CN104013584A - Thiamphenicol freeze-dried powder - Google Patents
Thiamphenicol freeze-dried powder Download PDFInfo
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- CN104013584A CN104013584A CN201410269840.8A CN201410269840A CN104013584A CN 104013584 A CN104013584 A CN 104013584A CN 201410269840 A CN201410269840 A CN 201410269840A CN 104013584 A CN104013584 A CN 104013584A
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- thiamphenicol
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- dried powder
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- valine
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Abstract
The invention relates to thiamphenicol freeze-dried powder, wherein the thiamphenicol freeze-dried powder is prepared from the following raw materials: 5g of thiamphenicol, 0.8g of tartaric acid, 1g of lecithin, 0.5g of valine, 8g of sodium chloride, 4g of mannitol and 1000ml of injection water.
Description
Technical field
The present invention relates to thiamphenicol freeze-dried powder.
Background technology
Thiamphenicol English/latin name: Thiamphenicol, another name thiomycin, thiamphenicol.This product is white crystalline powder; Odorless.
Thiamphenicol is synthetic broad ectrum antibiotic, is the substitute of chloromycetin, and vivo bacteria corrosion action is better than chloromycetin, and toxicity is less than chloromycetin.Thiamphenicol poorly water-soluble, dosage form and clinical practice are restricted.
Thiamphenicol is by synthetic the working of albumen of anti-bacteria; mainly to be reversibility with the ribosomal 50s subunit of the 70s of antibacterial to be combined; peptide for inhibiting acyltransferase; thereby stop specifically the receptors bind on aminoacyl tRNA and ribosome, suppress peptide chain prolongation and tropina can not be synthesized.Both have identical antimicrobial spectrum, whole gram positive bacterias, negative bacterium are had to very strong antimicrbial power, infect for various bacteria as: hemophilus influenza, streptococcus pneumoniae and Neisseria meningitidis, the anaerobe such as staphylococcus aureus, micrococcus scarlatinae, Streptococcus viridans, B group Hemolytic streptococcus, escherichia coli, Klebsiella Pneumoniae, proteus mirabilis, Salmonella typhi, bacillus paratyphosus, Shigella, bacteroides fragilis.Document is recorded and long-term is widely applied the existing serious untoward reaction of thiamphenicol, therefore be widely used in clinically, is mainly used in treating various surface infections, biliary tract infection, urinary tract infection, respiratory tract infection, Weber Christian disease etc.
Many countries are mainly used for veterinary drug by thiamphenicol, but can also be used for the treatment of human diseases at Chinese and this antibiotic of Italy.In Brazil, the application of thiamphenicol is also very extensive.
Thiamphenicol mainly contains the dosage forms such as tablet, capsule, injection at present for clinical, and these dosage forms are poor at gastrointestinal tract dissolution, and bioavailability is not high.
Present inventor, through repetition test, determines and adopts specific cosolvent can significantly strengthen the dissolubility of thiamphenicol in water, and then be prepared into thiamphenicol freeze-dried powder.
Summary of the invention
The invention provides a kind of stable thiamphenicol freeze-dried powder and preparation method thereof, described thiamphenicol freeze-dried powder adjuvant is less, good stability, and clinical safety in utilization is higher.
The invention provides a kind of thiamphenicol freeze-dried powder, wherein active component is thiamphenicol.
The invention provides a kind of thiamphenicol freeze-dried powder, comprising cosolvent.
The invention provides a kind of thiamphenicol freeze-dried powder, wherein cosolvent is the compositions of tartaric acid, lecithin and valine.
The invention provides a kind of thiamphenicol freeze-dried powder, wherein thiamphenicol freeze-dried powder is made up of following raw material: 5g thiamphenicol, 0.8g tartaric acid, 1g lecithin, 0.5g valine, 8g sodium chloride, 4g mannitol, 1000ml water for injection.
