CN106491549B - A kind of deccox dispersible tablet and its preparation method and application - Google Patents
A kind of deccox dispersible tablet and its preparation method and application Download PDFInfo
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- CN106491549B CN106491549B CN201611153467.5A CN201611153467A CN106491549B CN 106491549 B CN106491549 B CN 106491549B CN 201611153467 A CN201611153467 A CN 201611153467A CN 106491549 B CN106491549 B CN 106491549B
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- deccox
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- talcum powder
- starch
- dispersible tablet
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Classifications
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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
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K9/2009—Inorganic compounds
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Abstract
The invention discloses a kind of deccox dispersible tablets, it is prepared by the supplementary material of following weight proportion: 6 parts of deccox, 55-65 parts of microcrystalline cellulose, 9-18 parts of starch, 4-10 parts of low-substituted hydroxypropyl cellulose, 4 parts of crosslinked polyvinylpyrrolidone, 8 parts of talcum powder.Under conditions of the specific supplementary product kind of the present invention and consumption proportion, the disintegrating property for the deccox dispersible tablet being prepared is excellent, and release is good, overcomes the defect of existing deccox preparation, and application prospect is good.
Description
Technical field
The present invention relates to field of medicaments, and in particular to a kind of deccox dispersible tablet and its preparation method and application.
Background technique
Chicken coccidiasis is to parasitize chicken intestinal epithelial cell by a variety of coccidias of Eimeriidae, Eimeria (Eimeria)
A kind of caused parasitic protozoa disease, is in worldwide distribution, there is globidiosis in nearly all intensive chicken farm, to young bird
The harm of chicken is more serious, and disease incidence may be up to 50%~70%, and case fatality rate is generally 20%~30%, is up to when serious
80% chicken death brings huge economic loss to world's poultry husbandry.
Deccox (Decoquinate) is a kind of effective quinoline ester (Quinolone) class chemical coccidiostas, chemistry
Entitled 6-methoxy-7-ethoxy-4-hydroxyquinoline-3-carboxylic acid ethyl ester clinically has unique Anti-human globulin test, can
Globidiosis caused by displacement, tender, huge, heap-type, murder by poisoning and Bu Shi Amy ear for preventing and treating chicken etc., commonly uses anti-ball with other
Worm drug, which is compared, has higher chemical activity and lower toxicity, has good effect to a variety of Eimeria species.Due to last of the ten Heavenly stems oxygen
Quinoline ester using less, not yet develop drug resistance in China, is a kind of novel anticoccidial drug having wide application prospects.
Currently, the common deccox dosage form of veterinary clinic mainly has the dosage forms such as pre-mixing agent, solution, suspension, these
Dosage form is long placed in and the disadvantages of rotten easily occurs there are inconvenient to carry.
Therefore, it is necessary to develop it is a kind of carry, deccox preparation easy to use, with to provide one to veterinary clinic
Safely, effectively, the quality controllable drug for being used to prevent poultry against coccidia.
Summary of the invention
To solve the above problems, it is auxiliary by the original of following weight proportion the present invention provides a kind of deccox dispersible tablet
Material is prepared:
6 parts of deccox, 9-18 parts of starch, 4-10 parts of low-substituted hydroxypropyl cellulose, is handed over 55-65 parts of microcrystalline cellulose
Join 4 parts of polyvinylpyrrolidone, 8 parts of talcum powder.
Further, it is prepared by the supplementary material of following weight proportion:
6 parts of deccox, 55 parts of microcrystalline cellulose, 18 parts of starch, 9 parts of low-substituted hydroxypropyl cellulose, crosslinked polyethylene
4 parts of pyrrolidones, 8 parts of talcum powder.
Further, comprising the following steps:
(1) deccox is taken, is pulverized；Microcrystalline cellulose, starch, low-substituted hydroxypropyl cellulose, crosslinked polyethylene
Pyrrolidones and talcum powder, sieve for subsequent use respectively；
(2) by deccox, microcrystalline cellulose, starch, low-substituted hydroxypropyl cellulose and crosslinked polyvinylpyrrolidone
Mix, softwood processed, pelletize, dry, whole grain adds talcum powder, mix, tabletting to get.
Further, in step (1), the ultramicro grinding is pulverized deccox to partial size less than 50 μm.
Further, in step (1), the temperature of the ultramicro grinding is -20 DEG C.
Further, in step (1), by deccox, microcrystalline cellulose, starch, low-substituted hydroxypropyl cellulose, crosslinking
Polyvinylpyrrolidone and talcum powder cross 80 meshes respectively.
