载药量对后交联祖师麻凝胶贴膏剂流变学及体外经皮渗透特性的影响

Effect of drug loading on rheology and in vitro transdermal penetration properties of post-crosslinking Daphnes Giraldii Cortex gel plaster

目的通过载药量对后交联凝胶贴膏流变学及体外经皮渗透特性的影响,考察后交联凝胶贴膏基质的载药量。方法采用流变学技术测定不同载药量时胶料的各项流变学参数,并以祖师麻乙醇提取物为模型药物,以祖师麻甲素的累积透过率及皮肤滞留率为指标,对成品贴膏进行体外经皮渗透试验,确定基质载药量。结果当载药量在4.0%~12.4%时,含药胶料的结构强度、黏弹性、耐温耐剪切性及抗变形能力、稳定性均符合要求,其中以载药量为6.8%时最佳;祖师麻甲素的累积透过率随载药量逐渐增大,皮肤滞留率分别变化不明显。结论通过比较流变学及体外经皮渗透试验结果,确定基质处方的最佳载药量为6.8%。

Objective The effect of drug loading on the rheology and in vitro transdermal penetration of the post-crosslinking gel paster was investigated. Methods Rheological technology was used to determine the rheological parameters of the adhesive with different drug loading, using the ethanol extract of Daphnes Giraldii Cortex as the model drug and the cumulative penetration rate and skin retention rate of daphnetin as the indexes, in vitro transdermal penetration test was conducted to determine the substrate loading rate of the finished paster. Results When the drug loading was between 4.0% and 12.4%, the structural strength, viscoelasticity, temperature resistance, shear resistance, deformation resistance and stability of the drug containing adhesive met the requirements, and the best drug loading was 6.8%. The cumulative penetration rate of daphnetin increased gradually with the drug loading, but the skin retention rate did not change significantly. Conclusion By comparing the results of rheology and in vitro transdermal penetration test, the optimal drug loading of matrix prescription was determined to be 6.8%.