CN103340885B - Wettable albendazole ivermectin powder - Google Patents
Wettable albendazole ivermectin powder Download PDFInfo
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- CN103340885B CN103340885B CN201310302953.9A CN201310302953A CN103340885B CN 103340885 B CN103340885 B CN 103340885B CN 201310302953 A CN201310302953 A CN 201310302953A CN 103340885 B CN103340885 B CN 103340885B
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Abstract
The invention provides wettable albendazole ivermectin powder which is prepared from the following raw materials and auxiliary materials in parts by weight: 5-20 parts of albendazole, 0.1-1.6 parts of ivermectin, 0.5-3 parts of magnesium stearate, 33.9-70.7 parts of powdered sugar, 3-11 parts of sodium dodecyl sulfate, 0-8 parts of xanthan gum, 0.6-1 part of fresh milk essence, 0.6-1 part of saccharin sodium and 10-30 parts of sodium citrate. The invention also provides a preparation method and application of the wettable albendazole ivermectin powder. The wettable albendazole ivermectin powder significantly improves the dispersity of the ivermectin and albendazole in water to ensure that the ivermectin and the albendazole can be uniformly distributed in the water for a long time to facilitate clinical water drinking and administration; and the palatability of the albendazole ivermectin powder is greatly improved, and when used on faunas with sensitive tastes, such as pigs and the like, the albendazole ivermectin powder has a food calling function. The wettable albendazole ivermectin powder is simple in preparation process, low in production cost and suitable for industrial large-scale production.
Description
Technical field
The present invention relates to a kind of wettable albendazole ivermectin powder and its production and use.
Background technology
Since the forties in 20th century, the research and development of anthelmintic are always burning hot abnormal, obtain gratifying achievement therebetween; Particularly 1976 Avermectins medicine (Avermectins) discovery, opened especially anthelmintic research new era.This compounds has the nematicide and arthropod that parasitize animal extremely strong kills effect, thus makes antiCerbB2 monoclonal antibodies dosage drop to μ g/kg level by mg/kg level.Commercial in this kind of medicine at present have avilamycin (Avermectin, AVM), ivermectin (Ivermectin, IVM), doractin (Doramectin, DRM), acetylamino evericin (Eprinomectin, EPM, has another name called her and composes rhzomorph, Ai Purui rhzomorph), selamectin (Selamectin, SLM) and moxidectin (Moxidectin or Milbemycin, MXD, has another name called Moses Dinke, moxidectin) etc.Due to anthelmintic activity and the higher safety of its excellence, Avermectins medicine is regarded as the most excellent, most widely used anthelmintic for animals at present, is achievement in research the most outstanding in anti-parasite medicine research in recent years; But good medicine is still needed and is mixed with excellent preparation its drug effect can be made to be given full play to.Therefore be a Hot Contents studying of novel chiral synthon in the last few years to the preparation research of such medicine and exploitation.AVM powder, tablet, capsule, injection and dashing agent are developed now, IVM powder, tablet, paste, oral liquid, slow release bolus, injection and dashing agent, the injection of doractin injection and dashing agent and Ai Purui rhzomorph and dashing agent.
Because Avermectins medicine is never poison, its mechanism is the GABA receptor acting on parasite synapse or neuromuscular synapse, and the information transmission of teleneuron in interference polypide, finally causes polypide to benumb dead.And platyhelminthes, the GABA mediator as neural impulse is there is not in the polypide such as antibacterial and actinomycetes and thalline, so Avermectins has Strong pest-expellant effect to nematicide and epizoa and other arthropod, but to trematodiasis, cestode effect is very micro-, or do not have an active function, in order to obtain the wider product of pest-resistant spectrum, someone is by anti-trematodiasiss such as albendazoles, the good medicine of cestode effect and Avermectins make compound preparation by certain pharmaceutical technology, make its pest-resistant spectrum wider, usefulness is higher, to alleviate people for driving away the trouble of multiple parasite and multiple dosing simultaneously.In China market, commercial Related product has albendazole ivermectin powder, albendazole ivermectin sheet, albendazole ivermectin pre-mixing agent etc.Although these preparations meet the demand expanding pest-resistant spectrum, clinical practice but exist to jumpbogroup animals administer difficulty and feedstuff is difficult to mix homogeneously or cannot the shortcoming of mix homogeneously.Therefore, when clinical practice, animal is usually uneven and occur unsatisfactory curative effect or occur side reaction and even the situation such as poisoning because taking in medicine.In order to avoid the generation of this situation, develop a kind of be easy to uniformity of dosage Avermectins and albendazole compound product very necessary.
