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1.
Eur J Pharm Sci ; 133: 137-144, 2019 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-30946963

RESUMO

INTRODUCTION: Many factors can affect dry powder inhalers' (DPIs) aerosol emission and lung deposition. The fluctuation of environmental temperature and relative humidity (RH) that inhalers experience in realistic daily use has not been extensively evaluated. This work aimed to evaluate the delivered dose (DD) and aerodynamic particle size distribution (APSD) of tiotropium Handihaler DPI (H) after exposure to patients' real-life use environments. METHODS: Ethical approval was obtained to enrol adult patients already using H. Patients who gave written consent were given new H to use and HygroLog temperature and RH data loggers to keep in the vicinity of the given inhaler. The H and HygroLog were returned after 2 weeks. Patient recruitment was done during the summer (HS) and winter (HW). As control, other HC were stored as per the leaflet storage instructions. The Next Generation Impactor was used to evaluate the inhalers. RESULTS: The HC were stored under an average of 21.0 °C and 46.9% RH. The patients' HS and HW lived in an average (range) temperature (°C) 23.2 (18.3-38.2) and 17.8 (13.5-24.6), respectively, and RH 50.8% (24.3-65.3%) and 50.4% (30.6-72.4%), respectively. All H groups had comparable environments (p > 0.05). The HC, HS and HW gave similar tiotropium DD (µg) 7.60, 8.01 and 7.61, respectively (p > 0.05). Moreover, the fine particle dose µg (median diameter (µm)) were HC 2.41 (3.84), HS 2.55 (3.81) and HW 2.37 (3.83) (p > 0.05). CONCLUSIONS: The aerosol emission behaviour of tiotropium Handihaler was tolerant to real-life retention environments of patients in Amman, Jordan.


Assuntos
Broncodilatadores , Inaladores de Pó Seco , Umidade , Temperatura , Brometo de Tiotrópio , Administração por Inalação , Adulto , Aerossóis , Broncodilatadores/administração & dosagem , Broncodilatadores/química , Armazenamento de Medicamentos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Tamanho da Partícula , Brometo de Tiotrópio/administração & dosagem , Brometo de Tiotrópio/química
2.
J Nutr Metab ; 2012: 802924, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-23150812

RESUMO

Fasting and caloric restriction have been associated with reduced incidence of chronic diseases and cancers. These effects have been attributed to reduced oxidative stress. Since Ramadan intermittent fasting (RIF) has been associated with reduced caloric intake, it was hypothesized that RIF would alleviate oxidative stress in healthy volunteers. The study was designed to elucidate the impact of RIF on oxidative stress measured by 15-F(2t)-Isoprostane (15FIP). Fifty healthy subjects (23 men and 27 women) who intended to fast Ramadan were recruited. Urine and serum sampling and anthropometric and dietary assessments were conducted one week before Ramadan (T0), at the end of the third week of Ramadan (T1), and one month after Ramadan (T2). Biochemical measurements included urinary 15FIP, creatinine, and hematological indices. Results revealed that the urinary level of 15FIP measured at T0 was normal, while they showed a significantly (P < 0.05) higher level when measured at T1 concomitant with a significant (P < 0.05) increase in the body weight and total body fat percent. In conclusion, results suggest that increased body weight is associated with increased lipid peroxidation and oxidative stress, and the impact of RIF on oxidative stress is mediated by the changes in body weight at the end of the month.

3.
Biol Pharm Bull ; 32(4): 640-5, 2009 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-19336898

RESUMO

The structural similarity between papaverine and berberine, a known inhibitor of human protein tyrosine phosphatase 1B (h-PTP 1B), prompted us to investigate the potential of papaverine as h-PTP 1B inhibitor. The investigation included simulated docking experiments to fit papaverine into the binding pocket of h-PTP 1B. Papaverine was found to readily dock within the binding pocket of h-PTP 1B in a low energy orientation via an optimal set of attractive interactions. Experimentally, papaverine illustrated potent in vitro inhibitory effect against recombinant h-PTP 1B (IC(50)=1.20 microM). In vivo, papaverine significantly decreased fasting blood glucose level of Balb/c mice. Our findings should encourage screening of other natural alkaloids for possible anti-h-PTP 1B activities.


Assuntos
Papaverina/farmacologia , Inibidores de Fosfodiesterase/farmacologia , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores , Proteína Tirosina Fosfatase não Receptora Tipo 1/química , Animais , Glicemia/metabolismo , Simulação por Computador , Relação Dose-Resposta a Droga , Humanos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Modelos Moleculares , Papaverina/sangue , Inibidores de Fosfodiesterase/sangue , Software
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