Wu Xingxing, Chen Yulin, Gui Shuangying, Wu Xiaoqing, Chen Lei, Cao Yingji, Yin Dengke, Ma Ping
a Department of Pharmacy , Anhui University of Chinese Medicine , Hefei , P.R. China.
b Anhui Engineering Research Center for Chinese Medicine Preparation , Hefei , P.R. China , and.
Pharm Dev Technol. 2016 Nov;21(7):787-793. doi: 10.3109/10837450.2015.1055766. Epub 2015 Jun 30.
Sinomenine hydrochloride-loaded dissolving microneedles (SH-DM) were fabricated by maltose and poly-lactic-co-glycolic acid using a casting method. The mechanical strength of SH-DM was investigated by an insertion test. In vivo transdermal absorption experiment was performed to evaluate the percutaneous absorption of SH-DM, sinomenine hydrochloride gel (SH-G) was used as a control. The results demonstrated that prepared SH-DM was morphologically intact with sufficient mechanical strength after inserting into aluminum foil and rat skin. The value of area under curve obtained after administration of SH-DM through transdermal in rabbits showed a significantly rise and was 1.99 times higher than that of SH-G, and the relative bioavailability value was 199.21%. These results showed that SH-DM enhanced bioavailability and permeability of SH.
采用浇铸法,以麦芽糖和聚乳酸 - 乙醇酸共聚物制备了载盐酸青藤碱的溶蚀性微针(SH - DM)。通过插入试验研究了SH - DM的机械强度。进行体内透皮吸收实验以评估SH - DM的经皮吸收情况,以盐酸青藤碱凝胶(SH - G)作为对照。结果表明,制备的SH - DM插入铝箔和大鼠皮肤后形态完整,具有足够的机械强度。经皮给予SH - DM后,家兔体内获得的曲线下面积值显著升高,比SH - G高1.99倍,相对生物利用度值为199.21%。这些结果表明,SH - DM提高了盐酸青藤碱的生物利用度和渗透性。