Effect of Polacrilin Potassium as Disintegrant on Bioavailability of Diclofenac Potassium in Tablets: a Technical Note

被引:7
作者
Bele, Mrudula H. [1 ]
Derle, Diliprao V. [1 ]
机构
[1] MVPs Coll Pharm, Nasik 422002, Maharashtra, India
来源
AAPS PHARMSCITECH | 2012年 / 13卷 / 03期
关键词
bioavailability improvement; disintegrants; permeability enhancement; polacrilin potassium;
D O I
10.1208/s12249-012-9802-7
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Polacrilin potassium is an ion exchange resin used in oral pharmaceutical formulations as a tablet disintegrant. It is a weakly acidic cation exchange resin. Chemically, it is a partial potassium salt of a copolymer of methacrylic acid with divinyl benzene. It ionizes to an anionic polymer chain and potassium cations. It was hypothesized that polacrilin potassium may be able to improve the permeability of anionic drugs according to the Donnan membrane phenomenon. The effect of polacrilin potassium on the permeability of diclofenac potassium, used as a model anionic drug, was tested in vitro using diffusion cells and in vivo by monitoring serum levels in rats. The amount of drug permeated across a dialysis membrane in vitro was significantly more in the presence of polacrilin potassium. Significant improvement was found in the extent of drug absorption in vivo. It could be concluded that polacrilin potassium may be used as a high-functionality excipient for improving the bioavailability of anionic drugs having poor gastrointestinal permeability.
引用
收藏
页码:756 / 759
页数:4
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