Groupe Chimiothérapie Antiparasitaire, UMR 8076 CNRS, Faculté de Pharmacie, Université Paris-Sud, Rue Jean-Baptiste, 92296 Châtenay-Malabry Cedex, France.
Parasite. 2011 Nov;18(4):333-6. doi: 10.1051/parasite/2011184333.
2-n-propylquinoline is presently a drug-candidate for the treatment of visceral leishmaniosis in pre-clinical development. As this compound is in an oily state, it needs to be formulated and the objectives of this study are: to prepare a formulation; to demonstrate that the new salted formulation did not alter the activity of the active ingredient; and finally, that this activity was quite good compared to the reference oral drug, miltefosine. Therefore, a 2-n-propylquinoline formulation, as camphorsulfonic salt, was prepared and characterised. On the Leishmania donovani / Balb/c mice model, a treatment by oral route at 60 mmoles/kg/day for ten consecutive days with this formulation was compared to 2-n-propylquinoline alone and to miltefosine, the oral reference drug. The salt formulation did not alter the activity of the 2-n-propylquinoline. The formulation reduced the parasite burden of 76% compared to 89% for miltefosine (not significant). The characteristics of this formulation results in a suitable drugability of 2-n-propylquinoline for further studies.
2-正丙基喹啉目前是一种用于治疗内脏利什曼病的临床前开发药物候选物。由于该化合物呈油性状态，因此需要进行制剂研究。本研究的目的是：制备一种制剂；证明新的盐形式的制剂不会改变活性成分的活性；最后，与参考口服药物米替福新相比，该活性相当好。因此，制备并表征了 2-正丙基喹啉作为樟脑磺酸盐的制剂。在利什曼原虫/ Balb/c 小鼠模型中，通过口服途径在连续 10 天每天以 60mmol/kg 的剂量用该制剂进行治疗，与单独使用 2-正丙基喹啉和米替福新（口服参考药物）进行了比较。盐制剂没有改变 2-正丙基喹啉的活性。与米替福新（无显著差异）相比，该制剂将寄生虫负荷减少了 76%。该制剂的特点为进一步研究提供了适合的 2-正丙基喹啉的可药用性。
