CN1048628C - Prepn of cyclopropyloxacini injecta - Google Patents
Prepn of cyclopropyloxacini injecta Download PDFInfo
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- CN1048628C CN1048628C CN95111851A CN95111851A CN1048628C CN 1048628 C CN1048628 C CN 1048628C CN 95111851 A CN95111851 A CN 95111851A CN 95111851 A CN95111851 A CN 95111851A CN 1048628 C CN1048628 C CN 1048628C
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- ciprofloxacin
- injection
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Abstract
The present invention provides a method for preparing a ciprofloxacin injection as floqualone antimicrobial medicine. Ciprofloxacin hydrochloride is directly used as raw materials, and reacts with sodium lactate in injection water for generate ciprofloxacin lactate. The method comprises: a solution is diluted to specified concentration by water for injection after isosmotic regulation and solution pH value regulation; the solution is sterilized and filtered, and inert gas is filled into the solution; air in a bottle is displaced, the bottle is sealed; other conventional treatments are carried out, and the ciprofloxacin injection with quality standards consistent with those specified in pharmacopoeia is formed. The method of the present invention has the advantages of convenient technology, no environmental pollution, low cost, etc.
Description
The present invention relates to a kind of preparation method of afloqualone class antimicrobial drug ciprofloxacin injection, belong to field of pharmaceutical preparations.
Ciprofloxacin is succeeded in developing in nineteen eighty-three by German Bayer company the earliest,
Its hydrochlorate, promptly the ciprofloxacin structural formula is:
Molecular formula: C17H18FN3O3HClH2O
Molecular weight: 385,82
The tablet of ciprofloxacin be that the hydrochlorate by ciprofloxacin is that raw material is made, and how its injection is made by the lactate of ciprofloxacin.Because the aqueous solution of ciprofloxacin is placed instability for a long time, blood vessel is also had stimulation, so ciprofloxacin injection can not exist with the form of ciprofloxacin hydrochloride.According to Ger333719 patent report, the preparation of ciprofloxacin injection can be water-soluble by the lactate of ciprofloxacin, and accent etc. blends PH and makes, and also can react generation with lactic acid in solution by ciprofloxacin (claiming the Base body).External listing product (knowing again glad) is to be made by the molten water of ciprofloxacin lactate at present, and its prescription is:
Ciprofloxacin lactate (quite ciprofloxacin) 200mg
Sodium chloride 0.9%
Lactic acid (transferring PH) is an amount of
Water for injection 100ml
Chinese Pharmacopoeia regulation, employed raw material of useful in preparing drug formulations and adjuvant must be administrative department of public health's registration kinds, and its control of product quality standard of being assert is arranged, otherwise must not use in preparation prescription.The above-mentioned ciprofloxacin of mentioning (claiming the Base body) does not carry out the medicine registration in China as yet, it is only for making an intermediate of ciprofloxacin hydrochloride (registered), can not in prescription, directly use, therefore, the preparation of domestic ciprofloxacin injection is raw material with reference to the prescription of external listing product with ciprofloxacin lactate (registered).For obtaining ciprofloxacin lactate, domestic ciprofloxacin injection factory, need ciprofloxacin is changed through chemical reaction, this not only will increase the consersion unit of some, and to consume a large amount of alkali and organic solvent, cause the ciprofloxacin injection cost higher, complex production process.
The purpose of this invention is to provide a kind of is the method that raw material is made the injection of ciprofloxacin lactate by ciprofloxacin and sodium lactate directly, this method technology is easy, non-environmental-pollution, cost is low, has effectively overcome shortcomings such as the technological operation that prior art exists is loaded down with trivial details, cost height.
The object of the present invention is achieved like this: with ciprofloxacin, sodium lactate is raw material, at first sodium lactate solution is diluted in the water for injection, stir and add ciprofloxacin down, after it is fully dissolved, add convention amount isoosmotic adjusting agent-sodium chloride, reuse acid regulator-lactic acid is transferred PH to 3.5-4.5, with injection water it is diluted to normal concentration, carry out sterilising filtration, filling bottle, charge into inert nitrogen gas, air in the displacement bottle outlet after the sealing, promptly gets standard compliant ciprofloxacin injection.
