Comparative assessment of the absorption of a generic formulation of (2S)-2-[17-(cyclopropylmethyl)-4, 5a-epoxy-3-hydroxy-6-methoxy-6a, 14-ethano-14a-morphinan-7a-yl]-3, 3-dimethylbutan-2-ol transdermal patch against the innovator (2S)-2-[17-(cyclopropylmethyl)-4, 5a-epoxy-3-hydroxy-6-methoxy-6a, 14-ethano-14a-morphinan-7a-yl]-3, 3-dimethylbutan-2-ol transdermal patch conducted under fasting conditions with the inclusion of a naltrexone block in healthy male and female volunteers
- Conditions
- (2S)-2-[17-(cyclopropylmethyl)-4, 5a-epoxy-3-hydroxy-6-methoxy-6a, 14-ethano-14a-morphinan-7a-yl]-3, 3-dimethylbutan-2-ol is a partial opioid agonist indicated for the management of severe pain.Anaesthesiology - Pain management
- Registration Number
- ACTRN12622000133730
- Lead Sponsor
- Zenith Technology Corporation Limited
- Brief Summary
Not available
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- Completed
- Sex
- All
- Target Recruitment
- 26
Healthy male and non-pregnant females
Aged between 18 and 55
Non-smoker
BMI between 18 and 32 inclusive
Normal, healthy individuals as determined by medical history, physical examination, ECG, blood pressure and laboratory tests
Able to provide written informed consent
Any history of recent recurrent attacks of bronchitis, asthma, migraine headaches
Concomitant drug therapy of any kind
Sensitivity to (2S)-2-[17-(cyclopropylmethyl)-4, 5a-epoxy-3-hydroxy-6-methoxy-6a, 14-ethano-14a-morphinan-7a-yl]-3, 3-dimethylbutan-2-ol or any other similar class of medicines, or the excipients of (2S)-2-[17-(cyclopropylmethyl)-4, 5a-epoxy-3-hydroxy-6-methoxy-6a, 14-ethano-14a-morphinan-7a-yl]-3, 3-dimethylbutan-2-ol.
Sensitivity to naltrexone or any other similar class of medicines, or the excipients of naltrexone
History of any conditions that might interfere with the absorption, distribution, metabolism or excretion of the drug
Females who are pregnant and/or are breastfeeding
Smoker (anyone who has smoked in the last 6 months)
History of alcohol or drug abuse or dependency
Participation in a drug study within 60 days of the start of the study or donated blood in the 60 days preceding the study.
Volunteers for whom the Clinical Investigator believes, for any reason, that participation would not be an acceptable risk
Study & Design
- Study Type
- Interventional
- Study Design
- Not specified
- Primary Outcome Measures
Name Time Method To compare the bioavailability of (2S)-2-[17-(cyclopropylmethyl)-4, 5a-epoxy-3-hydroxy-6-methoxy-6a, 14-ethano-14a-morphinan-7a-yl]-3, 3-dimethylbutan-2-ol (as summarised by Cmax and AUC). All plasma samples will be assayed for (2S)-2-[17-(cyclopropylmethyl)-4, 5a-epoxy-3-hydroxy-6-methoxy-6a, 14-ethano-14a-morphinan-7a-yl]-3, 3-dimethylbutan-2-olusing one fully validated Liquid Chromatography with tandem mass spectrometry (LC-MS/MS) method. Validation will be conducted to comply with EU and FDA guidelines.[ 0 (pre-dose) and at 1, 4, 6, 10, 12, 18, 24, 36, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 176, 192, 200, 216, 224, 240 and 264 hours post dosing.]
- Secondary Outcome Measures
Name Time Method Time to maximum peak concentration (Tmax) will be determined by plasma sample analysis. Tmax will be the time where the maximum concentration occurred in the sample points.[ 0 (pre-dose) and at 1, 4, 6, 10, 12, 18, 24, 36, 48, 60, 72, 84, 96, 108, 120, 132, 144, 156, 168, 176, 192, 200, 216, 224, 240 and 264 hours post dosing.]