Pharmacokinetic Study of Single-Dose Modified Release Glipizide in Healthy Volunteers

NCT05159427 | Recruiting Phase 1 FDA Drug

• 1 other identifier: HUM00199603
• Study Type: interventional
• Target: 40
• Locations: 1 country
• Sites: 1

Brief Summary

In vivo drug dissolution in the gastrointestinal (GI) tract is largely unmeasured. The purpose of this clinical study is to evaluate the in vivo drug dissolution and systemic absorption of modified release formulations of the BCS Class II drug Glipizide by direct sampling of stomach and small intestinal luminal content, blood, urine and feces. Expanding current knowledge of drug dissolution in vivo will help to establish physiologically relevant in vitro models predictive of drug dissolution.

Conditions

Human Gastrointestinal Physiology Data

Keywords

Clinical study; Glipizide; Modified release; Pharmacokinetics; In vivo dissolution; Local gastrointestinal concentration

Outcome Measures

Primary Outcomes (1)

• Average Area Under the Plasma Concentration-time Curve to infinite time (AUCinfinity) of Glipizide After a Single Dose of Glipizide with Gastrointestinal Intubation and between Two Modified Release Glipizide formulations

  Average Area Under the Plasma Concentration-time Curve to infinite time (AUCinfinity) of Glipizide will be measured at multiple timepoints over a 78 hour period at each of the two study phases

  From time 0 to 78 hours

Secondary Outcomes (5)

• Plasma Cmax of Glipizide After a Single Dose of Glipizide with Gastrointestinal Intubation and between Two Modified Release Glipizide formulations

  From time 0 to 78 hours

• Plasma Tmax of Glipizide After a Single Dose of Glipizide with Gastrointestinal Intubation and between Two Modified Release Glipizide formulations

  From time 0 to 78 hours

• Urine and Feces concentrations of Glipizide After a Single Dose of Glipizide with Gastrointestinal Intubation and between Two Modified Release Glipizide formulations

  From time 0 to 78 hours

• Maximum Gastrointestinal fluid concentration of Glipizide after Oral Administration of a Single Dose Modified Released Formulation of Glipizide

  From time 0 to 7 hours

• Gastrointestinal pH after Oral Administration of Modified Release Formulation of Glipizide

  From time 0 to 7 hours

Study Arms (1)

G.I Intubation

EXPERIMENTAL

Single dose of Glipizide (5 mg modified-release tablet) and Rifaximin (200 mg tablet) administered with 200 mL of 20% glucose solution in water + 1 mg of the stable isotope Glipizide (13C6-Glipizide) with 40 ml of 14% glucose solution in water. A 'Stable isotope' means a heavier version of the drug that is not radioactive.

Drug: Glucotrol XL 5Mg Extended-Release Tablet; Drug: Glipizide ER 5 MG 24 HR Extended Release Oral Tablet; Drug: Rifaximin 200Mg Tab; Drug: 13C6-Glipizide

Interventions

Glipizide ER 5 MG 24 HR Extended Release Oral Tablet DRUG

Participants are randomized to take one tablet of this study drug by mouth.

G.I Intubation

Rifaximin 200Mg Tab DRUG

Participants will take one tablet of this study drug by mouth.

G.I Intubation

13C6-Glipizide DRUG

Participants will take 1 mg of this study drug dissolved in 40 ml glucose solution by mouth.

Also known as: Stable Isotope Glipizide

G.I Intubation

Glucotrol XL 5Mg Extended-Release Tablet DRUG

Participants are randomized to take one tablet of this study drug by mouth.

G.I Intubation

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Male or female adults age 18 to 55 years with BMI ranging from 18.5 to 35 kg/m2 inclusive
• Ability to independently provide an informed consent
• Demonstrate the ability to swallow a multivitamin pill that mimics a SmartPill capsule
• Negative serum pregnancy test (for women of child-bearing potential)

You may not qualify if:

• Unable to independently provide an informed consent for themselves or mentally incapacitated.
• Physical disability (including blindness or deafness) that requires special arrangements.
• Significant clinical illness, including cardiovascular disease, neurological disease, organ failure, or malignancy in the opinion of the investigator
• Any surgical procedure within 3 weeks prior to screening
• History and/or presence of severe seasonal allergies or severe allergic diseases including drug allergies, food allergies and allergy against the SmartPill® device
• History and/or presence of hypersensitivity to any of the study drugs or the products' excipients
• History and/or presence of hypersensitivity to Sulfonamide derivatives
• History and/or presence of hypersensitivity to Lidocaine
• History and/or presence of hypersensitivity to rifaximin, rifamycin antimicrobial agents, or any of the components of XIFAXAN
• History and/or presence of hypersensitivity to acrylate or methacrylate, commonly used components of medical adhesives
• Any other factor, condition, or disease, including, but not limited to, cardiovascular, respiratory, hematological, renal, hepatic, or gastrointestinal disorders that may, in the opinion of the Investigator, jeopardize the safety of the patient, alter drug absorption and pharmacokinetics or impact the validity of the study results.
• Subjects with Type 1 Diabetes Mellitus (DM), diabetic ketoacidosis, with or without coma
• Subjects with Glucose 6-phosphate dehydrogenase (G6PD) deficiency
• History and/or presence of drug addiction or alcohol abuse within the past 12 months.
• History of significant psychiatric or neurological illness, including seizure disorders.

Sponsors & Collaborators

• University of Michigan: lead
• Food and Drug Administration (FDA): collaborator

Study Sites (1)

University of Michigan

Ann Arbor, Michigan, 48109, United States

RECRUITING

MeSH Terms

Interventions

Glipizide; Rifaximin

Intervention Hierarchy (Ancestors)

Sulfonylurea Compounds; Sulfones; Sulfur Compounds; Organic Chemicals; Rifamycins; Heterocyclic Compounds, 4 or More Rings; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds; Lactams, Macrocyclic; Macrocyclic Compounds; Polycyclic Compounds

Study Officials

• Cathrin Ring

  University of Michigan

  STUDY DIRECTOR

Central Study Contacts

Cathrin Ring

CONTACT

3136221119; cathrinr@med.umich.edu

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: PARALLEL
• Sponsor Type: OTHER
• Responsible Party: PRINCIPAL INVESTIGATOR
• PI Title: Charles R. Walgreen Jr. Professor of Pharmacy and Professor of Pharmaceutical Sciences, College of Pharmacy, The University of Michigan

Model Details: This is a parallel study design. Subjects are asked to complete the study events/procedures in one phases (G.I intubation) with one of the two formulations of glipizide.

Study Record Dates

• First Submitted: November 17, 2021
• First Posted: December 16, 2021
• Study Start: March 15, 2022
• Primary Completion (Estimated): September 1, 2026
• Study Completion (Estimated): September 1, 2026
• Last Updated: March 17, 2026

Record last verified: 2026-03

Locations

US (1)