Huang Bo, Gu Miao-Ning, Li Guo-Feng, Lin Chun-Shui, Guo Dan
Department of Anesthesiology,First Military Medical University, Guangzhou 510515, China.
Di Yi Jun Yi Da Xue Xue Bao. 2002 Oct;22(10):895-7.
To investigate the in vitro transdermal permeation of buprenorphine hydrochloride gel through hairless mouse skin and the effect of permeation enhancers on the permeability of this transdermal drug delivery system.
Skin samples 1.0 cm in diameter were obtained from hairless mice for subsequent in vitro tests of the permeability of the drug. In permeation enhancer-free group, the permeability of buprenorphine hydrochloride at the concentrations of 0.5%, 1.0% and 2.0% was tested. The permeation enhancer group (all application containing 1% buprenorphine hydrochloride) was further divided into oleic group (including 3 subgroups with 2%, 4%, and 6% oleic), azone group (subdivided into 3 groups with 1%, 2%, and 4% azone) and mixed group (with 4% oleic plus 4% azone). The permeation parameters, namely steady state flux (Js) and Js enhancement ratio were evaluated.
Js in permeation enhancer-free groups were 0.69+/-0.11, 0.90+/-0.14 and 1.18+/-0.10 microgram/cm2.h respectively, which differed only insignificantly (P>0.05). The mixed group showed the maximum permeation, with Js and ER of 13.22+/-1.27 microgram/cm2.h and 14.6 respectively.
Permeation enhancers significantly increase Js of buprenorphine hydrochloride gel and renders its release kinetics approaching zero-order.
研究盐酸丁丙诺啡凝胶经无毛小鼠皮肤的体外透皮渗透情况以及渗透促进剂对该透皮给药系统渗透性的影响。
从无毛小鼠获取直径为1.0 cm的皮肤样本，用于后续药物渗透性的体外试验。在无渗透促进剂组，测试浓度为0.5%、1.0%和2.0%的盐酸丁丙诺啡的渗透性。渗透促进剂组（所有制剂含1%盐酸丁丙诺啡）进一步分为油酸组（包括含2%、4%和6%油酸的3个亚组）、氮酮组（细分为含1%、2%和4%氮酮的3组）和混合组（含4%油酸加4%氮酮）。评估渗透参数，即稳态通量（Js）和Js增强率。
无渗透促进剂组的Js分别为0.69±0.11、0.90±0.14和1.18±0.10 μg/cm²·h，差异无统计学意义（P>0.05）。混合组显示出最大渗透，Js和ER分别为13.22±1.27 μg/cm²·h和14.6。
渗透促进剂显著增加盐酸丁丙诺啡凝胶的Js，并使其释放动力学接近零级。
