CN102451181A - Prescription and preparation method of injection lansoprazole - Google Patents
Prescription and preparation method of injection lansoprazole Download PDFInfo
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- CN102451181A CN102451181A CN2010105311776A CN201010531177A CN102451181A CN 102451181 A CN102451181 A CN 102451181A CN 2010105311776 A CN2010105311776 A CN 2010105311776A CN 201010531177 A CN201010531177 A CN 201010531177A CN 102451181 A CN102451181 A CN 102451181A
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Abstract
The invention provides a prescription and preparation method of injection lansoprazole used for treating gastric ulcer, duodenal ulcer, reflux esophagitis, Zollinger-Ellison syndrome and Stomal ulcer. In the injection lansoprazole, the weight ratio of lansoprazole to mannitol to sodium hydroxide is 1:(3-5):0.11. The injection lansoprazole is prepared by dissolving the raw and auxiliary materials at certain temperature and acidity, and then lyophilizing. The invention aims at overcoming the defect of a medicinal preparation using lansoprazole as an active component, and provides the prescription of the injection lansoprazole and the preparation method thereof. The preparation prepared by the method is stable, the safety of clinical application is improved, and the production cost is reduced.
Description
Technical field:
The present invention relates to a kind of injection that is used to treat gastric ulcer, duodenal ulcer, reflux esophagitis, Zollinger-Ellison Syndrome, the oral area ulcer of coincideing, particularly relating to the lansoprazole is the lyophilized formulations of active component.
Background technology:
Its chemistry of lansoprazole is by name: (+)-2 [[[3-methyl-4-(2,2, the 2-trifluoro ethoxy)-2-pyridine radicals] methyl] sulfinyl] benzimidazole, molecular formula: C
16H
14F
3N
3O
2S, its structural formula is:
These article H/K-ATP enzyme inhibitor by Japan's military field drug company listing exploitation in 1992 is the benzimidazole substituent of exploitation after omeprazole, is proton pump inhibitor.After its mechanism of action is drug absorption, transfer to the sour secretory duct of gastric mucosa parietal cell, under acid condition, change the active body structure into, this kind active matter and proton pump (H
-, the K-ATP enzyme) SH base combine, thereby suppress the activity of this enzyme, so secretion that can gastric acid inhibitory is mainly used in treatment gastric ulcer, duodenal ulcer, reflux esophagitis, Zollinger-Ellison Syndrome, identical oral area ulcer.
Lansoprazole, its character is brownish white crystalline powder, is soluble in dimethyl formamide, dissolves in methanol, is insoluble in ethanol, ether, and is water-soluble hardly.It is unstable under acidic condition, and its oral formulations is degraded easily in gastric acid environment, need process enteric coated preparation and absorb at small intestinal and duodenum.So its solid preparation complicated process of preparation, production cost is high.
The lansoprazole lyophilized formulations that goes on the market at present; Many stable environment of keeping lansoprazole with organic base, antioxidant; The adding of organic base possibly cause the quality of the pharmaceutical preparations unstable, and adds too much antioxidant and can cause side effects of pharmaceutical drugs to increase, and medication is dangerous.We optimize to such an extent that a kind of new Lansoprazole for injecting is write out a prescription and method for preparing to above-mentioned phenomenon.
Summary of the invention
The objective of the invention is to replenish with the lansoprazole is the deficiency of the pharmaceutical preparation of active component, and a kind of prescription and method for preparing of Lansoprazole for injecting is provided, to replenish similar preparation weak point.Preparation stabilization through this law makes has improved clinical application safety, and production cost reduces.
The prescription of Lansoprazole for injecting provided by the invention is formed part by weight:
1 unit of weight of lansoprazole
3～5 unit of weights of mannitol
0.11 unit of weight of sodium hydroxide.
In the prescription that the present invention proposes, excipient can be selected mannitol for use.
In the prescription that the present invention proposes, PH regulator and cosolvent are sodium hydroxide.
The present invention proposes the method for preparing of Lansoprazole for injecting, may further comprise the steps: 1. take by weighing recipe quantity mannitol, join in the water for injection of preparing full dose 85% (30～40 ℃ of water temperatures); Stirring and dissolving adds lansoprazole, stirs down and transfers to PH11.0～12.0 with the 1mol/L sodium hydroxide; After-teeming is penetrated water to full dose; Add medicinal charcoal, stirring and adsorbing under the room temperature is filtered carbon removal; 2. get the filtrating fill, the fill certified products are inserted on the freeze drying box dividing plate ,-33 ℃ of pre-freeze 2.5h; Be evacuated to vacuum and reach 15pa; Be warming up to products temperature with 2 ℃/h and reach more than 5 ℃, set baffle temperature again and be 35 ℃ and carry out redrying, products temperature reaches more than 30 ℃; Balance 4h, tamponade promptly gets the Lansoprazole for injecting lyophilized formulations.
In the method for preparing that the present invention proposes, when water temperature is 30～40 ℃ raw material is added.
In the method for preparing that the present invention proposes, PH is controlled under 11.0～12.0 the alkali condition in the material dissolution process.
Technical characterstic of the present invention is the use that has reduced organic solvent through the improvement to disintegrating agent and coating materials in the prescription, has reduced production cost; Simultaneously, protect the active component of medicine effectively, improved drug bioavailability.
The specific embodiment
With by way of example the present invention is described further again below, provides the present invention and get implementation detail, but be not to be intended to limit protection scope of the present invention.
