RESUMEN
A method of determination of sulbaktam in human serum by capillary isotachophoresis with the use of a conductivity detector was worked out. Prior to the proper analysis, a pretreatment of the sample of serum was carried out by extracting sulbaktam to butyl acetate. The total yield of the proposed analytical procedure with an extraction first stage approaches 94%. The smallest determinable amount of the sample corresponds to 1 micrograms of sulbaktam in 1 ml of serum. The reported method was employed to evaluate the samples of sera of volunteers after intravenous administration of the dosage form sulbaktam-ampicillin (VUFB) and the foreign pharmaceutical preparation Unasyn (Pfizer). Statistically insignificant differences in pharmacokinetic parameters have confirmed that the preparations are highly bio-equivalent.
Asunto(s)
Electroforesis/métodos , Sulbactam/sangre , HumanosRESUMEN
A method for the determination of sulphated glycosaminoglycans is based on their precipitation with (1-ethoxycarbonyl)pentadecyltrimethylammonium bromide (Septonex), the excess of which is back-titrated with sodium tetraphenylborate. The titration is monitored by a simple coated-wire ion-selective electrode with a plasticized poly(vinyl chloride) membrane on aluminium wire. Under certain conditions the results are almost independent of the relative molecular mass of glycosaminoglycans. The method has been applied to the determination of the active ingredient in the pharmaceutical preparation, heparon injection.
Asunto(s)
Glicosaminoglicanos/análisis , Aluminio , Autoanálisis/métodos , Secuencia de Carbohidratos , Cationes , Electrodos , Membranas Artificiales , Datos de Secuencia Molecular , Peso Molecular , Potenciometría/instrumentación , Ácidos Sulfúricos/análisisAsunto(s)
Antineoplásicos/metabolismo , Fluorenos/metabolismo , Animales , Humanos , Ratones , Ratas , Porcinos , Porcinos EnanosAsunto(s)
Analgésicos , Quinazolinas/toxicidad , Animales , Femenino , Humanos , Ratones , Quinazolinas/síntesis química , RatasAsunto(s)
Antipsicóticos/metabolismo , Dibenzotiepinas/metabolismo , Animales , Haplorrinos , Humanos , Cinética , Ratas , Ratas EndogámicasRESUMEN
A new potential antiinflammatory substance serves as an example that substantiates the necessity of carrying out concurrent comparative pharmacokinetic and biotransformation studies of new drugs in experimental animals and man during the preclinical research stage, with adherence to all safety precautions. Such a procedure will facilitate the choice of an animal model that approaches human metabolism and pharmacokinetics as closely as possible. This serves in the further development of the test drug, and thus enhances the validity of the transfer of experimental data to man, especially from the toxicological aspect.
Asunto(s)
Efectos Colaterales y Reacciones Adversas Relacionados con Medicamentos , Adulto , Animales , Biotransformación , Embrión de Pollo , Evaluación Preclínica de Medicamentos , Femenino , Humanos , Cinética , Masculino , Preparaciones Farmacéuticas/metabolismo , Fenilacetatos/efectos adversos , Fenilacetatos/metabolismo , Fenilacetatos/toxicidad , Conejos , Ratas , Ratas Endogámicas , Especificidad de la EspecieAsunto(s)
Antineoplásicos/sangre , Fluorenos/sangre , Animales , Perros , Fluorenos/administración & dosificación , Cinética , Ratones , Conejos , RatasRESUMEN
Metabolites of benzofenac (3-chloro-4- benzyloxyphenylacetic acid) were determined in rat, rabbit, dog, and human urine by GC/MS. Before analysis the urine was extracted and the extracts were treated with diazomethane. Deuterium-labelled benzofenac , 3-chloro-4-[( methylene-2H2]- benzolyoxy ) phenylacetic acid was used for the elucidation of the structures of some main metabolites and the determination of trace metabolites. The structures of the metabolites were determined from spectra obtained by electron impact and chemical ionization.
Asunto(s)
Antiinflamatorios/metabolismo , Fenilacetatos/metabolismo , Animales , Perros , Femenino , Cromatografía de Gases y Espectrometría de Masas , Humanos , Masculino , Conejos , RatasRESUMEN
Biological effectiveness of bovine lung heparin and porcine mucosal heparin was tested in vitro and compared with the effectiveness of 12 semisynthetic heparinoids obtained by sulfation of waste heparin mucopolysaccharides and other biomolecules. Equieffective concentrations of these substances were determined in the sense of prolongation of the thrombin time and the APTT, inhibition of the thrombin- and collagen-induced aggregation, and potentiation of the primary ADP-induced aggregation. The influence of sulfation was proved on the biological effectiveness as well as the significance of the proper choice of the parent structure. Some polycondensates of the polysaccharide type were effective altogether with the sulfated waste heparin mucopolysaccharides. On the contrary, protein structures and low molecular weight glycosides exhibited little or no activity. The effective substances were related to heparin not only by the anticoagulant activity but also by the inhibitory action on the thrombin- and collagen-induced platelet aggregation. Contrary to heparin, higher concentrations of the studied heparinoids strongly potentiated the ADP-induced aggregation response. Strong inhibition of the collagen-induced aggregation was proved after administration of heparin to patients with end-stage renal failure on days without haemodialysis. Less significant changes in the secondary aggregation were observed also after administration of S-heparin (one of the studied heparinoids) to volunteers in the form of the rectal suppositories.