CN104324009A - Micro powder containing fenbendazole and preparation method thereof - Google Patents
Micro powder containing fenbendazole and preparation method thereof Download PDFInfo
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- CN104324009A CN104324009A CN201410579284.4A CN201410579284A CN104324009A CN 104324009 A CN104324009 A CN 104324009A CN 201410579284 A CN201410579284 A CN 201410579284A CN 104324009 A CN104324009 A CN 104324009A
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- fenbendazole
- micropowder
- micro powder
- anhydrous glucose
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- IRHZVMHXVHSMKB-UHFFFAOYSA-N fenbendazole Chemical compound [CH]1C2=NC(NC(=O)OC)=NC2=CC=C1SC1=CC=CC=C1 IRHZVMHXVHSMKB-UHFFFAOYSA-N 0.000 title claims abstract description 69
- 229960005473 fenbendazole Drugs 0.000 title claims abstract description 69
- 238000002360 preparation method Methods 0.000 title claims description 8
- 239000000843 powder Substances 0.000 title abstract description 11
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims abstract description 15
- 229960001031 glucose Drugs 0.000 claims abstract description 15
- 150000001875 compounds Chemical class 0.000 claims description 17
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 13
- 239000003814 drug Substances 0.000 claims description 8
- 150000007660 quinolones Chemical class 0.000 claims description 5
- 229940079593 drug Drugs 0.000 claims description 4
- 230000000694 effects Effects 0.000 abstract description 3
- 239000000203 mixture Substances 0.000 description 15
- 208000003495 Coccidiosis Diseases 0.000 description 9
- 206010023076 Isosporiasis Diseases 0.000 description 9
- 208000024891 symptom Diseases 0.000 description 7
- 230000002496 gastric effect Effects 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 244000144977 poultry Species 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 238000010521 absorption reaction Methods 0.000 description 3
- 230000000507 anthelmentic effect Effects 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 239000012141 concentrate Substances 0.000 description 3
- 241000239183 Filaria Species 0.000 description 2
- 241000287828 Gallus gallus Species 0.000 description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
- 210000004051 gastric juice Anatomy 0.000 description 2
- 210000001156 gastric mucosa Anatomy 0.000 description 2
- 238000011031 large-scale manufacturing process Methods 0.000 description 2
- 230000003340 mental effect Effects 0.000 description 2
- AZSNMRSAGSSBNP-UHFFFAOYSA-N 22,23-dihydroavermectin B1a Natural products C1CC(C)C(C(C)CC)OC21OC(CC=C(C)C(OC1OC(C)C(OC3OC(C)C(O)C(OC)C3)C(OC)C1)C(C)C=CC=C1C3(C(C(=O)O4)C=C(C)C(O)C3OC1)O)CC4C2 AZSNMRSAGSSBNP-UHFFFAOYSA-N 0.000 description 1
- SPBDXSGPUHCETR-JFUDTMANSA-N 8883yp2r6d Chemical compound O1[C@@H](C)[C@H](O)[C@@H](OC)C[C@@H]1O[C@@H]1[C@@H](OC)C[C@H](O[C@@H]2C(=C/C[C@@H]3C[C@@H](C[C@@]4(O[C@@H]([C@@H](C)CC4)C(C)C)O3)OC(=O)[C@@H]3C=C(C)[C@@H](O)[C@H]4OC\C([C@@]34O)=C/C=C/[C@@H]2C)/C)O[C@H]1C.C1C[C@H](C)[C@@H]([C@@H](C)CC)O[C@@]21O[C@H](C\C=C(C)\[C@@H](O[C@@H]1O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C1)[C@@H](C)\C=C\C=C/1[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\1)O)C[C@H]4C2 SPBDXSGPUHCETR-JFUDTMANSA-N 0.000 description 1
- 241000931177 Bunostomum trigonocephalum Species 0.000 description 1
- 206010016275 Fear Diseases 0.000 description 1
- 241000243976 Haemonchus Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000244206 Nematoda Species 0.000 description 1
- 241001137882 Nematodirus Species 0.000 description 1
- 241000510960 Oesophagostomum Species 0.000 description 1
- 208000030852 Parasitic disease Diseases 0.000 description 1
- 241001494479 Pecora Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 241000242541 Trematoda Species 0.000 description 1
- 241000197881 Trichocephalus Species 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 229960002549 enoxacin Drugs 0.000 description 1
- IDYZIJYBMGIQMJ-UHFFFAOYSA-N enoxacin Chemical compound N1=C2N(CC)C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCNCC1 IDYZIJYBMGIQMJ-UHFFFAOYSA-N 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 235000021050 feed intake Nutrition 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 229960002418 ivermectin Drugs 0.000 description 1
- 244000144972 livestock Species 0.000 description 1
- 229960002422 lomefloxacin Drugs 0.000 description 1
