RESUMO
The bioavailability (plasma concentrations, AUC) of a rectal formulation (suppository) of naproxen was investigated in six healthy volunteers by comparison with an oral preparation (tablets). Plasma half-lives after both formulations were identical 10 hr 15 min+/-25 min (S.D.). Determined by the AUC the bioavailability of naproxen in the suppositories was 94.8%+/-6.3% of the bioavailability of naproxen in the tablets. This paper describes also a new gas-liquid chromatographic method for determining unchanged naproxen in human plasma which is quick, sensitive, and specific.
Assuntos
Ácidos Naftalenoacéticos/sangue , Naproxeno/sangue , Administração Oral , Adulto , Disponibilidade Biológica , Cromatografia Gasosa , Feminino , Meia-Vida , Humanos , Cinética , Masculino , Naproxeno/administração & dosagem , Supositórios , Fatores de TempoRESUMO
A gas-liquid chromatographic method is described for the determination of tienilic acid (SKF 62.698), a diuretic with uricosuric properties, in human plasma and urine. The method, which is based on the methylation of the compound, is rapid, specific and sensitive. The lowest level accurately determined is about 50 ng/ml in plasma and 1 mug/ml in urine. The first results from a human volunteer are given.
Assuntos
Cromatografia Gasosa , Diuréticos/análise , Glicolatos/análise , Fenoxiacetatos/análise , Tiofenos/análise , Cromatografia Líquida , Diuréticos/sangue , Diuréticos/urina , Humanos , Métodos , Metilação , Fenoxiacetatos/sangue , Fenoxiacetatos/urina , Tiofenos/sangue , Tiofenos/urina , Uricosúricos/sangue , Uricosúricos/urinaRESUMO
The pharmacokinetics of practolol were studied after intravenous injection (5 mg/kg) in conscious normal rabbits and rabbits with experimental glomerulonephritis induced by daily intravenous injection of bovine gamma-globulin. The results obtained demonstrated that the practolol elimination was impaired in animals with experimental glomerulonephritis: significant lengthening of the half-life of the beta-phase, with marked decrease of the body clearance and diminution of the drug concentration decrease in plasma. Neither conjugates nor deacetylpractolol could be detected in the urine of the controls or immunized rabbits.
Assuntos
Glomerulonefrite/metabolismo , Practolol/metabolismo , Animais , Nitrogênio da Ureia Sanguínea , Creatinina/sangue , Feminino , Glomerulonefrite/induzido quimicamente , Meia-Vida , Masculino , Taxa de Depuração Metabólica/efeitos dos fármacos , Practolol/sangue , Practolol/farmacologia , CoelhosRESUMO
A gas-liquid chromatographic method is described for rapid, quantitative determination of adipate content of acetylated di-starch adipate. The adipate group is very labile and, under mild alkaline conditions at ambient temperature, is easily hydrolyzed from the starch. Free adipic acid is formed by acidification of the solution with HCl, and then extracted with ethyl acetate. Ethyl acetate is removed under vacuum distillation, and a silyl derivative of the adipic acid is formed. Glutaric acid internal standard is introduced into the original starch sample before hydrolysis. An aliquot of the silylated solution is injected into a gas chromatograph fitted with a column having silicone oil as the active phase. A flame ionization detector is also incorporated. Results correlate well the amount of adipylating reagent used. No adipic acid is detectable when a hydrolyzed, extracted sample of acetylated di-starch adipate is subjected to a second extraction. Recovery levels of adipic acid, from starches fortified with 100-500 ppm, are in the range of 97-102.5%.