Decoquinate

Product: Decoquinate, Deccox;
Ethyl 6-decyloxy-7-ethoxy-4-hydroxy-3-quinolinate
CAS NO: 18507-89-6
Molecular Formula: C24H35NO5
Molecular Weight: 417.54
Character: White or lemon powders
Assay: (by HPLC)：≥95.0 %
 

Decanoate ester oxygen quinoline (decoquinate) is a very effective use of anticoccidial quinolones animal drugs, it is mainly through the inhibition of sporozoite in the early stages of development, the middle stage of killing play a role in early schizonts. This article decanoate ester quinoline physical and chemical properties of oxygen, anticoccidial activity, pharmacokinetic characteristics, clinical application and combination therapy has done a systematic introduction.
Physical and chemical properties and technical specifications
Decanoate ester oxygen quinoline-white or yellowish crystalline powder, the chemical name is 6 - Kuei-oxygen -7-- ethoxy -4-- hydroxyquinoline -3-- carboxylate formula C24H35NO5, molecular weight 417.55; in chloroform or ether, very slightly soluble, insoluble in water or ethanol; melting point of 242 ℃ ~ 246 ℃, purity ≥ 98%, Residue on ignition ≤ 0.1%, heavy metals (Pb) ≤ 0.001%, Arsenic (As dollars) ≤ 0.0002%, chloride (Cl) ≤ 0.01%.
Anticoccidial activity
To determine the decanoate ester oxygen anticoccidial effect of chloroquine, the experts selected in 2007 is widely used in the current production of anti-coccidia drugs Ma degree m star ammonium nicarbazin + Ethyl methyl benzene and methyl amide salt sp factors and their contrast detection under the conditions of artificial infection of anticoccidial effects of several drugs, and 4 anticoccidial drugs compared to anticoccidial index (ACI) as a comprehensive assessment of drug treatment targets. The results were integrated anticoccidial index of oxygen decanoate ester group 194.53 chloroquine, nicarbazin + Ethyl methyl benzene amide group 189.87, 165.42 Narasin group, ammonium group MA degree 190.15 meters stars. Salinomycin in the stool when the group can see oocysts nicarbazin benzene + methyl group and the ethoxy amide MA degree m ammonium group only very few stars of the oocysts, decyl ester oxygen quinoline group and the healthy group no oocysts, fecal score was the highest salt ADM, MA degree m Nicarbazin Star + ammonium group and methyl group ethoxy benzene, followed by amide, decyl ester group had the lowest oxygen quinoline. According to evaluation criteria of anticoccidial effect, ACI <160, low anticoccidial effect; 160 <ACI <180, moderate anticoccidial effect; 180 <ACI, high anticoccidial effect. The results show that decanoate ester oxygen quinoline anticoccidial index (ACI) is greater than 190, are effective anticoccidial drugs, and with the same drugs are effective anticoccidial ammonium MA degree m stars compared with the unmatched safety sex.
Experts in 2002 with the decanoate ester oxygen quinoline 20ppm, 30ppm, 40ppm mixed feeding by the Eimeria strains Edmonton chicken meat inoculated with the AA and MA degrees m and compare the observed star ammonium, 20ppm ~ 40ppm oxygen quinoline capric 5ppm MA degree m ester and ammonium stars are on trial gondii strains of Eimeria tenella in force, but decanoate ester oxygen was better than chloroquine MA degree m ammonium stars. Check the oocysts found high, medium and low-dose chloroquine decanoate ester group oxygen in the feces and cecum were not oocysts, an explanation of the Eimeria strain is not resistant to Edmonton oxygen decanoate ester of the mutant insect strains of chloroquine; Madhu La feces and cecum in the azithromycin group had oocysts, although rarely, an explanation of the Edmonton Eimeria strains containing the mutant insect-resistant strains of Madura ADM. High, medium and low-dose group, and decyl ester oxygen quinoline MA degree m ammonium group, ACI stars were more than 180, are effective drugs.
Pharmacokinetic
Decanoate ester oxygen quinoline coccidian asexual reproductive stages in the role. Decanoate ester oxygen into the sporozoite quinoline cells, by interfering with DNA synthesis and prevent its development. Decanoate ester oxygen quinoline early in the coccidia life cycle began to play a role, thus avoiding damage to the poultry gut.
