CN103083243A - Doramectin soluble powder and preparation method thereof - Google Patents
Doramectin soluble powder and preparation method thereof Download PDFInfo
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- CN103083243A CN103083243A CN 201110343129 CN201110343129A CN103083243A CN 103083243 A CN103083243 A CN 103083243A CN 201110343129 CN201110343129 CN 201110343129 CN 201110343129 A CN201110343129 A CN 201110343129A CN 103083243 A CN103083243 A CN 103083243A
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- doramectin
- doractin
- soluble powder
- cyclodextrin
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Abstract
The invention relates to a doramectin soluble powder and a preparation method thereof. The doramectin soluble powder is a cyclodextrin inclusion compound of doramectin. The specific technical method comprises: adding certain amount of cyclodextrin into water, and heating it for dissolving, then adding doramectin dissolved by ethanol, cooling the obtained solution to precipitate a solid, conducting filtration, drying the solid, and crushing it, thus obtaining the cyclodextrin inclusion compound of doramectin. Compared with doramectin original powder, the doramectin soluble powder prepared by the invention has obviously enhanced solubility and substantially improved stability, and has uninfluenced biological activity.
Description
Technical field
The present invention relates to a kind of doractin soluble powder and preparation method thereof, belong to field of pharmaceutical preparations.
Background technology
Doractin (Doramectin) is added by the Avid kyowamycin genetic engineering variant that thiacyclohexane yl carboxylic acid artifact is synthetic to be obtained, and has the thiacyclohexane base on the C25 position.Doractin is the inside and outside double agent of killing, and is all effective to nematicide, arthropod.
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.Can cause blows after these parasite infestations, 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.
China's pig industry anthelmintic commonly used 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 in general to be repeatedly used just with two kinds of other products to reach good anthelminthic effect.
The therapeutic efficiency of doractin:
Doractin has good result to the swine alimentary canal nematicide, and according to 0.3mg/kg body weight dosage intramuscular injection administration, when 7d, 14d and 21d, weightening finish is apparently higher than matched group (pig p＜0.0001) after administration for artificial challenge and natural infection case as pig; Compare with matched group, polypide is driven away by 100%, the generation of being free from side effects simultaneously.
In the treatment of Sarcoptes suis, good result is all arranged, after the artificial challenge acaricide, according to 0.3mg/kg body weight intramuscular injection administration from the suckling pig to the sow, through 4 weeks tests, result is thought eradicating efficacy that polypide between scytitis, damage and pig is infected very obviously (p＜0.05).In treatment to farrowing sow kidney anthelmintic, the disposable injection of dosage cervical region of 0.3mg/kg, when detecting, the recall rate of urine worm's ovum was 0 in the 56th and 57 day, the 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. there is same effect.
Be used for parasiticide due to doractin respond well on animal cultivation, therefore in the Animal diseases treatment, extraordinary application prospect arranged, but because doractin dissolubility in water is low, so its route of administration is restricted.
Summary of the invention
The purpose of this invention is to provide a kind of doractin soluble powder and preparation method, concrete grammar is the cyclodextrin clathrate of preparation doractin, utilize the clathration of cyclodextrin, doractin is carried out enclose, improve the dissolubility of doractin in water, improve it to light, to the stability of heat, overcome the deficiency of the existing dosage form of doractin.
Technical scheme of the present invention is as follows:
The present invention is the clathrate of a kind of doractin and cyclodextrin, and the architectural feature of clathrate is: doractin in the cavity of cyclodextrin, is formed take cyclodextrin as host molecule by enclose, doractin is the clathrate of guest molecule.
Wherein, be one or more 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 heating for dissolving, then add the doractin with dissolve with ethanol, after resulting solution is cooling, there is solid to separate out, filter, with the solid oven dry, pulverize, can obtain the cyclodextrin clathrate of doractin.
Wherein, heating-up temperature is 50-100 ℃.
The doractin soluble powder of the present invention's preparation is compared the former powder of doractin, and its dissolubility obviously increases, and stability obviously increases, and its biological activity is uninfluenced.
The specific embodiment
The present invention is described further below by specific embodiment, but embodiment is not used in the scope that the present invention protects that limits.
Embodiment 1
The preparation of 25% doractin soluble powder: take the 30g beta-schardinger dextrin-and add and be heated to 100 ℃ of dissolvings in 200mL water, then add the alcoholic solution that contains the 10g doractin, be cooled to a period of time behind 0 ℃ of left and right, there is solid to generate, filter, pulverize after filtration cakes torrefaction, all can obtain the cyclodextrin clathrate of doractin.
Claims (2)
1. doractin soluble powder and preparation method thereof, is characterized in that described doractin soluble powder is the cyclodextrin clathrate of doractin.
2. doractin cyclodextrin clathrate as claimed in claim 1, its preparation method is for to be added to the water heating for dissolving with a certain amount of cyclodextrin, then add the doractin with dissolve with ethanol, after resulting solution is cooling, there is solid to separate out, filters, solid is dried, pulverize, can obtain the cyclodextrin clathrate of doractin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201110343129 CN103083243A (en) | 2011-11-03 | 2011-11-03 | Doramectin soluble powder and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201110343129 CN103083243A (en) | 2011-11-03 | 2011-11-03 | Doramectin soluble powder and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103083243A true CN103083243A (en) | 2013-05-08 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201110343129 Pending CN103083243A (en) | 2011-11-03 | 2011-11-03 | Doramectin soluble powder and preparation method thereof |
Country Status (1)
| Country | Link |
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| CN (1) | CN103083243A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103417484A (en) * | 2013-08-21 | 2013-12-04 | 成都乾坤动物药业有限公司 | Wettable doramectin solid dispersion powder and preparation method and application thereof |
| CN107087626A (en) * | 2017-05-08 | 2017-08-25 | 广西大学 | A kind of nematode killing agent composition containing doractin |
-
2011
- 2011-11-03 CN CN 201110343129 patent/CN103083243A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103417484A (en) * | 2013-08-21 | 2013-12-04 | 成都乾坤动物药业有限公司 | Wettable doramectin solid dispersion powder and preparation method and application thereof |
| CN107087626A (en) * | 2017-05-08 | 2017-08-25 | 广西大学 | A kind of nematode killing agent composition containing doractin |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 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: 20130508 |