Embodiment 1:
Lansoprazole 30.0g
Mannitol 90.0g
Sodium hydroxide 3.4g
Process 1000
Take by weighing recipe quantity mannitol, join in the water for injection of preparing full dose 85% (30～40 ℃ of water temperatures) stirring and dissolving; Add lansoprazole, stir down and transfer to PH11.0 with the 1mol/L sodium hydroxide, water to full dose is penetrated in after-teeming; Add medicinal charcoal, stirring and adsorbing under the room temperature is filtered carbon removal; Get the filtrating fill, the fill certified products are inserted on the freeze drying box dividing plate ,-33 ℃ of pre-freeze 2.5h; Be evacuated to vacuum and reach 15pa, be warming up to products temperature with 2 ℃/h and reach more than 5 ℃, set baffle temperature again and be 35 ℃ and carry out redrying; Products temperature reaches more than 30 ℃; Balance 4h, tamponade gets the Lansoprazole for injecting lyophilized formulations.
Embodiment 2
Lansoprazole 30.0g
Mannitol 150.0g
Sodium hydroxide 3.4g
Process 1000
Take by weighing recipe quantity mannitol, join in the water for injection of preparing full dose 85% (30～40 ℃ of water temperatures) stirring and dissolving; Add lansoprazole, stir down and transfer to PH12.0 with the 1mol/L sodium hydroxide, water to full dose is penetrated in after-teeming; Add medicinal charcoal, stirring and adsorbing under the room temperature is filtered carbon removal; Get the filtrating fill, the fill certified products are inserted on the freeze drying box dividing plate ,-33 ℃ of pre-freeze 2.5h; Be evacuated to vacuum and reach 15pa, be warming up to products temperature with 2 ℃/h and reach more than 5 ℃, set baffle temperature again and be 35 ℃ and carry out redrying; Products temperature reaches more than 30 ℃; Balance 4h, tamponade gets the Lansoprazole for injecting lyophilized formulations.
Claims (6)
1. a Lansoprazole for injecting is write out a prescription and method for preparing, it is characterized in that the prescription composition part by weight of said preparation is: lansoprazole: mannitol: sodium hydroxide=1: 3～5: 0.11.
2. the method for preparing of Lansoprazole for injecting as claimed in claim 1 is characterized in that, may further comprise the steps:
2.1 take by weighing recipe quantity mannitol, join in the water for injection of preparing full dose 85% (30～40 ℃ of water temperatures) stirring and dissolving; Add lansoprazole, stir down and transfer to PH11.0～12.0 with the 1mol/L sodium hydroxide, water to full dose is penetrated in after-teeming; Add medicinal charcoal, stirring and adsorbing under the room temperature is filtered carbon removal;
2.2 get the filtrating fill, the fill certified products are inserted on the freeze drying box dividing plate-33 ℃ of pre-freeze 2.5h; Be evacuated to vacuum and reach 15pa; Be warming up to products temperature with 2 ℃/h and reach more than 5 ℃, set baffle temperature again and be 35 ℃ and carry out redrying, products temperature reaches more than 30 ℃; Balance 4h, tamponade promptly gets the Lansoprazole for injecting preparation.
3. the method for preparing of Lansoprazole for injecting as claimed in claim 1, it is characterized in that: excipient is selected mannitol for use.
4. the method for preparing of Lansoprazole for injecting as claimed in claim 1 is characterized in that: with sodium hydroxide as PH regulator and cosolvent.
5. the method for preparing of Lansoprazole for injecting as claimed in claim 1, it is characterized in that: the water temperature during material dissolution is 30～40 ℃.
6. the method for preparing of Lansoprazole for injecting as claimed in claim 1, it is characterized in that: PH is under 11.0～12.0 alkali condition in the material dissolution process.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010105311776A CN102451181A (en) | 2010-10-26 | 2010-10-26 | Prescription and preparation method of injection lansoprazole |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010105311776A CN102451181A (en) | 2010-10-26 | 2010-10-26 | Prescription and preparation method of injection lansoprazole |
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| Publication Number | Publication Date |
|---|---|
| CN102451181A true CN102451181A (en) | 2012-05-16 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010105311776A Pending CN102451181A (en) | 2010-10-26 | 2010-10-26 | Prescription and preparation method of injection lansoprazole |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112353766A (en) * | 2020-10-27 | 2021-02-12 | 马鞍山丰原制药有限公司 | Lansoprazole lyophilized preparation and preparation method thereof |
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| CN1709248A (en) * | 2005-06-02 | 2005-12-21 | 江苏奥赛康药业有限公司 | Lansoprazole lyophilized powder injection and its preparing method |
| CN1810244A (en) * | 2006-02-27 | 2006-08-02 | 锦州九泰药业有限责任公司 | Freeze dried Lansoprazole sodium injection and its prepn process |
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Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1660092A (en) * | 2004-12-22 | 2005-08-31 | 陈庆财 | Injection preparation of sodium lansoprazole and preparing method |
| CN1709248A (en) * | 2005-06-02 | 2005-12-21 | 江苏奥赛康药业有限公司 | Lansoprazole lyophilized powder injection and its preparing method |
| CN1810244A (en) * | 2006-02-27 | 2006-08-02 | 锦州九泰药业有限责任公司 | Freeze dried Lansoprazole sodium injection and its prepn process |
| CN101129368A (en) * | 2007-08-23 | 2008-02-27 | 姚俊华 | Freeze-dried powder needle containing lansoprazole |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112353766A (en) * | 2020-10-27 | 2021-02-12 | 马鞍山丰原制药有限公司 | Lansoprazole lyophilized preparation and preparation method thereof |
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Application publication date: 20120516 |