CN101301280A - Sustained release tablet products used as helminthic of livestock - Google Patents
Sustained release tablet products used as helminthic of livestock Download PDFInfo
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- CN101301280A CN101301280A CNA2008100526986A CN200810052698A CN101301280A CN 101301280 A CN101301280 A CN 101301280A CN A2008100526986 A CNA2008100526986 A CN A2008100526986A CN 200810052698 A CN200810052698 A CN 200810052698A CN 101301280 A CN101301280 A CN 101301280A
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Abstract
The invention discloses a sustained release tablet product used for livestock to expel parasites, which relates to a pharmaceutical product for the livestock, in particular to a long acting anthelmintic pharmaceutical product. The product contains 5 portions of ivermectin, 30 to 50 portions of hydroxypropyl methyl cellulose (hereafter called 'HPMCK4M') with the specification of K4M, 8 to 15 portions of hexadecanol, 80 to 120 portions of lactose, 30 to 45 portions of microcrystalline cellulose, and 1 to 2.5 portions of magnesium stearate. The specification of each tablet can be between 150 and 230mg. The product can effectively expel the parasites inside and outside bodies of cattle and sheep, particularly has better effect on eelworms and arthropods, has the characteristics of sustained release and long acting, and further effectively solves the problems in the prior art such as the reduction of livestock production performance, quality decrease of livestock products, other infectious diseases brought to the livestock, falling ill of people and the livestock and so on, due to the fact that the parasites in the bodies of the livestock fail to be effectively prevented and cured.
Description
Technical field
The present invention relates to a kind of domestic animal and use drug products, particularly a kind of have a long lasting anthelmintic class drug products.
Background technology
China's domestic animal parasitic disease kind is kind more than 2000 nearly, parasite mainly is by consuming domestic animal endotrophic material, causing mechanical damage, domestic animal is descended to the utilization rate of feedstuff to domestic animal to the harm of domestic animal, thereby cause the domestic animal poor growth, the price of deed reduces, or nutrition for want of and death.In addition, parasitic disease can cause that also the domestic animal fertility performance reduces, the quality of animal product reduces, bring problems such as other infectious disease, zoonosis to domestic animal.Although present various anti-parasite medicines develop more and more wide spectrum, safety, but also there is not a kind of anti-parasite medicine can prevent and treat all parasites of domestic animal so far, this has brought the technical difficulty of selection medicine for peasant household and plant, and China overwhelming majority peasant household and plant are still poor to the use knowledge of parasitic disease and parasite medicine, or it is blank, therefore, people are higher to the requirement of anti-parasite medicine in reality.
The subject matter that control exists to the ruminant endoparasite and ectoparasite is at present: the firstth, and the limitation of the pest-resistant spectrum of single medicine.There is not a kind of medicine all effective to nematicide, trematodiasis, cestode and vermin thereof simultaneously.Even the wide spectrum pest-resistant medicine is also just to nematicide one class wide spectrum or only effective to trematodiasis and cestode.Second, lack ideal dosage form long-acting, easy to use, existing problems aspect drug residue and control thereof, drug effect is short behind conventional oral tablet, solution, powder or the injection a drug, and the conventional formulation that drug effect is the longest also can continue 1-3 about week, for example effective acting time, the present widely used Yi Wei bacterium of people ordinary tablet, in 15 minutes disintegrations, stripping quantity can reach more than 80%, can not realize the effect of drug effect slow release.And meat ruminant is longer in the time that spring, autumn, Xia Sanji herd, and the probability that infects worm's ovum in the open air is bigger, in order to control parasitic infection, need ruminate repeatedly medication.Culture not only uneconomical but also inconvenient for jumpbogroup like this.Therefore still lack a kind of safe, pest-resistant spectrum pest-resistant medicine wide, long-acting, easy to use in the present background technology.
The technology contents of invention
The objective of the invention is by a kind of anthelmintic sustained release tablet products of domestic animal that is applicable to is provided, can effectively drive away the cattle and sheep endoparasite and ectoparasite, especially nematicide and arthropod are all had better action, this product has the characteristics of slow release long-acting, and then has solved the problem that exists in the above-mentioned background technology.
