更新于：2024-12-06
Tandospirone Citrate
枸橼酸坦度螺酮
更新于：2024-12-06
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C27H37N5O9 |
InChIKeyDMLGUJHNIWGCKM-DPFKZJTMSA-N |
CAS号112457-95-1 |
关联
33
项与 枸橼酸坦度螺酮 相关的临床试验枸橼酸坦度螺酮片在健康受试者中随机、开放、两制剂、两序列、四周期、单次给药、完全重复交叉设计空腹和高脂餐后状态下生物等效性试验
枸橼酸坦度螺酮片在中国健康人群中空腹和餐后状态下单次给药的人体生物等效性临床试验
枸橼酸坦度螺酮片在健康受试者中单中心、开放、随机、单剂量、两制剂、两序列、四周期、完全重复空腹状态下的生物等效性试验
100 项与 枸橼酸坦度螺酮 相关的临床结果
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100 项与 枸橼酸坦度螺酮 相关的转化医学
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100 项与 枸橼酸坦度螺酮 相关的专利（医药）
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260
项与 枸橼酸坦度螺酮 相关的文献（医药）2024-12-01EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
Deep eutectic solvent combined with permeation enhancer strategy to convert tandospirone from oral to transdermal formulations improving drug bioavailability
Article
作者: Liu, Chao ; Zhang, Yang ; Fang, Liang ; Gong, Kaihua ; Li, Hui ; Sun, Peng ; Cai, Yu
Tandospirone(Tan) is a commonly used drug for anxiety treatment. However, it has a significant first-pass effect and needs to be taken three times a day. To increase the bioavailability of the drug and reduce the number of administrations, this work amid to prepare a Tan patch that can be administered once a day by using the strategy of therapeutic deep eutectic solvent(THEDES) in cooperation with chemical permeation enhancer(CPE). In this study, four organic acids and five permeation enhancers were selected, and the optimized formulation was obtained by single-factor investigation and Box-Behnken design. The optimized formulation could significantly enhance drug loading by 2.5-fold and skin permeation up to 586.6 ± 17 μg/cm2 in rats. Based on pharmacokinetic results, compared to oral administration, the drug exhibited a substantially elevated bioavailability, registering a 17-fold increase(from 3.01 % to 52.17 %), alongside a 10-fold rise in the mean residence time(MRT). Meanwhile, the patch was not irritating. The results of the mechanistic study showed that levulinic acid(LeA) acted as a bridge to increase the interaction between the Tan and the matrix and inhibited the crystallization of the drug in the patch, and THEDES together with CPE improved the matrix fluidity and skin permeability. This study provides a reference for the joint application of THEDES and CPEs in patch development.
2024-04-01Neurobiology of disease
Neonatal hypoxia impairs serotonin release and cognitive functions in adult mice
Article
作者: Moquin, Luc ; Rosa-Neto, Pedro ; Amilhon, Bénédicte ; Lee, Karen Ka Yan ; Di Cristo, Graziella ; Chattopadhyaya, Bidisha ; do Nascimento, Antônia Samia Fernandes
Children who experienced moderate perinatal asphyxia (MPA) are at risk of developing long lasting subtle cognitive and behavioral deficits, including learning disabilities and emotional problems. The prefrontal cortex (PFC) regulates cognitive flexibility and emotional behavior. Neurons that release serotonin (5-HT) project to the PFC, and compounds modulating 5-HT activity influence emotion and cognition. Whether 5-HT dysregulations contribute to MPA-induced cognitive problems is unknown. We established a MPA mouse model, which displays recognition and spatial memory impairments and dysfunctional cognitive flexibility. We found that 5-HT expression levels, quantified by immunohistochemistry, and 5-HT release, quantified by in vivo microdialysis in awake mice, are reduced in PFC of adult MPA mice. MPA mice also show impaired body temperature regulation following injection of the 5-HT1A receptor agonist 8-OH-DPAT, suggesting the presence of deficits in 5-HT auto-receptor function on raphe neurons. Finally, chronic treatment of adult MPA mice with fluoxetine, an inhibitor of 5-HT reuptake transporter, or the 5-HT1A receptor agonist tandospirone rescues cognitive flexibility and memory impairments. All together, these data demonstrate that the development of 5-HT system function is vulnerable to moderate perinatal asphyxia. 5-HT hypofunction might in turn contribute to long-term cognitive impairment in adulthood, indicating a potential target for pharmacological therapies.
