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Lipophilicity, permeability and transport of some antiviral barriersKristl, Albin ; Legen, IgorAbsorption of a drug from the gastrointestinal tract is very important stepeng for achieving high bioavailability after peroral application. In this work an insight in the permeation of some ... acyclovir antivirus derivatives through the rat jejunum in side-by-side diffusion cells is given. It was established in one of our previous works that eight antivirus derivatives (acyclovir and deoxyacyclovir with their acetyl congeners) permeate through the rat jejunum ćin vitroć passively, probably through the paracellular route only.1 Additionally, negative correlation between the permeability (Papp) through therat jejunum and log P(n-octanolžwater) of tested compounds was shown. The contradiction between the extreme low permeation (similar or even slower than for marker fluorescein) of acyclovir and deoxyacyclovir through tissue ćin vitroć and much better absorption, especially of deoxyacyclovir ćin vivoć, could not be explained. In the present work the permeabilities through the ratjejunum and through the dispersions of native porcine gastric mucus were evaluated and compared with the aim to determine hydrophilic and lipophilic absorption barrier for studied guanine derivatives. It was hypothesised that mucus represents hydrophilic barrier while the mucosal epithelial membrane represents lipophilic absorption barrier. For this purpose the permeability ofexamined substances through mucusžmucin dispersions in the equilibrium dialysis cells were studied. On the basis of the results obtained one could anticipate that mucus does not represent a major absorption barrier for examined substances and that the most important are the interactions of mucin molecules with polaržionised groups. The permeation through the mucusžmucin dispersions correlated well with the increasing log P, while negative correlation with the increasing molecular mass of tested substances was observed. Additionally, the application of different side-by-side diffusion cells was also discussed.Type of material - conference contributionPublish date - 2001Language - englishCOBISS.SI-ID - 1015153
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Database name | Field | Year |
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Kristl, Albin | 11122 |
Legen, Igor | 20369 |
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