CN104095871A - Veterinary injection containing lincomycin hydrochloride and spectinomycin sulfate - Google Patents
Veterinary injection containing lincomycin hydrochloride and spectinomycin sulfate Download PDFInfo
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- CN104095871A CN104095871A CN201410329394.5A CN201410329394A CN104095871A CN 104095871 A CN104095871 A CN 104095871A CN 201410329394 A CN201410329394 A CN 201410329394A CN 104095871 A CN104095871 A CN 104095871A
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- injection
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- 238000002347 injection Methods 0.000 title claims abstract description 47
- 239000007924 injection Substances 0.000 title claims abstract description 47
- XGBFWQUQYQIFLB-MTTMTQIXSA-N 23312-56-3 Chemical compound OS(O)(=O)=O.O([C@@H]1[C@@H](NC)[C@@H](O)[C@H]([C@@H]([C@H]1O1)O)NC)[C@]2(O)[C@H]1O[C@H](C)CC2=O XGBFWQUQYQIFLB-MTTMTQIXSA-N 0.000 title claims abstract description 24
- 229960001595 lincomycin hydrochloride Drugs 0.000 title claims abstract description 23
- POUMFISTNHIPTI-BOMBIWCESA-N hydron;(2s,4r)-n-[(1r,2r)-2-hydroxy-1-[(2r,3r,4s,5r,6r)-3,4,5-trihydroxy-6-methylsulfanyloxan-2-yl]propyl]-1-methyl-4-propylpyrrolidine-2-carboxamide;chloride Chemical compound Cl.CN1C[C@H](CCC)C[C@H]1C(=O)N[C@H]([C@@H](C)O)[C@@H]1[C@H](O)[C@H](O)[C@@H](O)[C@@H](SC)O1 POUMFISTNHIPTI-BOMBIWCESA-N 0.000 title claims abstract description 20
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 30
- 238000002360 preparation method Methods 0.000 claims abstract description 14
- 239000003814 drug Substances 0.000 claims abstract description 12
- 229940079593 drug Drugs 0.000 claims abstract description 9
- 239000002904 solvent Substances 0.000 claims abstract description 9
- 239000003381 stabilizer Substances 0.000 claims abstract description 8
- 239000003963 antioxidant agent Substances 0.000 claims abstract description 7
- 230000003078 antioxidant effect Effects 0.000 claims abstract description 7
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 27
- 241001465754 Metazoa Species 0.000 claims description 18
- 238000003756 stirring Methods 0.000 claims description 18
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 claims description 14
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 12
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 12
- 239000000725 suspension Substances 0.000 claims description 12
- OJMMVQQUTAEWLP-UHFFFAOYSA-N Lincomycin Natural products CN1CC(CCC)CC1C(=O)NC(C(C)O)C1C(O)C(O)C(O)C(SC)O1 OJMMVQQUTAEWLP-UHFFFAOYSA-N 0.000 claims description 9
- 150000001875 compounds Chemical class 0.000 claims description 9
- 229960005287 lincomycin Drugs 0.000 claims description 9
- OJMMVQQUTAEWLP-KIDUDLJLSA-N lincomycin Chemical compound CN1C[C@H](CCC)C[C@H]1C(=O)N[C@H]([C@@H](C)O)[C@@H]1[C@H](O)[C@H](O)[C@@H](O)[C@@H](SC)O1 OJMMVQQUTAEWLP-KIDUDLJLSA-N 0.000 claims description 9
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 7
- 229960000502 poloxamer Drugs 0.000 claims description 7
- 229920001983 poloxamer Polymers 0.000 claims description 7
- -1 polyoxyethylene Polymers 0.000 claims description 7
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims description 7
- 235000010234 sodium benzoate Nutrition 0.000 claims description 7
- 239000004299 sodium benzoate Substances 0.000 claims description 7
- 235000010265 sodium sulphite Nutrition 0.000 claims description 7
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 6
- CEAZRRDELHUEMR-URQXQFDESA-N Gentamicin Chemical compound O1[C@H](C(C)NC)CC[C@@H](N)[C@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](NC)[C@@](C)(O)CO2)O)[C@H](N)C[C@@H]1N CEAZRRDELHUEMR-URQXQFDESA-N 0.000 claims description 6
- 229930182566 Gentamicin Natural products 0.000 claims description 6
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 6
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 6
- 230000002421 anti-septic effect Effects 0.000 claims description 6
- 235000006708 antioxidants Nutrition 0.000 claims description 6
- 230000015572 biosynthetic process Effects 0.000 claims description 6
- 238000004090 dissolution Methods 0.000 claims description 6
- 150000005846 sugar alcohols Polymers 0.000 claims description 6
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 4
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 4
