CN101843586B - Water-soluble micro powder containing florfenicol and preparation method thereof - Google Patents
Water-soluble micro powder containing florfenicol and preparation method thereof Download PDFInfo
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- CN101843586B CN101843586B CN2010101600137A CN201010160013A CN101843586B CN 101843586 B CN101843586 B CN 101843586B CN 2010101600137 A CN2010101600137 A CN 2010101600137A CN 201010160013 A CN201010160013 A CN 201010160013A CN 101843586 B CN101843586 B CN 101843586B
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- florfenicol
- water
- sds
- micropowder
- anhydrous glucose
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- AYIRNRDRBQJXIF-NXEZZACHSA-N (-)-Florfenicol Chemical compound CS(=O)(=O)C1=CC=C([C@@H](O)[C@@H](CF)NC(=O)C(Cl)Cl)C=C1 AYIRNRDRBQJXIF-NXEZZACHSA-N 0.000 title claims abstract description 94
- 229960003760 florfenicol Drugs 0.000 title claims abstract description 94
- 239000000843 powder Substances 0.000 title abstract description 15
- 238000002360 preparation method Methods 0.000 title abstract description 6
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims abstract description 31
- 229960001031 glucose Drugs 0.000 claims abstract description 31
- 150000001875 compounds Chemical class 0.000 claims abstract description 21
- 239000002994 raw material Substances 0.000 claims abstract description 14
- 238000000034 method Methods 0.000 claims description 26
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 19
- 230000008569 process Effects 0.000 claims description 17
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 10
- XUBOMFCQGDBHNK-JTQLQIEISA-N (S)-gatifloxacin Chemical compound FC1=CC(C(C(C(O)=O)=CN2C3CC3)=O)=C2C(OC)=C1N1CCN[C@@H](C)C1 XUBOMFCQGDBHNK-JTQLQIEISA-N 0.000 claims description 5
- QNVKOSLOVOTXKF-UHFFFAOYSA-N 4-[(2-amino-3,5-dibromophenyl)methylamino]cyclohexan-1-ol;hydron;chloride Chemical compound Cl.NC1=C(Br)C=C(Br)C=C1CNC1CCC(O)CC1 QNVKOSLOVOTXKF-UHFFFAOYSA-N 0.000 claims description 5
- VKJGBAJNNALVAV-UHFFFAOYSA-M Berberine chloride (TN) Chemical compound [Cl-].C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 VKJGBAJNNALVAV-UHFFFAOYSA-M 0.000 claims description 5
- 229960000985 ambroxol hydrochloride Drugs 0.000 claims description 5
- UCDKONUHZNTQPY-UHFFFAOYSA-N bromhexine hydrochloride Chemical compound Cl.C1CCCCC1N(C)CC1=CC(Br)=CC(Br)=C1N UCDKONUHZNTQPY-UHFFFAOYSA-N 0.000 claims description 5
- 229960003923 gatifloxacin Drugs 0.000 claims description 5
- 229940098779 methanesulfonic acid Drugs 0.000 claims description 5
- CQCIBVPASWGWAZ-UHFFFAOYSA-M sodium;1-cyclopropyl-7-(4-ethylpiperazin-1-yl)-6-fluoro-4-oxoquinoline-2-carboxylate Chemical compound [Na+].C1CN(CC)CCN1C(C(=C1)F)=CC2=C1C(=O)C=C(C([O-])=O)N2C1CC1 CQCIBVPASWGWAZ-UHFFFAOYSA-M 0.000 claims description 5
- 239000003814 drug Substances 0.000 abstract description 17
- 229940079593 drug Drugs 0.000 abstract description 5
- 230000001965 increasing effect Effects 0.000 abstract description 5
- 210000004051 gastric juice Anatomy 0.000 abstract description 2
- 210000001156 gastric mucosa Anatomy 0.000 abstract description 2
- 238000011031 large-scale manufacturing process Methods 0.000 abstract description 2
- 238000000576 coating method Methods 0.000 abstract 1
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 1
- 238000007873 sieving Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 description 25
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 20
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 20
- -1 complexation Substances 0.000 description 7
- 208000024891 symptom Diseases 0.000 description 7
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- 230000000844 anti-bacterial effect Effects 0.000 description 5
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- 229960003722 doxycycline Drugs 0.000 description 4
- XQTWDDCIUJNLTR-CVHRZJFOSA-N doxycycline monohydrate Chemical compound O.O=C1C2=C(O)C=CC=C2[C@H](C)[C@@H]2C1=C(O)[C@]1(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@@H]1[C@H]2O XQTWDDCIUJNLTR-CVHRZJFOSA-N 0.000 description 4
- IZJAOWYNDLDRKM-UHFFFAOYSA-N sodium;(4-aminophenyl)sulfonyl-(6-methoxypyrimidin-4-yl)azanide Chemical compound [Na+].C1=NC(OC)=CC([N-]S(=O)(=O)C=2C=CC(N)=CC=2)=N1 IZJAOWYNDLDRKM-UHFFFAOYSA-N 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 208000035143 Bacterial infection Diseases 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- 241000271566 Aves Species 0.000 description 2
