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Drug Evaluation (Antitubercular)

"PA-824, A Nitroimidazopyran Antitubercular Agent: Favorable Pharmacokinetic Parameters in Mice After Delivery in a Novel Oral Formulation."

Published in TB and Outbreaks Week, October 21st, 1996

According to an abstract submitted by the authors to the 11th International Conference on AIDS, held July 7-12, 1996, in Vancouver, British Columbia, "PA-824 is a nitroimidazopyran with potent in vitro activity against Mycobacterium tuberculosis (MIC=0.13 (mu)g/ml, MBC=2 (mu)g/ml). However, the effort to establish good in vivo efficacy was hampered by poor solubility and inefficient drug delivery. To overcome this problem, several oral formulations were developed. Plasma pharmacokinetic parameters and tissue distribution were studied in female BALB/c mice following oral administration of PA-824 in the various vehicles. One formulation, a lipid coated cyclodextrin complex, CM-2,...

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