Decanoate ester quinoline rapid absorption of oxygen, can be achieved in 1 hour anticoccidial effective concentration, 3 days after the concentration reached peak levels. In cattle and sheep were given unlabeled oxygen decanoate ester 5 day and 7 days after chloroquine, using 14C labeled decanoate ester oxygen single dose of chloroquine intravenously to cattle and sheep, a half-hour after peak plasma radiation. Decanoate ester oxygen quinoline in rats, some metabolism, 3 metabolites, can not be determined from its structure. In ruminant animals, only two metabolites identified, and the proportion of lower than in rats. The main discharge in ruminants as manure, followed by urine. In sheep, the total dose excreted in urine 36%, 35% discharged within 24 hours, the urine within 3 days and the decyl ester oxygen metabolites chloroquine completely discharged.
Clinical application
Drug prevention is the prevention of chicken coccidiosis main method. However, the continual emergence of drug-resistant strains of insects, worms and even multi-drug resistant strains emerging, such as anti Diclazuril and salinomycin, anti-Diclazuril and salad Eimeria CTC ball Bugs The emergence of strains, which calls for a more varied and more flexible application of measures for the drug to improve their on-site sensitivity of coccidia to reduce the increasing cost of coccidiosis control. Studies have shown that continuous use of ammonium horse farm level meter and the use of star two years later with Diclazuril ammonium MA degree m star is no difference between the sensitivity of coccidia, it seems Diclazuril to improve the use of horses degree of resistance of rice Star ammonium did not make any difference. This and previous studies --- in the use of an anti-coccidial drug resistance after treatment can last for at least 90 weeks are consistent. Resistance to coccidiosis is likely to continue for so long because it is impossible to become extinct from the chicken coop. Therefore, the introduction of a drug, the resistance will soon be generated. Britain has confirmed that the latest reports, several Eimeria resistant mutant selection in the introduction of oxygen decanoate ester quinoline first 3 weeks to 6 weeks occur, however, the rapid creation of decyl ester oxygen resistance to chloroquine adverse effects on animal performance is not because the birds would have recycled the induction of immune oocysts. This is why the decanoate ester oxygen chloroquine resistance in the initial post, in many countries still in heavy use of reason.
Since the 70s of the 20th century, decanoate ester oxygen quinoline has been widely used in many countries, poultry coccidiosis, but has not been used in China. Ya come to the U.S. in 2006 the first sale in China decanoate ester oxygen quinoline has aroused great attention and widespread concern for the following reasons: 1. The first time in China to use, no resistance, the rotation is the best drug to kill coccidia, promote growth, improve color, with excellent anticoccidial effect and promote the growth performance; 2. coccidia life cycle in the early days of play, and the longest continuous role; 3. anticoccidial broad spectrum 6 most dangerous avian coccidiosis has a good effect; 4. stability, the appropriate temperature and humidity conditions, the decanoate ester oxygen quinoline in 4 years to maintain the quality and stability.
USP has a collection of 1% to 10% decanoate ester oxygen premix chloroquine. At present in China, including Shandong Sinder Technology has Ltd. and other manufacturers in the production of raw materials decanoate ester oxygen quinoline drugs commonly used in the domestic market, agents for the quinoline oxygen decanoate ester of 6% premix, mixed feeding, adding 27.2 per ton of feed g (O quinoline ester of capric dollars); there decanoate ester oxygen quinoline soluble powder, mixed drink, add 13.6 grams per ton of water (oxygen quinoline ester of capric dollars), generally for 7 days to 14 days.
Combination
To improve the anticoccidial effect of reducing drug resistance, combination therapy can be taken. In the early coccidiosis (coccidia of asexual reproduction), the use of oxygen decanoate ester + chloroquine or Diclazuril Toltrazuril, decyl acetate + MA degrees quinoline oxygen meter star ammonium, decyl acetate + quinoline oxygen and other joint clopidol Drug treatment can play a synergistic role in enhancing the killing effect, while allowing each drug dose reduced by 1 / 2. Incidence in the whole of coccidia can be used decanoate ester oxygen quinoline + Sulfaquinoxaline sodium decanoate ester chloroquine + sulfadoxine-oxygen and sodium chloride combination pyrazine programs to asexual reproduction and sexual reproduction of coccidia may also be inhibited and kill.
Conclusion
Decanoate ester is the only oxygen quinoline by Japan, the European Union, the United States and the Chinese government approved the use of chemical-based anticoccidial drugs. And China allows the use of feed additives, veterinary drugs without any incompatibility. Low toxicity and well tolerated; 80 times the recommended amount is still safe. Fast metabolism, drug withdrawal after 3 days, the tissue residue concentration below 1 × 10-6. In summary, decyl oxygen toxicity as a novel quinoline ester broad-spectrum anticoccidial drugs, and has broad market prospects.