Kailasam S, Wise D L, Gangadharam P R
Mycobacteriology Research Laboratories, University of Illinois College of Medicine at Chicago 60612.
J Antimicrob Chemother. 1994 Feb;33(2):273-9. doi: 10.1093/jac/33.2.273.
We have studied the bioavailability of clofazimine following administration of a single dose of the drug in the biodegradable polymer polylactic-co-glycolic acid (PLGA). We compared the levels of clofazimine achieved in the liver with single implants with those obtained with daily oral treatment. Even though the levels achieved with implants were much lower than those obtained after daily oral treatment, they were higher than the MIC of clofazimine for Mycobacterium leprae, Mycobacterium tuberculosis and Mycobacterium avium complex (MAC). Experimental studies in beige mice after infection with MAC strain 101 showed similar reductions in cfu counts, after both single dose polymer and daily oral treatment. Macroscopically, hyperpigmentation giving an orange-yellow colour to all visceral organs, was seen in animals after daily oral treatment but not in those animals that received polymer implants.
我们研究了在可生物降解聚合物聚乳酸-乙醇酸共聚物（PLGA）中单次给药后氯法齐明的生物利用度。我们将单次植入氯法齐明后肝脏中的药物水平与每日口服治疗后的水平进行了比较。尽管植入后达到的水平远低于每日口服治疗后的水平，但仍高于氯法齐明对麻风分枝杆菌、结核分枝杆菌和鸟分枝杆菌复合群（MAC）的最低抑菌浓度（MIC）。对感染MAC菌株101的米色小鼠进行的实验研究表明，单剂量聚合物治疗和每日口服治疗后，菌落形成单位（cfu）计数均有类似程度的降低。肉眼可见，每日口服治疗后的动物所有内脏器官均出现色素沉着过度，呈橙黄色，但接受聚合物植入的动物未出现这种情况。
