A kind of wettability fenbendazole ivermectin powder
Technical field
The present invention relates to a kind of wettability fenbendazole ivermectin powder and its production and use.
Background technology
Since the forties in 20th century, the research and development of anthelmintic are burning hot unusual always, obtain gratifying achievement therebetween; Particularly 1976 Avermectins medicine (Avermectins) discovery, opened new era of anthelmintic research especially.This compounds has the extremely strong effect of killing to nematicide and the arthropod that parasitizes animal, thereby makes anthelmintic medicine dosage drop to μ g/kg level by the mg/kg level.Commercial in this class medicine at present have an avilamycin (Avermectin, AVM), ivermectin (Ivermectin, IVM), doractin (Doramectin, DRM), acetylamino evericin (Eprinomectin, EPM has another name called her and composes rhzomorph, Ai Purui rhzomorph), match draw rhzomorph (Selamectin, SLM) and moxidectin (Moxidectin or Milbemycin, MXD has another name called Moses Dinke, moxidectin) etc.Because its excellent anthelmintic activity and higher safety, Avermectins medicine is regarded as the best, most widely used anthelmintic for animals at present, is the most outstanding achievement in research in the anti-parasite medicine research in recent years; But good medicine is still needed and is mixed with good preparation its drug effect is given full play to.Therefore be a focus content of new veterinary drug research in the last few years to the preparation research of such medicine and exploitation.AVM powder, tablet, capsule, injection and dashing agent have been developed out now, IVM powder, tablet, paste, oral liquid, slow release bolus, injection and dashing agent, injection and the dashing agent of doractin injection and dashing agent and Ai Purui rhzomorph.
Because Avermectins medicine is never poison, its mechanism is the GABA receptor that acts on parasite synapse or neuromuscular synapse, disturbs the information transmission of teleneuron in the polypide, causes that finally the polypide paralysis is dead.And there is not GABA mediator as neural impulse in polypide such as platyhelminthes, antibacterial and actinomycetes and the thalline, so Avermectins has the Strong pest-expellant effect to nematicide and epizoa and other arthropod, but very little to the effect of trematodiasis, cestode, or do not have an active function.Facts have proved, anti-trematodiasis, cestodes such as Avermectins and fenbendazole are acted on compatibility of drugs use preferably, can remedy the deficiency of two kinds of medicines on pest-resistant spectrum, make its pest-resistant spectrum wider, usefulness is higher, alleviates people for driving away the trouble of multiple parasite multiple dosing simultaneously.Commercial Related product has fenbendazole ivermectin sheet etc. on China market.Though these preparations have satisfied the demand that enlarges pest-resistant spectrum,, in clinical practice, but exist jumpbogroup animals administer difficulty, be difficult to mix homogeneously or shortcoming that can't mix homogeneously with feedstuff.Therefore, when clinical practice, usually medicine is inhomogeneous unsatisfactory curative effect to be occurred or side reaction occurs and even situation such as poisoning animal because taking in.For fear of the generation of this situation, it is very necessary to develop a kind of Avermectins and fenbendazole compound product that is easy to even administration.
The present invention is directed to existing Avermectins and the awkward shortcoming of fenbendazole compound product, provide a kind of and be dispersed in the water, by drinking water or being sprayed at the fenbendazole ivermectin powder of the mode administration on the feedstuff.
Summary of the invention
The object of the present invention is to provide a kind of wettability fenbendazole ivermectin powder, and its production and use.
The invention provides a kind of wettability fenbendazole ivermectin powder, it is that supplementary material by following weight proportion is prepared from:
2.5~10 parts of fenbendazoles, 0.1~0.8 part of ivermectin, 0.5~3 part of magnesium stearate, 43.9~74 parts of Icing Sugar, 3~11 parts of sodium lauryl sulphates, 0~8 part of xanthan gum, 0.6~1 part of fresh milk essence, 0.6~1 part of saccharin sodium, 10~30 parts of sodium citrates.
Wherein, it is that supplementary material by following weight proportion is prepared from:
2.5~5 parts of fenbendazoles, 0.2~0.8 part of ivermectin, 0.5~2.5 part of magnesium stearate, 54.5~74 parts of Icing Sugar, 3~9 parts of sodium lauryl sulphates, 2~8 parts of xanthan gum, 0.6~0.9 part of fresh milk essence, 0.6~0.9 part of saccharin sodium, 10~25 parts of sodium citrates.
