CN101264054A - Rifamycin sodium injection and preparation thereof - Google Patents
Rifamycin sodium injection and preparation thereof Download PDFInfo
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- CN101264054A CN101264054A CNA200810098144XA CN200810098144A CN101264054A CN 101264054 A CN101264054 A CN 101264054A CN A200810098144X A CNA200810098144X A CN A200810098144XA CN 200810098144 A CN200810098144 A CN 200810098144A CN 101264054 A CN101264054 A CN 101264054A
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- rifamycin
- rifamycin sodium
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Abstract
The invention relates to a rifamycin sodium injection and the preparation method which enhance the stability of the rifamycin sodium and the quality is stabilized. The invention is characterized in that in every 1000ml injection comprising 35 to 65g rifamycin sodium, 0.1 to 10g vitamin C sodium, 0.1 to 10g glycine, 500 to 900ml organic solvent for injection, the rest is injection water. The production procedure of the injection is: the injection water of proper amount is added into the antioxidant and solution stabilizer for disolving; then the pH value is adjusted; the organic solvent for injection of proper amount is added and blended well; the rifamycin sodium is added and agitated to dissolve and is made rough filteration; and then the solution is filtered by the 0.22 Mum microporous filtering column and is filled into the bottle; then the nitrogen is filled, sealing is made, vapor is circulated, sterilization is continued for 30m; after inspecing and packaging, the injection is obtained.
Description
Technical field
The present invention relates to a kind of injection and production method thereof, particularly relate to rifamycin sodium injection and production method thereof.
Background technology
Rifamycin sodium injection is the broad spectrum antibiotic of semi-synthetic rifamycin apoplexy due to endogenous wind, its mechanism of action is the activity that specificity suppresses RNA polymerase in the tuberculosis thalline, suppress the synthetic of bacteria RNA and tropina, cause bacterial reproduction to stop and reaching the sterilization purpose, with other antitubercular agent combined chemotherapy, Synergistic.
Rifamicina can be used for treating each the paratuberculosis disease that is caused by mycobacterium tuberculosis, is used for the treatment of by the microbial following infection of sensitivity: infect in respiratory tract infection, surgical infection, urinary tract infection, otorhinolaryngology infection, peritonitis, cholecystitis, cholangitis and other abdomen; Septicemia, skin and soft tissue infection; Pelvic inflammatory disease, endometritis, gonorrhea and genital infection etc. and the various tuberculosis diseases that cause by mycobacteria.
So rifamicina malabsorption is clinical employing intramuscular injection or intravenous injection.Injection back distributes with liver and bile for the highest, also can reach treatment concentration at kidney, lung, the heart, spleen.
The rifamycin sodium injection impurity content of producing is higher at present, and it is very fast that room temperature condition is placed degraded down, influences curative effect of medication.
Summary of the invention
The purpose of this invention is to provide a kind of stable rifamycin sodium injection, its active component is a rifamicina, and rifamycin sodium injection is made in adding adjuvant sodium ascorbate, glycine, water for injection, injection organic solvent and pH regulator agent; Contain rifamicina 35～65g in every 1000ml rifamycin sodium injection.
Solution stabilizer of the present invention is a glycine; When the glycine amount ranges in every 1000ml injection, when described solution stabilizer contained 0.1～10g, the rifamycin sodium injection impurity content of preparation was low, product quality height, and good stability.
PH regulator agent of the present invention is a kind of in sodium hydroxide, sodium carbonate, the carboprost tromethamine.
In addition, the production method of rifamycin sodium injection of the present invention to produce the 1000ml injection, comprises the steps:
(1) with sodium ascorbate 0.1～10g and glycine 0.1～10g, add water for injection 100～500ml and make dissolving, regulate pH to 7.0～9.0, add among injection organic solvent 500～900ml mix homogeneously.
(2) add rifamicina 35～65g, stir and make dissolving.
(3) medicinal liquid adds remaining organic solvent and water for injection to full dose through coarse filtration, and mix homogeneously is regulated pH to 6.5～8.5.
(4) medicinal liquid reuse 0.22 μ m micropore filter post filters the back fill, and inflated with nitrogen seals.
(5) 100 ℃ of sterilizations of flowing steam are 30 minutes, cooling, and check, packing, promptly.
The specific embodiment
Embodiment one
A kind of production method of rifamycin sodium injection comprises the steps:
(1) with sodium ascorbate 1g and glycine 1g, add water for injection and make dissolving in right amount, transfer pH7.0～9.0 with trometamol solution, add among the propylene glycol 500ml mix homogeneously.
(2) add rifamicina 50g, stir and make dissolving.