Contain 5 parts of ivermectins in the product of the present invention, specification is 30～50 parts of hypromelloses (hereinafter referred to as " HPMCK4M "), 8～15 parts of hexadecanols, 80～120 parts of lactose, 30～45 parts of microcrystalline Cellulose, 1～2.5 part of the magnesium stearate of K4M.Above-mentioned every composition is commercially available product, and every specification can be 150～230mg.
In above-mentioned every composition, be preferable addition for 1.5 parts with 5 parts of ivermectins, 40 parts of HPMCK4M, 10 parts of hexadecanols, 100 parts of lactose, 32 parts of microcrystalline Cellulose, magnesium stearate.The specification of every finished product is preferably 190mg.
Umber of the present invention is meant: when solid unit of weight was mg, the volume unit of liquid was ml; When solid unit of weight was kg, the volume unit of liquid was L.
In every composition of the present invention, ivermectin is novel wide spectrum, efficient, low toxicity antibiotics parasiticide class medicine, and endoparasite and ectoparasite especially nematicide and arthropod are all had anthelmintic action preferably.Mainly contain ivermectin B in its main component
1Character is white crystalline powder, and is tasteless.Be soluble in methanol, ethanol, ethyl acetate, the acetone dissolving hardly in water.It can pass through the release of the inhibitory transmitter r-aminobutyric acid of increase polypide, and the Cl that opens glutamic acid control
-Passage strengthens neurolemma to Cl
-Permeability, thereby the transmission of block nerves signal, final neural paralysis makes muscle cell lose contractility, and causes polypide death.
The controlled release of medicine or slow-released system are in the given time a kind of, and drug level is maintained drug effect delivery mode in the valid density scope for a long time.The preparation principle of controlled release, slow releasing preparation mainly is based on reducing of dissolution rate and slowing down of diffusion rate, thereby reaches the purpose of slow release and prolongation curative effect.In the control of medicine dissolution rate, macromolecular material commonly used is made little salt of dissolubility or esters as blocker or slow releasing agent skeleton or medicine, also makes oil-in-water powder Emulsion or coating powder suspension sometimes to delay the release of medicine.
Hypromellose (HPMC) is a high molecular weight hydrophilic gel skeleton material, meets water and forms gel, and the water-insoluble drug rate of release depends on the progressively speed of corrosion of gel layer, and when treating that gel skeleton dissolves fully, medicine all discharges.Therefore can come adjustment release speed by regulating ratio and the specification of HPMC in prescription, the HPMC specification that the present invention uses is K4M (4000cPas).Hexadecanol is the water-insoluble slow-release material, is used for the release time of prolong drug in the domestic animal digestive tract, improves drug absorption, helps improving drug bioavailability.Reach medicine effective release at the appointed time by adjusting HPMC, the ratio of hexadecanol in prescription.Lactose and microcrystalline Cellulose are the filler in the product of the present invention among the present invention, and magnesium stearate or Pulvis Talci are lubricant.
Product of the present invention is when manufacturing; can be at normal temperatures with above-mentioned main ingredient ivermectin, HPMCK4M, hexadecanol, lactose, microcrystalline Cellulose according to the aforementioned proportion mixing; add an amount of water 1-5 part and make soft material; then one-step-granulating method 18 orders with routine sieve, conventional pelletizing machine 14 order granulate; make granule neat; after adding the magnesium stearate mixing, with conventional tablet machine tabletting, 80 ℃ of dryings 4 hours, promptly can be made into sheet weight-normality lattice was the white tablet that also has micro-moisture of 150～230mg.
Product of the present invention can be for bottled, and shading when depositing, sealing are preserved.Can be during use by once measuring the administration of 0.2mg/kg domestic animal body weight.
Product of the present invention guarantees that by screening the rational formula that can delay drug release medicine reaches the effect of disposable administration, slow release, long-acting anti-parasite clinically.On the basis that slow release method breaks through, utilize the different proportion research of framework material hypromellose (HPMC) and hexadecanol, the slow-release time and the stripping quantity of decision product make the stripping quantity of ivermectin reach the slow release effect of strippings in 16 hours more than 75%.Than comparing in the background technology, the slow releasing effect of the drug effect that product of the present invention has can make ivermectin blood drug level steady, avoids peak valley phenomenon, reduces the advantage of the toxic and side effects of medicine.
