parts, alkaline matter 0.5 0.7 parts, 0.3 0.5 parts of buffer solution and osmotic pressure regulator 0.1 0.3 parts；Wherein, acidic materials are D tartaric acid and the tartaric mixture of L, and D tartaric acid with and the tartaric mass ratio of L be 1:2.1 2.5；Alkaline matter is the mixture of sodium hydroxide and potassium hydroxide, and the mass ratio of sodium hydroxide and potassium hydroxide is 1:1.3 1.7.It is an advantage of the current invention that: the present invention, by adding mixture and the alkaline matter mixture of acidic materials in injection, can increase substantially levetiracetam stability in water；The sample of preparation is after pressure sterilizing, sterilizing, and levetiracetam acid, without substantially increasing, adds the safety of use.
Description
Technical field
The invention belongs to pharmaceutical technology field, relate to a kind of new medicine comprising levetiracetam
Compositions, particularly to a kind of levetiracetam injection.
Background technology
Levetiracetam is the LEV in piracetam derivant, and its chemical name is (S)-a-second
Base-2-oxo-1-pyrrolidine ethanamide, molecular formula C8H14N2O2, relative molecular mass is 170.21.
Levetiracetam is a kind of new antiepileptic medicine of UCB. S.A. (BE) Bruxelles Belgium of Belgium research and development, exists through FDA approval in 1999
The U.S. lists, and is mainly used in treating limitation and Secondary cases generalized epileptic, be current U.S. epilepsy therapy is applied most new
Type antiepileptic.Levetiracetam is compared with other antiepileptics, and epilepsy medicine machine-processed, the preferable generation with uniqueness is dynamic
Mechanical characteristics, has preferable curative effect, and has preferable safety and toleration Adult Refractory partial epilepsy.
The levetiracetam dosage form listed at present has tablet, oral liquid, because tablet and oral liquid are by gastrointestinal tract,
Dissolution rate is slow, and bioavailability is low, should not take for child and coma patient.Injection drug effect is rapid, and intravenous is directly entered
Entering blood circulation, the injection the most relatively gastrointestinal absorption such as Intradermal subdermal muscle is quick, is suitable to the medicine that should not be administered orally and can not mouth
The patient that clothes are administered.
Through retrieval, China Patent No. 200810116329.9 discloses a kind of levetiracetam injection formula, including: left
Etiracetam 10%, sodium chloride 0.9%, glacial acetic acid 0.5%, sodium hydroxide 0.7%, water for injection 87.9%, use the injection of routine
Configuration technique is prepared.
Also finding through retrieval, China Patent No. 2012100168292.4 discloses the levetiracetam of such as formula as below
Injection: levetiracetam 100g, sodium chloride 9g, sodium acetate 1.6g, acetic acid 0.2g, water for injection add to 1000ml, often uses
The injection configuration technique of rule is prepared.But above-mentioned injection all exists compositions to be not sufficiently stable, it is impossible to meet terminal sterilization
Technique.
Therefore, research and develop a kind of steady quality and disclosure satisfy that the levetiracetam injection of terminal sterilization technique is to have very much
Necessary.
Summary of the invention
The technical problem to be solved in the present invention is to provide a kind of steady quality and disclosure satisfy that the left second of terminal sterilization technique
La Xitan injection.
For solving above-mentioned technical problem, the technical scheme is that a kind of levetiracetam injection, its innovative point exists
In: described levetiracetam injection is mainly made up of the component of following weight portion: levetiracetam 40-60 part, acidic materials
0.5-0.7 part, alkaline matter 0.5-0.7 part, buffer solution 0.3-0.5 part and osmotic pressure regulator 0.1-0.3 part；Wherein, acid
Property material be the mixture of D-tartaric acid and L-TARTARIC ACID, and D-tartaric acid with and the mass ratio of L-TARTARIC ACID be 1:2.1-2.5；
Alkaline matter is the mixture of sodium hydroxide and potassium hydroxide, and the mass ratio of sodium hydroxide and potassium hydroxide is 1:1.3-1.7.
Further, described buffer solution is disodium hydrogen phosphate-sodium chloride.
Further, described osmotic pressure regulator is glucose.
Further, the concentration of described levetiracetam is 9-11%(w/v).
Further, the concentration of described acidic materials is 30-40mmol/L.
Further, the concentration of described alkaline matter is 30-40mmol/L.
It is an advantage of the current invention that: the present invention is mixed by the mixture and alkaline matter adding acidic materials in injection
Compound, can increase substantially levetiracetam stability in water；Preparation sample after pressure sterilizing, sterilizing, Zuo Yila
Western smooth acid, without substantially increasing, adds the safety of use.