- 235000015165 citric acid Nutrition 0.000 claims description 4
- 239000001509 sodium citrate Substances 0.000 claims description 4
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims description 4
- 235000010352 sodium erythorbate Nutrition 0.000 claims description 4
- JXKPEJDQGNYQSM-UHFFFAOYSA-M sodium propionate Chemical compound [Na+].CCC([O-])=O JXKPEJDQGNYQSM-UHFFFAOYSA-M 0.000 claims description 3
- 235000010334 sodium propionate Nutrition 0.000 claims description 3
- 239000004324 sodium propionate Substances 0.000 claims description 3
- 229960003212 sodium propionate Drugs 0.000 claims description 3
- FJKROLUGYXJWQN-UHFFFAOYSA-M 4-hydroxybenzoate Chemical compound OC1=CC=C(C([O-])=O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-M 0.000 claims description 2
- 239000005711 Benzoic acid Substances 0.000 claims description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 2
- CIWBSHSKHKDKBQ-DUZGATOHSA-N D-isoascorbic acid Chemical compound OC[C@@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-DUZGATOHSA-N 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
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- QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 claims description 2
- 239000011786 L-ascorbyl-6-palmitate Substances 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 2
- 235000001630 Pyrus pyrifolia var culta Nutrition 0.000 claims description 2
- 240000002609 Pyrus pyrifolia var. culta Species 0.000 claims description 2
- 229930003427 Vitamin E Natural products 0.000 claims description 2
- 235000010323 ascorbic acid Nutrition 0.000 claims description 2
- 229960005070 ascorbic acid Drugs 0.000 claims description 2
- 239000011668 ascorbic acid Substances 0.000 claims description 2
- 235000010385 ascorbyl palmitate Nutrition 0.000 claims description 2
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 2
- 235000010233 benzoic acid Nutrition 0.000 claims description 2
- 229960004365 benzoic acid Drugs 0.000 claims description 2
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 2
- 235000021466 carotenoid Nutrition 0.000 claims description 2
- 150000001747 carotenoids Chemical class 0.000 claims description 2
- 239000004359 castor oil Substances 0.000 claims description 2
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- 150000002148 esters Chemical class 0.000 claims description 2
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 claims description 2
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims description 2
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 2
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 2
- 239000010452 phosphate Substances 0.000 claims description 2
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims description 2
- 229960003885 sodium benzoate Drugs 0.000 claims description 2
- 239000004320 sodium erythorbate Substances 0.000 claims description 2
- RBWSWDPRDBEWCR-RKJRWTFHSA-N sodium;(2r)-2-[(2r)-3,4-dihydroxy-5-oxo-2h-furan-2-yl]-2-hydroxyethanolate Chemical compound [Na+].[O-]C[C@@H](O)[C@H]1OC(=O)C(O)=C1O RBWSWDPRDBEWCR-RKJRWTFHSA-N 0.000 claims description 2
- 235000010199 sorbic acid Nutrition 0.000 claims description 2
- 239000004334 sorbic acid Substances 0.000 claims description 2
- 229940075582 sorbic acid Drugs 0.000 claims description 2
- 229940095064 tartrate Drugs 0.000 claims description 2
- 235000019165 vitamin E Nutrition 0.000 claims description 2
- 229940046009 vitamin E Drugs 0.000 claims description 2
- 239000011709 vitamin E Substances 0.000 claims description 2
- 241000283690 Bos taurus Species 0.000 abstract description 4
- 241000282326 Felis catus Species 0.000 abstract description 4
- 230000003115 biocidal effect Effects 0.000 abstract description 4
- 244000144977 poultry Species 0.000 abstract description 4
- 241000282472 Canis lupus familiaris Species 0.000 abstract 1
- 241000282887 Suidae Species 0.000 abstract 1
- 229920005862 polyol Polymers 0.000 abstract 1
- 150000003077 polyols Chemical class 0.000 abstract 1
- 239000003755 preservative agent Substances 0.000 abstract 1
- 230000002335 preservative effect Effects 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 10
- 241000894006 Bacteria Species 0.000 description 5
- 241001662103 Cryptocarya corrugata Species 0.000 description 5
- VVTDHOIRNPCGTH-UHFFFAOYSA-N Mycosporin 1 Natural products COC1=C(NC(CO)CO)CC(O)(CO)CC1=O VVTDHOIRNPCGTH-UHFFFAOYSA-N 0.000 description 5
