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This is a single-center, open-label, randomized, single dose, 3-way crossover study in healthy volunteers designed to evaluate the relative bioavailability of a new oral tablet formulation of linaprazan glurate in comparison to a previously studied oral tablet formulation under fasting conditions, and to assess the effect of a high fat, high calorie meal on the pharmacokinetics (PK) of linaprazan glurate and the active substance linaprazan after the administration of the new oral tablet formulation.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Reference formulation (Treatment A) | Active Comparator | 100 mg linaprazan glurate reference formulation (4x25 mg oral tablets) in fasting conditions |
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| Test formulation (Treatment B) | Experimental | 100 mg linaprazan glurate test formulation (1x100 mg oral tablet) in fasting conditions |
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| Test Formulation (Treatment C) | Experimental | 100 mg linaprazan glurate test formulation (1x100 mg oral tablet) in fed conditions |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Linaprazan glurate | Drug | 100 mg |
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| Measure | Description | Time Frame |
|---|---|---|
| Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratios of AUCinf and AUClast | The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprazan, comparing test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan exposure is increased or decreased with the new formulation. | From pre-dose up to 72 h post dose |
| Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratio of Cmax | The Ratio of Cmax (highest measured concentration) of linaprazan comparing the test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan exposure is increased or decreased with the new formulation. | From pre-dose up to 72 h post dose |
| Relative Bioavailability of Linaprazan Test Formulation in Fed vs. Fasting Conditions, Based on the Means Ratios for AUCinf and AUClast | The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprazan, comparing test formulation vs reference formulation (treatments C vs treatment B) for Relative Bioavailability, i.e. how much linaprazan exposure is increased or decreased in a fed vs fasted state. | From pre-dose up to 72 h post dose |
| Relative Bioavailability of Linaprazan Test Formulation in Fed vs. Fasting Conditions, Based on the Means Ratios for Cmax | The Ratio of Cmax of linaprazan when comparing test formulation vs reference formulation (treatments C vs treatment B), i.e. how much linaprazan exposure is increased or decreased with the new formulation. | From pre-dose up to 72 h post dose |
| Measure | Description | Time Frame |
|---|---|---|
| Relative Bioavailability of Linaprazan Glurate for the Test Formulation vs. Reference Formulation of Linaprazan Glurate, Based on the Means Ratios of PK Parameters. | The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprzan glurate, comparing test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan glurate exposure is increased or decreased with the new formulation. |
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Main Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| CRS d.o.o. | Ljubljana | Ukmarjeva Ulica 6 | 1000 | Slovenia |
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Approximately 84 healthy volunteers were planned to be screened to achieve 54 randomized subjects. 97 Volunteers were actually screened for eligibility, of those, 67 were Randomized and 49 Analyzed.
Subjects were recruited form CRS's database of healthy volunteers. All Volunteers were recruited in Slovenia, Ljubljana.
