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含奥昔布宁的新型透皮生物黏附膜:体外透过兔耳皮肤的渗透作用

New transdermal bioadhesive film containing oxybutynin: In vitro permeation across rabbit ear skin.

作者信息

Nicoli S, Penna E, Padula C, Colombo P, Santi P

机构信息

Dipartimento Farmaceutico, Università degli Studi di Parma, Viale G.P. Usberti 27/A, 43100 Parma, Italy.

出版信息

Int J Pharm. 2006 Nov 15;325(1-2):2-7. doi: 10.1016/j.ijpharm.2006.06.010. Epub 2006 Jun 9.

Abstract

Oxybutynin is used extensively in the treatment of patients with overactive bladder. The aim of this work was to realize and test in vitro a new transdermal bioadhesive film containing oxybutynin. Transdermal films were prepared by dissolving in water an adhesive (Plastoid), a film-forming polymer (polyvinyl alcohol), a plasticizer (sorbitol) and the drug. The mixture was then spread on siliconized paper and oven-dried. Permeation experiments were conducted in Franz-type diffusion cells using rabbit ear skin as barrier. The donor compartment contained a water solution, the prepared film (with or without backing) or the commercial patch (Oxytrol). The experiments were performed for 24h. Oxybutynin showed good permeation characteristics across the skin. When the film was applied in occlusive conditions the release profiles were much higher than in non-occlusive conditions, reaching 50% of drug permeated after 24h. Compared to the commercial patch Oxytrol, the film was more efficient suggesting that a smaller area or a lower drug loading could be employed. The results obtained show that the bioadhesive film can be a promising and innovative therapeutic system for the transdermal administration of oxybutynin.

摘要

奥昔布宁被广泛用于治疗膀胱过度活动症患者。这项工作的目的是在体外制备并测试一种含奥昔布宁的新型透皮生物黏附膜。透皮膜是通过将一种黏合剂(Plastoid)、一种成膜聚合物(聚乙烯醇)、一种增塑剂(山梨醇)和药物溶解于水中制备而成。然后将混合物铺展在硅化纸上并烘干。渗透实验在Franz型扩散池中进行,使用兔耳皮肤作为屏障。供体室含有水溶液、制备的膜(有或没有背衬)或市售贴剂(奥昔布宁贴片)。实验进行24小时。奥昔布宁在皮肤上显示出良好的渗透特性。当膜在封闭条件下应用时,释放曲线比在非封闭条件下高得多,24小时后药物渗透达到50%。与市售贴剂奥昔布宁贴片相比,该膜更有效,这表明可以使用更小的面积或更低的药物载量。所获得的结果表明,生物黏附膜对于奥昔布宁的透皮给药可能是一种有前景的创新治疗系统。

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