(3) medicinal liquid adds remaining propylene glycol and water for injection to full dose through coarse filtration, and mix homogeneously is regulated pH to 6.5～8.5.
(4) medicinal liquid reuse 0.22 μ m micropore filter post filters the back fill, and inflated with nitrogen seals.
(5) 100 ℃ of sterilizations of flowing steam are 30 minutes, cooling, and check, packing, promptly.
Embodiment two
A kind of production method of rifamycin sodium injection comprises the steps:
(1) with sodium ascorbate 0.1g and glycine 0.1g, add water for injection and make dissolving in right amount, regulate pH to 7.0～9.0 with sodium hydroxide solution, add among the ethanol 900ml mix homogeneously.
(2) add rifamicina 35g, stir and make dissolving.
(3) medicinal liquid adds to the full amount of water for injection through coarse filtration, and mix homogeneously is regulated pH to 6.5～8.5.
(4) medicinal liquid reuse 0.22 μ m micropore filter post filters the back fill, and inflated with nitrogen seals.
(5) 100 ℃ of sterilizations of flowing steam are 30 minutes, cooling, and check, packing, promptly.
Embodiment three
A kind of production method of rifamycin sodium injection comprises the steps:
(1) with sodium ascorbate 10g and glycine 10g, add water for injection and make dissolving in right amount, regulate pH to 7.0～9.0 with sodium carbonate liquor, add in the 500ml PEG400 mix homogeneously.
(2) add rifamicina 65g, stir and make dissolving.
(3) medicinal liquid adds remaining PEG400 and water for injection to full dose through coarse filtration, and mix homogeneously is transferred pH6.5～8.5.
(4) medicinal liquid reuse 0.22 μ m micropore filter post filters the back fill, and inflated with nitrogen seals.
(5) 100 ℃ of sterilizations of flowing steam are 30 minutes, cooling, and check, packing, promptly.
Embodiment four
A kind of production method of rifamycin sodium injection comprises the steps:
(1) with sodium ascorbate 1g and glycine 1g, add water for injection and make dissolving in right amount, regulate pH to 7.0～9.0 with trometamol solution, add among the propylene glycol 750ml mix homogeneously.
(2) add rifamicina 50g, stir and make dissolving.
(3) medicinal liquid adds remaining propylene glycol and water for injection to full dose through coarse filtration, and mix homogeneously is regulated pH to 6.5～8.5.
(4) medicinal liquid reuse 0.22 μ m micropore filter post filters the back fill, and inflated with nitrogen seals.
(5) 100 ℃ of sterilizations of flowing steam are 30 minutes, cooling, and check, packing, promptly.
Experimental example 1
This experimental example is the screening test of glycine in the product of the present invention.
Owing to consider that this product principal agent rifamicina and fixed adjuvant sodium ascorbate are the material of less stable, and in line with the principle of selecting adjuvant as few as possible for use, add an amount of solution stabilizer in the design prescription, to keep the heat stability and the long-time stability of preparation.
Through a large amount of trial test researchs, filter out with glycine as solution stabilizer, and the lab scale sample to existing prescription, after not adding glycine and adding glycine is compared, appearance character inspection and related substance inspection have been carried out emphatically (for easy to detect, adopt the high performance liquid chromatography area normalization method as inspection method), the results are shown in Table 1.
Table 1 result of the test
| Inspection item | Existing prescription | Do not add the glycine prescription | Add the glycine prescription |
| Appearance character | The kermesinus clear liquid | The kermesinus clear liquid | The kermesinus clear liquid |
| Total impurities % | 1.78 | 2.13 | 1.01 |
Result of the test: by testing result as can be known, add glycine rear impurity total amount and obviously reduce.
Experimental example 2
This experimental example is the stability experiment parameter of product of the present invention.
We have carried out the test that keeps sample of constant temperature accelerated test, room temperature to the rifamycin sodium injection of trial-production, its stability has been carried out preliminary investigation, press rifamycin sodium injection national drug standards WS-10001-(HD-0138)-2002 assay method, sample character, clarity, acid-base value, related substance, content project are detected.
Sample is that Shuangding Pharmaceutical Co., Ltd., Shenyang adopts embodiment one formulation and technology to make three batch samples by oneself, and lot number is respectively 030101,030102,030103; Control sample is the existing commercially available sample that Shuangding Pharmaceutical Co., Ltd., Shenyang produces, and lot number is 021201.
1. accelerated test
Get this product, press commercially available back, put 40 ℃ ± 2 ℃, relative humidity and be in 75% ± 5% the calorstat, place, take a sample when 0,1,2,3,6 the end of month, the method inspection by stipulating in the quality standard the results are shown in Table 2.
