Clinical trial NCT00751699: Pharmacokinetics of Asacol 2.4 g/Day and Lialda 2.4 g/Day in Healthy Volunteers
Official title: A Randomized, Open-label, Multiple Dose, Parallel Group Study to Evaluate 5 ASA and N Ac 5 ASA Pharmacokinetics Following Administration of Oral Doses of Asacol 2.4 g/Day and Lialda 2.4 g/Day for 7 Days in Healthy Volunteers
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Keywords: Pharmacokinetics
Lead sponsor: Warner Chilcott
Sponsor class: INDUSTRY
First posted: 2008-09-12
Enrollment: 37
Sex: ALL
Minimum age (years): 18
Maximum age (years): 45
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL

Brief summary: This study evaluated pharmacokinetics of 5-ASA and N-Ac-5-ASA associated with each of 3 regimens of oral mesalamine 2.4 g/day (Lialda 2.4 g/day 2 x 1.2 g every 24 hours, Asacol® 6 x 400 mg every 24 hours, or Asacol 2 x 400 mg every 8 hours). Primary endpoints were 5-ASA area under the plasma concentration versus time curve from zero to 24 hours (AUC24) and total 5-ASA percent of dose excreted (A'e \[%\]) over the 24-hour period on Day 7.


Eligibility criteria: Inclusion Criteria:

* Males or females between 18 and 45 years of age, inclusive, at screening and in good general health based on medical history, physical examination, and laboratory evaluation;
* If female, must be (as documented by patient reported medical history):
* postmenopausal (at least 1 year without spontaneous menses), or
* surgically sterile (tubal ligation or hysterectomy), or
* using acceptable contraception \[e.g., sexual partner with non-reversed vasectomy (with azoospermia in 2 tests), 2 barrier methods (e.g., condom, diaphragm, or spermicide), or intra-uterine device\];
* Body mass index (BMI) between 18 and 32 kg/m2, inclusive;
* Able to swallow the assigned study medication tablet whole; and,
* Able to fulfill the requirements of the protocol and provide written informed consent.

Exclusion Criteria:

* History or presence of any condition or gastrointestinal (GI) surgery causing malabsorption or an effect on GI motility;
* Any uncontrolled acute disease or major surgical operation requiring hospitalization within 1 month of screening;
* History of diabetes, syncope, cardiovascular, hepatic, or renal disease;
* Uncontrolled chronic diseases such as hypertension, systemic lupus erythematosus, or rheumatoid arthritis;
* History of cancer within the last 5 years (except for basal cell carcinoma with a documented 6-month remission);
* Any known enzyme-inducer, enzyme-inhibitor, or reported chronic exposure to enzyme-inducers such as paint solvents or pesticides within 30 days of treatment;
* Any prescription drug or herbal remedy within 14 days prior to scheduled dosing

Primary outcomes:
measure: Pharmacokinetic endpoints of primary interest include AUC24 and the amount of 5-ASA excreted in the urine by subjects dosed with Asacol and Lialda.
timeFrame: Day 7
Secondary outcomes:
Other outcomes:
Locations:
city: Miami
country: United States
facility: Research Site
state: Florida
Study officials:
affiliation: Procter and Gamble
name: William S Aronstein, MD, PhD
role: STUDY_DIRECTOR
References:
citation: Vande Casteele N, Jakate A, McNamee B, Sandborn WJ. Similar pharmacokinetics of three dosing regimens comprising two oral delayed-release mesalamine formulations in healthy adult volunteers: Randomised, open-label, parallel-group study. Br J Clin Pharmacol. 2021 Mar;87(3):1141-1149. doi: 10.1111/bcp.14479. Epub 2020 Aug 10.