Detailed description of the invention
The following examples can make professional and technical personnel that the present invention is more fully understood, but the most therefore by this
Bright it is limited among described scope of embodiments.
Embodiment 1
Weigh the water for injection about 400g of less than 30 degrees Celsius, add the disodium hydrogen phosphate-sodium chloride of 0.3g, the hydrogen-oxygen of 0.23g
After changing the potassium hydroxide of sodium and 0.47g, stirring and dissolving is complete；The levetiracetam crude drug of 60g is added in above-mentioned solution, stirs
Mix solution, be 5-6 by the D-tartaric acid of 0.3g and the L-TARTARIC ACID regulation solution ph of 0.4g；Add the glucose regulation of 0.3g
Osmotic pressure, and mend inject water to 500ml；Through the improvement PVDF membrane filtration of 22 m, fill after filtration, 121 degrees Celsius
15min sterilizing, obtains levetiracetam injection.
Embodiment 2
Weigh the water for injection about 400g of less than 30 degrees Celsius, add the disodium hydrogen phosphate-sodium chloride of 0.3g, the hydroxide of 0.2g
After the potassium hydroxide of sodium and 0.5g, stirring and dissolving is complete；The levetiracetam crude drug of 60g is added in above-mentioned solution, stirs molten
Liquid, is 5-6 by the D-tartaric acid of 0.26g and the L-TARTARIC ACID regulation solution ph of 0.44g；The glucose regulation adding 0.3g is oozed
Thoroughly press, and benefit injects water to 500ml；Through the improvement PVDF membrane filtration of 22 m, fill after filtration, 121 degrees Celsius of 15min
Sterilizing, obtains levetiracetam injection.
Embodiment 3
Weigh the water for injection about 400g of less than 30 degrees Celsius, add the disodium hydrogen phosphate-sodium chloride of 0.3g, the hydrogen-oxygen of 0.21g
After changing the potassium hydroxide of sodium and 0.49g, stirring and dissolving is complete；The levetiracetam crude drug of 60g is added in above-mentioned solution, stirs
Mix solution, be 5-6 by the D-tartaric acid of 0.28g and the L-TARTARIC ACID regulation solution ph of 0.42g；The glucose adding 0.3g is adjusted
Save osmotic pressure, and benefit injects water to 500ml；Through the improvement PVDF membrane filtration of 22 m, fill after filtration, 121 degrees Celsius
15min sterilizing, obtains levetiracetam injection.
Embodiment 4
Weigh the water for injection about 400g of less than 30 degrees Celsius, add the disodium hydrogen phosphate-sodium chloride of 0.5g, the hydrogen-oxygen of 0.15g
After changing the potassium hydroxide of sodium and 0.35g, stirring and dissolving is complete；The levetiracetam crude drug of 40g is added in above-mentioned solution, stirs
Mix solution, be 5-6 by the D-tartaric acid of 0.2g and the L-TARTARIC ACID regulation solution ph of 0.3g；Add the glucose regulation of 0.1g
Osmotic pressure, and mend inject water to 500ml；Through the improvement PVDF membrane filtration of 22 m, fill after filtration, 121 degrees Celsius
15min sterilizing, obtains levetiracetam injection.
Embodiment 5
Weigh the water for injection about 400g of less than 30 degrees Celsius, add the disodium hydrogen phosphate-sodium chloride of 0.4g, the hydrogen-oxygen of 0.18g
After changing the potassium hydroxide of sodium and 0.42g, stirring and dissolving is complete；The levetiracetam crude drug of 50g is added in above-mentioned solution, stirs
Mix solution, be 5-6 by the D-tartaric acid of 0.24g and the L-TARTARIC ACID regulation solution ph of 0.36g；The glucose adding 0.2g is adjusted
Save osmotic pressure, and benefit injects water to 500ml；Through the improvement PVDF membrane filtration of 22 m, fill after filtration, 121 degrees Celsius
15min sterilizing, obtains levetiracetam injection.
The sample of embodiment 1-5 is placed under high temperature and illumination condition, uses high-efficient liquid phase technique detection to have related substance, result
It is shown in Table 1 and table 2.
Table 1: have related substance to detect under high temperature 60 degrees celsius
Table 2: have related substance to detect under illumination condition
Conclusion: in group involved in this test, sample, under high temperature and illumination condition, is investigated character, is had related substance, pH
Value, result table name embodiment 5 sample solution is the most stable.
