吲哚美辛不同鼻用乳剂的渗透研究及其可能的抗炎作用。
Permeation studies of indomethacin from different emulsions for nasal delivery and their possible anti-inflammatory effects.
作者信息
Karasulu H Yeşim, Sanal Z Evren, Sözer Sumru, Güneri Tamer, Ertan Gökhan
机构信息
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ege, 35100 Bornova, Izmir, Turkey.
出版信息
AAPS PharmSciTech. 2008;9(2):342-8. doi: 10.1208/s12249-008-9053-9. Epub 2008 Feb 14.
The purpose of this research was to develop an emulsion formulation of indomethacin (IND) suitable for nasal delivery. IND was incorporated into the oil phases of oil in water (O/W) and water in oil (W/O) emulsions. For this purpose, different emulsifying agents (Tween 80, Span 80 and Brij 58) were used in two emulsion formulations. When the effects of several synthetic membranes (nylon, cellulose, cellulose nitrate) were compared with the sheep nasal mucosa, the cellulose membrane and sheep nasal mucosa showed similar permeation properties for O/W emulsion (P > 0.05). To examine the absorption characteristics of IND, the anti-inflammatory properties of intravenous solution of IND, intranasal O/W emulsions of IND (with or without enhancers) and intranasal solution of IND (IND-Sol) were investigated in rats with carrageenan-induced paw edema. When citric acid was added to the nasal emulsion, the anti-inflammatory activity was similar to that of intravenous solution (P > 0.05). Finally, it was concluded that, intranasal administration of IND emulsion with citric acid may be considered as an alternative to intravenous and per oral administrations of IND to overcome their adverse effects.
本研究的目的是开发一种适合鼻腔给药的吲哚美辛（IND）乳剂配方。将IND掺入水包油（O/W）和油包水（W/O）乳剂的油相中。为此，在两种乳剂配方中使用了不同的乳化剂（吐温80、司盘80和Brij 58）。当将几种合成膜（尼龙、纤维素、硝酸纤维素）与绵羊鼻黏膜的效果进行比较时，纤维素膜和绵羊鼻黏膜对O/W乳剂表现出相似的渗透特性（P>0.05）。为了研究IND的吸收特性，在角叉菜胶诱导爪水肿的大鼠中研究了IND静脉溶液、IND鼻内O/W乳剂（有或无增强剂）和IND鼻内溶液（IND-Sol）的抗炎特性。当向鼻用乳剂中加入柠檬酸时，其抗炎活性与静脉溶液相似（P>0.05）。最后得出结论，经鼻给予含柠檬酸的IND乳剂可被视为IND静脉给药和口服给药的替代方法，以克服它们的不良反应。
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