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| ID | Title | Description |
|---|---|---|
| FG000 | Treatment Sequence A B C | Treatments A = 100 mg reference formulation (formulation A) non-fasted B = 100 mg test formulation (formulation B) non-fasted C = 100 mg test formulation (formulation B) fasted |
| FG001 | Treatment Sequence A C B | Treatments A = 100 mg reference formulation (formulation A) non-fasted C = 100 mg test formulation (formulation B) fasted B = 100 mg test formulation (formulation B) non-fasted |
| FG002 | Treatment Sequence B A C | Treatments B = 100 mg test formulation (formulation B) non-fasted A = 100 mg reference formulation (formulation A) non-fasted C = 100 mg test formulation (formulation B) fasted |
| FG003 | Treatment Sequence B C A | Treatments B = 100 mg test formulation (formulation B) non-fasted C = 100 mg test formulation (formulation B) fasted A = 100 mg reference formulation (formulation A) non-fasted |
| FG004 | Treatment Sequence C A B | Treatments C = 100 mg test formulation (formulation B) fasted A = 100 mg reference formulation (formulation A) non-fasted B = 100 mg test formulation (formulation B) non-fasted |
| FG005 | Treatment Sequence C B A | Treatment C = 100 mg test formulation (formulation B) fasted B = 100 mg test formulation (formulation B) non-fasted A = 100 mg reference formulation (formulation A) non-fasted |
| FG006 | Exploratory Arm A B C | Subjects underdosed when receiving treatment A, receiving only 1x25 mg LG instead of 4x25. Subjects were excluded from the PK analysis set and their data are instead presented here as exploratory. Treatment sequence as in the title. |
| FG007 | Exploratory Arm A C B | Subjects underdosed when receiving treatment A, receiving only 1x25 mg LG instead of 4x25. Subjects were excluded from the PK analysis set and their data are instead presented here as exploratory. Treatment sequence as in the title. |
| Title | Milestones | Reasons Not Completed | ||||||||||||||||||
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| Treatment Period 1 |
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| Treatment Period 2 |
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| Treatment Period 3 |
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13 subjects were erroneously underdosed with 1x25 mg LG instead of 4x25 mg in the sequence arms starting with treatment A. These 13 subjects were excluded from the analysis set and replaced. Data was collected nevertheless and presented as "exploratory". This is why there is an imbalance between the number in the first two sequence arms.
In addition, in error, one subject recieved the treatments in reverse order from his/her randomization. E.g. B C A instead of as randomized to A C B.
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| ID | Title | Description |
|---|---|---|
| BG000 | Treatment Sequence A B C | Treatments A = 100 mg reference formulation non-fasted B = 100 mg test formualtion non-fasted C = 100 mg test formulation fasted |
| BG001 | Treatment A C B |
| Units | Counts |
|---|---|
| Participants |
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| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Categorical | Count of Participants |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | ||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratios of AUCinf and AUClast | The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprazan, comparing test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan exposure is increased or decreased with the new formulation. | PK Analysis Set | Posted | Geometric Mean | Standard Deviation | hours * nmol/Liter | From pre-dose up to 72 h post dose |
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Baseline to Visit 5, 1 month
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | Reference Formulation (Treatment A) | 100 mg linaprazan glurate reference formulation (4x25 mg), fasting conditions Linaprazan glurate: 100 mg |
| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Skin Bacterial Infection | Skin and subcutaneous tissue disorders | Systematic Assessment | Soft tissue infection with sepsis |
| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Tachycardia | Cardiac disorders | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Kristofer Katkits Nilsson, Global Trial Manager | Cinclus Pharma AB | +46 7064955 | kristofer.katkits@cincluspharma.com |
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| Type | Includes Protocol | Includes SAP | Includes ICF | Document Label | Document Date | Document Uploaded Date | Document File Name |
|---|---|---|---|---|---|---|---|
| Prot | Yes | No | No | Study Protocol | Dec 23, 2022 | Mar 17, 2025 | Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Jan 16, 2023 | Jul 2, 2024 | SAP_001.pdf |
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| From pre-dose up to 72 h post dose |
| Relative Bioavailability of Linaprazan Glurate Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratio of Cmax | The Ratio of Cmax (highest measured concentration) of linaprazan glurate comparing the test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan glurate exposure is increased or decreased with the new formulation. | From pre-dose up to 72 h post dose |