- ZEKZLJVOYLTDKK-UHFFFAOYSA-N lomefloxacin Chemical compound FC1=C2N(CC)C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCNC(C)C1 ZEKZLJVOYLTDKK-UHFFFAOYSA-N 0.000 description 1
- 239000005645 nematicide Substances 0.000 description 1
- 229960001180 norfloxacin Drugs 0.000 description 1
- OGJPXUAPXNRGGI-UHFFFAOYSA-N norfloxacin Chemical compound C1=C2N(CC)C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCNCC1 OGJPXUAPXNRGGI-UHFFFAOYSA-N 0.000 description 1
- 244000045947 parasite Species 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 235000013599 spices Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- GPTONYMQFTZPKC-UHFFFAOYSA-N sulfamethoxydiazine Chemical compound N1=CC(OC)=CN=C1NS(=O)(=O)C1=CC=C(N)C=C1 GPTONYMQFTZPKC-UHFFFAOYSA-N 0.000 description 1
- 229960002229 sulfametoxydiazine Drugs 0.000 description 1
- FDDDEECHVMSUSB-UHFFFAOYSA-N sulfanilamide Chemical compound NC1=CC=C(S(N)(=O)=O)C=C1 FDDDEECHVMSUSB-UHFFFAOYSA-N 0.000 description 1
- 229940124530 sulfonamide Drugs 0.000 description 1
- 230000001550 time effect Effects 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses micro powder containing fenbendazole. The micro powder is composed of the following components in percentage by weight: 5-10% of fenbendazole, 2.5-2.75% of PVPK 30, 2.5-2.75% of SDS and the balance being anhydrous glucose. The micro powder containing fenbendazole disclosed by the invention has enhanced adsorptivity and solubility, and is easier to be absorbed by astrointestinal tract; and the micro powder can enhance efficacy and shorten treatment time, and is obvious in treatment effect and high in curing rate.
Description
Technical field
The present invention relates to fowl, domestic animal anthelmintic field, be specifically related to a kind of micropowder containing fenbendazole and preparation method thereof.
Background technology
Coccidiosis is a kind of to poultry, the prejudicial parasitic disease of livestock intestinal tract.Coccidiosis is a kind of disease that the U.S. many commercial poultry culturist fears, and death loss is very general phenomenon more than 20%.Family home poultry raising amount is usually little, and coccidiosis is not a problem, but along with the increase of home poultry raising quantity, coccidiosis has become a very large threat.
Coccidiosis morbidity is very unexpected, and can only take the method first aid of injecting after acute onset, needing certain Professional knowledge could operate.For cultivating factory on a large scale, large area being infected, carrying out injection and to sue and labour obvious poor effect.Therefore, for coccidiosis to put prevention first.
Fenbendazole is benzimidazole anthelmintic, and it not only has height anthelmintic activity to gastrointestinal nematode parasites adult and larva, and has good result to coccidiosis, net filaria, fasciola and cestode, also has extremely strong killing egg effect.Especially, all have efficiently the adult of sheep haemonchus, ostertagi, trichostrongyle, cooperid, nematodirus, Bunostomum trigonoce phalum, Xia Baite nematicide, Oesophagostomum, Trichocephalus, net filaria and larva.
But the therapeutic effect that the fenbendazole oral agents used at present infects coccidiosis for chicken is not too remarkable, and it is shorter that the half-life eliminated routinely by this medicine, and medication is frequent, and widely distributed in vivo, treatment cycle is long, and cure rate is on the low side.
Summary of the invention
The invention provides a kind of micropowder containing fenbendazole and preparation method thereof, solve current fenbendazole oral agents therapeutic effect not obvious, treatment cycle is long, the problem that cure rate is low.
The object of the invention is to realize in the following manner:
A micropowder containing fenbendazole, it is characterized by and be made up of the component of following percentage by weight: fenbendazole 5-10%, PVPK30 2.5-2.75%, SDS 2.5-2.75%, all the other are anhydrous glucose.
The fenbendazole of described formula ratio, PVPK30, SDS are pulverized, sieves, and then add the anhydrous glucose of formula ratio, mix homogeneously.
Comprise the micropowder containing fenbendazole described in claim 1, also containing quinolones or sulfa drugs.
Relative to prior art, micropowder adsorptivity and the dissolubility enhancing containing fenbendazole of the present invention, more easily by gastrointestinal absorption, improve drug effect, shorten treatment time, and therapeutic effect is remarkable, cure rate is high.
