CN103877025A - Fenbendazole soluble powder and preparation method thereof - Google Patents
Fenbendazole soluble powder and preparation method thereof Download PDFInfo
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- CN103877025A CN103877025A CN201210552306.9A CN201210552306A CN103877025A CN 103877025 A CN103877025 A CN 103877025A CN 201210552306 A CN201210552306 A CN 201210552306A CN 103877025 A CN103877025 A CN 103877025A
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- fenbendazole
- cyclodextrin
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- soluble powder
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Abstract
The invention relates to a fenbendazole soluble powder and a preparation method thereof, and the fenbendazole soluble powder is a cyclodextrin clathrate of fenbendazole. The specific preparation method comprises: adding a certain amount of cyclodextrin into water, heating and dissolving, then adding fenbendazole dissolved in ethanol, cooling the obtained solution to precipitate a solid, filtering, drying the solid, and crushing to obtain the cyclodextrin clathrate of fenbendazole. Compared with fenbendazole original powder, the prepared fenbendazole soluble power is obviously increased in solubility and stability, and the fenbendazole bioactivity is not influenced.
Description
Technical field
The present invention relates to a kind of fenbendazole soluble powder and preparation method thereof, belong to field of pharmaceutical preparations.
Background technology
The main parasite of China's large-scale pig farm has ascarid, trichinella, nodular worm, thread lungworm, kidney worm (Eustrongylus gigas), whipworm etc. in body, and vermin has acaricide, blood louse etc.After these parasite infestations, can cause blows, become thin, growth promoter is obstructed, feed conversion rate reduces, and also increases the susceptibility to Other diseases simultaneously, causes serious economic loss to pig industry.
The conventional anthelmintic of China's pig industry has at present: (1) entozoa medicine: albendazole, levamisole, metrifonate, destomycins, hygromycin, ivermectin, avilamycin; (2) epizoa medicine: metrifonate, Amitraz, basudin, dichlorvos, chrysanthemum esters medicine, avilamycin, ivermectin.Above-mentioned any product all can not be controlled endoparasite and ectoparasite simultaneously, needs to be in general repeatedly used and just can to reach good anthelminthic effect with two kinds of other products.
The therapeutic efficiency of fenbendazole:
Fenbendazole has good result to swine alimentary canal nematicide; if pig is according to 0.3mg/kg body weight dosage intramuscular injection administration; artificial challenge and natural infection case are after administration when 7d, 14d and 21d, and weightening finish is apparently higher than matched group (pig p<0.0001); Compared with matched group, polypide is by 100% expeling, the generation of being simultaneously free from side effects.
In the treatment of Sarcoptes suis, from suckling pig to sow, all there is good result, after artificial challenge acaricide, according to 0.3mg/kg body weight intramuscular injection administration, through the test of 4 weeks, result is thought to very obviously (p<0.05) of the eradicating efficacy of polypide infection between scytitis, damage and pig.In the treatment of farrowing sow kidney anthelmintic, the disposable injection of dosage cervical region of 0.3mg/kg, the 56th and while within 57 days, detecting, the recall rate of urine worm's ovum is 0, expeling rate is 100%, and matched group is 3762 ovum of every milliliter of urine.Pulmonis Sus domestica anthelmintic, digestive tract roundworm, pig louse etc. are had to same effect.
Because fenbendazole is respond well for parasiticide on animal cultivation, therefore in Animal diseases treatment, have extraordinary application prospect, but because fenbendazole dissolubility in water is low, therefore its route of administration is restricted.
Summary of the invention
the object of this invention is to provide a kind of fenbendazole soluble powder and preparation method, concrete grammar is the cyclodextrin clathrate of preparing fenbendazole, utilize the clathration of cyclodextrin, fenbendazole is carried out to enclose, improve the dissolubility of fenbendazole in water, improve it to light, to hot stability, overcome the deficiency of the existing dosage form of fenbendazole.
Technical scheme of the present invention is as follows:
The present invention is the clathrate of a kind of fenbendazole and cyclodextrin, and the architectural feature of clathrate is: fenbendazole, is formed taking cyclodextrin as host molecule by enclose in the cavity of cyclodextrin, fenbendazole is the clathrate of guest molecule.