Further, it is that supplementary material by following weight proportion is prepared from:
3~5 parts of fenbendazoles, 0.2~0.6 part of ivermectin, 1.5~2.5 parts of magnesium stearate, 54.5~67.5 parts of Icing Sugar, 5~9 parts of sodium lauryl sulphates, 2~6 parts of xanthan gum, 0.7~0.9 part of fresh milk essence, 0.7~0.9 part of saccharin sodium, 15~25 parts of sodium citrates.
Further, it is that supplementary material by following weight proportion is prepared from:
4~5 parts of fenbendazoles, 0.2~0.4 part of ivermectin, 2~2.5 parts of magnesium stearate, Icing Sugar 54.5~61,7~9 parts of sodium lauryl sulphates, 2~4 parts of xanthan gum, 0.8~0.9 part of fresh milk essence, 0.8~0.9 part of saccharin sodium, 20~25 parts of sodium citrates.
Preferably, it is that supplementary material by following weight proportion is prepared from:
4 parts of fenbendazoles, 0.4 part of ivermectin, 2 parts of magnesium stearate, 61 parts of Icing Sugar, 7 parts of sodium lauryl sulphates, 4 parts of xanthan gum, 0.8 part of fresh milk essence, 0.8 part of saccharin sodium, 20 parts of sodium citrates;
Or, 5 parts of fenbendazoles, 0.2 part of ivermectin, 2.5 parts of magnesium stearate, 54.5 parts of Icing Sugar, 9 parts of sodium lauryl sulphates, 2 parts of xanthan gum, 0.9 part of fresh milk essence, 0.9 part of saccharin sodium, 25 parts of sodium citrates.
The present invention also provides the preparation method of above-mentioned wettability fenbendazole ivermectin powder, and it comprises following operating procedure:
(1) takes by weighing supplementary material by weight ratio;
(2) with behind the various supplementary material mixings, be crushed to 200 orders, namely get wettability fenbendazole ivermectin powder.
The present invention also provides the purposes of above-mentioned wettability fenbendazole ivermectin powder in preparation anthelmintic drug for animals.
Further, described medicine is the medicine of control nematicide or arthropod parasitic disease.
Preferably, described nematicide is ascarid; Described arthropod is acarid.
Wettability fenbendazole ivermectin powder of the present invention has significantly improved ivermectin and the fenbendazole dispersibility in water, and it is evenly distributed in the water for a long time, convenient clinical drinking-water administration; Increase luring function, the faunichron that be used for olfactory sensation such as pig, has a sharp sense of taste there is luring function; Preparation technology of the present invention is simple, and low production cost is fit to industrialized great production.
The present invention is described in further detail below in conjunction with the specific embodiment.But this should be interpreted as that the scope of the above-mentioned theme of the present invention only limits to following embodiment, all technology that realizes based on content of the present invention all belong to scope of the present invention.
The specific embodiment
The preparation of embodiment 1 wettability fenbendazole ivermectin powder
Get fenbendazole 4g, ivermectin 0.4g, magnesium stearate 2g, Icing Sugar 61g, sodium lauryl sulphate 7g, xanthan gum 4g, fresh milk essence 0.8g, saccharin sodium 0.8g, sodium citrate 20g, behind above-mentioned supplementary material mix homogeneously, be crushed to 200 purpose impalpable powders, packing namely gets wettability fenbendazole ivermectin powder of the present invention.
The preparation of embodiment 2 wettability fenbendazole ivermectin powder
Get fenbendazole 5g, ivermectin 0.2g, magnesium stearate 2.5g, Icing Sugar 54.5g, sodium lauryl sulphate 9g, xanthan gum 2g, fresh milk essence 0.9g, saccharin sodium 0.9g, sodium citrate 25g, behind above-mentioned supplementary material mix homogeneously, be crushed to 200 purpose impalpable powders, packing namely gets wettability fenbendazole ivermectin powder of the present invention.
The supplementary material compatibility screening of embodiment 3 wettability fenbendazole ivermectin powder
(1) preparation of different formulations product
Get the supplementary material in table 1 prescription, prepare wettability fenbendazole ivermectin powder according to the method for embodiment 1, and estimate quality of each prescription.
