A single-dose, open-label, randomized, scintigraphic study to investigate the gastrointestinal behavior of 2 triple-combination cold products (acetaminophen, phenylephrine, and dextromethorphan) in healthy male volunteers
Abstract Background Common cold symptoms may be mitigated by products in caplet, nasal spray, and oral solution formulations, although variations exist in the bioavailability of the active ingredients contained within these products. Rapid gastric emptying (GE) of these active ingredients is importa...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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BMC
2022-02-01
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| Series: | Trials |
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| Online Access: | https://doi.org/10.1186/s13063-022-06037-x |
| _version_ | 1818977020842868736 |
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| author | Pascal Mallefet Marianna Armogida Walter J. Doll Richard C. Page Erik P. Sandefer |
| author_facet | Pascal Mallefet Marianna Armogida Walter J. Doll Richard C. Page Erik P. Sandefer |
| author_sort | Pascal Mallefet |
| collection | DOAJ |
| description | Abstract Background Common cold symptoms may be mitigated by products in caplet, nasal spray, and oral solution formulations, although variations exist in the bioavailability of the active ingredients contained within these products. Rapid gastric emptying (GE) of these active ingredients is important for reducing the delay between drug absorption and onset of cold symptom relief. Hot drink cold remedies are associated with greater comfort and may enhance the bioavailability of active ingredients. The objective of this study was to characterize the gastrointestinal transit of powder (reconstituted in hot water) and caplet formulations of commercially available multisymptom cold medications. Methods This was an open-label, single-dose, parallel-group study. Healthy male adults under fasted conditions were randomized 1:1 to receive a single dose of radiolabeled Theraflu Daytime Severe Cold and Cough powder for oral solution or radiolabeled Theraflu ExpressMax Daytime Severe Cold and Cough caplet. External gamma scintigraphy was utilized to monitor GE and intestinal transit of two radiolabeled drug formulations. Results A total of 28 participants completed the study. The mean ± SE GE onset times were 1.1 ± 0.3 min and 8.5 ± 1.8 min for powder and caplet formulations, respectively. The mean ± SE GE completion times were 121 ± 13 min and 65 ± 13 min, respectively. Despite the similar mean times to GE25%, the powder had later mean GE50% (23 ± 3.0 vs 16 ± 3.2 min, respectively) and GE90% (85 ± 12 vs 36 ± 9 min, respectively) than caplets. Caplets had a shorter overall GE half-life, lower total gastric exposure, and faster transit time through the small intestine versus the powder formulation. No serious safety events were observed. Conclusion The results of this study in healthy male adults suggest that the Theraflu powder formulation had a more rapid GE onset but longer time to GE completion than the caplet formulation. Trial registration ClinicalTrials.gov NCT03415243 |
| first_indexed | 2024-12-20T16:21:06Z |
| format | Article |
| id | doaj.art-f92f71a112464a4c832f03e113e6e48c |
| institution | Directory Open Access Journal |
| issn | 1745-6215 |
| language | English |
| last_indexed | 2024-12-20T16:21:06Z |
| publishDate | 2022-02-01 |
| publisher | BMC |
| record_format | Article |
| series | Trials |
| spelling | doaj.art-f92f71a112464a4c832f03e113e6e48c2022-12-21T19:33:37ZengBMCTrials1745-62152022-02-0123111010.1186/s13063-022-06037-xA single-dose, open-label, randomized, scintigraphic study to investigate the gastrointestinal behavior of 2 triple-combination cold products (acetaminophen, phenylephrine, and dextromethorphan) in healthy male volunteersPascal Mallefet0Marianna Armogida1Walter J. Doll2Richard C. Page3Erik P. Sandefer4GSK Consumer HealthcareGSK Consumer HealthcareScintipharma, Inc.Scintipharma, Inc.Scintipharma, Inc.Abstract Background Common cold symptoms may be mitigated by products in caplet, nasal spray, and oral solution formulations, although variations exist in the bioavailability of the active ingredients contained within these products. Rapid gastric emptying (GE) of these active ingredients is important for reducing the delay between drug absorption and onset of cold symptom relief. Hot drink cold remedies are associated with greater comfort and may enhance the bioavailability of active ingredients. The objective of this study was to characterize the gastrointestinal transit of powder (reconstituted in hot water) and caplet formulations of commercially available multisymptom cold medications. Methods This was an open-label, single-dose, parallel-group study. Healthy male adults under fasted conditions were randomized 1:1 to receive a single dose of radiolabeled Theraflu Daytime Severe Cold and Cough powder for oral solution or radiolabeled Theraflu ExpressMax Daytime Severe Cold and Cough caplet. External gamma scintigraphy was utilized to monitor GE and intestinal transit of two radiolabeled drug formulations. Results A total of 28 participants completed the study. The mean ± SE GE onset times were 1.1 ± 0.3 min and 8.5 ± 1.8 min for powder and caplet formulations, respectively. The mean ± SE GE completion times were 121 ± 13 min and 65 ± 13 min, respectively. Despite the similar mean times to GE25%, the powder had later mean GE50% (23 ± 3.0 vs 16 ± 3.2 min, respectively) and GE90% (85 ± 12 vs 36 ± 9 min, respectively) than caplets. Caplets had a shorter overall GE half-life, lower total gastric exposure, and faster transit time through the small intestine versus the powder formulation. No serious safety events were observed. Conclusion The results of this study in healthy male adults suggest that the Theraflu powder formulation had a more rapid GE onset but longer time to GE completion than the caplet formulation. Trial registration ClinicalTrials.gov NCT03415243https://doi.org/10.1186/s13063-022-06037-xCommon coldGastric emptyingRadionuclide imagingPowdersBeveragesDuodenum |
| spellingShingle | Pascal Mallefet Marianna Armogida Walter J. Doll Richard C. Page Erik P. Sandefer A single-dose, open-label, randomized, scintigraphic study to investigate the gastrointestinal behavior of 2 triple-combination cold products (acetaminophen, phenylephrine, and dextromethorphan) in healthy male volunteers Trials Common cold Gastric emptying Radionuclide imaging Powders Beverages Duodenum |
| title | A single-dose, open-label, randomized, scintigraphic study to investigate the gastrointestinal behavior of 2 triple-combination cold products (acetaminophen, phenylephrine, and dextromethorphan) in healthy male volunteers |
| title_full | A single-dose, open-label, randomized, scintigraphic study to investigate the gastrointestinal behavior of 2 triple-combination cold products (acetaminophen, phenylephrine, and dextromethorphan) in healthy male volunteers |
| title_fullStr | A single-dose, open-label, randomized, scintigraphic study to investigate the gastrointestinal behavior of 2 triple-combination cold products (acetaminophen, phenylephrine, and dextromethorphan) in healthy male volunteers |
| title_full_unstemmed | A single-dose, open-label, randomized, scintigraphic study to investigate the gastrointestinal behavior of 2 triple-combination cold products (acetaminophen, phenylephrine, and dextromethorphan) in healthy male volunteers |
| title_short | A single-dose, open-label, randomized, scintigraphic study to investigate the gastrointestinal behavior of 2 triple-combination cold products (acetaminophen, phenylephrine, and dextromethorphan) in healthy male volunteers |
| title_sort | single dose open label randomized scintigraphic study to investigate the gastrointestinal behavior of 2 triple combination cold products acetaminophen phenylephrine and dextromethorphan in healthy male volunteers |
| topic | Common cold Gastric emptying Radionuclide imaging Powders Beverages Duodenum |
| url | https://doi.org/10.1186/s13063-022-06037-x |
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