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Solubility of lamotrigine in age-specific biorelevant media that simulated the fasted- and fed-conditions of the gastric and intestinal environments in pediatrics and adults: implications for traditional, re-formulated, modified, and new oral formulations.
Shawahna, Ramzi; Saba'aneh, Hala; Daraghmeh, Amal; Qassarwi, Yara; Franco, Valentina; Declèves, Xavier.
Afiliação
  • Shawahna R; Department of Physiology, Pharmacology and Toxicology, Faculty of Medicine and Health Sciences, An-Najah National University, New Campus, Building: 19, Office: 1340, P.O. Box 7, Nablus, Palestine. ramzi_shawahna@hotmail.com.
  • Saba'aneh H; Clinical Research Center, An-Najah National University Hospital, Nablus, 44839, Palestine. ramzi_shawahna@hotmail.com.
  • Daraghmeh A; Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine.
  • Qassarwi Y; Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine.
  • Franco V; Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine.
  • Declèves X; Section of Translational Neurovascular Research, IRCCS Mondino Foundation, Via Mondino 2, Pavia, 27100, Italy.
BMC Biotechnol ; 23(1): 36, 2023 09 08.
Article em En | MEDLINE | ID: mdl-37684623
ABSTRACT

BACKGROUND:

Lamotrigine is an effective antiseizure medication that can be used in the management of focal and generalized epilepsies in pediatric patients. This study was conducted to quantify and compare the solubility of lamotrigine in age-specific biorelevant media that simulated the fasted and fed conditions of the gastric and intestinal environments in pediatrics and adults. Another aim was to predict how traditional, re-formulated, modified, and new oral formulations would behave in the gastric and intestinal environments across different age groups.

METHODS:

Solubility studies of lamotrigine were conducted in 16 different age-specific biorelevant media over the pH range and temperature specified by the current biopharmaceutical classification system-based criteria. The age-specific biorelevant media simulated the environments in the stomach and proximal gastrointestinal tract in both fasted and fed conditions of adults and pediatric sub-populations. The solubility of lamotrigine was determined using a pre-validated HPLC-UV method.

RESULTS:

Lamotrigine showed low solubility in the 16 age-specific biorelevant media as indicated by a dose number of > 1. There were significant age-specific variabilities in the solubility of lamotrigine in the different age-specific biorelevant media. Pediatric/adult solubility ratios of lamotrigine fell outside the 80-125% range in 6 (50.0%) and were borderline in 3 (25.0%) out of the 12 compared media. These ratios indicated that the solubility of lamotrigine showed considerable differences in 9 out of the 12 (75.0%) of the compared media.

CONCLUSION:

Future studies are still needed to generate more pediatric biopharmaceutical data to help understand the performances of oral dosage forms in pediatric sub-populations.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Estômago / Produtos Biológicos Tipo de estudo: Prognostic_studies Limite: Adult / Child / Humans Idioma: En Revista: BMC Biotechnol Ano de publicação: 2023 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Estômago / Produtos Biológicos Tipo de estudo: Prognostic_studies Limite: Adult / Child / Humans Idioma: En Revista: BMC Biotechnol Ano de publicação: 2023 Tipo de documento: Article