GC20, a novel soluble bis-chelated gold(I)-diphosphine compound, has been reported\nas a promising anticancer candidate. Assessing the pharmacokinetic properties of GC20 is critical\nfor its medicinal evaluation. First, a sensitive and specific liquid chromatography tandem mass\nspectrometry (LC-MS/MS) was developed and well validated to determine GC20 in rat plasma\nand rat tissue homogenate after one step protein precipitation. Chromatographic separation was\nachieved on an Angilent ZORBAX-C18 column (3.5 microm, 2.1*50 mm) with gradient elution and\nmass spectrometry was performed on a triple quadrupole in positive ion mode using an electrospray\nionization source. This method was then applied to investigate the pharmacokinetics and tissue\ndistribution of GC20 in rats after intravenous administration. The results showed that the plasma\nexposure of GC20 in vivo increased with increasing doses after a single dose. However, after multiple\ndoses, a significant accumulation and a saturation at elimination were observed for GC20 in rats.\nMoreover, after intravenous administration, GC20 was widely distributed in various tissues, with the\nhighest levels in the lung, spleen, liver, and pancreas, followed by the kidney and heart, while the\nlowest level was found in the brain. This is the first report on the pharmacokinetic properties of GC20.
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