CN106580896A - Febantel dispersible tablet and preparation method thereof - Google Patents
Febantel dispersible tablet and preparation method thereof Download PDFInfo
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- CN106580896A CN106580896A CN201611130572.7A CN201611130572A CN106580896A CN 106580896 A CN106580896 A CN 106580896A CN 201611130572 A CN201611130572 A CN 201611130572A CN 106580896 A CN106580896 A CN 106580896A
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- febantel
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- dispersible tablet
- magnesium stearate
- pulvis talci
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a febantel dispersible tablet, which is prepared from the following raw materials and adjuvant materials in percentage by mass: 10-30% of febantel, 30-50% of starch, 15-30% of microcrystalline cellulose, 8-10% of sodium carboxymethyl starch, 1-3% of low-substituted hydroxypropyl cellulose, 0.5-2% of magnesium stearate and 0.5-2% of talcum powder. The febantel dispersible tablet prepared by the invention, under conditions of the type and dosage proportioning of the selected specific adjuvant materials, is high in disintegration speed and high in release degree; shortcomings of an existing febantel preparation are overcome; and the febantel dispersible tablet has a good application prospect.
Description
Technical field
The present invention relates to a kind of febantel dispersible tablet and preparation method thereof, belongs to field of medicaments.
Background technology
Animal parasitosis are the diseases caused by the various pathogenicity parasites for parasitizing animal body.Due to parasite it is normal
Chronic consumption is carried out to animal in a kind of extremely hidden mode, therefore is infected and is fallen ill not substantially, the loss for causing easily quilt
People ignore.Parasitic disease can consume Animal nutrition, reduce efficiency of feed utilization, and the economic loss for causing is quite serious, to herding
The fast development of industry causes greatly infringement.Major determinant is mainly manifested in and causes animal dead, reduces breeding performonce fo animals, shadow
Growth of animal is rung, is spread disease and animal product can be caused seriously to be discarded.
Febantel is one of antiparasitic conventional at present, and itself is converted in animal body sweet smell without anthelmintic activity
Parbendazole, fenbendazole sulfoxide and oxfendazole sulfone and play anthelmintic action, its effect and application be equal to fenbendazole, effect
Mechanism mainly plays a role with the tubulin binding of nematicide, and to the affinity of nematicide tubulin mammal is significantly higher than
Tubulin, it is not only strong to adult effect, also there are strong effect, also killing egg effect etc. to immaturity polypide and larva.
At present the conventional main dosage form of febantel of veterinary clinic is conventional tablet, granule etc., after taking administration orally, is existed
Disintegrate is slow, the low defect of release, and slow, blood medicine peak time is longer, bioavailability is low to cause animal to absorb.Therefore, urgently
A kind of new febantel preparation need to be developed, to overcome the drawbacks described above of existing dosage form.
The content of the invention
It is an object of the invention to provide a kind of febantel dispersible tablet and preparation method thereof.
The invention provides a kind of febantel dispersible tablet, it is prepared from by the supplementary material of following mass percents：
Febantel 10%～30%, starch 30%～50%, Microcrystalline Cellulose 15%～30%, carboxymethyl starch sodium 8%～10%,
Low-substituted hydroxypropyl cellulose 1%～3%, magnesium stearate 0.5%～2%, Pulvis Talci 0.5%～2%.
Preferably, it is prepared from by the supplementary material of following mass percents：It is febantel 20%, starch 40%, micro-
Crystalline cellulose 28%, carboxymethyl starch sodium 8%, low-substituted hydroxypropyl cellulose 1%, magnesium stearate 2%, Pulvis Talci 1%.
Further, the particle diameter of the febantel is less than 50 μm.
The invention provides a kind of preparation method of the febantel dispersible tablet, comprises the steps：
A, febantel is crushed to superfine powder, separately each adjuvant sieves for subsequent use respectively；
B, febantel, starch, Microcrystalline Cellulose, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose are mixed evenly,
Soft material processed, granulation is dried, granulate；
C, addition magnesium stearate and Pulvis Talci are mixed evenly, and tabletting is obtained final product.
Further, a steps by febantel in -20 DEG C of micronizing 30 minutes.
Further, a steps are crossed respectively 80 mesh sieves by each adjuvant.
Further, b step adds 20%v/v ethanol water soft materials.
Further, b step crosses the granulation of 20 mesh sieves, granulate.
Further, b step was in 50 DEG C of dryings more than 12 hours.
