CN104027301B - Oxiracetam composition injection - Google Patents
Oxiracetam composition injection Download PDFInfo
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- CN104027301B CN104027301B CN201310068438.9A CN201310068438A CN104027301B CN 104027301 B CN104027301 B CN 104027301B CN 201310068438 A CN201310068438 A CN 201310068438A CN 104027301 B CN104027301 B CN 104027301B
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- injection
- oxiracetam
- ammonium chloride
- activated carbon
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Abstract
The invention relates to an oxiracetam composition injection, comprising oxiracetam, ammonium chloride and injection water. The oxiracetam composition injection is characterized in that the injection contains ammonium chloride, each 1000 ml of the injection contains 200 g of oxiracetam and 0.5 to 50 g of ammonium chloride, and the pH value of the injection is adjusted to 4.6 to 5.5. The injection has better stability compared with conventional injections.
Description
Technical field
The present invention relates to a kind of injection solution of oxiracetam composition, including oxiracetam, ammonium chloride and water for injection, it is special
Levying is：Containing ammonium chloride, wherein containing oxiracetam 200mg, 0.5～50mg of ammonium chloride per 1ml injection, it is characterised in that note
The pH regulator of liquid is penetrated to 4.6～5.5.The stability of this injection is more preferable than existing injection stability.
Background technology
Oxiracetam is synthesized first most earlier than 1974 by Italy, is that Italian ISFS.P.A companies develop, 1987
, in Italian Initial Public Offering, trade name Neupan, there are peroral dosage form and injection type in December.Oxiracetam is a kind of new
The derivant of γ-aminobutyric acid (GABA).Its chemical name Esomeprazole, structural formula：
Molecular formula：C6H10N2O3；Molecular weight：158.16；
Oxiracetam is the cancellated Cholinergic activity nootropics of the maincenter that acts on, and can pass through blood brain barrier, stimulates special
Sexual centre nervous pathway, can improve thinking, memory and school grade, reduce the memory injury caused by shock；Antagonism is primary
Property hypertensive cerebral blood vessel injury rat learning capacity reduction, improve the operating of rat cortex and Hippocampus part acetylcholine, increase
Plus the affinity to Choline uptake.Phosphorylcholine and phosphatidyl ethanolamine synthesis can be promoted, cerebral cortex function is optionally activated,
Improve cerebrum metabolism, EEG after anoxia can be promoted to recover, activate adenylic acid kinase, increase ATP synthesis and energy storage,
ATP conversions and RNA synthesis are improved, and has anti-platelet aggregation to act on.
Oxiracetam is clinically used to treat the brain injury that various chemical factors cause, various cerebral anoxiies and chronic brain function
It is not congruent.To dull-witted, shock, old mental deterioration syndrome (such as hypomnesis, adaptability reduction, old weak and spirit
Sexual activity obstacle etc.), the brain development of feeble-minded children and the memory of normal person, the raising of work efficiency have a constant current modulation
Effect.Clinical usage and dosage is：Intravenous injection, 2～4g every time, one time a day；Intravenous drip, 4～8g every time, one time a day (uses
0.9% sodium chloride injection is diluted to 100ml～200ml), can take the circumstances into consideration to subtract consumption, shake up.Treatment to afunction is generally treated
Journey is 2 weeks, is 3 weeks to memory and the usual course for the treatment of of the treatment of disturbance of intelligence.
Domestic capsule listing (trade name Ou Laining) in 2 months 1997 approval Shijiazhuang pharmacy group Ou Yi Pharmaceuticaies,
Subsequently the said firm develops its injection again.The domestic oxiracetam preparation of Jing retrievals has following several patents.
Application number 02135957.1 is " preparation method and product of a kind of oxiracetam injection ", discloses one kind
The preparation method of oxiracetam injection, its prescription is oxiracetam, glucose, Sodium Chloride, water for injection.Wherein Fructus Vitis viniferae
Sugar with Sodium Chloride can the adjuvant similar with xylitol for injection or alcohol or Fructose etc. replace.
