Abstract |
Nicarbazin, a drug used to control the protozoal disease coccidiosis in poultry, is a complex of the highly insoluble drug 4,4'-dinitrocarbanilide with 2-hydroxy-4,6-dimethylpyrimidine. The structures of this and other 4,4'-dinitrocarbanilide complexes have not been determined, but an analogous 2:1 complex of 4,4'-dinitrodiphenylamine with 1,4-diacetylpiperazine has been prepared in which the only possible bonds are hydrogen bonds between the amide carbonyls and amino hydrogens. Scanning electron microscopy revealed that micron-size crystals of nicarbazin disintegrate in water to form much smaller dinitrocarbanilide crystals. Similar complex dissolution in the gut of poultry may account for the greater effectiveness of dinitrocarbanilide when administered as complexed rather than uncomplexed drug. Particle size problems associated with other highly insoluble drugs and pesticides may be resolved by the use of nicarbazin-like complexes.
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Authors | E F Rogers, R D Brown, J E Brown, D M Kazazis, W J Leanza, J R Nichols, D A Ostlind, T M Rodino |
Journal | Science (New York, N.Y.)
(Science)
Vol. 222
Issue 4624
Pg. 630-2
(Nov 11 1983)
ISSN: 0036-8075 [Print] United States |
PMID | 6635662
(Publication Type: Journal Article)
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Chemical References |
- Carbanilides
- Coccidiostats
- Nicarbazin
- 4,4'-dinitrocarbanilide
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Topics |
- Animals
- Carbanilides
(administration & dosage)
- Chickens
- Coccidiostats
- Crystallization
- Intestinal Absorption
- Nicarbazin
(administration & dosage)
- Poultry Diseases
(prevention & control)
- Solubility
- Structure-Activity Relationship
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