秋水仙碱醇质体贴剂的制备及其体外透皮释药

Preparation of colchicine ethosome patches and evaluation of their in vitro transdermal diffusion

目的:制备秋水仙碱醇质体贴剂并研究其体外透皮释药性能。方法:采用注入法制备秋水仙碱醇质体,以Ⅳ#丙烯酸树脂、柠檬酸三乙酯和琥珀酸压敏胶材料制备压敏胶作为骨架,制成秋水仙碱贴剂;用高效液相色谱(HPLC)法测定贴剂中秋水仙碱的含量,并以改良的Franz扩散池研究贴剂体外透皮释药性能。结果:秋水仙碱经制成醇质体,再用丙烯酸压敏胶制成秋水仙醇质体贴剂,符合Higuchi方程;不含月桂氮芯卓酮与含5%、10%比例月桂氮卓芯酮的醇质体药物透皮释药速率分别为(2.64±0.16),(3.92±0.12)μg.cm-2.h-1和(4.26±0.18)μg.cm-2.h-1,明显高于不含醇质体贴剂(P<0.05);不含月桂氮芯卓酮与含5%、10%月桂氮芯卓酮的醇质体皮肤药物滞留量分别为(2.94±0.12),(3.64±0.09)μg.cm-2和(4.03±0.12)μg.cm-2,可改变透皮吸收促进剂的用量控制贴剂的释药速率(P<0.05)。结论:所制备的秋水仙碱醇质体贴剂具有明显的缓释作用和较高的透皮吸收促进作用。

OBJECTIVE To prepare the colchicines ethosome patches and to evaluate their in vitro transdermal diffusion. METHOI）N Colchicine ethosomes were prepared by the injection method. The IV# polyacrylic resin, triethyl citrate and sue- cinic acid were used to prepare the pressure sensitive adhesive as matrix Then it was used to prepare colchicine ethosome pat- ches. The HPLC was adopted to determine the content of colchicine of colchicine ethosome patches. The reformed Franz diffu- sion cell was adopted to investigate the in vitro transdermal diffusion. RESULTS The Colchicine ethosome patches, which were prepared by colchieine ethosomes and acrylate pressure-sentitive adhesive, complied with the Higuchi equation. Comparing with the ordinary patches, the colchicine ethosome patches without azone, and with azone of 5% and 10%, which had the release rates of （2.64±0. 16）, （3.92±0. 12）μg·cm- 2 o h- 1 and （4. 26 ±0. 18）μg·cm- 2·h- 1 respectively, had the higher transdermal absorption （P（0. 05）. The drug retentions of colchicine ethosome patches without azone,and with azone of 5% and 10%were （2. 94±0. 12）, （3.64±0. 09）gg.cm-2 and （4. 03±0.12）μg·cm-2 respectively. Thus the release rate of eolehicine ethosome pat- ehes could be changed by changing the amount of transdermal absorption enhancer（P〈0. 05）. CONCLUSION The colchicine ethosome patches have the obvious sustained-released effect and higher transdermal absorption enhancing effect.