不同基质及促渗剂对奥氮平贴剂体外透皮吸收的影响

Effect of Matrixes and Different Penetration Enhancers on Transdermal Permeability of Olanzapine in vitro

目的:研究不同基质及促渗剂对奥氮平贴剂体外透皮促渗作用的影响。方法:采用不同基质及促渗剂制备奥氮平贴剂;采用卧式双室扩散池,以离体大鼠皮肤为模型,通过HPLC法测定药物浓度,拟合奥氮平透皮吸收的累积透过量和透过速率。结果:由Duro-Tak 87-4098型压敏胶制备的贴剂具有较好的稳态渗透速率,5%薄荷脑+10%肉豆蔻酸异丙酯合用对奥氮平促渗效果明显,促渗倍率达5.86倍。结论:奥氯平在以5%薄荷脑+10%内豆蔻酸异丙酯为促渗剂,Duro-Tak 87-4098型压敏胶为基质时具有较好的透皮吸收。

To study effects of matrixes and penetration enhances on the permeability of olanzapine in vitro.Method： Olanzapine patch was prepared by different concentration and type of penetration enhancers.Using modified Franz diffusion cell and excised male rat skin as model,the concentration of olanzapine was determined by HPLC.Accumulative permeation quantity and velocity constant of olanzapine were fitted.Result：It was found Duro-Tak 87-4098 existed a significant higher flux on the penetration of pentazocine. The patch consisting of 5%menthanol and 10%isopropyl myristate showed the optimal permeation with 5.86-fold enhancement. Conclusion：Olanzapine patch with Duro-Tak 87-4098 as matrix and 5%menthanol and 10%isopropyl myristate as permeability enhancer shows nice drug transdermal delivery effects.