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Volumn 336, Issue 2, 2007, Pages 233-240

Intestinal absorption of novel-dipeptide prodrugs of saquinavir in rats

Author keywords

Effective intestinal permeability across rat jejunum (Peff); Intestinal absorption rate constant (ka); Net water flux (NWF); P glycoprotein (P gp); Saquinavir (SQV); Single pass intestinal perfusion (SPIP)

Indexed keywords

CYCLOSPORIN; DIPEPTIDE; GLYCINE; GLYCOPROTEIN P; GLYCYLSARCOSINE; PRODRUG; SAQUINAVIR; VALINE;

EID: 34247567472     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2006.11.058     Document Type: Article
Times cited : (74)

References (36)
  • 1
    • 0031896882 scopus 로고    scopus 로고
    • Active apical secretory efflux of the HIV protease inhibitors saquinavir and ritonavir in Caco-2 cell monolayers
    • Alsenz J., Steffen H., and Alex R. Active apical secretory efflux of the HIV protease inhibitors saquinavir and ritonavir in Caco-2 cell monolayers. Pharm. Res. 15 (1998) 423-428
    • (1998) Pharm. Res. , vol.15 , pp. 423-428
    • Alsenz, J.1    Steffen, H.2    Alex, R.3
  • 2
    • 6344288793 scopus 로고    scopus 로고
    • Pharmacokinetics of novel dipeptide ester prodrugs of acyclovir after oral administration: intestinal absorption and liver metabolism
    • Anand B.S., Katragadda S., and Mitra A.K. Pharmacokinetics of novel dipeptide ester prodrugs of acyclovir after oral administration: intestinal absorption and liver metabolism. J. Pharmacol. Exp. Ther. 311 (2004) 659-667
    • (2004) J. Pharmacol. Exp. Ther. , vol.311 , pp. 659-667
    • Anand, B.S.1    Katragadda, S.2    Mitra, A.K.3
  • 3
    • 23844497838 scopus 로고    scopus 로고
    • Quantitative assessment of HIV-1 protease inhibitor interactions with drug efflux transporters in the blood-brain barrier
    • Bachmeier C.J., Spitzenberger T.J., Elmquist W.F., and Miller D.W. Quantitative assessment of HIV-1 protease inhibitor interactions with drug efflux transporters in the blood-brain barrier. Pharm. Res. 22 (2005) 1259-1268
    • (2005) Pharm. Res. , vol.22 , pp. 1259-1268
    • Bachmeier, C.J.1    Spitzenberger, T.J.2    Elmquist, W.F.3    Miller, D.W.4
  • 5
    • 1442333442 scopus 로고    scopus 로고
    • Characterization of jejunal absorption and apical efflux of ropivacaine, lidocaine and bupivacaine in the rat using in situ and in vitro absorption models
    • Berggren S., Hoogstraate J., Fagerholm U., and Lennernas H. Characterization of jejunal absorption and apical efflux of ropivacaine, lidocaine and bupivacaine in the rat using in situ and in vitro absorption models. Eur. J. Pharm. Sci. 21 (2004) 553-560
    • (2004) Eur. J. Pharm. Sci. , vol.21 , pp. 553-560
    • Berggren, S.1    Hoogstraate, J.2    Fagerholm, U.3    Lennernas, H.4
  • 7
    • 0017184389 scopus 로고
    • A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
    • Bradford M.M. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal. Biochem. 72 (1976) 248-254
    • (1976) Anal. Biochem. , vol.72 , pp. 248-254
    • Bradford, M.M.1
  • 8
    • 0037382316 scopus 로고    scopus 로고
    • In vivo modulation of intestinal CYP3A metabolism by P-glycoprotein: studies using the rat single-pass intestinal perfusion model
    • Cummins C.L., Salphati L., Reid M.J., and Benet L.Z. In vivo modulation of intestinal CYP3A metabolism by P-glycoprotein: studies using the rat single-pass intestinal perfusion model. J. Pharmacol. Exp. Ther. 305 (2003) 306-314
