CN1729977A - Freeze dry powdered injection of moxfloxacin or its salts and preparation process thereof - Google Patents
Freeze dry powdered injection of moxfloxacin or its salts and preparation process thereof Download PDFInfo
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- CN1729977A CN1729977A CN 200510092828 CN200510092828A CN1729977A CN 1729977 A CN1729977 A CN 1729977A CN 200510092828 CN200510092828 CN 200510092828 CN 200510092828 A CN200510092828 A CN 200510092828A CN 1729977 A CN1729977 A CN 1729977A
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- moxifloxacin
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- acid
- injection
- injectable powder
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Abstract
The invention provides a moxfloxacin for injection or freeze dried powder injection of its salts, and its preparation process, which is prepared from moxifloxacin or its salts, excipient, pH modifier and water for injection through freeze drying.
Description
Technical field
This is bright to relate to a kind of have the injection Moxifloxacin of broad-spectrum antibacterial action or lyophilized injectable powder of its salt and preparation method thereof.
Background technology
Moxifloxacin (moxifloxacin) is a novel super wide spectrum Comprecin of the 4th generation, and this novel quinolone medicine is except that the powerful anti-gram-negative bacteria activity of maintenance, to the strong antibacterial activity of gram positive bacteria and other atypia pathogenic bacterium also tool.For moraxelle catarrhalis, chlamydia, bacteroides fragilis, staphylococcus, streptococcus, the antibacterial activity of enterobacteria and anaerobe is strong than ciprofloxacin and ofloxacin.Its antimicrobial spectrum has covered the main pathogenic bacterium of whole respiratory tracts, the most outstanding a kind of be exactly streptococcus pneumoniae.This product mechanism of action is similar to other quinolones, mainly be to suppress topology isomerase IV and DNA helicase, but to the influence or the chemical sproof generation of indivedual gene mutation, but than other quinolones for few.
Existing Moxifloxacin preparation is injection or tablet etc.Injection formulation have medicine stability poor, be not easy to carry and shortcoming such as transportation, and tablet for numerous critical bacterial infection patients because of can not the oral clinical practice that limits this medicine greatly.
Summary of the invention
The object of the present invention is to provide a kind ofly to stable performances such as light, heat, oxygen, water, pollution-free, and be convenient to operation, transportation and storage, applied range, be fit to Moxifloxacin or its salt freeze-dried powder-injection of large-scale production.
Another object of the present invention is to provide the preparation method of this injectable powder.
The objective of the invention is to be achieved through the following technical solutions:
The material composition that the injection Moxifloxacin that the present invention proposes or the lyophilized injectable powder of its salt comprise and before lyophilizing in the solution shared percentage composition be:
Moxifloxacin or its salt, amount to into Moxifloxacin and be 1～40% (g/100ml, w/v),
Excipient 0～80% (g/100ml, w/v).
The pH regulator agent is an amount of
Wherein, described excipient is a kind of, any two or more mixture wherein such as lactose, mannitol, dextran 20, dextran 40, dextran 70, glucose, gelatin hydrolysate, sorbitol, Aspartic Acid, glycine, alanine, serine, isoleucine, threonine, glutamic acid, phenylalanine, histidine, valine, cysteine hydrochloride, arginine hydrochloride, sodium chloride, calcium chloride, sucrose, fructose, sodium citrate, sodium ascorbyl phosphate.A kind of, any two or more mixture among preferred lactose, mannitol, dextran, the glucose.
The invention allows for the preparation method of the lyophilized injectable powder of injection Moxifloxacin or its salt, this procedure is as follows: under aseptic condition, get recipe quantity Moxifloxacin or its salt and excipient, add the water for injection stirring and make dissolving, transfer pH to proper range with the pH regulator agent, after-teeming is penetrated water to capacity, crosses 0.22 μ m microporous filter membrane, after measuring content, fill is in the control cillin bottle; Carry out lyophilization by following technological process and parameter:
Temp(℃) P(mba) Time(min)
Loading -10 - -
Freezing -40 - 40
-40 - 90
- 0.4 60
Primary?drying 25 0.4 60
27 0.4 120
30 0.4 160
32 0.4 120
35 0.4 60
37 0.4 120
40 0.4 60
52 0.4 120
Second?drying 52 0.002 120
Then outlet, jump a queue, roll lid, the qualified back packing of product inspection is promptly.
