盐酸丁丙诺啡凝胶体外透皮渗透实验研究 |
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摘 要: |
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关 键 词: | 丁丙诺啡 投药 剂量 皮肤吸收 油酸 吖庚因类 色谱法 高效液相 |
Experimental study of in vitro buprenorphine hydrochloride transdermal permeation through hairless mouse skin. |
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Authors: | Bo Huang Miao-Ning Gu Guo-Feng Li Chun-Shui Lin Dan Guo |
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Institution: | Department of Anesthesiology,First Military Medical University, Guangzhou 510515, China. |
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Abstract: | OBJECTIVE: 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. METHODS: 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. RESULTS: 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. CONCLUSION: Permeation enhancers significantly increase Js of buprenorphine hydrochloride gel and renders its release kinetics approaching zero-order. |
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