The Introduction of Bicozamycin

Posted in Pharmaceutical materials, Pharmaceutical Raw Materials 28. Dec, 2011 · Edit

 
Bicozamycin is equated on a placebo fashionable an expected, randomised, double-blind experiment of the prevention of discriminating looseness of the bowels amid thirty American language travellers fresh came inward Guadalajara, United Mexican States. None from the eleven branches of knowledge applied bicozamycin by word of mouth because leash wk at a dosage of five hundred magnesium fourfold a mean solar day educated looseness of the bowels equally compared with an relative incidence of 53% looseness of the bowels (decade by nineteen branches of knowledge) in the placebo mathematical group (atomic number 15 = 0.003). Bicozamycin cost comfortably allowed. Branches of knowledge of commutes inwards predominate aerophilous feculent plant life amidst the eleven branches of knowledge dealt with bicozamycin displayed the coming into court of entirely one and only highly insubordinate Citrobacter freundii at the end of 1 wk of therapy and only a absolute of six insubordinate sequesters at the death of 3 wk. Altogether insubordinate sequesters broke to channelize this electrical resistance to a recipient role Escherichia coli. Bicozamycin appears to cost substantially accommodated and good because a contraceptive federal agent versus traveller looseness of the bowels.
The efficacy of bicozamycin, a poorly absorbable antibiotic, in the treatment of acute diarrhea was assessed in a prospective, double-blind study of 140 adults from the United States visiting Guadalajara, Mexico. Patients randomly received bicozamycin (500 mg orally four times daily) or placebo for 3 days. The mean duration of illness was shorter in the bicozamycin than the placebo treatment groups for patients with diarrhea due to Shigella (37 versus 96 hours; p = 0.01), toxigenic Escherichia coli (31 versus 60 hours; p = 0.003), and unknown pathogens (18 versus 41 hours; p = 0.02). Cramps were significantly relieved by bicozamycin in all patients. Treatment failed in significantly fewer patients treated with bicozamycin than those treated with placebo when diarrhea was associated with Shigella, Salmonella or toxigenic E. coli. Bicozamycin was well tolerated and appears to be effective therapy for acute travelers’ diarrhea of diverse causes. These data show the value of an antibiotic in the therapy of toxigenic E. coli infection and indicate a need to reevaluate the clinical dictum that nonabsorbable antibiotics are ineffective against invasive enteropathogens.
Bicozamycin (BZM) is an antibiotic obtained from a fermented culture of Streptomyces sapporonensi.For physicochemical properties, BZM technical occurs as white to brownish white crystals or powder, and has no odor or slightly has a characteristic odor. It is freely soluble in water, soluble in methanol, slightly soluble in acetone and in ethanol, and practically insoluble in ether and in chloroform.BZM has an antibacterial effect on Gram-negative bacteria and a growth promoting effect on chickens (including broilers) and pigs.Bicozamycin (8,10- diaza-6-hydroxy-5-methylene- 1- (2-methyl-1,2,3-trihydroxypropyl)-2-oxabicyclo[4.2.2]decan-7,9-dione), formerly called bicyclomycin, is an antibiotic witha unique chemical structure produced from the culture filtrate of a strain of Streptomyces sapporonensis (Nishida et aL, 1972). It is a weakly basic substance which is freely soluble in water, soluble in methanol, but practically insoluble in chloroform,ethyl acetate, benzene or n-hexane (Miyoshi et aL, 1972). It is active against Gram-negative bacteria, such as Esche,Schia coli, Salmonella spp., Shigella spp. And Klebsiella spp., but excluding Proteus spp. and Pseudomonas aeruginosa. In antibacterial tests in vitro, the minimum inhibitory concentration (MIC) values for E.coli were found to be 25-50 tzg/ml (Kanai et al., 1983; Wang and Namioka, 1983;Kawarasaki et al., 1994). Oral administration of this antibiotic is appropriate in the treatment of bacterial diarrhoea in pigs and calves and a daily dose of 5-10 mg/kg has been established as the recommended dose. Double the recommended dose may be indicated in severe cases. Kanai and colleagues (1983) and Wang and Namioka (1983) demonstrated the drug’s usefulness as a therapeutic agent against colibacillosis in piglets. Although the distribution of bicozamycin in rats, rabbits and dogs has already been studied (Nishida et al., 1972), there are no published reports on the plasma pharmacokinetics and tissue residues in other domestic animals.
The purpose of this study was to determine whether the concentration of bicozamycin increased in the plasma of pigs after consecutive daily oral dosing andhow long bicozamycin residues remained in the tissues after its withdrawal.
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