Further, step c adds magnesium stearate and Pulvis Talci to mix 30 minutes.
The invention provides a kind of febantel dispersible tablet.Under conditions of from specific supplementary product kind and consumption proportion,
The febantel dispersible tablet disintegration rate that the present invention is prepared is fast, and release is high, overcomes existing febantel preparation
Defect, application prospect is good.
Obviously, the above of the invention, according to the ordinary technical knowledge and customary means of this area, without departing from
Under the premise of the above-mentioned basic fundamental thought of the present invention, the modification of other various ways can also be made, is replaced or is changed.
By the following examples the specific embodiment of form, remakes further specifically to the above of the present invention
It is bright.But this scope for being interpreted as above-mentioned theme of the invention should not be only limitted to Examples below.It is all based on the above of the present invention
The technology realized belongs to the scope of the present invention.
Specific embodiment
Raw material, equipment used in the specific embodiment of the invention is known product, is obtained by buying commercially available prod.
The preparation of the febantel dispersible tablet of the present invention of embodiment 1
Preparation prescription (with 1000 gauge)
Preparation method：
(1) by A (- 20 DEG C) micronizing 30 minutes under cryogenic, superfine powder of the particle diameter less than 50 μm is obtained, B-G point
80 mesh sieves are not crossed, it is standby；
(2) A-E is mixed 30 minutes, obtains mixture, plus 20%v/v ethanol water soft materials, cross the granulation of 20 mesh sieves,
50 DEG C of dryings more than 12 hours, make pellet moisture control below 3%, after 20 mesh sieve granulate, add magnesium stearate and cunning
Stone powder is mixed 30 minutes, and tabletting is obtained final product.
The preparation of the febantel dispersible tablet of the present invention of embodiment 2
Preparation prescription (with 1000 gauge)
| Numbering | Supplementary material | Ratio | Weight |
| A | Febantel | 20% | 200 |
| B | Starch | 40% | 400 |
| C | Microcrystalline Cellulose | 28% | 280 |
| D | Carboxymethyl starch sodium | 8% | 80 |
| E | Low-substituted hydroxypropyl cellulose | 1% | 10 |
| F | Magnesium stearate | 2% | 20 |
| G | Pulvis Talci | 1% | 10 |
Preparation method：
(1) by A (- 20 DEG C) micronizing 30 minutes under cryogenic, superfine powder of the particle diameter less than 50 μm is obtained, B-G point
80 mesh sieves are not crossed, it is standby；
(2) A-E is mixed 30 minutes, obtains mixture, plus 20%v/v ethanol water soft materials, cross the granulation of 20 mesh sieves,
50 DEG C of dryings more than 12 hours, make pellet moisture control below 3%, after 20 mesh sieve granulate, add magnesium stearate and cunning
Stone powder is mixed 30 minutes, and tabletting is obtained final product.
The preparation of the febantel dispersible tablet of the present invention of embodiment 3
Preparation prescription (with 1000 gauge)
| Numbering | Supplementary material | Ratio | Weight |
| A | Febantel | 20% | 200 |
| B | Starch | 50% | 500 |
| C | Microcrystalline Cellulose | 15% | 150 |
| D | Carboxymethyl starch sodium | 10% | 100 |
| E | Low-substituted hydroxypropyl cellulose | 2% | 20 |
| F | Magnesium stearate | 1% | 10 |
| G | Pulvis Talci | 2% | 20 |
Preparation method：
(1) by A (- 20 DEG C) micronizing 30 minutes under cryogenic, superfine powder of the particle diameter less than 50 μm is obtained, B-G point
80 mesh sieves are not crossed, it is standby；
(2) A-E is mixed 30 minutes, obtains mixture, plus 20%v/v ethanol water soft materials, cross the granulation of 20 mesh sieves,
50 DEG C of dryings more than 12 hours, make pellet moisture control below 3%, after 20 mesh sieve granulate, add magnesium stearate and cunning
Stone powder is mixed 30 minutes, and tabletting is obtained final product.