The present invention also provides the preparation method of above-mentioned thiamphenicol freeze-dried powder:
1, get tartaric acid, lecithin and the valine of recipe quantity, add the water for injection of 50% amount, be heated to 50～55 DEG C, stir it is dissolved, the thiamphenicol of getting recipe quantity adds in solution, continues to stir 15 minutes after stirring and dissolving.
2, get sodium chloride and the mannitol of recipe quantity, add the water for injection of 40% amount, stir and make its dissolving.
3,1,2 solution are merged, add to the full amount of water for injection, add 0.15% needle-use activated carbon, stir 25 minutes, filter decarburization, intermediate inspection, qualified rear use 0.22 μ m membrane filtration degerming.
4, filtrate is poured in cillin bottle, carry out lyophilization, obtain freeze-dried powder, after the assay was approved, packaging.
Inventor finds amazedly, use the tartaric acid of specified quantitative and the combination of lecithin as cosolvent, and add the valine of specified quantitative, can significantly increase the dissolubility of thiamphenicol in water, the thiamphenicol freeze-dried powder stability preparing is high, and its related substances is few.And thiamphenicol freeze-dried powder adjuvant of the present invention is less, good stability, clinical safety in utilization is higher.
Detailed description of the invention
Below test further illustrates the present invention:
The investigation of cosolvent
The dissolving of thiamphenicol needs cosolvent, and we investigate several cosolvents.Respectively getting 1g thiamphenicol adds and adds respectively in the 200ml water of various cosolvents in advance.Place 10 hours at 60 DEG C, investigate the variation of thiamphenicol content, the results are shown in Table 1:
Table 1
Result of the test surface, place after 10 hours for 60 DEG C, the thiamphenicol content that various cosolvents dissolve increases not obvious, but the sample size that makees cosolvent by tartaric acid, lecithin and valine compositions obviously increases, even than tartaric acid and lecithin, the two is combined more as cosolvent increase, and compositions of this explanation tartaric acid, lecithin and valine three can significantly increase the dissolubility of thiamphenicol in water.
Further study us and surprisingly find that the tartaric acid of specified quantitative and the quality stability using improving thiamphenicol of combining of lecithin and valine have played beyond thought remarkable result.
Embodiment 1:
Technique:
1, get tartaric acid, lecithin and the valine of recipe quantity, add the water for injection of 50% amount, be heated to 50～55 DEG C, stir it is dissolved, the thiamphenicol of getting recipe quantity adds in solution, continues to stir 15 minutes after stirring and dissolving.
2, get sodium chloride and the mannitol of recipe quantity, add the water for injection of 40% amount, stir and make its dissolving.
3,1,2 solution are merged, add to the full amount of water for injection, add 0.15% needle-use activated carbon, stir 25 minutes, filter decarburization, intermediate inspection, qualified rear use 0.22 μ m membrane filtration degerming.
4, filtrate is poured in cillin bottle, carry out lyophilization, obtain freeze-dried powder, after the assay was approved, packaging.
Control Example 1:
Preparation method is with embodiment 1.
Control Example 2:
Preparation method is with embodiment 1.
Control Example 3:
Preparation method is with embodiment 1.
Control Example 4:
Preparation method is with embodiment 1.
Control Example 5:
Preparation method is with embodiment 1.
Control Example 6:
Preparation method is with embodiment 1.
Control Example 7
Preparation method is with embodiment 1.
Control Example 8
Preparation method is with embodiment 1.
Control Example 1-8 adjusts the adjuvant or the weight that use in embodiment 1, and concrete situation of change is as follows:
| Group | Situation of change |
| Embodiment 1 | - |
| Comparative example 1 | Without lecithin and valine |
| Comparative example 2 | Without tartaric acid and valine |
| Comparative example 3 | Without tartaric acid and lecithin |
| Comparative example 4 | Without valine |
| Comparative example 5 | Without lecithin |
| Comparative example 6 | Without tartaric acid |
| Comparative example 7 | Consumption changes |
| Comparative example 8 | Use Macrogol 2000, polyvidone and glycine to replace tartaric acid, lecithin and valine |
The product that above-described embodiment 1 and control Example 1-8 are made is positioned in 60 DEG C of climatic chambers, in sampling calibrating in the 5th, 10 days, and result and comparison (in table 2) in 0 day:
Related substance, content are pressed high effective liquid chromatography for measuring.
