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tacrine hydrochloride
相关语句
  盐酸他克林
     Determination of Tacrine Hydrochloride Content in Suppositories by Ultraviolet Spectrophotometry
     紫外分光光度法测定盐酸他克林栓的含量
短句来源
     Aim To synthesize acylated prodrug of tacrine hydrochloride (THA) to improve the infiltration ability across the blood brain barrier (BBB).
     目的 制备盐酸他克林 (THA)的酰化前体药物以提高其透过血脑屏障 (BBB)的能力。
短句来源
     This paper evaluates the determination method of tacrine hydrochloride content in suppositories. Content of tacrine hydrochloride in suppository was determined by ultraviolet spectrophotometry. The average recovery is 99.65% and RSD is 0.18%,respectively.
     采用紫外分光光度法测定盐酸他克林栓剂中盐酸他克林的含量 ,该方法的平均回收率为99.65% ,RSD为 0 .1 8%。
短句来源
     Determination of tacrine hydrochloride by HPLC
     高效液相色谱法测定盐酸他克林的含量
短句来源
     It is the intent of these studies to synthesize acylated prodrugs of tacrine hydrochloride for improving the penetrating ability across the blood-brain barrier (BBB).
     为了提高盐酸他克林 (THA)透过血脑屏障 (BBB)的能力 ,以 THA和苯甲酰氯反应制得其酰化前体药物 :N-苯甲酰 - THA和 N-二苯甲酰 - THA。
短句来源
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  相似匹配句对
     Determination of tacrine hydrochloride by HPLC
     高效液相色谱法测定盐酸他克林的含量
短句来源
     Determination of Tacrine Hydrochloride Content in Suppositories by Ultraviolet Spectrophotometry
     紫外分光光度法测定盐酸他克林栓的含量
短句来源
     Betahistne hydrochloride
     盐酸陪它啶(原名陪它胺)
短句来源
     Doxepin Hydrochloride
     多虑平
短句来源
     Synthesis of Tacrine
     他克林的合成研究
短句来源
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  tacrine hydrochloride
Response Surface Methodology to Investigate the Iontophoretic Delivery of Tacrine Hydrochloride
      
The aim of this study was to characterise the plasma protein binding of tacrine hydrochloride (THA) in vitro.
      
Characteristics of plasma protein binding of tacrine hydrochloride: a new drug for Alzheimer's disease
      


An HPLC method for measuring tacrine hydrochloride was established with C18 column and amobile phase of the mixture of the solution of 0.2% phosphoric acid and 0.2% triethyIamine and acetoni-trile (80: 20) at a flow rate of 1.0 ml/min. The detector set at 240 nm. The results showed that the de-tection limit of tacrine hydrochloride was 10 ng/ml(S/N= 3), the linear range was 0. 5~3.0 pg/ml, andthe relative standard deviations within a day or among 5 days were all less than 2. 0%.

HPLC法测定盐酸他克林的含量。采用十八烷基硅烷键合硅胶填充柱,流动相为0.2%磷酸三乙胺溶液-乙腈(80:20,v/v),检测波长为240nm,最低检测浓度为10ng/ml(S/N=3),在0.5~3.0μg/ml范围内呈良好的线性关系,日内及日间相对标准差均小于2.0%。

This paper evaluates the determination method of tacrine hydrochloride content in suppositories.Content of tacrine hydrochloride in suppository was determined by ultraviolet spectrophotometry.The average recovery is 99.65% and RSD is 0.18%,respectively.

采用紫外分光光度法测定盐酸他克林栓剂中盐酸他克林的含量 ,该方法的平均回收率为99.65% ,RSD为 0 .1 8%。

Aim To synthesize acylated prodrug of tacrine hydrochloride (THA) to improve the infiltration ability across the blood brain barrier (BBB). Methods A series of prodrugs were prepared by acylation of the 7-amino group of THA. The degradation of prodrugs was investigated under different conditions. Biodistribution studies of N -butyramide-THA (BTHA) in mice were carried out to evaluate the function of brain targeting. Results The structures of prodrugs were confirmed by IR, 1HNMR and MS. All prodrugs...

Aim To synthesize acylated prodrug of tacrine hydrochloride (THA) to improve the infiltration ability across the blood brain barrier (BBB). Methods A series of prodrugs were prepared by acylation of the 7-amino group of THA. The degradation of prodrugs was investigated under different conditions. Biodistribution studies of N -butyramide-THA (BTHA) in mice were carried out to evaluate the function of brain targeting. Results The structures of prodrugs were confirmed by IR, 1HNMR and MS. All prodrugs were stable in different medium. Octanol-water partition coefficients indicated increased lipophlicity for various prodrugs compared to the THA. In vivo distribution studies showed that BTHA was mainly distributed in brain, blood and liver (the maximum concentrations were 17.572 5 , 13.140 0 and 22.827 9 mg·L -1 , respectively), while the THA concentration were very low in lung and heart (the maximum concentrations were 4.947 5 and 4.492 5 mg·L -1 , respectively). The BTHA concentration ( 2.415 9 mg·L -1 ) was relatively high even 12 h after administration, showing that BTHA degraded more slowly in brain than in other tissues. Conclusion The infiltration ability of THA across BBB was increased in the form of N -acylate-THA prodrug, indicating that this kind of prodrug is a promising brain-targeting delivery system.

目的 制备盐酸他克林 (THA)的酰化前体药物以提高其透过血脑屏障 (BBB)的能力。方法 THA和酸酐反应制得N 酰化 THA系列前体药物 ;考察了前体药物在不同介质中的降解情况 ,并以N 单丁酰 他克林 (BTHA)为模型药物 ,考察其在小鼠体内的分布和降解情况。结果 合成的化合物经1 HNMR ,MS和IR鉴定为目标化合物。前体药物在不同介质中均较稳定。与原药相比 ,前药的脂水分布系数增大。BTHA主要分布于脑、血浆和肝脏中 (最高浓度分别为 17 5 72 5 ,13 14 0 0和 2 2 82 79mg·L- 1 ) ,在肺和心中的分布浓度很低 (最高浓度分别为 4 94 75和 4 4 92 5mg·L- 1 )。BTHA在脑内的降解速率较慢 ,给药 12h后仍有较高浓度 (2 4 15 9mg·L- 1 )。结论 N 羧酰 THA系列前体药物提高了THA透过BBB的能力 ,有望成为脑内定向给药的有效途径。

 
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