The preparation of the febantel dispersible tablet of the present invention of embodiment 4
Preparation prescription (with 1000 gauge)
| Numbering | Supplementary material | Ratio | Weight |
| A | Febantel | 30% | 300 |
| B | Starch | 35% | 350 |
| C | Microcrystalline Cellulose | 20% | 200 |
| D | Carboxymethyl starch sodium | 10% | 100 |
| E | Low-substituted hydroxypropyl cellulose | 3% | 30 |
| F | Magnesium stearate | 0.50% | 5 |
| G | Pulvis Talci | 1.50% | 15 |
Preparation method：
(1) by A (- 20 DEG C) micronizing 30 minutes under cryogenic, superfine powder of the particle diameter less than 50 μm is obtained, B-G point
80 mesh sieves are not crossed, it is standby；
(2) A-E is mixed 30 minutes, obtains mixture, plus 20%v/v ethanol water soft materials, cross the granulation of 20 mesh sieves,
50 DEG C of dryings more than 12 hours, make pellet moisture control below 3%, after 20 mesh sieve granulate, add magnesium stearate and cunning
Stone powder is mixed 30 minutes, and tabletting is obtained final product.
The preparation of the common febantel piece of comparative example 1
Prescription is as follows with 1000 gauge：
| Numbering | Supplementary material | Ratio | Weight |
| A | Febantel | 35% | 875g |
| B | Starch | 40% | 1000g |
| C | Pulvis Talci | 18% | 450g |
| D | Dextrin | 5% | 125g |
| E | Magnesium stearate | 2% | 50g |
Preparation method：
(1) by A (- 20 DEG C) micronizing 30 minutes under cryogenic, superfine powder of the particle diameter less than 50 μm is obtained, B-E point
80 mesh sieves are not crossed, it is standby.
(2) A-D is mixed 30 minutes, obtains mixture, plus 20%v/v ethanol water soft materials, cross the granulation of 20 mesh sieves,
50 DEG C of dryings more than 12 hours, make pellet moisture control below 3%, after 20 mesh sieve granulate, add magnesium stearate to mix
30 minutes, tabletting was obtained final product.
Beneficial effects of the present invention are proved below by way of experimental example.
The disintegration of the febantel dispersible tablet of the present invention of experimental example 1
Press《Chinese veterinary pharmacopoeia》(version one in 2010) annex checks the febantel point for preparing according to embodiments of the present invention
The disintegration of discrete piece, inspection result such as table 1.
Table 1 disintegration of inspection result
Note：*, with conventional tablet group ratio, P<0.05；*, with conventional tablet group ratio, P<0.01.
◇, with 2 groups of ratios of embodiment, P<0.05；◇ ◇, with 2 groups of ratios of embodiment, P<0.01.
From inspection result disintegration, conventional tablet disintegration time is most long, and average time is 13.80 minutes, is owned
Embodiment group complete disintegrate, significant difference (P compared with conventional tablet group in 2 minutes<0.01)；Between each group, wherein in fact
Apply the difference extremely significantly (P compared with 2 groups of embodiment of example 4<0.01), the significant difference (P compared with 2 groups of embodiment of embodiment 3<
0.05), the disintegration time of embodiment 2 is most short.
The release of the febantel dispersible tablet of the present invention of experimental example 2
Press《Chinese veterinary pharmacopoeia》(version one in 2010) annex determines the febantel point for preparing according to embodiments of the present invention
The release of discrete piece.Febantel dispersible tablet and conventional tablet are taken, in putting stripping rotor, the time is rotated and record, respectively at certain
Time sampling, supplements immediately isothermal equal-volume dissolution medium, and 0.2 μm of filtering with microporous membrane of filtrate Jing, chloroform dissolving is simultaneously dilute
Release to scale, according to its content of high effective liquid chromatography for measuring, calculate Accumulation dissolution percentage rate (%), measurement result is shown in Table 2,3.
The drug release determination result of table 2
The 50min release comparative results of table 3
Note：*, with conventional tablet group ratio, P<0.05；*, with conventional tablet group ratio, P<0.01.
◇, with 2 groups of ratios of embodiment, P<0.05；◇◇, with 3 groups of ratios of embodiment, P<0.01.
Tested from drug release determination, it is of the invention by prepared composition discrete piece after febantel micronization, with common non-class
Tai Er pieces are compared, and release is significantly superior, and dissolution time significantly shortens, and the dissolution after 50 minutes shows up to more than 90%
Write and be better than conventional tablet.
Meanwhile, each group release results contrast determined from 50min, embodiment 1-4 group is compared with conventional tablet group
Difference extremely significantly (P<0.01), 3 groups of the embodiment significant difference (P compared with 2 groups of embodiment<0.05), 4 groups of embodiment and embodiment
2 groups are compared difference extremely significantly (P<0.01), 2 groups of dissolution rates of embodiment are most fast, the average release of 50 minutes up to 96.21%,
For the optimum prescription of febantel dispersible tablet screening.