Further, in step (2), softwood processed uses 30% ethyl alcohol, crosses the granulation of 20 meshes, and drying to pellet moisture exists
3% hereinafter, sieving whole grain.
The present invention also provides aforementioned deccox dispersible tablets to prepare the purposes in coccidiostat.
Further, the coccidiostat is drug for treating animal coccidiosis.
Further, the coccidiostat is anticoccidial drugs object.
Experiment results proved, under conditions of the specific supplementary product kind of the present invention and consumption proportion, the last of the ten Heavenly stems oxygen quinoline that is prepared
The disintegrating property of ester dispersible tablet is excellent, and release is good, overcomes the defect of existing deccox preparation, and application prospect is good.
Obviously, above content according to the present invention is not being departed from according to the ordinary technical knowledge and customary means of this field
Under the premise of the above-mentioned basic fundamental thought of the present invention, the modification, replacement or change of other diversified forms can also be made.
The specific embodiment of form by the following examples remakes further specifically above content of the invention
It is bright.But the range that this should not be interpreted as to the above-mentioned theme of the present invention is only limitted to example below.It is all to be based on above content of the present invention
The technology realized all belongs to the scope of the present invention.
Specific embodiment
Raw material, equipment used in the specific embodiment of the invention are known product, are obtained by purchase commercial product.
The preparation of the deccox dispersible tablet of the present invention of embodiment 1 (raw material does not carry out micro mist processing)
Prescription is as follows with 1000 meters:
| Number | Supplementary material | Ratio (%) | Weight (g) |
| A | Deccox | 6 | 108 |
| B | Microcrystalline cellulose | 60 | 1080 |
| C | Starch | 18 | 324 |
| D | Low-substituted hydroxypropyl cellulose | 4 | 72 |
| E | Crosslinked polyvinylpyrrolidone | 4 | 72 |
| F | Talcum powder | 8 | 144 |
Preparation method:
(1) A is sieved with 100 mesh sieve, B-F crosses 80 meshes respectively, spare.
(2) A-E is mixed, obtains mixture, add 30% ethyl alcohol softwood, cross the granulation of 20 meshes, 50 DEG C drying 12 hours
More than, make pellet moisture control 3% hereinafter, sieving whole grain after, add talcum powder to mix, tabletting to get.
The preparation of the deccox dispersible tablet of the present invention of embodiment 2
Prescription is as follows with 1000 meters:
| Number | Supplementary material | Ratio (%) | Weight (g) |
| A | Deccox | 6 | 108 |
| B | Microcrystalline cellulose | 60 | 1080 |
| C | Starch | 18 | 324 |
| D | Low-substituted hydroxypropyl cellulose | 4 | 72 |
| E | Crosslinked polyvinylpyrrolidone | 4 | 72 |
| F | Talcum powder | 8 | 144 |
Preparation method:
(1) A is pulverized 30 minutes for (- 20 DEG C) under cryogenic, obtains Ultramicro-powder of the partial size less than 50 μm, B-F divides
80 meshes are not crossed, it is spare.
(2) A-E is mixed, obtains mixture, add 30% ethyl alcohol softwood, cross the granulation of 20 meshes, 50 DEG C drying 12 hours
More than, make pellet moisture control 3% hereinafter, sieving whole grain after, add talcum powder to mix, tabletting to get.
The preparation of the deccox dispersible tablet of the present invention of embodiment 3
Prescription is as follows with 1000 meters:
| Number | Supplementary material | Ratio (%) | Weight (g) |
| A | Deccox | 6 | 108 |
| B | Microcrystalline cellulose | 65 | 1170 |
| C | Starch | 9 | 162 |
| D | Low-substituted hydroxypropyl cellulose | 8 | 144 |
| E | Crosslinked polyvinylpyrrolidone | 4 | 72 |
| F | Talcum powder | 8 | 144 |
Preparation method:
(1) A is pulverized 30 minutes for (- 20 DEG C) under cryogenic, obtains Ultramicro-powder of the partial size less than 50 μm, B-F divides
80 meshes are not crossed, it is spare.
(2) A-E is mixed, obtains mixture, add 30% ethyl alcohol softwood, cross the granulation of 20 meshes, 50 DEG C drying 12 hours
More than, make pellet moisture control 3% hereinafter, sieving whole grain after, add talcum powder to mix, tabletting to get.
