Pharmacokinetic Characterization of Two Novel CG5503 Tablet Formulations in Healthy Volunteers

NCT03956134 | Completed Phase 1

• 1 other identifier: HP5503/12
• Study Type: interventional
• Target: 10
• Locations: 1 country
• Sites: 1

Brief Summary

This study investigated the pharmacokinetics (how a drug is taken up and excreted from the body), safety, and tolerability of 2 new tapentadol (CG5503) tablet formulations compared to a previously characterized tapentadol prolonged-release (PR) tablet formulation.

Conditions

Pharmacokinetics

Outcome Measures

Primary Outcomes (4)

• Pharmacokinetic parameter: Cmax

  19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the maximum observed serum concentration (Cmax) was based on the tapentadol base concentrations measured in serum samples using a validated liquid chromatography/tandem mass spectrometry (LC-MS/MS) method.

  Pre-dose up to 32 hours post-dose

• Pharmacokinetic parameter: AUC0-t

  19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the area under the concentration time curve (AUC) from 0 hours to time t (=32 hours) (AUC0-t) was based on the tapentadol base concentrations measured in serum samples.

  Pre-dose up to 32 hours post-dose

• Pharmacokinetic parameter: AUC0-inf

  19 Blood samples were collected from pre-dose up to 32 hours post-dose. The AUC from 0 hours to infinity (AUC0-inf) was extrapolated from the AUC from administration to the last measured concentration.

  Pre-dose up to 32 hours post-dose

• Pharmacokinetic parameter: tmax

  19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the time to reach Cmax (tmax) was determined based on the tapentadol base concentrations measured in serum samples.

  Pre-dose up to 32 hours post-dose

Secondary Outcomes (5)

• Pharmacokinetic parameter: MRT

  Pre-dose up to 32 hours post-dose

• Pharmacokinetic parameter: CL/f

  Pre-dose up to 32 hours post-dose

• Pharmacokinetic parameter: Vz/f

  Pre-dose up to 32 hours post-dose

• Pharmacokinetic parameter: tlag

  Pre-dose up to 32 hours post-dose

• Pharmacokinetic parameter: t1/2z

  Pre-dose up to 32 hours post-dose

Study Arms (5)

Tapentadol Test Product 1 (fasting)

EXPERIMENTAL

Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fasting condition.

Drug: Tapentadol Test Product 1

Tapentadol Test Product 2 (fasting)

EXPERIMENTAL

Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fasting condition.

Drug: Tapentadol Test Product 2

Tapentadol Test Product 1 (fed)

EXPERIMENTAL

Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fed condition.

Drug: Tapentadol Test Product 1

Tapentadol Test Product 2 (fed)

EXPERIMENTAL

Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fed condition.

Drug: Tapentadol Test Product 2

Tapentadol PR Reference Product

ACTIVE COMPARATOR

Tapentadol PR tablet formulation given as single oral dose with 240 mL of still mineral water under fasting condition.

Drug: Tapentadol Prolonged-release Reference Product

Interventions

Tapentadol Test Product 1 DRUG

Tapentadol tablet containing 116 mg of tapentadol hydrochloride; Tapentadol Test Product 1 contains different amounts of excipients than Tapentadol Test Product 2

Tapentadol Test Product 1 (fasting); Tapentadol Test Product 1 (fed)

Tapentadol Test Product 2 DRUG

Tapentadol tablet containing 116 mg of tapentadol hydrochloride; Tapentadol Test Product 2 contains different amounts of excipients than Tapentadol Test Product 1

Tapentadol Test Product 2 (fasting); Tapentadol Test Product 2 (fed)

Tapentadol Prolonged-release Reference Product DRUG

Tapentadol PR tablet containing 116 mg of tapentadol hydrochloride

Tapentadol PR Reference Product

Eligibility Criteria

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

You may qualify if:

• Male Caucasian participants, aged 18-55 years;
• Body Mass Index between 18 and 30 kg/m2 inclusive;
• Participants must be in good health as determined by medical history, physical examination, 12-lead electrocardiogram, vital signs, and clinical laboratory parameters;
• Participants giving written informed consent to participate within this study.

You may not qualify if:

• Resting pulse rate equal to or less than 45 or equal to or above 95 beats / min;
• Resting blood pressure: systolic blood pressure equal to or less than 100 and equal to or above 140 mmHg, diastolic blood pressure equal to or less than 50 and equal to or above 90 mmHg;
• Positive human immunodeficiency virus (HIV) type 1/2 antibodies, hepatitis B surface (HBs) antigen, hepatitis B core (HBc) antibodies, hepatitis C virus (HCV) antibodies;
• History or presence of orthostatic hypotension;
• Participation in another clinical study in the last three months before starting this study (exception: characterization of metabolizer status);
• Positive screening of drug abuse;
• Diseases or condition known to interfere with the absorption, distribution, metabolism or excretion of drugs;
• Marked repolarization abnormality (e.g., suspicious or definite congenital long QT syndrome);
• Bronchial asthma;
• Definite or suspected history of drug allergy or hypersensitivity;
• Participants who have received any prescribed and non-prescribed systemic or topical medication two weeks before and during the study with the exception of short term medication, e.g. headache with paracetamol;
• Evidence of alcohol or drug abuse;
• Not able to abstain from drinking of caffeine containing beverages (tea, coffee, chocolate or cola),
• Consumption of any quinine containing beverages (bitter lemon, tonic water) or food within two weeks before and during the study;
• Drinking of alcohol containing beverages within 48 hours before administration of investigational product(s);

Sponsors & Collaborators

• Grünenthal GmbH: lead

Study Sites (1)

Department of Clinical Pharmacology, Grünenthal GmbH

Aachen, 52099, Germany

Location

Study Officials

• Grünenthal Study Director

  Grünenthal GmbH

  STUDY DIRECTOR

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: Randomization was performed according to Williams' design, with 5 periods and 10 sequences. There was a washout of at least 3 days between the consecutive administrations.

Study Record Dates

• First Submitted: May 14, 2019
• First Posted: May 20, 2019
• Study Start: April 1, 2005
• Primary Completion: June 1, 2005
• Study Completion: June 1, 2005
• Last Updated: May 20, 2019

Record last verified: 2019-05

Data Sharing

• IPD Sharing: Will not share

Locations

DE (1)