CN104940133A - Fluconazole injection and preparation method thereof - Google Patents
Fluconazole injection and preparation method thereof Download PDFInfo
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- CN104940133A CN104940133A CN201510320605.3A CN201510320605A CN104940133A CN 104940133 A CN104940133 A CN 104940133A CN 201510320605 A CN201510320605 A CN 201510320605A CN 104940133 A CN104940133 A CN 104940133A
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- fluconazole
- glucose
- injection
- glycine
- fluconazol
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Abstract
The invention provides a fluconazole glucose injection which comprises fluconazole, glucose, glycine and citric acid according to a specific ratio. The added glycine and citric acid in the fluconazole injection have functions of a cosolvent and a stabilizer; the product stability can be enhanced, the generation of related substances is reduced, the product always keeps high quality and high stability in the production and storage processes, and clinical use is facilitated. Meanwhile, the fluconazole glucose injection is simple in production process, auxiliary materials are easy to obtain, and the production cost can be reduced.
Description
Technical field
The present invention relates to a kind of fluconazole and glucose injection and preparation method thereof, belong to field of pharmaceutical preparations.
Background field
Fluconazol is white crystals or crystalline powder, odorless, and slightly soluble in water is insoluble in ethanol, acetone, chloroform.Fluconazol is a kind of antifungal drug in triazole class, has spectrum antifungal effect, can the black alcohol synthesis of optionally Antifungi, and inhibitory action fungal cytochrome P-450 being relied on to enzyme has high selectivity.It has good antibacterially to rent to cryptococcus, Candida in vivo and in vitro, is the choice drug of clinical anti-fungal infection.
There is heat stability, problem that its related substances is higher in the fluconazole and glucose injection sold, be unfavorable for the safety of medication in producing and storing.
Summary of the invention:
The present invention, by groping and many experiments, finds to be dissolved in by fluconazol in glucose, glycine, citron aqueous acid, can significantly improve the stability of fluconazole and glucose injection, significantly reduce the generation of related substance.
Technical solution of the present invention comprises:
A kind of fluconazole and glucose injection, containing fluconazol, glucose, glycine, citric acid.
Wherein, the weight ratio of fluconazol, glucose, glycine, citric acid is 2-5:40:1.8-2:1.3-1.5; Preferred proportion is 3:40:1.8:1.3.
The invention provides a kind of preparation method of above-mentioned fluconazole and glucose injection, the glucose of recipe quantity, glycine, citric acid is water-soluble, then fluconazol is added, after dissolving, adjust ph is 5.5-5.6, inject water to 1000ml, filtering with microporous membrane, obtain fluconazole and glucose injection.
Compared with prior art, fluconazole and glucose injection tool of the present invention has the following advantages:
The glycine added in injection and citric acid have the effect of cosolvent and stabilizing agent for fluconazol; Can product stability be strengthened, reduce the generation of related substance, make product remain high-quality, high stability in production and storage process, be conducive to Clinical practice.Meanwhile, fluconazole and glucose injection production technology of the present invention is simple, and adjuvant is easy to get, and can reduce production cost.
Detailed description of the invention:
Further illustrate the present invention by the following examples, but these embodiments do not limit the present invention in any way.Detection method and standard perform 2010 editions Chinese Pharmacopoeias.
Embodiment 1
Formula is as follows:
Preparation technology: by water-soluble to glucose, glycine and citric acid, stirs and makes it dissolve, then add fluconazol, stirring makes it dissolve, the sodium hydroxide adjust ph using 0.1mol/L is 5.5, and inject and be settled to 1000ml with water, namely filtering with microporous membrane obtains fluconazole and glucose injection.
Embodiment 2
Formula is as follows:
Preparation technology: with embodiment 1, wherein, the sodium hydroxide adjust ph using 0.1mol/L is 5.5.
Embodiment 3
Formula is as follows:
Preparation technology: with embodiment 1, wherein, the sodium hydroxide adjust ph using 0.1mol/L is 5.6.
Embodiment 4
Formula is as follows:
Preparation technology: with embodiment 1, wherein, the sodium hydroxide adjust ph using 0.1mol/L is 5.6.
Comparative example 1
Formula is as follows:
Fluconazol 2500mg
Glucose 50000mg
Inject water to 1000ml.
Preparation technology: glucose, fluconazol is water-soluble, stirs and makes it dissolve, and the sodium hydroxide adjust ph using 0.1mol/L is 5.6, and inject and be settled to 1000ml with water, namely filtering with microporous membrane obtains fluconazole and glucose injection.
Comparative example 2
Formula is as follows:
Preparation technology: fluconazol, glucose, glycine is water-soluble, and stir and make it dissolve, the sodium hydroxide adjust ph using 0.1mol/L is 5.6, and inject and be settled to 1000ml with water, namely filtering with microporous membrane obtains fluconazole and glucose injection.
Comparative example 3
Formula is as follows:
Preparation technology: fluconazol, glucose, glycine, citric acid is water-soluble, and stir and make it dissolve, the sodium hydroxide adjust ph using 0.1mol/L is 5.6, and inject and be settled to 1000ml with water, namely filtering with microporous membrane obtains fluconazole and glucose injection.