Also reaction solution can be filtered through routine, heated sealed is sterilization treatment again.
The mole ratio of raw materials used ciprofloxacin hydrochloride and sodium lactate is 1: (1-1.05).
Isoosmotic adjusting agent commonly used, except that sodium chloride and, can also adopt anhydrous or water glucose, sorbitol, mannitol are arranged, its conventional amount used generally makes injection satisfy following content requirement and gets final product;
Selecting sodium chloride for use is isoosmotic adjusting agent, and sodium chloride-containing 0.9% in the injection;
Selecting anhydrous glucose for use is isoosmotic adjusting agent, contains anhydrous glucose 5% in the injection;
Selecting dextrose hydrate for use is isoosmotic adjusting agent, contains band water glucose 5.5% in the injection;
Selecting sorbitol for use is isoosmotic adjusting agent, contains sorbitol 5.6% in the injection;
Selecting mannitol for use is isoosmotic adjusting agent, contains mannitol 5% in the injection.
Acid regulator commonly used, except that lactic acid and, still can select organic acid and mineral acids such as glutamic acid, aspartic acid, citric acid, malic acid, ascorbic acid, succinic acid, tartaric acid, acetic acid, boric acid, hydrochloric acid for use, its consumption exceeds with control injection PH3.5-4.5.
Among the present invention, ciprofloxacin and sodium lactate react in water and generate ciprofloxacin lactate, and produced simultaneously sodium chloride has participated in waiting in solution and oozed regulating action.
What adopt the inventive method preparation is the discriminatory analysis that the ciprofloxacin injection of the ciprofloxacin injection of isoosmotic adjusting agent and India's import has carried out chemical analysis with sodium chloride, all is identical identification.Measure through ultraviolet spectral analysis and the three-dimensional collection of illustrative plates of diode display detector, the two collection of illustrative plates is consistent.Show ciprofloxacin injection that adopts the inventive method preparation and the injection that directly is dissolved in gained in the water for injection with ciprofloxacin lactate, though the initiation material difference, the injection composition that finally makes is identical.
Testing result is seen accompanying drawing.
Fig. 1: India produces the ultraviolet spectrogram of ciprofloxacin injection.
Fig. 2: the ciprofloxacin injection ultraviolet spectrogram of Dongbei Pharmaceutical General Factory development.
Fig. 3; India's imported product ciprofloxacin (knowing again glad) injection collection of illustrative plates that I-II detects for HP1040A diode display detector.
Fig. 4; The Dongbei Pharmaceutical General Factory ciprofloxacin injection collection of illustrative plates that I-II detects for HP1040A diode display detector.
Fig. 5; India's imported product ciprofloxacin (knowing again glad) injection collection of illustrative plates that I-VIII detects for HP1040A diode display detector.
The Dongbei Pharmaceutical General Factory ciprofloxacin injection collection of illustrative plates that Fig. 6: I-VIII detects for HP1040A diode display detector.
Fig. 7; India's imported product ciprofloxacin (knowing again glad) injection collection of illustrative plates that I-IV detects for HP1040A diode display detector.
The Dongbei Pharmaceutical General Factory ciprofloxacin injection collection of illustrative plates that Fig. 8: I-IV detects for HP1040A diode display detector.
To the parenteral solution that adopts the inventive method to make, hemolytic test and mistake have been carried out respectively The test of quick property, and carried out long-time stability examination and acute toxicity test, result of the test table Bright, the parenteral solution that the method makes does not contain allergin, no haemolysis, and good stability, Non-toxic and safe, the clinical practice determined curative effect.
Adopting the inventive method to prepare ciprofloxacin injection needs hydrochloric acid ring third with adopting in advance Sha Xing changes into Ciprofloxacin Lactate, makes the method for ciprofloxacin injection again and compares, no Only save chemical industry equipment, and saved a large amount of organic solvents, avoided organic solvent pair The pollution of environment has reduced the loss of Ciprofloxacin Lactate conversion ratio in the conversion process simultaneously, Make its cost about 30%, and operation is greatly easy.
