To Evaluate the Food Effect and the Absorption Profile of Ibuprofen Modified-Release Tablets 800 mg

NCT05329454 | Completed Phase 1 FDA Drug

• 1 other identifier: OVEIBUA20181121
• Study Type: interventional
• Target: 30
• Locations: 1 country
• Sites: 1

Brief Summary

An open-label, randomized, 3-way crossover study to evaluate the pharmacokinetics of investigational product "Ibuprofen Modified-Release Tablets 800 mg" in comparison to the reference standard "Ibuprofen Regular-Release Tablets 600 mg/800 mg" in normal healthy volunteers Primary objective: To evaluate the food effect of IBUMR and its bioavailability of single and multiple doses compared with reference drugs in normal healthy volunteers. Secondary objectives:

1. 1.To determine and compare the single and multiple dose PK profiles of IBUMR and reference drugs.
2. 2.To identify the effect duration for IBUMR after dose administration by detecting ibuprofen concentrations in plasma.
3. 3.To evaluate the safety profile of single and multiple doses of IBUMR.

Conditions

Chronic Pain

Keywords

Ibuprofen Modified-Release Tablets; Overseas Pharmaceuticals; pain relief

Outcome Measures

Primary Outcomes (8)

• Comparison of single-dose and multiple-dose bioavailability between IBUMR and IBURed

  Comparison of single-dose and multiple-dose bioavailability between IBUMR and IBURed in log-transformed values of area under the curve from time 0 to the last measurable concentration (AUCL)

  After collecting blood samples from the last participant, up to 30 days

• Comparison of single-dose and multi-dose bioavailability of IBUMR and IBURed

  Comparison of single-dose and multiple-dose bioavailability between IBUMR and IBURed in log-transformed values of the peak concentration (Cmax)

  After collecting blood samples from the last participant, up to 30 days

• Comparison of single - and multi-dose bioavailability of IBUMR and IBURed

  Comparison of single-dose and multiple-dose bioavailability between IBUMR and IBURed in log-transformed values of area under the curve from time 0 to infinity (AUCinf).

  After collecting blood samples from the last participant, up to 30 days

• To assess the food effect of IBUMR in the PK parameters

  To assess the food effect of IBUMR in the PK parameters including Cmax

  After collecting blood samples from the last participant, up to 30 days

• To evaluate the food effect of IBUMR on PK parameters

  To assess the food effect of IBUMR in the PK parameters including time to reach peak concentration (Tmax)

  After collecting blood samples from the last participant, up to 30 days

• To evaluate the food effects of IBUMR on PK parameters

  To assess the food effect of IBUMR in the PK parameters including AUCL

  After collecting blood samples from the last participant, up to 30 days

• Evaluate the food effect of IBUMR in PK parameters

  To assess the food effect of IBUMR in the PK parameters including AUCinf

  After collecting blood samples from the last participant, up to 30 days

• Determine the food effect of IBUMR in PK parameters

  To assess the food effect of IBUMR in the PK parameters including elimination half-life (t1/2)

  After collecting blood samples from the last participant, up to 30 days

Secondary Outcomes (23)

• Single-dose PK measures

  After collecting blood samples from the last participant, up to 30 days

• Single dose PK method

  After collecting blood samples from the last participant, up to 30 days

• Single dose PK

  After collecting blood samples from the last participant, up to 30 days

• Single dose PK step

  After collecting blood samples from the last participant, up to 30 days

• Single dose PK design

  After collecting blood samples from the last participant, up to 30 days

Study Arms (6)

Treatment ABC

EXPERIMENTAL

Receive the investigational product and active comparator in a sequence of treatment A, treatment B and treatment C.

Drug: Ibuprofen Tablets

Treatment ACB

EXPERIMENTAL

Receive the investigational product and active comparator in a sequence of treatment A, treatment C and treatment B.

Drug: Ibuprofen Tablets

Treatment BAC

EXPERIMENTAL

Receive the investigational product and active comparator in a sequence of treatment B, treatment A and treatment C.

Drug: Ibuprofen Tablets

Treatment BCA

EXPERIMENTAL

Receive the investigational product and active comparator in a sequence of treatment B, treatment C and treatment A.

Drug: Ibuprofen Tablets

Treatment CAB

EXPERIMENTAL

Receive the investigational product and active comparator in a sequence of treatment C, treatment A and treatment B.

