Correlation of Mesalamine Pharmacokinetics With Local Availability

May 2, 2017 updated by: Duxin Sun, University of Michigan
This study is designed to provide data to the FDA correlating pharmacokinetics with local availability of medications within the gastrointestinal tract. This study will support the establishment of scientifically based standards for evaluating drugs which act locally within the gastrointestinal tract. Specific objectives of this study are to: (1) quantify how the plasma concentrations of mesalamine, an agent used to treat inflammatory bowel disease, are correlated with the concentrations in gastrointestinal fluids; and (2) improve the physiologically based models for drug absorption from the intestine. Information from this study in concert with in vitro dissolution data will be used to evaluate in vivo-in vitro correlation (IVIVC) for concentrations in plasma and intestinal lumen and dissolution of mesalamine products.

Study Overview

Status

Status

Indicates the current recruitment status or the expanded access status.
Completed

Conditions

Conditions

The disease, disorder, syndrome, illness, or injury that is being studied. On ClinicalTrials.gov, conditions may also include other health-related issues, such as lifespan, quality of life, and health risks.

Intervention / Treatment

Intervention / Treatment

A process or action that is the focus of a clinical study. Interventions include drugs, medical devices, procedures, vaccines, and other products that are either investigational or already available. Interventions can also include noninvasive approaches, such as education or modifying diet and exercise.

Detailed Description

This study evaluated the pharmacokinetics of mesalamine and its major metabolite of mesalamine known as N-acetyl-mesalamine in plasma. Mesalamine is available in different formulations that control the rate at which they are released in the gastrointestinal tract. Three formulations of mesalamine, Pentasa, Apriso, and Lialda, were studied in the crossover phase, while an oral solution formulation of mesalamine was studied in the single-arm phase. Each subject participated in a crossover phase study with one of the three formulations assigned at random using block randomization. Then the subject entered the single-arm phase study. After participation in one crossover phase study and one single-arm phase study, the subject could opt to participate in crossover phase studies using the other formulations also chosen at random until all three formulations were studied. The single-arm phase study was not repeated on returning subjects who participated in more than one crossover phase study.

Study Type

Study Type

Describes the nature of a clinical study. Study types include interventional studies (also called clinical trials), observational studies (including patient registries), and expanded access.
Interventional

Enrollment (Actual)

Enrollment

The number of participants in a clinical study. The "anticipated" enrollment is the target number of participants that the researchers need for the study.
30

Phase

Phase

The stage of a clinical trial studying a drug or biological product, based on definitions developed by the U.S. Food and Drug Administration (FDA). The phase is based on the study's objective, the number of participants, and other characteristics. There are five phases: Early Phase 1 (formerly listed as Phase 0), Phase 1, Phase 2, Phase 3, and Phase 4. Not Applicable is used to describe trials without FDA-defined phases, including trials of devices or behavioral interventions.
  • Not Applicable

Contacts and Locations

This section provides the contact details for those conducting the study, and information on where this study is being conducted.

Study Locations

  • United States
    • Michigan
      • Ann Arbor, Michigan, United States, 48109
        • University of Michigan

Participation Criteria

Researchers look for people who fit a certain description, called eligibility criteria. Some examples of these criteria are a person's general health condition or prior treatments.

Eligibility Criteria

Eligibility Criteria

The key requirements that people who want to participate in a clinical study must meet or the characteristics they must have. Eligibility criteria consist of both inclusion criteria (which are required for a person to participate in the study) and exclusion criteria (which prevent a person from participating). Types of eligibility criteria include whether a study accepts healthy volunteers, has age or age group requirements, or is limited by sex.

Ages Eligible for Study

18 years to 55 years (Adult)

Accepts Healthy Volunteers

Yes

Genders Eligible for Study

All

Description

Inclusion Criteria

  1. Adults age 18 to 55.
  2. Male or female voluntarily able to give informed consent.
  3. Body mass index (BMI) 18.5 to 35.