Detailed description of the invention
For the micropowder containing fenbendazole, choose following examples:
Embodiment 1:
Produce water-soluble micropowder that 100kg contains fenbendazole, get 5kg fenbendazole, 2.5kg PVPK30,2.5kg SDS, mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mixing of 90kg, equal increments mix homogeneously is made.
Embodiment 2:
Produce water-soluble micropowder that 100kg contains fenbendazole, get 10kg fenbendazole, 2.6kgPVPK30,2.6kg SDS, mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mixing of 84.8kg, equal increments mix homogeneously is made.
Embodiment 3:
Produce water-soluble micropowder that 100kg contains fenbendazole, get 8kg fenbendazole, 2.75kgPVPK30,2.75kg SDS, mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mixing of 86.5kg, equal increments mix homogeneously is made.
All the other embodiments are carried out according to the preparation method of embodiment 1, and composition of raw materials is in table 1:
Table 1 unit: kilogram
Micropowder containing fenbendazole of the present invention also can make water solublity compound recipe fenbendazole micropowder with other drug is composite.
Embodiment 16:
Produce 100kg water solublity compound recipe fenbendazole micropowder, get 5kg fenbendazole, 2.5kg PVPK30,2.5kgSDS, 5kg quinolones norfloxacin, mix homogeneously, pulverize, cross 150 mesh sieves, the anhydrous glucose adding 85kg is mixed.
Embodiment 17:
Produce 100kg water solublity compound recipe fenbendazole micropowder, get 5kg fenbendazole, 2.55kg PVPK30,2.55kgSDS, 5.5kg quinolones enoxacin, mix homogeneously, pulverize, cross 150 mesh sieves, the anhydrous glucose adding 85kg is mixed.
Embodiment 18:
Produce 100kg water solublity compound recipe fenbendazole micropowder, get 6kg fenbendazole, 2.6kg PVPK30,2.5kgSDS, 5.5kg quinolones lomefloxacin, mix homogeneously, pulverize, cross 150 mesh sieves, the anhydrous glucose adding 85kg is mixed.
Embodiment 19:
Produce 100kg water solublity compound recipe fenbendazole micropowder, get 5kg fenbendazole, 2.65kg PVPK30, the close pyridine of 2.5kgSDS, 5.5kg sulfanilamide, mix homogeneously, pulverize, cross 150 mesh sieves, the anhydrous glucose adding 85kg is mixed.
Embodiment 20:
Produce 100kg water solublity compound recipe fenbendazole micropowder, get 5kg fenbendazole, 2.7kg PVPK30,2.5kgSDS, 5kg bacteresulf, mix homogeneously, pulverize, cross 150 mesh sieves, the anhydrous glucose adding 85kg is mixed.
Embodiment 21:
Produce 100kg water solublity compound recipe fenbendazole micropowder, get 5kg fenbendazole, 2.6kg PVPK30,2.5kgSDS, 5.5kg sulfametoxydiazine, mix homogeneously, pulverize, cross 150 mesh sieves, the anhydrous glucose adding 85kg is mixed.
Embodiment 22:
Produce 100kg water solublity compound recipe fenbendazole micropowder, get 5kg fenbendazole, 2.6kg PVPK30,2.5kgSDS, 5kg ivermectin, mix homogeneously, pulverize, cross 150 mesh sieves, the anhydrous glucose adding 85kg is mixed.
Its granularity of fenbendazole after micropowder is trickleer, even, therefore surface area increases, porosity increases, adsorptivity and dissolubility strengthen, medicine can disperse preferably, be dissolved in gastric juice, increase the contact area with gastric mucosa, thus more easily by gastrointestinal absorption, substantially increase bioavailability.
Preparation method of the present invention is more convenient by technique than bag, is more suitable for large-scale production.
Adopt the micropowder containing fenbendazole in the present invention and the water solublity compound recipe fenbendazole micropowder containing above micropowder, do following test:
1, experimental animal:
Random selecting infects the sick broiler 120 of coccidiosis, is divided into 4 groups at random, and often organize 30, body weight is at 1-2kg.
2, Experimental agents:
Fenbendazole powder: in mass percentage, the fenbendazole of 5% is mixed homogeneously with the starch of 95% and be get final product.
Fenbendazole micropowder: the micropowder containing fenbendazole prepared by the embodiment of the present invention 1;
Compound recipe fenbendazole micropowder: water solublity compound recipe fenbendazole micropowder prepared by the embodiment of the present invention 16.
3, experimental technique:
1 group is blank group, without medicine.
2 groups of fenbendazole powder are treated, usage: 100g mass percent is the fenbendazole powder spice 50kg of 5%, once-a-day, concentrate and are finished for 3 hours, be used in conjunction 4.
