CN103705474B - Lyophilized pharmaceutical composition containing omeprazole sodium - Google Patents
Lyophilized pharmaceutical composition containing omeprazole sodium Download PDFInfo
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- CN103705474B CN103705474B CN201310737574.2A CN201310737574A CN103705474B CN 103705474 B CN103705474 B CN 103705474B CN 201310737574 A CN201310737574 A CN 201310737574A CN 103705474 B CN103705474 B CN 103705474B
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Abstract
The invention relates to the field of drug preparations, and particularly relates to a lyophilized pharmaceutical composition containing omeprazole sodium and a preparation method of the pharmaceutical composition. The lyophilized drug composition provided by the invention comprises the following components: omeprazole sodium, chlorogenic acid, edetate disodium, mannitol and sodium hydroxide.
Description
Technical field:
The present invention relates to field of pharmaceutical preparations, particularly a kind of freeze-drying medicinal composition and preparation thereof containing Omeprazole Sodium.Freeze-drying medicinal composition of the present invention comprises following composition: Omeprazole Sodium, chlorogenic acid, disodium edetate, mannitol, sodium hydroxide.
background technology:
Omeprazole Sodium, its chemical name is: 5-methoxyl group-2-{ [(4-methoxyl group-3,5-dimethyl-2-pyridine radicals)-methyl]-sulfinyl }-1H-benzimidazole sodium.
Omeprazole Sodium is the racemic mixture of a pair active optical antimer, is reduced the secretion of gastric acid by the mechanism of action of high targeted, is the specific inhibitor of sour pump in parietal cell.This product effect is rapid, and dosage once a day can the secretion of reversible gastric acid inhibitory.
Omeprazole Sodium is a kind of alkalescence material, is concentrated and is converted into active substance in parietal cell in this peracidity environment of tubule, suppresses H+, K+-ATP enzyme (proton pump).This inhibitory action to gastric acid formation final step is dosage correlation, and highly suppresses basal gastric acid secretion and zest gastric acid secretion, but has nothing to do with stimulus object.
Human vein gives Omeprazole Sodium, the gastric acid secretion inhibiting in dosage correlation, in order to reach rapidly the effect with repeatedly oral 20 milligrams of identical reduction Acidity in the stomachs, advises that intravenous gives 40 milligrams of omeprazoles first.Quiet note 40 milligrams of omeprazoles reduce Acidity in the stomach rapidly, average decline 90% in 24 hours.The gastric acid secretion inhibiting effect of omeprazole is relevant to area under drug-time curve (AUC), and has nothing to do with blood drug level during administration.
Helicobacter pylori is relevant with sour digestion disease, comprises duodenal ulcer and gastric ulcer, relevant with helicobacter pylori infections with gastric ulcer with the duodenal ulcer of 70% by 95% respectively.Helicobacter pylori is the principal element causing gastritis.Helicobacter pylori is the principal element causing peptic ulcer together with gastric acid.
Omeprazole Sodium and antibiotic share can eradicate helicobacter pylori, this to quick symptom relief, gastric mucosal rate long-term remission that is high and peptic ulcer disease is relevant, and because this reducing the complication such as gastrointestinal hemorrhage, decrease the long-term anti-needs secreting the treatment of sour medicine simultaneously.
Any method, comprises gastric acid caused by proton pump inhibitor and reduces, all increase the quantity of normal flora in gastrointestinal tract, and with antisecretory treatment, then salmonella and campylobacter infect gastrointestinal danger may slightly increase.
Give for a long time in the research of Omeprazole Sodium rat, observe stomach ECL cell and increase and benign tumor, this is the result that persistence hypergastrinemia suppresses because of gastric acid.After with bisfentidine, proton pump inhibitor therapy and also have similar discovery after section bottom excision.Obviously these changes are not the direct effect of said medicine.
Omeprazole Sodium can with treatment digestive ulcerative bleeding, stoma ulcer is hemorrhage; Acute Gastric Mucosal infringement concurrent during stress state, and the acute gastric mucosal injury that nonsteroidal antiinflammatory drug causes; Also prevent again hemorrhage etc. after being usually used in prevention seriously disease (as cerebral hemorrhage, severe trauma etc.) stomach operation; After general anesthesia or major operation and weak comatose patient prevent regurgitation of gastric juice from merging aspiration pneumonitis.
