CN109364042A - A kind of Chinese medicine targeting Tilmicosin pellet and preparation method thereof - Google Patents
A kind of Chinese medicine targeting Tilmicosin pellet and preparation method thereof Download PDFInfo
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Abstract
The present invention relates to a kind of Chinese medicine targeting Tilmicosin pellets and preparation method thereof, by weight include the following raw material: 20 parts of Tilmicosin；5-10 parts of campanulaceae Ultramicro-powder；1-8 parts of ilex pubescens Ultramicro-powder；Disintegrating agent: 10-35 parts；Adhesive: 5-10 parts；Filler: 1-15 parts.Preparation method includes the following steps: 1, campanulaceae, ilex pubescens crush respectively, cross 350 meshes, obtain campanulaceae Ultramicro-powder and ilex pubescens Ultramicro-powder；2, bletilla striata polyoses glue is dissolved with water, and stirred evenly, obtain bletilla polysaccharide glue solution；3, it after Tilmicosin, campanulaceae Ultramicro-powder, ilex pubescens Ultramicro-powder, disintegrating agent, filler, will stir 10 minutes, bletilla polysaccharide glue solution be then added, continues stirring 30 minutes, softwood is made；4, softwood obtained is through granulation, ball blast, drying, coating to get pellet.The present invention can be improved Tilmicosin in the effective concentration of lung, increase the Absorption And Metabolism rate and utilization rate of drug.
Description
Technical field
The invention belongs to field of traditional Chinese veterinary, and in particular to a kind of Chinese medicine targeting Tilmicosin pellet and preparation method thereof.
Background technique
Tilmicosin is by a kind of dedicated antibiotic of the semi-synthetic livestock and poultry of hydrolysate of tylosin, to gram sun
Property bacterium, certain Gram-negative bacterias, mycoplasma, conveyor screw etc. have inhibiting effect；To pleuropneumonia actinomyces, Pasteurella tool
Have antibacterial activity more stronger than tylosin, be mainly used for prevent and treat domestic animal pneumonia (by Actinobacillus pleuropneumoniae, Pasteurella,
The infection such as mycoplasma cause), avian mycoplasmas disease and lactating mammal mazoitis.Tilmicosin belongs to macrolide antibiotics,
The lactone structure of specific 16 member ring can act on the site P in conjunction with the ribosomal 50S subunit of bacterium, inhibit transfer
The combination of enzyme prevent peptide bond is from from A to P bit shift, therefore inhibits protein to hinder the displacement of mRNA
Synthesis generates fungistatic effect.
Currently, taking orally there are two types of the administration routes of Tilmicosin and subcutaneous routes being administered, for the side of subcutaneous administration
For formula since clinical application is cumbersome, toxic side effect is big, and use is relatively fewer；And Oral administration the problem of being primarily present, is: 1)
Tilmicosin bitter, easily reduction appetite of livestock and poultry, to substantially reduce the feed intake of livestock and poultry, 2) active drug of pulmonary lesion is reached
Concentration is low and unstable, affects the curative effect of Tilmicosin.
Summary of the invention
It is an object of the invention to overcome the deficiencies of existing technologies, a kind of Chinese medicine targeting Tilmicosin pellet and its system are provided
Preparation Method can not only cover Tilmicosin bitter taste, additionally it is possible to improve Tilmicosin in the effective concentration of lung, increase drug
Absorption And Metabolism rate and utilization rate.
To achieve the goals above, the technical solution adopted by the present invention is as follows:
Technical solution one:
A kind of Chinese medicine targeting Tilmicosin pellet, includes the following raw material by weight:
20 parts of Tilmicosin；
5-10 parts of campanulaceae Ultramicro-powder；
1-8 parts of ilex pubescens Ultramicro-powder；
10-35 parts of disintegrating agent；
5-10 parts of adhesive；
1-15 parts of filler.
Further, the disintegrating agent is microcrystalline cellulose, sodium carboxymethylcellulose one or two.
Further, the disintegrating agent is microcrystalline cellulose.
Further, described adhesive is one or more of bletilla striata polyoses glue, dextrin, Icing Sugar.
Further, described adhesive is bletilla striata polyoses glue.
