Comparative Pharmacokinetics and Food-Effect Bioavailability of Lubiprostone Sprinkle in Healthy Volunteers

Comparative Pharmacokinetics and Food-Effect Bioavailability of a Sprinkle Formulation of Lubiprostone After Oral Administration in Healthy Volunteers

A study to compare the pharmacokinetics and food-effect bioavailability of sprinkle formulation of lubiprostone, as compared to lubiprostone capsules in healthy volunteers.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteers
• Intervention / Treatment: Drug: Cohort 1: Lubiprostone Capsule, Fasted; Drug: Cohort 1: Lubiprostone Sprinkle Formulation, Fasted; Drug: Cohort 2: Lubiprostone Sprinkle Formulation, Fed; Drug: Cohort 2: Lubiprostone Sprinkle Formulation, Fasted

Detailed Description

To compare the pharmacokinetics of the sprinkle formulation of lubiprostone, as compared to lubiprostone capsules and to determine the effect of food on the bioavailability and plasma pharmacokinetics of lubiprostone sprinkle.

• Study Type: Interventional
• Enrollment (Actual): 49
• Phase: Phase 3

Contacts and Locations

Study Locations

• United States
  • Texas
    • San Antonio, Texas, United States, 78209
      • ICON

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Is male or female, between 18 and 55 years of age, inclusive.
• Has a 12-lead electrocardiogram (ECG) within normal limits and is in good health based upon review of medical history, physical examination results, vital signs (within normal range), and normal laboratory profile for both blood and urine.

Exclusion Criteria:

• Has an active or recent history of alcoholism or drug addiction (within 1 year prior)
• Is a smoker or has a recent history of smoking (within 6 months)
• Routinely consumes food known to alter drug metabolism (i.e., grapefruit juice, coffee, tea, cola, chocolate, cocoa, or other caffeine or methyl-xanthine containing foods or beverages) and/or cannot refrain from these items
• Has donated blood within 3 months
• Has a medical/surgical condition that might interfere with the absorption, distribution, metabolism, or excretion of the study medication.

Study Plan

How is the study designed?

Design Details

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

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Active Comparator: Cohort 1 (Treatment Sequence AB); Cohort 1: Treatment A. Capsule Fasted (7-day Washout) then Treatment B. Sprinkle Formulation, Fasted	Drug: Cohort 1: Lubiprostone Capsule, Fasted; Lubiprostone soft gelatin capsule administered under fasted conditions; Other Names: Treatment A; AMITIZA®; Drug: Cohort 1: Lubiprostone Sprinkle Formulation, Fasted; Lubiprostone sprinkle formulation administered under fasted conditions; Other Names: Treatment B; Lubiprostone microbeads
Experimental: Cohort 1 (Treatment Sequence BA); Cohort 1: Treatment B. Sprinkle Formulation, Fasted (7-day Washout) then Treatment A. Capsule Fasted	Drug: Cohort 1: Lubiprostone Capsule, Fasted; Lubiprostone soft gelatin capsule administered under fasted conditions; Other Names: Treatment A; AMITIZA®; Drug: Cohort 1: Lubiprostone Sprinkle Formulation, Fasted; Lubiprostone sprinkle formulation administered under fasted conditions; Other Names: Treatment B; Lubiprostone microbeads
Experimental: Cohort 2 (Treatment Sequence CD); Cohort 2: Treatment C: Sprinkle Formulation, Fed (7-day Washout) then Treatment D: Sprinkle Formulation, Fasted	Drug: Cohort 2: Lubiprostone Sprinkle Formulation, Fed; Lubiprostone sprinkle formulation administered under fed conditions; Other Names: Treatment C; Lubiprostone microbeads; Drug: Cohort 2: Lubiprostone Sprinkle Formulation, Fasted; Lubiprostone sprinkle formulation administered under fasted conditions; Other Names: Treatment D; Lubiprostone microbeads
Experimental: Cohort 2 (Treatment Sequence DC); Cohort 2: Treatment D: Sprinkle Formulation, Fasted (7-day Washout) then Treatment C. Sprinkle Formulation, Fed	Drug: Cohort 2: Lubiprostone Sprinkle Formulation, Fed; Lubiprostone sprinkle formulation administered under fed conditions; Other Names: Treatment C; Lubiprostone microbeads; Drug: Cohort 2: Lubiprostone Sprinkle Formulation, Fasted; Lubiprostone sprinkle formulation administered under fasted conditions; Other Names: Treatment D; Lubiprostone microbeads

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Cohort 1: Area Under the Concentration-time Curve (AUC) From Hour 0 to the Last Measurable Concentration (AUC0-t) of M3 Metabolite	1 day
Cohort 1: Maximum Observed Concentration (Cmax) of M3 Metabolite	1 day

Secondary Outcome Measures

Outcome Measure	Time Frame
Cohort 2: Total Exposure (AUC0-t) of M3 With Administration of Sprinkle Lubiprostone Under Fed Versus (vs) Fasted Condition	1 day
Cohort 2: Maximum Observed Concentration (Cmax) of M3 Metabolite in Fed vs Fasted Conditions	1 day

Other Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)	An AE is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An SAE is any untoward medical occurrence that results in death;is life-threatening;requires inpatient hospitalization or prolongation of present hospitalization;results in persistent or significant disability/incapacity;is a congenital anomaly/birth defect;or is a medically important event that may not be immediately life-threatening or result in death or hospitalization, but may jeopardize the participant or may require intervention to prevent one of other outcomes listed in definition above, or involves suspected transmission via a medicinal product of an infectious agent.	From the first dose of study drug up to 28 days

Collaborators and Investigators

• Sponsor: Sucampo Pharma Americas, LLC
• Collaborators: Takeda

Publications and helpful links

General Publications

• Adams A, Barish C, Chen A, Dennis P, Krause R, Lichtlen P, Losch-Beridon T, Mareya S, Schneider J. Capsule and Sprinkle Formulations of Lubiprostone Are Not Biologically Similar in Patients with Functional Constipation. Adv Ther. 2021 Jun;38(6):2936-2952. doi: 10.1007/s12325-021-01707-9. Epub 2021 Apr 8. Erratum In: Adv Ther. 2021 May 24;:

Study record dates

Study Major Dates

• Study Start (Actual): November 16, 2016
• Primary Completion (Actual): December 23, 2016
• Study Completion (Actual): May 1, 2017

Study Registration Dates

• First Submitted: December 20, 2016
• First Submitted That Met QC Criteria: January 3, 2017
• First Posted (Estimate): January 5, 2017

Study Record Updates

• Last Update Posted (Actual): March 9, 2020
• Last Update Submitted That Met QC Criteria: February 18, 2020
• Last Verified: March 1, 2018

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Membrane Transport Modulators; Chloride Channel Agonists; Lubiprostone
• Other Study ID Numbers: SCMP-0211-304

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No