The clinical trial example:
In vivo test project standard in the clinical trial of anthelmintic medicament in " the new veterinary drug and the veterinary drug novel formulation management method " of in JIUYUE, 1989 promulgation of the execution Ministry of Agriculture is in Xinzhou District stud farm goat cultivation base, Wuhan City, Hubei Province.150 of goats (2-3 monthly age) are divided into 2 groups according to the completely random method, and one group is used the product of making according to embodiment 4 of the present invention, as test group; Organize in contrast with common ivermectin sheet for one group.
1.1 feedstuff mode: herd naturally.
1.2 dosage scheme: test group is pressed 0.2mg/kg body weight (1 amount) administration.Positive controls is pressed 0.2mg/kg body weight (1 amount) administration equally.
1.3 inspection index:
(1) sheep nematicide (esophageal orifice nematicide, Bunostomum trigonoce phalum);
(2) worm's ovum is supported before rate (%)=anthelmintic average worm's ovum number/g * 100% after average worm's ovum number/g-anthelmintic
(3) after the continuous review medication 60 days with interior anthelminthic effect;
1.4 worm's ovum inspection technique: get fresh excreta 10g.Add the saturated sodium-chloride fluid injection, 100ml mixes, and by 60 order copper sieve, filters in the inflow beaker, leaves standstill 30min, the worm's ovum come-up; With diameter is the iron wire loop of 8cm, and parallel contact with liquid level is glued and got surperficial liquid film, shakes off with section slide and checks a worm's ovum number.
2, result of the test
The test of pesticide effectiveness of control goat nematicide the results are shown in following table:
Statistical test result shows, test group and matched group after medication the 3rd day and the 10th day, and 20 days, average worm's ovum slip difference is significantly (P＞0.05) not, the 30th day, 45 days, 60 days average worm's ovum slip difference extremely significantly (P＜0.01) after the medication.
The specific embodiment
The present invention is further illustrated below in conjunction with specific embodiment.
Embodiment 1
With granulate behind ivermectin 5mg, HPMCK4M 30mg, hexadecanol 10mg, lactose 80mg, microcrystalline Cellulose 30mg and the water 1ml mixing, with one-step-granulating method 18 orders of routine sieve, conventional pelletizing machine 14 order granulate; make granule neat; add magnesium stearate 1mg mixing, conventional tablet machine tabletting, 80 ℃ of dryings 4 hours, make the white plates product of every 150mg.
Embodiment 2
Ivermectin 5mg, HPMCK4M 35mg, hexadecanol 8mg, lactose 95mg, microcrystalline Cellulose 36mg added behind the water 3ml mixing granulate, with one-step-granulating method 18 orders of routine sieve, conventional pelletizing machine 14 order granulate; make granule neat; add magnesium stearate 1.5mg mixing, conventional tablet machine tabletting, 80 ℃ of dryings 4 hours, make the white plates product of every 160mg.
Embodiment 3
Add behind the water 3ml mixing with ivermectin 5mg, HPMCK4M 38mg, hexadecanol 15mg, lactose 100mg, microcrystalline Cellulose 40mg granulate, with one-step-granulating method 18 orders of routine sieve, conventional pelletizing machine 14 order granulate; make granule neat; add magnesium stearate 1.8mg mixing, conventional tablet machine tabletting, 80 ℃ of dryings 4 hours, make the white plates product of every 230mg.
Embodiment 4
Ivermectin 5mg, HPMCK4M 40mg, hexadecanol 10mg, lactose 100mg, microcrystalline Cellulose 32mg added behind the water 4ml mixing granulate, with one-step-granulating method 18 orders of routine sieve, conventional pelletizing machine 14 order granulate; make granule neat; add magnesium stearate 1.5mg mixing, conventional tablet machine tabletting, 80 ℃ of dryings 4 hours, make the white plates product of every 180mg.
Embodiment 5
Ivermectin 5mg, HPMCK4M 35mg, hexadecanol 20mg, lactose 100mg, microcrystalline Cellulose 32mg added behind the water 4ml mixing granulate, with one-step-granulating method 18 orders of routine sieve, conventional pelletizing machine 14 order granulate; make granule neat; add magnesium stearate 2.5mg mixing, conventional tablet machine tabletting, 80 ℃ of dryings 4 hours, make the white plates product of every 180mg.
