RESUMEN
PIP: 3-aza-A-homo steroids have been of interest to these authors in their efforts to develop novel progestational agents. Because it exhibits antifertility activity both in humans and animals, 17alpha-ethynyl-19-nortestosterone (norethindrone) was chosen to undergo molecular modification. The syntheses of a number of oximino and 3-aza-A-homoandrostenes are described in the experimental section of the article. The progestational responses of the compounds were tested through the observation of rabbit uteri. The capacity of a compound to inhibit fertility in rate was noted from the minimum effective dose, i.e., the amount of compound in mg/kg per day which completely suppressed litter production (compound given to both male and female). Because of the suspicion that the oximino steroids were acting postcoitally, 17-beta-acetoxy-19-norandrost-4-en-3-one oxime was studied for its postcoital activity in rats. The postcoital antifertility action of the compound appears to be due to lytic degeneration of zygotes and/or their rapid expulsion from the reproductive tract. Some structure-function observations are made concerning the various compounds.^ieng
Asunto(s)
Androstenos/síntesis química , Anticonceptivos Poscoito/síntesis química , Progestinas/síntesis química , Androstenos/farmacología , Animales , Compuestos Aza/síntesis química , Compuestos Aza/farmacología , Anticonceptivos Poscoito/farmacología , Femenino , Fertilidad/efectos de los fármacos , Homoesteroides/síntesis química , Homoesteroides/farmacología , Noresteroides/síntesis química , Noresteroides/farmacología , Oximas/síntesis química , Oximas/farmacología , Progestinas/farmacología , Conejos , Ratas , Espectrofotometría Ultravioleta , Útero/efectos de los fármacosRESUMEN
A high-pressure liquid chromatographic method is described for analyzing triflubazam [1-methyl-5-phenyl-7-trifluoromethyl-1H-1,5-benzodiazepine-2,4(3H,5H)-dione] and its primary metabolites in blood and urine. Adsorption chromatography, using pellicular silica gel as the stationary phase and dioxane-isooctane as the mobile phase, permitted rapid sample analysis. After extraction of blood and urine samples with toluene, quantitation is achieved using liquid chromatography with an internal standard. The method is sensitive above 50 ng/ml of triflubazam and its known metabolites. Recoveries for all compounds from blood or urine averaged above 95 percent. The specificity of the method was established by collecting samples separated by liquid chromatography and characterizing them by mass spectrometry. Human and animal data are presented to illustrate the utility of the method.
Asunto(s)
Ansiolíticos/análisis , Benzodiazepinas/análisis , Animales , Benzodiazepinas/sangre , Benzodiazepinas/orina , Cromatografía , Perros , Haplorrinos , Humanos , Métodos , Conejos , RatasRESUMEN
A high pressure liquid chromatographic determination of a steroidal oxime in the pharmaceutical dosage form is reported. The reversed phase liquid-liquid partition chromatography employing ODS-Permaphase as support allows thirty to forty individual tablets to be analyzed per hour at a dose level of 50 micrograms to 1 milligram per tablet. The method is simple, rapid, accurate and sensitive.