Dipartimento Farmaceutico, Università degli Studi di Parma, Viale G.P. Usberti 27/A, Parma, Italy.
Int J Pharm. 2009 May 8;372(1-2):12-6. doi: 10.1016/j.ijpharm.2008.12.028. Epub 2008 Dec 31.
The aim of this work was to realize innovative transdermal formulations containing sodium levothyroxine in view of topical administration. Permeation experiments were performed in vitro, using rabbit ear skin as barrier. At the end of the permeation experiments levothyroxine retained in the skin was extracted and quantified by HPLC. Formulations tested were microemulsions and transdermal films. Microemulsions containing isopropyl myristate and isobutanol were shown to be able to increase levothyroxine solubility by the inclusion in reverse micelles. However, the inclusion in reversed micelles reduced the drug release to a significant extent, and consequently skin retention, compared to aqueous solutions. When the microemulsion was included in the transdermal film, drug retention was increased, probably for the enhancer effect of its excipients. The transdermal film proposed in this work could be an interesting alternative to semisolid formulations for the ease of use and the control in the amount of active applied. Additional benefit can be obtained if the film is used in occlusive conditions.
本工作旨在开发含有左甲状腺素钠的经皮创新制剂,用于局部给药。通过兔耳皮肤作为屏障进行体外渗透实验。在渗透实验结束时,通过 HPLC 从皮肤中提取并定量测定左甲状腺素钠的含量。所测试的制剂为微乳剂和透皮贴剂。含有肉豆蔻异丙酯和异丁醇的微乳剂能够通过包含在反胶束中来增加左甲状腺素钠的溶解度。然而,与水溶液相比,包含在反胶束中显著降低了药物的释放,进而减少了皮肤滞留。当微乳剂被包含在透皮贴剂中时,药物滞留增加,可能是由于其赋形剂的增强作用。与半固体制剂相比,本文提出的透皮贴剂具有使用方便和控制应用活性成分量的优势。如果在封闭条件下使用该膜,还可以获得额外的益处。