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Antimicrob Agents Chemother. 2010 Aug;54(8):3481-3. doi: 10.1128/AAC.00271-10. Epub 2010 May 24.
Biophysical methods to study the binding of oritavancin, a lipoglycopeptide, to serum protein are confounded by nonspecific drug adsorption to labware surfaces. We assessed oritavancin binding to serum from mouse, rat, dog, and human by a microbiological growth-based method under conditions that allow near-quantitative drug recovery. Protein binding was similar across species, ranging from 81.9% in human serum to 87.1% in dog serum. These estimates support the translation of oritavancin exposure from nonclinical studies to humans.
生物物理方法研究糖肽类药物奥他万古霉素与血清蛋白的结合时,会受到实验器具表面非特异性药物吸附的干扰。我们采用基于微生物生长的方法,在允许近乎定量回收药物的条件下,评估了奥他万古霉素与人、鼠、犬和狗血清的结合情况。在各物种中,蛋白结合情况相似,范围从人血清中的 81.9%到狗血清中的 87.1%。这些估计结果支持将非临床研究中的奥他万古霉素暴露量数据外推至人体。