    • (2003) J. Pharmacol. Exp. Ther. , vol.305 , pp. 306-314
    • Cummins, C.L.1    Salphati, L.2    Reid, M.J.3    Benet, L.Z.4
  • 10
    • 0035984821 scopus 로고    scopus 로고
    • GF120918, a P-glycoprotein modulator, increases the concentration of unbound amprenavir in the central nervous system in rats
    • Edwards J.E., Brouwer K.R., and McNamara P.J. GF120918, a P-glycoprotein modulator, increases the concentration of unbound amprenavir in the central nervous system in rats. Antimicrob. Agents Chemother. 46 (2002) 2284-2286
    • (2002) Antimicrob. Agents Chemother. , vol.46 , pp. 2284-2286
    • Edwards, J.E.1    Brouwer, K.R.2    McNamara, P.J.3
  • 11
    • 0029855969 scopus 로고    scopus 로고
    • Comparison between permeability coefficients in rat and human jejunum
    • Fagerholm U., Johansson M., and Lennernas H. Comparison between permeability coefficients in rat and human jejunum. Pharm. Res. 13 (1996) 1336-1342
    • (1996) Pharm. Res. , vol.13 , pp. 1336-1342
    • Fagerholm, U.1    Johansson, M.2    Lennernas, H.3
  • 12
    • 0031024382 scopus 로고    scopus 로고
    • Selective biotransformation of the human immunodeficiency virus protease inhibitor saquinavir by human small-intestinal cytochrome P4503A4: potential contribution to high first-pass metabolism
    • Fitzsimmons M.E., and Collins J.M. Selective biotransformation of the human immunodeficiency virus protease inhibitor saquinavir by human small-intestinal cytochrome P4503A4: potential contribution to high first-pass metabolism. Drug Metab. Dispos. 25 (1997) 256-266
    • (1997) Drug Metab. Dispos. , vol.25 , pp. 256-266
    • Fitzsimmons, M.E.1    Collins, J.M.2
  • 13
    • 0029954843 scopus 로고    scopus 로고
    • P-glycoprotein-a mediator of multidrug resistance in tumour cells
    • Germann U.A. P-glycoprotein-a mediator of multidrug resistance in tumour cells. Eur. J. Cancer 32A (1996) 927-944
    • (1996) Eur. J. Cancer , vol.32 A , pp. 927-944
    • Germann, U.A.1
  • 14
    • 0141430022 scopus 로고    scopus 로고
    • Implications of density correction in gravimetric method for water flux determination using rat single-pass intestinal perfusion technique: a technical note
    • Issa C., Gupta P., and Bansal A.K. Implications of density correction in gravimetric method for water flux determination using rat single-pass intestinal perfusion technique: a technical note. AAPS PharmSciTech 4 (2003) E16
    • (2003) AAPS PharmSciTech , vol.4
    • Issa, C.1    Gupta, P.2    Bansal, A.K.3
  • 15
    • 0033007704 scopus 로고    scopus 로고
    • Effects of intestinal CYP3A4 and P-glycoprotein on oral drug absorption-theoretical approach
    • Ito K., Kusuhara H., and Sugiyama Y. Effects of intestinal CYP3A4 and P-glycoprotein on oral drug absorption-theoretical approach. Pharm. Res. 16 (1999) 225-231
    • (1999) Pharm. Res. , vol.16 , pp. 225-231
    • Ito, K.1    Kusuhara, H.2    Sugiyama, Y.3
  • 16
    • 22844452183 scopus 로고    scopus 로고
    • Circumventing P-glycoprotein-mediated cellular efflux of quinidine by prodrug derivatization
    • Jain R., Majumdar S., Nashed Y., Pal D., and Mitra A.K. Circumventing P-glycoprotein-mediated cellular efflux of quinidine by prodrug derivatization. Mol. Pharm. 1 (2004) 290-299
    • (2004) Mol. Pharm. , vol.1 , pp. 290-299
    • Jain, R.1    Majumdar, S.2    Nashed, Y.3    Pal, D.4    Mitra, A.K.5
  • 17
    • 24944465665 scopus 로고    scopus 로고
    • Evasion of P-gp mediated cellular efflux and permeability enhancement of HIV-protease inhibitor saquinavir by prodrug modification