Application No. 02114302.1 is the system that " oxiracetam injection " discloses oxiracetam lyophilized injectable powder
Preparation Method, its prescription consists of oxiracetam, Mannitol.
Application number 03138998.8 is that " preparation method and product of a kind of oxiracetam lyophilized injectable powder " equally announces Austria
The preparation method of La Xitan lyophilized injectable powders, different with 02114302.1 be prescription consist of oxiracetam, Sorbitol,
Citric acid or Lactose or sodium lactonic.
Application number 200710151608.4 is that " oxiracetam injection " discloses a kind of preparation method of oxiracetam, i.e.,
Oxiracetam and glucose or Sodium Chloride are with the pH of citric acid or sodium citrate regulation solution in 3.8～4.5.
The content of the invention
The present invention prepares a kind of injection solution of oxiracetam composition and has following several advantages：
(1) from upper oxiracetam structural formula, there are a hydroxyl and a carbonyl on pyrrole ring, the two groups may
There are two kinds of situations positioned at pyrrole ring homonymy and heteropleural, the current oxiracetam oxiracetam different to both space conformations does not have
Can separate, therefore when the hydroxyl and carbonyl of oxiracetam are located at the homonymy of pyrrole ring simultaneously, easily be formed intramolecular
Hydrogen bond, the dissolubility that can so make oxiracetam declines so that the visible foreign matters of oxiracetam are unqualified, the present invention in ammonia from
Son exists and adjusts pH 4.6～5.5, solves this problem.
(2) from upper oxiracetam structural formula, there is an amido link, amido link can be hydrolyzed, and particularly meet high temperature
Hydrolysis becomes apparent from, and adjusts pH 4.6～5.5 in the present invention, solves this problem.
Contrast test is as follows.
Prescription 1
Prepare：900ml waters for injection are taken, adds the oxiracetam of 1000g, stirring to make to be completely dissolved, add injection stage
Activated carbon, is filtered to remove activated carbon, adjusts pH4.5～5.5 of solution, then injects water to 5000ml, filters to clear and bright, fills
Dress, sealing, 121 DEG C sterilize for 12 minutes.
Prescription 2
Prepare：
70 DEG C～80 DEG C of 800ml waters for injection, plus ammonium chloride are weighed, stirring makes to be completely dissolved, and water temperature is down to room temperature, plus
Enter the oxiracetam of 1000g, stirring makes to be completely dissolved, and adds the activated carbon of injection stage, is filtered to remove activated carbon, adjusts solution
PH4.5～5.5, then inject water to 5000ml, filter to clear and bright, fill, sealing.
Two prescriptions are prepared after sample lamp inspection, taking the qualified sample of visible foreign matters carries out 121 DEG C of sterilizings in 12 minutes.Sterilizing
Visible foreign matters and Related substances separation result such as following table in front and back.
The prescription comparing result of table one
From upper result, two prescription differences are obvious, and prepared by the prescription of the present invention sample Jing 121 DEG C sterilizes for 12 minutes
Afterwards, there is obvious advantage in terms of visible foreign matters and relevant material.
(3) this preparation method can be with 121 DEG C of high temperature sterilizes, it is ensured that the safety of product.
A kind of injection solution of oxiracetam composition, including oxiracetam, ammonium chloride and water for injection, is characterized in that：Contain
Ammonium chloride, wherein containing oxiracetam 200mg, 0.5～50mg of ammonium chloride per 1ml injection, it is characterised in that the pH of injection
It is adjusted to 4.6～5.5.
Specific embodiment：
The preparation of the oxiracetam injection of embodiment 1
70 DEG C～80 DEG C of 800ml waters for injection, plus the ammonium chloride of 5g are weighed, stirring makes to be completely dissolved, and water temperature is down to room
Temperature, adds the oxiracetam of 2000g, stirring to make to be completely dissolved, and adds the activated carbon of injection stage, is filtered to remove activated carbon, adjusts molten
PH4.8～5.0 of liquid, then inject water to 10000ml, filter to clear and bright, fill, sealing, and 121 DEG C sterilize for 12 minutes.