The present invention is directed to existing Avermectins and the awkward shortcoming of albendazole compound product, provide one can be dispersed in water, by drinking water or being sprayed at the wettable albendazole ivermectin powder of the mode administration on feedstuff.
Summary of the invention
The object of the present invention is to provide a kind of wettable albendazole ivermectin powder, and its production and use.
The invention provides a kind of wettable albendazole ivermectin powder, it is prepared from by the supplementary material of following weight proportion:
Albendazole 5 ~ 20 parts, ivermectin 0.1 ~ 1.6 part, magnesium stearate 0.5 ~ 3 part, Icing Sugar 33.9 ~ 70.7 parts, sodium lauryl sulphate 3 ~ 11 parts, xanthan gum 0 ~ 8 part, fresh milk essence 0.6 ~ 1 part, saccharin sodium 0.6 ~ 1 part, sodium citrate 10 ~ 30 parts.
Further, it is prepared from by the supplementary material of following weight proportion:
Albendazole 5 ~ 10 parts, ivermectin 0.2 ~ 1.6 part, magnesium stearate 0.5 ~ 2.5 part, Icing Sugar 49.5 ~ 70.7 parts, sodium lauryl sulphate 3 ~ 9 parts, xanthan gum 2 ~ 8 parts, fresh milk essence 0.6 ~ 0.9 part, saccharin sodium 0.6 ~ 0.9 part, sodium citrate 10 ~ 25 parts.
Further, it is prepared from by the supplementary material of following weight proportion:
Albendazole 6 ~ 10 parts, ivermectin 0.2 ~ 0.8 part, magnesium stearate 1.5 ~ 2.5 parts, Icing Sugar 49.5 ~ 64.3 parts, sodium lauryl sulphate 5 ~ 9 parts, xanthan gum 2 ~ 6 parts, fresh milk essence 0.7 ~ 0.9 part, saccharin sodium 0.7 ~ 0.9 part, sodium citrate 15 ~ 25 parts.
Preferably, it is prepared from by the supplementary material of following weight proportion:
Albendazole 8 ~ 10 parts, ivermectin 0.2 ~ 0.4 part, magnesium stearate 2 ~ 2.5 parts, Icing Sugar 49.5 ~ 57 parts, sodium lauryl sulphate 7 ~ 9 parts, xanthan gum 2 ~ 4 parts, fresh milk essence 0.8 ~ 0.9 part, saccharin sodium 0.8 ~ 0.9 part, sodium citrate 20 ~ 25 parts.
Further preferably, it is prepared from by the supplementary material of following weight proportion:
Albendazole 8 parts, ivermectin 0.4 part, magnesium stearate 2 parts, Icing Sugar 57 parts, sodium lauryl sulphate 7 parts, xanthan gum 4 parts, fresh milk essence 0.8 part, saccharin sodium 0.8 part, sodium citrate 20 parts;
Or, albendazole 10 parts, ivermectin 0.2 part, magnesium stearate 2.5 parts, Icing Sugar 49.5 parts, sodium lauryl sulphate 9 parts, xanthan gum 2 parts, fresh milk essence 0.9 part, saccharin sodium 0.9 part, sodium citrate 25 parts.
Present invention also offers the preparation method of above-mentioned wettable albendazole ivermectin powder, it comprises following operating procedure:
(1) supplementary material is taken by weight ratio;
(2) by after various supplementary material mixing, be crushed to 200 orders, obtain wettable albendazole ivermectin powder.
Present invention also offers the purposes of above-mentioned wettable albendazole ivermectin powder in preparation anthelmintic drug for animals.
Further, described medicine is the medicine of control nematicide or arthropod parasites disease.
Preferably, described nematicide is ascarid; Described arthropod is acarid.
Wettable albendazole ivermectin powder of the present invention, significantly improves ivermectin and the dispersibility of albendazole in water, makes it be evenly distributed on for a long time in water, facilitate clinical drinking water administration; Increase luring function, for the olfactory sensation such as pig, the faunichron that has a sharp sense of taste, have luring function; Preparation technology of the present invention is simple, low production cost, is applicable to industrialized great production.
Below in conjunction with detailed description of the invention, the present invention is described in further detail.But this should be interpreted as that the scope of the above-mentioned theme of the present invention is only limitted to following embodiment, all technology realized based on content of the present invention all belong to scope of the present invention.
Detailed description of the invention
The preparation of embodiment 1 wettable albendazole ivermectin powder of the present invention
Get albendazole 10g, ivermectin 0.2g, magnesium stearate 2.5g, Icing Sugar 49.5g, sodium lauryl sulphate 9g, xanthan gum 2g, fresh milk essence 0.9g, saccharin sodium 0.9g, sodium citrate 25g, after above-mentioned supplementary material mix homogeneously, be crushed to 200 object impalpable powders, packaging, obtains wettable albendazole ivermectin powder of the present invention.