- 241000287828 Gallus gallus Species 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 206010057190 Respiratory tract infections Diseases 0.000 description 2
- 208000022362 bacterial infectious disease Diseases 0.000 description 2
- 230000003115 biocidal effect Effects 0.000 description 2
- WIIZWVCIJKGZOK-RKDXNWHRSA-N chloramphenicol Chemical compound ClC(Cl)C(=O)N[C@H](CO)[C@H](O)C1=CC=C([N+]([O-])=O)C=C1 WIIZWVCIJKGZOK-RKDXNWHRSA-N 0.000 description 2
- 229940097572 chloromycetin Drugs 0.000 description 2
- 239000012141 concentrate Substances 0.000 description 2
- 210000002249 digestive system Anatomy 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 230000003340 mental effect Effects 0.000 description 2
- 229960001180 norfloxacin Drugs 0.000 description 2
- OGJPXUAPXNRGGI-UHFFFAOYSA-N norfloxacin Chemical compound C1=C2N(CC)C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCNCC1 OGJPXUAPXNRGGI-UHFFFAOYSA-N 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- TYCOFFBAZNSQOJ-UHFFFAOYSA-N 2-[4-(3-fluorophenyl)phenyl]propanoic acid Chemical compound C1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC(F)=C1 TYCOFFBAZNSQOJ-UHFFFAOYSA-N 0.000 description 1
- GSDSWSVVBLHKDQ-UHFFFAOYSA-N 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid Chemical compound FC1=CC(C(C(C(O)=O)=C2)=O)=C3N2C(C)COC3=C1N1CCN(C)CC1 GSDSWSVVBLHKDQ-UHFFFAOYSA-N 0.000 description 1
- 208000032467 Aplastic anaemia Diseases 0.000 description 1
- 241000972773 Aulopiformes Species 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- 235000016936 Dendrocalamus strictus Nutrition 0.000 description 1
- 241000192125 Firmicutes Species 0.000 description 1
- 206010017553 Furuncle Diseases 0.000 description 1
- 206010022678 Intestinal infections Diseases 0.000 description 1
- GSDSWSVVBLHKDQ-JTQLQIEISA-N Levofloxacin Chemical compound C([C@@H](N1C2=C(C(C(C(O)=O)=C1)=O)C=C1F)C)OC2=C1N1CCN(C)CC1 GSDSWSVVBLHKDQ-JTQLQIEISA-N 0.000 description 1
- 241000204031 Mycoplasma Species 0.000 description 1
- 206010033971 Paratyphoid fever Diseases 0.000 description 1
- 239000004141 Sodium laurylsulphate Substances 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 206010057179 Toxoplasma infections Diseases 0.000 description 1
- 208000037386 Typhoid Diseases 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000012670 alkaline solution Substances 0.000 description 1
- 239000003674 animal food additive Substances 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 239000003945 anionic surfactant Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 230000001914 calming effect Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- VDUWPHTZYNWKRN-UHFFFAOYSA-N cinoxacin Chemical compound C1=C2N(CC)N=C(C(O)=O)C(=O)C2=CC2=C1OCO2 VDUWPHTZYNWKRN-UHFFFAOYSA-N 0.000 description 1
- 229960004621 cinoxacin Drugs 0.000 description 1
- 238000010668 complexation reaction Methods 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 230000001804 emulsifying effect Effects 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 229960002549 enoxacin Drugs 0.000 description 1
- IDYZIJYBMGIQMJ-UHFFFAOYSA-N enoxacin Chemical compound N1=C2N(CC)C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCNCC1 IDYZIJYBMGIQMJ-UHFFFAOYSA-N 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 235000021050 feed intake Nutrition 0.000 description 1
- 229950001284 fluprofen Drugs 0.000 description 1
- 238000005187 foaming Methods 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 208000003512 furunculosis Diseases 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 239000008233 hard water Substances 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 229960003376 levofloxacin Drugs 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000693 micelle Substances 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 229960001699 ofloxacin Drugs 0.000 description 1
- 229960004236 pefloxacin Drugs 0.000 description 1
- FHFYDNQZQSQIAI-UHFFFAOYSA-N pefloxacin Chemical compound C1=C2N(CC)C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCN(C)CC1 FHFYDNQZQSQIAI-UHFFFAOYSA-N 0.000 description 1
- 239000003208 petroleum Substances 0.000 description 1
- 229920006316 polyvinylpyrrolidine Polymers 0.000 description 1