The preparation of the oxiracetam injection of embodiment 2
70 DEG C～80 DEG C of 800ml waters for injection, plus the ammonium chloride of 5g are weighed, stirring makes to be completely dissolved, and water temperature is down to room
Temperature, adds the oxiracetam of 2000g, stirring to make to be completely dissolved, and adds the activated carbon of injection stage, is filtered to remove activated carbon, adjusts molten
PH5.0～5.2 of liquid, then inject water to 10000ml, filter to clear and bright, fill, sealing, and 121 DEG C sterilize for 12 minutes.
Embodiment 3
70 DEG C～80 DEG C of 800ml waters for injection, plus the ammonium chloride of 10g are weighed, stirring makes to be completely dissolved, and water temperature is down to room
Temperature, adds the oxiracetam of 2000g, stirring to make to be completely dissolved, and adds the activated carbon of injection stage, is filtered to remove activated carbon, adjusts molten
PH4.8～5.0 of liquid, then inject water to 10000ml, filter to clear and bright, fill, sealing, and 121 DEG C sterilize for 12 minutes.
Embodiment 4
70 DEG C～80 DEG C of 800ml waters for injection, plus the ammonium chloride of 10g are weighed, stirring makes to be completely dissolved, and water temperature is down to room
Temperature, adds the oxiracetam of 2000g, stirring to make to be completely dissolved, and adds the activated carbon of injection stage, is filtered to remove activated carbon, adjusts molten
PH5.0～5.2 of liquid, then inject water to 10000ml, filter to clear and bright, fill, sealing, and 121 DEG C sterilize for 12 minutes.
Above example carries out stability experiment to this product.
The pilot scale oxiracetam injection stability test of table two
Embodiment 5
70 DEG C～80 DEG C of 800ml waters for injection, plus the ammonium chloride of 20g are weighed, stirring makes to be completely dissolved, and water temperature is down to room
Temperature, adds the oxiracetam of 2000g, stirring to make to be completely dissolved, and adds the activated carbon of injection stage, is filtered to remove activated carbon, adjusts molten
PH4.8～5.0 of liquid, then inject water to 10000ml, filter to clear and bright, fill, sealing, and 121 DEG C sterilize for 12 minutes.
Embodiment 6
70 DEG C～80 DEG C of 800ml waters for injection, plus the ammonium chloride of 20g are weighed, stirring makes to be completely dissolved, and water temperature is down to room
Temperature, adds the oxiracetam of 2000g, stirring to make to be completely dissolved, and adds the activated carbon of injection stage, is filtered to remove activated carbon, adjusts molten
PH4.0～5.2 of liquid, then inject water to 10000ml, filter to clear and bright, fill, sealing, and 121 DEG C sterilize for 12 minutes.
The oxiracetam injection safety testing of embodiment 7
Safety experiment investigation is carried out with product of the present invention, is given to rabbit vein after product clinical administration amount conversion of the present invention
Medicine, product of the present invention is to the non-stimulated generation of blood vessel.After 3 hours being incubated with 37 ± 0.5 DEG C in rabbit erythrocyte suspension thermostatic bath,
Haemolysis and aggregation are not produced.To the allergy not caused after Cavia porcelluss Formulations for systemic administration after the conversion of invention product clinical administration amount
Reaction.
Claims (5)
1. a kind of injection solution of oxiracetam composition, including oxiracetam, ammonium chloride and water for injection, it is characterised in that contain
Ammonium chloride, wherein contain oxiracetam 200mg per 1ml injection, 0.5～50mg of ammonium chloride, the pH regulator of injection to 4.5～
5.5。
2. injection solution of oxiracetam composition as claimed in claim 1, including oxiracetam and water for injection, its feature exists
In containing ammonium chloride, wherein containing oxiracetam 200mg, 0.5～50mg of ammonium chloride, the pH regulator of injection per 1ml injection
To 4.8～5.2.
