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1.
Bioanalysis ; 12(24): 1711-1724, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33275040

RESUMO

Aim: Develop and validate a method of solid-phase microextraction (SPME) and liquid chromatography to investigate three major polycyclic aromatic hydrocarbons (PAHs) in oral fluid. Results/Methodology: The extraction phase was exposed to 1.5 ml of diluted oral fluid under stirring at 1000 rpm for 60 min, at 70°C. Then, it was immersed in 200 µl of acetonitrile for 10 min at 25°C for desorption of the analytes. Linearity, absolute recovery, and inter- and intra-assay relative standard deviations and relative errors were 50-300 ng.ml-1, ≥24% and ≤15% for all analytes, respectively. A full factorial design was used to SPME optimization. Discussion/Conclusion: The method is suitable for the exploratory analysis of some PAHs in the oral fluid of crack smokers.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Fumar Cocaína/metabolismo , Microextração em Fase Sólida/métodos , Adolescente , Adulto , Humanos , Pessoa de Meia-Idade , Hidrocarbonetos Policíclicos Aromáticos , Adulto Jovem
2.
Eur J Pharm Sci ; 136: 104937, 2019 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-31128208

RESUMO

Thalidomide (TLD) is used to treat erythema nodosum leprosum (ENL), multiple myeloma, aphthous ulceration and wasting syndrome in HIV patients. The API can be found in two crystalline habits known as α-TLD and ß-TLD. The saturation solubility (Cs) and the dissolution profiles under non-sink and sink conditions of both polymorphs were assessed. In addition, mini-capsules containing α-TLD or ß-TLD without excipients were orally given (10 mg/kg) to Wistar rats. An intravenous (i.v.) dose was also administrated (5 mg/kg). The Cs values for α-TLD and ß-TLD were not significantly different (α = 56.2 ±â€¯0.5 µg·mL-1; ß = 55.2 ±â€¯0.2 µg·mL-1). However, the dissolution profile of α-TLD presented the fastest rate and the largest extension of drug dissolution than that from ß-TLD (80% in 4 h versus 55% in 4 h). The α-TLD provided a more favorable pharmacokinetic than the ß-TLD (maximum plasma concentration - Cmax: 5.4 ±â€¯0.90 µg·mL-1versus 2.6 ±â€¯0.2 µg·mL-1; area under the curve of the concentration-time profile from time zero to infinity - AUC0-∞: 44.3 ±â€¯8.8 µg·h·mL-1versus 33.9 ±â€¯4.7 µg·h·mL-1; absolute bioavailability - F: 92.2 ±â€¯18.5% versus 70.5 ±â€¯9.9%, respectively). Drug suppliers and pharmaceutical companies should strictly control the technological processes involved in the TLD API synthesis as well as in the production of the pharmaceutical dosage form in order to guarantee the inter-batch homogeneity and therefore, product compliance.


Assuntos
Talidomida/química , Talidomida/farmacocinética , Animais , Área Sob a Curva , Disponibilidade Biológica , Cápsulas/química , Cápsulas/farmacocinética , Liberação Controlada de Fármacos/efeitos dos fármacos , Excipientes/química , Infecções por HIV/tratamento farmacológico , Infecções por HIV/metabolismo , Masculino , Ratos , Ratos Wistar , Solubilidade/efeitos dos fármacos
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