The objective of the present research work is to develop a gradient, reversed-phase liquid chromatographic (RP-UPLC) method for the determination of Finasteride in pharmaceutical bulk drugs for assay and its related i...The objective of the present research work is to develop a gradient, reversed-phase liquid chromatographic (RP-UPLC) method for the determination of Finasteride in pharmaceutical bulk drugs for assay and its related impurities. The chromatographic separation was achieved on a Waters ACQUITY UPLC BEH Phenyl Column (150 mm × 2.1 mm, 1.7 μm), The gradient LC method employs solutions A and B as mobile phase. The solution A Contains 2.5 mM ortho phosphoric acid (Buffer) and solution B contains a mixture of acetonitrile and water in the ratio of (90:10 v/v). The flow rate was 0.22 ml/min and the detection wavelength was 210 nm. In the developed UPLC method, the resolution between Finasteride and its potential impurities, namely Imp-1, Imp-2, Imp-3 and Imp-4 was found to be greater than 2.0. The drug was subjected to stress conditions of hydrolysis, oxidation, photolysis and thermal degradation. Considerable degradation was found to occur in alkaline medium and oxidative stress conditions. Degradation product formed during oxidative hydrolysis was found to be Imp-1. The stress samples were assayed against a qualified reference standard and the mass balance was found close to 99.5%. The developed RP-UPLC method was validated with respect to linearity, accuracy, precision and robustness. The limit of quantification of Imp-1, Imp-2, Imp-3 and Imp-4 were 0.06, 0.06, 0.05 and 0.036% (of analyte concentration, i.e. 0.5 mg/ml) with 1μl injection volume. The developed method was found to be linear in the range of 2.5 - 15 μg/mL with correlation coefficient of 0.999 for assay procedures and found to be linear in the range of 0.05 - 3 μg/mL with correlation coefficient of 0.999 for related impurities.展开更多
Objective: To evaluate variations in sexual and erectile function in subjects taking 1 mg of finasteride for androgenetic alopecia by administering the abridged 5-item version of the International Index of Erectile Fu...Objective: To evaluate variations in sexual and erectile function in subjects taking 1 mg of finasteride for androgenetic alopecia by administering the abridged 5-item version of the International Index of Erectile Function (IIEF-5) questionnaire before and during treatment. Design: In a multicenter study, 186 patientswith androgenetic alopeciawere asked to complete the IIEF-5 regarding the domain of erectile function before (at baseline) and 4 to 6 months after beginning finasteride treatment. The test was self-administered. Setting: The study was conducted in 7 institutional dermatology departments in Italy (Bologna, Rome, Genoa, Cagliari, Milan, Florence, and Bari). Patients: A total of 186 patients with androgenetic alopecia were evaluated before and 4 to 6 months after the initiation of finasteride therapy (1 mg). All patients (age range, 19-43 years; mean age, 28.3 years) were followed up as outpatients. Results: The score on each of the 5 domains of the IIEF-5 did not showany significant change after 4 to 6months of treatment. Conclusions: Our results support the clinical impression that sexual side effects are actually much less common than reported in clinical trials. The sexual function of all patients remained stable during treatment with 1 mg of finasteride.展开更多
Screening and confirmation methods of the major urinary metabolite of finasteride–carboxy-finasteride for doping control purpose were developed.Liquid–liquid extraction was adopted for the sample preparation.Analyte...Screening and confirmation methods of the major urinary metabolite of finasteride–carboxy-finasteride for doping control purpose were developed.Liquid–liquid extraction was adopted for the sample preparation.Analytes were detected by positive electrospray ionization in single quadrupole and triple quadrupole mass spectrometer.In the screening method,selected ion monitoring(SIM)mode was used to monitor m/z 403 for carboxy-finasteride.In the confirmation method,product ion mode was used to monitor the precursor ion m/z 403.The limit of detection was below 2 ng/mL for the screening method.Good linearity was obtained in the range 10.0–500.0 ng/mL.The intra-run and inter-run precision calculated from quality control(QC)samples was less than 5.3%.The accuracy as determined from QC samples was within ±6.6%.The screening method was applied for the analysis of excretion samples,allowing the detection of carboxy-finasteride for up to 49 h in urine specimen collected after an oral administration of 5 mg of finasteride.展开更多
