Effect of penetration enhancers on the transdermal delivery of bupranolol through rat skin

Effect of penetration enhancers on the transdermal delivery of bupranolol through rat skin
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DOI:
10.1080/10717540590931936
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发表时间:
2005-05-01
期刊:
影响因子:
6
通讯作者:
Pandit, JK
Pandit, JK
中科院分区:
医学2区
文献类型:
--
作者:
Babu, RJ;Pandit, JK

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布萘洛尔(BPL)具有良好的理化性质和药代动力学特性,是一种理想的经皮给药系统候选药物。采用并行扩散池研究了不同渗透促进剂对BPL经皮渗透的影响。2-将不同浓度的吡咯烷酮(PY)、1-甲基-2-吡咯烷酮(MPY)和丙二醇(PG)与0.4%w/v的BPL水悬浮液一起沿着用作渗透促进剂。在异丙醇-水(6:4)混合物中的不同浓度的薄荷脑也用作增强剂,其中0.4%w/v的BPL完全溶解。用所有上述促进剂进行皮肤预处理研究,以了解它们在渗透促进作用中的作用。5%w/v浓度的PY和MPY分别使BPL的渗透增加了3.8倍和2.4倍(P
Bupranolol (BPL) is a suitable drug candidate for transdermal drug delivery system development based on its favorable physicochemical and pharmacokinetic properties. The effect of different penetration enhancers on the permeation of BPL across rat skin was studied using side-by-side diffusion cells. 2-pyrrolidone (PY), 1-methyl-2-pyrrolidone (MPY), and propylene glycol (PG) at various concentrations were used as penetration enhancers along with 0.4% w/v aqueous suspension of BPL. Menthol at different concentrations in isopropanol-water (6:4) mixture also was used as an enhancer wherein BPL at 0.4% w/v was completely solubilized. Skin pretreatment studies were carried out with all the above enhancers to understand their role in the penetration enhancement effect. PY and MPY at 5% w/v concentrations increased the permeation of BPL by 3.8- and 2.4-fold, respectively, versus control (P