Related Experiment Video
Updated: Nov 6, 2025
07:00
Mechanisms Underlying Gut Hormone Secretion Using the Isolated Perfused Rat Small Intestine
Published on: February 26, 2019
9.8K
Intestinal Absorption of Alogliptin Is Mediated by a Fruit-Juice-Sensitive Transporter
Kaori Morimoto1, Momona Sasaki1, Erika Oikawa1
1Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University.
Biological & Pharmaceutical Bulletin
|May 6, 2021
Summary
Alogliptin, a diabetes drug, is absorbed via a carrier-mediated process in the intestine. This absorption is inhibited by fruit juices, suggesting a transporter other than OATP2B1 is involved.
Area of Science:
- Pharmacology
- Drug Metabolism and Transport
Background:
- Alogliptin (ALG) is a dipeptidylpeptidase-4 inhibitor for type 2 diabetes.
- ALG exhibits high oral absorption (>60-71%) despite low lipophilicity (logP=-1.4).
Purpose of the Study:
- To elucidate the intestinal absorption mechanism of Alogliptin.
- To identify the specific transporters involved in ALG absorption.
Main Methods:
- In vitro studies using Caco-2 cells and HEK293 cells overexpressing OATP2B1.
- Inhibition assays with known transporter substrates and inhibitors.
- In vivo studies in rats using apple juice intervention.
Main Results:
- ALG uptake in Caco-2 cells was time-, temperature-, and concentration-dependent, not saturable up to 10 mmol/L.
- Uptake was inhibited by OATP inhibitors (fexofenadine, DIDS) and fruit juices, but not by OCT/OCTN or PEPT1 substrates.
- No difference in ALG uptake was observed in HEK293 cells overexpressing OATP2B1.
- Apple juice reduced oral ALG systemic exposure in rats.
Conclusions:
- Alogliptin intestinal absorption is carrier-mediated.
- A fruit-juice-sensitive transporter, distinct from OATP2B1, is likely involved in ALG absorption.
Related Concept Videos
01:26Glucose Absorption Into the Small Intestine
33.6K
Complex carbohydrates consumed cannot be absorbed into the small intestine in their original form. First, they must be hydrolyzed to a monosaccharide form such as glucose or galactose. These monosaccharides are then transported across the intestinal membrane and into the blood via transcellular transport. The intestinal epithelial cells allow the movement of these monosaccharides with a defined 'entry' through membrane transporter proteins present on their apical membrane and...
33.6K
01:19Drug Absorption: Factors Affecting GI Absorption
5.4K
The process of oral drug absorption can be influenced by several factors. Weakly acidic drugs tend to be absorbed more readily from the stomach due to their nonionized state. However, absorption may be less efficient in the upper intestine, where drugs are often ionized. Interestingly, despite the stomach's apparent advantage for drug absorption, its mucous layer can hinder diffusion. Its surface area is also smaller than the intestine's, which can further slow down the absorption rate.
5.4K
01:06Carrier-Mediated Transport
722
Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
722
01:17Drug Absorption: Overview
1.2K
The process of drug absorption signifies the transition of a drug from its site of administration into the plasma. This process is influenced by various factors, including the route of administration, the anatomy of the absorption site, the mechanism of absorption, gut motility, and the drug's physicochemical properties.
When drugs are injected intravenously, they directly enter the systemic circulation. Alternatively, orally administered drugs navigate through the gastrointestinal (GI)...
When drugs are injected intravenously, they directly enter the systemic circulation. Alternatively, orally administered drugs navigate through the gastrointestinal (GI)...
1.2K
01:23Factors Influencing Drug Absorption: Anatomical Parameters
389
Drug absorption involves the movement of drugs from the point of administration into the systemic circulation. Initially, Gastrointestinal (GI) motility propels the drug through the digestive tract and into the stomach. However, the stomach's high acidity and limited surface area restrict its role in drug absorption for most drugs. The drug then moves from the stomach to the small intestine via gastric emptying, which can be slowed by various factors, including interactions with other...
389
01:25Carbohydrate Absorption
2.1K
Carbohydrates are essential macronutrients that serve as the body's primary energy source. Their digestion begins in the mouth, where salivary amylase partially breaks down complex carbohydrates such as starch into smaller oligosaccharides. This mechanical and enzymatic activity prepares carbohydrates for further processing in the gastrointestinal tract.
After being swallowed, the partially digested carbohydrates mix with gastric secretions in the stomach. However, the acidic environment...
After being swallowed, the partially digested carbohydrates mix with gastric secretions in the stomach. However, the acidic environment...
2.1K