- 244000144977 poultry Species 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 235000019515 salmon Nutrition 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 235000013599 spices Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 230000009967 tasteless effect Effects 0.000 description 1
- 230000008719 thickening Effects 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 201000008297 typhoid fever Diseases 0.000 description 1
- 239000000273 veterinary drug Substances 0.000 description 1
- 239000002699 waste material Substances 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a water-soluble micro powder containing florfenicol and a preparation method thereof. The micro powder is prepared from the following raw materials, by weight, 5-10% of florfenicol, 302.5-2.75% of PVPK, 2.5-2.75% of SDS, and the balance of anhydrous glucose. Uniformly mixing PVPK30, SDS and florfenicol, crushing, sieving by a 150-mesh sieve, then adding anhydrous glucose, and uniformly mixing. The micro powder can also be compounded with other medicines to prepare water-soluble compound florfenicol micro powder. The florfenicol after being micronized has finer and more uniform granularity, so the surface area is increased, the porosity is increased, the adsorbability and the solubility are enhanced, the medicament can be better dispersed and dissolved in gastric juice, the contact area with gastric mucosa is increased, the medicament is easier to be absorbed by gastrointestinal tracts, and the bioavailability is greatly improved. Compared with the coating process, the preparation method of the invention is more convenient and is more suitable for large-scale production.
Description
Technical field
The present invention relates to a kind of water-soluble micropowder that contains florfenicol and preparation method thereof, belong to the veterinary drug technical field.
Background technology
Florfenicol (Florfenicol) Chinese: fluprofen, florfenicol, Florfenicol; It is the broad spectrum antibiotic of the special-purpose chloromycetin of a kind of new veterinary successfully developed in the late nineteen eighties; Nineteen ninety goes on the market in Japan first; The furunculosis of this medicine treatment salmon of Norway in 1993 approval, nineteen ninety-five France, Britain, Austria, Mexico and Spain ratify to be used to treat cattle respiratory system bacterial disease.Also ratify feed additive in Japan and Mexico as pig, the bacterial disease (Qiu Yinsheng etc., 1996) of prevention and treatment pig, China has passed through examining of this medicine at present.Florfenicol all has the excellent antibiotic effect to poultry gram positive bacteria and gram negative bacteria, is the choice drug of bacterial diseases such as treatment avian typhoid, paratyphoid fever.The prodrug chloromycetin of florfenicol bans use of in food animal owing to can cause very serious aplastic anemia at present.As for animals special-purpose antibacterials few in number, florfenicol has a wide range of applications, but because its poorly water-soluble, this uses inconvenience medicine in the large-scale cultivation field, its use is had very big restriction.
The hydrotropy method that adopts at present owing to adopt very complicated production technology, causes use cost to increase; Be not suitable for the large-scale cultivation field; And present hydrotropy method causes this rate of release in intestinal of florfenicol slack-off, because the birds digestive system is short, medicine is shorter through the used time ratio of whole system; The absorption and the effect of medicine are reduced, cause the waste of medicine.
Summary of the invention
The present invention's first purpose provides a kind of water-soluble micropowder that contains florfenicol, improves absorption and the blood drug level of florfenicol at digestive system, strengthens the therapeutic effect of florfenicol.Its granularity of florfenicol behind micropowder is trickleer, even; Therefore surface area increases, and porosity increases, adsorptivity and solubility enhanced; Medicine can disperse preferably, be dissolved in the gastric juice; The contact area of increase and gastric mucosa, thus more be prone to improved bioavailability greatly by gastrointestinal absorption.Another object of the present invention provides a kind of water-soluble micropowder preparing process that contains florfenicol, and it is convenient that the method ratio encapsulates technology, is more suitable in large-scale production.