    • Jain R., Agarwal S., Majumdar S., Zhu X., Pal D., and Mitra A.K. Evasion of P-gp mediated cellular efflux and permeability enhancement of HIV-protease inhibitor saquinavir by prodrug modification. Int. J. Pharm. 303 (2005) 8-19
    • (2005) Int. J. Pharm. , vol.303 , pp. 8-19
    • Jain, R.1    Agarwal, S.2    Majumdar, S.3    Zhu, X.4    Pal, D.5    Mitra, A.K.6
  • 18
    • 0032007325 scopus 로고    scopus 로고
    • Protease inhibitors for the treatment of human immunodeficiency virus infection
    • Kakuda T.N., Struble K.A., and Piscitelli S.C. Protease inhibitors for the treatment of human immunodeficiency virus infection. Am. J. Health Syst. Pharm. 55 (1998) 233-254
    • (1998) Am. J. Health Syst. Pharm. , vol.55 , pp. 233-254
    • Kakuda, T.N.1    Struble, K.A.2    Piscitelli, S.C.3
  • 19
    • 0032518290 scopus 로고    scopus 로고
    • The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors
    • Kim R.B., Fromm M.F., Wandel C., Leake B., Wood A.J., Roden D.M., and Wilkinson G.R. The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors. J. Clin. Invest. 101 (1998) 289-294
    • (1998) J. Clin. Invest. , vol.101 , pp. 289-294
    • Kim, R.B.1    Fromm, M.F.2    Wandel, C.3    Leake, B.4    Wood, A.J.5    Roden, D.M.6    Wilkinson, G.R.7
  • 23
    • 33644692007 scopus 로고    scopus 로고
    • P-glycoprotein recognition of substrates and circumvention through rational drug design
    • Raub T.J. P-glycoprotein recognition of substrates and circumvention through rational drug design. Mol. Pharm. 3 (2006) 3-25
    • (2006) Mol. Pharm. , vol.3 , pp. 3-25
    • Raub, T.J.1
  • 24
    • 0642309504 scopus 로고    scopus 로고
    • Overcoming the blood-brain barrier to taxane delivery for neurodegenerative diseases and brain tumors
    • Rice A., Michaelis M.L., Georg G., Liu Y., Turunen B., and Audus K.L. Overcoming the blood-brain barrier to taxane delivery for neurodegenerative diseases and brain tumors. J. Mol. Neurosci. 20 (2003) 339-343
    • (2003) J. Mol. Neurosci. , vol.20 , pp. 339-343
    • Rice, A.1    Michaelis, M.L.2    Georg, G.3    Liu, Y.4    Turunen, B.5    Audus, K.L.6
  • 25
    • 0036845777 scopus 로고    scopus 로고
    • Transepithelial transport of prodrugs of the HIV protease inhibitors saquinavir, indinavir, and nelfinavir across Caco-2 cell monolayers
    • Rouquayrol M., Gaucher B., Roche D., Greiner J., and Vierling P. Transepithelial transport of prodrugs of the HIV protease inhibitors saquinavir, indinavir, and nelfinavir across Caco-2 cell monolayers. Pharm. Res. 19 (2002) 1704-1712
    • (2002) Pharm. Res. , vol.19 , pp. 1704-1712
    • Rouquayrol, M.1    Gaucher, B.2    Roche, D.3    Greiner, J.4    Vierling, P.5
  • 26
    • 0034126420 scopus 로고    scopus 로고
    • New advances in the transport of doxorubicin through the blood-brain barrier by a peptide vector-mediated strategy
    • Rousselle C., Clair P., Lefauconnier J.M., Kaczorek M., Scherrmann J.M., and Temsamani J. New advances in the transport of doxorubicin through the blood-brain barrier by a peptide vector-mediated strategy. Mol. Pharmacol. 57 (2000) 679-686
    • (2000) Mol. Pharmacol. , vol.57 , pp. 679-686
    • Rousselle, C.1    Clair, P.2    Lefauconnier, J.M.3    Kaczorek, M.4    Scherrmann, J.M.5    Temsamani, J.6
  • 27
    • 0036237761 scopus 로고    scopus 로고
    • Effects of a P-glycoprotein inhibitor on brain and plasma concentrations of anti-human immunodeficiency virus drugs administered in combination in rats