Comprehensive disintegration and release, the prescription of preferred embodiment 2.
Comprehensive above experimental result, the febantel dispersible tablet disintegration rate that the present invention is prepared is fast, and release is high,
The defect of existing febantel preparation is overcome, application prospect is excellent.
Claims (10)
1. a kind of febantel dispersible tablet, is characterized in that：It is prepared from by the supplementary material of following mass percents：Febantel
That 10%～30%, starch 30%～50%, Microcrystalline Cellulose 15%～30%, carboxymethyl starch sodium 8%～10%, low replacement
Hydroxypropyl cellulose 1%～3%, magnesium stearate 0.5%～2%, Pulvis Talci 0.5%～2%.
2. febantel dispersible tablet as claimed in claim 1, is characterized in that：It is by the supplementary material system of following mass percents
It is standby to form：Febantel 20%, starch 40%, Microcrystalline Cellulose 28%, carboxymethyl starch sodium 8%, low substituted hydroxy-propyl fiber
Element 1%, magnesium stearate 2%, Pulvis Talci 1%.
3. febantel dispersible tablet as claimed in claim 1 or 2, is characterized in that：The particle diameter of the febantel is less than 50 μm.
4. a kind of preparation method of febantel dispersible tablet described in claims 1 to 3 any one, is characterized in that：Including as follows
Step：
A, febantel is crushed to superfine powder, separately each adjuvant sieves for subsequent use respectively；
B, febantel, starch, Microcrystalline Cellulose, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose are mixed evenly, are made soft
Material, granulation is dried, granulate；
C, addition magnesium stearate and Pulvis Talci are mixed evenly, and tabletting is obtained final product.
5. preparation method as claimed in claim 4, is characterized in that：A steps are by febantel in -20 DEG C of 30 points of micronizing
Clock.
6. preparation method as claimed in claim 4, is characterized in that：A steps are crossed respectively 80 mesh sieves by each adjuvant.
7. preparation method as claimed in claim 4, is characterized in that：B step adds 20%v/v ethanol water soft materials.
8. preparation method as claimed in claim 4, is characterized in that：B step crosses the granulation of 20 mesh sieves, granulate.
9. preparation method as claimed in claim 4, is characterized in that：B step was in 50 DEG C of dryings more than 12 hours.
10. preparation method as claimed in claim 4, is characterized in that：Step c adds magnesium stearate and Pulvis Talci to mix 30 points
Clock.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611130572.7A CN106580896A (en) | 2016-12-07 | 2016-12-07 | Febantel dispersible tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611130572.7A CN106580896A (en) | 2016-12-07 | 2016-12-07 | Febantel dispersible tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106580896A true CN106580896A (en) | 2017-04-26 |
Family
ID=58598493
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201611130572.7A Withdrawn CN106580896A (en) | 2016-12-07 | 2016-12-07 | Febantel dispersible tablet and preparation method thereof |
Country Status (1)
| Country | Link |
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| CN (1) | CN106580896A (en) |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060228399A1 (en) * | 2005-04-08 | 2006-10-12 | John Rose | Taste masked veterinary formulation |
| CN102100674A (en) * | 2009-12-16 | 2011-06-22 | 青岛康地恩药业有限公司 | Febantel chewable tablets for dogs and cats |
| CN103127019A (en) * | 2013-03-22 | 2013-06-05 | 成都乾坤动物药业有限公司 | Florfenicol dispersible tablet as well as preparation method and application thereof |
| CN105025885A (en) * | 2012-12-19 | 2015-11-04 | 拜耳动物保健有限责任公司 | Tablets with improved acceptance and good storage stability |
-
2016
- 2016-12-07 CN CN201611130572.7A patent/CN106580896A/en not_active Withdrawn
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060228399A1 (en) * | 2005-04-08 | 2006-10-12 | John Rose | Taste masked veterinary formulation |
| CN102100674A (en) * | 2009-12-16 | 2011-06-22 | 青岛康地恩药业有限公司 | Febantel chewable tablets for dogs and cats |
| CN105025885A (en) * | 2012-12-19 | 2015-11-04 | 拜耳动物保健有限责任公司 | Tablets with improved acceptance and good storage stability |
| CN103127019A (en) * | 2013-03-22 | 2013-06-05 | 成都乾坤动物药业有限公司 | Florfenicol dispersible tablet as well as preparation method and application thereof |
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Application publication date: 20170426 |
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