3. the preparation method of injection solution of oxiracetam composition as claimed in claim 1, comprises the steps：Weigh 70～80
DEG C 800ml waters for injection, plus 0.5～ammonium chloride of 50g, stirring makes to be completely dissolved, and water temperature is down to room temperature, adds Austria of 200g
La Xitan, stirring makes to be completely dissolved, and adds the activated carbon of injection stage, is filtered to remove activated carbon, adjusts the pH 4.5～5.5 of solution,
Then 1000ml is injected water to, is filtered to clear and bright, fill, sealing, 121 DEG C sterilize for 12 minutes.
4. preparation method as claimed in claim 3, it is characterised in that be filtered to remove activated carbon, with ammonia adjust pH value to 4.5～
5.5。
5. preparation method as claimed in claim 3, it is characterised in that be filtered to remove activated carbon, with ammonia adjust pH value to 4.8～
5.2。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310068438.9A CN104027301B (en) | 2013-03-05 | 2013-03-05 | Oxiracetam composition injection |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310068438.9A CN104027301B (en) | 2013-03-05 | 2013-03-05 | Oxiracetam composition injection |
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| Publication Number | Publication Date |
|---|---|
| CN104027301A CN104027301A (en) | 2014-09-10 |
| CN104027301B true CN104027301B (en) | 2017-05-10 |
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| CN201310068438.9A Active CN104027301B (en) | 2013-03-05 | 2013-03-05 | Oxiracetam composition injection |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101396358A (en) * | 2007-09-25 | 2009-04-01 | 广东世信药业有限公司 | Oxiracetam injection |
| CN102552125A (en) * | 2012-01-18 | 2012-07-11 | 陈先武 | Injection composition containing oxiracetam and preparation method and application thereof |
| CN102784098A (en) * | 2011-05-20 | 2012-11-21 | 湖南省湘中制药有限公司 | Magnesium valproate injection and preparation method thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102227222B (en) * | 2008-12-22 | 2012-11-21 | 奥列格·谢尔盖耶维奇·索基尔科 | Antitumor agent, method for production of the agent and method for stabilisation thereof |
-
2013
- 2013-03-05 CN CN201310068438.9A patent/CN104027301B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101396358A (en) * | 2007-09-25 | 2009-04-01 | 广东世信药业有限公司 | Oxiracetam injection |
| CN102784098A (en) * | 2011-05-20 | 2012-11-21 | 湖南省湘中制药有限公司 | Magnesium valproate injection and preparation method thereof |
| CN102552125A (en) * | 2012-01-18 | 2012-07-11 | 陈先武 | Injection composition containing oxiracetam and preparation method and application thereof |
Non-Patent Citations (2)
| Title |
|---|
| HPLC DETERMINATION OF OXIRACETAM, ITS IMPURITIES, ANDPIRACETAM IN PHARMACEUTICAL FORMULATIONS;L. Gagliardia et al;《ANALYTICAL LETTERS》;19941231;第27卷(第5期);879-885 * |
| 奥拉西坦注射液的研制;颜素华等;《中国现代医学杂志》;20100531;第20卷(第10期);1541-1545，1550 * |
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| CN104027301A (en) | 2014-09-10 |
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Effective date of registration: 20210419 Address after: 071000 1st floor, block D, science and Technology Industrial Park, 723 Cuiyuan street, Baoding City, Hebei Province Patentee after: Baoding Aihui Pharmaceutical Co.,Ltd. Address before: 100077, room 23, building two, 401 West Third Ring Road, West Third Ring Road, Fengtai District, Beijing Patentee before: Xiao Yuncai Patentee before: Shen Yinfu |