Pharmacokinetic Characterization of a Prototype Mini Nicotine Lozenge
Introduction Cigarette smoking remains a substantial public health problem. Nicotine replacement therapy (NRT) is an effective treatment that increases the success of a quit attempt. There are different NRT formats with no difference in efficacy, but their pharmaceutical form or route of administration may translate into individual preferences. A novel prototype mini lozenge was developed to offer smokers a new NRT option to aid in their quit attempt. Two studies were conducted to characterize the pharmacokinetic parameters and to evaluate its bioequivalence to a commercially available nicotine mini lozenge. Methods Two randomized, open-label, crossover studies were conducted to evaluate either the 2 or 4 mg dose level. Heavy smokers in otherwise good health were randomly assigned to one of two treatment sequences: the prototype mini lozenge followed by a commercially available mini lozenge, or the converse. After a 5 to 7 day washout period, subjects crossed over to receive the other study treatment. Blood sampling occurred pre- and post-dose nicotine and was assessed using a validated solid-phase extraction with ultra-high-performance liquid chromatography and tandem mass spectrometry. The primary endpoint was bioequivalence as determined by maximal plasma nicotine concentration (Cmax) and the extent of nicotine absorption ($ AUC_{0–t} $ and $ AUC_{0–∞} $). The secondary endpoints included the time to Cmax (Tmax), half-life, the elimination constant (Kel), and safety. Results The prototype mini lozenge was bioequivalent to the commercially available mini lozenge, with no significant difference in Cmax, $ AUC_{0–t} $, or $ AUC_{0–∞} $ or any of the secondary outcomes. The most common treatment-emergent adverse event was throat irritation, of which all cases were mild in severity. There were no serious adverse events. Conclusion The prototype mini lozenge is bioequivalent to a commercially available mini lozenge and may provide smokers with a new oral NRT option to aid in smoking cessation and of tobacco dependence through the relief of nicotine withdrawal symptoms, including cravings..
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:38 |
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| Enthalten in: |
Advances in therapy - 38(2021), 7 vom: 09. Juni, Seite 3997-4012 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Lai, Pamela M. [VerfasserIn] |
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| Links: |
Volltext [lizenzpflichtig] |
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| Themen: |
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| Anmerkungen: |
© The Author(s), under exclusive licence to Springer Healthcare Ltd., part of Springer Nature 2021 |
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| doi: |
10.1007/s12325-021-01798-4 |
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| funding: |
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| 520 | |a Introduction Cigarette smoking remains a substantial public health problem. Nicotine replacement therapy (NRT) is an effective treatment that increases the success of a quit attempt. There are different NRT formats with no difference in efficacy, but their pharmaceutical form or route of administration may translate into individual preferences. A novel prototype mini lozenge was developed to offer smokers a new NRT option to aid in their quit attempt. Two studies were conducted to characterize the pharmacokinetic parameters and to evaluate its bioequivalence to a commercially available nicotine mini lozenge. Methods Two randomized, open-label, crossover studies were conducted to evaluate either the 2 or 4 mg dose level. Heavy smokers in otherwise good health were randomly assigned to one of two treatment sequences: the prototype mini lozenge followed by a commercially available mini lozenge, or the converse. After a 5 to 7 day washout period, subjects crossed over to receive the other study treatment. Blood sampling occurred pre- and post-dose nicotine and was assessed using a validated solid-phase extraction with ultra-high-performance liquid chromatography and tandem mass spectrometry. The primary endpoint was bioequivalence as determined by maximal plasma nicotine concentration (Cmax) and the extent of nicotine absorption ($ AUC_{0–t} $ and $ AUC_{0–∞} $). The secondary endpoints included the time to Cmax (Tmax), half-life, the elimination constant (Kel), and safety. Results The prototype mini lozenge was bioequivalent to the commercially available mini lozenge, with no significant difference in Cmax, $ AUC_{0–t} $, or $ AUC_{0–∞} $ or any of the secondary outcomes. The most common treatment-emergent adverse event was throat irritation, of which all cases were mild in severity. There were no serious adverse events. Conclusion The prototype mini lozenge is bioequivalent to a commercially available mini lozenge and may provide smokers with a new oral NRT option to aid in smoking cessation and of tobacco dependence through the relief of nicotine withdrawal symptoms, including cravings. | ||
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