Exclusion Criteria

  1. Adults unable to consent for themselves or mentally incapacitated.
  2. Prisoners.
  3. Significant clinical illness within 3 weeks prior to Screening.
  4. Use of concomitant medications within 2 weeks prior to receiving study drug, including but not limited to prescription drugs, herbal and dietary supplements, over the counter medications, and vitamins. Oral contraception is permitted.
  5. History of gastrointestinal surgery.
  6. History of allergy to non-steroidal anti-inflammatory drugs (NSAIDs) or to any of the ingredients of Asacol, Pentasa, Apriso, or Lialda.
  7. History of severe allergic diseases including drug allergies, with the exception of seasonal allergies.
  8. Any other factor, condition, or disease, including, but not limited to, cardiovascular, renal, hepatic, or gastrointestinal disorders that may, in the opinion of the Investigator, jeopardize the safety of the patient or impact the validity of the study results.
  9. History of drug addiction or alcohol abuse within the past 12 months.
  10. Pregnant or lactating females.
  11. Surgery within the past 3 months.
  12. Received an investigational drug within 60 days prior to receiving the study drug.
  13. Any clinically significant abnormal lab values during Screening.

Study Plan

This section provides details of the study plan, including how the study is designed and what the study is measuring.

How is the study designed?

Design Details

  • Primary Purpose: Basic Science
  • Allocation: Randomized
  • Interventional Model: Crossover Assignment
  • Masking: None (Open Label)

Arms and Interventions

Participant Group / Arm

Participant Group / Arm

A group or subgroup of participants in a clinical trial that receives a specific intervention/treatment, or no intervention, according to the trial's protocol.
Intervention / Treatment

Intervention / Treatment

A process or action that is the focus of a clinical study. Interventions include drugs, medical devices, procedures, vaccines, and other products that are either investigational or already available. Interventions can also include noninvasive approaches, such as education or modifying diet and exercise.
Experimental: Arm 1: Pentasa then Delzicol then Apriso then Lialda
  1. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
  2. Washout period of 10 days.
  3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
  4. Washout period of 10 days.
  5. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
  6. Washout period of 10 days.
  7. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
Drug: Pentasa 500 mg capsule x 2 with 240 mL water; single dose
Drug: Apriso 375 mg capsule x 3 with 240 mL water; single dose
Drug: Lialda 1200 mg tablet x 1 with 240 mL water; single dose
Drug: Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose
Experimental: Arm 2: Pentasa then Delzicol then Lialda then Apriso
  1. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
  2. Washout period of 10 days.
  3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
  4. Washout period of 10 days.
  5. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
  6. Washout period of 10 days.
  7. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
Drug: Pentasa 500 mg capsule x 2 with 240 mL water; single dose
Drug: Apriso 375 mg capsule x 3 with 240 mL water; single dose
Drug: Lialda 1200 mg tablet x 1 with 240 mL water; single dose
Drug: Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose
Experimental: Arm 3: Apriso then Delzicol then Pentasa then Lialda
  1. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
  2. Washout period of 10 days.
  3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
  4. Washout period of 10 days.
  5. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
  6. Washout period of 10 days.
  7. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
Drug: Pentasa 500 mg capsule x 2 with 240 mL water; single dose
Drug: Apriso 375 mg capsule x 3 with 240 mL water; single dose
Drug: Lialda 1200 mg tablet x 1 with 240 mL water; single dose
Drug: Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose
Experimental: Arm 4: Apriso then Delzicol then Lialda then Pentasa
  1. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
  2. Washout period of 10 days.
  3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
  4. Washout period of 10 days.
  5. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
  6. Washout period of 10 days.
  7. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
Drug: Pentasa 500 mg capsule x 2 with 240 mL water; single dose
Drug: Apriso 375 mg capsule x 3 with 240 mL water; single dose
Drug: Lialda 1200 mg tablet x 1 with 240 mL water; single dose
Drug: Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose
Experimental: Arm 5: Lialda then Delzicol then Pentasa then Apriso
  1. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
  2. Washout period of 10 days.
  3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
  4. Washout period of 10 days.
  5. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
  6. Washout period of 10 days.
  7. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
Drug: Pentasa 500 mg capsule x 2 with 240 mL water; single dose
Drug: Apriso 375 mg capsule x 3 with 240 mL water; single dose
Drug: Lialda 1200 mg tablet x 1 with 240 mL water; single dose
Drug: Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose
Experimental: Arm 6: Lialda then Delzicol then Apriso then Pentasa
  1. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
  2. Washout period of 10 days.
  3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
  4. Washout period of 10 days.
  5. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
  6. Washout period of 10 days.
  7. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
Drug: Pentasa 500 mg capsule x 2 with 240 mL water; single dose
Drug: Apriso 375 mg capsule x 3 with 240 mL water; single dose
Drug: Lialda 1200 mg tablet x 1 with 240 mL water; single dose
Drug: Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose

What is the study measuring?