Wherein, described pH value regulator is a kind of, any two or more the mixture in hydrochloric acid, sulphuric acid, acetic acid, lactic acid, methanesulfonic acid, phosphoric acid, citric acid, boric acid, tartaric acid, malic acid, Aspartic Acid, glycine, alanine, serine, isoleucine, threonine, glutamic acid, phenylalanine, histidine, valine, cysteine hydrochloride, arginine hydrochloride, sodium carbonate, sodium bicarbonate, the sodium hydroxide etc.Preferably: a kind of among hydrochloric acid, sodium bicarbonate, the sodium hydroxide, any two or more mixture.
The quality height of the lyophilized injectable powder of the designed Moxifloxacin of the present invention or its salt, good stability, the finished product water content is low, helps long term store.The Moxifloxacin proposed by the invention or the manufacture method of its salt are to adopt vacuum freeze-drying at lower temperature technology, produce medicine in hermetic container, guarantee that medicine is difficult for oxidation and takes place rottenly, also overcome Yin Gaowen in the production process and cause the problem of medicine decomposition etc.
The content of Moxifloxacin or its salt can be decided as required in the preparation, contains Moxifloxacin or its salt (amounting to into Moxifloxacin) of 50mg, 100mg, 200mg, 400mg in can making every bottle, or surpasses this scope as required.
The quality of the pharmaceutical preparations of the present invention is stable, through 4500Lx illumination 10 days, 60 ℃ of insulations 10 days, the equal no change of appearance luster and catabolite.After solvent was added lyophilized formulations of the present invention, lyophilized products dissolved rapidly, and dissolving is complete, and the solution clarity is good.Preparation of the present invention can be used for treating human or animal's bacterial infection, and toxic and side effects is low.
To illustrate rather than to limit mode of the present invention, the following example is provided, further specify injection Moxifloxacin of the present invention or its salt injectable powder and preparation method thereof.
The specific embodiment:
Embodiment 1
Under aseptic condition, take by weighing moxifloxacin hydrochloride (amounting to into Moxifloxacin) 20.0g, mannitol 20.0g, get the moxifloxacin hydrochloride of described weight, to the water for injection that wherein adds 100ml, stirring is all dissolved moxifloxacin hydrochloride, the mannitol that adds described weight, stirring makes it whole dissolvings, the sodium bicarbonate solution or the sodium bicarbonate powder adjust pH to 5.5 that add 1mol/L, adding water for injection to overall solution volume is 200mL, just filter with 0.45 μ m microporous filter membrane, filtrate is with 0.22 μ m microporous filter membrane fine straining.Gained filtrate is sub-packed in the control antibiotic cillin bottle of 5mL, every bottle of fill 2ml, vacuum lyophilization, technological process and parameter are as follows:
Temp(℃) P(mba) Time(min)
Loading -10 - -
Freezing -40 - 40
-40 - 90
- 0.4 60
Primary?drying 25 0.4 60
27 0.4 120
30 0.4 160
32 0.4 120
35 0.4 60
37 0.4 120
40 0.4 60
52 0.4 120
Second?drying 52 0.002 120
Then outlet, jump a queue, roll lid, the qualified back packing of product inspection is promptly.
Gained Moxifloxacin lyophilized formulations is white block, and quality is loose, and containing the active medicine moxifloxacin hydrochloride in every bottle, to amount to into Moxifloxacin be 200mg.
Embodiment 2
Under aseptic condition, taking by weighing moxifloxacin hydrochloride (amounting to into Moxifloxacin) is 10g, glucose 20g, get the moxifloxacin hydrochloride of described weight, to the water for injection that wherein adds 100ml, stirring is all dissolved moxifloxacin hydrochloride, the glucose that adds described weight, stirring makes it whole dissolvings, the sodium bicarbonate solution or the sodium bicarbonate powder adjust pH to 5.0 that add 1mol/L, adding water for injection to overall solution volume is 200mL, just filter with 0.45 μ m microporous filter membrane, filtrate is used 0.22um microporous filter membrane fine straining.Gained filtrate is sub-packed in the control antibiotic cillin bottle of 5mL, every bottle of fill 2ml, vacuum lyophilization, freeze-dry process is with embodiment 1.Then outlet, jump a queue, roll lid, the qualified back packing of product inspection is promptly.
Gained Moxifloxacin lyophilized formulations is the off-white color block, and quality is loose, and containing the active medicine moxifloxacin hydrochloride in every bottle, to amount to into Moxifloxacin be 100mg.
