Docosahexaenoic acid (DHA) inhibits saquinavir metabolism in-vitro and enhances its bioavailability in rats

Journal of Pharmacy and Pharmacology

Volumn 58, Issue 5, 2006, Pages 651-658

  Hirunpanich, Vilasinee ^a   Sato, Hitoshi ^b  

^a MAHASARAKHAM UNIVERSITY   (Thailand)

^b SHOWA UNIVERSITY   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450 3A; DOCOSAHEXAENOIC ACID; ERYTHROMYCIN; KETOCONAZOLE; SAQUINAVIR;

ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG HALF LIFE; DRUG INHIBITION; DRUG METABOLISM; IN VITRO STUDY; INTESTINE; LIVER MICROSOME; MALE; NONHUMAN; RAT;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CYTOCHROME P-450 CYP3A; DOCOSAHEXAENOIC ACIDS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; ENZYME INHIBITORS; HIV PROTEASE INHIBITORS; INJECTIONS, INTRAVENOUS; INTESTINES; MALE; MICROSOMES, LIVER; RATS; RATS, WISTAR; SAQUINAVIR;

EID: 33646458518     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/jpp.58.5.0010     Document Type: Article

References (20)

1. Benet, L. Z., Izumi, T., Zhang, Y., Silverman, J. A., Wacher, V. J. (1999) Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery. J. Control. Release 62: 25-31
2. Benet, L. Z., Cummins, C. L., Wu, C. Y. (2004) Unmasking the dynamic interplay between efflux transporters and metabolic enzymes. Int. J. Pharm. 277: 3-9
3. Busnach, G., Stragliotto, E., Minetti, E., Perego, A., Brando, B., Broggi, M. L., Civati, G. (1998) Effect of n-3 polyunsaturated fatty acids on cyclosporine pharmacokinetics in kidney graft recipients: a randomized placebo-controlled study. J. Nephrol. 11: 87-93
4. Eagling, V. A., Back, D. J., Barry, M. G. (1997) Differential inhibition of cytochrome P450 isoforms by the protease inhibitors, ritonavir, saquinavir and indinavir. Br. J. Clin. Pharmacol. 44: 190-194
5. Eagling, V. A., Profit, L., Back, D. J. (1999) Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-1 protease inhibitor saquinavir by grapefruit juice components. Br. J. Clin. Pharmacol. 48: 543-552
6. Fitzsimmons, M. E., Collins, J. M. (1997) 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: 256-266
7. Hayes, K. A., Brennen, B., Chenery, R., Houston, J. B. (1995) In vivo disposition of caffeine predicted from hepatocyte data. Drug Metab. Dispos. 23: 349-353
8. Hirunpanich, V., Kataki, J., Sethabouppha, B., Sato, H. (2006) Demonstration of docosahexaenoic acid (DHA) as a bioavailability enhancer for CYP3A substrates: in vitro and in vivo evidence using cyclosporine in rats. Drug Metab. Dispos. 34: 305-310
9. Horrocks, L. A., Yeo, Y. K. (1999) Health benefits of docosahexaenoic acid (DHA) Pharm. Res. 40: 211-225
10. Kupferschmidt, H. H., Fattinger, K. E., Ha, H. R., Follath, F., Krahenbuhl, S. (1998) Grapefruit juice enhances the bioavailability of the HIV protease inhibitor saquinavir in man. Br. J. Clin. Pharmacol. 45: 355-359
11. Liu, Q. Y., Tan, B. K. (2000) Effects of cis-unsaturated fatty acids on doxorubicin sensitivity in P388/DOX resistant and P388 parental cell lines. Life Sci. 67:1207-1218
12. Lown, K. S., Bailey, D. G., Fontana, R. J., Janardan, S. K., Adair, C. H., Fortlage, L. A., Brown, M. B., Guo, W., Watkins, P. B. (1997) Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. J. Clin. Invest. 99: 2545-2553
13. Lowry, O. H., Rosebrough, N. J., Farr, A. L., Randall, R. J. (1951) Protein measurement with the Polin phenol reagent. J. Biol. Chem. 193: 265-275
14. Martin-Facklam, M., Burhenne, J., Ding, R., Fricker, R., Mikus, G., Walter-Sack, I., Haefeli, W. E. (2002) Dose-dependent increase of saquinavir bioavailability by the pharmaceutic aid, cremophor EL. Br. J. Clin. Pharmacol. 53: 576-581
15. Noble, S., Faulds, D. (1996) Saquinavir. A review of its pharmacology and clinical potential in the management of HIV infection. Drugs 52: 93-112
16. Pereira de Oliveira, M., Olivier, J. C., Pariat, C., Roche, D., Greiner, J., Vierling, P., Couet, W. (2005) Investigation of oral bioavailability and brain distribution of the Ind(8)-Val conjugate of indinavir in rodents. J. Pharm. Pharmacol. 57: 453-458
17. Wacher, V. J., Silverman, J. A., Zhang, Y., Benet, L. Z. (1998) Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics. J. Pharm. Sci. 87: 1322-1330
18. Walson, P. D., Cox, S., Utkin, I., Gerber, N., Crim, L., Brady, M., Koranyi, K. (2003) Clinical use of a simultaneous HPLC assay for indinavir, saquinavir, ritonavir, and nelfinavir in children and adults. Ther. Drug Monit. 25: 588-592
19. Yamaji, H., Matsumura, Y., Yoshikawa, Y., Takada, K. (1999) Pharmacokinetic interactions between HIV-protease inhibitors in rats. Biopharm. Drug Dispos. 20: 241-247
20. Zhou, S., Yung Chan, S., Cher Goh, B., Chan, E., Duan, W., Huang, M., McLeod, H. L. (2005) Mechanism-based inhibition of cytochrome P450 3A4 by therapeutic drugs. Clin. Pharmacokinet. 44: 279-304