In order further to understand the present invention, see also following embodiment:
The sodium lactate solution of 100mg 70% concentration is diluted in the 80ml water for injection, stir and add ciprofloxacin 233mg down, complete molten back adding 865mg sodium chloride accent etc. oozes, transfer its PH to 3.5-4.5 with lactic acid, with water for injection it is diluted to 100ml again, concentration is 0.2%, carries out sterilising filtration, filling bottle, charge into nitrogen, displacement bottle outlet inner air seal.
Its prescription is:
Ciprofloxacin 233mg (being equivalent to the 200mg ciprofloxacin)
Sodium lactate 100mg (70%)
Sodium chloride 865mg
Lactic acid is an amount of
Water for injection 100ml.
Implementation method 2
The sodium lactate solution of 50mg 70% concentration is diluted in the 8ml water for injection, stir and add ciprofloxacin 116.5mg down, complete molten back adding 72.5mg sodium chloride accent etc. oozes, transfer its PH to 3.5-4.5 with lactic acid, with water for injection it is diluted to 10ml again, concentration is 1%, carries out sterilising filtration, filling bottle, charge into nitrogen, displacement bottle outlet inner air seal.
Its prescription is:
Ciprofloxacin 116.5mg (being equivalent to the 100mg ciprofloxacin)
Sodium lactate (70%) 50mg
Sodium chloride 72.5mg
Lactic acid is an amount of
Water for injection 10ml.
Implementation method 3
The sodium lactate solution of 105mg 70% concentration is diluted in the 80ml water for injection, stir and add ciprofloxacin 233mg down, complete molten back adding 865mg sodium chloride accent etc. oozes, transfer its PH to 3.5-4.5 with lactic acid, with water for injection it is diluted to 100ml again, concentration is 0.2%, carries out sterilising filtration, filling bottle, charge into nitrogen, displacement bottle outlet inner air seal.
Its prescription is:
Ciprofloxacin 233mg
Sodium lactate (70%) 105mg
Sodium chloride 865mg
Lactic acid is an amount of
Water for injection 100ml.
Implementation method 4
The sodium lactate solution of 100mg 70% concentration is diluted in the 80ml water for injection, stir and add ciprofloxacin 233mg down, complete molten back adds anhydrous glucose 5000mg, continue to be stirred to molten entirely, add lactic acid and transfer its PH to 3.5-4.5, with water for injection it is diluted to 100ml again, concentration is 0.2%, carry out sterilising filtration, filling bottle, charge into nitrogen, displacement bottle outlet inner air seal.
Its prescription is:
Ciprofloxacin 233mg
Sodium lactate 100mg (70%)
Anhydrous glucose 5000mg
Lactic acid is an amount of
Water for injection 100ml.
Implementation method 5
In the last example, anhydrous glucose changes into uses mannitol, and all the other operations are the same.
Its prescription is:
Ciprofloxacin 233mg
Sodium lactate (70%) 105mg
Mannitol 5000mg
Lactic acid is an amount of
Water for injection 100ml.
Implementation method 6
Operation is with implementation method 4, and wherein glucose changes sorbitol into.
Its prescription is:
Ciprofloxacin 233mg
Sodium lactate (70%) 100mg
Mannitol 5600mg
Lactic acid is an amount of
Water for injection 100ml.
Implementation method 7
Operation is with implementation method 1, and acid regulator is used aspartic acid instead.
Its prescription is;
Ciprofloxacin 233mg
Sodium lactate (70%) 100mg
Sodium chloride 865mg
Aspartic acid is an amount of
Water for injection 100ml.
Operation is the same.
Its prescription is:
Ciprofloxacin 116.5mg
Sodium lactate (70%) 50mg
Sodium chloride 72.5mg
Acetic acid is an amount of
Water for injection 10ml.
Implementation method 9
Operation is the same.