Technical scheme of the present invention is: a kind of water-soluble micropowder that contains florfenicol, it is characterized in that, and process by following raw material by weight percentage, florfenicol 5-10%, PVPK30 2.5-2.75%, SDS2.5-2.75%, all the other are anhydrous glucose.
The further technical scheme of the present invention is: a kind of water-soluble micropowder that contains florfenicol, it is characterized in that, and process by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, anhydrous glucose 90%.
The PVPK30 chemical name is polyvinylpyrrolidone K30, and white is to off-white powder; Odorless or have special smellyly, tasteless slightly has hygroscopicity.These article dissolve in water, ethanol, isopropyl alcohol or chloroform, and are insoluble in acetone or ether, and the solution viscosity below 10% is identical with water base.These article have characteristic and effects such as bonding, thickening, suspending, dispersion, complexation, film forming, in medicament, are used as thickening agent, suspending agent, dispersant, chelating agent etc.
The SDS chemical name is a sodium lauryl sulphate, is white or yellowish crystallization thin slice or powder, have slight special smelly, similar fat, bitter in the mouth, soluble in water.Be partially soluble in ethanol, be insoluble to chloroform, ether and petroleum ether.Critical micelle concentration (20 ℃) is 8.2 * 10
-3Mol/L.Relative density is 1.07, and HLB is 40, and interfacial tension is 11.8mN/m.These article are anion surfactant, have effects such as emulsifying, de-sludging, dispersion, moistening, foaming, and are all effective in acid, alkaline solution and hard water.
PVPK30, SDS all play solubilising and hydrotropy effect in the present invention.
The above-mentioned water-soluble micropowder method for preparing that contains florfenicol is: with PVPK30, SDS, florfenicol mix homogeneously, pulverize, cross 150 mesh sieves, and then add anhydrous glucose, mix homogeneously.
The present invention also provides a kind of water solublity compound florfenicol micropowder, it is characterized in that, is mainly processed by florfenicol, PVPK30, SDS and anhydrous glucose.
The further technical scheme of the present invention is: a kind of water solublity compound florfenicol micropowder, it is characterized in that, and process by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, QNS 5%, anhydrous glucose 85%.With florfenicol, PVPK30, SDS and QNS mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mix homogeneously.Said QNS can be norfloxacin, ofloxacin, levofloxacin, pefloxacin, enoxacin, cinoxacin etc.This compound recipe adds QNS on the basis of the highly dissoluble of the water-soluble micropowder that keeps containing florfenicol and rate of release, play the effect of Synergistic, makes the antibacterial activity enhancing of two kinds of medicines.
Technical scheme of the present invention is: a kind of water solublity compound florfenicol micropowder, it is characterized in that, and process by following raw material by weight percentage; Florfenicol 5%, PVPK30 2.5%, and SDS 2.5%; Bisolvon 5%, enrofloxacin sodium 7%, anhydrous glucose 78%.With florfenicol, PVPK30, SDS, Bisolvon, enrofloxacin sodium mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mix homogeneously.This compound recipe is on the basis of the highly dissoluble of the water-soluble micropowder that keeps containing florfenicol and rate of release; Add Bisolvon and enrofloxacin sodium; Make it not only have antibacterial functions, and have function of relieving cough and calming asthma, quicken the rehabilitation of respiratory tract infection.
Technical scheme of the present invention is: a kind of water solublity compound florfenicol micropowder, it is characterized in that, and process by following raw material by weight percentage; Florfenicol 5%, PVPK30 2.5%, and SDS 2.5%; Sulfamonomethoxine sodium 10%, doxycycline pulverizes 5%, anhydrous glucose 75%.With florfenicol, PVPK30, SDS, sulfamonomethoxine sodium, doxycycline mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mix homogeneously.This compound recipe adds sulfamonomethoxine sodium and doxycycline on the basis of the highly dissoluble of the water-soluble micropowder that keeps containing florfenicol and rate of release, make it not only have antibacterial functions, and can treat Eperythrozoon and the toxoplasma infection of pig.
Technical scheme of the present invention is: a kind of water solublity compound florfenicol micropowder, it is characterized in that, and process by following raw material by weight percentage; Florfenicol 5%, PVPK30 2.5%, and SDS 2.5%; Methanesulfonic acid Gatifloxacin 5%, ambroxol hydrochloride 5%, anhydrous glucose 80%.With florfenicol, PVPK30, SDS, methanesulfonic acid Gatifloxacin, ambroxol hydrochloride mix homogeneously, pulverize, cross 150 mesh sieves, add the anhydrous glucose mix homogeneously.This compound recipe adds methanesulfonic acid Gatifloxacin and ambroxol hydrochloride on the basis of the highly dissoluble of the water-soluble micropowder that keeps containing florfenicol and rate of release, strengthened the antibacterial action and the effect of treating respiratory tract infection of florfenicol.