Aim: To evaluate possible results with the stimulation use of minoxidil and the strengthening of hair roots with nutritional cyclical supplements, resulting in increased hair regrowth, without the use of anti androgen...Aim: To evaluate possible results with the stimulation use of minoxidil and the strengthening of hair roots with nutritional cyclical supplements, resulting in increased hair regrowth, without the use of anti androgens and enzyme blockers. Methods: This prospective controlled clinical trial compares the current acknowledged form of treatment for hair loss within two controlled groups for both men and women against the use of cyclical nutritional therapy and minoxidil 2%. One hundred patients in each of the 4 groups, a total of 400 patients, were followed for 1 year. The progress was evaluated every 2 months with computerised measurements of hair density, hair calibre, global photography and uniquely designed self-assessment scores. Results: The use of nutritional supplements showed consistent improvements in both treatment groups of men and women against the controlled groups with a correction of hair fall and minimum 18% increased density within 2 months with further improvement to a maximum of 156% over 1 year. Conclusion: Hair loss occurs when weak, sensitive, follicles are affected by multiple causes. Hair regrowth can be achieved consistently and safely by strengthening the hair roots and promoting hair growth without necessarily depending on the use of anti androgens.展开更多
Objective: To explore the effects of aqueous extract from Phthirusa pyrifolia leaves(67 mg/kg body weight for 12 days) on the reproductive function of male Wistar rats through oral administration.Methods: Animals(n = ...Objective: To explore the effects of aqueous extract from Phthirusa pyrifolia leaves(67 mg/kg body weight for 12 days) on the reproductive function of male Wistar rats through oral administration.Methods: Animals(n = 30), aged 13 weeks and weighing(378.5 ± 5.0) g, were housed in a vivarium under controlled environmental conditions [photoperiod of 12 h light/dark,temperature of(23 ± 1)C] and were fed standard rations ad libitum. The experiment ran for 12 days, wherein animals were divided into three groups: negative control(n = 6)received water, positive control(n = 12) with finasteride at a concentration of 1.0 mg/kg;and a test group(n = 12) submitted to aqueous extract. At the end of the experiment, the animals were sacrificed and submitted to analyses.Results: The morphological results of the testes showed that the aqueous extract induced significant changes in the diameter and cross-sectional area of the seminiferous tubules as well as the thickness of the seminiferous epithelium. Furthermore, the extract was able to abruptly decrease testosterone concentrations by about 81.88% in the treated group when compared with the negative control,(47.0 ± 4.8) ng/d L and(255.0 ± 2.0) ng/d L,respectively, and 76.8%,(211.0 ± 8.7) ng/d L, when compared with finasteride. However,the extract causes neither liver damage nor impairment of renal function.Conclusions: These results suggest that the high amounts of flavonoids shown to be in the extract may be responsible for its hepato-protective effects and suggest a possible decrease in the libido and reproduction of rats.展开更多
文摘The objective of the present research work is to develop a gradient, reversed-phase liquid chromatographic (RP-UPLC) method for the determination of Finasteride in pharmaceutical bulk drugs for assay and its related impurities. The chromatographic separation was achieved on a Waters ACQUITY UPLC BEH Phenyl Column (150 mm × 2.1 mm, 1.7 μm), The gradient LC method employs solutions A and B as mobile phase. The solution A Contains 2.5 mM ortho phosphoric acid (Buffer) and solution B contains a mixture of acetonitrile and water in the ratio of (90:10 v/v). The flow rate was 0.22 ml/min and the detection wavelength was 210 nm. In the developed UPLC method, the resolution between Finasteride and its potential impurities, namely Imp-1, Imp-2, Imp-3 and Imp-4 was found to be greater than 2.0. The drug was subjected to stress conditions of hydrolysis, oxidation, photolysis and thermal degradation. Considerable degradation was found to occur in alkaline medium and oxidative stress conditions. Degradation product formed during oxidative hydrolysis was found to be Imp-1. The stress samples were assayed against a qualified reference standard and the mass balance was found close to 99.5%. The developed RP-UPLC method was validated with respect to linearity, accuracy, precision and robustness. The limit of quantification of Imp-1, Imp-2, Imp-3 and Imp-4 were 0.06, 0.06, 0.05 and 0.036% (of analyte concentration, i.e. 0.5 mg/ml) with 1μl injection volume. The developed method was found to be linear in the range of 2.5 - 15 μg/mL with correlation coefficient of 0.999 for assay procedures and found to be linear in the range of 0.05 - 3 μg/mL with correlation coefficient of 0.999 for related impurities.