Wherein, be one or more the mixture in alpha-cyclodextrin, beta-schardinger dextrin-, gamma-cyclodextrin as the cyclodextrin of host molecule.
The invention provides is to realize by following technical method:
A certain amount of cyclodextrin is added to the water to heating for dissolving, then adds the fenbendazole with dissolve with ethanol, after cooling obtained solution, have solid to separate out, filter, solid is dried, pulverize, can obtain the cyclodextrin clathrate of fenbendazole.
Wherein, heating-up temperature is 50-100 degree.
Fenbendazole soluble powder prepared by the present invention is compared the former powder of fenbendazole, and its dissolubility obviously increases, and stability obviously increases, and its biological activity is uninfluenced.
Detailed description of the invention
Below by specific embodiment, the present invention is described further, but embodiment is not used in the scope that the present invention protects that limits.
Embodiment 1
The preparation of 25% fenbendazole soluble powder:
Take 30g beta-schardinger dextrin-and add and in 200mL water, be heated to 100 degree and dissolve, then add the alcoholic solution that contains 10g fenbendazole, be cooled to a period of time behind 0 degree left and right, there is solid to generate, filter, after filtration cakes torrefaction, pulverize, all can obtain the cyclodextrin clathrate of fenbendazole.
Claims (2)
1. fenbendazole soluble powder and preparation method thereof, is characterized in that the cyclodextrin clathrate that described fenbendazole soluble powder is fenbendazole.
2. fenbendazole cyclodextrin clathrate as claimed in claim 1, its preparation method is for to be added to the water heating for dissolving by a certain amount of cyclodextrin, then add the fenbendazole with dissolve with ethanol, after cooling obtained solution, there is solid to separate out, filter, solid is dried, pulverize, can obtain the cyclodextrin clathrate of fenbendazole.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210552306.9A CN103877025A (en) | 2012-12-19 | 2012-12-19 | Fenbendazole soluble powder and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210552306.9A CN103877025A (en) | 2012-12-19 | 2012-12-19 | Fenbendazole soluble powder and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103877025A true CN103877025A (en) | 2014-06-25 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210552306.9A Pending CN103877025A (en) | 2012-12-19 | 2012-12-19 | Fenbendazole soluble powder and preparation method thereof |
Country Status (1)
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| CN (1) | CN103877025A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523684A (en) * | 2014-12-24 | 2015-04-22 | 浙江万方生物科技有限公司 | Preparation method of high-dissolution-rate fenbendazole medicinal preparation |
| CN104892524A (en) * | 2015-06-18 | 2015-09-09 | 信阳农林学院 | Preparation method of FBZ (fenhendazole) minicrystal |
| CN116602964A (en) * | 2023-07-18 | 2023-08-18 | 山东国邦药业有限公司 | Fenbendazole powder and preparation method and application thereof |
-
2012
- 2012-12-19 CN CN201210552306.9A patent/CN103877025A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523684A (en) * | 2014-12-24 | 2015-04-22 | 浙江万方生物科技有限公司 | Preparation method of high-dissolution-rate fenbendazole medicinal preparation |
| CN104523684B (en) * | 2014-12-24 | 2016-08-31 | 浙江万方生物科技有限公司 | A kind of preparation method of high-dissolution fenbendazole pharmaceutical preparation |
| CN104892524A (en) * | 2015-06-18 | 2015-09-09 | 信阳农林学院 | Preparation method of FBZ (fenhendazole) minicrystal |
| CN104892524B (en) * | 2015-06-18 | 2017-12-05 | 信阳农林学院 | The preparation method of Fenbendazole microcrystal |
| CN116602964A (en) * | 2023-07-18 | 2023-08-18 | 山东国邦药业有限公司 | Fenbendazole powder and preparation method and application thereof |
| CN116602964B (en) * | 2023-07-18 | 2023-09-22 | 山东国邦药业有限公司 | Fenbendazole powder and preparation method and application thereof |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20140625 |