Laboratory of Experimental Pathology, University of Pennsylvania, Philadelphia, Pa.
J Exp Med. 1912 May 1;15(5):498-509. doi: 10.1084/jem.15.5.498.
Salvarsan in capsule and in solution in doses varying from 0.1 to 0.6 of a gram was administered by mouth to seven patients suffering from syphilis. Five patients were given full doses of 0.6 of a gram. One patient (case 3) received in the aggregate within four weeks 2.4 grams without loss of weight or any disturbing effects. An ulcerating gumma of the knee was practically healed after a period of five weeks. This was the only patient of the seven, however, in whom notable improvement in the cutaneous manifestations followed the administration of the drug. This ulceration would probably have healed as soon, or possibly sooner, under the influence of mercury and the iodids. From the above observations, it would appear that salvarsan administered by mouth up to the full dose of 0.6 of a gram, has a perceptible though feeble therapeutic effect on cutaneous syphilitic manifestations. We should naturally expect the influence of any drug to be more evident in the case of a gumma, in which spirochaetes are only sparsely present, than in the secondary syphilides in which the spirochaetes are present in enormous numbers. Cutaneous gummata are readily healed at times by very small doses of mercury or iodids. It is interesting to note that the administration of the full dose of the drug by mouth does not appear to give rise to symptoms of systemic arsenical poisoning, unless the vomiting and diarrhea be regarded as such. After some of the full dose administrations, there was neither vomiting nor diarrhea. As salvarsan contains 34 per cent. of arsenic, these patients received the equivalent of five grains of arsenic. In case 3, in the course of four weeks the patient took by mouth the equivalent of over twelve grains of arsenic, without vomiting or having diarrhea, and with no loss of weight or disturbance of health. The urine of this patient was entirely normal. It would seem, therefore, that salvarsan is not converted in the gastro-intestinal tract into an organotropic arsenical compound, and it is possible that it may remain practically unchanged.
六〇六胶囊及溶液，剂量自 0.1 至 0.6 克，口服用于七例梅毒患者。五例用全量 0.6 克。一例（3 号病例）在四周内服共 2.4 克，未见体重减轻或其他不良影响。膝部溃疡性树胶肿在五星期后几乎痊愈。在七例中，此例是唯一的在服药后皮肤表现有显著进步者。此溃疡在应用汞剂及碘剂后，可能早就痊愈，或者更快痊愈。从上述观察，可知六〇六口服用至全量 0.6 克，对皮肤梅毒病变有显著而微弱的疗效。我们自然会期望任何药物的影响在树胶肿病例中比在二期梅毒疹病例中较为显著，因为后者螺旋体的数目极多。皮肤树胶肿有时用很小剂量的汞剂或碘剂即很容易治愈。有趣的是，全量药物的口服，似乎并不引起全身性砷中毒的症状，除非把呕吐和下泻算作是这样的症状。在几次全量投药后，既无呕吐，亦无下泻。因为六〇六含有 34%的砷，这些病人服下相当于五格令的砷。在 3 号病例中，在四周内服下相当于十二格令以上的砷，既无呕吐，亦无下泻，体重不减，健康不受影响。病人的尿完全正常。因此，六〇六在胃肠道内似乎不变成对组织有选择作用的砷化合物，而可能仍保持原形不变。
