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
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 fas...
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| Format: | Article |
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BMC
2023-09-01
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| Series: | BMC Biotechnology |
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| Online Access: | https://doi.org/10.1186/s12896-023-00809-2 |
| _version_ | 1797452177066688512 |
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| author | Ramzi Shawahna Hala Saba’aneh Amal Daraghmeh Yara Qassarwi Valentina Franco Xavier Declèves |
| author_facet | Ramzi Shawahna Hala Saba’aneh Amal Daraghmeh Yara Qassarwi Valentina Franco Xavier Declèves |
| author_sort | Ramzi Shawahna |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-09T15:04:03Z |
| format | Article |
| id | doaj.art-7ec863eb36074ac6bf6cd4010ceb8bba |
| institution | Directory Open Access Journal |
| issn | 1472-6750 |
| language | English |
| last_indexed | 2024-03-09T15:04:03Z |
| publishDate | 2023-09-01 |
| publisher | BMC |
| record_format | Article |
| series | BMC Biotechnology |
| spelling | doaj.art-7ec863eb36074ac6bf6cd4010ceb8bba2023-11-26T13:43:59ZengBMCBMC Biotechnology1472-67502023-09-0123111210.1186/s12896-023-00809-2Solubility 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 formulationsRamzi Shawahna0Hala Saba’aneh1Amal Daraghmeh2Yara Qassarwi3Valentina Franco4Xavier Declèves5Department of Physiology, Pharmacology and Toxicology, Faculty of Medicine and Health Sciences, An-Najah National UniversityDepartment of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National UniversityDepartment of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National UniversityDepartment of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National UniversitySection of Translational Neurovascular Research, IRCCS Mondino FoundationBiologie du Médicament-Toxicologie, AP-HP, Hôpital CochinAbstract 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.https://doi.org/10.1186/s12896-023-00809-2LamotriginePediatricSolubilityDosage form performanceBiopharmaceuticsBiorelevant |
| spellingShingle | Ramzi Shawahna Hala Saba’aneh Amal Daraghmeh Yara Qassarwi Valentina Franco Xavier Declèves 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 BMC Biotechnology Lamotrigine Pediatric Solubility Dosage form performance Biopharmaceutics Biorelevant |
| title | 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 |
| title_full | 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 |
| title_fullStr | 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 |
| title_full_unstemmed | 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 |
| title_short | 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 |
| title_sort | 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 |
| topic | Lamotrigine Pediatric Solubility Dosage form performance Biopharmaceutics Biorelevant |
| url | https://doi.org/10.1186/s12896-023-00809-2 |
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