Its prescription is:
Ciprofloxacin 233mg
Sodium lactate (70%) 100mg
Anhydrous glucose 5000mg
Ascorbic acid is an amount of
Water for injection 100ml.
Claims (3)
1, a kind of preparation method of ciprofloxacin injection, it is characterized in that: with ciprofloxacin and sodium lactate is raw material, at first sodium lactate solution is diluted in the water for injection, stir and add ciprofloxacin down, after it is fully dissolved, add convention amount isoosmotic adjusting agent-sodium chloride, reuse acid regulator-lactic acid is transferred PH to 3.5-4.5, with injection water it is diluted to normal concentration, carry out sterilising filtration, filling bottle, charge into inert nitrogen gas, air in the displacement bottle outlet after the sealing, promptly gets standard compliant ciprofloxacin injection;
Also reaction solution can be filtered through routine, heated sealed is sterilization treatment again;
The mole ratio of raw materials used ciprofloxacin hydrochloride and sodium lactate is 1: (1-1.05).
2, the preparation method of the described ciprofloxacin injection of a kind of claim 1 is characterized in that: isoosmotic adjusting agent also can be selected one or more in anhydrous glucose, dextrose hydrate, sorbitol, the mannitol for use.
3, a kind of preparation method as claimed in claim 1 is characterized in that: used acid regulator also can be selected a kind of in glutamic acid, aspartic acid, boric acid, acetic acid, tartaric acid, citric acid, succinic acid, malic acid, ascorbic acid, the hydrochloric acid for use.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN95111851A CN1048628C (en) | 1995-07-06 | 1995-07-06 | Prepn of cyclopropyloxacini injecta |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN95111851A CN1048628C (en) | 1995-07-06 | 1995-07-06 | Prepn of cyclopropyloxacini injecta |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1115641A CN1115641A (en) | 1996-01-31 |
| CN1048628C true CN1048628C (en) | 2000-01-26 |
Family
ID=5079090
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN95111851A Expired - Fee Related CN1048628C (en) | 1995-07-06 | 1995-07-06 | Prepn of cyclopropyloxacini injecta |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1048628C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8187632B2 (en) | 2000-06-26 | 2012-05-29 | Bayer Schering Pharma Ag | Sustained-release preparations of quinolone antibiotics |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101884612A (en) * | 2010-06-29 | 2010-11-17 | 上海华中药业有限公司 | Preparation method of large volume ribavirin injection |
| CN102274169A (en) * | 2011-07-27 | 2011-12-14 | 安徽环球药业股份有限公司 | Preparation method of ciprofloxacin lactate sodium chloride injection |
| CN102716072B (en) * | 2012-06-13 | 2014-06-18 | 广州南新制药有限公司 | Method for preparing ciprofloxacin lactate sodium chloride injection |
| CN103977006B (en) * | 2014-05-30 | 2016-06-08 | 成都乾坤动物药业有限公司 | A kind of pharmaceutical composition treating mammitis of cow and its production and use |
| CN108938636A (en) * | 2018-09-10 | 2018-12-07 | 贵州天地药业有限责任公司 | A kind of preparation method of Ciprofloxacin Lactate and Sodium Chloride Injection |
| CN110693828A (en) * | 2019-11-22 | 2020-01-17 | 天津金耀集团湖北天药药业股份有限公司 | Ciprofloxacin glucose injection and preparation process thereof |
| CN114767627B (en) * | 2022-05-17 | 2024-05-31 | 广州南鑫药业有限公司 | Preparation method of ciprofloxacin lactate sodium chloride injection |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5531028A (en) * | 1978-08-25 | 1980-03-05 | Dai Ichi Seiyaku Co Ltd | Injection |
-
1995
- 1995-07-06 CN CN95111851A patent/CN1048628C/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5531028A (en) * | 1978-08-25 | 1980-03-05 | Dai Ichi Seiyaku Co Ltd | Injection |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8187632B2 (en) | 2000-06-26 | 2012-05-29 | Bayer Schering Pharma Ag | Sustained-release preparations of quinolone antibiotics |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1115641A (en) | 1996-01-31 |
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