Embodiment 6
Ivermectin 5mg, HPMCK4M 45mg, hexadecanol 13mg, lactose 120mg, microcrystalline Cellulose 45mg added behind the water 5ml mixing granulate, with one-step-granulating method 18 orders of routine sieve, conventional pelletizing machine 14 order granulate; make granule neat; add magnesium stearate 2.0mg mixing, conventional tablet machine tabletting, 80 ℃ of dryings 4 hours, make the white plates product of every 200mg.
Embodiment 7
Ivermectin 5mg, HPMCK4M 50mg, hexadecanol 15mg, lactose 115mg, microcrystalline Cellulose 32mg added behind the water 4ml mixing granulate, with one-step-granulating method 18 orders of routine sieve, conventional pelletizing machine 14 order granulate; make granule neat; add magnesium stearate 1.2mg mixing, conventional tablet machine tabletting, 80 ℃ of dryings 4 hours, make the white plates product of every 160mg.
Embodiment 8
Ivermectin 5mg, HPMCK4M 35mg, hexadecanol 12mg, lactose 95mg, microcrystalline Cellulose 36mg added behind the water 3ml mixing granulate, with one-step-granulating method 18 orders of routine sieve, conventional pelletizing machine 14 order granulate; make granule neat; add magnesium stearate 2.0mg mixing, conventional tablet machine tabletting, 80 ℃ of dryings 4 hours, make the white plates product of every 190mg.
Claims (3)
1. one kind is applicable to the anthelmintic sustained release tablet products of domestic animal, wherein contain 5 parts of ivermectins, it is characterized in that also containing in the described slow releasing tablet 30～50 parts of HPMCK4M, 8～15 parts of hexadecanols, 80～120 parts of lactose, 30～45 parts of microcrystalline Cellulose, 1～2.5 part of magnesium stearate; Above-mentioned various compositions are the commercial goods.
2. a kind of anthelmintic sustained release tablet products of domestic animal that is applicable to according to claim 1 is characterized in that the preferable use amount of various compositions is in the described slow releasing tablet: 5 parts of ivermectins, 40 parts of HPMCK4M, 10 parts of hexadecanols, 100 parts of lactose, 32 parts of microcrystalline Cellulose, 1.5 parts of magnesium stearate.
3. a kind of anthelmintic sustained release tablet products of domestic animal that is applicable to according to claim 1 is characterized in that described slow releasing tablet finished product is white, lamellar, and every specification can be 150～230mg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100526986A CN101301280A (en) | 2008-04-11 | 2008-04-11 | Sustained release tablet products used as helminthic of livestock |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100526986A CN101301280A (en) | 2008-04-11 | 2008-04-11 | Sustained release tablet products used as helminthic of livestock |
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| Publication Number | Publication Date |
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| CN101301280A true CN101301280A (en) | 2008-11-12 |
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| CNA2008100526986A Pending CN101301280A (en) | 2008-04-11 | 2008-04-11 | Sustained release tablet products used as helminthic of livestock |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN108653228A (en) * | 2018-08-15 | 2018-10-16 | 重庆市畜牧科学院 | Matrix type is sustained doractin tablet and preparation method thereof |
| CN109966438A (en) * | 2019-05-17 | 2019-07-05 | 石家庄九鼎动物药业有限公司 | A kind of antiparasite drugs for animals ivermectin injection and preparation method thereof |
| CN109985054A (en) * | 2017-12-29 | 2019-07-09 | 瑞普（天津）生物药业有限公司 | A kind of band regulation layer gel skeleton type ivermectin sustained release tablets |
-
2008
- 2008-04-11 CN CNA2008100526986A patent/CN101301280A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN109985054A (en) * | 2017-12-29 | 2019-07-09 | 瑞普（天津）生物药业有限公司 | A kind of band regulation layer gel skeleton type ivermectin sustained release tablets |
| CN108653228A (en) * | 2018-08-15 | 2018-10-16 | 重庆市畜牧科学院 | Matrix type is sustained doractin tablet and preparation method thereof |
| CN108653228B (en) * | 2018-08-15 | 2021-05-28 | 重庆市畜牧科学院 | Skeleton type sustained-release doramectin tablet and preparation method thereof |
| CN109966438A (en) * | 2019-05-17 | 2019-07-05 | 石家庄九鼎动物药业有限公司 | A kind of antiparasite drugs for animals ivermectin injection and preparation method thereof |
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Open date: 20081112 |