SummaryBackgroundPotassium‐competitive acid blockers (P‐CABs) are emerging as novel treatments for acid‐related disorders including gastroesophageal reflux disease. Tegoprazan and revaprazan are approved P‐CABs in South Korea, but the pharmacodynamics and safety/tolerability of the two drugs have never been compared.AimsTo evaluate the pharmacodynamics and safety/tolerability of tegoprazan and revaprazan after single and multiple oral dosesMethodsA randomised, open‐label, active‐controlled study was conducted in Helicobacter pylori‐negative healthy Korean male subjects. Tegoprazan 50 mg or revaprazan 200 mg was administered orally, once daily for 7 days; 24‐h intragastric pH monitoring and serum gastrin were measured for pharmacodynamic evaluation. Safety parameters including serum microRNA‐122 (miR‐122) level were also collected.ResultsAfter a single dose, the %Time pH ≥4 for tegoprazan was greater than that for revaprazan (54.5% vs 25.1%). After multiple doses, the %Time pH ≥4 for tegoprazan was also greater than that for revaprazan (68.2% vs 25.3%). %Time pH ≥4 during 12 hours at nighttime for tegoprazan was greater than that for revaprazan (71.8% vs 31.9%). The changes in the serum gastrin were not clinically significant for either drug. Despite the slight increases of serum miR‐122 for each drug, tegoprazan and revaprazan were well tolerated considering other safety parameters including AST and ALT levels.ConclusionTegoprazan 50 mg showed stronger gastric acid suppression than revaorazan 200 mg. Both drugs were well tolerated.
Natural protopanaxadiol ginsenosides exhibit low absorption in the human intestine. However, ginsenoside compound K (CK) with 1 conjugated glucose molecule exhibits favorable absorption. The purpose of this study was to compare the pharmacokinetics of ginsenoside CK from a CK fermentation product, CK‐30, and from a red ginseng extract. A randomized, open‐label, 2‐treatment, 2×2 crossover study was conducted. The volunteers were randomly divided into 2 groups. One group received CK‐30, and the other group received 2.94 g of a red ginseng extract. After a 7‐day washout period, the subjects received an alternative treatment for a single dose. The pharmacokinetic parameters, including the maximum plasma concentration (Cmax) and area under the plasma concentration–time curve from time 0 to time of last measurable concentration, were calculated. The median time to reach Cmax of ginsenoside CK after administration of CK‐30 was 3.0 hours, whereas the corresponding value of the red ginseng extract was 10.0 hours. Compared with the red ginseng extract, CK‐30 resulted in a higher systemic exposure to ginsenoside CK, with a 118.3‐fold increase in Cmax and a 135.1‐fold increase in area under the plasma concentration–time curve from time 0 to time of last measurable concentration. The systemic exposure to ginsenoside CK was significantly higher after administration of CK‐30 than red ginseng extract.
Background
Esomeprazole, a proton pump inhibitor (PPI), is widely used to treat acid-related disorders, but it has short plasma half-life which can cause insufficient gastric acid suppression, such as nocturnal acid breakthrough. A new dual delayed-release (DR) formulation of esomeprazole (Esomezol DR), was developed to extend the duration of gastric acid suppression.
Purpose
This study aimed to evaluate the pharmacokinetics (PKs) and pharmacodynamics (PDs) of esomeprazole for the DR formulation compared to a conventional enteric-coated (EC) formulation (Nexium) in healthy male subjects.
Methods
Two randomized, open-label, multiple-dose, two-way crossover studies with esomeprazole 20 mg and 40 mg were conducted. Subjects received the DR formulation or the EC formulation once daily for 7 days in each period with a 7-day washout. Serial blood samples were collected up to 24 hours after the 1st dose, and 24-hour intragastric pH was continuously monitored before the 1st dose as baseline and after the 1st and the 7th dose.
Results
In 20 mg and 40 mg dose groups, 38 and 44 subjects completed the study, respectively. The DR formulation exhibited the dual-release pattern of esomeprazole, resulting in more sustained plasma concentration–time profiles compared to the EC formulation. The systemic exposure of esomeprazole for the DR formulation was comparable to that for the EC formulation, showing the similar area under the plasma concentration–time curve. The 24-hour gastric acid suppression was also similar between the two formulations, while the inhibition during night-time (22:00–06:00) showed a better tendency in the DR formulation.
Conclusion
The sustained exposure of esomeprazole in the DR formulation led to well-maintained and higher acid inhibition compared to the EC formulation, especially during the night-time. These results suggest that the DR formulation can be an alternative formulation to the conventional EC formulation, expecting the potential of relieving nocturnal acid-related symptoms.
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