Kamme C, Kahlmeter G, Melander A
Scand J Infect Dis. 1978;10(2):135-42. doi: 10.3109/inf.1978.10.issue-2.07.
Varying doses of spiramycin were administered orally to healthy volunteers, and concentrations in serum and saliva were determined. The absorption of the drug was not significantly influenced by concomitant food intake. Saliva peak concentrations were 1.3--4.8 times higher than peak concentrations in serum. The elimination half life was 2--3 h in serum, and 4--8 h in saliva. Accumulation of the drug was seen in saliva but not in serum. The possible effect of spiramycin in eliminating bacteria from the nasopharynx was evaluated in vitro by comparing the spiramycin saliva concentrations with the MICs of bacteria known to establish themselves in the nasopharynx. At a concentration of 1.2 microgram/ml, spiramycin inhibited all investigated strains of group A streptococci, pneumococci and Branhamella catarrhalis, and at 2.4 microgram/ml all investigated gonococci. Concentrations of 19 and 38 microgram/ml, respectively, were required to inhibit all meningococci and Haemophilus influenzae. Following administration of 1.5 g spiramycin as a single daily dose for 3 days, the mean concentration in saliva reached or surpassed the MIC values of streptococci, pneumococci and Branhamella for 45 h, and of gonococci for 25 h. The possible use of spiramycin for prevention of relapses in acute otitis media and in treatment of serous otitis media is discussed, as well as the possible use of the drug in gonococcal and meningococcal nasopharyngeal carriage.
将不同剂量的螺旋霉素口服给予健康志愿者,并测定血清和唾液中的浓度。药物的吸收未受到同时进食的显著影响。唾液中的峰值浓度比血清中的峰值浓度高1.3至4.8倍。血清中的消除半衰期为2至3小时,唾液中为4至8小时。该药物在唾液中有蓄积,但在血清中没有。通过将螺旋霉素唾液浓度与已知在鼻咽部定植的细菌的最低抑菌浓度(MIC)进行比较,在体外评估了螺旋霉素消除鼻咽部细菌的可能效果。在浓度为1.2微克/毫升时,螺旋霉素抑制了所有被研究的A组链球菌、肺炎球菌和卡他布兰汉菌菌株,在2.4微克/毫升时抑制了所有被研究的淋球菌。分别需要19和38微克/毫升的浓度来抑制所有脑膜炎球菌和流感嗜血杆菌。每日单次服用1.5克螺旋霉素,连续服用3天,唾液中的平均浓度在45小时内达到或超过了链球菌、肺炎球菌和卡他布兰汉菌的MIC值,在25小时内达到或超过了淋球菌的MIC值。文中讨论了螺旋霉素在预防急性中耳炎复发和治疗浆液性中耳炎方面的可能用途,以及该药物在淋球菌和脑膜炎球菌鼻咽部携带方面的可能用途。