草酸艾司西酞普兰凝胶贴膏的制备及经皮透过性考察
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摘要
目的制备以草酸艾司西酞普兰为模型药物的薄型凝胶贴膏,研究药物体外经皮透过性。方法以亲水性高分子材料制备交联型凝胶贴膏剂,以离体大鼠经皮肤透过速率及24 h累积透过量为指标,探讨艾司西酞普兰凝胶贴膏剂的体外经皮透过性。结果乙二胺促进草酸艾司西酞普兰的经皮透过作用最为显著。所制备的薄型凝胶贴膏的含膏量为传统型凝胶贴膏的1/3,初黏力大,且药物的体外经皮透过量高;不同背衬层对艾司西酞普兰凝胶贴膏的初黏力及经皮透过性无显著影响。结论薄型草酸艾司西酞普兰凝胶贴膏的研发具有重要意义,乙二胺可作为草酸艾司西酞普兰凝胶贴膏的经皮透过促进剂以提高药物的经皮透过性。
Objective To study the preparation and transdermal penetration of escitalopram oxalate hydrogel patch in vitro. Methods The escitalopram oxalate hydrogel patch w as prepared w ith high polymer hydrophilic materials as matrix. The in vitro permeation flux( Jssand Q24) of escitalopram oxalate across the rat abdominal skin w as evaluated. Results Of all the penetration enhancers,ethylenediamine had the best penetration enhancing effect. Compared w ith the traditional type of hydrogel patch,the flimsy type hydrogel patch containing ointment w as about 1/3 of the traditional type,and the tack w as stronger and the cumulative amount of permeated drug w as higher. There w as no significant effect of backing layers on the tack and cumulative amount of drug permeated through the rat skin of escitalopram oxalate hydrogel patch.Conclusions A new type of hydrogel transdermal patch w ith less content of ointment has good potential for transdermal delivery. Ethylenediamine w ill be the proper percutaneous enhancer in the transdermal preparations of escitalopram oxalate.
Objective To study the preparation and transdermal penetration of escitalopram oxalate hydrogel patch in vitro. Methods The escitalopram oxalate hydrogel patch w as prepared w ith high polymer hydrophilic materials as matrix. The in vitro permeation flux( Jssand Q24) of escitalopram oxalate across the rat abdominal skin w as evaluated. Results Of all the penetration enhancers,ethylenediamine had the best penetration enhancing effect. Compared w ith the traditional type of hydrogel patch,the flimsy type hydrogel patch containing ointment w as about 1/3 of the traditional type,and the tack w as stronger and the cumulative amount of permeated drug w as higher. There w as no significant effect of backing layers on the tack and cumulative amount of drug permeated through the rat skin of escitalopram oxalate hydrogel patch.Conclusions A new type of hydrogel transdermal patch w ith less content of ointment has good potential for transdermal delivery. Ethylenediamine w ill be the proper percutaneous enhancer in the transdermal preparations of escitalopram oxalate.
引文
[1]国家药典委员会.中华人民共和国药典:四部[M].北京:中国医药科技出版社,2015:22-23.
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[7]CIMEN B,GUMUS C,CETIN I,et al.The effects of escitalopram treatment on oxidative/antioxidative parameters in patients with depression[J].Bulletin of Clinical Psychopharmacology,2015,25(3):272-279.
[8]MIKROULI E,WRTWEIN G,SOYLU R,et al.Increased numbers of orexin/hypocretin neurons in a genetic rat depression model[J].Neuropeptides,2011,45(6):401-406.
[9]HUSKA M T,CATALANO G,CATALANO M C.Serotonin syndrome associated with the use of escitalopram[J].Cns Spectrums,2007,12(4):270-274.
[10]PJREK E,WINKLER D,STASTNY J,et al.Escitalopram in seasonal affective disorder:results of an open trial[J].Pharmacopsychiatry,2007,40(1):20-24.
[11]HUANG C T,TSAI M J,LIN Y H,et al.Effect of microemulsions on transdermal delivery of citalopram:optimization studies using mixture design and response surface methodology[J].International Journal of Nanomedicine,2013,8(13):2295-2304.
[12]李伟泽,张光伟,赵宁,等.中药水凝胶巴布剂产业化工艺技术攻关研究[J].中草药,2012,43(10):1928-1933.
[2]张韻慧,王春杰,晋兴华,等.吲哚美辛凝胶贴膏小鼠体外透皮性能研究[J].现代生物医学进展,2013,13(34):6619-6622.
[3]呼永河,刘爱琴,李静,等.中药巴布剂的基质研究进展[J].医学综述,2012,18(13):2093-2096.
[4]张洪兵,朱雪瑜,张铁军,等.星点设计-效应面优化法优选复方止痛巴布剂基质处方[J].中草药,2013,44(8):985-988.
[5]张斯杰,刘力,郭建博,等.交联水凝胶基质的中药巴布膏剂制备[J].中国现代中药,2015(6):587-589.
[6]IAN P.Stolerman,Encyclopedia of Psychopharmacology[M].Berlin Heidelberg:Springer-Verlag,2010:490.
[7]CIMEN B,GUMUS C,CETIN I,et al.The effects of escitalopram treatment on oxidative/antioxidative parameters in patients with depression[J].Bulletin of Clinical Psychopharmacology,2015,25(3):272-279.
[8]MIKROULI E,WRTWEIN G,SOYLU R,et al.Increased numbers of orexin/hypocretin neurons in a genetic rat depression model[J].Neuropeptides,2011,45(6):401-406.
[9]HUSKA M T,CATALANO G,CATALANO M C.Serotonin syndrome associated with the use of escitalopram[J].Cns Spectrums,2007,12(4):270-274.
[10]PJREK E,WINKLER D,STASTNY J,et al.Escitalopram in seasonal affective disorder:results of an open trial[J].Pharmacopsychiatry,2007,40(1):20-24.
[11]HUANG C T,TSAI M J,LIN Y H,et al.Effect of microemulsions on transdermal delivery of citalopram:optimization studies using mixture design and response surface methodology[J].International Journal of Nanomedicine,2013,8(13):2295-2304.
[12]李伟泽,张光伟,赵宁,等.中药水凝胶巴布剂产业化工艺技术攻关研究[J].中草药,2012,43(10):1928-1933.