Further, the filler is selected from one or both of astragalus polyose, starch.
Further, the filler is selected from astragalus polyose.
Technical solution two:
A kind of preparation method of Chinese medicine targeting Tilmicosin pellet, specifically includes the following steps:
Step 1, campanulaceae, ilex pubescens are crushed with airslide disintegrating mill respectively, are crossed 350 meshes, are obtained campanulaceae Ultramicro-powder and ilex pubescens
Ultramicro-powder, it is spare；
Step 2, after weighing each raw material by weight, by the mass ratio 2:1 of bletilla striata polyoses glue and water, by bletilla striata polyoses glue with water-soluble
Solution, and stir evenly, obtain bletilla polysaccharide glue solution；
Step 3, by Tilmicosin, campanulaceae Ultramicro-powder, ilex pubescens Ultramicro-powder, microcrystalline cellulose and astragalus polyose in 60 turns/min revolving speed
Lower stirring 10 minutes, is then added the bletilla polysaccharide glue solution, continues stirring 30 minutes, softwood is made；
Step 4, softwood obtained are through granulation, ball blast, drying, coating to get pellet.
Further, the step 4 specifically includes following operation:
Step 4-1, after the softwood prepared being squeezed granulation, 40 meshes is crossed, drug granule is obtained；
Step 4-2, by drug granule obtained use shot-blasting machine with the speed of 150 turns/min carry out ball blast to the ball heart it is round as a ball after,
Fluidized drying 30 minutes, 45 DEG C are naturally cooling to, obtains the ball heart；
Step 4-3, coating auxiliary material is dissolved first with solvent, prepares coating solution, then, the ball heart is packed into multifunctional fluidized bed packet
Clothing machine, after air outlet temperature rises to 60 DEG C, by the ball heart and coating auxiliary material dry weight than 8 ~ 15:1, by coating solution through peristaltic pump
Gun spraying coating (frequency of the peristaltic pump is 70 ~ 80 times/min) is squeezed into, coating process air outlet temperature keeps 65 DEG C of left sides
It is right；Coating finishes, and continues at multifunctional fluidized bed seed-coating machine and keeps being dried for 15 minutes.
Further, the coating solution includes the raw material of following parts by weight: 5 ~ 10 parts of auxiliary material of coating；Solvent: anhydrous second
60 parts of alcohol；
Wherein, the coating auxiliary material includes hydroxypropyl methyl cellulose phthalate/5-8 parts of polyacrylic resin；Lemon triethylenetetraminehexaacetic acid
1-3 parts of ester；1-2 parts of talcum powder.
Compared with prior art, the beneficial effects of the present invention are:
1, drug Tilmicosin is entered lung channel using tying-in drug campanulaceae as targeting vector by the present invention, is improved Tilmicosin and is existed
Distribution in lung tissue improves its bioavilability to improve Tilmicosin in the effective concentration of lung；In addition, campanulaceae is also
The dissolubility of Tilmicosin can be effectively increased, to increase the absorption rate of Tilmicosin.
2, ilex pubescens activating microcirculation and removing stasis medicinal of the present invention, is verified through a large number of experiments, can be cooperateed with campanulaceae, and campanulaceae priming is promoted to return
It is acted on, campanulaceae is made to improve Tilmicosin in the significant effect enhancing of the effective concentration of lung；And it is used alone without this
Effect, may be related with the function of promoting blood circulation to disperse blood clots of ilex pubescens, by activating microcirculation and removing stasis medicinal, changes lung tissue and whole lectin from hemolymph
Change, be more conducive to campanulaceae priming channel tropism, increases the concentration that Tilmicosin enters lung；Tilmicosin is improved in lung tissue to reach
The purpose of effective concentration increases the Absorption And Metabolism rate and utilization rate of drug indirectly.In addition, campanulaceae and ilex pubescens can also play taste masking
Effect, solve the Entrance Problem of Tilmicosin.
3, campanulaceae of the present invention and ilex pubescens use Ultramicro-powder, and drug particle size is smaller, and the particle diameter of 350 mesh is 25 μm,
The cell dia of plant is 10-100 μm, selects 350 mesh, drug can be allowed to achieve the effect that broken wall, the drug effect of drug is made more
It brings into play.
