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The objectives of this study were (a) to evaluate the pharmacokinetics and to evaluate and compare the pharmacodynamics of ilaprazole and esomeprazole following a single dose (Day 1) and once daily (QD) administration for 5 consecutive days each of 10-mg, 20-mg, and 40-mg ilaprazole tablets and 40-mg esomeprazole tablets; (b) to evaluate the safety of 10-mg, 20-mg, and 40-mg ilaprazole tablets following QD oral administration for 5 consecutive days; and (c) to characterize the plasma gastrin concentration profile on Day 1 and Day 5 following QD oral administration of 10-mg, 20-mg, and 40-mg ilaprazole and 40-mg esomeprazole tablets for 5 consecutive days.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Treatment sequence ADBC | Experimental | Regimen A: 10 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen B: 20 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen C: 40 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen D: 40 mg of esomeprazole administered QD for 5 days with 240 mL of water. |
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| Treatment sequence BACD | Experimental | Regimen A: 10 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen B: 20 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen C: 40 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen D: 40 mg of esomeprazole administered QD for 5 days with 240 mL of water. |
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| Treatment sequence CBDA | Experimental | Regimen A: 10 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen B: 20 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen C: 40 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen D: 40 mg of esomeprazole administered QD for 5 days with 240 mL of water. |
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| Treatment sequence DCAB | Experimental | Regimen A: 10 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen B: 20 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen C: 40 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen D: 40 mg of esomeprazole administered QD for 5 days with 240 mL of water. |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Ilaprazole | Drug |
| ||
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacodynamics of mean pH and percentage of time pH | For each regimen and day, mean pH and percentage of time pH exceeded 3, 4, 5, and 6 were tabulated and descriptive statistics were provided for 24-hour postdose intervals and each of the following intervals of time relative to dosing: 0 to 4 hours, >4 to 9 hours, >9 to 12 hours, >12 to 16 hours, and >16 to 24 hours. | for 24 hours dosing of Ilaprazole |
| Measure | Description | Time Frame |
|---|---|---|
| ilaprazole and esomeprazole plasma concentration data and pharmacokinetic parameter estimates were tabulated and descriptive statistics computed | The assessments of dose proportionality for ilaprazole regimens were performed via 90% confidence intervals for the ratio of the central values obtained within the framework of the ANOVA on natural logarithms of dose-normalized Cmax, AUCt, and AUC | for 24 hours dosing of Ilaprazole |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Gaetano Morelli, MD | MDS Pharma Services | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| MDS Pharma Services | Québec | Canada |
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| ID | Term |
|---|---|
| C119615 | ilaprazole |
| D064098 | Esomeprazole |
| ID | Term |
|---|---|
| D009853 | Omeprazole |
| D053799 | 2-Pyridinylmethylsulfinylbenzimidazoles |
| D013454 | Sulfoxides |
| D013457 | Sulfur Compounds |
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|
| Esomeprazole |
| Drug |
|
| D009930 |
| Organic Chemicals |
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D001562 | Benzimidazoles |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |