cover
Article Per Year (5 Year)
All
Home Page
OAI Link
Editorial Team
Contact
Reviewer
Google Scholar
Contact Name
-
Contact Email
-
Phone
-
Journal Mail Official
-
Editorial Address
-
Location
Kab. sleman,
Daerah istimewa yogyakarta
INDONESIA
INDONESIAN JOURNAL OF PHARMACY
Published by Universitas Gadjah Mada
ISSN : 23389427     EISSN : 23389486     DOI : -
Core Subject : Health,
Medicine & Pharmacology
Indonesian Journal of Pharmacy (ISSN-e: 2338-9486, ISSN-p: 2338-9427), formerly Majalah Farmasi Indonesia (ISSN: 0126-1037). The journal had been established in 1972, and online publication was begun in 2008. Since 2012, the journal has been published in English by Faculty of Pharmacy Universitas Gadjah Mada (UGM) Yogyakarta Indonesia in collaboration with IAI (Ikatan Apoteker Indonesia or Indonesian Pharmacist Association) and only receives manuscripts in English. Indonesian Journal of Pharmacy is Accredited by Directorate General of Higher Education (DGHE) DIKTI No. 58/DIKTI/Kep/2013.
Arjuna Subject : -
Articles 1 Documents
 1 
Search results for , issue " Vol 27 No 3, 2016" : 1 Documents clear
INFLUENCE OF POMEGRANATE JUICE ON THE CYP3A4-MEDIATED METABOLISM AND P-GLYCOPROTEIN MEDIATED TRANSPORT OF SAQUINAVIR IN VIVO AND EX VIVO MODELS Vemulapalli, Sridhar
INDONESIAN JOURNAL OF PHARMACY Vol 27 No 3, 2016
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (800.658 KB) | DOI: 10.14499/indonesianjpharm27iss3pp152

Abstract

Cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp) play an important role in the first pass metabolism thereby limits the oral bioavailability of many clinically important and frequently prescribed drugs. The absolute oral bioavailability of saquinavir is very low (i. e. 4%) due to its extensive first pass metabolism by the major metabolizing isozyme CYP3A4 and it is also a substrate of P-gp. Pomegranate juice (PGJ) was known to be a modulator of CYP3A4 and P-gp. Therefore, the aim of this study was to evaluate the influence of PGJ on the pharmacokinetics (PK) of saquinavir in wistar rats and on the P-gp mediated intestinal transport of saquinavir in everted gut sacs ex vivo.  Rats were treated orally with saquinavir (100 mg/kg) alone and in combination with PGJ (0.5, 1.0 and 2.0 mL/200g, body weight) for 15 consecutive days. Blood samples were collected on 1st day in single dose pharmacokinetic study (SDS) and on 15th day in multiple dose pharmacokinetic study (MDS). The peak plasma concentration (Cmax)and area under the plasma concentration-time curve (AUC0-24) of saquinavir was increased with PGJ in SDS (p<0.001) may be due to inhibition of CYP3A4 and P-gp. But interestingly, the Cmax and AUC0-24 of saquinavir was decreased significantly with PGJ in MDS. This is may be due to induction of CYP3A4. The transport of saquinavir was increased in presence of PGJ and known P-gp inhibitors (Verapamil, Ketoconazole and Quinindine) across the rat everted gut sacs ex vivo. The present study results suggested that PGJ has both effects (inhibition, in SDS and induction, in MDS) on CYP3A4-mediated saquinavir metabolism in vivo and inhibitory effect on the P-gp mediated intestinal transport of saquinavir ex vivo. Further studies are needed to confirm this interaction at cellular level using cell lines and in humans.