4, the present invention is using microcrystalline cellulose as disintegrating agent, using bletilla striata polyoses glue as adhesive, using astragalus polyose as filler,
And be coated with hydroxypropyl methyl cellulose phthalate, triethyl citrate, talcum powder and solvent absolute ethyl alcohol, it can be realized
The controlled release of drug discharges, and discharges it in enteron aisle and dissolves, medicine irritation and signs of degradation caused by avoiding it from discharging in stomach.
Campanulaceae of the present invention, ilex pubescens can not only improve Tilmicosin in the effective concentration of lung, while campanulaceae has only
Cough resolving sputum, the effect of freeinging lung and relieving asthma, ilex pubescens, also have clearing heat and detoxicating effect, all medicines share, act synergistically between each drug,
Effect complements each other, and plays the role for the treatment of pig pulmonary infection class disease (such as swine plague, asthma, blue ear) jointly.
Specific embodiment
Further details of narration is carried out to the present invention with reference to embodiments.
Embodiment 1
A kind of Chinese medicine targeting Tilmicosin pellet, includes the following raw material by weight:
Tilmicosin 20kg；
Campanulaceae Ultramicro-powder 8kg；
Ilex pubescens Ultramicro-powder 6kg；
Disintegrating agent: microcrystalline cellulose 25kg；
Adhesive: bletilla striata polyoses glue 8kg；
Filler: astragalus polyose 8kg；
Hydroxypropyl methyl cellulose phthalate 5kg；
Triethyl citrate 2kg；
Talcum powder 1.5kg；
Solvent: dehydrated alcohol 60kg；
Water 4kg；
Preparation method are as follows:
Step 1, campanulaceae, ilex pubescens are crushed with airslide disintegrating mill respectively, are crossed 350 meshes, are obtained campanulaceae Ultramicro-powder and ilex pubescens
Ultramicro-powder, it is spare.
Step 2, after weighing each raw material by weight, by the mass ratio 2:1 of bletilla striata polyoses glue and water, by bletilla striata polyoses glue water
Dissolution, and stir evenly, obtain bletilla polysaccharide glue solution；
Tilmicosin, campanulaceae Ultramicro-powder, ilex pubescens Ultramicro-powder, microcrystalline cellulose and astragalus polyose are used trough-type mixture machine by step 3
It is stirred 10 minutes under 60 turns/min revolving speed, the bletilla polysaccharide glue solution is then added, continued stirring 30 minutes, be made soft
Material；
Step 4, softwood obtained are through granulation, ball blast, drying, coating to get pellet；
Step 4-1, after the softwood prepared being squeezed granulation, 40 meshes is crossed, drug granule is obtained；
Step 4-2, by drug granule obtained use shot-blasting machine with the speed of 150 turns/min carry out ball blast to the ball heart it is round as a ball after,
Fluidized drying 30 minutes, 45 DEG C are naturally cooling to, obtains the ball heart；
Step 4-3, first will coating auxiliary material hydroxypropyl methyl cellulose phthalate, triethyl citrate, talcum powder solvent without
Water-ethanol dissolution, prepares coating solution, then, the ball heart is packed into multifunctional fluidized bed seed-coating machine, rises to 60 DEG C to air outlet temperature
Afterwards, by the ball heart and coating auxiliary material dry weight ratio 10:1, by coating solution through peristaltic pump (frequency of the peristaltic pump be 75 times/
Min gun spraying coating) is squeezed into, coating process air outlet temperature is kept for 65 DEG C or so；Coating finishes, and continues at multi-functional fluidisation
Bed seed-coating machine keeps being dried for 15 minutes.
Embodiment 2
A kind of Chinese medicine targeting Tilmicosin pellet, includes the following raw material by weight:
Tilmicosin 20kg；
Campanulaceae Ultramicro-powder 5kg；
Ilex pubescens Ultramicro-powder 8kg；
Disintegrating agent: microcrystalline cellulose 10kg；
Adhesive: bletilla striata polyoses glue 5kg；
Filler: astragalus polyose 3kg；
Hydroxypropyl methyl cellulose phthalate 8kg；
Triethyl citrate 1kg；
Talcum powder 1kg；
Solvent: dehydrated alcohol 60kg；
Water 2.5kg；
Preparation method are as follows: with embodiment 1.
