A5023193081- Inflammatory mediators and NSAID effects
- Pharmacogenetics and Drug Metabolism
- Research on Leishmaniasis Studies
- Drug Transport and Resistance Mechanisms
- Antibiotics Pharmacokinetics and Efficacy
- Trypanosoma species research and implications
- Analytical Methods in Pharmaceuticals
- Nanoparticle-Based Drug Delivery
- Synthesis and biological activity
- Computational Drug Discovery Methods
- Veterinary Pharmacology and Anesthesia
- Veterinary Equine Medical Research
- Drug-Induced Hepatotoxicity and Protection
- Synthesis and Reactions of Organic Compounds
- HIV/AIDS drug development and treatment
- HIV Research and Treatment
- Analytical Chemistry and Chromatography
- Advanced Drug Delivery Systems
- Pancreatic function and diabetes
- Synthesis and Biological Evaluation
- Natural Antidiabetic Agents Studies
- Phytochemistry Medicinal Plant Applications
- Ocular Surface and Contact Lens
- Tuberculosis Research and Epidemiology
- Cancer therapeutics and mechanisms
Universidade Estadual Paulista (Unesp)
2013-2023
Universidade Federal de Pernambuco
2018
Universidade Federal do Paraná
2018
Centro Universitário de Araraquara
2012-2017
Universidade de São Paulo
2013
Instituto de Ciências Farmacêuticas
2011
This study measures the curcumin concentration in rat plasma by liquid chromatography and investigates changes glucose tolerance insulin sensitivity of streptozotocin-diabetic rats treated with curcumin-enriched yoghurt. The analytical method for detection was linear from 10 to 500 ng/mL. C max time reach (t max) were 3.14 ± 0.9 μg/mL 5 minutes (10 mg/kg, i.v.) 0.06 0.01 14 (500 p.o.). elimination half-time 8.64 2.31 (i.v.) 32.70 12.92 (p.o.) minutes. oral bioavailability about 0.47%....
The Musa x paradisiaca L. inflorescence, known as banana blossom or heart, is used in traditional medicine for the treatment of diabetes mellitus. Aim study: aim study was to investigate antidiabetic activity aqueous extracts and fractions prepared from bracts flowers streptozotocin (STZ)-induced diabetic rats chemically characterize extracts. Standard flowers, bracts, their were chemical composition determined tentatively by high-performance liquid chromatography coupled diode-array...
Plasmodium vivax is the most prevalent of five species causing malaria in humans. The current available treatment for P. limited and unsatisfactory due to at least two drawbacks: undesirable side effects primaquine (PQ) drug resistance chloroquine. Phenylalanine-alanine-PQ (Phe-Ala-PQ) a PQ prodrug with more favorable pharmacokinetic profile compared PQ. toxicity this was evaluated vitro assays using human hepatoma cell line (HepG2), monkey kidney (BGM), red blood cells deficient enzyme...
ABSTRACT A novel series of furoxan (1,2,5-oxadiazole 2-oxide) (compounds 3, 4a and -b, 13a 14a to -f) benzofuroxan (benzo[c][1,2,5]oxadiazole 1-oxide) 7 8a -c) derivatives were synthesized, characterized, evaluated for in vitro activity against promastigote intracellular amastigote forms Leishmania amazonensis . The exhibited the ability generate nitric oxide at different levels (7.8% 27.4%). derivative was able increase nitrite production medium supernatant from murine macrophages infected...
Abstract Monitoring the plasma concentrations of metformin and sodium‐glucose cotransporter‐2 inhibitors (canagliflozin, dapagliflozin empagliflozin) is essential for pharmacokinetic bioequivalence studies therapeutic monitoring. The present work therefore aimed to develop validate a high‐performance liquid chromatography coupled tandem mass spectrometry (HPLC–MS/MS) method simultaneous quantification these drugs in human plasma. analyses were performed using an Agilent 1200 HPLC system...
For decades guaco species have been empirically used for the treatment of respiratory diseases. However, studies shown that toxic and therapeutic effects main metabolites are dose-dependent, none clinical study was done to evaluate behavior these substances in humans. In this work, a pilot measuring kinetic profile performed leading knowledge an alternative route coumarin metabolism Initial screenings demonstrated administration 60 mL syrup (single dose) did not provide sufficient levels...
