Erectile dysfunction （ED） is a major complication of diabetes mellitus （DM）. This study investigates the relationship between ED and the downregulation of constitutive nitric oxide synthase （cNOS） in the corpus ...Erectile dysfunction （ED） is a major complication of diabetes mellitus （DM）. This study investigates the relationship between ED and the downregulation of constitutive nitric oxide synthase （cNOS） in the corpus cavernosum （CC） of diabetic rats. It also examines the effects of udenafil, a phosphodiesterase type 5 （PDE5） inhibitor, on ED and cNOS expression levels. After 16 weeks of daily oral treatment with udenafil in diabetic rats, the intracavernous pressure/mean arterial pressure （ICP/MAP） ratio was recorded to measure erectile function, and cNOS expression was measured using reverse transcriptase （RT）-PCR and immunoblots. Although the ICP/ MAP ratio and the expression levels of endothelial NOS （eNOS） and neuronal NOS （nNOS） in the CC were markedly decreased in diabetic rats, long-term udenafil treatment improved the erectile function and increased cNOS expression compared with diabetic controls. These findings suggest that ED in DM is closely related to decreased cNOS expression in the CC and that udenafil has the ability to compensate for this pathological change by modulating cNOS expression. Udenafil also has an inhibitory role in cyclic guanosine monophosphate （cGMP） degradation.展开更多
We compared the efficacy and safety between once-daily dosing and on-demand use of udenafil for type 2 diabetic patients with erectile dysfunction （ED）. A multi-center, randomized, open-label, parallel-group, 12-wee...We compared the efficacy and safety between once-daily dosing and on-demand use of udenafil for type 2 diabetic patients with erectile dysfunction （ED）. A multi-center, randomized, open-label, parallel-group, 12-week study was conducted. 161 patients who improved with on-demand 200 mg of udenafil according to Sexual Encounter Profile （SEP） diary Question 2 and 3 （Q2 and Q3） were randomized into 200 mg on-demand （n = 80） or 50 mg once-daily （n = 81） dosing groups for 8 weeks. The dosing period was followed by a 4-week treatment-free period. The primary efficacy endpoint was the change of the International Index of Erectile Function （IIEF） erectile function domain （EFD） score. The secondary efficacy endpoints included changes to the SEP diary Q2, Q3, IIEF Q3, Q4, other domains of IIEF, Global Assessment Question, and shift to the normal rate （EFD 〉 26）. Vascular endothelial markers were also assessed. The IIEF-EFD score of both groups improved after 8 weeks of treatment （P 〈 0.0001）. There was no statistically significant difference between two groups. Improvement was not maintained after the treatment-free follow-up period. Similar results were observed in the secondary efficacy endpoints. There was also no significant difference in vascular endothelial markers. Daily udenafil was well-tolerated, and there was no significant difference in the adverse drug reactions and adverse events between the two groups. Flushing and headache were the most frequent adverse events. Both regimens improved ED in diabetic patients and were well-tolerated. Further studies are needed to assess the effect of daily udenafil treatment in diabetic patients.展开更多
目的:建立一种超高效液相色谱串联质谱法(Ultra Performance Liquid Chromatography Tandem Mass Spectrometry,UPLC-MS)法测定保健食品中非法添加乌地那非、氯地那非含量的检测方法。方法:色谱柱为Agilent ZORBX Eclipse Plus C_(18)柱...目的:建立一种超高效液相色谱串联质谱法(Ultra Performance Liquid Chromatography Tandem Mass Spectrometry,UPLC-MS)法测定保健食品中非法添加乌地那非、氯地那非含量的检测方法。方法:色谱柱为Agilent ZORBX Eclipse Plus C_(18)柱(50 mm×2.1 mm,1.8μm),以0.1%甲酸水溶液-乙腈(65∶35)为流动相梯度洗脱,流速0.2 mL·min^(-1),柱温35℃;采用电喷雾离子源正模式多反应监测模式,外标法定量。结果:溶剂空白无干扰,乌地那非、氯地那非在10~200 ng·mL^(-1)时线性关系良好,相关系数分别为0.9990和0.9997;乌地那非的平均回收率为90.0%~104.3%,相对标准偏差为0.2%~3.8%;氯地那非的平均回收率为92.3%~105.8%,相对标准偏差为0.3%~2.2%;两者方法检出限、定量限分别为25μg·kg^(-1)和50μg·kg^(-1)。结论:建立的方法准确、灵敏、专属性强,适用于保健食品中非法添加乌地那非、氯地那非的痕量分析。展开更多