Embodiment 3
A kind of Chinese medicine targeting Tilmicosin pellet, includes the following raw material by weight:
Tilmicosin 20kg；
Campanulaceae Ultramicro-powder 10kg；
Ilex pubescens Ultramicro-powder 3kg；
Disintegrating agent: microcrystalline cellulose 35kg；
Adhesive: bletilla striata polyoses glue 10kg；
Filler: astragalus polyose 15kg；
Hydroxypropyl methyl cellulose phthalate 5kg；
Triethyl citrate 3kg；
Talcum powder 2kg；
Solvent: dehydrated alcohol 60kg；
Water 5kg.
Preparation method are as follows: with embodiment 1.
Comparative example 1
A kind of Chinese medicine targeting Tilmicosin pellet, includes the following raw material by weight:
Tilmicosin 20kg；
Campanulaceae Ultramicro-powder 8kg；
Disintegrating agent: microcrystalline cellulose 25kg；
Adhesive: bletilla striata polyoses glue 8kg；
Filler: astragalus polyose 8kg；
Hydroxypropyl methyl cellulose phthalate 5kg；
Triethyl citrate 2kg；
Talcum powder 1.5kg；
Solvent: dehydrated alcohol 60kg；
Water 4kg；
Preparation method are as follows:
Step 1, campanulaceae are crushed with airslide disintegrating mill, are crossed 350 meshes, are obtained campanulaceae Ultramicro-powder, spare；
Step 2, after weighing each raw material by weight, by the mass ratio 2:1 of bletilla striata polyoses glue and water, by bletilla striata polyoses glue with water-soluble
Solution, and stir evenly, obtain bletilla polysaccharide glue solution；
Step 3 turns Tilmicosin, campanulaceae Ultramicro-powder, microcrystalline cellulose and astragalus polyose using trough-type mixture machine in 60 turns/min
Speed lower stirring 10 minutes, the bletilla polysaccharide glue solution is then added, continues stirring 30 minutes, softwood is made；
Step 4, softwood obtained are through granulation, ball blast, drying, coating to get pellet；
Step 4-1, after the softwood prepared being squeezed granulation, 40 meshes is crossed, drug granule is obtained；
Step 4-2, by drug granule obtained use shot-blasting machine with the speed of 150 turns/min carry out ball blast to the ball heart it is round as a ball after,
Fluidized drying 30 minutes, 45 DEG C are naturally cooling to, obtains the ball heart；
Step 4-3, first will coating auxiliary material hydroxypropyl methyl cellulose phthalate, triethyl citrate, talcum powder solvent without
Water-ethanol dissolution, prepares coating solution, then, the ball heart is packed into multifunctional fluidized bed seed-coating machine, rises to 60 DEG C to air outlet temperature
Afterwards, by the ball heart and coating auxiliary material dry weight ratio 10:1, by coating solution through peristaltic pump (frequency of the peristaltic pump be 75 times/
Min gun spraying coating) is squeezed into, coating process air outlet temperature is kept for 65 DEG C or so；Coating finishes, and continues at multi-functional fluidisation
Bed seed-coating machine keeps being dried for 15 minutes.
Comparative example 2
A kind of Chinese medicine targeting Tilmicosin pellet, includes the following raw material by weight:
Tilmicosin 20kg；
Ilex pubescens Ultramicro-powder 6kg；
Disintegrating agent: microcrystalline cellulose 25kg；
Adhesive: bletilla striata polyoses glue 8kg；
Filler: astragalus polyose 8kg；
Hydroxypropyl methyl cellulose phthalate 5kg；
Triethyl citrate 2kg；
Talcum powder 1.5kg；
Solvent: dehydrated alcohol 60kg；
Water 4kg；
Preparation method are as follows:
Step 1 crushes ilex pubescens with airslide disintegrating mill, crosses 350 meshes, obtains ilex pubescens Ultramicro-powder, spare.