The further technical scheme of the present invention is: a kind of water solublity compound florfenicol micropowder, it is characterized in that, and process by following raw material by weight percentage, florfenicol 5%, PVPK30 2.5%, and SDS 2.5%, berberine hydrochloride 10%, anhydrous glucose 80%.With florfenicol, PVPK30, SDS and berberine hydrochloride mix homogeneously, pulverize, cross 150 mesh sieves, add anhydrous glucose and be mixed and made into.This compound recipe is on the basis of the highly dissoluble of the water-soluble micropowder that keeps containing florfenicol and rate of release, and the adding berberine hydrochloride has strengthened the therapeutic effect of florfenicol to intestinal infection.
Beneficial effect of the present invention: present technique adopts PVPK30, SDS as surfactant; Superfine grinding method makes the water-soluble micropowder that contains florfenicol; Make the florfenicol granularity be reduced to 90um by original 250um; Dissolubility is increased to 5% by original 0.01%, and rate of release is 99.12% to be florfenicol powder (rate of release 30.25%) and former powder (rate of release 2.3%) 3.27 times and 43.1 times.This method for preparing is that a kind of method is simple, cost is low and can improves the hydrotropy method of the rate of release of medicine own.
The specific embodiment
Below in conjunction with specific embodiment the present invention is further specified.
Embodiment 1:
As produce water-soluble micropowder that 100kg contains florfenicol, and the 5kg florfenicol, 2.5kgPVPK30,2.5kg SDS, mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 90kg mixes, and equivalent increases progressively mix homogeneously and processes.This water-soluble micropowder that contains florfenicol is following to the influence of broiler:
1, experimental animal:
Picked at random is suffered from 90 of colibacillosis broiler, is divided into 3 groups at random, and 30 every group, body weight is at 1～2kg.
2, experiment medicine:
The water-soluble micropowder that contains florfenicol of the embodiment of the invention 1 preparation;
5% florfenicol powder: the quality percentage composition is 5% florfenicol, and the quality percentage composition is that 95% starch mix homogeneously promptly gets.
3, experimental technique:
1 group is blank group, not medicament.
2 group of 5% florfenicol powder treated usage: 100g florfenicol powder (5%) spice 50kg, once-a-day, concentrate to use up logotype 4 days in 3 hours.
3 groups contain water-soluble micropowder of florfenicol with the present invention, and usage: 100g converts water 100kg, once-a-day, concentrates to use up logotype 4 days in 3 hours.
After the treatment beginning, write down disease fowl mental condition every day and distribute, treat and add up therapeutic effect after 4 days, wherein with dead.
Invalid: after referring to 4 days, sick fowl symptom has the situation of increasing the weight of or dead.
Effectively: after referring to 4 days, sick fowl symptom changes, and symptom is controlled or with respect to having obviously and alleviate before the treatment.
Cure: after referring to 4 days, transference cure, the sick fowl mental status and feed intake are recovered normal condition.Its digital packets is contained in the significant digits.
Symptom is arranged during end: after referring to treat 4 days, sick fowl still has certain symptom, and the performance of its symptom is superior to before the treatment or does not have change, and sick fowl is cured fully, and its numeral has been included in the numeral of invalid number of elements and effective number of elements.
Result of the test is as shown in table 1:
Table 1: each organizes therapeutic effect
| Numbering | Group | Invalid number of elements | Effective number of elements | Cure number of elements | The symptom number of elements is arranged during end |
| 1 group | Matched group | 30 | 0 | 0 | 30 |
| 2 groups | 5% florfenicol powder | 8 | 22 | 12 | 18 |
| 3 groups | The water-soluble micropowder that contains florfenicol | 2 | 28 | 27 | 3 |
4, conclusion:
Through statistical analysis, water-soluble micropowder, 5% florfenicol treated powder group and the matched group difference that contains florfenicol is (P＜0.01) extremely significantly from the result of the test of table 1.Treatment of the present invention is better than existing powder.
Embodiment 2:
As produce 100kg water solublity compound florfenicol micropowder, and the 5kg florfenicol, 2.5kg PVPK30,2.5kgSDS, 5kg QNS (norfloxacin), mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 85kg is mixed and made into.