Primary Outcome Measures

Primary Outcome Measures

In a clinical study's protocol, the planned outcome measure that is the most important for evaluating the effect of an intervention/treatment. Most clinical studies have one primary outcome measure, but some have more than one.
Outcome Measure
Measure Description
Time Frame
The AUC of Mesalamine in Plasma
Time Frame: 0 hours pre-dose and up to 96 hours post-dose
The AUC is the area under the concentration-time curve from time 0 to last time point. The data are organized by the different drug formulations of mesalamine, which include Pentasa (0 to 72 hours), Apriso (0 to 72 hours), Lialda (0 to 96 hours), and Delzicol (0 to 24 hours). The AUC is measured in units of nanomoles of mesalamine per liter of plasma (nM) multiplied by time in hours (nM*h). The AUC results are reported over the time-period because this provides a more meaningful comparison of potential differences in the bioequivalence of formulations.
0 hours pre-dose and up to 96 hours post-dose
The AUC of Metabolite (N-acetyl-mesalamine) in Plasma
Time Frame: 0 hours pre-dose and up to 96 hours post-dose
The AUC is the area under the concentration-time curve from time 0 to last time point. The data are organized by the different drug formulations of mesalamine, which include Pentasa (0 to 72 hours), Apriso (0 to 72 hours), Lialda (0 to 96 hours), and Delzicol (0 to 24 hours). The AUC is measured in units of nanomoles of N-acetyl-mesalamine per liter of plasma (nM) multiplied by time in hours (nM*h). The AUC results are reported over the time-period because this provides a more meaningful comparison of potential differences in the bioequivalence of formulations.
0 hours pre-dose and up to 96 hours post-dose

Secondary Outcome Measures

Secondary Outcome Measures

In a clinical study's protocol, a planned outcome measure that is not as important as the primary outcome measure for evaluating the effect of an intervention but is still of interest. Most clinical studies have more than one secondary outcome measure.
Outcome Measure
Measure Description
Time Frame
The AUC of Mesalamine in Distal Jejunum
Time Frame: 0 hours pre-dose and up to 7 hours post-dose
The AUC is the area under the concentration-time curve from time 0 to 7 hours. The data are organized by the different drug formulations of mesalamine, which include Pentasa, Apriso, and Lialda. The AUC is measured in units of micromoles of mesalamine per liter of plasma (µM) multiplied by time in hours (µM*h).The AUC results are reported over the time-period because this provides a more meaningful comparison of potential differences in the bioequivalence of formulations. The solution formulation (Delzicol) was not administered in this portion of the study. Therefore no results pertaining to the solution formulation are included in this outcome measure.
0 hours pre-dose and up to 7 hours post-dose
The AUC of Metabolite (N-acetyl-mesalamine) in Distal Jejunum
Time Frame: 0 hours pre-dose and up to 7 hours post-dose
The AUC is the area under the concentration-time curve from time 0 to 7 hours. The data are organized by the different drug formulations of mesalamine, which include Pentasa, Apriso, and Lialda. The AUC is measured in units of micromoles of mesalamine per liter of plasma (µM) multiplied by time in hours (µM*h).The AUC results are reported over the time-period because this provides a more meaningful comparison of potential differences in the bioequivalence of formulations. The solution formulation (Delzicol) was not administered in this portion of the study. Therefore no results pertaining to the solution formulation are included in this outcome measure.
0 hours pre-dose and up to 7 hours post-dose

Collaborators and Investigators

This is where you will find people and organizations involved with this study.

Sponsor

Sponsor

The organization or person who initiates the study and who has authority and control over the study.
University of Michigan

Collaborators

Collaborators

An organization other than the sponsor that provides support for a clinical study. This support may include activities related to funding, design, implementation, data analysis, or reporting.
Food and Drug Administration (FDA)

Investigators

Investigators

A researcher involved in a clinical study. Related terms include site principal investigator, site sub-investigator, study chair, study director, and study principal investigator.
  • Principal Investigator: Duxin Sun, Ph.D., University of Michigan, College of Pharmacy

Publications and helpful links

The person responsible for entering information about the study voluntarily provides these publications. These may be about anything related to the study.

