Azole pharmaceutical formulations for parenteral administration and methods for their preparation and their use as treatment of diseases sensitive to azole compounds
A parenteral azole composition comprises a first solvent, made of benzyl alcohol and/or an acidified alcohol such as ethanol, and a lipophilic component such as PEG400, and the azole, or triazole, such as itraconazole or posaconazole dissolved in this first composite solvent vehicle that is essentially free of surfactants, particularly non-ionic surfactants, and has low levels of water, preferably less than 5% water. The composition may be further diluted with an infusion fluid, such as normal saline or 5% or 10% dextrose in water, before infusion into an immunocompromized mammal, preferably a human. The composition is useful for the treatment and suppression of infections caused by microbes such as yeast and molds that are sensitive to azoles, but it may be extended to dissolve other pharmaceutically active agents that can be used to treat other types of infectious diseases or other ailments, such as malignant and autoimmune diseases.非経口アゾール組成物は、ベンジルアルコールおよび／もしくは酸性化アルコール（例えば、エタノール）、ならびに親油性成分（例えば、ＰＥＧ４００）から作製される第１の溶媒、ならびにこの第１の複合溶媒ビヒクル中に溶解された上記アゾールもしくはトリアゾール（例えば、イトラコナゾールもしくはポサコナゾール）を含み、界面活性剤、特に、非イオン性界面活性剤を本質的に含まず、低レベルの水、好ましくは、５％未満の水を有する。上記組成物は、免疫不全状態の哺乳動物（好ましくは、ヒト）への注入の前に、注入液（例えば、生理食塩水、または５％もしくは１０％デキストロース水溶液）でさらに希釈され得る。