Embodiment 3
Under aseptic condition, take by weighing moxifloxacin hydrochloride (amounting to into Moxifloxacin) 5g, lactose 10g, get the moxifloxacin hydrochloride of described weight, to the water for injection that wherein adds 100ml, stirring is all dissolved moxifloxacin hydrochloride, the lactose that adds described weight, stirring makes it whole dissolvings, the sodium bicarbonate solution or the sodium bicarbonate powder adjust pH to 5.3 that add 1mol/L, adding water for injection to overall solution volume is 200mL, just filter with 0.45 μ m microporous filter membrane, filtrate is with 0.22 μ m microporous filter membrane fine straining.Gained filtrate is sub-packed in the control antibiotic cillin bottle of 5mL, every bottle of fill 2ml, vacuum lyophilization, freeze-dry process is with embodiment 1.Then outlet, jump a queue, roll lid, the qualified back packing of product inspection is promptly.
Gained Moxifloxacin lyophilized formulations is the off-white color block, and quality is loose, and containing the active medicine moxifloxacin hydrochloride in every bottle, to amount to into Moxifloxacin be 50mg.
Embodiment 4
Under aseptic condition, taking by weighing moxifloxacin hydrochloride (amounting to into Moxifloxacin) is 40g, dextran 15g, get the moxifloxacin hydrochloride of described weight, to the water for injection that wherein adds 200ml, stirring is all dissolved moxifloxacin hydrochloride, the dextran that adds described weight, stirring makes it whole dissolvings, the sodium bicarbonate solution or the sodium bicarbonate powder adjust pH to 6.0 that add 1mol/L, adding water for injection to overall solution volume is 400mL, just filter with 0.45 μ m microporous filter membrane, filtrate is with 0.22 μ m microporous filter membrane fine straining.Gained filtrate is sub-packed in the control antibiotic cillin bottle of 5mL, every bottle of fill 2ml, vacuum lyophilization, freeze-dry process is with embodiment 1.Then outlet, jump a queue, roll lid, the qualified back packing of product inspection is promptly.
Gained Moxifloxacin lyophilized formulations is the off-white color block, and quality is loose, and containing the active medicine moxifloxacin hydrochloride in every bottle, to amount to into Moxifloxacin be 400mg.
Embodiment 5
Under aseptic condition, take by weighing moxifloxacin hydrochloride (amounting to into Moxifloxacin) 20g, get the moxifloxacin hydrochloride of described weight, to the water for injection that wherein adds 100ml, stirring is all dissolved moxifloxacin hydrochloride, adds sodium bicarbonate solution or the sodium bicarbonate powder adjust pH to 5.5 of 1mol/L, and adding water for injection to overall solution volume is 200mL, just filter with 0.45 μ m microporous filter membrane, filtrate is with 0.22 μ m microporous filter membrane fine straining.Gained filtrate is sub-packed in the control antibiotic cillin bottle of 5mL, every bottle of fill 2ml, vacuum lyophilization, freeze-dry process is with embodiment 1.Then outlet, jump a queue, roll lid, the qualified back packing of product inspection is promptly.
Gained Moxifloxacin lyophilized formulations is faint yellow block, and quality is loose, and containing the active medicine moxifloxacin hydrochloride in every bottle, to amount to into Moxifloxacin be 200mg.
Claims (9)
1 one kinds of injection Moxifloxacin or its salt injectable powder and preparation method thereof, it is characterized in that: this lyophilized injectable powder is formed and is comprised Moxifloxacin or its salt, excipient and pH regulator agent, wherein various compositions before lyophilizing in the solution shared percentage composition be: Moxifloxacin or its salt 1～40% (g/100ml, w/v); Excipient 0～80% (g/100ml, w/v); The pH regulator agent is an amount of.
The lyophilized injectable powder of 2 injection Moxifloxacin according to claim 1 or its salt, it is characterized in that wherein the salt of Moxifloxacin comprises for example acid-addition salts example hydrochloric acid salt, acetate, phosphate, sulfate, nitrate, hydrobromate, lactate, citrate, tartrate, oxalates, maleate, fumarate, malate, mesylate, aspartate etc., and with the salt of alkali such as sodium hydroxide, potassium hydroxide etc.
3 according to claim 1 and 2 described Moxifloxacin or its salt freeze-dried powder-injection, it is characterized in that the present invention particularly preferably is Moxifloxacin hydrochlorate (moxifloxacin hydrochloride).
4 Moxifloxacin according to claim 1 or its salt injectable powder, it is characterized in that described excipient is a kind of, any two or more mixture wherein such as lactose, mannitol, dextran 20, dextran 40, dextran 70, glucose, gelatin hydrolysate, sorbitol, Aspartic Acid, glycine, alanine, serine, isoleucine, threonine, glutamic acid, phenylalanine, histidine, valine, cysteine hydrochloride, arginine hydrochloride, sodium chloride, calcium chloride, sucrose, fructose, sodium citrate, sodium ascorbyl phosphate.