Comparative example 4
Formula is as follows:
Preparation technology is with comparative example 3
Comparative example 5
Formula is as follows:
Preparation technology: fluconazol, glucose, malic acid, sodium sulfite is water-soluble, and stir and make it dissolve, the sodium hydroxide adjust ph using 0.1mol/L is 5.6, and inject and be settled to 1000ml with water, namely filtering with microporous membrane obtains fluconazole and glucose injection.
Comparative example 6
Formula is as follows:
Preparation technology: fluconazol, glucose, sodium sulfite, glycine is water-soluble, stirring makes it dissolve, the sodium hydroxide adjust ph using 0.1mol/L is 5.6, and inject and be settled to 1000ml with water, namely filtering with microporous membrane obtains fluconazole and glucose injection.
Embodiment 7
Formula is as follows:
Preparation technology: molten to fluconazol, glucose, glycine and citric acid are together added to the water, stir and make it dissolve, dissolution time is 25mim, than the 15min of embodiment, long 10min, filter after activated carbon adsorption, sodium hydroxide is used to regulate pH to be 5.9, filtering with microporous membrane.
Checking embodiment 1:
Be positioned in the climatic chamber of 60 DEG C by the product that above-mentioned 4 embodiments and 7 comparative examples obtain, detect in sampling in the 5th, 10 day, result compared with 0 day.Related substance, content press high effective liquid chromatography for measuring, and concrete outcome is in table 1
Table 1
Data from table 1: embodiment 1-4: select the glycine of special ratios and citric acid as cosolvent and stabilizing agent, and specific preparation method, more excellent in, drug content less in visible foreign matters, pH stability, its related substances than comparative example 1-7, significantly can increase the dissolubility of fluconazol in water, and significantly improve the stability of fluconazole injection.
Stability test 2: long-term stable experiment
The fluconazole injection of the fluconazole injection prepared by embodiment of the present invention 1-4 and comparative example 1-7 carries out long-time stability investigation (40 DEG C, RH is 75%), the results are shown in Table 2:
Table 2
As seen from the results in Table 2: embodiment 1-4 than comparative example 1-7 character, visible foreign matters, pH stability, its related substances, drug content and aseptic in more excellent, significantly can increase the long-time stability of fluconazole injection.
Claims (3)
1. a fluconazole and glucose injection, is characterized in that, it comprises fluconazol, glucose, glycine, citric acid; And the weight ratio of fluconazol, glucose, glycine, citric acid is 2-5:40:1.8-2:1.3-1.5.
2. the preparation method of a kind of fluconazole and glucose injection as claimed in claim 1, is characterized in that, the weight ratio of described fluconazol, glucose, glycine, citric acid is 3:40:1.8:1.3.
3. the preparation method of a kind of fluconazole and glucose injection as claimed in claim 1 or 2, it is characterized in that, method is as follows: the glucose of recipe quantity, glycine, citric acid is water-soluble, then fluconazol is added, after dissolving, adjust ph is 5.5-5.6, injects water to 1000ml, filtering with microporous membrane, obtains fluconazole and glucose injection.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510320605.3A CN104940133A (en) | 2015-06-11 | 2015-06-11 | Fluconazole injection and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510320605.3A CN104940133A (en) | 2015-06-11 | 2015-06-11 | Fluconazole injection and preparation method thereof |
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| CN104940133A true CN104940133A (en) | 2015-09-30 |
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| CN201510320605.3A Pending CN104940133A (en) | 2015-06-11 | 2015-06-11 | Fluconazole injection and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106265540A (en) * | 2016-08-31 | 2017-01-04 | 安徽省润生医药股份有限公司 | A kind of good fortune department fluconazol lyophilized formulations compositions and preparation method thereof |
| CN106902077A (en) * | 2017-03-03 | 2017-06-30 | 安徽环球药业股份有限公司 | The compound method of fluorine exchange |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1442138A (en) * | 2003-04-07 | 2003-09-17 | 江西制药有限责任公司 | Fukangzuo injection fluid and its preparation method |
| CN1565446A (en) * | 2003-06-17 | 2005-01-19 | 刘智 | Freeze-drying fluconazole injection and its preparation method |
| CN104027304A (en) * | 2014-06-04 | 2014-09-10 | 回音必集团(江西)东亚制药有限公司 | Citicoline sodium glucose injection |
-
2015
- 2015-06-11 CN CN201510320605.3A patent/CN104940133A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1442138A (en) * | 2003-04-07 | 2003-09-17 | 江西制药有限责任公司 | Fukangzuo injection fluid and its preparation method |
| CN1565446A (en) * | 2003-06-17 | 2005-01-19 | 刘智 | Freeze-drying fluconazole injection and its preparation method |
| CN104027304A (en) * | 2014-06-04 | 2014-09-10 | 回音必集团(江西)东亚制药有限公司 | Citicoline sodium glucose injection |
Non-Patent Citations (2)
| Title |
|---|
| 付桂英等: "注射用氟康唑的制备工艺及稳定性研究", 《中国药房》 * |
| 国家药典委员会: "《国家食品药品监督管理局 国家药品标准 新药转正标准 第64册》", 31 March 2008 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106265540A (en) * | 2016-08-31 | 2017-01-04 | 安徽省润生医药股份有限公司 | A kind of good fortune department fluconazol lyophilized formulations compositions and preparation method thereof |
| CN106902077A (en) * | 2017-03-03 | 2017-06-30 | 安徽环球药业股份有限公司 | The compound method of fluorine exchange |
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Application publication date: 20150930 |