2024-03-01CNS neuroscience & therapeutics
Efficacy and safety of venlafaxine hydrochloride combined with tandospirone citrate for patients with vascular depression accompanied by somatic symptoms: An open‐labeled randomized control trial
Article
作者: Liu, Nan ; Chen, Ronghua ; Zeng, Guiying ; Chen, Hongbin ; Zhao, Zijun ; Xiao, Yingchun ; Wu, Weiwei ; Lin, Yongsen ; Lin, Qianwen ; Chen, Xinyan ; Chen, Hui ; Wu, Shufang ; Lin, Ting
Abstract:
Aims:
To explore the pharmacological treatment of vascular depression (VaDep) and whether the blood levels of neurotransmitters can reflect the VaDep severity.
Methods:
VaDep patients with somatic symptoms were enrolled and randomly received venlafaxine + tandospirone (Combined Group) or venlafaxine (Monotherapy Group). The treatment efficacy was assessed by Hamilton Depression Scale (HAMD), Hamilton Anxiety Scale (HAMA), and Patient Health Questionnaire‐15 (PHQ‐15). The levels of blood monoamine neurotransmitters were measured by enzyme‐linked immunosorbent assay.
Results:
Both groups reported a progressive decrease in HAMD, HAMA, and PHQ‐15 scores to below the baseline after the respective treatment. Compared with the Monotherapy Group, the Combined Group reported a significant decrease in HAMD score at week 2 and markedly lower HAMA and PHQ‐15 scores at weeks 1, 2, 4, and 8. Both groups showed a decrease in the levels of blood monoamine neurotransmitters at weeks 4 and 8 when compared with the baseline. A strong positive association was evident between the plasma 5‐HT levels and the HAMD score.
Conclusion:
The combined therapy rapidly acts on VaDep comorbid with anxiety and somatic symptoms and significantly alleviates the anxiety and somatic symptoms. The plasma levels of 5‐HT may serve as potential objective candidates in evaluating VaDep severity and the efficacy of the undertaken treatment regimen.
100 项与 枸橼酸坦度螺酮 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 焦虑症 | 中国 | 2003-05-21 | |
| 神经症性障碍 | 日本 | 1996-07-10 | |
| 心理生理性障碍 | 日本 | 1996-07-10 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 年龄相关性黄斑变性 | 临床3期 | - | 2009-04-01 | |
| 地图样萎缩 | 临床3期 | - | 2009-04-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 274 | High-dose tandospirone (60 mg/d) | 範餘顧廠製願鹹襯鏇範(鬱衊齋襯窪鹹醖衊夢鏇) = 鏇網廠壓築憲壓鹽簾蓋 鬱鏇淵簾構餘齋簾願鏇 (製夢夢築獵壓餘廠膚鹽 ) 更多 | - | 2023-02-26 | ||
Low-dose tandospirone (30 mg/d) | 範餘顧廠製願鹹襯鏇範(鬱衊齋襯窪鹹醖衊夢鏇) = 夢窪壓憲觸構餘憲憲糧 鬱鏇淵簾構餘齋簾願鏇 (製夢夢築獵壓餘廠膚鹽 ) 更多 | ||||||
临床4期 | 274 | (醖鹽鬱鬱顧憲衊襯鬱襯) = 淵鏇範觸顧壓選繭鹽糧 糧獵鑰壓艱鹹艱築憲積 (鑰願簾構窪艱襯簾醖鏇 ) | - | 2022-08-01 | |||
(醖鹽鬱鬱顧憲衊襯鬱襯) = 齋範膚網膚窪網衊繭糧 糧獵鑰壓艱鹹艱築憲積 (鑰願簾構窪艱襯簾醖鏇 ) | |||||||
临床3期 | 772 | (AL-8309B 1.0%) | 襯蓋齋選範網夢鏇鑰積(簾顧齋餘壓襯簾鏇遞鹹) = 構鏇衊簾壓繭淵鬱衊餘 遞膚範鏇衊醖鏇築艱壓 (夢網遞淵顧膚壓窪膚淵, 繭製製齋鹽壓願鑰鑰顧 ~ 繭窪繭構網醖鑰網願製) 更多 | - | 2014-07-03 | ||
(AL-8309B 1.75%) | 襯蓋齋選範網夢鏇鑰積(簾顧齋餘壓襯簾鏇遞鹹) = 壓簾艱鹹鏇齋餘簾遞蓋 遞膚範鏇衊醖鏇築艱壓 (夢網遞淵顧膚壓窪膚淵, 範願範鹽築衊憲繭壓蓋 ~ 窪淵遞鬱鹽膚淵糧鬱壓) 更多 |
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