After weighing each raw material by weight, by the mass ratio 2:1 of bletilla striata polyoses glue and water, bletilla striata polyoses glue is used for step 2
Water dissolution, and stir evenly, obtain bletilla polysaccharide glue solution；
Tilmicosin, ilex pubescens Ultramicro-powder, microcrystalline cellulose and astragalus polyose are used trough-type mixture machine in 60 turns/min by step 3
It is stirred 10 minutes under revolving speed, the bletilla polysaccharide glue solution is then added, continued stirring 30 minutes, softwood is made；
Step 4, softwood obtained are through granulation, ball blast, drying, coating to get pellet；
Step 4-1, after the softwood prepared being squeezed granulation, 40 meshes is crossed, drug granule is obtained；
Step 4-2, by drug granule obtained use shot-blasting machine with the speed of 150 turns/min carry out ball blast to the ball heart it is round as a ball after,
Fluidized drying 30 minutes, 45 DEG C are naturally cooling to, obtains the ball heart；
Step 4-3, first will coating auxiliary material hydroxypropyl methyl cellulose phthalate, triethyl citrate, talcum powder solvent without
Water-ethanol dissolution, prepares coating solution, then, the ball heart is packed into multifunctional fluidized bed seed-coating machine, rises to 60 DEG C to air outlet temperature
Afterwards, by the ball heart and coating auxiliary material dry weight ratio 10:1, by coating solution through peristaltic pump (frequency of the peristaltic pump be 75 times/
Min gun spraying coating) is squeezed into, coating process air outlet temperature is kept for 65 DEG C or so；Coating finishes, and continues at multi-functional fluidisation
Bed seed-coating machine keeps being dried for 15 minutes.
Comparative example 3
A kind of Chinese medicine targeting Tilmicosin pellet, includes the following raw material by weight:
Tilmicosin 20kg；
Root bark of white mulberry Ultramicro-powder 8kg；
Disintegrating agent: microcrystalline cellulose 25kg；
Adhesive: bletilla striata polyoses glue 8kg；
Filler: astragalus polyose 8kg；
Hydroxypropyl methyl cellulose phthalate 5kg；
Triethyl citrate 2kg；
Talcum powder 1.5kg；
Solvent: dehydrated alcohol 60kg；
Water 4kg；
Preparation method are as follows:
Step 1 crushes the root bark of white mulberry with airslide disintegrating mill, crosses 350 meshes, obtains root bark of white mulberry Ultramicro-powder, spare.
Step 2, after weighing each raw material by weight, by the mass ratio 2:1 of bletilla striata polyoses glue and water, by bletilla striata polyoses glue water
Dissolution, and stir evenly, obtain bletilla polysaccharide glue solution；
Tilmicosin, root bark of white mulberry Ultramicro-powder, microcrystalline cellulose and astragalus polyose are used trough-type mixture machine in 60 turns/min by step 3
It is stirred 10 minutes under revolving speed, the bletilla polysaccharide glue solution is then added, continued stirring 30 minutes, softwood is made；
Step 4, softwood obtained are through granulation, ball blast, drying, coating to get pellet；
Step 4-1, after the softwood prepared being squeezed granulation, 40 meshes is crossed, drug granule is obtained；
Step 4-2, by drug granule obtained use shot-blasting machine with the speed of 150 turns/min carry out ball blast to the ball heart it is round as a ball after,
Fluidized drying 30 minutes, 45 DEG C are naturally cooling to, obtains the ball heart；
Step 4-3, first will coating auxiliary material hydroxypropyl methyl cellulose phthalate, triethyl citrate, talcum powder solvent without
Water-ethanol dissolution, prepares coating solution, then, the ball heart is packed into multifunctional fluidized bed seed-coating machine, rises to 60 DEG C to air outlet temperature
Afterwards, by the ball heart and coating auxiliary material dry weight ratio 10:1, by coating solution through peristaltic pump (frequency of the peristaltic pump be 75 times/
Min gun spraying coating) is squeezed into, coating process air outlet temperature is kept for 65 DEG C or so；Coating finishes, and continues at multi-functional fluidisation
Bed seed-coating machine keeps being dried for 15 minutes.
