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目的:研究麝丹眼用即型凝胶中麝香酮与丹酚酸B经家兔离体角膜的渗透特性,为该制剂的开发提供参考。方法:以含1.0%聚山梨酯-80的生理盐水为释放介质,采用Franz扩散池法考察麝丹凝胶中麝香酮和丹酚酸B经家兔角膜的渗透性;以2,4-二硝基苯肼为衍生剂,衍生温度60℃,衍生时间30 min,对麝丹眼用即型凝胶剂家兔离体角膜渗透的接受液进行衍生,采用高效液相色谱法进行梯度洗脱,同时测定接收液中麝香酮、丹酚酸B的含量;考察不同p H和麝香酮质量分数对麝丹眼用即型凝胶中麝香酮、丹酚酸B离体角膜渗透性的影响,绘制累积释药曲线,建立动力学模型,计算表观渗透系数和稳态流量。结果:麝香酮和丹酚酸B通过角膜的扩散行为均符合零级动力学特征,麝丹凝胶中麝香酮离体角膜渗透特性对p H不敏感,丹酚酸B随p H降低而渗透速率增大;丹酚酸B渗透性随麝香酮质量分数增加而渗透量增加,在麝香酮质量分数为0.5%时,麝香酮表观渗透系数1.530×10-6cm·s-1,稳态渗透速率7.651×10-3μg·s-1·cm-2;在此质量分数下,丹酚酸B的表观渗透系数1.218×10-6cm·s-1,稳态渗透速率6.558×10-3μg·s-1·cm-2。结论:麝香酮可促进麝丹眼用即型凝胶中丹酚酸B的角膜渗透,该凝胶中麝香酮最佳用量0.5%。
Objective: To study the permeation characteristics of musk ketone and salvianolic acid B in cornea of instant musk eye gel, and to provide references for the development of this preparation. Methods: The permeation of musk ketone and salvianolic acid B in musk dextran gel was investigated by Franz diffusion cell method using physiological saline containing 1.0% polysorbate-80 as the release medium. Nitrophenylhydrazine as a derivatizing agent, derivatization temperature 60 ℃, derivatization time 30 min, derivation of corneal eye gel with instant gel transdermal rabbit corneal penetration of the solution, using high performance liquid chromatography gradient elution , And the content of musk ketone and salvianolic acid B in the receiving solution was measured simultaneously. The effects of different p H and musk ketone mass fractions on the in vitro corneal permeability of musk ketone and salvianolic acid B, Cumulative release curve was plotted, and kinetic model was established to calculate apparent permeability coefficient and steady state flow rate. RESULTS: The diffusion behavior of musk ketone and salvianolic acid B through the cornea was consistent with the zero-order kinetic characteristics. Muskmelon corneal keratinocyte corneal permeability was not sensitive to p H and salvianolic acid B was permeated with p H decrease The permeation rate of salvianolic acid B increased with the increase of the mass fraction of musk ketone, while the apparent permeation coefficient of musk ketone was 1.530 × 10-6cm · s-1 when the mass fraction of musk ketone was 0.5% The rate of 7.651 × 10-3μg · s-1 · cm-2; at this mass fraction, the apparent permeation coefficient of salvianolic acid B was 1.218 × 10-6cm · s-1, the steady state permeation rate was 6.558 × 10-3μg · s-1 · cm-2. CONCLUSION: Musk ketone promotes the corneal permeation of salvianolic acid B in the gel of instant muskmelon, and the optimum amount of muscone in the gel is 0.5%.