摘要
【目的】建立RP-HPLC法测定离体透皮接受液中辣椒碱的浓度，研究辣椒碱的体外透皮性能。【方法】采用反相高效液相色谱法，用shim-packVP-ODS色谱柱（150mm×4．6inIn，5μm）及保护柱，乙腈-水（60：40）为流动相，流速为1ml／min，检测波长280nm，柱温40℃。采用改良的Franz扩散池，以离体鼠皮为透皮屏障，考察不同浓度辣椒碱在不同时间的累积透过量，采用滞留时间法评价辣椒碱的经皮渗透特性。【结果】辣椒碱在2．71-86．80μg/ml范围内呈良好的线性关系（r=0．9990，n=5），平均回收率为100．97％。日内、日间RSD分别在1．84％。3．88％及2．76％～5．19％。体外透皮研究显示，3种浓度的辣椒碱的累积透过量随浓度增高反而下降。其中5mg／ml辣椒碱溶液稳态流量、渗透系数较大，滞留时间较短，表观扩散系数大，表观分配系数小。【结论】本法灵敏、精确、可信，适用于离体透皮液中辣椒碱浓度的测定。辣椒碱的体外经皮渗透研究表明辣椒碱的浓度对透皮吸收有影响，但是不与浓度成正比，5mg／ml辣椒碱体外经皮渗透性良好。
[ Objective] To establish a RP-HPLC method for quantitative determination of capsaicin in vitro percutaneous solution and to investigate the transdermal delivery characteristics of eapsaicinin vitro. [Methods] Shim-pack VP-ODS column was used as the fixed phase and a mixture of acetonitrile and purified water （60： 40） as a mobile phase.The flow rate was 1 ml/min.The detection wavelength was at 280 nm, and column temperature was 40℃ o Using improved Franz type diffusion cell and excised rat skin in vitro as transdennal barrier, the concentration of capsaicin in samples was determined by HPLC method. The cumulative permeation quantities of capsaicin were observed at 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 24, 48, 72 h respectively.The characteristic of permeation for capsaicin was evaluated by lag time method. [Results] The linear range of capsaiein was 2.71 -86.80μg/ml （ r = 0.9990, n = 5）. The average recovery was 100.97%. The RSD of intra-day was 1.84% -3.88% and the RSD of inter-day was 2.76% - 5.19%. The appearance of capsaiein was very good at the concentration of 1% and 5%. The amount of transdermal absorption, the steady - state flux （Jss） and apparent permeability coefficient （Pm） of eapsaiein in three different concentrations were difference, significantly, the Jss and Pm of 1% eapsaiein and 5% capsaiein were more than 10% capsaicin.The lag time （Tlag） of 5 mg/ml eapsaiein was shorter, and skin/donor phase partition coefficient （Kapp） was smaller, and the diffusion eoefficent （Dapp） was bigger. [Conclusions] This method is sensitive, accurate and reliable and is suitable permeation permetion for analysis of capsaicin in vitro pereutaneous solution. Pereutaneous permetion for capsaicin in different eoneentration is difference. It is shown that 5 nag/ ml eapsaiein is good for percutaneous capability.
出处
《武警医学院学报》
CAS
2009年第4期300-303,共4页
Acta Academiae Medicinae CPAPF
作者简介
【通讯作者】张莉，女，教授，硕士生导师。Tel：022-60578196。E-mail：zhli62tianjin@yahoo．com．cn。
