Разработка и регистрация лекарственных средств (Jan 2019)

Сасо-2 INTESTINAL PERMEABILITY AND Pgp-AFFINITY OF PHOSPHAZIDE

  • D. Yu. Grebenkin,
  • Ya. M. Stanishevskiy,
  • I. E. Shohin,
  • A. M. Stoinova,
  • M. A. Karpova,
  • A. G. Koryakova,
  • A. V. Ryabova,
  • B. V. Brovchenko,
  • A. A. Smirnov

Journal volume & issue
Vol. 0, no. 4
pp. 238 – 242

Abstract

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In this work the intestinal permeability of phospazide in vitro was investigated using Caco-2 cell model in apical-basolateral (A-B) and basolateral-apical (B-A) directions as well as with the option of adding of P-glycoprotein (Pgp) inhibitor cyclosporine A. The following standard substances were used: ranitidine and propranolol. Papp values of test and standard substances were obtained. The obtained data were compared with the values (A) log P for the test and standard substances. According the results of this study, the phosphatide presumably has a low intestinal permeability in terms of BCS. The affinity of phosphazide for the efflux transporter Pgp was demonstrated.

Keywords