Pharmacokinetics and Pharmacodynamics of Esomeprazole/Sodium Bicarbonate Immediate-Release Capsules in Healthy Chinese Volunteers: A Cross-Over, Randomized Controlled Trial

Shan, Jing; Zhu, Yi; Liu, Wenfang; Yang, Kexu; Hu, Lili; Deng, Dan; Lu, Chin‐Song; Yang, Lin

doi:10.1007/s12325-021-01644-7

Cited by 7 publications

(12 citation statements)

References 45 publications

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“…Percent decrease from baseline in the integrated acidity was used as a parameter for comparing the PD effects in previous studies. 15 , 16 , 34 It compares the acidity of the baseline and after a single- or multiple-dose. Considering that only about 2/3 of the proton pumps are inhibited after a single PPI dose, anticipation of the variability of the parameter after a single-dose was expected to be demanding.…”

Section: Discussionmentioning

confidence: 99%

“…In previous studies, 800 mg and 1100 mg of NaHCO 3 were used compared to only 600 mg of CaCO 3 in AD-206. 15 , 16 Development of fixed dose combination medication with smaller size is expected to improve patients’ compliance and adherence.…”

Section: Discussionmentioning

confidence: 99%

“…14 Since its successful launch, there have been efforts to develop a combination of various PPIs with various antacid salts. 15,16 AD-206 is a fixed-dose combination of esomeprazole with 600 mg of calcium carbonate (CaCO 3 ) developed by Addpharma Pharmaceutical Corp, Korea. This is the first fixed dose combination of PPI with CaCO 3 as the antacid counterpart.…”

Section: Introductionmentioning

confidence: 99%

“… 14 Since its successful launch, there have been efforts to develop a combination of various PPIs with various antacid salts. 15 , 16 …”

Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

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Comparative Pharmacokinetics/Pharmacodynamics of Fixed-Dose Combination of Esomeprazole and Calcium Carbonate (AD-206) to the Conventional Esomeprazole

Bae¹,

Kwon²,

Lee³

et al. 2021

DDDT

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Purpose: Proton pump inhibitors (PPIs) are used for the treatment of acid-related disorders. Demands for enhanced stability and faster onset led to the development of AD-206, a fixeddose combination of a PPI (esomeprazole) with an antacid salt (calcium carbonate). This study compared the pharmacokinetics (PKs) and pharmacodynamics (PDs) of AD-206 (Addpharma) with conventional esomeprazole (Nexium ® , AstraZeneca). Materials and Methods:A randomized, open-label, two-treatment, two-sequence crossover study was conducted with 2 different doses of esomeprazole at 20 and 40 mg with a fixed calcium carbonate dose of 600 mg in AD-206. Forty-four subjects were included in each dose group and randomly received either AD-206 or the conventional esomeprazole for 7 consecutive days in each period. After a single-and multiple-dose, blood samples for the PK analysis were analyzed, and 24-hour intragastric pH monitoring was conducted. Results:The systemic exposure of esomeprazole after a multiple-dose of AD-206 was similar to that of the conventional esomeprazole in both doses, but the time to reach the peak concentration was faster in AD-206. The percentage decrease from baseline in the integrated gastric acidity for a 24-hour interval after the dose was not significantly different between the AD-206 and the conventional esomeprazole after a single-and multiple-dose for both doses, and the time to reach pH 4 was faster for AD-206. Conclusion: AD-206 showed a similar systemic exposure and suppression of gastric acid secretion after a multiple-dose compared to the conventional esomeprazole.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

“… 14 Since its successful launch, there have been efforts to develop a combination of various PPIs with various antacid salts. 15 , 16 …”

Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

See 3 more Smart Citations

Comparative Pharmacokinetics/Pharmacodynamics of Fixed-Dose Combination of Esomeprazole and Calcium Carbonate (AD-206) to the Conventional Esomeprazole

Bae¹,

Kwon²,

Lee³

et al. 2021

DDDT

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Pharmacokinetics and Pharmacodynamics of Lansoprazole/Sodium Bicarbonate Immediate‐release Capsules in Healthy Chinese Subjects: An Open, Randomized, Controlled, Crossover, Single‐, and Multiple‐dose Trial