- VNFPBHJOKIVQEB-UHFFFAOYSA-N clotrimazole Chemical compound ClC1=CC=CC=C1C(N1C=NC=C1)(C=1C=CC=CC=1)C1=CC=CC=C1 VNFPBHJOKIVQEB-UHFFFAOYSA-N 0.000 description 5
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- UNFWWIHTNXNPBV-WXKVUWSESA-N spectinomycin Chemical compound O([C@@H]1[C@@H](NC)[C@@H](O)[C@H]([C@@H]([C@H]1O1)O)NC)[C@]2(O)[C@H]1O[C@H](C)CC2=O UNFWWIHTNXNPBV-WXKVUWSESA-N 0.000 description 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 2
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- 230000001225 therapeutic effect Effects 0.000 description 2
- OQUFOZNPBIIJTN-UHFFFAOYSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;sodium Chemical compound [Na].OC(=O)CC(O)(C(O)=O)CC(O)=O OQUFOZNPBIIJTN-UHFFFAOYSA-N 0.000 description 1
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention belongs to the field of veterinary antibiotic drugs, particularly relates to veterinary injection containing lincomycin hydrochloride and spectinomycin sulfate, a preparation method of the veterinary injection and an application of the veterinary injection in poultry, pigs, dogs, cats and cattle. The veterinary injection comprises components at the mass-volume ratio as follows: (a),3%-10% of lincomycin hydrochloride bulk drugs; (b), 8%-20% of spectinomycin sulfate; (c), 8%-20% of polyol; (d), 0.1%-0.5% of a solubilizer; (e), 0.05%-0.50% of preservative; (f), 0.1%-1% of an antioxidant; (g), 0.2%-0.6% of a stabilizer; and (h), the balance of water.
Description
Technical field
The invention belongs to the compound recipe preparation method of antibiotic medicine for animals and the technical field of application, be specifically related to Injection for animals of a kind of hydrochloric lincomycin and Spectinomycin Sulfate and preparation method thereof, and the application on poultry, pig, dog, cat, cattle.
Technical background
Lincomycin hydrochloride is narrow-spectrum antibiotic, acts on similarly to erythromycin, and gram positive coccus is had to better effect, especially anaerobic bacteria, golden Portugal bacterium and streptococcus pneumoniae is had efficiently.It can enter in osseous tissue, and bone has special affinity, therefore the microbial infection Ji Jin Portugal bacterium property osteomyelitis that is specially adapted to be sick of.
Spectinomycin Sulfate all has stronger inhibition ability to gram positive bacteria and negative bacterium, all effective to staphylococcus aureus, Hemolytic streptococcus, Diplococcus pneumoniae, proteus vulgaris, pneumobacillus etc. and mycoplasma micro-slurry bacterium and some lonely bacterium.On veterinary clinic, hydrochloric acid woods Mycosporin and Spectinomycin Sulfate all can be applicable to poultry,, the antibacterials of pig, dog, cat, cattle etc. infects, and has good therapeutic effect.
Actinobacillus, Pasteurella, the secondary haemophilus of pig, escherichia coli, Salmonella, jejunum campylobacter Pseudomonas, Fusobacterium, clostridium etc. are the encountered pathogenic bacterias that causes the diseases such as poultry, cattle, pig, dog, cat, often there is the mixed infection that one or more are equal in veterinary clinic at present, to aquaculture, caused huge economic loss, hydrochloric acid woods Mycosporin and Spectinomycin Sulfate can be applied to the infection of above-mentioned antibacterial.
The development of compound preparation, has great importance for control antibacterial comprehensive infection, can reduce antibioticly, reduces the generation of bacterial drug resistance, ensures human food's safety.At present, hydrochloric acid woods Mycosporin and Spectinomycin Sulfate compound preparation are mainly pre-mixing agent, soluble powder etc., and the dosage of these two kinds of dosage forms is generally large compared with injection, and in daily use, easily cause escalated dose to use, and cause antibiotic abuse.Injection is on veterinary clinic, to use comparatively common dosage form, has advantages of that absorption is rapid, bioavailability is high, dosage is little.Therefore, hydrochloric acid woods Mycosporin and Spectinomycin Sulfate are prepared into injection, can improve the scope of application on veterinary clinic effectively in conjunction with the antibacterial action of two kinds of medicines, play the object of whole body therapeutic.