Multiple report is had to omeprazole sodium injection in prior art, the present invention finds, existing omeprazole sodium injection has blood vessel irritation when injecting, even cause local pain, Omeprazole Sodium and chlorogenic acid are injected discovery when studying chlorogenic acid by the present invention simultaneously, and blood vessel irritation alleviates greatly.Chlorogenic acid is prepared into lyophilized formulations together with Omeprazole Sodium simultaneously, the redissolution speed of medicine can be accelerated, be conducive to the use of lyophilized formulations, summary of the invention:
The invention provides a kind of freeze-drying medicinal composition of Omeprazole Sodium, it is freeze-dried pharmaceutical formulation form, and every 1000 following components of freeze dried injection are prepared from:
The present invention also provides the preparation method of the freeze-drying medicinal composition of Omeprazole Sodium of the present invention, and preparation process is as follows:
1) get sodium hydroxide, Omeprazole Sodium, chlorogenic acid, disodiumedetate add in water for injection, be stirred to and dissolve completely,
2) add 2g medicinal carbon, stir 10-30 minute, add mannitol, stir 10-30 minute after dissolving, with the filter decarbonization filtering of 0.45um.
3) regulate medicinal liquid pH value to 10.90-11.00 with the sodium hydroxide solution of 1mol/L or the hydrochloric acid of 1mol/L, water for injection is settled to dosing, stirring, mix homogeneously;
4) medicinal liquid carries out aseptic filtration through 0.22um microporous filter membrane, fill, lyophilizing, gland, lamp inspection, packaging, warehouse-in.
The depside that chlorogenic acid (Chlorogenicacid) is made up of caffeic acid (Caffeic acid) and quinic acid (Quinic acid), different name chlorogenic acid, chemical name 3-O-caffeoyl Kui acid (3-O-caffeoylquinic acid) molecular formula: C16H18O9, molecular weight: 354.30 is plant a kind of benzene-like compounds through shikimic acid pathway generation in aerobic respiration process.Chlorogenic acid is extensively present in high dicotyledon and pteridophyta, mainly richly be that in Caprifoliaceae Lonicera (Lonicera), Compositae artemisia (Artemisia) plant, the plant that wherein content is higher is mainly the Cortex Eucommiae, Flos Lonicerae, Helianthi, the wood that continues, coffee, cocoa tree etc.Chlorogenic acid has biological activity widely, and modern science has been deep into multiple fields such as food, health care, medicine and daily-use chemical industry to the bioactive research of chlorogenic acid.Chlorogenic acid is a kind of important bioactive substance, has antibacterial, antiviral, increases the effects such as leukocyte, hepatic cholagogic, antitumor, blood pressure lowering, blood fat reducing, scavenging free radicals and stimulating central nervous system system.
The present invention finds in research chlorogenic acid injection process, it can reduce blood vessel irritation and local pain, through screening, the present invention simultaneously finds that the use amount of chlorogenic acid is at 10mg, this dosage can not produce any side effect, but can play the effect of auxiliary Omeprazole Sodium.
Below by way of experimental data, beneficial effect of the present invention is described:
Contrast experiment:
The indices of injection omeprazole sodium sample investigated embodiment 1 and the comparative example not adding chlorogenic acid and gone on the market
1. vascular stimulation test method
Select the white big ear rabbit 9 of body weight 2.5 ~ 3.0kg, male and female half and half, random point four groups, often organize 3.Be set to embodiment 1 sample (adding chlorogenic acid) group, comparative example 1 sample (not adding chlorogenic acid) group, the omeprazole sample sets of going on the market respectively.The sample under Clinical practice concentration is given, administration in continuous 7 days, 48 ~ 96 hours perusal animals and injection site before administration every day and after administration respectively at auricular vein.After last administration, 48 ~ 96 hour observation period terminated, and got Some Animals medicine-feeding part tissue slice and carried out pathological examination.The animal stayed, according to the feature of tested material and irritative response situation, continues to observe and carries out histopathological examination again in 14-21 days.
2. local pain experimental technique
Randomly draw from the Healthy People of voluntary participation experimental study 60 example, men and women half and half, age 25-55 year.Be divided into 3 groups at random, often organize 20 people.Be set to embodiment 1 sample (adding chlorogenic acid) group, comparative example 1 sample (not adding chlorogenic acid) group, the omeprazole sample sets of going on the market respectively.After vein gives sample, observe the pain reaction of experimenter.Adopt Wong-Banker facial expression scale (FPS-R) to assess, indicate the numeral of 0-5 under the types of facial makeup in Beijing operas, numeral is larger, represents that pain intensity is larger.After off-test, adopting SPSS11.5 version software to carry out statistical procedures, is that difference has statistical significance with P<0.05.
3. dissolution velocity experimental technique
Get omeprazole sample 40mg, be dissolved in 10ml sterilized water for injection.Observe sample dissolution situation.
