Down W H, Sacharin R M, Chasseaud L F, Kirkpatrick D, Franklin E R
Toxicology. 1977 Dec;8(3):333-46. doi: 10.1016/0300-483x(77)90081-6.
Plasma concentrations of radioactivity declined biphasically with half-lives of about 15 and 58 h respectively in rats dosed with monosodium DL-[14C]tartrate for 7 days at a dose level of 2.73 g/kg/day. Uptake and retention of radioactivity occurred in blood cells, kidneys and bones where it was detected for at least 12 days after dosing. Renal retention (11202 +/- 4469 ppm at 6 h, n = 7) was probably due to precipitation of the poorly soluble calcium DL-tartrate in the tubules leading to increased kidney weight, nephrotoxicity and even death. The more soluble, naturally-occurring L(+)-[14C] tartrate was not retained in the kidneys (1287 +/- 118 ppm at 6 h, n = 8) when administered to rats under the same conditions, and the initial decline of plasma concentrations of radioactivity was more rapid (t 0.5 approx. 3 h). For this reason, monosodium L(+)-tartrate was non-toxic at 2.73 g/kg/day whereas monosodium DL-tartrate was toxic at this dosage.
给大鼠按2.73 g/kg/天的剂量连续7天投喂DL-[14C]酒石酸钠后，血浆放射性浓度呈双相下降，半衰期分别约为15小时和58小时。血细胞、肾脏和骨骼摄取并保留了放射性，给药后至少12天仍能检测到。肾脏潴留（6小时时为11202±4469 ppm，n = 7）可能是由于难溶性DL-酒石酸钙在肾小管中沉淀，导致肾脏重量增加、肾毒性甚至死亡。在相同条件下给大鼠投喂时，更易溶的天然L(+)-[14C]酒石酸在肾脏中无潴留（6小时时为1287±118 ppm，n = 8），且血浆放射性浓度的初始下降更快（t0.5约为3小时）。因此，L(+)-酒石酸钠在2.73 g/kg/天的剂量下无毒，而DL-酒石酸钠在此剂量下有毒。
