ABSTRACT
Fluorescence enhancement reaction of flavoxate hydrochloride (FX) in strong alkali solution was studied, the mechanism of the reaction was investigated, and a novel fluorimetric method for analysis of FX in drug sample was established. FX has no intrinsic fluorescence, but it can slowly produce fluorescence in strong alkali solution. Heating can promote the fluorescence enhancement reaction. In 3D fluorescence spectra of the decomposition product of FX, two fluorescence peaks, located respectively at excitation wavelengths λex/ emission wavelength λem =223/410 nm, and 302/410 nm, were observed. Using quinine sulfate as a reference, fluorescence quantum yield of the decomposition product was measured to be 0.50. The structural characteriza- tion and spectral analysis of the decomposition product reveal that ester bond hydrolysis reaction of FX is firstly occurred during heating process, forming 3-methylflavone-8-carboxylic acid (MFA), then a cleavage reaction of the γ-pyrone ring of MFA occurred, producing α, β-unsaturated ketone. This product includes adjacent hydroxyl benzoic acid group in its molecule, which can form intramolecular hydrogen bond under alkaline condition, so that increase the conjugate degree and enhance the rigidity of the molecule, and thereby cause fluorescence enhancement. Based on this fluorescence enhancement reaction, a fluorimetric method was proposed for the determination of FX. A linear calibration curve covered the concentration range 0.020 3-0.487 µg · mL. The regression equation was I(F) = 23.9 + 5357.3 c, with correlation coefficient r = 0.999 7 (n = 8), detection limit D = 1.1 ng · mL(-1). The method was applied to the analysis of FX tablets, with a spiked recovery rate of 100.2%. The reliability of the method was verified by a UV-spectrophotometric method.
Subject(s)
Alkalies , Calibration , Chemistry, Pharmaceutical , Flavoxate , Chemistry , Fluorescence , Limit of Detection , Reproducibility of Results , Solutions , TabletsABSTRACT
<p><b>OBJECTIVE</b>The National Institutes of Health (NIH) category IIIa chronic prostatitis syndromes (non bacterial chronic prostatitis) were common disorders but with few effective therapies. Alpha-blockers and bioflavonoids had recently been reported in randomized controlled trials to improve the symptom of these disorders in a significant proportion of men. The aim of this study was to confirm these findings in a prospective randomized, placebo-controlled trial.</p><p><b>METHODS</b>Forty-five men with category IIIa chronic non bacterial protatitis were randomized into three groups as follows: (1) placebo; (2) phenoxybenzamine-hydrochloride:10 mg two times a day for one month; (3) flavoxate HCI-neptumus: 200 mg three times a day for one month. The NIH chronic prostatitis symptom score was used to grade symptoms at the beginning and conclusion of the study.</p><p><b>RESULTS</b>All the patients in three groups completed the study except three dropout patients in placebo group because of sever symptoms. The three groups were similar in age, duration of symptoms and initial symptom score. Patients taking placebo had a mean improvement in NIH-CPSI from 21.85 to 19.55 (not significant), while the phenoxybenzamine-hydrochloride group had a mean improvement from 21.95 to 13.75 (P < 0.01), and those taking flavoxate HCI-neptumus had a mean improvement from 21.75 to 16.95 (P < 0.05). The decrease in NIH-CPSI was associated with significant improvement in patients' clinical manifestations.</p><p><b>CONCLUSION</b>Therapy with alpha-blockers was well tolerated with significant symptomatic improvement in most men having chronic non-bacterial chronic protatitis while the bioflavonoids group had no significant improvement. Mechanism of both medicines needs further study.</p>
Subject(s)
Adult , Humans , Male , Adrenergic alpha-Antagonists , Therapeutic Uses , Chronic Disease , Flavonoids , Therapeutic Uses , Flavoxate , Therapeutic Uses , Parasympatholytics , Therapeutic Uses , Prospective Studies , Prostatitis , Drug Therapy , Treatment OutcomeABSTRACT
Para el tratamiento de la urgencia y de la incontinencia por inestabilidad del detrusor, se han utilizado innumerables medicamentos. Los más usados han sido drogas anticolinérgicas (p.e. oxibutinina, propantelina, imipramina, bloqueantes alfa androenérgicos) que desafortunadamente tienen una alta incidencia de efectos secundarios que no son tolerados por los pacientes. El flavoxate, un derivado flavónico, ha demostrado sin embargo, ejercer una actividad selectiva y directa sobre el músculo liso del tracto urinario inferior sin efectos atropínicos secundarios. En el presente estudio se comparó la eficacia y la tolerancia del Flavoxate contra Placebo en el tratamiento de pacientes con diagnóstico de incontinencia urinaria por detrusor inestable. Fueron seleccionadas 25 pacientes en la consulta externa de urología del Hospital General del Este Dr. "Domingo Luciani" de las cuales 5 recibieron el Flavoxate y 10 Placebo, evidenciándose una respuesta efectiva, segura y con muy leves efectos secundarios indeseables a dosis de 1.200 mgr v.o/día con Flavoxate, razones por lo cual lo recomendamos como tratamiento de elección en el síndrome de incontinencia y de urgencia miccional por inestabilidad del detrusor.
Subject(s)
Adult , Middle Aged , Humans , Female , Placebos/therapeutic use , Urinary Incontinence/therapy , Flavoxate/therapeutic useABSTRACT
Foram avaliadas 24 pacientes com história de perdas urinárias aos esforços acompanhadas de urgência miccional. Efetuou-se estudo duplo cego com uso de placebo e flavoxato, tendo sido realizadas, antes e após cada droga, avaliaçöes radiológicas, urodinâmicas, laboratoriais e clínicas. Alta incidência de contraçöes vesicais näo inibidas (CNI) foi observada neste grupo, sendo preconizada avaliaçäo urodinâmica de rotina quando a paciente se queixa de incontinência de esforço com urgência miccional. Quinze pacientes completaram o protocolo, das quais 10 referiram melhora da sintomatologia, com uso de flavoxato. Nas 10 pacientes que apresentaram contraçöes vesicais näo inibidas na avaliaçäo urodinâmica inicial ou com uso de placebo, somente 4 as apresentaram com o emprego da droga, correspondendo a 60% de resposta à medicaçäo