Page 1 of 1 | Total Record : 1

 1 

Filter by Year

2016 2016


Reset
Filter By Issues
All Issue Vol 31 No 2, 2020 Vol 31 No 1, 2020 Vol 31 No 1, 2020 In Press Vol 30 No 4, 2019 Vol 30 No 3, 2019 Vol 30 No 2, 2019 Vol 30 No 2, 2019 Vol 30 No 1, 2019 Vol 30 No 1, 2019 Vol 29 No 4, 2018 Vol 29 No 4, 2018 Vol 29 No 3, 2018 Vol 29 No 3, 2018 Vol 29 No 2, 2018 Vol 29 No 1, 2018 Vol 28 No 4, 2017 Vol 28 No 4, 2017 Vol 28 No 3, 2017 Vol 28 No 3, 2017 Vol 28 No 2, 2017 Vol 28 No 2, 2017 Vol 28 No 1, 2017 Vol 27 No 4, 2016 Vol 27 No 4, 2016 Vol 27 No 3, 2016 Vol 27 No 3, 2016 Vol 27 No 2, 2016 Vol 27 No 2, 2016 Vol 27 No 1, 2016 Vol 27 No 1, 2016 Vol 26 No 4, 2015 Vol 26 No 4, 2015 Vol 26 No 3, 2015 Vol 26 No 3, 2015 Vol 26 No 2, 2015 Vol 26 No 1, 2015 Vol 26 No 1, 2015 Vol 25 No 4, 2014 Vol 25 No 4, 2014 Vol 25 No 3, 2014 Vol 25 No 3, 2014 Vol 25 No 2, 2014 Vol 25 No 1, 2014 Vol 25 No 1, 2014 Vol 24 No 4, 2013 Vol 24 No 4, 2013 Vol 24 No 3, 2013 Vol 24 No 3, 2013 Vol 24 No 2, 2013 Vol 24 No 2, 2013 Vol 24 No 1, 2013 Vol 24 No 1, 2013 Vol 23 No 4, 2012 Vol 23 No 3, 2012 Vol 23 No 2, 2012 Vol 23 No 2, 2012 Vol 23 No 1, 2012 Vol 23 No 1, 2012 Vol 22 No 4, 2011 Vol 22 No 4, 2011 Vol 22 No 3, 2011 Vol 22 No 3, 2011 Vol 22 No 2, 2011 Vol 22 No 2, 2011 Vol 22 No 1, 2011 Vol 21 No 4, 2010 Vol 21 No 4, 2010 Vol 21 No 3, 2010 Vol 21 No 2, 2010 Vol 21 No 2, 2010 Vol 21 No 1, 2010 Vol 21 No 1, 2010 Vol 20 No 4, 2009 Vol 20 No 4, 2009 Vol 20 No 3, 2009 Vol 20 No 3, 2009 Vol 20 No 2, 2009 Vol 20 No 1, 2009 Vol 20 No 1, 2009 Vol 19 No 4, 2008 Vol 19 No 3, 2008 Vol 19 No 3, 2008 Vol 19 No 2, 2008 Vol 19 No 1, 2008 Vol 19 No 1, 2008 Vol 18 No 4, 2007 Vol 18 No 3, 2007 Vol 18 No 3, 2007 Vol 18 No 2, 2007 Vol 18 No 1, 2007 Vol 17 No 4, 2006 Vol 17 No 3, 2006 Vol 17 No 3, 2006 Vol 17 No 2, 2006 Vol 17 No 2, 2006 Vol 17 No 1, 2006 Vol 17 No 1, 2006 Vol 16 No 4, 2005 Vol 16 No 4, 2005 Vol 16 No 3, 2005 Vol 16 No 2, 2005 Vol 16 No 2, 2005 Vol 16 No 1, 2005 Vol 16 No 1, 2005 Vol 15 No 4, 2004 Vol 15 No 4, 2004 Vol 15 No 3, 2004 Vol 15 No 2, 2004 Vol 15 No 2, 2004 Vol 15 No 1, 2004 Vol 15 No 1, 2004 Vol 14 No 4, 2003 Vol 14 No 3, 2003 Vol 14 No 2, 2003 Vol 14 No 1, 2003 Vol 14 No 1, 2003 Vol 13 No 4, 2002 Vol 13 No 4, 2002 Vol 13 No 3, 2002 Vol 13 No 3, 2002 Vol 13 No 2, 2002 Vol 13 No 2, 2002 Vol 13 No 1, 2002 Vol 12 No 4, 2001 Vol 12 No 4, 2001 Vol 12 No 3, 2001 Vol 12 No 2, 2001 Vol 12 No 2, 2001 Vol 12 No 1, 2001 Vol 12 No 1, 2001 More Issue