Comparative example 4
A kind of Chinese medicine targeting Tilmicosin pellet, includes the following raw material by weight:
Tilmicosin 20kg；
Disintegrating agent: microcrystalline cellulose 25kg；
Adhesive: bletilla striata polyoses glue 8kg；
Filler: astragalus polyose 8kg.
Hydroxypropyl methyl cellulose phthalate 5kg；
Triethyl citrate 2kg；
Talcum powder 1.5kg；
Solvent: dehydrated alcohol 60kg；
Water 4kg；
Preparation method are as follows:
Step 1, after weighing each raw material by weight, by the mass ratio 2:1 of bletilla striata polyoses glue and water, by bletilla striata polyoses glue with water-soluble
Solution, and stir evenly, obtain bletilla polysaccharide glue solution；
Tilmicosin, microcrystalline cellulose and astragalus polyose are stirred 10 points using trough-type mixture machine by step 2 under 60 turns/min revolving speed
Then the bletilla polysaccharide glue solution is added in clock, continue stirring 30 minutes, softwood is made；
Step 3, softwood obtained are through granulation, ball blast, drying, coating to get pellet；
Step 3-1, after the softwood prepared being squeezed granulation, 40 meshes is crossed, drug granule is obtained；
Step 3-2, by drug granule obtained use shot-blasting machine with the speed of 150 turns/min carry out ball blast to the ball heart it is round as a ball after,
Fluidized drying 30 minutes, 45 DEG C are naturally cooling to, obtains the ball heart；
Step 3-3, first will coating auxiliary material hydroxypropyl methyl cellulose phthalate, triethyl citrate, talcum powder solvent without
Water-ethanol dissolution, prepares coating solution, then, the ball heart is packed into multifunctional fluidized bed seed-coating machine, rises to 60 DEG C to air outlet temperature
Afterwards, by the ball heart and coating auxiliary material dry weight ratio 10:1, by coating solution through peristaltic pump (frequency of the peristaltic pump be 75 times/
Min gun spraying coating) is squeezed into, coating process air outlet temperature is kept for 65 DEG C or so；Coating finishes, and continues at multi-functional fluidisation
Bed seed-coating machine keeps being dried for 15 minutes.
Effect example 1: the Drug-time curve of lung
One, sample:
Health pig 65,5 groups are randomly divided into, one group is respectively tested, one group of comparison, two groups of comparison, compares three groups and comparison four
Group, Tilmicosin is according to per kilogram of body weight respectively: Tilmicosin dosage 40mg/kg(feed addition dosage 400mg/kg)
Fed and (when each test group and contrast groups are fed, carry out equivalent administration according to Tilmicosin actual content), after feeding
0.25,0.5,1,2,4,6,8,12,24,36,48,72,96h is butchered, sterile to take lung tissue, dry with normal saline flushing
Only, it is cut into small pieces, after the homogenate of 12000rpm high-speed homogenization machine, -20 DEG C of freezen protectives, and carry out Tilmicosin assay, medicine
When curve data be shown in Table 1.
Two, it is grouped situation
It tests one group: being administered using pellet made from embodiment 1；
It compares one group: being administered using pellet made from comparative example 1；
It compares two groups: being administered using pellet made from comparative example 2；
It compares three groups: being administered using pellet made from comparative example 3；
It compares four groups: being administered using pellet made from comparative example 4；
Three, Tilmicosin measuring method: HPLC method is used；It is specific as follows:
1, sample pre-treatments:
Preparation weighs 5.0g lung tissue, is placed in 50ml polypropylene centrifuge tube, adds 8ml acetonitrile, and whirling motion mixes, middling speed concussion
30min, 3000rpm are centrifuged 10 minutes, and supernatant is taken to set 100ml centrifuge tube, are separately added into 5ml biphosphate into tissue grumeleuse
Potassium buffer and 8ml acetonitrile, stirring make tissue grumeleuse scatter, and whirling motion mixes, and middling speed shakes 30min, and 3000rpm is centrifuged 10 points
Clock merges supernatant twice and adds water 40ml, 3000rpml to be centrifuged 10min in 100ml centrifuge tube, supernatant is taken to hold in appropriate
In device, 10ml water is added to mix, crosses SPE column.
