Objective:To find a viable alternative to reduce the number of doses required for the patients with post-traumatic stress disorder(PTSD),and to improve efficacy and patient compliance.Methods: In this study,we used gi...Objective:To find a viable alternative to reduce the number of doses required for the patients with post-traumatic stress disorder(PTSD),and to improve efficacy and patient compliance.Methods: In this study,we used ginger oil,a phytochemical with potential therapeutic properties,to prepare ginger oil patches.High-performance liquid chromatography(HPLC)was used to quantify the main active component of ginger oil,6-gingerol.Transdermal absorption experiments were conducted to optimize the various pressure-sensitive adhesives and permeation enhancers,including their type and concentration.Subsequently,the ginger oil patches were optimized and subjected to content determination and property evaluations.A PTSD mouse model was established using the foot-shock method.The therapeutic effect of ginger oil patches on PTSD was assessed through pathological sections,behavioral tests,and the evaluation of biomarkers such as tumor necrosis factor-α(TNF-α),interleukin-6(IL-6),brain-derived neurotrophic factor(BDNF),and melatonin(MT).Results: The results demonstrated that ginger oil patches exerted therapeutic effects against PTSD by inhibiting inflammatory responses and modulating MT and BDNF levels.Pharmacokinetic experiments revealed that ginger oil patches maintained a stable blood drug concentration for at least one day,addressing the rapid metabolism drawback of 6-gingerol and enhancing its therapeutic efficacy.Conclusions: Ginger oil can be prepared as a transdermal drug patch that meets these requirements,and the bioavailability of the prepared patch is better than that of oral administration.It can improve PTSD with good patient compliance and ease of administration.Therefore,it is a promising therapeutic formulation for the treatment of PTSD.展开更多
目的以体外释放度和经皮渗透性为指标,制备醋氯芬酸贴剂并优化压敏胶和促渗剂的处方。方法采用不同类型丙烯酸酯压敏胶为基质制备醋氯芬酸贴剂,以体外释放度为指标考察筛选压敏胶;以不同种类促渗剂制备醋氯芬酸贴剂,采用改良Franz扩散池...目的以体外释放度和经皮渗透性为指标,制备醋氯芬酸贴剂并优化压敏胶和促渗剂的处方。方法采用不同类型丙烯酸酯压敏胶为基质制备醋氯芬酸贴剂,以体外释放度为指标考察筛选压敏胶;以不同种类促渗剂制备醋氯芬酸贴剂,采用改良Franz扩散池,以离体大鼠皮肤为渗透屏障,考察其经皮渗透性能,筛选经皮渗透促进剂。结果醋氯芬酸贴剂在12 h内体外释放曲线遵循Higuchi动力学方程,经皮渗透曲线遵循零级动力学方程,且以Duro Tak 87-2677为压敏胶基质、质量分数为5%的氮酮为促渗剂时醋氯芬酸贴剂具有较快的释放和经皮渗透速率。结论醋氯芬酸贴剂为皮肤控释型骨架释药系统,选择适宜的基质和促渗剂可保证足够的药物释放并穿透皮肤发挥理想的治疗作用。展开更多
基金supported by the National Natural Scientific Foundation(82172186)Beijing Natural Scientific Foundation(L222126).
文摘Objective:To find a viable alternative to reduce the number of doses required for the patients with post-traumatic stress disorder(PTSD),and to improve efficacy and patient compliance.Methods: In this study,we used ginger oil,a phytochemical with potential therapeutic properties,to prepare ginger oil patches.High-performance liquid chromatography(HPLC)was used to quantify the main active component of ginger oil,6-gingerol.Transdermal absorption experiments were conducted to optimize the various pressure-sensitive adhesives and permeation enhancers,including their type and concentration.Subsequently,the ginger oil patches were optimized and subjected to content determination and property evaluations.A PTSD mouse model was established using the foot-shock method.The therapeutic effect of ginger oil patches on PTSD was assessed through pathological sections,behavioral tests,and the evaluation of biomarkers such as tumor necrosis factor-α(TNF-α),interleukin-6(IL-6),brain-derived neurotrophic factor(BDNF),and melatonin(MT).Results: The results demonstrated that ginger oil patches exerted therapeutic effects against PTSD by inhibiting inflammatory responses and modulating MT and BDNF levels.Pharmacokinetic experiments revealed that ginger oil patches maintained a stable blood drug concentration for at least one day,addressing the rapid metabolism drawback of 6-gingerol and enhancing its therapeutic efficacy.Conclusions: Ginger oil can be prepared as a transdermal drug patch that meets these requirements,and the bioavailability of the prepared patch is better than that of oral administration.It can improve PTSD with good patient compliance and ease of administration.Therefore,it is a promising therapeutic formulation for the treatment of PTSD.
文摘目的以体外释放度和经皮渗透性为指标,制备醋氯芬酸贴剂并优化压敏胶和促渗剂的处方。方法采用不同类型丙烯酸酯压敏胶为基质制备醋氯芬酸贴剂,以体外释放度为指标考察筛选压敏胶;以不同种类促渗剂制备醋氯芬酸贴剂,采用改良Franz扩散池,以离体大鼠皮肤为渗透屏障,考察其经皮渗透性能,筛选经皮渗透促进剂。结果醋氯芬酸贴剂在12 h内体外释放曲线遵循Higuchi动力学方程,经皮渗透曲线遵循零级动力学方程,且以Duro Tak 87-2677为压敏胶基质、质量分数为5%的氮酮为促渗剂时醋氯芬酸贴剂具有较快的释放和经皮渗透速率。结论醋氯芬酸贴剂为皮肤控释型骨架释药系统,选择适宜的基质和促渗剂可保证足够的药物释放并穿透皮肤发挥理想的治疗作用。