Embodiment 3:
As produce water-soluble micropowder that 100kg contains florfenicol, and the 10kg florfenicol, 2.6kgPVPK30,2.6kg SDS, mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 84.8kg mixes, and equivalent increases progressively mix homogeneously and processes.
Embodiment 4:
As produce water-soluble micropowder that 100kg contains florfenicol, and the 8kg florfenicol, 2.75kgPVPK30,2.75kg SDS, mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 86.5kg mixes, and equivalent increases progressively mix homogeneously and processes.
Embodiment 5:
As produce 100kg water solublity compound florfenicol micropowder, and the 5kg florfenicol, 2.5kg PVPK30,2.5kgSDS, the 5kg Bisolvon, 7kg enrofloxacin sodium mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 78kg is mixed and made into.
Embodiment 6:
As produce 100kg water solublity compound florfenicol micropowder, and the 5kg florfenicol, 2.5kg PVPK30,2.5kgSDS, the 10kg sulfamonomethoxine sodium, 5kg doxycycline mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 75kg is mixed and made into.
Embodiment 7:
As produce 100kg water solublity compound florfenicol micropowder, and the 5kg florfenicol, 2.5kg PVPK30,2.5kgSDS, 5kg methanesulfonic acid Gatifloxacin, 5kg ambroxol hydrochloride mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 80kg is mixed and made into.
Embodiment 8:
As produce 100kg water solublity compound florfenicol micropowder, and the 5kg florfenicol, 2.5kg PVPK30,2.5kgSDS, 10kg berberine hydrochloride mix homogeneously is pulverized, and crosses 150 mesh sieves, and the anhydrous glucose that adds 80kg is mixed and made into.
Claims (6)
1. a water-soluble micropowder that contains florfenicol is characterized in that, process by following raw material by weight percentage, and florfenicol 5-10%, PVPK302.5-2.75%, SDS 2.5-2.75%, all the other are anhydrous glucose; With PVPK30, SDS, florfenicol mix homogeneously, pulverize, cross 150 mesh sieves, and then add anhydrous glucose, mix homogeneously.
2. a kind of water-soluble micropowder that contains florfenicol as claimed in claim 1 is characterized in that, processes by following raw material by weight percentage, and florfenicol 5%, PVPK302.5%, SDS 2.5%, anhydrous glucose 90%.
3. a water solublity compound florfenicol micropowder is characterized in that, process by following raw material by weight percentage, and florfenicol 5%, PVPK302.5%, SDS 2.5%, QNS 5%, anhydrous glucose 85%.
4. a water solublity compound florfenicol micropowder is characterized in that, process by following raw material by weight percentage, and florfenicol 5%, PVPK302.5%, SDS 2.5%, Bisolvon 5%, enrofloxacin sodium 7%, anhydrous glucose 78%.
5. a water solublity compound florfenicol micropowder is characterized in that, process by following raw material by weight percentage, and florfenicol 5%, PVPK302.5%, SDS 2.5%, methanesulfonic acid Gatifloxacin 5%, ambroxol hydrochloride 5%, anhydrous glucose 80%.
6. a water solublity compound florfenicol micropowder is characterized in that, process by following raw material by weight percentage, and florfenicol 5%, PVPK302.5%, SDS 2.5%, berberine hydrochloride 10%, anhydrous glucose 80%.
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| CN102429918A (en) * | 2011-11-02 | 2012-05-02 | 南京威泰珐玛兽药研究所有限公司 | Pharmaceutical composition containing florfenicol and tea saponin and preparation method thereof |
| CN102697730A (en) * | 2012-05-07 | 2012-10-03 | 郑州后羿制药有限公司 | Florfenicol soluble power and preparation method thereof |
| CN102885777B (en) * | 2012-10-25 | 2014-07-16 | 上海邦森生物科技有限公司 | Efficient florfenicol powder composition and preparation method thereof |
| CN103127019B (en) * | 2013-03-22 | 2015-04-22 | 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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| CN109172528A (en) * | 2018-10-30 | 2019-01-11 | 河南后羿实业集团有限公司 | A kind of florfenicol soluble powder and preparation method thereof |
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Denomination of invention: A water-soluble micro powder containing florfenicol and its preparation method Granted publication date: 20120523 Pledgee: Weihai commercial bank Limited by Share Ltd. Ji'nan branch Pledgor: SHANDONG SOOCOM ANIMAL REMEDY CO.,LTD. Registration number: Y2024980033096 |