A Bioavailability Study of Sebacoyl Dinalbuphine Ester IM Injection in Healthy Volunteers

A Bioavailability Study of Sebacoyl Dinalbuphine Ester IM Injection vs. Bain®. Nalbuphine HCl IM Injection, in Healthy Volunteers

This study is to evaluate the relative bioavailability of nalbuphine after single IM injection of Sebacoyl Dinalbuphine Ester (SDE) injection and Bain®, Nalbuphine HCl IM injection in healthy volunteers.

Study Overview

• Status: Completed
• Conditions: Pain; Analgesia Disorder
• Intervention / Treatment: Drug: Bain®; Drug: SDE

• Study Type: Interventional
• Enrollment (Actual): 12
• Phase: Phase 1

Contacts and Locations

Study Locations

• Taiwan
  • New Taipei City, Taiwan, 23561
    • Taipei Medical University - Shuang Ho Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years and older (ADULT, OLDER_ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

1. Subjects must be male or female adults in good health on the basis of medical history, physical examination, electrocardiogram, chest X-ray, and routine laboratory evaluations.

2. Vital signs (after 3 minutes resting in a upright position) which are within the following ranges:

   Ear body temperature between 35.0-37.5°C. Systolic blood pressure, 90-140 mm Hg. Diastolic blood pressure, 50-90 mm Hg. Pulse rate, 50-90 bpm. Fasting blood glucose, < 110 mg/dL.

3. Within -20% to +20% of the ideal body weight. For male subjects, body weight must be above 50 kg and for female subjects, body weight must be above 45 kg.
4. Able to sign informed consent prior to study.
5. Able to communicate well with the investigator and comply with the requirements of the study.

Exclusion Criteria:

1. Use of any alcohol-containing products, prescription medications or over-the-counter, non-prescription preparations (including herbal preparations) within 2 weeks prior to study entry unless deemed acceptable by the Investigator (except up to 5 doses of ≤ 1000 mg of acetaminophen or ≤ 400 mg ibuprofen within this 2 week period).
2. Alcohol or caffeine ingested within 48 hours prior to dosing.
3. Significant illness within 2 weeks prior to dosing.
4. Participation in any clinical investigation within 2 months prior to dosing or longer as required by local regulation.
5. Donation or loss of more than 500 mL of blood within 3 months prior to dosing. Donation or loss of more than 250 mL of blood within 2 months prior to dosing.
6. Presence of cardiovascular disease.
7. Presence of gastrointestinal disease.
8. Presence of asthma or lung disease.
9. Presence of liver disease or liver injury as indicated by an abnormal liver function profile such as AST, ALT, gamma-GT, Alkaline Phosphatase, or Total Bilirubin. (value of AST or ALT above 3 times of the upper limit of the normal range; other items clinically significant abnormality judged by investigator).
10. Presence of impaired renal function as indicated by abnormal creatinine or BUN values or abnormal urinary constituents. (value of creatinine or BUN beyond the range from -20% of the lower limit of the normal range to +20% of the upper limit of the normal range; other items clinically significant abnormality judged by investigator)
11. Presence of neurological disease.
12. Presence of psychiatric disease.
13. Subject is positive for HIV immunology test.
14. A known hypersensitivity to nalbuphine or its analogs.
15. History of drug or alcohol abuse within 12 months prior to dosing.
16. Permanent confinement to an institution.
17. Pregnant or lactating women.
18. Individuals are judged by the investigator or pharmacokineticist to be undesirable as subjects for other reasons

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: NON_RANDOMIZED
• Interventional Model: CROSSOVER
• Masking: NONE

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Period I (reference drug); Before administration of investigational products, subjects should be fasted for 10 hours. On the dosing day, subjects will be confined after administration and won't be discharged until after completion of sample collections for 24 hours following dosing in Period I (Bain® IM injection).	Drug: Bain®; Nalbuphine HCl 20mg, IM injection; Other Names: Nalbuphine HCl
Experimental: Period II (Test drug); Subjects will be back to the clinical site to join Period II (SDE IM injection) and will be discharged after completion for sample collections for 24 hours post drug administration.	Drug: SDE; Sebacoyl Dinalbuphine Ester 150mg/2ml, IM injection; Other Names: Sebacoyl Dinalbuphine Ester Injection; LT1001

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Blood concentration of Nalbuphine HCl	Protocol-specified pharmacokinetic parameters will be determined from blood samples collected after each administration of study drug to assess the relative bioavailability of SDE.	Period I: pre-dose (0 h) and 0.083, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours post dose for Bain®, Nalbuphine HCl IM injection ; Period II: pre-dose (0 h) and 6, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post dose for SDE IM injection

Collaborators and Investigators

• Sponsor: Lumosa Therapeutics Co., Ltd.

Study record dates

Study Major Dates

• Study Start: January 1, 2015
• Primary Completion (Actual): April 1, 2015
• Study Completion (Actual): April 1, 2015

Study Registration Dates

• First Submitted: May 13, 2015
• First Submitted That Met QC Criteria: May 15, 2015
• First Posted (Estimate): May 18, 2015

Study Record Updates

• Last Update Posted (Estimate): May 19, 2015
• Last Update Submitted That Met QC Criteria: May 18, 2015
• Last Verified: May 1, 2015

More Information

Terms related to this study

• Keywords: pain; Nalbuphine; SDE; dinalbuphine; SDN; LT1001
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Central Nervous System Depressants; Peripheral Nervous System Agents; Analgesics; Sensory System Agents; Analgesics, Opioid; Narcotics; Nalbuphine
• Other Study ID Numbers: LT1001-103