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filingDate 1994-08-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 1995-04-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-9508991-A1
titleOfInvention Parenteral busulfan for treatment of malignant disease
abstract Stable parenteral formulations of busulfan safe for parenteral administration. An HPLC assay for busulfan sensitive enough to dependably quantitate concentrations in plasma as low as approximately 100 ng/ml was developed. The stability of these formulations was investigated to select preparations providing desirable plasma pharmacokinetic parameters with parenteral versus oral administration. In addition, quantitative extraction technology was established for reliable quantification of bulsulfan in plasma samples after both oral and parenteral drug administration. When administered to experimental animals, the parenteral busulfan formulation yielded significantly higher plasma drug concentrations and higher area under the plasma concentration vs. time curve than did the oral (standard) tablet preparation. The improved bioavailability of the parenteral formulation optimizes high dose busulfan thepary against malignant disease and improves the safety of such therapy.
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