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目的对制备的猫爪草提取物离子敏感型原位凝胶(RTRE-ISG)进行肺部滞留性、安全性及局部药物浓度的评价。方法以海藻酸钠作为辅料,猫爪草提取物(70%乙醇)作为溶剂,在室温下磁力搅拌使其充分溶胀,制备得到RTRE-ISG。大鼠通过气管介入给药后,测定肺部灌洗液中的炎症因子和致纤维化因子水平,筛选出相对安全的处方;再采用Cy5.5作为荧光染料,借助小动物活体成像系统对RTRE-ISG肺部滞留性进行评价;最后运用改良肺泡灌洗技术,对大鼠肺部进行灌洗,测定局部药物浓度。结果 1%海藻酸钠RTRE-ISG在肺部安全性较好,荧光活体成像技术显示其可在肺部滞留120~144 h,肺部局部药物浓度的测定显示1%海藻酸钠RTRE-ISG在5 h释放达到峰值为5.24μg/m L,144 h药物浓度为0.08μg/m L。结论 RTRE-ISG在肺部可滞留120 h以上,可为中药治疗肺结核提供一种新型的缓释制剂。
OBJECTIVE To evaluate the lung retentivity, safety and local drug concentration of Radix Angelicae Sinensis extract ion sensitive in situ gels (RTRE-ISG). Methods RTRE-ISG was prepared by using sodium alginate as excipient and cat’s paw extract (70% ethanol) as solvent, and then magnetic stirring at room temperature to make it fully swollen. After tracheal administration in rats, the level of inflammatory factors and fibrogenic factors in the lung lavage fluid were measured, and the relatively safe prescription was screened out. Cy5.5 was used as fluorescent dye, and the live animal imaging system of RTRE -ISG lung retention assessment; Finally, the use of modified alveolar lavage technology, the lungs of rats lavage, determination of local drug concentration. Results 1% sodium alginate RTRE-ISG was safe in the lungs. Fluorescence biopsy showed that it could be retained in the lungs for 120-144 h. The local drug concentrations in the lungs showed that 1% sodium alginate RTRE-ISG 5h release reached a peak of 5.24μg / m L, 144h drug concentration of 0.08μg / m L. Conclusion RTRE-ISG can be retained in the lungs for more than 120 h, which can provide a new type of sustained-release preparation for TCM treatment of pulmonary tuberculosis.