不同晶型的甲苯达唑对小鼠继发性细粒棘球蚴病的疗效比较(摘要)

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甲苯达唑(Meb)在不同或同一溶剂体系中,若改变其结晶条件可获得不同晶型的Meb,即MebⅠ、MebⅡ和MebⅢ晶型,与国外报道的MebB、C和A晶型相一致,一般认为,亚稳态晶型具有较好的生物活性,而Meb3种晶型的稳态性依次为Ⅲ>Ⅱ>Ⅰ。驱虫试验证明,Ⅰ和Ⅱ为有效晶型,而Ⅲ为无效晶型,故目前国内外均取MebⅡ型(即C型)供药用。本文系进一步观察Meb3种晶型对小鼠继发性细粒棘球蚴病的治疗作用。 小鼠于感染后5~8月用MebⅠ、MebⅡ或MebⅢ口服治疗,剂量为12.5和25mg·kg~(-1)·d(-1),连给14~28d对,MebⅠ和MebⅡ各组的平均囊重均明显小于对照组,MebⅢ各组的囊重则与对照组的相仿,但明显大于MebⅠ的各相应组。另一方面,尽管统计学上的差别不显著,但MebⅠ各组的平均囊重小于而囊重抑制率则高于MebⅡ的各相应组。 感染8个月的小鼠口服MebⅠ12.5或25mg·kg~(-1)·d~(-1),连给14d后,囊的生发层即示有不同程度的变化,且以剂量较大组为重。MebⅡ25mg·kg~(-1)组与MebⅠ相应组的相仿,但小剂量组的变化则较轻。当疗程延长至28d时,MebⅠ各组生发层的病变进一步加重。尤其25mg·kg~(-1)组,生发层示严重变化的占观察切面数的32.2%。MebⅡ组的生发层变化较MebⅠ相应组的为轻。感染小鼠口服MebⅢ12.5或25mg·kg~(-1)·d~(-1),连给 14 Mebendazole (Meb) in different or the same solvent system, if you change the crystallization conditions can be obtained Meb Me, Meb Ⅱ and Meb Ⅲ crystal form, with the reported MebB, C and A crystal form consistent, It is generally believed that the metastable crystal has better biological activity, while the steady state of the Meb3 crystal is Ⅲ> Ⅱ> Ⅰ. Deworming test proved that, Ⅰ and Ⅱ as the effective crystal form, and Ⅲ as the invalid crystal form, so at home and abroad are taking Meb Ⅱ type (ie C type) for medicinal purposes. This article is to further observe the Meb3 crystal form of mouse secondary particle hydatid disease treatment. Mice were orally treated with Meb I, Meb II or Meb III at doses of 12.5 and 25 mg · kg -1 (d -1) for 5-8 days after infection, respectively. The mice in groups Meb Ⅰ and Meb Ⅱ The mean cystic weight was significantly less than that of the control group. The cystic weight of each group was similar to that of the control group, but significantly higher than that of the corresponding group of Meb I. On the other hand, although the statistical difference was not significant, the mean cystic weight in Meb I groups was lower than that in Meb II, while the cystic weight was higher in each group. Mice infected with 8-month-old oral MebI12.5 or 25mg · kg -1 · d -1, even after 14d, the cystic germinal layer showed varying degrees of change, and the larger dose Group is heavy. Meb II25mg · kg -1 group was similar to the corresponding group Meb Ⅰ, but the changes in the low-dose group were lighter. When the course of treatment was prolonged to 28 days, the lesions of germinal layers in Meb I groups were further aggravated. Especially 25mg · kg ~ (-1) group, the germinal layer showed serious changes accounted for 32.2% of the number of observed sections. Meb Ⅱ group germinal layer changes compared with the corresponding group of MebI is light. Mice infected with oral MebⅢ12.5 or 25mg · kg ~ (-1) · d ~ (-1), even to 14
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