Study to Evaluate the Pharmacokinetics, Pharmacodynamics and Safety

NCT01820143 | Completed Phase 1

• 1 other identifier: Z-P104-099
• Study Type: interventional
• Target: 40
• Locations: 1 country
• Sites: 1

Brief Summary

The objectives of this study were (a) to evaluate the pharmacokinetics and to evaluate and compare the pharmacodynamics of ilaprazole and esomeprazole following a single dose (Day 1) and once daily (QD) administration for 5 consecutive days each of 10-mg, 20-mg, and 40-mg ilaprazole tablets and 40-mg esomeprazole tablets; (b) to evaluate the safety of 10-mg, 20-mg, and 40-mg ilaprazole tablets following QD oral administration for 5 consecutive days; and (c) to characterize the plasma gastrin concentration profile on Day 1 and Day 5 following QD oral administration of 10-mg, 20-mg, and 40-mg ilaprazole and 40-mg esomeprazole tablets for 5 consecutive days.

Conditions

Healthy; Pharmacokinetics; Pharmacodynamics; Ilaprazole

Outcome Measures

Primary Outcomes (1)

• Pharmacodynamics of mean pH and percentage of time pH

  For each regimen and day, mean pH and percentage of time pH exceeded 3, 4, 5, and 6 were tabulated and descriptive statistics were provided for 24-hour postdose intervals and each of the following intervals of time relative to dosing: 0 to 4 hours, \>4 to 9 hours, \>9 to 12 hours, \>12 to 16 hours, and \>16 to 24 hours.

  for 24 hours dosing of Ilaprazole

Secondary Outcomes (1)

• ilaprazole and esomeprazole plasma concentration data and pharmacokinetic parameter estimates were tabulated and descriptive statistics computed

  for 24 hours dosing of Ilaprazole

Study Arms (4)

Treatment sequence ADBC

EXPERIMENTAL

Regimen A: 10 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen B: 20 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen C: 40 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen D: 40 mg of esomeprazole administered QD for 5 days with 240 mL of water.

Drug: Ilaprazole; Drug: Esomeprazole

Treatment sequence BACD

EXPERIMENTAL

Regimen A: 10 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen B: 20 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen C: 40 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen D: 40 mg of esomeprazole administered QD for 5 days with 240 mL of water.

Drug: Ilaprazole; Drug: Esomeprazole

Treatment sequence CBDA

EXPERIMENTAL

Regimen A: 10 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen B: 20 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen C: 40 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen D: 40 mg of esomeprazole administered QD for 5 days with 240 mL of water.

Drug: Ilaprazole; Drug: Esomeprazole

Treatment sequence DCAB

EXPERIMENTAL

Regimen A: 10 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen B: 20 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen C: 40 mg of ilaprazole administered QD for 5 days with 240 mL of water. Regimen D: 40 mg of esomeprazole administered QD for 5 days with 240 mL of water.

Drug: Ilaprazole; Drug: Esomeprazole

Interventions

Ilaprazole DRUG

Treatment sequence ADBC; Treatment sequence BACD; Treatment sequence CBDA; Treatment sequence DCAB

Esomeprazole DRUG

Treatment sequence ADBC; Treatment sequence BACD; Treatment sequence CBDA; Treatment sequence DCAB

Eligibility Criteria

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

You may qualify if:

• Prior to any study-specific procedures being performed, the subject voluntarily signed the approved informed consent/PIPEDA authorization form after having it fully explained and all questions answered.
• The subject was between 18 and 55 years, inclusive, and was generally in good health.
• Pregnancy test results for all females were negative in order to enter and remain in the study. A serum pregnancy test was performed on all females at Screening, Day -1 of each period, and Day 6 of Period 4 only, or if a subject prematurely discontinued. Results must have been negative in order for study drug to be administered.
• Female subject was using, and agreed to continue the use of, a double-barrier method of birth control. Oral, patch, implants, or injectable contraceptives were accepted as 1 method if the subject had been taking them for greater than 2 months at the Screening Visit. Subjects who had a bilateral tubal ligation, hysterectomy, or bilateral oophorectomy for a minimum of 6 months, or surgical sterilization of partner (vasectomy for 6 months minimum), or were postmenopausal (defined as the absence of menses for 2 years or the absence of menses for 12 months and follicle-stimulating hormone \[FSH\] level of \>40 IU/L) did not require the use of birth control.
• Subject had a negative breath test result for H pylori prior to enrollment.
• At the Screening Visit, subject had a body mass index (BMI) within the range of 18 to 30 kg/m2, as determined by the following calculation.
• Subject was in general good health as evidenced by a medical history, a complete physical examination, and ECG without clinically significant abnormalities.

You may not qualify if:

• Subject had current evidence of cardiovascular, central nervous system, hepatic, hematopoietic, renal, or metabolic dysfunction; serious allergy, asthma, history of significant sensitivity to any drug; or lactose intolerance that would contraindicate taking ilaprazole or esomeprazole or would interfere with the conduct of the study.

Sponsors & Collaborators

• Il-Yang Pharm. Co., Ltd.: lead

Study Sites (1)

MDS Pharma Services

Québec, Canada

Location

MeSH Terms

Interventions

ilaprazole; Esomeprazole

Intervention Hierarchy (Ancestors)

Omeprazole; 2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring

Study Officials

• Gaetano Morelli, MD

  MDS Pharma Services

  PRINCIPAL INVESTIGATOR

Study Design

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

Study Record Dates

• First Submitted: March 25, 2013
• First Posted: March 28, 2013
• Study Start: February 1, 2005
• Primary Completion: April 1, 2005
• Study Completion: April 1, 2005
• Last Updated: March 28, 2013

Record last verified: 2005-06

Locations

CA (1)