A Pharmacokinetic Study of the Relative Bioavailability of Paliperidone ER Formulations With Different Release Profiles and a Comparison to Paliperidone IR

NCT00791193 | Completed Phase 1

• 1 other identifier: CR013474
• Study Type: interventional
• Target: 80
• Locations: 0 countries
• Sites: N/A

Brief Summary

The primary purpose of this study is to evaluate the pharmacokinetics and relative bioavailability of paliperidone ER formulations with slow, target, and fast in vitro release rates after administration of a single 12 mg dose. The slow and fast releasing ER tablets have in vitro release rates outside the current commercial specifications. Therefore, in order to support widening of the specification limits, this study will be performed. The target formulation to be used is representative of the commercial formulation. Other objectives of this study are 1) to compare the relative bioavailability of paliperidone ER formulations with slow, target, and fast in vitro release rates to the paliperidone IR formulation; 2) to explore the in vitro in vivo correlation (IVIVC) for the paliperidone ER formulation; and 3) to evaluate the safety and tolerability of the different paliperidone ER formulations.

Conditions

Schizophrenia

Keywords

Paliperidone ER; Antipsychotic drugs; Schizophrenia; Mood disorders

Outcome Measures

Primary Outcomes (1)

• To evaluate the pharmacokinetics and relative bioavailability of paliperidone ER formulations with different in vitro release rates (slow, fast) compared to the target formulation after a single 12 mg dose.

Secondary Outcomes (1)

• To evaluate the relative bioavailability of paliperidone ER formulations with different in vitro release rates compared to the paliperidone IR formulation, to explore an IVIVC for the paliperidone ER formulation, and to assess safey and tolerability

Interventions

Paliperidone ER DRUG

Eligibility Criteria

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

You may qualify if:

• Must agree to use an efficient method of birth control as deemed appropriate by the investigator and to not donate sperm during the study and for 3 months after receiving the last dose of study drug
• Body mass index (weight \[kg\]/height \[m2\]) between 18 and 30 kg/m2 (inclusive), and body weight not less than 50 kg
• Blood pressure (after the volunteer is supine for 5 minutes) between 100 and 140 mmHg systolic, inclusive, and between 50 and 90 mmHg diastolic. Pulse rate measured over 60 seconds should be between 40 and 100 beats per minute (bpm)
• Non-smoker

You may not qualify if:

• History of or current significant medical illness including (but not limited to) cardiac arrhythmias or other cardiac disease, hematologic disease, coagulation disorders (including any abnormal bleeding or blood dyscrasias), lipid abnormalities, significant pulmonary disease, including bronchospastic respiratory disease, diabetes mellitus, renal or hepatic insufficiency, thyroid disease, neurologic or psychiatric disease, infection, or any other illness that the investigator considers should exclude the volunteer
• History or presence of circumstances that may increase the risk of the occurrence of torsade de pointes and/or sudden death in association with the use of drugs that prolong the QTc interval, including: bradycardia (heart rate \< 40 bpm on the ECG), clinically significant abnormality on the ECG, demonstration of repeated prolonged QTcF \> 450 ms (QTc interval corrected for heart rate using Fridericia's formula), as measured on more than one ECG (either during screening, or from prior medical record)
• The following cardiac conditions: sick sinus syndrome, complete AV block, congestive heart failure, polymorphic ventricular tachycardia
• Clinically relevant hypocalcemia, hypokalemia or hypomagnesemia
• Presence of congenital prolongation of the QT interval (Romano-Ward Syndrome, Jervell and Lange-Nielsen syndrome)
• History of any cancer, with the exception of basal cell carcinoma: Clinically significant abnormal values for hematology, clinical chemistry or urinalysis at screening or at admission to the study center, in the opinion of the investigator
• Clinically significant abnormality on physical examination, in the opinion of the investigator
• At screening, has signs of orthostatic hypotension defined as a decrease in systolic ( \> 20 mmHg) or diastolic (\> 10 mmHg) blood pressure after standing for at least 2 minutes, that is associated with an increase in pulse rate of \>15 bpm compared with supine measurements
• Use of any prescription or nonprescription medication (including vitamins and herbal supplements), except for paracetamol (acetaminophen) or ibuprofen, within 14 days before the first dose of the study drug is scheduled

Sponsors & Collaborators

• Johnson & Johnson Pharmaceutical Research & Development, L.L.C.: lead

Related Links

• A pharmacokinetic study of the relative bioavailability of paliperidone ER formulations with different release profiles and a comparison to paliperidone IR

MeSH Terms

Conditions

Schizophrenia; Mood Disorders

Interventions

Paliperidone Palmitate

Condition Hierarchy (Ancestors)

Schizophrenia Spectrum and Other Psychotic Disorders; Mental Disorders

Intervention Hierarchy (Ancestors)

Isoxazoles; Azoles; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Pyrimidines

Study Officials

• Johnson & Johnson Pharmaceutical Research and Development, L.L.C. Clinical Trial

  Johnson & Johnson Pharmaceutical Research & Development, L.L.C.

  STUDY DIRECTOR

Study Design

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

Study Record Dates

• First Submitted: November 13, 2008
• First Posted: November 14, 2008
• Study Start: March 1, 2007
• Study Completion: May 1, 2007
• Last Updated: May 18, 2011

Record last verified: 2010-04