The preparation of the deccox dispersible tablet of the present invention of embodiment 4
Prescription is as follows with 1000 meters:
| Number | Supplementary material | Ratio (%) | Weight (g) |
| A | Deccox | 6 | 108 |
| B | Microcrystalline cellulose | 55 | 990 |
| C | Starch | 18 | 324 |
| D | Low-substituted hydroxypropyl cellulose | 9 | 162 |
| E | Crosslinked polyvinylpyrrolidone | 4 | 72 |
| F | Talcum powder | 8 | 144 |
Preparation method:
(1) A is pulverized 30 minutes for (- 20 DEG C) under cryogenic, obtains Ultramicro-powder of the partial size less than 50 μm, B-F divides
80 meshes are not crossed, it is spare.
(2) A-E is mixed, obtains mixture, add 30% ethyl alcohol softwood, cross the granulation of 20 meshes, 50 DEG C drying 12 hours
More than, make pellet moisture control 3% hereinafter, sieving whole grain after, add talcum powder to mix, tabletting to get.
The preparation of the deccox dispersible tablet of the present invention of embodiment 5
Prescription is as follows with 1000 meters:
| Number | Supplementary material | Ratio (%) | Weight (g) |
| A | Deccox | 6 | 108 |
| B | Microcrystalline cellulose | 60 | 1080 |
| C | Starch | 12 | 216 |
| D | Low-substituted hydroxypropyl cellulose | 10 | 180 |
| E | Crosslinked polyvinylpyrrolidone | 4 | 72 |
| F | Talcum powder | 8 | 144 |
Preparation method:
(1) A is pulverized 30 minutes for (- 20 DEG C) under cryogenic, obtains Ultramicro-powder of the partial size less than 50 μm, B-F divides
80 meshes are not crossed, it is spare.
(2) A-E is mixed, obtains mixture, add 30% ethyl alcohol softwood, cross the granulation of 20 meshes, 50 DEG C drying 12 hours
More than, make pellet moisture control 3% hereinafter, sieving whole grain after, add talcum powder to mix, tabletting to get.
Illustrate beneficial effects of the present invention with the mode of experimental example below:
1, disintegration time limited checks
Checked that inspection result is as shown in table 1 below by " Chinese veterinary pharmacopoeia " (version one in 2010) annex.
Table 1 disintegration time limited inspection result
Note: *, with 4 groups of ratios of embodiment, P < 0.05；*, with 4 groups of ratios of embodiment, P < 0.01.
By disintegration time limited inspection result it is found that all embodiment groups are disintegrated in 1 minute completely, meet States Pharmacopoeia specifications.
Wherein, example 1 group, 2 groups, 3 groups compared with 4 groups of embodiment, significant difference (P < 0.01), 4 disintegration time of embodiment is most short.
2, drug release determination
It is measured by " Chinese veterinary pharmacopoeia " (version one in 2010) annex, revolving speed is (100 ± 1) 100rmin-1, temperature perseverance
Temperature is in (37 ± 0.5) DEG C.Precision weighs deccox dispersible tablet, sets in stripping rotor, the time is started turning and record, respectively at one
It fixes time and samples 5mL, supplement the isometric dissolution medium of isothermal immediately, filtrate is diluted to through 0.8 μm of filtering with microporous membrane with ethyl alcohol
Scale measures absorbance A at Yu Bochang 265nm, calculates cumulative release percentage (%) with calibration curve equation.Drug release determination
As a result it see the table below.
2 drug release determination result of table
3 50min release comparison result of table
Note: *, with example 1 group ratio, P < 0.05；*, with example 1 group ratio, P < 0.01.
◇, with 4 groups of ratios of embodiment, P < 0.05；◇◇, with 4 groups of ratios of embodiment, P < 0.01.
It is tested by drug release determination it is found that dispersible tablet (embodiment 2-5) is prepared after deccox is micronized, with non-micro mist
The dispersible tablet (embodiment 1) of change is compared, and release has extremely significant difference (P < 0.05), and dissolution time shortens obviously, can be improved
With overcome the problems, such as that deccox solubility is poor；Meanwhile 2,3 groups of embodiment compared with 4 groups of embodiment, difference it is extremely significant (P <
0.05), it was demonstrated that prepare dispersible tablet after being micronized deccox, 4 groups of dissolution rates of embodiment are most fast, disperse for deccox
The optimal prescription of piece.
In conclusion the deccox being prepared divides under conditions of the specific supplementary product kind of the present invention and consumption proportion
The disintegrating property of discrete piece is excellent, and release is good, overcomes the defect of existing deccox preparation, and application prospect is good.
