Effect of meal timing on pharmacokinetics and pharmacodynamics of tegoprazan in healthy male volunteers

Autor: Bong Tae Kim, Naree Shin, Jung Sunwoo, In-Jin Jang, Geun Seog Song, Deok Yong Yoon, Ah Rong Kim, Seunghwan Lee
Rok vydání: 2020
Předmět:
Male
030213 general clinical medicine
Time Factors
Administration
Oral
Pharmacology
030226 pharmacology & pharmacy
law.invention
Food-Drug Interactions
0302 clinical medicine
law
Benzene Derivatives
Medicine
General Pharmacology
Toxicology and Pharmaceutics
Meals
Meal
Cross-Over Studies
Clinical pharmacology
General Neuroscience
digestive
oral
and skin physiology
Imidazoles
Articles
Fasting
General Medicine
PK Parameters
Healthy Volunteers
Fasted state
Area Under Curve
Gastroesophageal Reflux
Antacids
Public aspects of medicine
RA1-1270
Adult
Single administration
Peptic Ulcer
Biological Availability
RM1-950
Absorption (skin)
Ph monitoring
Article
General Biochemistry
Genetics and Molecular Biology
Gastric Acid
03 medical and health sciences
Pharmacokinetics
Humans
business.industry
Research
Crossover study
Pharmacodynamics
Gastric acid
Therapeutics. Pharmacology
business
Zdroj: Clinical and Translational Science, Vol 14, Iss 3, Pp 934-941 (2021)
Clinical and Translational Science
Popis: Tegoprazan, a novel potassium‐competitive acid blocker, is used to treat acid‐related diseases. However, there is no information on the pharmacokinetic (PK) and pharmacodynamic (PD) profiles of the marketed dosage of tegoprazan under various meal timings in a fed and fasted state. The study aimed to assess the effect of meal timing on PKs and PDs of tegoprazan 50 mg after a single administration in healthy male subjects. An open‐label, single‐dose, three‐treatment, three‐period crossover study was conducted. A total of 12 subjects were orally administered a single dose of tegoprazan 50 mg among various conditions: in a fasted state, at 30 min before or 30 min after a high‐fat meal. PK parameters were estimated by the noncompartmental method. Continuous 24‐h intragastric pH monitoring was done for PD analysis. The PKs and PDs of tegoprazan were compared among the various meal timings. Compared with the fasting condition, the PK profile of tegoprazan was similar when administered 30 min before a high‐fat meal; however, delayed absorption with similar systemic exposure was observed when administered 30 min after a high‐fat meal. The magnitude of acid suppression evaluated through the PD parameters increased when administered 30 min after a high‐fat meal compared with fasting the condition and when administered 30 min before a high‐fat meal. However, the increased difference in acid suppression was not clinically significant. Meal timing had no clinically significant effect on the PKs and PDs of tegoprazan 50 mg. Therefore, the marketed dosage of tegoprazan could be administered regardless of the meal timing. Study Highlights WHAT IS THE CURRENT KNOWLEDGE ON THE TOPIC? Tegoprazan, a novel potassium‐competitive acid blocker, is used to treat acid‐related diseases. WHAT QUESTION DID THIS STUDY ADDRESS? This study evaluated the effect of food on pharmacokinetics (PKs) and pharmacodynamics (PDs) of tegoprazan under various mealtime conditions. WHAT DOES THIS STUDY ADD TO OUR KNOWLEDGE? This study showed that delayed absorption of tegoprazan was observed at “after meal condition,” however, the amount of systemic exposure of “after meal condition” was similar to “fasting condition” and “before meal condition.” In addition, gastric acid suppression of tegoprazan was similar between fasting condition and before meal condition, whereas increased gastric acid suppression was observed at after meal condition. HOW MIGHT THIS CHANGE CLINICAL PHARMACOLOGY OR TRANSLATIONAL SCIENCE? In the actual clinical environment, patients take medicine under various fed conditions. This study evaluated the effect of food on PKs and PDs of tegoprazan in various clinical conditions, and provided the important information about meal timing when administering tegoprazan.
Databáze: OpenAIRE
Externí odkaz: