Effect of Polacrilin Potassium as Disintegrant on Bioavailability of Diclofenac Potassium in Tablets : a Technical Note
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...
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Veröffentlicht in: | AAPS PharmSciTech 2012-09, Vol.13 (3), p.756-759 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | 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. |
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ISSN: | 1530-9932 1530-9932 |
DOI: | 10.1208/s12249-012-9802-7 |