Drug: Ibuprofen Tablets

Treatment CBA

EXPERIMENTAL

Receive the investigational product and active comparator in a sequence of treatment C, treatment B and treatment A.

Drug: Ibuprofen Tablets

Interventions

Ibuprofen Tablets DRUG

Treatment A: One tablet of IBUMR will be administered to the subjects under fasted condition, followed by a minimum of 72-hour washout interval. After the washout period, subjects will receive 1 × IBUMR every 12 hours for a total of 7 doses. Treatment B: One tablet of IBURed will be administered to the subjects under fasted condition, followed by a minimum of 72-hour washout interval. After the washout period, subjects will receive 1 × IBURed every 8 hours for a total of 10 doses. Treatment C: Single dose of IBUMR will be given to the subjects under fed condition (a standard high-fat, high calorie breakfast should be consumed within 30 minutes prior to dosing).

Treatment ABC; Treatment ACB; Treatment BAC; Treatment BCA; Treatment CAB; Treatment CBA

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Subjects whose body mass index (BMI) at screening is within a range of ≥18.5 kg/m2 and \<25.0 kg/m2.
• BMI = Body Weight (kg) / \[Height (m)\]2 And body weight is not less than 50 kg and 45 kg for males and females, respectively.
• Subject's medical history shows no contraindication to the test medications (hypersensitivity to ibuprofen or any component of test and reference products) and non-steroidal anti-inflammatory drugs (NSAIDs).
• Subjects who are judged to be in good health by the investigator based upon the results of physical examination (PE), vital signs, and routine laboratory tests.
• The female subject shows negative pregnancy test results within 30 days prior to the first dose of the study.
• The subject did not take any of the following medications in the specified durations:
• Any systemically absorbed medication within 14 days (excluding vitamins, food supplements and hormone contraceptives not ibuprofen drug interactions) prior to the first dose of the study
• Any enzyme inducer/inhibitor and/or known hepatic or renal clearance-altering agents (e.g., erythromycin, cimetidine, barbiturates, phenothiazine, clarithromycin, troleandomycin, ketoconazole, miconazolem fluconazole, itraconazole) within 30 days prior to the first dose of the study.
• Subjects are willing to comply with protocol-stated requirements, instructions and restrictions, followed by understanding and signing the written informed consent form by the subject or legal representative if he/she is under the statutory age of consent as per the local authority.

You may not qualify if:

• Subjects with any properly diagnosed disease within 30 days prior to the first dose of the study.
• Subjects with a clinically significant hematological, endocrine, cardiovascular, hepatic, renal, gastrointestinal, and/or pulmonary disorder; subjects with any predisposing condition that might interfere with the absorption, distribution, metabolism and excretion of drugs; subjects who has had any previous gastrointestinal surgery or coronary artery bypass graft.
• Subjects who require treatment with any medications, either prescription or non-prescription (excluding vitamins and food supplements), within 30 days prior to the first dose of the study
• Subjects have participated in investigational drug trials and took any investigational drug within 60 days prior to the first does of the study.
• Subjects had blood donation more than 250 and 500 mL within 60 and 90 days, respectively prior to the first dose of the study.
• Subjects had a history of drug abuse or alcohol abuse according to the Diagnostic and Statistical Manual of Mental Disorders 4th edition (DSM-IV) criteria.
• Subjects cannot stop smoking and caffeine-intakes for 48 hours prior to the first dose of the study and during the entire study period.
• Subjects who are pregnant or lactating.
• Subjects who have been tested positive for the following tests:
• Human immunodeficiency virus (HIV)
• Hepatitis B virus (HBV)
• Hepatitis C virus (HCV)
• Treponema pallidum (STS test)
• For enrollment of female subjects with child-bearing potential, the subject must be practicing sexual abstinence or be using and willing to continue to use a medically acceptable form of birth control for at least 30 days prior to screening (that period will extend to 3 months for oral contraceptive use) and for at least 30 days after the last dose of study drug. For a subject to be considered not to be of child-bearing potential, she must have been amenorrheic for at least 2 years, or must have had a hysterectomy, a bilateral tubal ligation, and/or a bilateral oophorectomy (as determined by the medical history). The male partner of a female study subject with childbearing potential must use a condom and ensure that his partner uses a suitable method of contraception as outlined above.
• Subjects with underlying medical, mental, psychological, or other inappropriate conditions that would impair treatment compliance, or in the opinion of the investigator would not permit to participate in the study.

