Bioavailability and swallowability of an age-appropriate, delayed-release mesalamine formulation in healthy volunteers

Abhijeet Jakate,1 Brian McNamee,2 Donald Burkindine31Clinical Pharmacology, Allergan plc, Madison, NJ, USA; 2Clinical Pharmacology, Allergan Biologics Ltd, Liverpool, UK; 3QPS Bio-Kinetic, Springfield, MO, USAObjective: Delayed-release mesalamine 400 mg capsules containing four 100 mg tablets have b...

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Autores principales:	Jakate A, McNamee B, Burkindine D
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Delzicol Asacol mesalamine inflammatory bowel disease ulcerative colitis Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/02aecee68087414c8e7a96c3eed0a793
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spelling	oai:doaj.org-article:02aecee68087414c8e7a96c3eed0a7932021-12-02T02:25:29ZBioavailability and swallowability of an age-appropriate, delayed-release mesalamine formulation in healthy volunteers1179-1438https://doaj.org/article/02aecee68087414c8e7a96c3eed0a7932019-07-01T00:00:00Zhttps://www.dovepress.com/bioavailability-and-swallowability-of-an-age-appropriate-delayed-relea-peer-reviewed-article-CPAAhttps://doaj.org/toc/1179-1438Abhijeet Jakate,1 Brian McNamee,2 Donald Burkindine31Clinical Pharmacology, Allergan plc, Madison, NJ, USA; 2Clinical Pharmacology, Allergan Biologics Ltd, Liverpool, UK; 3QPS Bio-Kinetic, Springfield, MO, USAObjective: Delayed-release mesalamine 400 mg capsules containing four 100 mg tablets have been developed for children with ulcerative colitis who have difficulty swallowing. Bioavailability of the mesalamine capsules was compared with existing mesalamine tablets in healthy adults, and the effect of food on bioavailability from mesalamine capsules was determined. Tablet swallowability in healthy children was evaluated.Methods: In the open-label, replicate-treatment, single-dose, crossover, comparative bioavailability study, healthy adult volunteers were randomized to one of four treatment sequences to receive mesalamine 400 mg tablets (fasted) twice, mesalamine 400 mg capsules (fasted) twice, and a mesalamine 400 mg capsule (with food) once, with ≥7 days between treatments. Pharmacokinetic (PK) parameters were calculated and analyzed using the reference-scaled average bioequivalence procedure. In the open-label, single-dose swallowability study, healthy children aged 5–11 years were asked to swallow eight placebo tablets identical to those contained in two mesalamine capsules.Results: In the bioavailability study (n=160), mesalamine capsules and tablets in fasted volunteers exhibited similarly delayed absorption and were shown to be bioequivalent; statistical parameters calculated from PK values met the criteria for bioequivalence. A slight increase in mesalamine bioavailability was observed with food administration, but the delayed-release performance of the capsules was not affected. Overall safety profiles between capsules and tablets were similar. In the swallowability study (n=60), the majority of children swallowed eight placebo tablets, with slight variability between age groups.Conclusion: Evaluation of PK parameters confirmed mesalamine capsules are bioequivalent to mesalamine tablets. Mesalamine capsules were well tolerated, can be administered with or without food, and are an age-appropriate product for children.Keywords: Delzicol, Asacol, mesalamine, inflammatory bowel disease, ulcerative colitisJakate AMcNamee BBurkindine DDove Medical PressarticleDelzicolAsacolmesalamineinflammatory bowel diseaseulcerative colitisTherapeutics. PharmacologyRM1-950ENClinical Pharmacology: Advances and Applications, Vol Volume 11, Pp 93-101 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Delzicol Asacol mesalamine inflammatory bowel disease ulcerative colitis Therapeutics. Pharmacology RM1-950
spellingShingle	Delzicol Asacol mesalamine inflammatory bowel disease ulcerative colitis Therapeutics. Pharmacology RM1-950 Jakate A McNamee B Burkindine D Bioavailability and swallowability of an age-appropriate, delayed-release mesalamine formulation in healthy volunteers
description	Abhijeet Jakate,1 Brian McNamee,2 Donald Burkindine31Clinical Pharmacology, Allergan plc, Madison, NJ, USA; 2Clinical Pharmacology, Allergan Biologics Ltd, Liverpool, UK; 3QPS Bio-Kinetic, Springfield, MO, USAObjective: Delayed-release mesalamine 400 mg capsules containing four 100 mg tablets have been developed for children with ulcerative colitis who have difficulty swallowing. Bioavailability of the mesalamine capsules was compared with existing mesalamine tablets in healthy adults, and the effect of food on bioavailability from mesalamine capsules was determined. Tablet swallowability in healthy children was evaluated.Methods: In the open-label, replicate-treatment, single-dose, crossover, comparative bioavailability study, healthy adult volunteers were randomized to one of four treatment sequences to receive mesalamine 400 mg tablets (fasted) twice, mesalamine 400 mg capsules (fasted) twice, and a mesalamine 400 mg capsule (with food) once, with ≥7 days between treatments. Pharmacokinetic (PK) parameters were calculated and analyzed using the reference-scaled average bioequivalence procedure. In the open-label, single-dose swallowability study, healthy children aged 5–11 years were asked to swallow eight placebo tablets identical to those contained in two mesalamine capsules.Results: In the bioavailability study (n=160), mesalamine capsules and tablets in fasted volunteers exhibited similarly delayed absorption and were shown to be bioequivalent; statistical parameters calculated from PK values met the criteria for bioequivalence. A slight increase in mesalamine bioavailability was observed with food administration, but the delayed-release performance of the capsules was not affected. Overall safety profiles between capsules and tablets were similar. In the swallowability study (n=60), the majority of children swallowed eight placebo tablets, with slight variability between age groups.Conclusion: Evaluation of PK parameters confirmed mesalamine capsules are bioequivalent to mesalamine tablets. Mesalamine capsules were well tolerated, can be administered with or without food, and are an age-appropriate product for children.Keywords: Delzicol, Asacol, mesalamine, inflammatory bowel disease, ulcerative colitis
format	article
author	Jakate A McNamee B Burkindine D
author_facet	Jakate A McNamee B Burkindine D
author_sort	Jakate A
title	Bioavailability and swallowability of an age-appropriate, delayed-release mesalamine formulation in healthy volunteers
title_short	Bioavailability and swallowability of an age-appropriate, delayed-release mesalamine formulation in healthy volunteers
title_full	Bioavailability and swallowability of an age-appropriate, delayed-release mesalamine formulation in healthy volunteers
title_fullStr	Bioavailability and swallowability of an age-appropriate, delayed-release mesalamine formulation in healthy volunteers
title_full_unstemmed	Bioavailability and swallowability of an age-appropriate, delayed-release mesalamine formulation in healthy volunteers
title_sort	bioavailability and swallowability of an age-appropriate, delayed-release mesalamine formulation in healthy volunteers
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/02aecee68087414c8e7a96c3eed0a793
work_keys_str_mv	AT jakatea bioavailabilityandswallowabilityofanageappropriatedelayedreleasemesalamineformulationinhealthyvolunteers AT mcnameeb bioavailabilityandswallowabilityofanageappropriatedelayedreleasemesalamineformulationinhealthyvolunteers AT burkindined bioavailabilityandswallowabilityofanageappropriatedelayedreleasemesalamineformulationinhealthyvolunteers
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Bioavailability and swallowability of an age-appropriate, delayed-release mesalamine formulation in healthy volunteers

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