| Relative Bioavailability of Linaprazan Glurate in Fed vs. Fasting Conditions, Based on the Means Ratios for AUCinf, AUClast | The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprazan glurate, comparing test formulation vs reference formulation (treatments C vs treatment B) for Relative Bioavailability, i.e. how much linaprazan glurate exposure is increased or decreased in a fed vs fasted state. | From pre-dose up to 72 h post dose |
| Relative Bioavailability of Linaprazan Glurate in Fed vs. Fasting Conditions, Based on the Means Ratio of Cmax | The Ratio of Cmax of linaprazan glurate when comparing test formulation vs reference formulation (treatments C vs treatment B), i.e. how much linaprazan glurate exposure is increased or decreased with the new formulation. | From pre-dose up to 72 h post dose |
| Withdrawal by Subject |
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| Protocol Violation |
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| COMPLETED |
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| NOT COMPLETED |
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| COMPLETED |
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| NOT COMPLETED |
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Treatments A = 100 mg reference formulation non-fasted B = 100 mg test formualtion non-fasted C = 100 mg test formulation fasted
| BG002 | Treatment B A C | Treatments A = 100 mg reference formulation non-fasted B = 100 mg test formualtion non-fasted C = 100 mg test formulation fasted |
| BG003 | Treatment B C A | Treatments A = 100 mg reference formulation non-fasted B = 100 mg test formualtion non-fasted C = 100 mg test formulation fasted |
| BG004 | Treatment C A B | Treatments A = 100 mg reference formulation non-fasted B = 100 mg test formualtion non-fasted C = 100 mg test formulation fasted |
| BG005 | Treatment C B A | Treatments A = 100 mg reference formulation non-fasted B = 100 mg test formualtion non-fasted C = 100 mg test formulation fasted |
| BG006 | Total | Total of all reporting groups |
| Participants |
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| Age, Continuous | In error, one subject recieved the treatments in reverse order from what he/she was randomized to. E.g. in the order B C A as opposed to randomized A C B. | Mean | Full Range | years |
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| Sex: Female, Male | Count of Participants | Participants |
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| Ethnicity (NIH/OMB) | Count of Participants | Participants |
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| Region of Enrollment | Number | participants |
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| Test Formulation (Treatment B) |
100 mg linaprazan glurate test formulation, fasting conditions Linaprazan glurate: 100 mg |
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| Primary | Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratio of Cmax | The Ratio of Cmax (highest measured concentration) of linaprazan comparing the test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan exposure is increased or decreased with the new formulation. | PK analysis set | Posted | Geometric Mean | Standard Deviation | nmol/L | From pre-dose up to 72 h post dose |
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| Primary | Relative Bioavailability of Linaprazan Test Formulation in Fed vs. Fasting Conditions, Based on the Means Ratios for AUCinf and AUClast | The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprazan, comparing test formulation vs reference formulation (treatments C vs treatment B) for Relative Bioavailability, i.e. how much linaprazan exposure is increased or decreased in a fed vs fasted state. | PK Analysis Set. | Posted | Geometric Mean | Standard Deviation | hours * nmol/Liter | From pre-dose up to 72 h post dose |
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| Primary | Relative Bioavailability of Linaprazan Test Formulation in Fed vs. Fasting Conditions, Based on the Means Ratios for Cmax | The Ratio of Cmax of linaprazan when comparing test formulation vs reference formulation (treatments C vs treatment B), i.e. how much linaprazan exposure is increased or decreased with the new formulation. | PK analysis set | Posted | Geometric Mean | Standard Deviation | nmol/L | From pre-dose up to 72 h post dose |
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| Secondary | Relative Bioavailability of Linaprazan Glurate for the Test Formulation vs. Reference Formulation of Linaprazan Glurate, Based on the Means Ratios of PK Parameters. | The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprzan glurate, comparing test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan glurate exposure is increased or decreased with the new formulation. | PK Analysis Set | Posted | Geometric Mean | Standard Deviation | hours * nmol/Liter | From pre-dose up to 72 h post dose |
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| Secondary | Relative Bioavailability of Linaprazan Glurate Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratio of Cmax | The Ratio of Cmax (highest measured concentration) of linaprazan glurate comparing the test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan glurate exposure is increased or decreased with the new formulation. | PK Analysis Set | Posted | Geometric Mean | Standard Deviation | nmol/L | From pre-dose up to 72 h post dose |