Sponsors & Collaborators

• Overseas Pharmaceuticals, Ltd.: lead

Study Sites (1)

Taipei Medical University Hospital

Taiwan, China

Location

Related Publications (10)

• Albert KS, Gernaat CM. Pharmacokinetics of ibuprofen. Am J Med. 1984 Jul 13;77(1A):40-6. doi: 10.1016/s0002-9343(84)80017-0.

  PMID: 6465162 BACKGROUND

• Albert KS, Gillespie WR, Wagner JG, Pau A, Lockwood GF. Effects of age on the clinical pharmacokinetics of ibuprofen. Am J Med. 1984 Jul 13;77(1A):47-50. doi: 10.1016/s0002-9343(84)80018-2.

  PMID: 6380280 BACKGROUND

• Barkin RL, Buvanendran A. Focus on the COX-1 and COX-2 agents: renal events of nonsteroidal and anti-inflammatory drugs-NSAIDs. Am J Ther. 2004 Mar-Apr;11(2):124-9. doi: 10.1097/00045391-200403000-00007.

  PMID: 14999364 BACKGROUND

• Davies NM. Clinical pharmacokinetics of ibuprofen. The first 30 years. Clin Pharmacokinet. 1998 Feb;34(2):101-54. doi: 10.2165/00003088-199834020-00002.

  PMID: 9515184 BACKGROUND

• Goldberg DS, McGee SJ. Pain as a global public health priority. BMC Public Health. 2011 Oct 6;11:770. doi: 10.1186/1471-2458-11-770.

  PMID: 21978149 BACKGROUND

• Legg T, Paluch E, Jayawardena S. Single- and Multiple-Dose Pharmacokinetics of Immediate-Release/Extended-Release Ibuprofen Tablets. Clin Pharmacol Drug Dev. 2017 Jan;6(1):36-43. doi: 10.1002/cpdd.288. Epub 2016 Sep 22.

  PMID: 27364900 BACKGROUND

• Devarakonda K, Kostenbader K, Giuliani MJ, Young JL. Single- and multiple-dose pharmacokinetics of biphasic immediate-release/extended-release hydrocodone bitartrate/acetaminophen (MNK-155) compared with immediate-release hydrocodone bitartrate/ibuprofen and immediate-release tramadol HCl/acetaminophen. J Pain Res. 2015 Sep 30;8:647-56. doi: 10.2147/JPR.S83416. eCollection 2015.

  PMID: 26508885 BACKGROUND

• O'Connor TP, Anderson AM, Lennox B, Muldoon C. A novel sustained-release formulation of ibuprofen provides effective once-daily therapy in the treatment of rheumatoid arthritis and osteoarthritis. Br J Clin Pract. 1993 Jan-Feb;47(1):10-3.

  PMID: 8461240 BACKGROUND

• Varrassi G, Pergolizzi JV, Dowling P, Paladini A. Ibuprofen Safety at the Golden Anniversary: Are all NSAIDs the Same? A Narrative Review. Adv Ther. 2020 Jan;37(1):61-82. doi: 10.1007/s12325-019-01144-9. Epub 2019 Nov 8.

  PMID: 31705437 BACKGROUND

• Volans G, Hartley V, McCrea S, Monaghan J. Non-opioid analgesic poisoning. Clin Med (Lond). 2003 Mar-Apr;3(2):119-23. doi: 10.7861/clinmedicine.3-2-119. No abstract available.

  PMID: 12737366 BACKGROUND

MeSH Terms

Conditions

Chronic Pain

Interventions

Ibuprofen

Condition Hierarchy (Ancestors)

Pain; Neurologic Manifestations; Signs and Symptoms; Pathological Conditions, Signs and Symptoms

Intervention Hierarchy (Ancestors)

Phenylpropionates; Acids, Carbocyclic; Carboxylic Acids; Organic Chemicals

Study Officials

• Ming-Che Liu, M.D

  Taipei Medical University Hospital

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: An open label, randomized, single and multiple-dose, test-versus-reference drug, fed-versus-fasted, 3-way crossover study.

Study Record Dates

• First Submitted: February 4, 2021
• First Posted: April 15, 2022
• Study Start: December 24, 2020
• Primary Completion: February 6, 2021
• Study Completion: July 18, 2021
• Last Updated: April 15, 2022

Record last verified: 2021-12

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)