Anti-filarial activity of novel formulations of albendazole against experimental bruglan filariasis
Anti-filarial activity of novel formulations of albendazole against experimental bruglan filariasis
复制标题
DOI：
10.1017/s0031182006001612
复制
发表时间：
2007-04-01
期刊：
影响因子：
2.4
通讯作者：
Murthy, P. K.
中科院分区：
文献类型：
--
作者：
Gaur, R. L.;Dixit, S.;Murthy, P. K.
本研究旨在开发较好的口服活性阿苯达唑（ALB）制剂。制备了6种配方（ALB-1 ~ ALB-6），以200 mg/kg的剂量，连续5 d口服，测定其对马褐菌的抑制作用。对微丝虫、成虫和雌性生殖潜能进行了抗丝效果评价。6种ALB制剂中有3种对马来白僵菌- coucha模型的雌虫绝育率（ALB-1: 90%; ALB-3: 63%; ALB-4: 77%）有显著提高。ALB-1的杀菌效果也优于纯alb （P < 0）。001)或其上市片剂制剂Zentel （P < 0(.)）ALB-4优于纯alb （P < 0.05）。ALB-3、纯alb和Zentel的活性具有可比性。ALB-1也表现出较晚的杀丝活性，最高达78%，微丝计数下降。相比之下，纯ALB和Zentel均未表现出任何杀微丝活性。在j3 - b - malayi模型中，ALB-1和ALB-4具有边际杀菌效果，而纯ALB或Zentel则无效。综上所述，ALB-1的抗丝虫效果优于纯alb或Zentel。
The study was aimed at developing better orally active albendazole (ALB) formulations. Six formulations (ALB-1 to ALB-6) were prepared and tested against Brugia malayi in Mastomys coucha and jird (Meriones unguiculatus) at 200 mg/kg, orally, for 5 consecutive days. The anti-filarial efficacy was assessed against microfilariae (mf), adult worms and female reproductive potential. Three of the 6 ALB formulations showed greatly improved female worm sterilizing potential (ALB-1 : 90%; ALB-3: 63%; ALB-4: 77% of untreated control) in B. malayi - M. coucha model. Sterilization efficacy of ALB-1 was also better than that shown by pure-ALB (P < 0(.)001) or its marketed tablet formulation, Zentel (P < 0(.)01), while that of ALB-4 was better than pure-ALB (P < 0(.)05). The activity of ALB-3, pure-ALB and Zentel was, however, comparable. ALB-1 also showed late microfilaricidal activity with a maximum of 78%, fall in microfilarial count. In contrast, neither the pure ALB nor Zentel showed any microfilaricidal activity. In the jird - B. malayi model, ALB-1 and ALB-4 showed marginal sterilizing efficacy whereas pure ALB or Zentel were ineffective. In conclusion the anti-filarial efficacy of ALB-1 was found to be superior to pure-ALB or Zentel.