Li-xiu

Zhai

et al. 2023

Clinical Pharm in Drug Dev

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Proton pump inhibitors (PPIs) differ in onset of action and bioavailability. This trial was conducted to investigate the pharmacokinetics and pharmacodynamics of an immediate‐release capsule formulation containing lansoprazole 30 mg and sodium bicarbonate 1100 mg (T preparation) in healthy Chinese subjects. This was an open, single‐center, randomized, single and multiple oral doses, and two‐period crossover study in 30 healthy subjects. After single‐ and multiple‐dose oral administration, blood samples were obtained and lansoprazole concentration in serum was measured for pharmacokinetic analysis. Meanwhile, the intragastric pH was monitored continuously to evaluate the pharmacodynamics of the investigational drugs. The Tmax of the T preparation was 0.5 hours, while the Tmax of the R preparation was 1.5 hours after multiple doses, which indicated that the absorption speed of the T preparation was significantly faster than that of the R preparation. The same characteristics also existed after single‐dose administration. The area under the curve (AUC)ss of the T preparation was bio‐equivalent to that of the R preparation under steady state. The time percentage of intragastric pH > 4.0 for the T preparation was higher than that of the R preparation after 1 hour for both single‐ and multiple‐dose. It suggested compared with R preparation, the time percentage of intragastric pH > 4.0 met the criteria for superiority after 1 hour administration for the T preparation. In addition, no serious adverse events occurred in this study. Across this study, the T preparation was better than the R preparation at improving drug absorption and increasing intragastric pH, and had a favorable safety profile.

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Pharmacokinetics and bioequivalence evaluation of omeprazole and sodium bicarbonate dry suspensions in healthy Chinese volunteers

Zhang

Guo

Zhou

et al. 2023

Sci Rep

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Omeprazole and sodium bicarbonate dry suspension are effective treatments for acid-related disorders. This study compared the bioequivalence and safety of the two formulations of omeprazole and sodium bicarbonate powder and assessed how CYP2C19 gene polymorphisms affect pharmacokinetics (PK). A single-center, randomized, single-dose, 2-sequence and 2-period crossover method was performed in forty healthy Chinese subjects. Blood samples were collected after a single dose for PK (AUC0–∞, AUC0–t, and Cmax) analysis. The concentrations of Omeprazole in human plasma were determined by HPLC–MS/MS. Besides, the gene polymorphisms of CYP2C19 were assessed by Sanger sequencing. The geometric mean ratios (90% confidence interval) [GMR (95% CI)] of Test/Reference preparation for Cmax: 95.2% (88.48%, 102.43%), AUC0–t: 97.47% (94.4%, 101.02%), AUC0–∞: 97.68% (94.27%, 101.21%) were within the range of 80.00–125.00%. The non-parametric test showed no statistical difference in Tmax between the two groups (p > 0.05). All drugs were well tolerated, no severe adverse reactions occurred, and no significant differences in adverse events between the two drugs. For CYP2C19 gene polymorphisms, the results showed that of 40 subjects, 12 subjects were extensive metabolizers, 24 were intermediate metabolizers, and 4 were poor metabolizers, the frequency of metabolic genotypes were 30%, 60%, and 10%. And the allele distributions for CYP2C19 were *1, *2, and *3 at 60%, 38.75%, and 1.25%. Both the CYP2C19 alleles and metabolic genotypes were consistent with other studies in Chinese. The results of PK parameters showed that different genotypes of CYP2C19 lead to significant differences in t1/2, AUC0–t, AUC0–∞ and Cmax, but no significant differences in Tmax in each group. At the same time, we confirmed that the PK parameters of the test and reference had no differences between the males and females. This study has shown that the pharmacokinetic parameters of the two formulations are not significantly different, which showed bioequivalence and exemplary safety. CYP2C19 gene polymorphism significantly differed in the PK parameters of omeprazole sodium bicarbonate powder.

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Pharmacokinetics and Pharmacodynamics of Esomeprazole/Sodium Bicarbonate Immediate-Release Capsules in Healthy Chinese Volunteers: A Cross-Over, Randomized Controlled Trial

Cited by 7 publications

References 45 publications

Comparative Pharmacokinetics/Pharmacodynamics of Fixed-Dose Combination of Esomeprazole and Calcium Carbonate (AD-206) to the Conventional Esomeprazole

Comparative Pharmacokinetics/Pharmacodynamics of Fixed-Dose Combination of Esomeprazole and Calcium Carbonate (AD-206) to the Conventional Esomeprazole

Pharmacokinetics and Pharmacodynamics of Lansoprazole/Sodium Bicarbonate Immediate‐release Capsules in Healthy Chinese Subjects: An Open, Randomized, Controlled, Crossover, Single‐, and Multiple‐dose Trial

Pharmacokinetics and bioequivalence evaluation of omeprazole and sodium bicarbonate dry suspensions in healthy Chinese volunteers

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