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Formulation and evaluation of sublingual tablets containing Sumatriptan succinate
OBJECTIVE: Sumatriptan succinate is a selective 5-hydroxytryptamine-1 receptor agonist effective in the acute treatment of migraine headaches, having low bioavailability of about 15% orally due to first-pass metabolism. The purpose of this research was to mask the intensely bitter taste of Sumatript...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Medknow Publications & Media Pvt Ltd
2012
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3555012/ https://www.ncbi.nlm.nih.gov/pubmed/23373008 http://dx.doi.org/10.4103/2230-973X.104400 |
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author | Prajapati, Shailesh T Patel, Parth B Patel, Chhagan N |
author_facet | Prajapati, Shailesh T Patel, Parth B Patel, Chhagan N |
author_sort | Prajapati, Shailesh T |
collection | PubMed |
description | OBJECTIVE: Sumatriptan succinate is a selective 5-hydroxytryptamine-1 receptor agonist effective in the acute treatment of migraine headaches, having low bioavailability of about 15% orally due to first-pass metabolism. The purpose of this research was to mask the intensely bitter taste of Sumatriptan succinate and to formulate fast-acting, taste-masked sublingual tablet formulation. MATERIALS AND METHODS: Taste masking was performed by solid dispersion method with mannitol and ion exchange with Kyron T 114 because it releases the drug in salivary pH. The resultant batches were evaluated for in-vivo taste masking as well compatability study (Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC)). For a better feel in the mouth, menthol and sweetener Na saccharine were added to the tablet formulation. The tablets were prepared by direct compression and evaluated for weight variation, thickness, friability, drug content, hardness, disintegration time, wetting time, in vitro drug release, and in vitro permeation study. RESULTS AND DISCUSSION: Optimized batches disintegrated in vitro within 28-34 s. Maximum drug release could be achieved with in 10 min for the solid dispersion batches and 14-15 min for the ion-exchange batches with Kyron T 114. The optimized tablet formulation showed better taste and the formulated sublingual tablets may act as a potential alternate for the Sumatriptan succinate oral tablet. CONCLUSION: Sumatriptan succinate can be successfully taste-masked by both the solid dispersion method using mannitol by the melting method and Ion exchange resin with Kyron T114. It was also concluded that prepared formulation improve bioavailability by prevention of first pass metabolism. |
format | Online Article Text |
id | pubmed-3555012 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2012 |
publisher | Medknow Publications & Media Pvt Ltd |
record_format | MEDLINE/PubMed |
spelling | pubmed-35550122013-01-31 Formulation and evaluation of sublingual tablets containing Sumatriptan succinate Prajapati, Shailesh T Patel, Parth B Patel, Chhagan N Int J Pharm Investig Original Research Article OBJECTIVE: Sumatriptan succinate is a selective 5-hydroxytryptamine-1 receptor agonist effective in the acute treatment of migraine headaches, having low bioavailability of about 15% orally due to first-pass metabolism. The purpose of this research was to mask the intensely bitter taste of Sumatriptan succinate and to formulate fast-acting, taste-masked sublingual tablet formulation. MATERIALS AND METHODS: Taste masking was performed by solid dispersion method with mannitol and ion exchange with Kyron T 114 because it releases the drug in salivary pH. The resultant batches were evaluated for in-vivo taste masking as well compatability study (Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC)). For a better feel in the mouth, menthol and sweetener Na saccharine were added to the tablet formulation. The tablets were prepared by direct compression and evaluated for weight variation, thickness, friability, drug content, hardness, disintegration time, wetting time, in vitro drug release, and in vitro permeation study. RESULTS AND DISCUSSION: Optimized batches disintegrated in vitro within 28-34 s. Maximum drug release could be achieved with in 10 min for the solid dispersion batches and 14-15 min for the ion-exchange batches with Kyron T 114. The optimized tablet formulation showed better taste and the formulated sublingual tablets may act as a potential alternate for the Sumatriptan succinate oral tablet. CONCLUSION: Sumatriptan succinate can be successfully taste-masked by both the solid dispersion method using mannitol by the melting method and Ion exchange resin with Kyron T114. It was also concluded that prepared formulation improve bioavailability by prevention of first pass metabolism. Medknow Publications & Media Pvt Ltd 2012 /pmc/articles/PMC3555012/ /pubmed/23373008 http://dx.doi.org/10.4103/2230-973X.104400 Text en Copyright: © International Journal of Pharmaceutical Investigation http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Original Research Article Prajapati, Shailesh T Patel, Parth B Patel, Chhagan N Formulation and evaluation of sublingual tablets containing Sumatriptan succinate |
title | Formulation and evaluation of sublingual tablets containing Sumatriptan succinate |
title_full | Formulation and evaluation of sublingual tablets containing Sumatriptan succinate |
title_fullStr | Formulation and evaluation of sublingual tablets containing Sumatriptan succinate |
title_full_unstemmed | Formulation and evaluation of sublingual tablets containing Sumatriptan succinate |
title_short | Formulation and evaluation of sublingual tablets containing Sumatriptan succinate |
title_sort | formulation and evaluation of sublingual tablets containing sumatriptan succinate |
topic | Original Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3555012/ https://www.ncbi.nlm.nih.gov/pubmed/23373008 http://dx.doi.org/10.4103/2230-973X.104400 |
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