Table 2 accelerated test result
Accelerated test result shows: this product is under 40 ℃ ± 2 ℃ relative humidity 75% conditions, and in 6 months of having investigated, the every index of test specimen does not have significant change, and relatively has good stability with existing control sample.
2. the room temperature test that keeps sample
Get this product, press commercially available back, placing 25 ℃ ± 2 ℃, relative humidity is that respectively at sampling in 0,3,6,9,12,18,24 month, the method inspection by stipulating in the quality standard the results are shown in Table 3 under 60% ± 10% the condition.
Table 3 long term test is investigated the result
Keep sample for a long time and investigate result of the test and show: this product is under 25 ℃ ± 2 ℃, RH60 ± 10% condition, and in 24 months of having investigated, every index does not have significant change, and relatively has good stability with existing control sample.
Through the preliminarily stabilised evidence: rifamycin sodium injection keeps sample through constant temperature accelerated test and room temperature and investigates test and think that this product is stable; Compare with existing street drug rifamycin sodium injection, content and determination of related substances result obviously are better than commercially available sample.
The present invention shows that through comparative study preparation of the present invention and prescription all are better than existing known technology at aspects such as stability, bioavailability, infiltration rate, preparation method, industrialization, obtained beyond thought technique effect.
Claims (9)
1. a rifamycin sodium injection is characterized in that comprising the rifamicina as effective ingredient, and as sodium ascorbate, glycine, water for injection, injection organic solvent and the pH regulator agent of adjuvant; Wherein the every 1000ml of this rifamycin sodium injection contains rifamicina 35～65g.
2. rifamycin sodium injection according to claim 1 is characterized in that in every 1000ml injection, described glycine is 0.1～10g.
3. rifamycin sodium injection according to claim 1 is characterized in that in every 1000ml injection, described sodium ascorbate is 0.1～10g.
4. rifamycin sodium injection according to claim 1 is characterized in that described injection organic solvent is at least a in ethanol, propylene glycol, the PEG400.
5. rifamycin sodium injection according to claim 1 is characterized in that described pH regulator agent is at least a in sodium hydroxide, sodium carbonate, the trometamol.
6. the preparation method of the described rifamycin sodium injection of claim 1 is characterized in that, comprises the steps: in preparation 1000ml rifamycin sodium injection
1) with sodium ascorbate and glycine, add water for injection and make dissolving, regulate pH value to 7.0～9.0, add among injection organic solvent 500～900ml mix homogeneously;
2) add rifamicina 35～65g, stir and make dissolving;
3) in medicinal liquid, add remaining organic solvent and water for injection to full dose, mix homogeneously, regulating pH value is 6.5～8.5;
4) fill behind the medical filtration, inflated with nitrogen seals;
5) flowing steam sterilization, cooling, check.
7. the preparation method of rifamycin sodium injection according to claim 6 is characterized in that the amount of the glycine that adds is 0.1～10g.
8. the preparation method of rifamycin sodium injection according to claim 7 is characterized in that the amount of the sodium ascorbate that adds is 0.1～10g.
9. the preparation method of rifamycin sodium injection according to claim 8 is characterized in that described injection organic solvent is at least a in ethanol, propylene glycol, the PEG400.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200810098144XA CN101264054A (en) | 2008-05-19 | 2008-05-19 | Rifamycin sodium injection and preparation thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200810098144XA CN101264054A (en) | 2008-05-19 | 2008-05-19 | Rifamycin sodium injection and preparation thereof |
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| CN101264054A true CN101264054A (en) | 2008-09-17 |
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| CNA200810098144XA Pending CN101264054A (en) | 2008-05-19 | 2008-05-19 | Rifamycin sodium injection and preparation thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579327A (en) * | 2012-02-12 | 2012-07-18 | 王伟志 | Rifamycin SV sodium injection and preparation method thereof |
| CN103908674A (en) * | 2014-01-21 | 2014-07-09 | 邓学峰 | Rifamycin sodium combinatorial drug |
| CN112386572A (en) * | 2020-12-18 | 2021-02-23 | 艾美科健（中国）生物医药有限公司 | Gamithromycin injection and preparation method thereof |
-
2008
- 2008-05-19 CN CNA200810098144XA patent/CN101264054A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579327A (en) * | 2012-02-12 | 2012-07-18 | 王伟志 | Rifamycin SV sodium injection and preparation method thereof |
| CN103908674A (en) * | 2014-01-21 | 2014-07-09 | 邓学峰 | Rifamycin sodium combinatorial drug |
| CN112386572A (en) * | 2020-12-18 | 2021-02-23 | 艾美科健（中国）生物医药有限公司 | Gamithromycin injection and preparation method thereof |
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Open date: 20080917 |