scholarly journals In Situ Absorption Study of Acebutolol by Modulating P-glycoprotein with Verapamil in Rats

2019 ◽  
Vol 0 (0) ◽  
pp. 0-0
Author(s):  
Issam Mohammed Abushammala ◽  
Elham Abed Abuwaked ◽  
Hanan Mohammed Fayyad ◽  
Ahmed Fadel Elqedra ◽  
Mai Abdelrahman Ramadan ◽  
...  
2020 ◽  
Vol 17 (6) ◽  
pp. 673-678
Author(s):  
Issam Mohammed ABUSHAMMALA ◽  
Elham Abed ABUWAKED ◽  
Hanan Mohammed FAYYAD ◽  
Ahmed Fadel ELQEDRA ◽  
Mai Abdelrahman RAMADAN ◽  
...  

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Xiaoyu Sun ◽  
Shunxiong Tang ◽  
Binbin Hou ◽  
Zhijun Duan ◽  
Zhen Liu ◽  
...  

Abstract Background Portal hypertension (PH) is the main cause of complications and death in liver cirrhosis. The effect of oral administration of octreotide (OCT), a drug that reduces PH by the constriction of mesenteric arteries, is limited by a remarkable intestinal first-pass elimination. Methods The bile duct ligation (BDL) was used in rats to induce liver cirrhosis with PH to examine the kinetics and molecular factors such as P-glycoprotein (P-gp), multidrug resistance-associated protein 2 (MRP2) and cytochrome P450 3A4 (CYP3A4) influencing the intestinal OCT absorption via in situ and in vitro experiments on jejunal segments, transportation experiments on Caco-2 cells and experiments using intestinal microsomes and recombinant human CYP3A4. Moreover, RT-PCR, western blot, and immunohistochemistry were performed. Results Both in situ and in vitro experiments in jejunal segments showed that intestinal OCT absorption in both control and PH rats was largely controlled by P-gp and, to a lesser extent, by MRP2. OCT transport mediated by P-gp and MRP2 was demonstrated on Caco-2 cells. The results of RT-PCR, western blot, and immunohistochemistry suggested that impaired OCT absorption in PH was in part due to the jejunal upregulation of these two transporters. The use of intestinal microsomes and recombinant human CYP3A4 revealed that CYP3A4 metabolized OCT, and its upregulation in PH likely contributed to impaired drug absorption. Conclusions Inhibition of P-gp, MRP2, and CYP3A4 might represent a valid option for decreasing intestinal first-pass effects on orally administered OCT, thereby increasing its bioavailability to alleviate PH in patients with cirrhosis.


2011 ◽  
Vol 58 (04) ◽  
pp. 188-192
Author(s):  
Parvin Zakeri-Milani ◽  
Hadi Valizadeh ◽  
Ziba Islambulchilar ◽  
Sanaz Damani ◽  
Maryam Mehtari

1985 ◽  
Vol 156 ◽  
pp. A323-A324
Author(s):  
G. Tourillon ◽  
E. Dartyge ◽  
H. Dexpert ◽  
A. Fontaine ◽  
A. Jucha ◽  
...  

1986 ◽  
Vol 38 (S12) ◽  
pp. 37P-37P
Author(s):  
J. Bell ◽  
G. E. Peters ◽  
C. McMartin ◽  
N. W. Thomas ◽  
C. G. Wilson

2019 ◽  
Vol 3 (12) ◽  
pp. 3399-3405
Author(s):  
Jenny Reichert ◽  
Stephanie Maerten ◽  
Katharina Meltzer ◽  
Alexander Tremel ◽  
Manfred Baldauf ◽  
...  

A promising way to increase the methanol yields in CO2 hydrogenation significantly up to 60% by in situ sorption of methanol and water in alkali salt-doped ionic liquids (ILs) is demonstrated.


1992 ◽  
Vol 61 (6) ◽  
pp. 2160-2160
Author(s):  
Toshinori Iwasa ◽  
Tsuyoshi Kawai ◽  
Mitsuyoshi Onoda ◽  
Jyunzo Nakayama ◽  
Hiroo Nakahara ◽  
...  

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