文摘Erectile dysfunction （ED） is a major complication of diabetes mellitus （DM）. This study investigates the relationship between ED and the downregulation of constitutive nitric oxide synthase （cNOS） in the corpus cavernosum （CC） of diabetic rats. It also examines the effects of udenafil, a phosphodiesterase type 5 （PDE5） inhibitor, on ED and cNOS expression levels. After 16 weeks of daily oral treatment with udenafil in diabetic rats, the intracavernous pressure/mean arterial pressure （ICP/MAP） ratio was recorded to measure erectile function, and cNOS expression was measured using reverse transcriptase （RT）-PCR and immunoblots. Although the ICP/ MAP ratio and the expression levels of endothelial NOS （eNOS） and neuronal NOS （nNOS） in the CC were markedly decreased in diabetic rats, long-term udenafil treatment improved the erectile function and increased cNOS expression compared with diabetic controls. These findings suggest that ED in DM is closely related to decreased cNOS expression in the CC and that udenafil has the ability to compensate for this pathological change by modulating cNOS expression. Udenafil also has an inhibitory role in cyclic guanosine monophosphate （cGMP） degradation.
文摘We compared the efficacy and safety between once-daily dosing and on-demand use of udenafil for type 2 diabetic patients with erectile dysfunction （ED）. A multi-center, randomized, open-label, parallel-group, 12-week study was conducted. 161 patients who improved with on-demand 200 mg of udenafil according to Sexual Encounter Profile （SEP） diary Question 2 and 3 （Q2 and Q3） were randomized into 200 mg on-demand （n = 80） or 50 mg once-daily （n = 81） dosing groups for 8 weeks. The dosing period was followed by a 4-week treatment-free period. The primary efficacy endpoint was the change of the International Index of Erectile Function （IIEF） erectile function domain （EFD） score. The secondary efficacy endpoints included changes to the SEP diary Q2, Q3, IIEF Q3, Q4, other domains of IIEF, Global Assessment Question, and shift to the normal rate （EFD 〉 26）. Vascular endothelial markers were also assessed. The IIEF-EFD score of both groups improved after 8 weeks of treatment （P 〈 0.0001）. There was no statistically significant difference between two groups. Improvement was not maintained after the treatment-free follow-up period. Similar results were observed in the secondary efficacy endpoints. There was also no significant difference in vascular endothelial markers. Daily udenafil was well-tolerated, and there was no significant difference in the adverse drug reactions and adverse events between the two groups. Flushing and headache were the most frequent adverse events. Both regimens improved ED in diabetic patients and were well-tolerated. Further studies are needed to assess the effect of daily udenafil treatment in diabetic patients.
文摘目的:建立一种超高效液相色谱串联质谱法(Ultra Performance Liquid Chromatography Tandem Mass Spectrometry,UPLC-MS)法测定保健食品中非法添加乌地那非、氯地那非含量的检测方法。方法:色谱柱为Agilent ZORBX Eclipse Plus C_(18)柱(50 mm×2.1 mm,1.8μm),以0.1%甲酸水溶液-乙腈(65∶35)为流动相梯度洗脱,流速0.2 mL·min^(-1),柱温35℃;采用电喷雾离子源正模式多反应监测模式,外标法定量。结果:溶剂空白无干扰,乌地那非、氯地那非在10~200 ng·mL^(-1)时线性关系良好,相关系数分别为0.9990和0.9997;乌地那非的平均回收率为90.0%~104.3%,相对标准偏差为0.2%~3.8%;氯地那非的平均回收率为92.3%~105.8%,相对标准偏差为0.3%~2.2%;两者方法检出限、定量限分别为25μg·kg^(-1)和50μg·kg^(-1)。结论:建立的方法准确、灵敏、专属性强,适用于保健食品中非法添加乌地那非、氯地那非的痕量分析。
