SOME FACTORS AFFECTING THE TOXICITY OF TRIVALENT ANTIMONYL AMMONIUM GLUCONATE

Clinical reports on trivalent antimonyl ammonium gluconate (AAG) in the therapy of Schistosomiasis Japonieum revealed certain advantages of this compound over tartar emetic. This prompted a study of some factors which may alter the toxicity of this compound. The LD₅₀ of AAG after intraperitoneal injection in 10、20 and 30 grams mice were found to be 155、160 and 137 mg/kg respectively. For mice of 3.5、5.5、7.5 and 9.5 weeks of age, the LD₅₀ were respectively 114、123、117 and 123 mg/kg. The difference is not statistically significant. AAG did not show a sex difference in toxicity in 3.5、7.5 and 9.5 week old mice; but in 5.5 week old mice, AAG did show a higher toxicity in females than in males. For example, in one experiment the LD₅₀ for female mice was 110(102-118) mg/kg, whereas that for males was 140(123-147) mg/kg. At temperatures of 4℃、10℃、20℃、24℃ and 30℃, the LD₅₀ of AAG were 160、147、122、117 and 94 mg/kg respectively. It is likely that AAG is more toxic at higher room temperature than at lower temperatures. The intravenous, intramuscular and intraperitoneal LD₅₀ of AAG were approximately the same (123-150 mg/kg), whereas the oral LD₅₀ was about eight times as high (1000 mg/kg). The intraperitoneal LD₅₀ of AAG was 120(114-125) mg/kg for mice on a normal diet, 96(87-105) mg/kg for mice on a diet low in protein and 150(141-173) mg/kg for animals fed a high protein diet. The acute toxicity of AAG is independent of its antimony content since the intraperitoneal LD₅₀ were respectively 102、105、92 and 105 mg/kg for AAG containing 12.2% 18.7%、33.5% and 41.0% of antimony.