Chinese patent CN101991594A discloses the injection preparation of a kind of hydrochloric lincomycin and Spectinomycin Sulfate, it consists of hydrochloric acid woods Mycosporin 3%-7%, Spectinomycin Sulfate is 8%-12%, and stabilizing agent sorbitol is 3%-7%, and all the other are water for injection.Chinese patent CN101829082A discloses the preparation method of a kind of hydrochloric lincomycin, spectinomycin hydrochloride injection, and the method is carried out enclose by spectinomycin hydrochloride with cyclodextrin, prepares clathrate, then is prepared into compound injection with lincomycin hydrochloride.
But because the solvent for injection using in above-mentioned document is water, and lincomycin hydrochloride and Spectinomycin Sulfate are unstable in water, have certain zest during injection, do not there is slow releasing function simultaneously, cause injection volume large and frequent.
The invention provides a kind of new lincomycin hydrochloride and Spectinomycin Sulfate compound injection, a kind of mixed solvent that utilizes is provided especially, the method by lincomycin hydrochloride and Spectinomycin Sulfate dissolving, is prepared into a kind of slow release Injection for animals.The Injection for animals good stability of the lincomycin hydrochloride of preparing by this method and Spectinomycin Sulfate, nonirritant, and have slow releasing function, the safety that tool is good, provides a kind of new preparation for China's veterinary clinic utilizes lincomycin hydrochloride and Spectinomycin Sulfate better.
Summary of the invention
The Injection for animals that the object of the invention is to develop a kind of lincomycin hydrochloride and Spectinomycin Sulfate, heightens the effect of a treatment, and improves stability and the safety of medicine, tool long-acting.
The present invention, for achieving the above object, provides the Injection for animals of a kind of hydrochloric lincomycin and Spectinomycin Sulfate, it is characterized in that, specifically consists of:
(a) lincomycin hydrochloride crude drug 3-10% (W/V);
(b) Spectinomycin Sulfate 8-20% (W/V);
(c) polyhydric alcohol 8-20% (W/V);
(d) solubilizing agent 0.1-0.5% (W/V);
(e) antiseptic 0.05-0.50% (W/V);
(f) antioxidant 0.1-1% (W/V);
(g) stabilizing agent 0.2-0.6% (W/V)
(h) surplus is water
Wherein said polyhydric alcohol, is selected from: ethylene glycol, propylene glycol, glycerol, preferably propylene glycol.
Wherein said solubilizing agent, is selected from: poly yamanashi esters, spans, glycerol, propylene glycol, polyoxyethylene castor oil, poloxamer, preferential poloxamer.
Wherein said antiseptic, is selected from: benzyl alcohol, benzalkonium chloride, p-hydroxybenzoate, n-butyl alcohol, benzoic acid, citric acid, sorbic acid, sodium benzoate, sodium propionate, preferred sodium benzoate or sodium propionate.
Wherein said antioxidant, is selected from: a certain in vitamin E, carotenoid, ascorbic acid, ascorbyl palmitate, arabo-ascorbic acid, sodium erythorbate, citric acid, sodium sulfite EDTA and phosphoric acid derivatives, preferably sodium sulfite.
Wherein said stabilizing agent, is selected from: a certain in citrate (acid salt or normal salt), tartrate (acid salt or normal salt), phosphate, optimization citric acid sodium.
The injection of lincomycin hydrochloride of the present invention and Spectinomycin Sulfate, is characterized in that preparation method is as follows:
Get lincomycin hydrochloride, gentamycin sulfate and polyhydric alcohol, solubilizing agent, antiseptic, the suitable quantity of water formation suspension that stirs, separately getting stabilizing agent adds after suitable quantity of water, add in above-mentioned suspension, with adding with stirring, by antioxidant with adding after water dissolution, finally add water to recipe quantity, stir, make compound injection.
