Biological solubility is one of the important basic parameters in the development process of poorly soluble drugs,but the current measurement methods are mainly based on a large number of experiments,which are time-co...Biological solubility is one of the important basic parameters in the development process of poorly soluble drugs,but the current measurement methods are mainly based on a large number of experiments,which are time-consuming and cost-intensive.There is still a lack of effective theoretical models to accurately describe and predict the biological solubility of drugs to reduce costs.Therefore,in this study,osaprazole and irbesartan were selected as model drugs,and their solubility in solutions containing surfactants and biorelevant media was measured experimentally.By calculating the parameters of each component using the perturbed-chain statistical associating fluid theory(PC-SAFT)model,combined with pH-dependent and micellar solubilization models,the thermodynamic phase behavior of the two drugs was successfully modeled,and the predicted results were in good agreement with the experimental values.These results demonstrate that the model combination used provides important basic parameters and theoretical guidance for the development and screening of poorly soluble drugs and related formulations.展开更多
基金the financial support from the National Natural Science Foundation of China(22278070,21978047,21776046)。
文摘Biological solubility is one of the important basic parameters in the development process of poorly soluble drugs,but the current measurement methods are mainly based on a large number of experiments,which are time-consuming and cost-intensive.There is still a lack of effective theoretical models to accurately describe and predict the biological solubility of drugs to reduce costs.Therefore,in this study,osaprazole and irbesartan were selected as model drugs,and their solubility in solutions containing surfactants and biorelevant media was measured experimentally.By calculating the parameters of each component using the perturbed-chain statistical associating fluid theory(PC-SAFT)model,combined with pH-dependent and micellar solubilization models,the thermodynamic phase behavior of the two drugs was successfully modeled,and the predicted results were in good agreement with the experimental values.These results demonstrate that the model combination used provides important basic parameters and theoretical guidance for the development and screening of poorly soluble drugs and related formulations.
基金supported by the Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine(ZYYCXTD-C-202006)Gansu Cheezheng Tibetan Medicine(BUCM-2021-JS-FW-087,Beijing,China).
文摘目的:评价白脉软膏在腰椎间盘突出症(lumbar disc herniation)患者中的疗效与安全性。方法:本研究设计了一项前瞻、随机、双盲、安慰剂对照的多中心临床试验方案。计划招募194例患者,按1:1的比例平均分配至试验组和对照组。患者将接受为期14天的白脉软膏或安慰剂的干预,随后进行为期1周的随访。通过视觉模拟评分法(visual analogue scale score)评估疼痛程度,日本骨科协会评估治疗分数(Japanese Orthopedic Association score)评估功能状态,Likert量表将用于评估麻木程度,此外还将记录应急处理的使用和对健康教育的依从情况。安全性评估将包括实验室检查和不良事件记录。讨论:这项试验将首次对白脉软膏在腰椎间盘突出症患者中进行临床疗效和安全性评价。使用安慰剂的优势在于排除因盲法不充分而导致的偏倚。为了避免由研究对象和研究者的主观因素引起的任何偏倚,对于结局评价者、数据管理人员、统计分析人员以及所有相关研究人员都将实施盲法。本试验结果将为腰椎间盘突出症的治疗以及白脉软膏的未来研究方向提供重要依据。