文摘Objective: To evaluate variations in sexual and erectile function in subjects taking 1 mg of finasteride for androgenetic alopecia by administering the abridged 5-item version of the International Index of Erectile Function (IIEF-5) questionnaire before and during treatment. Design: In a multicenter study, 186 patientswith androgenetic alopeciawere asked to complete the IIEF-5 regarding the domain of erectile function before (at baseline) and 4 to 6 months after beginning finasteride treatment. The test was self-administered. Setting: The study was conducted in 7 institutional dermatology departments in Italy (Bologna, Rome, Genoa, Cagliari, Milan, Florence, and Bari). Patients: A total of 186 patients with androgenetic alopecia were evaluated before and 4 to 6 months after the initiation of finasteride therapy (1 mg). All patients (age range, 19-43 years; mean age, 28.3 years) were followed up as outpatients. Results: The score on each of the 5 domains of the IIEF-5 did not showany significant change after 4 to 6months of treatment. Conclusions: Our results support the clinical impression that sexual side effects are actually much less common than reported in clinical trials. The sexual function of all patients remained stable during treatment with 1 mg of finasteride.
文摘Screening and confirmation methods of the major urinary metabolite of finasteride–carboxy-finasteride for doping control purpose were developed.Liquid–liquid extraction was adopted for the sample preparation.Analytes were detected by positive electrospray ionization in single quadrupole and triple quadrupole mass spectrometer.In the screening method,selected ion monitoring(SIM)mode was used to monitor m/z 403 for carboxy-finasteride.In the confirmation method,product ion mode was used to monitor the precursor ion m/z 403.The limit of detection was below 2 ng/mL for the screening method.Good linearity was obtained in the range 10.0–500.0 ng/mL.The intra-run and inter-run precision calculated from quality control(QC)samples was less than 5.3%.The accuracy as determined from QC samples was within ±6.6%.The screening method was applied for the analysis of excretion samples,allowing the detection of carboxy-finasteride for up to 49 h in urine specimen collected after an oral administration of 5 mg of finasteride.
文摘Aim: To evaluate possible results with the stimulation use of minoxidil and the strengthening of hair roots with nutritional cyclical supplements, resulting in increased hair regrowth, without the use of anti androgens and enzyme blockers. Methods: This prospective controlled clinical trial compares the current acknowledged form of treatment for hair loss within two controlled groups for both men and women against the use of cyclical nutritional therapy and minoxidil 2%. One hundred patients in each of the 4 groups, a total of 400 patients, were followed for 1 year. The progress was evaluated every 2 months with computerised measurements of hair density, hair calibre, global photography and uniquely designed self-assessment scores. Results: The use of nutritional supplements showed consistent improvements in both treatment groups of men and women against the controlled groups with a correction of hair fall and minimum 18% increased density within 2 months with further improvement to a maximum of 156% over 1 year. Conclusion: Hair loss occurs when weak, sensitive, follicles are affected by multiple causes. Hair regrowth can be achieved consistently and safely by strengthening the hair roots and promoting hair growth without necessarily depending on the use of anti androgens.
基金Supported by the National Research Council(CNPq)Foundation for Science and Technology of the State of Pernambuco(FACEPE)Personnel Improvement Coordination-CAPES/PROCAD/NF/no 1415/2007,Brazil
文摘Objective: To explore the effects of aqueous extract from Phthirusa pyrifolia leaves(67 mg/kg body weight for 12 days) on the reproductive function of male Wistar rats through oral administration.Methods: Animals(n = 30), aged 13 weeks and weighing(378.5 ± 5.0) g, were housed in a vivarium under controlled environmental conditions [photoperiod of 12 h light/dark,temperature of(23 ± 1)C] and were fed standard rations ad libitum. The experiment ran for 12 days, wherein animals were divided into three groups: negative control(n = 6)received water, positive control(n = 12) with finasteride at a concentration of 1.0 mg/kg;and a test group(n = 12) submitted to aqueous extract. At the end of the experiment, the animals were sacrificed and submitted to analyses.Results: The morphological results of the testes showed that the aqueous extract induced significant changes in the diameter and cross-sectional area of the seminiferous tubules as well as the thickness of the seminiferous epithelium. Furthermore, the extract was able to abruptly decrease testosterone concentrations by about 81.88% in the treated group when compared with the negative control,(47.0 ± 4.8) ng/d L and(255.0 ± 2.0) ng/d L,respectively, and 76.8%,(211.0 ± 8.7) ng/d L, when compared with finasteride. However,the extract causes neither liver damage nor impairment of renal function.Conclusions: These results suggest that the high amounts of flavonoids shown to be in the extract may be responsible for its hepato-protective effects and suggest a possible decrease in the libido and reproduction of rats.