The preparation of embodiment 2 wettable albendazole ivermectin powder of the present invention
Get albendazole 8g, ivermectin 0.4g, magnesium stearate 2g, Icing Sugar 57g, sodium lauryl sulphate 7g, xanthan gum 4g, fresh milk essence 0.8g, saccharin sodium 0.8g, sodium citrate 20g, after above-mentioned supplementary material mix homogeneously, be crushed to 200 object impalpable powders, packaging, obtains wettable albendazole ivermectin powder of the present invention.
The preparation of embodiment 3 wettable albendazole ivermectin powder of the present invention
Get albendazole 6g, ivermectin 0.8g, magnesium stearate 1.5g, Icing Sugar 64.3g, sodium lauryl sulphate 5g, xanthan gum 6g, fresh milk essence 0.7g, saccharin sodium 0.7g, sodium citrate 15g, after above-mentioned supplementary material mix homogeneously, be crushed to 200 object impalpable powders, packaging, obtains wettable albendazole ivermectin powder agent of the present invention.
The supplementary material compatibility screening of embodiment 4 wettable albendazole ivermectin powder
(1) preparation of different formulations product
Get the supplementary material in table 1 formula, prepare wettable albendazole ivermectin powder according to the method for embodiment 1, and evaluate the quality of each formula.
The preferred version of table 1 wettable albendazole ivermectin powder formula
(2) quality evaluation of wettable albendazole ivermectin powder
Dispersion is evaluated: get each 1g of wettable albendazole ivermectin powder by the preparation of table 1 formula 1 ~ formula 6, drops in 1000ml drinking water, observes or stir and observe its deployment conditions.Disperse slower and to be unevenly chosen as " poor "; Dispersion is comparatively slow, and have caking or granule in dispersive process, agitation as appropriate can be uniformly dispersed, and is chosen as " qualified "; Dispersion is fast, and gentle agitation can be uniformly dispersed, and is chosen as " good "; Dispersion is fast, need not stir and can be uniformly dispersed, be chosen as " excellent ".The results are shown in Table 2.
Sedimentation volume ratio is evaluated: by " solution for oral administration, suspensoid for oral administration, Emulsion for oral administration " sedimentation volume ratio inspection technique requirement in " People's Republic of China's veterinary drug allusion quotation (version in 2010) " annex, sedimentation volume ratio mensuration is carried out to the wettable albendazole ivermectin powder prepared by formula 1 ~ formula 6, sample thief 0.25g puts in 50ml tool plug graduated cylinder, add water to 50ml, fill in close, firmly jolting 1min, writes down suspended matter and starts height H
0, leave standstill and within 3 hours, write down the final height H of suspended matter, be calculated as follows: sedimentation volume ratio=H/H
0, sedimentation volume ratio should be not less than 0.90.The results are shown in Table 2.
Table 2 wettable albendazole ivermectin powder quality evaluation result
Listed 4 indexs of his-and-hers watches 1 are carried out comprehensive analysis and can be obtained: formula 2 ~ formula 6 is all qualified, be wherein optimum with formula 4, formula 5 again.
Beneficial effect of the present invention is illustrated below by way of test example.
Test example 1 wettable albendazole ivermectin powder therapeutic effect that is sick to ascaris suum and acariasis is investigated
Material: albendazole ivermectin powder (10%+0.2%, market products); Wettable albendazole ivermectin powder (10%+0.2%, prepared by embodiment 1).
Case: (sick pig continues to become thin ascaris suum case 48 example 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, get disease swine excrement, carry out worm's ovum inspection, detect oval in yellowish-brown, chorion is thicker, and adventitia is rough wavy ascaris suum germ cell); (sick pig becomes thin pig acarid case 56 example of Person B pig farm, suburb, Chengdu natural occurrence, down in spirits, likes in wall friction, the vesicle, incrustation, depilation etc. that occur after visible galling skin; Collect the scurf of disease pig injury moistening, be directly coated on microscope slide, can be observed the demodicid mite that lives).
Method: select the clinical onset growing and fattening pigs that body weight is substantially suitable, be divided into matched group, test group and negative control group at random under identical rearing conditions in same pig house; Matched group albendazole ivermectin powder presses 0.1% concentration spice, feeding for sick pig, is used in conjunction 3 days; Test group wettable albendazole ivermectin powder converts drinking water 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.
