The absolute bioavailability of racemic ketamine from a novel sublingual formulation
AIM: The principal study objective was to investigate the pharmacokinetic characteristics of a new sublingual ketamine wafer and to establish its absolute bioavailability and local tolerability. METHODS: The study was of open label, two way randomized crossover design in eight healthy male volunteer...
| Main Authors: | , , , , |
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| Format: | Journal Article |
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Blackwell Publishing
2014
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| Online Access: | http://hdl.handle.net/20.500.11937/25299 |
| _version_ | 1848751670120415232 |
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| author | Rolan, P. Lim, Stephen Sunderland, Bruce Liu, Yandi Molnar, V. |
| author_facet | Rolan, P. Lim, Stephen Sunderland, Bruce Liu, Yandi Molnar, V. |
| author_sort | Rolan, P. |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | AIM: The principal study objective was to investigate the pharmacokinetic characteristics of a new sublingual ketamine wafer and to establish its absolute bioavailability and local tolerability. METHODS: The study was of open label, two way randomized crossover design in eight healthy male volunteers. Each participant received either a single 10 mg intravenous dose as a constant rate 30 min infusion or a 25 mg sublingual dose of ketamine wafer in two treatment periods with a 7 day wash out. Pharmacokinetic blood sampling and local tolerability and safety assessments were carried out during 24 h following both dosing occasions. Plasma concentrations were analyzed by non-compartmental methods and local tolerability was assessed using modified Likert scales. RESULTS: The median (90% CI lower, upper limit) absolute bioavailability of sublingual ketamine was 29% (27, 31%). The first quantifiable plasma ketamine concentration was observed within 5 min for all eight participants for both routes of administration and the median (min–max) time of the peak plasma concentration was 0.75 h (0.25–1.0 h) after sublingual administration. The ketamine wafer had very good local tolerability. CONCLUSION: Sublingual administration of the ketamine wafer resulted in rapid absorption. The ketamine wafer has comparable bioavailability with other oral transmucosal formulations of ketamine but with markedly reduced inter-subject variability, warranting further evaluation as analgesic adjunct. |
| first_indexed | 2025-11-14T07:56:25Z |
| format | Journal Article |
| id | curtin-20.500.11937-25299 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T07:56:25Z |
| publishDate | 2014 |
| publisher | Blackwell Publishing |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-252992017-09-13T15:19:09Z The absolute bioavailability of racemic ketamine from a novel sublingual formulation Rolan, P. Lim, Stephen Sunderland, Bruce Liu, Yandi Molnar, V. ketamine sublingual bioavailability pharmacokinetics AIM: The principal study objective was to investigate the pharmacokinetic characteristics of a new sublingual ketamine wafer and to establish its absolute bioavailability and local tolerability. METHODS: The study was of open label, two way randomized crossover design in eight healthy male volunteers. Each participant received either a single 10 mg intravenous dose as a constant rate 30 min infusion or a 25 mg sublingual dose of ketamine wafer in two treatment periods with a 7 day wash out. Pharmacokinetic blood sampling and local tolerability and safety assessments were carried out during 24 h following both dosing occasions. Plasma concentrations were analyzed by non-compartmental methods and local tolerability was assessed using modified Likert scales. RESULTS: The median (90% CI lower, upper limit) absolute bioavailability of sublingual ketamine was 29% (27, 31%). The first quantifiable plasma ketamine concentration was observed within 5 min for all eight participants for both routes of administration and the median (min–max) time of the peak plasma concentration was 0.75 h (0.25–1.0 h) after sublingual administration. The ketamine wafer had very good local tolerability. CONCLUSION: Sublingual administration of the ketamine wafer resulted in rapid absorption. The ketamine wafer has comparable bioavailability with other oral transmucosal formulations of ketamine but with markedly reduced inter-subject variability, warranting further evaluation as analgesic adjunct. 2014 Journal Article http://hdl.handle.net/20.500.11937/25299 10.1111/bcp.12264 Blackwell Publishing unknown |
| spellingShingle | ketamine sublingual bioavailability pharmacokinetics Rolan, P. Lim, Stephen Sunderland, Bruce Liu, Yandi Molnar, V. The absolute bioavailability of racemic ketamine from a novel sublingual formulation |
| title | The absolute bioavailability of racemic ketamine from a novel sublingual formulation |
| title_full | The absolute bioavailability of racemic ketamine from a novel sublingual formulation |
| title_fullStr | The absolute bioavailability of racemic ketamine from a novel sublingual formulation |
| title_full_unstemmed | The absolute bioavailability of racemic ketamine from a novel sublingual formulation |
| title_short | The absolute bioavailability of racemic ketamine from a novel sublingual formulation |
| title_sort | absolute bioavailability of racemic ketamine from a novel sublingual formulation |
| topic | ketamine sublingual bioavailability pharmacokinetics |
| url | http://hdl.handle.net/20.500.11937/25299 |