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| Secondary | Relative Bioavailability of Linaprazan Glurate in Fed vs. Fasting Conditions, Based on the Means Ratios for AUCinf, AUClast | The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprazan glurate, comparing test formulation vs reference formulation (treatments C vs treatment B) for Relative Bioavailability, i.e. how much linaprazan glurate exposure is increased or decreased in a fed vs fasted state. | PK Analysis Set. | Posted | Geometric Mean | Standard Deviation | hours * nmol/Liter | From pre-dose up to 72 h post dose |
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| Secondary | Relative Bioavailability of Linaprazan Glurate in Fed vs. Fasting Conditions, Based on the Means Ratio of Cmax | The Ratio of Cmax of linaprazan glurate when comparing test formulation vs reference formulation (treatments C vs treatment B), i.e. how much linaprazan glurate exposure is increased or decreased with the new formulation. | PK Analysis Set. | Posted | Geometric Mean | Standard Deviation | nmol/L | From pre-dose up to 72 h post dose |
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| 0 |
| 51 |
| 0 |
| 51 |
| 17 |
| 51 |
| EG001 | Test Formulation (Treatment B) | 100 mg linaprazan glurate reference formulation (1x100 mg), fasting conditions Linaprazan glurate: 100 mg | 0 | 53 | 1 | 53 | 12 | 53 |
| EG002 | Test Formulation (Treatment C) | 100 mg linaprazan glurate test formulation (1x100 mg), fed conditions Linaprazan glurate: 100 mg | 0 | 50 | 0 | 50 | 14 | 50 |
| EG003 | Reference | 25 mg linaprazan glurate reference formulation fasting conditions | 0 | 13 | 0 | 13 | 4 | 13 |
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| Diarrhoea | Gastrointestinal disorders | Systematic Assessment |
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| Vomiting | Gastrointestinal disorders | Systematic Assessment |
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| Constipation | Gastrointestinal disorders | Systematic Assessment |
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| Nasopharyngitis | Infections and infestations | Systematic Assessment |
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| Rhinitis | Infections and infestations | Systematic Assessment |
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| Blood pressure diastolic inceased | Investigations | Systematic Assessment |
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| Headache | Nervous system disorders | Systematic Assessment |
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| Sciatica | Nervous system disorders | Systematic Assessment |
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| Papula | Skin and subcutaneous tissue disorders | Systematic Assessment |
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| Vascular disorders | Skin and subcutaneous tissue disorders | Systematic Assessment |
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| Hypertension | Vascular disorders | Systematic Assessment |
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| Phlebitis | Vascular disorders | Systematic Assessment |
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| Skin and subcutaneous tissue disorders | Skin and subcutaneous tissue disorders | Systematic Assessment |
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| Cardiac disorders | Cardiac disorders | Systematic Assessment |
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| Liver disorder | Hepatobiliary disorders | Systematic Assessment |
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| AUClast |
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| Ratio of geometric mean AUClast comparing treatment C (fed) versus treatment B (fasted). This is a relative comparison, thus there is no unit. The ratio is given under the Estimated value. | Mixed Models Analysis | <0.0001 | Ratio | 0.7684 | 2-Sided | 95 | 0.7102 | 0.8313 | Treatment C (1x100 mg test formulation fed) divided by treament B (100 mg test formulation fasted) | Other | Ratio |
| AUClast |
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| Ratio of geometric mean AUClast comparing test formulation fasted (treatment B) vs. reference formulation fasted (treatment A). This is a relative comparison, thus there is no unit. The ratio is given under the Estimated value. | Mixed Models Analysis | <0.0001 | Ratio | 3.5277 | 2-Sided | 95 | 2.9076 | 4.2799 | Treatment B (1x100 mg test formulation) divided by treament A (4x25 mg reference formulation) | Other | Ratio |
| AUClast |
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| Ratio of geometric mean AUClast comparing treatment C (fed) versus treatment B (fasted). This is a relative comparison, thus there is no unit. The ratio is given under the Estimated value. | Mixed Models Analysis | <0.0001 | Ratio | 0.4923 | 2-Sided | 95 | 0.4047 | 0.5989 | Treatment C (1x100 mg test formulation fed) divided by treament B (100 mg test formulation fasted) | Other | Ratio |