Comparative Bioavailability Study of an Immediate Release and Controlled Release Oral Formulations of Huperzine A

An Open-label, Three-period, Crossover Study in Healthy Volunteers to Evaluate the Relative Bioavailability of Two Different Release Rate Controlled Release Formulations of Huperzine A (0.4mg)Compared to the Equivalent Dose of an Immediate Release Formulation.

The purpose of this study is to develop oral controlled release formulation of Huperzine A that will provide optimal pharmacokinetic profile of the drug enhancing safety and compliance, as possible cure to neurodegenerative disorders.

Study Overview

• Status: Unknown
• Conditions: Healthy; Bioavailability
• Intervention / Treatment: Drug: Huperzine A

• Study Type: Interventional
• Enrollment (Anticipated): 8
• Phase: Not Applicable

Contacts and Locations

• Study Contact: Name: Gregory Burshtein, MA; Phone Number: 97226758665/4; Email: bursht@gmail.com

Study Locations

• Israel
  • Jerusalem, Israel
    • Hadassah University Hospital
    • Contact: Eliad Davidson, MD; Phone Number: 97226776911; Email: edavidson@hadassah.org.il

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 35 years (ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

1. Healthy males between the age of 18 and 35, inclusive (ASA = 1)
2. Body weight > 50 kg
3. Subject has a BMI less than 27 and more than 20
4. Participants should be able to ingest oral medication
5. The ability to understand and sign a written informed consent form, prior to participation and the willingness to comply with all study requirements

Exclusion Criteria:

1. History of drug sensitivity or drug allergy
2. History of sensitivity to eggs
3. Subject has a BMI less than 20 and more than 27
4. Previous participation in an investigational trial involving administration of any investigational compound within 1 month prior to the current study
5. History of alcoholism or drug addiction
6. Any medication taken including over-the-counter medications and herbal products within 14 days of commencing study drug dosing with the exception of vitamins and/or paracetamol. When a concomitant medication is necessary, this will be reviewed by the investigator and if not contraindicated, may be continued at the same dose and frequency during the study period
7. History of clinically important illness (ASA>1); Disorders or conditions that could affect the absorption, distribution, metabolism and/or excretion of drugs (e.g. malabsorption, edema, renal or hepatic insufficiency)
8. Inability to relate to and/or cooperate with the investigators
9. Blood loss or donation greater than 200ml in the 3 months prior to the trial
10. Exhausting physical exercise during the previous 48 hours to drug administration
11. Subjects who have smoked or used nicotine-containing products within 6 months prior to study entry

Study Plan

How is the study designed?

Design Details

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

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
ACTIVE_COMPARATOR: IR formulation; Healthy volunteers will receive imediate release formulation of Huperzine A (0.4mg)	Drug: Huperzine A; Each volunteer will receive single dose of three different formulations of Huperzine A. One immediate release formulation of 0.4mg and two different controlled release formulations at same dose. Between the study phases will be a washout period of at least 21 days.
EXPERIMENTAL: CR 1; CR formulation Healthy volunteers will receive controlled release formulation 1 of Huperzine A (0.4mg)	Drug: Huperzine A; Each volunteer will receive single dose of three different formulations of Huperzine A. One immediate release formulation of 0.4mg and two different controlled release formulations at same dose. Between the study phases will be a washout period of at least 21 days.
EXPERIMENTAL: CR 2; CR formulation Same volunteers will receive controlled release formulation 2 of Huperzine A (0.4mg)	Drug: Huperzine A; Each volunteer will receive single dose of three different formulations of Huperzine A. One immediate release formulation of 0.4mg and two different controlled release formulations at same dose. Between the study phases will be a washout period of at least 21 days.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetic parameters of Huperzine A different formulations	Pharmacokinetic parameters: C max, T max, AUC, t1/2	Blood samples will be taken for 36 hours after Huperzine A administration

Secondary Outcome Measures

Outcome Measure	Time Frame
Laboratory testing of peripheral AchE inhibition by Huperzine A. Evaluation of adverse events. Laboratory testing of peripheral AchE inhibition by Huperzine A. Evaluation of adverse events.	36 hours

Collaborators and Investigators

• Sponsor: Hadassah Medical Organization
• Collaborators: Hebrew University of Jerusalem
• Investigators: Principal Investigator: Michael Friedman, Proffesor, Institute for Drug Research, Hebrew University of Jerusalem, Israel

Study record dates

Study Major Dates

• Study Start: September 1, 2010
• Primary Completion (ANTICIPATED): January 1, 2011
• Study Completion (ANTICIPATED): April 1, 2011

Study Registration Dates

• First Submitted: June 2, 2010
• First Submitted That Met QC Criteria: June 2, 2010
• First Posted (ESTIMATE): June 3, 2010

Study Record Updates

• Last Update Posted (ESTIMATE): June 3, 2010
• Last Update Submitted That Met QC Criteria: June 2, 2010
• Last Verified: May 1, 2010

More Information

Terms related to this study

• Keywords: Pharmacokinetic profile of controlled release formulation of Huperzine A; Bioequivalence of Huperzine A IR formulation and CR formulation
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Cholinergic Agents; Enzyme Inhibitors; Neuroprotective Agents; Protective Agents; Cholinesterase Inhibitors; Huperzine A
• Other Study ID Numbers: HUPA - CR- HMO-CTIL; HUPA-HU-1 (REGISTRY: Haddasah University Hospital)