4. accelerate 3 months medicine assay experimental techniques
The sample getting 3 batches at random carries out accelerated test, is placed on and commercially produces in the same or analogous packing container of product, and experimental condition is 40 DEG C ± 2 DEG C/RH75% ± 5%, and the investigation time is 3 months.Adopt the content of high effective liquid chromatography for measuring omeprazole.Method And Principle: test sample makes mobile phase solution, enters high performance liquid chromatograph and carries out chromatographic isolation, with ultraviolet absorption detector, detects omeprazole absorption value, calculate its content in wavelength 280nm place.(content acceptability limit: 94.0% ~ 106.0%)
Detailed description of the invention:
Embodiment 1
Every 1000 following components of freeze dried injection are prepared from:
The present invention also provides the preparation method of the freeze-drying medicinal composition of Omeprazole Sodium of the present invention, and preparation process is as follows:
1) get sodium hydroxide, Omeprazole Sodium, chlorogenic acid, disodiumedetate add in water for injection, be stirred to and dissolve completely,
2) add 2g medicinal carbon, stir 10-30 minute, add mannitol, stir 10-30 minute after dissolving, with the filter decarbonization filtering of 0.45um.
3) regulate medicinal liquid pH value to 10.90-11.00 with the sodium hydroxide solution of 1mol/L or the hydrochloric acid of 1mol/L, water for injection is settled to dosing, stirring, mix homogeneously;
4) medicinal liquid carries out aseptic filtration through 0.22um microporous filter membrane, fill, lyophilizing, gland, lamp inspection, packaging, warehouse-in.
Comparative example
Every 1000 following components of freeze dried injection are prepared from:
The present invention also provides the preparation method of the freeze-drying medicinal composition of Omeprazole Sodium of the present invention, and preparation process is as follows:
1) get sodium hydroxide, Omeprazole Sodium, disodiumedetate add in water for injection, be stirred to and dissolve completely,
2) add 2g medicinal carbon, stir 10-30 minute, add mannitol, stir 10-30 minute after dissolving, with the filter decarbonization filtering of 0.45um.
3) regulate medicinal liquid pH value to 10.90-11.00 with the sodium hydroxide solution of 1mol/L or the hydrochloric acid of 1mol/L, water for injection is settled to dosing, stirring, mix homogeneously;
4) medicinal liquid carries out aseptic filtration through 0.22um microporous filter membrane, fill, lyophilizing, gland, lamp inspection, packaging, warehouse-in.
Claims (1)
1. a freeze-drying medicinal composition for Omeprazole Sodium, it is freeze-dried pharmaceutical formulation form, and every 1000 following components of freeze dried injection are prepared from:
Its preparation process is as follows:
1) get sodium hydroxide, Omeprazole Sodium, chlorogenic acid, disodiumedetate add in water for injection, be stirred to and dissolve completely,
2) add 2g medicinal carbon, stir 10-30 minute, add mannitol, after dissolving, stir 10-30 minute, with the filter decarbonization filtering of 0.45 μm,
3) regulate medicinal liquid pH value to 10.90-11.00 with the sodium hydroxide solution of 1mol/L or the hydrochloric acid of 1mol/L, water for injection is settled to dosing, stirring, mix homogeneously,
4) medicinal liquid carries out aseptic filtration through 0.22 μm of microporous filter membrane, fill, lyophilizing, gland, lamp inspection, packaging, warehouse-in.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310737574.2A CN103705474B (en) | 2013-12-27 | 2013-12-27 | Lyophilized pharmaceutical composition containing omeprazole sodium |
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| CN201310737574.2A CN103705474B (en) | 2013-12-27 | 2013-12-27 | Lyophilized pharmaceutical composition containing omeprazole sodium |
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| CN103705474A CN103705474A (en) | 2014-04-09 |
| CN103705474B true CN103705474B (en) | 2015-04-22 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105311624A (en) * | 2015-11-23 | 2016-02-10 | 哈药集团生物工程有限公司 | Pharmaceutical composition containing recombinant human erythropoietin |
| CN105311625A (en) * | 2015-11-23 | 2016-02-10 | 哈药集团生物工程有限公司 | Pharmaceutical composition containing recombinant human granulocyte colony-stimulating factors |
| CN109984998B (en) * | 2019-05-23 | 2020-09-15 | 山东和兴药业有限公司 | Preparation method of omeprazole sodium for injection |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100998593A (en) * | 2006-01-12 | 2007-07-18 | 黄玉明 | Stable omeprazol sodium preparation for injection |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100998593A (en) * | 2006-01-12 | 2007-07-18 | 黄玉明 | Stable omeprazol sodium preparation for injection |
Non-Patent Citations (1)
| Title |
|---|
| 天然产物绿原酸的研究进展;陈绍华等;《食品科技》;20081231(第2期);第198页第5.6栏 * |
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