3 groups with fenbendazole micropowder of the present invention, usage: the micropowder containing fenbendazole prepared by 100g embodiment 1 is watered 100kg, once-a-day, concentrates and is finished for 3 hours, be used in conjunction 4.
4 groups with compound recipe fenbendazole micropowder of the present invention, usage: water solublity compound recipe fenbendazole micropowder prepared by 100g embodiment 16 is watered 100kg, once-a-day, concentrates and is finished for 3 hours, be used in conjunction 4.
After treatment starts, the sick fowl mental condition of every day entry and dead distribution, treat and add up therapeutic effect after 4 days, wherein:
Invalid: after referring to 4 days, sick fowl symptom has the situation of increasing the weight of or death.
Effective: after referring to 4 days, sick fowl symptom changes, and symptom is controlled or obviously alleviates relative to having before treatment.
Cure: after referring to 4 days, transference cure, the sick fowl mental status and feed intake recover normal condition.Its digital packets is contained in significant digits.
At the end of have symptom: refer to that treatment is after 4 days, sick fowl still has certain symptom, its Symptoms be better than treatment before or without change, sick fowl is not cured completely, its numeral has been included in the numeral of invalid number of elements and effective number of elements.
Result of the test is as shown in table 2:
Table 2
| Numbering | Group | Invalid number of elements | Effective number of elements | Cure number of elements | At the end of have symptom number of elements |
| 1 group | Matched group | 30 | 0 | 0 | 30 |
| 2 groups | Fenbendazole powder | 8 | 22 | 12 | 18 |
| 3 groups | Fenbendazole micropowder | 2 | 28 | 27 | 3 |
| 4 groups | Compound recipe fenbendazole micropowder | 1 | 29 | 28 | 3 |
4, conclusion:
As can be seen from the result of the test of table 2, fenbendazole powder, fenbendazole micropowder, compound recipe fenbendazole micropowder treatment group and matched group difference are extremely remarkable, and significantly, the treatment of the micropowder and water solublity compound recipe fenbendazole micropowder that contain fenbendazole of the present invention is than existing fenbendazole powder successful.
Fenbendazole of the present invention is after micropowder processes, granularity is trickleer, even, therefore surface area increases, porosity increases, adsorptivity and dissolubility strengthen, and medicine can disperse preferably, be dissolved in gastric juice, increase the contact area with gastric mucosa, thus more easily by gastrointestinal absorption, substantially increase bioavailability.Preparation method of the present invention is more convenient by technique than bag, is more suitable for large-scale production.
Above-described is only the preferred embodiment of the present invention, it should be pointed out that for a person skilled in the art, and not departing under general idea prerequisite of the present invention, can also make some changes and improvements, these also should be considered as protection scope of the present invention.
Claims (3)
1. the micropowder containing fenbendazole, it is characterized by and be made up of the component of following percentage by weight: fenbendazole 5-10%, PVPK30 2.5-2.75%, SDS 2.5-2.75%, all the other are anhydrous glucose.
2. the preparation method of the micropowder containing fenbendazole according to claim 1, is characterized by: the fenbendazole of described formula ratio, PVPK30, SDS are pulverized, sieve, and then add the anhydrous glucose of formula ratio, mix homogeneously.
3. a water solublity compound recipe fenbendazole micropowder, is characterized by: comprise the micropowder containing fenbendazole described in claim 1, also containing quinolones or sulfa drugs.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410579284.4A CN104324009A (en) | 2014-10-27 | 2014-10-27 | Micro powder containing fenbendazole and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410579284.4A CN104324009A (en) | 2014-10-27 | 2014-10-27 | Micro powder containing fenbendazole and preparation method thereof |
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| Publication Number | Publication Date |
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| CN104324009A true CN104324009A (en) | 2015-02-04 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410579284.4A Pending CN104324009A (en) | 2014-10-27 | 2014-10-27 | Micro powder containing fenbendazole and preparation method thereof |
Country Status (1)
| Country | Link |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101843586A (en) * | 2010-04-29 | 2010-09-29 | 山东迅达康兽药有限公司 | Water-soluble micro powder containing florfenicol and preparation method thereof |
| CN101984958A (en) * | 2010-11-01 | 2011-03-16 | 新疆医科大学第一附属医院 | Nanoscale albendazole micropowder and preparation method thereof |
-
2014
- 2014-10-27 CN CN201410579284.4A patent/CN104324009A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101843586A (en) * | 2010-04-29 | 2010-09-29 | 山东迅达康兽药有限公司 | Water-soluble micro powder containing florfenicol and preparation method thereof |
| CN101984958A (en) * | 2010-11-01 | 2011-03-16 | 新疆医科大学第一附属医院 | Nanoscale albendazole micropowder and preparation method thereof |
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Application publication date: 20150204 |