酮洛芬贴剂的体外经皮渗透性考察

In vitro permeability study of ketoprofen patches

目的制备酮洛芬压敏胶分散型贴剂并考察其体外经皮的渗透性。方法将药物及促渗剂溶解于压敏胶中搅拌均匀,涂布制备压敏胶分散型贴剂,采用卧式双室扩散池,进行体外经皮渗透实验,以24 h累积透过量Q_(24)、渗透速率J_S及滞后时间t_(lag)(h)为指标筛选载药量及促渗剂的种类和用量。结果体外经皮渗透实验结果表明,肉豆蔻酸异丙酯具有最强的促渗透能力,当其用量的质量分数为2.5%时,Q_(24)、J_S及t_(lag)均与参比贴一致(P>0.05),而其他3种渗透剂与其联用均表现出一定的抑制作用。结论载药量质量分数为2.5%、加入质量分数2.5%肉豆蔻酸异丙酯作为促渗剂制备贴剂,其经皮渗透性与参比贴一致。

Objective To prepare ketoprofen-loaded drug-in adhesive patches and investigate the effect of penetration enhancers on the permeation of ketoprofen. Methods In our study, ketoprofen transdermal patches were prepared by the solvent evaporation technique. Drugs and percutaneous enhancers were dissolved in ethyl acetate and then incorporated in pressure-sensitive adhesive. The mixture was homogenized and then spread on the polyester film. The patches were kept in oven to remove organic solvent and then covered with backing film. Thereafter, the dry film was cut into standard sizes. The in vitro transdermal permeation experiments were performed by two-compartment horizontal diffusion cells to evaluate percutaneous permeability of ketoprofen self-made patches compared with reference patches. Results Among the permeation enhancers investigated, isopropyl myristate(IPM) significantly enhanced drug transdermal amount through rabbit skin, and the enhancement ratio reached to 4.37-fold. There were no significant difference(P>0.05) between the self-made patch containing 2.5% ketoprofen and 2.5% IPM and reference patch with respect to 24 h cumulative amount, permeation flux and lag time. Whereas, when IPM was combined with the other three enhancers, the permeation ability was restrained. Conclusion There is no significant difference in permeability between the self-made patch containing of 2.5% ketoprofen and 2.5% IPM and reference patch.