Extracting solution is crossed into SPE column, first uses 10ml methanol to activate and purified with 10ml and balances SPE column, when sample passes through SPE column
When, the pressure for adjusting vacuum pump keeps flow velocity too fast, about 1 drop/sec, flow speed stability is kept, with 25% acetonitrile-pure water-pure acetonitrile
Washing methods washed, 1 drop/sec of flow velocity, after acetonitrile is flowed out from SPE column, allow the dry at least 5min of SPE column, finally use
In scale test tube, Rotary Evaporators are evaporated 2.5ml elution, and flowing phase dilution is settled to 1ml, whirling motion 30s, are placed
15min, 0.22 micrometer pinhole formula membrane filtration take 20 microlitres to analyze into HPLC.
2, chromatographic condition:
Chromatographic column: 5 μm of C18 chromatographic column 150*4.6mm
Mobile phase: acetonitrile: tetrahydrofuran: dibutyl amine phosphate buffer: water=130:55:25:790
Flow velocity: 0.7ml/min
Column temperature: 30 DEG C
Table 1
As the result is shown: four groups of control, one group of comparison, two groups of comparison, the drug concentration for comparing Tilmicosin in lung tissue in three groups
It significantly lower than testing one group, therefore, can prove that ilex pubescens can cooperate with campanulaceae, promote the effect of campanulaceae priming channel tropism, make tangerine
Obstruct and is improving Tilmicosin in the significant effect enhancing of the effective concentration of lung.In addition, two groups of comparison reached blood medicine at 2 hours
Peak, may be as caused by changing that it changes blood flow, but general effect still not as good as comparison one group and test one
Group.
Effect example 2: release profiles
Operating process described in 160 drug dissolution of annex and drug release determination in 2015 editions veterinary drug allusion quotations, prepares embodiment 1
Pellet, carries out slaking test, and release profiles data are shown in Table 2；
Table 2
It can be seen that, the enteric-coated micro-pill of preparation can be realized place release, reach the quality standard of enteric coated preparations from table.
Effect example 3: clinical trial result analysis
Clinical natural occurrence swinery, 116 growing and fattening pigs, part body temperature increase, and foam sample liquid is flowed out in cough, asthma from mouth, nose
Body；Have difficulty in breathing into sitting position of dog gesture；Neck, bottleneck throat have inflammatory swelling；Dissect: subcutaneous, thoracic cavity, pericardium have hydrops；Liver,
Lungs, lymph node bleeding, enlargement；It raises flowers line in marble lung section；It is diagnosed as swine plague, 104 pigs of survival are divided at random
It is 4 groups, drug treatment, dosage are administered according to per kilogram feed addition dosage 400mg Tilmicosin, the full group of spice respectively,
Treatment results are recorded, see the table below 3 and table 4, when administration, each test group and contrast groups are converted into according to Tilmicosin actual content
Administration.
Grouping situation: it see the table below；
It tests one group: being administered using pellet made from embodiment 1；
It compares one group: being administered using pellet made from comparative example 1；
It compares two groups: being administered using pellet made from comparative example 4；
Conventional medicine group: Tilmicosin pulvis.
Table 3
Table 4
It is shown from above-mentioned experimental result, one group of effect of test is optimal, the time required to treated effect, cure rate and healing
Better than missing ilex pubescens one group of comparison, lack the common pellets group of campanulaceae and ilex pubescens, can prove campanulaceae, ilex pubescens with
Tilmicosin can cooperate with action, significantly improve therapeutic effect, and treatment time greatly shortens, may can be with ilex pubescens
Campanulaceae collaboration promotes the effect of campanulaceae priming channel tropism, and campanulaceae is made to improve Tilmicosin in the significant effect of the effective concentration of lung
Enhance related.And two groups are compared compared with conventional medicine group, treated effect is preferable, it may be possible to, coating related with following factors
Afterwards, 1) feed intake improves, and reduces the factor that part pig does not search for food by the addition of Tilmicosin, and 2) reduce Tilmicosin in stomach
Medicine irritation caused by portion discharges and signs of degradation, and clinical effectiveness is higher than normal packet by pellet.
