Rice R J, Thompson S E, Arko R J, Hunter E F, Burleigh P M, Craig B T, Larsen S A
Division of Sexually Transmitted Diseases, Centers for Disease Control, Atlanta, GA 30333.
Sex Transm Dis. 1988 Jul-Sep;15(3):152-5. doi: 10.1097/00007435-198807000-00008.
The antitreponemal activity of trospectomycin (a novel 6'-propyl analog of spectinomycin) was correlated with concentrations in serum and tissue chamber fluid in a cutaneously-infected rabbit model of syphilis. After single-dose intramuscular (im) injections of trospectomycin, spectinomycin hydrochloride, and aqueous procaine penicillin G(APPG), concentrations of the drugs in paired specimens of serum and tissue fluid were determined and correlated with response of Treponema pallidum-infected lesions. Lesions responded most rapidly in APPG-treated animals. Rapid response correlated with more prolonged levels of APPG in both serum and tissue fluid. Trospectomycin, when given in single doses exceeding 40 mg/kg, surpassed penicillin in peak serum levels (greater than 60 micrograms/ml at 1 hr) but not in duration of activity. Higher and prolonged concentrations of trospectomycin in tissue fluid correlated with more effective clearance of treponemes from cutaneous lesions. Animals treated with less than 40 mg of trospectomycin/kg or with 20-80 mg/kg of the parent compound (spectinomycin hydrochloride) had cutaneous lesions that were persistently darkfield-positive, as confirmed by three or more consecutive smears.
曲古大观霉素（大观霉素的一种新型6'-丙基类似物）的抗梅毒螺旋体活性与梅毒皮肤感染兔模型血清和组织腔液中的浓度相关。在单剂量肌内注射曲古大观霉素、盐酸大观霉素和普鲁卡因青霉素G（APPG）后，测定血清和组织液配对样本中的药物浓度，并与梅毒螺旋体感染病变的反应相关联。APPG治疗的动物病变反应最快。快速反应与血清和组织液中APPG水平持续时间更长相关。单剂量超过40mg/kg的曲古大观霉素，血清峰值水平超过青霉素（1小时时大于60μg/ml），但活性持续时间未超过。组织液中曲古大观霉素浓度更高且持续时间更长，与皮肤病变中梅毒螺旋体的更有效清除相关。用低于40mg/kg的曲古大观霉素或20-80mg/kg的母体化合物（盐酸大观霉素）治疗的动物，经连续三次或更多次涂片证实，其皮肤病变暗视野检查持续呈阳性。