The present invention preferably fills a prescription composed as follows:
The most preferred formula of the present invention is composed as follows:
The most preferred formula of the present invention obtains through screening, and screening process is as follows:
Table 1,6 groups of prescription comparisons to be selected
With the injection in the embodiment of the present invention 1 and Chinese patent CN101991594A Chinese patent CN101829082A, carry out 3 months 40 ℃ of incubators and place, detect the stability control experiment of active constituent content, experimental result is as follows:
Table 2, compared to the prior art, stability improves
With the injection in the embodiment of the present invention 1 and Chinese patent CN101991594A Chinese patent CN101829082A, carry out blood drug level test in body, observe slow release effect control experiment, experimental result is as follows:
Table 3, compared to the prior art, has slow release effect
With the injection in the embodiment of the present invention 1 and Chinese patent CN101991594A Chinese patent CN101829082A, carry out local irritation control experiment, experimental result is as follows:
Table 4, compared to the prior art, zest reduces
With the injection in the embodiment of the present invention 1 and Chinese patent CN101991594A Chinese patent CN101829082A, carry out 3 months 40 ℃ of incubators and place, observe clarity control experiment, experimental result is as follows:
Table 5, compared to the prior art, clarity is good
In the embodiment of the present invention 1 animal body, slow release effect detection data are as follows:
| Time h | The embodiment of the present invention 1 lincomycin blood drug level | The embodiment of the present invention 1 spectinomycin blood drug level |
| 0.03 | 2.27±0.12 | 5.11±0.38 |
| 0.08 | 3.25±0.21 | 9.34±0.41 |
| 0.17 | 4.32±0.17 | 13.87±0.42 |
| 0.25 | 4.94±0.20 | 15.77±0.45 |
| 0.33 | 4.58±0.22 | 18.69±0.65 |
| 0.50 | 3.80±0.20 | 19.51±0.72 |
| 0.75 | 3.18±0.21 | 17.70±0.57 |
| 1 | 2.54±0.21 | 15.81±0.31 |
| 1.5 | 2.02±0.10 | 12.50±0.56 |
| 2 | 1.50±0.09 | 10.07±0.24 |
| 3 | 0.99±0.07 | 6.84±0.45 |
| 4 | 0.65±0.04 | 3.34±0.25 |
| 6 | 0.47±0.02 | 1.82±0.16 |
| 8 | 0.26±0.02 | 0.73±0.05 |
| 12 | 0.13±0.01 | 0.14±0.01 |
Lincomycin and spectinomycin blood drug level detection method:
Accurately measure blood plasma 0.5ml, add 1ml acetonitrile, mediate and mix 1min, the centrifugal 5min of 15000r/min, shift supernatant in 15ml centrifuge tube, add 50ul, 0.4molL NaoH solution, after vortex mixes, add 5ml ethyl acetate, vortex mixes, after 200r level concussion 20min, the centrifugal 10min of 8000r/min, shifts lower floor to glass tubing, and 60 ℃ of nitrogen dry up.Finally use 0.5ml mobile phase standardize solution, use 0.22um filtering with microporous membrane, the accurate 50uL that draws carries out HPLC analysis.
After pig single intramuscular injection lincomycin hydrochloride-Spectinomycin Sulfate injection injection, absorb relatively slowly, in this patent, adopt mixed solvent solvent the most, contribute to medicine in the slow absorption of medicine-feeding part.
The specific embodiment
Below by embodiment, further illustrate the present invention, but example do not limit the scope of the invention, scope of the present invention and core content are determined according to claims.
Example 1: compound lincomycin hydrochloride, Spectinomycin Sulfate injection
[preparation]
Get lincomycin hydrochloride, gentamycin sulfate and propylene glycol, poloxamer, sodium benzoate, the 20ml water formation suspension that stirs, separately getting sodium citrate adds after 20ml water, add in above-mentioned suspension, with adding with stirring, by sodium sulfite with adding after 20ml water dissolution, finally add water to full dose, stir, make compound injection.
Example 2: compound lincomycin hydrochloride, Spectinomycin Sulfate injection
[preparation]
Get lincomycin hydrochloride, gentamycin sulfate and propylene glycol, poloxamer, sodium benzoate, the 20ml water formation suspension that stirs, separately getting sodium citrate adds after 20ml water, add in above-mentioned suspension, with adding with stirring, by sodium sulfite with adding after 20ml water dissolution, finally add water to full dose, stir, make compound injection.
Example 3: compound lincomycin hydrochloride, Spectinomycin Sulfate injection
[preparation]
Get lincomycin hydrochloride, gentamycin sulfate and propylene glycol, poloxamer, sodium benzoate, the 20ml water formation suspension that stirs, separately getting sodium citrate adds after 20ml water, add in above-mentioned suspension, with adding with stirring, by sodium sulfite with adding after 20ml water dissolution, finally add water to full dose, stir, make compound injection.