Claims (4)
1. a kind of deccox dispersible tablet, it is characterised in that: it is prepared by the supplementary material of following weight proportion:
6 parts of deccox, 55 parts of microcrystalline cellulose, 18 parts of starch, 9 parts of low-substituted hydroxypropyl cellulose, crosslinked polyethylene pyrroles
4 parts of alkanone, 8 parts of talcum powder；
The preparation method of the dispersible tablet the following steps are included:
(1) deccox is taken, is pulverized；Microcrystalline cellulose, starch, low-substituted hydroxypropyl cellulose, crosslinked polyethylene pyrroles
Alkanone and talcum powder, sieve for subsequent use respectively；
(2) deccox, microcrystalline cellulose, starch, low-substituted hydroxypropyl cellulose and crosslinked polyvinylpyrrolidone are mixed,
Softwood processed is pelletized, dry, and whole grain adds talcum powder, is mixed, tabletting to get；
Wherein, in step (1), the ultramicro grinding is to pulverize deccox to partial size less than 50 μm, ultramicro grinding
Temperature is -20 DEG C；In step (1), by deccox, microcrystalline cellulose, starch, low-substituted hydroxypropyl cellulose, the poly- second of crosslinking
Alkene pyrrolidone and talcum powder cross 80 meshes respectively；In step (2), softwood processed uses 30% ethyl alcohol, crosses the granulation of 20 meshes, dry
To pellet moisture 3% hereinafter, sieving whole grain.
2. deccox dispersible tablet described in claim 1 is preparing the purposes in coccidiostat.
3. purposes according to claim 2, it is characterised in that: the coccidiostat is anti-Avian Coccidia drug.
4. purposes according to claim 2, it is characterised in that: the coccidiostat is anticoccidial drugs object.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611153467.5A CN106491549B (en) | 2016-12-14 | 2016-12-14 | A kind of deccox dispersible tablet and its preparation method and application |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611153467.5A CN106491549B (en) | 2016-12-14 | 2016-12-14 | A kind of deccox dispersible tablet and its preparation method and application |
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| CN106491549A CN106491549A (en) | 2017-03-15 |
| CN106491549B true CN106491549B (en) | 2019-10-22 |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5200418A (en) * | 1991-07-12 | 1993-04-06 | The Ohio State University | Cryptosporidiosis amelioration |
| WO2001087290A1 (en) * | 2000-05-17 | 2001-11-22 | Virginia Tech Intellectual Properties, Inc. | Decoquinate, 4-hydroxyquinolones and napthoquinones for the prevention and treatment of equine protozoal myeloencephalitis caused by sarcocystis neurona hughesi and other apicomplexan protozoans |
| CN101606908A (en) * | 2009-07-10 | 2009-12-23 | 华南农业大学实验兽药厂 | Decoquinate soluble powder and preparation method thereof |
| CN104721216A (en) * | 2013-12-20 | 2015-06-24 | 青岛康地恩动物药业有限公司 | Decoquinate and lincomycin hydrochloride-containing pet insect repellent tablet and preparation method thereof |
-
2016
- 2016-12-14 CN CN201611153467.5A patent/CN106491549B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5200418A (en) * | 1991-07-12 | 1993-04-06 | The Ohio State University | Cryptosporidiosis amelioration |
| WO2001087290A1 (en) * | 2000-05-17 | 2001-11-22 | Virginia Tech Intellectual Properties, Inc. | Decoquinate, 4-hydroxyquinolones and napthoquinones for the prevention and treatment of equine protozoal myeloencephalitis caused by sarcocystis neurona hughesi and other apicomplexan protozoans |
| CN101606908A (en) * | 2009-07-10 | 2009-12-23 | 华南农业大学实验兽药厂 | Decoquinate soluble powder and preparation method thereof |
| CN104721216A (en) * | 2013-12-20 | 2015-06-24 | 青岛康地恩动物药业有限公司 | Decoquinate and lincomycin hydrochloride-containing pet insect repellent tablet and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 新型抗球虫药癸氧喹酯研究进展;聂月美;《饲料工业》;20111231;第32卷(第18期);第60-62页 * |
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Effective date of registration: 20190916 Address after: 611130, No. 259, Golden Road, Chengdu science and Technology Industrial Development Zone, Wenjiang District, Sichuan, China Applicant after: Chengdu Qiankun animal pharmaceutical Limited by Share Ltd Applicant after: Chengdu Vocational College of Agricultural Science and Technology Address before: 611130 Chengdu, Wenjiang, Taiwan Strait science and Technology Industrial Park Road, the middle of the road, No. 259, No. Applicant before: Chengdu Qiankun animal pharmaceutical Limited by Share Ltd |
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