Greenwood D, Slack R C
Infection. 1981;9(5):223-7. doi: 10.1007/BF01640720.
The antibacterial activity of hexamine and two of its organic acid salts was compared by continuous turbidimetric monitoring of static cultures exposed to the drugs and in an in vitro model of the treatment of bacterial cystitis. At pH 5.5, concentrations of 32 to 125 mg hexamine per 1 caused some inhibition of bacterial growth, but 250 to 500 mg/l were needed to suppress growth overnight. Hexamine hippurate was found to be less active than hexamine itself, whereas hexamine mandelate was as active as the parent compound. The antibacterial effect was not inoculum dependent over the range 10(6) to 10(8) bacteria per ml, but the activity observed in pooled urine was rather less than that found in broth at the same pH. When a dense bacterial culture was exposed to changing concentrations of hexamine compounds in the bladder model, a 1 g dose infused over a 12-hour period suppressed bacterial growth for 16 to 20 hours. No systematic difference was found in the activity of the three hexamine compounds, but a similar effect was achieved by a very much lower concentration of ampicillin.
通过对暴露于药物的静态培养物进行连续比浊法监测以及在细菌性膀胱炎的体外模型中,比较了乌洛托品及其两种有机酸盐的抗菌活性。在pH 5.5时,每升32至125毫克乌洛托品的浓度对细菌生长有一定抑制作用,但需要250至500毫克/升才能抑制过夜生长。发现马尿酸乌洛托品的活性低于乌洛托品本身,而扁桃酸乌洛托品与母体化合物活性相当。在每毫升10(6)至10(8)个细菌的范围内,抗菌效果不依赖于接种量,但在混合尿液中观察到的活性比在相同pH值的肉汤中要低得多。当在膀胱模型中将密集的细菌培养物暴露于不同浓度的乌洛托品化合物时,在12小时内输注1克剂量可抑制细菌生长16至20小时。在三种乌洛托品化合物的活性方面未发现系统性差异,但氨苄西林浓度低得多时也能达到类似效果。