Claims (10)
1. an Injection for animals for hydrochloric lincomycin and Spectinomycin Sulfate, is characterized in that, it consists of:
(a) lincomycin hydrochloride crude drug 3-10% (W/V);
(b) Spectinomycin Sulfate 8-20% (W/V);
(c) polyhydric alcohol 8-20% (W/V);
(d) solubilizing agent 0.1-0.5% (W/V);
(e) antiseptic 0.05-0.50% (W/V);
(f) antioxidant 0.1-1% (W/V);
(g) stabilizing agent 0.2-0.6% (W/V)
(h) surplus is water.
2. by Injection for animals claimed in claim 1, it is characterized in that, described polyhydric alcohol, is selected from: ethylene glycol, propylene glycol, glycerol.
3. by Injection for animals claimed in claim 1, it is characterized in that, described solubilizing agent, is selected from: poly yamanashi esters, spans, glycerol, propylene glycol, polyoxyethylene castor oil, poloxamer.
4. by Injection for animals claimed in claim 1, it is characterized in that, described antiseptic, is selected from: benzyl alcohol, benzalkonium chloride, p-hydroxybenzoate, n-butyl alcohol, benzoic acid, citric acid, sorbic acid, sodium benzoate, sodium propionate.
5. by Injection for animals claimed in claim 1, it is characterized in that, described antioxidant, is selected from: vitamin E, carotenoid, ascorbic acid, ascorbyl palmitate, arabo-ascorbic acid, sodium erythorbate, citric acid, sodium sulfite EDTA and phosphoric acid derivatives.
6. by Injection for animals claimed in claim 1, it is characterized in that, described stabilizing agent, is selected from: citrate, tartrate, phosphate.
7. by Injection for animals claimed in claim 1, it is characterized in that, composed as follows:
。
8. by Injection for animals claimed in claim 1, it is characterized in that, composed as follows:
。
9. by Injection for animals claimed in claim 8, it is characterized in that, composed as follows:
Its preparation method is as follows:
Get lincomycin hydrochloride, gentamycin sulfate and propylene glycol, poloxamer, sodium benzoate, the 20ml water formation suspension that stirs, separately getting sodium citrate adds after 20ml water, add in above-mentioned suspension, with adding with stirring, by sodium sulfite with adding after 20ml water dissolution, finally add water to full dose, stir, make compound injection.
10. the preparation method of Injection for animals claimed in claim 1, is characterized in that, step is as follows:
Get lincomycin hydrochloride, gentamycin sulfate and polyhydric alcohol, solubilizing agent, antiseptic, the suitable quantity of water formation suspension that stirs, separately getting stabilizing agent adds after suitable quantity of water, add in above-mentioned suspension, with adding with stirring, by antioxidant with adding after water dissolution, finally add water to recipe quantity, stir, make compound injection.
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| CN108670951A (en) * | 2018-07-05 | 2018-10-19 | 河南牧翔动物药业有限公司 | A kind of compound sustained-released injection of gentamicin sulphate-Lincomycin Hydrochloride for animals and preparation method thereof |
| CN110354352A (en) * | 2019-07-16 | 2019-10-22 | 车媛媛 | A kind of youngster's internal medicine nebulization equipment |
| CN111388498A (en) * | 2020-03-23 | 2020-07-10 | 山东迅达康兽药有限公司 | Spectinolincomycin hydrochloride soluble powder capable of being mutually dissolved with oil seedlings after being dissolved in water and preparation method thereof |
| CN111437249A (en) * | 2020-04-21 | 2020-07-24 | 上海公谊药业有限公司 | Compound gentamicin sulfate injection and preparation method and application thereof |
| CN112043720A (en) * | 2020-09-24 | 2020-12-08 | 厦门惠盈动物药业有限公司 | Spectinomycin lincomycin soluble powder capable of being completely dissolved in various solvents and preparation method thereof |
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| CN111437249A (en) * | 2020-04-21 | 2020-07-24 | 上海公谊药业有限公司 | Compound gentamicin sulfate injection and preparation method and application thereof |
| CN112043720A (en) * | 2020-09-24 | 2020-12-08 | 厦门惠盈动物药业有限公司 | Spectinomycin lincomycin soluble powder capable of being completely dissolved in various solvents and preparation method thereof |
| CN112043720B (en) * | 2020-09-24 | 2021-07-02 | 厦门惠盈动物药业有限公司 | Spectinomycin lincomycin soluble powder capable of being completely dissolved in various solvents and preparation method thereof |
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