Embodiment described above is merely a preferred embodiment of the present invention, and the simultaneously exhaustion of the feasible implementation of non-present invention.It is right
For persons skilled in the art, any aobvious to made by it under the premise of without departing substantially from the principle of the invention and spirit and
The change being clear to should be all contemplated as falling within claims of the invention.
Claims (7)
1. a kind of Chinese medicine targets Tilmicosin pellet, which is characterized in that by weight include the following raw material:
20 parts of Tilmicosin；
5-10 parts of campanulaceae Ultramicro-powder；
1-8 parts of ilex pubescens Ultramicro-powder；
10-35 parts of disintegrating agent；
5-10 parts of adhesive；
1-15 parts of filler.
2. a kind of Chinese medicine according to claim 1 targets Tilmicosin pellet, which is characterized in that the disintegrating agent is crystallite
Fiber, sodium carboxymethylcellulose are one or two kinds of.
3. a kind of Chinese medicine according to claim 1 targets Tilmicosin pellet, which is characterized in that described adhesive is the bletilla striata
One or more of polysaccharide gum, dextrin, Icing Sugar.
4. a kind of Chinese medicine according to claim 1 targets Tilmicosin pellet, which is characterized in that the filler is selected from Huang
One or both of astragalus polysaccharides, starch.
5. any one a kind of preparation method of Chinese medicine targeting Tilmicosin pellet according to claim 1 ~ 4, which is characterized in that
Specifically includes the following steps:
Step 1, campanulaceae, ilex pubescens are crushed with airslide disintegrating mill respectively, are crossed 350 meshes, are obtained campanulaceae Ultramicro-powder and ilex pubescens
Ultramicro-powder, it is spare；
Step 2, after weighing each raw material by weight, by the mass ratio 2:1 of bletilla striata polyoses glue and water, by bletilla striata polyoses glue with water-soluble
Solution, and stir evenly, obtain bletilla polysaccharide glue solution；
Step 3, by Tilmicosin, campanulaceae Ultramicro-powder, ilex pubescens Ultramicro-powder, microcrystalline cellulose and astragalus polyose in 60 turns/min revolving speed
Lower stirring 10 minutes, is then added the bletilla polysaccharide glue solution, continues stirring 30 minutes, softwood is made；
Step 4, softwood obtained are through granulation, ball blast, drying, coating to get pellet.
6. a kind of preparation method of Chinese medicine targeting Tilmicosin pellet according to claim 5, which is characterized in that the step
4 specifically include following operation:
Step 4-1, after the softwood prepared being squeezed granulation, 40 meshes is crossed, drug granule is obtained；
Step 4-2, by drug granule obtained use shot-blasting machine with the speed of 150 turns/min carry out ball blast to the ball heart it is round as a ball after,
Fluidized drying 30 minutes, 45 DEG C are naturally cooling to, obtains the ball heart；
Step 4-3, coating auxiliary material is dissolved first with solvent, prepares coating solution, then, the ball heart is packed into multifunctional fluidized bed packet
Clothing machine, after air outlet temperature rises to 60 DEG C, by the ball heart and coating auxiliary material dry weight than 8 ~ 15:1, by coating solution through peristaltic pump
Gun spraying coating is squeezed into, coating process air outlet temperature is kept for 65 DEG C or so；Coating finishes, and continues at multifunctional fluidized bed packet
Clothing machine keeps being dried for 15 minutes.
7. a kind of preparation method of Chinese medicine targeting Tilmicosin pellet according to claim 6, which is characterized in that the packet
Clothing liquid includes the raw material of following parts by weight: 5 ~ 10 parts of auxiliary material of coating；Solvent: 60 parts of dehydrated alcohol；
Wherein, the coating auxiliary material includes hydroxypropyl methyl cellulose phthalate or 3-8 parts of polyacrylic resin；Lemon triethylenetetraminehexaacetic acid
1-3 parts of ester；1-2 parts of talcum powder.
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Application publication date: 20190222 Assignee: Beijing Leguan Pet Products Co.,Ltd. Assignor: HEBEI DEPOND ANIMAL HEALTH TECHNOLOGY CO.,LTD. Contract record no.: X2023980036556 Denomination of invention: A Chinese medicine targeted Tilmicosin pellets and its preparation method Granted publication date: 20210402 License type: Common License Record date: 20230613 |