Benznidazole (BNZ) is the first-line drug for treatment of Chagas disease. The available in form immediate-release tablets 100-mg (adult) and 12.5-mg (pediatric) doses. administered two or three times daily 60 days. high frequency administrations long period are factors that significantly contribute to abandonment therapy, affecting therapeutic success. Accordingly, this study aimed evaluate preclinical pharmacokinetics BNZ as extended-release (200-mg dose) formulated with different types...
The compound 1-(2,6-dichlorophenyl)indolin-2-one (1), planned as a pro-drug of diclofenac (2), was easily synthesized in 94% yield by an intramolecular reaction the presence coupling agent (i.e., EDC). Compound 1 showed anti-inflammatory and analgesic activity without gastro-ulcerogenic effects. chemical enzymatic hydrolysis profile lactam derivative does not indicate conversion to (2). This is new non-ulcerogenic prototype for treatment chronic inflammatory diseases.
Hydroxymethylnitrofurazone (NFOH) is a trypanocidal prodrug of nitrofurazone (NF), devoid mutagenic toxicity. The purpose this work was to study the chemical conversion NFOH into NF in sodium acetate buffer (pH 1.2 and 7.4) human plasma determine preclinical pharmacokinetic parameters rats. At pH 1.2, totally transformed NF, parent drug, after 48 h, while at 7.4, same period, hydrolysis rate 20%. In plasma, 50% hydrolyzed 24 h. investigation kinetic disposition, concentration drug serum...
Abstract An enantioselective high‐performance liquid chromatographic method for the analysis of carvedilol in plasma and urine was developed validated using (‐)‐menthyl chloroformate (MCF) as a derivatizing reagent. Chloroform used extraction, performed by HPLC on C18 column with fluorescence detector. The quantitation limit 0.25 ng/ml S(−)‐carvedilol 0.5 R(+)‐carvedilol both enantiomers urine. applied to study enantioselectivity pharmacokinetics administered multiple dose regimen (25 mg/12...
Long-term nonsteroidal anti-inflammatory drugs (NSAIDs) therapy has been associated with several adverse effects such as gastric ulceration and cardiovascular events. Among the molecular modifications strategies, prodrug approach is a useful tool to discover new safe NSAIDs. The 1-(2,6-dichlorophenyl)indolin-2-one diclofenac which demonstrated relevant properties without gastro effect. In addition, decreases PGE2 levels, COX-2 expression cellular influx into peritoneal cavity induced by...
Copaiba oleoresin has been used in folk medicine the treatment of bronchitis, syphilis, skin diseases and ulcers due to its anti-inflammatory antiseptic activities, but there is no information about major compounds oral absorption support traditional use. Considering potential copalic (CA) kaurenoic acid (KA) – biological activity (in vitro) diterpenes found oleoresin, this study aimed evaluate intestinal permeability CA KA using Caco-2 cells model as predictive test for drug absorption....
Abstract Benznidazole (BNZ) and nifurtimox are the only drugs available for treating Chagas disease. In this work, we validated a bioanalytical method quantification of BNZ in plasma aimed at improving sensitivity time analysis compared with assays already published. Furthermore, demonstrated application preclinical pharmacokinetic study after administration single oral dose Wistar rats. A Waters® Acquity UHPLC system equipped UV–vis detector was employed. The established using an Acquity®...
The prodrug hydroximethylnitrofurazone (NFOH) presents antichagasic activity with greatly reduced toxicity compared to its drug matrix nitrofurazone (NF). Besides these new characteristics, the was more active against parasite T. cruzi amastigotes. These advantages make a possible therapeutic alternative for treatment of both acute and chronic phase Chagas disease. However, knowledge pharmacokinetic profile is crucial evaluate feasibility drug. In this study, our objective in vivo formation...
Thiazolidinediones (TZDs) are drugs used to treat type 2 diabetes mellitus; however, several safety concerns remain regarding the available in this class. Therefore, search for new TZD candidates is ongoing; metabolism studies play a crucial step development of candidates. Pioglitazone, one most commonly TZDs, and GQ-11, <i>N</i>-substituted TZD, were investigated terms their metabolic activity rat human liver microsomes assess stability investigate metabolites. Methods preparation samples...