5 according to claim 1 and 4 described Moxifloxacin or its salt injectable powder, it is characterized in that a kind of, any two or more mixture among the preferred lactose of excipient, mannitol, dextran, the glucose.
6 according to the Moxifloxacin of claim 1 or the preparation method of its salt lyophilized formulations, it is characterized in that described pH value regulator is a kind of, any two or more the mixture in hydrochloric acid, sulphuric acid, acetic acid, lactic acid, methanesulfonic acid, phosphoric acid, the acid of structure rafter, boric acid, tartaric acid, malic acid, Aspartic Acid, glycine, alanine, serine, isoleucine, threonine, glutamic acid, phenylalanine, histidine, valine, hydrochloric acid half skin propylhomoserin, arginine hydrochloride, sodium carbonate, sodium bicarbonate, the sodium hydroxide etc.
7 according to the Moxifloxacin of claim 1 and 6 or the preparation method of its salt lyophilized formulations, it is characterized in that a kind of, any two or more mixture among the preferred hydrochloric acid of pH value regulator, sodium bicarbonate, the sodium hydroxide.
8 according to the described Moxifloxacin of claim 1 or its salt injectable powder and preparation method thereof, it is characterized in that: under aseptic condition, get recipe quantity Moxifloxacin or its salt and excipient, add the water for injection stirring and make dissolving, transfer pH to proper range with the pH regulator agent, after-teeming is penetrated water to capacity, crosses 0.22 μ m microporous filter membrane, behind the mensuration content, fill is in the control cillin bottle, carry out lyophilization, then outlet, jump a queue, roll lid, the qualified back packing of product inspection is promptly.
9 according to claim 1 and 8 described lyophilized injectable powder and preparation methoies, it is characterized in that its pH value is between 2～8.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510092828 CN1729977A (en) | 2005-08-22 | 2005-08-22 | Freeze dry powdered injection of moxfloxacin or its salts and preparation process thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510092828 CN1729977A (en) | 2005-08-22 | 2005-08-22 | Freeze dry powdered injection of moxfloxacin or its salts and preparation process thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1729977A true CN1729977A (en) | 2006-02-08 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200510092828 Pending CN1729977A (en) | 2005-08-22 | 2005-08-22 | Freeze dry powdered injection of moxfloxacin or its salts and preparation process thereof |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1992626A1 (en) * | 2007-05-10 | 2008-11-19 | Sandoz AG | Process for the preparation of moxifloxacin hydrochloride |
| CN101234116B (en) * | 2006-07-21 | 2010-11-24 | 哈药集团制药总厂 | Powder needle injection containing caderofloxacin lactate |
| CN102100666A (en) * | 2011-01-17 | 2011-06-22 | 南京新港医药有限公司 | New moxifloxacin hydrochloride injection |
| CN102895178A (en) * | 2011-07-29 | 2013-01-30 | 成都国为医药科技有限公司 | Strong solution-type moxifloxacin hydrochloride injection and preparation method thereof |
| CN103919779A (en) * | 2010-09-10 | 2014-07-16 | 杭州民生药业有限公司 | Medicinal composition containing moxifloxacin |
-
2005
- 2005-08-22 CN CN 200510092828 patent/CN1729977A/en active Pending
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101234116B (en) * | 2006-07-21 | 2010-11-24 | 哈药集团制药总厂 | Powder needle injection containing caderofloxacin lactate |
| EP1992626A1 (en) * | 2007-05-10 | 2008-11-19 | Sandoz AG | Process for the preparation of moxifloxacin hydrochloride |
| WO2008138759A1 (en) * | 2007-05-10 | 2008-11-20 | Sandoz Ag | Process for the preparation of moxifloxacin hydrochloride |
| CN103919779A (en) * | 2010-09-10 | 2014-07-16 | 杭州民生药业有限公司 | Medicinal composition containing moxifloxacin |
| CN103919779B (en) * | 2010-09-10 | 2016-02-10 | 杭州民生药业有限公司 | A kind of pharmaceutical composition containing Moxifloxacin |
| CN102100666A (en) * | 2011-01-17 | 2011-06-22 | 南京新港医药有限公司 | New moxifloxacin hydrochloride injection |
| CN102100666B (en) * | 2011-01-17 | 2012-07-18 | 南京新港医药有限公司 | New moxifloxacin hydrochloride injection |
| CN102895178A (en) * | 2011-07-29 | 2013-01-30 | 成都国为医药科技有限公司 | Strong solution-type moxifloxacin hydrochloride injection and preparation method thereof |
| CN102895178B (en) * | 2011-07-29 | 2015-04-08 | 成都国弘医药有限公司 | Strong solution-type moxifloxacin hydrochloride injection and preparation method thereof |
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
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