The ultimate principle of the present invention and principal character and advantages of the present invention have more than been shown and described.The skill of the industry
The art personnel simply explanation it should be appreciated that the present invention is not restricted to the described embodiments, described in above-described embodiment and description
The principle of the present invention, without departing from the spirit and scope of the present invention, the present invention also has various changes and modifications, these
Changes and improvements both fall within scope of the claimed invention.Claimed scope by appending claims and
Its equivalent defines.
Claims (6)
1. a levetiracetam injection, it is characterised in that: described levetiracetam injection is mainly by following weight portion
Component forms: levetiracetam 40-60 part, acidic materials 0.5-0.7 part, alkaline matter 0.5-0.7 part, buffer solution 0.3-
0.5 part and osmotic pressure regulator 0.1-0.3 part；Wherein, acidic materials are the mixture of D-tartaric acid and L-TARTARIC ACID, and D-wine
Stone acid with and the mass ratio of L-TARTARIC ACID be 1:2.1-2.5；Alkaline matter is the mixture of sodium hydroxide and potassium hydroxide, and hydrogen
Sodium oxide is 1:1.3-1.7 with the mass ratio of potassium hydroxide.
Levetiracetam injection the most according to claim 1, it is characterised in that: described buffer solution is phosphoric acid hydrogen two
Sodium-sodium chloride.
Levetiracetam injection the most according to claim 1, it is characterised in that: described osmotic pressure regulator is Fructus Vitis viniferae
Sugar.
Levetiracetam injection the most according to claim 1, it is characterised in that: the concentration of described levetiracetam is 9-
11%(w/v).
Levetiracetam injection the most according to claim 1, it is characterised in that: the concentration of described acidic materials is 30-
40mmol/L。
Levetiracetam injection the most according to claim 1, it is characterised in that: the concentration of described alkaline matter is 30-
40mmol/L。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610568954.1A CN106109402A (en) | 2016-07-20 | 2016-07-20 | A kind of levetiracetam injection |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610568954.1A CN106109402A (en) | 2016-07-20 | 2016-07-20 | A kind of levetiracetam injection |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106109402A true CN106109402A (en) | 2016-11-16 |
Family
ID=57289925
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610568954.1A Pending CN106109402A (en) | 2016-07-20 | 2016-07-20 | A kind of levetiracetam injection |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106109402A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107115293A (en) * | 2017-05-19 | 2017-09-01 | 万特制药(海南)有限公司 | A kind of injection containing levetiracetam medicinal composition and preparation method thereof |
| CN107213114A (en) * | 2017-05-19 | 2017-09-29 | 万特制药(海南)有限公司 | A kind of injection containing levetiracetam medicinal composition and preparation method thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101919811A (en) * | 2009-06-09 | 2010-12-22 | 北京博时安泰液体制剂科技有限公司 | Levetiracetam injection and preparation method thereof |
| CN103462886A (en) * | 2013-09-13 | 2013-12-25 | 四川鼎诺泰宸科技有限公司 | Stable levetiracetam injection |
| CN103550143A (en) * | 2013-10-19 | 2014-02-05 | 浙江华海药业股份有限公司 | Preparation method of levetiracetam injection |
| WO2014078568A1 (en) * | 2012-11-14 | 2014-05-22 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
| EP2878296A1 (en) * | 2013-11-29 | 2015-06-03 | UCB Pharma GmbH | Pharmaceutical composition comprising lacosamide and levetiracetam |
-
2016
- 2016-07-20 CN CN201610568954.1A patent/CN106109402A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101919811A (en) * | 2009-06-09 | 2010-12-22 | 北京博时安泰液体制剂科技有限公司 | Levetiracetam injection and preparation method thereof |
| WO2014078568A1 (en) * | 2012-11-14 | 2014-05-22 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
| CN103462886A (en) * | 2013-09-13 | 2013-12-25 | 四川鼎诺泰宸科技有限公司 | Stable levetiracetam injection |
| CN103550143A (en) * | 2013-10-19 | 2014-02-05 | 浙江华海药业股份有限公司 | Preparation method of levetiracetam injection |
| EP2878296A1 (en) * | 2013-11-29 | 2015-06-03 | UCB Pharma GmbH | Pharmaceutical composition comprising lacosamide and levetiracetam |
Non-Patent Citations (1)
| Title |
|---|
| 孟胜男主编: "《药剂学》", 31 January 2012 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107115293A (en) * | 2017-05-19 | 2017-09-01 | 万特制药(海南)有限公司 | A kind of injection containing levetiracetam medicinal composition and preparation method thereof |
| CN107213114A (en) * | 2017-05-19 | 2017-09-29 | 万特制药(海南)有限公司 | A kind of injection containing levetiracetam medicinal composition and preparation method thereof |
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| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
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| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20161116 |
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| RJ01 | Rejection of invention patent application after publication |