Table 2
Result shows: embodiment 1 and control Example 1-8 comparison, and related substance, stable content have obvious advantage, and the use of combining of tartaric acid and lecithin and valine is used more separately the stability that can obviously strengthen thiamphenicol freeze-dried powder.
Thiamphenicol freeze-dried powder prepared by the embodiment of the present invention 1 and control Example 1-8 carry out long-time stability investigation (25 DEG C ± 2 DEG C, RH60% ± 10%), the results are shown in Table 3:
Table 3
Result shows: rifampicin freeze-dried powder (embodiment 1) prepared by the present invention is compared with control Example 1-8, and quality stability increases significantly.
Claims (4)
1. a thiamphenicol freeze-dried powder, wherein active component is thiamphenicol.
2. a kind of thiamphenicol freeze-dried powder as claimed in claim 1, comprising cosolvent.
3. a kind of thiamphenicol freeze-dried powder as claimed in claim 2, wherein cosolvent is the compositions of tartaric acid, lecithin and valine.
4. a thiamphenicol freeze-dried powder, wherein thiamphenicol freeze-dried powder is made up of following raw material: 5g thiamphenicol, 0.8g tartaric acid, 1g lecithin, 0.5g valine, 8g sodium chloride, 4g mannitol, 1000ml water for injection.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410269840.8A CN104013584B (en) | 2014-06-17 | 2014-06-17 | Thiamphenicol freeze-dried powder |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410269840.8A CN104013584B (en) | 2014-06-17 | 2014-06-17 | Thiamphenicol freeze-dried powder |
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| CN104013584A true CN104013584A (en) | 2014-09-03 |
| CN104013584B CN104013584B (en) | 2016-06-29 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101361729A (en) * | 2008-09-25 | 2009-02-11 | 沈阳双鼎科技有限公司 | Thiamphenicol aminoacetate hydrochloride sterile freeze-drying preparation for injection and preparation method thereof |
| CN103536540A (en) * | 2013-09-16 | 2014-01-29 | 南通丝乡丝绸有限公司 | Rifampin lyophilized powder and preparation method thereof |
-
2014
- 2014-06-17 CN CN201410269840.8A patent/CN104013584B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101361729A (en) * | 2008-09-25 | 2009-02-11 | 沈阳双鼎科技有限公司 | Thiamphenicol aminoacetate hydrochloride sterile freeze-drying preparation for injection and preparation method thereof |
| CN103536540A (en) * | 2013-09-16 | 2014-01-29 | 南通丝乡丝绸有限公司 | Rifampin lyophilized powder and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 吴俊伟等: "甲砜霉素注射液的研制及稳定性实验", 《四川畜牧兽医学院学报》 * |
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| CN104013584B (en) | 2016-06-29 |
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| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Li Na Inventor after: Lin Yuerong Inventor after: Ren Shuyu Inventor before: Huang Xiangbin Inventor before: Li Zhizheng Inventor before: Zhou Dai Inventor before: Xie Panjin |
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Effective date of registration: 20160425 Address after: 261500 Shandong province Gaomi City Liquan street community Wenchang Street No. 569 Applicant after: Luan Huanjun Address before: The new Chengdu high tech Zone of Sichuan province 611731 City Road No. 22 Applicant before: Sichuan Xingkerong Pharmaceutical Co., Ltd. |
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Effective date of registration: 20170908 Address after: 226156 Nantong Binhai New Area, Haimen City, Hong Kong West Road, No. 999, No. Patentee after: HAIMEN HUANGHAI PIONEER PARK SERVICES CO., LTD. Address before: 261500 Shandong province Gaomi City Liquan street community Wenchang Street No. 569 Patentee before: Luan Huanjun |
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