盐酸青藤碱传递体关节贴剂的制备与性能评价  

Preparation and Performance Evaluation of Sinomenine Hydrochloride Transfersomes Joint Patch

作　　者：李晓杰 范博 任雷 杨钧 张志伟 李芳[3] Li Xiaojie;Fan Bo;Ren Lei;Yang Jun;Zhang Zhiwei;Li Fang(Medicine Researchinstitute of Shaanxi Pharmaceutical Holding Cooperationc,Xian 710075;Shaanxi Pharmaceutical Holding Group Co.,Ltd.,Xian 710075;Shaanxi Academy of Traditional Chinese Medicine,Xian 710003,China)

机构地区：[1]陕西医药控股医药研究院有限公司,陕西西安710075 [2]陕西医药控股集团有限责任公司,陕西西安710075 [3]陕西省中医药研究院,陕西西安710003

出　　处：《广东化工》2023年第20期38-40,14,共4页Guangdong Chemical Industry

摘　　要：制备盐酸青藤碱传递体关节贴剂,采用试验优选了盐酸青藤碱传递体关节贴剂的制备处方,并对优选处方进行了皮肤刺激性考察;同时通过HPLC法对盐酸青藤碱传递体关节贴剂的体外释放及经皮渗透规律进行探索。结果显示盐酸青藤碱传递体制备的较优处方为:大豆卵磷脂600 mg、胆固醇200 mg、脱氧胆酸钠40 mg、盐酸青藤碱200 mg、无水乙醇5 mL、磷酸盐缓冲液(pH 6.8)45 mL;贴剂基质为:Eudragit E1000.65 g、丁二酸0.25 g、柠檬酸三乙酯0.08 g、甘油0.02 g;传递体与基质配比为1∶10。皮肤刺激性试验结果显示单次给药24 h后无明显的皮肤刺激性。体外释药行为研究结果显示盐酸青藤碱传递体关节贴剂体外释放符合Higuchi方程,24 h时盐酸青藤碱的累积释放率达87.7%。经皮渗透试验结果显示将盐酸青藤碱制成传递体后增加了其的皮肤渗透性。To prepare the joint patch of sinomenine hydrochloride transfersomes,and to optimize the formulation of the joint patch of sinomenine hydrochloride transfersomes meanwhile,the release and transdermal permeation of sinomenine hydrochloride transfersomes joint patch in vitro were studied by HPLC.The results showed that the optimal formulation for preparation of sinomenine hydrochloride transfersomes was soybean lecithin 600 mg,cholesterol 200 mg,sodium deoxycholate 40 mg,sinomenine hydrochloride 200 mg,anhydrous alcohol 5 mL,phosphate buffer(pH 6.8)45 mL;The substrate was EUDRAGIT E1000.65 g,succinic acid 0.25 g,triethyl citrate 0.08 g and glycerol 0.02 g;The ratio of transmitter to substrate was 1∶10.The results of skin irritation test showed that there was no obvious skin irritation after 24 h of single administration.The release behavior of sinomenine hydrochloride transfersomes joint patch in vitro was in accordance with Higuchi equation.The cumulative release rate of sinomenine hydrochloride was 87.7%at 24 h.The results of transdermal permeation test showed that sinomenine hydrochloride could increase the skin permeability of the transfersomes.

关 键 词：盐酸青藤碱传递体 乙醇注入法 皮肤刺激性 累积释放率 性能评价 

分 类 号：R944.9[医药卫生—药剂学]