en فارماکولوژی Pharmacology پژوهشي Original Research <pre style="text-align: justify;"> Benznidazole and nifurtimox are two drugs that are used to treat trypanosomiasis. Ursolic acid (UA) reportedly acts against trypomastigotes and intracellular amastigotes of <em>Trypanosoma cruzi</em>. Accordingly, it is expected to have therapeutic benefits in the treatment of trypanosomiasis. Therapeutic application of a compound requires the investigation of its pharmacokinetic properties in order to obtain relevant information to design the <em>in vivo</em> assays and dose regimen. Regarding this, the current study aimed to evaluate the pharmacokinetic profile of UA administered to rats at different doses and routes (i.e., 1 mg/kg intravenously and 20 and 50 mg/kg orally). According to the results, the oral bioavailability was significantly different between the two groups that orally received the UA doses of 20 mg/kg (2.8%) and 50 mg/kg (1.55 %). The result suggests the interference of the poor aqueous solubility of UA on its absorption process. The pharmacokinetic parameters related to the distribution and elimination were similar. Accordingly, it can be concluded that at this dose range, there is no saturation in this process rendering a linear the kinetics. The pharmacokinetic properties of UA were observed in this study indicated that the improvement of water solubility in this medicine through pharmacotechnical resources would be a great utility for its oral bioavailability and development of a product with the potential therapeutic application. The oral administration of this new pharmaceutical formulation should be investigated in future studies. </pre> Pharmacokinetics, Ursolic acid, HPLC, Trypanosomiasis 25 31 http://pbr.mazums.ac.ir/browse.php?a_code=A-10-483-2&slc_lang=en&sid=1 Manuel Alejandro Henao Alzate manuelhenao888@hotmail.com 10031947532846003675 10031947532846003675 No Department of Natural Active Principles and Toxicology, School of Pharmaceutical Sciences, University of Estadual Paulista, Araraquara, Sao Paulo, Brazil Marco Antonio Ferraz Nogueira Filho nogueira.maf@gmail.com 10031947532846003676 10031947532846003676 No Department of Natural Active Principles and Toxicology, School of Pharmaceutical Sciences, University of Estadual Paulista, Araraquara, Sao Paulo, Brazil Taisa Busaranho Franchin taisabf@hotmail.com 10031947532846003677 10031947532846003677 No Department of Natural Active Principles and Toxicology, School of Pharmaceutical Sciences, University of Estadual Paulista, Araraquara, Sao Paulo, Brazil Jonata Augusto de Oliveira jonataaugustooliveira@gmail.com 10031947532846003678 10031947532846003678 No Department of Natural Active Principles and Toxicology, School of Pharmaceutical Sciences, University of Estadual Paulista, Araraquara, Sao Paulo, Brazil Caroline Damico Candido carol_narya@hotmail.com 10031947532846003679 10031947532846003679 No Department of Natural Active Principles and Toxicology, School of Pharmaceutical Sciences, University of Estadual Paulista, Araraquara, Sao Paulo, Brazil Junior Furini jfurini@usp.br 10031947532846003680 10031947532846003680 No Department of Clinical Analysis, Toxicological and Bromatological, School of Pharmaceutical Sciences, University of Sao Paulo, Ribeirao Preto, Sao Paulo, Brazil Sergio de Albuquerque sdalbuqu@fcfrp.usp.br 10031947532846003681 10031947532846003681 No Department of Clinical Analysis, Toxicological and Bromatological, School of Pharmaceutical Sciences, University of Sao Paulo, Ribeirao Preto, Sao Paulo, Brazil Rosangela Gonçalves Peccinini rosangela.peccinini@unesp.br 10031947532846003682 10031947532846003682 Yes Department of Natural Active Principles and Toxicology, School of Pharmaceutical Sciences, University of Estadual Paulista, Araraquara, Sao Paulo, Brazil