Efficacy determination method: medication is after 5 days, and spiritual appetite recovers normal, and microscopy, without the parasite lived or worm's ovum, is judged to recovery from illness; Medication is after 5 days, and spiritual appetite takes a turn for the better, the parasite that microscopy is lived as seen on a small quantity, is judged to effectively; Medication is after 5 days, and symptom is not improved, and it is invalid to be judged to.
Experimental result: in table 3, table 4.
Table 3 wettable albendazole ivermectin powder is to the clinical tests result of ascaris suum disease
Table 4 wettable albendazole ivermectin powder is to the clinical tests result of acariasis
As can be seen from experimental result, wettable albendazole ivermectin powder therapeutic effect that is sick to ascaris suum and pig acariasis is all better than commercially available albendazole ivermectin powder; The convenience that wettable albendazole ivermectin powder uses is better than commercially available albendazole ivermectin powder, greatly reduces the working strength of administration.Also find in test, owing to taking the mode administration added of drinking water, wettable albendazole ivermectin powder does not affect the feed intake of disease pig.
Claims (5)
1. a wettable albendazole ivermectin powder, is characterized in that:
It is prepared from by the supplementary material of following weight proportion:
Albendazole 8 parts, ivermectin 0.4 part, magnesium stearate 2 parts, Icing Sugar 57 parts, sodium lauryl sulphate 7 parts, xanthan gum 4 parts, fresh milk essence 0.8 part, saccharin sodium 0.8 part, sodium citrate 20 parts;
Or, albendazole 10 parts, ivermectin 0.2 part, magnesium stearate 2.5 parts, Icing Sugar 49.5 parts, sodium lauryl sulphate 9 parts, xanthan gum 2 parts, fresh milk essence 0.9 part, saccharin sodium 0.9 part, sodium citrate 25 parts.
2. the preparation method of wettable albendazole ivermectin powder described in claim 1, is characterized in that: it comprises following operating procedure:
(1) supplementary material is taken by weight ratio;
(2) by after various supplementary material mixing, be crushed to 200 orders, obtain wettable albendazole ivermectin powder.
3. the purposes of wettable albendazole ivermectin powder described in claim 1 in preparation anthelmintic drug for animals.
4. purposes according to claim 3, is characterized in that: described medicine is the medicine of control nematicide or arthropod parasites disease.
5. purposes according to claim 4, is characterized in that: described nematicide is ascarid; Described arthropod is acarid.
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Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103536624B (en) * | 2013-10-31 | 2016-08-17 | 成都乾坤动物药业有限公司 | A kind of wettable three-ingredient white composition powder and preparation method thereof |
| CN103800354A (en) * | 2013-12-24 | 2014-05-21 | 沈阳伟嘉牧业技术有限公司 | Compound albendazole dry suspension and preparation method thereof |
| CN109316486A (en) * | 2018-11-14 | 2019-02-12 | 天津市诺维动物药业有限公司 | Albendazole ivermectin powder |
| CN110812330A (en) * | 2019-12-08 | 2020-02-21 | 成都博大金点生物技术有限公司 | Albendazole ivermectin premix and preparation method thereof |
| CN113952308A (en) * | 2021-12-02 | 2022-01-21 | 山东国邦药业有限公司 | Albendazole granules and preparation method thereof |
| CN116236448A (en) * | 2023-03-07 | 2023-06-09 | 四川新益峰生物制药有限公司 | Efficient albendazole ivermectin premix dispersion particle composition and production process |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102935084A (en) * | 2012-11-13 | 2013-02-20 | 河南亚卫动物药业有限公司 | Compound ivermectin sustained release tablet and preparation method thereof |
| CN103083348A (en) * | 2012-05-10 | 2013-05-08 | 重庆金邦动物药业有限公司 | Albendazole/ivermectin powder for livestock |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103083348A (en) * | 2012-05-10 | 2013-05-08 | 重庆金邦动物药业有限公司 | Albendazole/ivermectin powder for livestock |
| CN102935084A (en) * | 2012-11-13 | 2013-02-20 | 河南亚卫动物药业有限公司 | Compound ivermectin sustained release tablet and preparation method thereof |
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Address after: 611130 Wenjiang City, Chengdu Province, Chengdu cross strait science and Technology Industrial Park Road, No. 259 Jin Fu Road, No. Patentee after: Chengdu Qiankun animal pharmaceutical Limited by Share Ltd Patentee after: Shanghai Simenon Biotech Co., Ltd. Address before: 611130 Wenjiang, Chengdu, Chengdu cross strait science and Technology Industrial Development Zone, Jin Fu Road, Sichuan Patentee before: Chengdu Qiankun Animal Pharmaceutical Co.,Ltd. Patentee before: Shanghai Simenon Biotech Co., Ltd. |
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Granted publication date: 20150715 Termination date: 20200718 |
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