The preferred version of table 1 wettability fenbendazole ivermectin powder prescription
(2) quality evaluation of wettability fenbendazole ivermectin powder
Dispersion is estimated: get each 1g of wettability fenbendazole ivermectin powder by 6 preparations of table 1 prescription 1~prescription, drop in the 1000ml drinking water, observe or stir and observe its deployment conditions.Disperse slower and inhomogeneous being chosen as " poor "; Disperse slower, have in the dispersive process caking or granule, agitation as appropriate can be uniformly dispersed, and is chosen as " qualified "; Disperse soon, gentle agitation can be uniformly dispersed, and is chosen as " very "; Disperse to stir and to be uniformly dispersed soon, be chosen as " excellent ".The results are shown in Table 2.
Settling volume is than estimating: by " taking solution orally, take suspensoid orally, take Emulsion orally " settling volume in " People's Republic of China's veterinary drug allusion quotation (version in 2010) " appendix than inspection technique requirement, wettability fenbendazole ivermectin powder by prescription 1~prescription 6 preparations is carried out settling volume than measuring, sample thief 0.25g puts in the 50ml tool plug graduated cylinder, add water to 50ml, fill in close, firmly jolting 1min writes down suspended matter and begins height H
0, leave standstill and write down the final height H of suspended matter in 3 hours, be calculated as follows: settling volume ratio=H/H
0, the settling volume ratio should be not less than 0.90.The results are shown in Table 2.
Table 2 wettability fenbendazole ivermectin opaque amount evaluation result
His-and-hers watches 1 listed 4 indexs are carried out analysis-by-synthesis and can be got: prescription 2~prescription is 6 all qualified, wherein again with fill a prescription 4, prescription 5 is optimum.
Below specify beneficial effect of the present invention by testing example.
The sick therapeutic effect with acariasis to ascaris suum of test example 1 wettability fenbendazole ivermectin powder is investigated
Material: fenbendazole powder (5%, the market sale product); Ivermectin powder (0.2%, the market sale product); Fenbendazole ivermectin powder (5%+0.2%, embodiment 2 preparations).
Case: (sick pig continues to become thin ascaris suum case 48 examples of Chengdu suburbs and counties under the jurisdiction of a large city first pig farm natural occurrence, is off one's feed, and spirit is depressed etc., get the disease swine excrement, carry out the worm's ovum inspection, detect and be the yellowish-brown ellipse, chorion is thicker, and adventitia is rough wavy ascaris suum germ cell); Pig acarid case 56 examples of Person B pig farm, suburb, Chengdu natural occurrence (sick pig becomes thin, down in spirits, and as seen happiness frays the vesicle that occurs behind the skin, incrustation, depilation etc. in wall friction; Collect the scurf of disease pig injury moistening, directly be coated on the microscope slide, can be observed demodicid mite alive).
Method: select the suitable substantially clinical onset growing and fattening pigs of body weight, in same pig house, be divided into matched group, test group and negative control group at random under the identical raising condition; Matched group by 0.2% concentration spice, supplies sick pig feeding with fenbendazole powder+ivermectin powder (1:1 mixing), is used in conjunction 3 days; Test group is converted drinking water with wettability fenbendazole ivermectin powder by 0.05% concentration, drinks for sick pig, is used in conjunction 3 days; Negative control group is raised by daily feeding manner, not administration.
The efficacy determination method: medication is after 5 days, and it is normal that spiritual appetite is recovered, and microscopy does not have parasite alive or worm's ovum, is judged to recovery from illness; After the medication 5 days, spiritual appetite takes a turn for the better, and the visible a small amount of parasite that lives of microscopy is judged to effectively; After the medication 5 days, symptom does not have obvious improvement, and it is invalid to be judged to.
Experimental result: see Table 3, table 4.
Table 3 wettability fenbendazole ivermectin powder is investigated the result to the curative effect of ascaris suum disease
Table 4 wettability fenbendazole ivermectin powder is investigated the result to the curative effect of acariasis
From experimental result as can be seen, wettability fenbendazole ivermectin powder all is better than commercially available fenbendazole ivermectin powder to the sick therapeutic effect with the pig acariasis of ascaris suum; The convenience that wettability fenbendazole ivermectin powder uses is better than commercially available fenbendazole ivermectin powder, reduces the working strength of administration greatly.Find also that in test owing to the mode administration of taking to drink water and add, wettability fenbendazole ivermectin powder does not influence the feed intake of disease pig.