Applying Theoretical Approach for Predicting the Selective Calcium Channel Blockers Pharmacological Parameter by Biopartitioning Micellar Chromatography
- ISSN号:1001-604X
- 期刊名称:《中国化学:英文版》
- 时间:0
- 分类:R96[医药卫生—药理学;医药卫生—药学]
- 作者机构:[1]College of Pharmacy, Hebei University, Baoding, Hebei 071002, China, [2]Department of Pharmacology, Hebei Medical University, Shijiazhuang, Hebei 050017, China, [3]Center for Molecular Science, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100080, China, [4]Shijiazhuang Pharmaceutical Group, Shijiazhuang, Hebei 050091, China
- 相关基金:Project supported by the National Natural Science Foundation of China (No. 20375010), Natural Science Foundation of Hebei Province (No. 202096), Bairen Project of Chinese Academy of Sciences, and the Excellent Teacher Program and the Specialized Research Fund for the Doctoral Program of Higher Education.Acknowledgements The authors wish to thank professor Yang LIANG and Yongjian ZHANG for a generous gift of m-nisoldipine, nisoldipine and nicardipine.
中文摘要:
为预言口头的药的 biopartitioning micellar 层析(BMC ) 的实用性尖锐毒性和明显的 bioavailability 被表明。一个对数的模型(一个 LD50 模型) 和第二个顺序多项式模型(明显的 bioavailability 模型) 用选择的钙隧道 blockers 的保留数据被获得了预言混合物的药理学性质。BMC 的使用简单,可再现并且能在药发现过程期间关于尖锐毒性和新混合物的运输性质提供关键信息。
英文摘要:
The usefulness of biopartitioning micellar chromatography (BMC) for predicting oral drug acute toxicity and apparent bioavailability was demonstrated. A logarithmic model (an LD50 model) and the second order polynomial models (apparent bioavailability model) have been obtained using the retention data of the selective calcium channel blockers to predict pharmacological properties of compounds. The use of BMC is simple, reproducible and can provide key information about the acute toxicity and transport properties of new compounds during the drug discovery process.