    • Savolainen J., Edwards J.E., Morgan M.E., McNamara P.J., and Anderson B.D. Effects of a P-glycoprotein inhibitor on brain and plasma concentrations of anti-human immunodeficiency virus drugs administered in combination in rats. Drug Metab. Dispos. 30 (2002) 479-482
    • (2002) Drug Metab. Dispos. , vol.30 , pp. 479-482
    • Savolainen, J.1    Edwards, J.E.2    Morgan, M.E.3    McNamara, P.J.4    Anderson, B.D.5
  • 29
    • 0033812228 scopus 로고    scopus 로고
    • Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2
    • Sugawara M., Huang W., Fei Y.J., Leibach F.H., Ganapathy V., and Ganapathy M.E. Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2. J. Pharm. Sci. 89 (2000) 781-789
    • (2000) J. Pharm. Sci. , vol.89 , pp. 781-789
    • Sugawara, M.1    Huang, W.2    Fei, Y.J.3    Leibach, F.H.4    Ganapathy, V.5    Ganapathy, M.E.6
  • 30
    • 0033756459 scopus 로고    scopus 로고
    • Transporter-mediated permeation of drugs across the blood-brain barrier
    • Tamai I., and Tsuji A. Transporter-mediated permeation of drugs across the blood-brain barrier. J. Pharm. Sci. 89 (2000) 1371-1388
    • (2000) J. Pharm. Sci. , vol.89 , pp. 1371-1388
    • Tamai, I.1    Tsuji, A.2
  • 32
    • 0029782485 scopus 로고    scopus 로고
    • Carrier-mediated intestinal transport of drugs
    • Tsuji A., and Tamai I. Carrier-mediated intestinal transport of drugs. Pharm. Res. 13 (1996) 963-977
    • (1996) Pharm. Res. , vol.13 , pp. 963-977
    • Tsuji, A.1    Tamai, I.2
  • 33
    • 0037281280 scopus 로고    scopus 로고
    • Quantitative determination of saquinavir from Caco-2 cell monolayers by HPLC-UV. High performance liquid chromatography
    • Ucpinar S.D., and Stavchansky S. Quantitative determination of saquinavir from Caco-2 cell monolayers by HPLC-UV. High performance liquid chromatography. Biomed. Chromatogr. 17 (2003) 21-25
    • (2003) Biomed. Chromatogr. , vol.17 , pp. 21-25
    • Ucpinar, S.D.1    Stavchansky, S.2
  • 34
    • 0042167430 scopus 로고    scopus 로고
    • P-glycoprotein inhibitors and their screening: a perspective from bioavailability enhancement
    • Varma M.V., Ashokraj Y., Dey C.S., and Panchagnula R. P-glycoprotein inhibitors and their screening: a perspective from bioavailability enhancement. Pharmacol. Res. 48 (2003) 347-359
    • (2003) Pharmacol. Res. , vol.48 , pp. 347-359
    • Varma, M.V.1    Ashokraj, Y.2    Dey, C.S.3    Panchagnula, R.4
  • 35
    • 0342762062 scopus 로고    scopus 로고
    • The barrier function of CYP3A4 and P-glycoprotein in the small bowel
    • Watkins P.B. The barrier function of CYP3A4 and P-glycoprotein in the small bowel. Adv. Drug Deliv. Rev. 27 (1997) 161-170
    • (1997) Adv. Drug Deliv. Rev. , vol.27 , pp. 161-170
    • Watkins, P.B.1
  • 36
    • 0036839699 scopus 로고    scopus 로고
    • Direct evidence that saquinavir is transported by multidrug resistance-associated protein (MRP1) and canalicular multispecific organic anion transporter (MRP2)
    • Williams G.C., Liu A., Knipp G., and Sinko P.J. Direct evidence that saquinavir is transported by multidrug resistance-associated protein (MRP1) and canalicular multispecific organic anion transporter (MRP2). Antimicrob. Agents Chemother. 46 (2002) 3456-3462
    • (2002) Antimicrob. Agents Chemother. , vol.46 , pp. 3456-3462
    • Williams, G.C.1    Liu, A.2    Knipp, G.3    Sinko, P.J.4


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