General Publications

Study record dates

These dates track the progress of study record and summary results submissions to ClinicalTrials.gov. Study records and reported results are reviewed by the National Library of Medicine (NLM) to make sure they meet specific quality control standards before being posted on the public website.

Study Major Dates

Study Start

Study Start

The actual date on which the first participant was enrolled in a clinical study. The "anticipated" study start date is the date that the researchers think will be the study start date.
April 1, 2012

Primary Completion (Actual)

Primary Completion

The date on which the last participant in a clinical study was examined or received an intervention to collect final data for the primary outcome measure. Whether the clinical study ended according to the protocol or was terminated does not affect this date. For clinical studies with more than one primary outcome measure with different completion dates, this term refers to the date on which data collection is completed for all the primary outcome measures. The "anticipated" primary completion date is the date that the researchers think will be the primary completion date for the study.
September 1, 2015

Study Completion (Actual)

Study Completion

The date on which the last participant in a clinical study was examined or received an intervention/treatment to collect final data for the primary outcome measures, secondary outcome measures, and adverse events (that is, the last participant's last visit). The "anticipated" study completion date is the date that the researchers think will be the study completion date.
April 1, 2017

Study Registration Dates

First Submitted

First Submitted

The date on which the study sponsor or investigator first submitted a study record to ClinicalTrials.gov. There is typically a delay of a few days between the first submitted date and the record's availability on ClinicalTrials.gov (the first posted date).
November 25, 2013

First Submitted That Met QC Criteria

First Submitted That Met QC Criteria

The date on which the study sponsor or investigator first submits a study record that is consistent with National Library of Medicine (NLM) quality control (QC) review criteria. The sponsor or investigator may need to revise and submit a study record one or more times before NLM's QC review criteria are met. It is the responsibility of the sponsor or investigator to ensure that the study record is consistent with the NLM QC review criteria.
November 25, 2013

First Posted (Estimate)

First Posted

The date on which the study record was first available on ClinicalTrials.gov after National Library of Medicine (NLM) quality control (QC) review has concluded. There is typically a delay of a few days between the date the study sponsor or investigator submitted the study record and the first posted date.
December 3, 2013

Study Record Updates

Last Update Posted (Actual)

Last Update Posted

The most recent date on which changes to a study record were made available on ClinicalTrials.gov. There may be a delay between when the changes were submitted to ClinicalTrials.gov by the study's sponsor or investigator (the last update submitted date) and the last update posted date.
May 15, 2017

Last Update Submitted That Met QC Criteria

Last Update Submitted That Met QC Criteria

The most recent date on which the study sponsor or investigator submitted changes to a study record that are consistent with National Library of Medicine (NLM) quality control (QC) review criteria. It is the responsibility of the sponsor or investigator to ensure that the study record is consistent with the NLM QC review criteria.
May 2, 2017

Last Verified

Last Verified

The most recent date on which the study sponsor or investigator confirmed the information about a clinical study on ClinicalTrials.gov as accurate and current. If a study with a recruitment status of recruiting; not yet recruiting; or active, not recruiting has not been confirmed within the past 2 years, the study's recruitment status is shown as unknown.
May 1, 2017

More Information

Terms related to this study

Additional Relevant MeSH Terms

Other Study ID Numbers

Other Study ID Numbers

Identifiers or ID numbers other than the NCT number that are assigned to a clinical study by the study's sponsor, funders, or others. These numbers may include unique identifiers from other trial registries and National Institutes of Health grant numbers.
  • FDA-SOL-1120920
  • HHSF223201300460A (Other Grant/Funding Number: U.S. Food and Drug Administration)
  • HHSF223201000082C (Other Grant/Funding Number: U.S. Food and Drug Administration)

This information was retrieved directly from the website clinicaltrials.gov without any changes. If you have any requests to change, remove or update your study details, please contact register@clinicaltrials.gov. As soon as a change is implemented on clinicaltrials.gov, this will be updated automatically on our website as well.

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