NRL-4, a nasal spray formulation of the atypical antipsychotic olanzapine is being developed by Neurelis Inc. for use as a rescue medication for acute episodes of agitation in schizophrenia, schizoaffective and bipolar I disorder. Also being tested are different concentrations of Intravail A3. Intravail A3 belongs to a class of nonionic surfactants known as alkylglycosides. Alkylglycosides have been extensively studied for their ability to promote increased bioavailability of drugs via the nasal, oral, and ocular routes. In this study it will be tested if the olanzapine in the two Test products will show comparable pharmacokinetics, safety and tolerability in comparison to the Reference product through the primary pharmacokinetic parameters Cmax, AUC from time 0 to time t and AUC from time 0 to infinity, and safety assessments, including nasal irritation, sedation and pain scales.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
24
7.5 mg
International Pharmaceutical Research Center (IPRC) Clinical Site
Amman, Jordan, Jordan
(1) Bioavailability of test products compared to reference product based on pharmacokinetic parameter of AUC from time 0 to time t
Characterize the pharmacokinetics of two Test Products (one product, A, is 7.5 mg olanzapine per 100 µL with 0.25% Intravail A3 as absorption enhancer and another product is, B, 7.5 mg olanzapine per 100 µL with 0.50% Intravail A3 as absorption enhancer via nasal spray) relative to Reference Product (C, intramuscular injection) after a single dose of 7.5 mg olanzapine to healthy male adults under fasting conditions.
Time frame: 240 hours
(2) Bioavailability of test products compared to reference product based on pharmacokinetic parameter of Cmax
Characterize the pharmacokinetics of two Test Products (one product, A, is 7.5 mg olanzapine per 100 µL with 0.25% Intravail A3 as absorption enhancer and another product is, B, 7.5 mg olanzapine per 100 µL with 0.50% Intravail A3 as absorption enhancer via nasal spray) relative to Reference Product (C, intramuscular injection) after a single dose of 7.5 mg olanzapine to healthy male adults under fasting conditions.
Time frame: 240 hours
(3) Bioavailability of test products compared to reference product based on pharmacokinetic parameter of AUC from time 0 to infinity
Characterize the pharmacokinetics of two Test Products (one product, A, is 7.5 mg olanzapine per 100 µL with 0.25% Intravail A3 as absorption enhancer and another product is, B, 7.5 mg olanzapine per 100 µL with 0.50% Intravail A3 as absorption enhancer via nasal spray) relative to Reference Product (C, intramuscular injection) after a single dose of 7.5 mg olanzapine to healthy male adults under fasting conditions.
Time frame: 240 hours
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