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Preparation and evaluation of sublingual tablets of zolmitriptan

AIM: Zolmitriptan is a 5-HT receptor agonist (1B/1D). It is used in the acute treatment of migraine having low bioavailability about 40% orally due to hepatic first pass metabolism. The purpose of the present research was to formulate fast acting sublingual tablets of zolmitriptan. MATERIALS AND MET...

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Autores principales: Prajapati, Shailesh T, Patel, Manoj V, Patel, Chhaganbhai N
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3944614/
https://www.ncbi.nlm.nih.gov/pubmed/24678459
http://dx.doi.org/10.4103/2230-973X.127737
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author Prajapati, Shailesh T
Patel, Manoj V
Patel, Chhaganbhai N
author_facet Prajapati, Shailesh T
Patel, Manoj V
Patel, Chhaganbhai N
author_sort Prajapati, Shailesh T
collection PubMed
description AIM: Zolmitriptan is a 5-HT receptor agonist (1B/1D). It is used in the acute treatment of migraine having low bioavailability about 40% orally due to hepatic first pass metabolism. The purpose of the present research was to formulate fast acting sublingual tablets of zolmitriptan. MATERIALS AND METHODS: Sublingual tablets were prepared using ispaghula husk powder, gellan gum, sodium alginate as super disintegrating polymers and citric acid, tartaric acid and camphor as permeation enhancers by direct compressible technique and evaluated for weight variation, thickness, friability, content uniformity, hardness, disintegration time, wetting time, in-vitro drug release, in-vitro and ex-vivo permeation study. Stability study of optimized formulation was performed as per ICH (International Conference on Harmonisation) guideline. RESULTS: The in-vitro disintegration time of the optimized formulation (D5) was 9 ± 2 s and all formulations showed 100% of dissolution within 6 ± 2 min. Formulation containing 4% of gellan gum (D5) showed highest disintegration and 2% of citric acid formulation (P3) showed highest permeation 88% within 30 min and ex-vivo permeation was 52% within 30 min. Optimized formulation was stable for 1 month during stability study as per ICH guideline. CONCLUSION: The sublingual tablet formulation gives better results using natural super disintegrant for fast onset of action.
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spelling pubmed-39446142014-03-27 Preparation and evaluation of sublingual tablets of zolmitriptan Prajapati, Shailesh T Patel, Manoj V Patel, Chhaganbhai N Int J Pharm Investig Original Research Article AIM: Zolmitriptan is a 5-HT receptor agonist (1B/1D). It is used in the acute treatment of migraine having low bioavailability about 40% orally due to hepatic first pass metabolism. The purpose of the present research was to formulate fast acting sublingual tablets of zolmitriptan. MATERIALS AND METHODS: Sublingual tablets were prepared using ispaghula husk powder, gellan gum, sodium alginate as super disintegrating polymers and citric acid, tartaric acid and camphor as permeation enhancers by direct compressible technique and evaluated for weight variation, thickness, friability, content uniformity, hardness, disintegration time, wetting time, in-vitro drug release, in-vitro and ex-vivo permeation study. Stability study of optimized formulation was performed as per ICH (International Conference on Harmonisation) guideline. RESULTS: The in-vitro disintegration time of the optimized formulation (D5) was 9 ± 2 s and all formulations showed 100% of dissolution within 6 ± 2 min. Formulation containing 4% of gellan gum (D5) showed highest disintegration and 2% of citric acid formulation (P3) showed highest permeation 88% within 30 min and ex-vivo permeation was 52% within 30 min. Optimized formulation was stable for 1 month during stability study as per ICH guideline. CONCLUSION: The sublingual tablet formulation gives better results using natural super disintegrant for fast onset of action. Medknow Publications & Media Pvt Ltd 2014 /pmc/articles/PMC3944614/ /pubmed/24678459 http://dx.doi.org/10.4103/2230-973X.127737 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, Manoj V
Patel, Chhaganbhai N
Preparation and evaluation of sublingual tablets of zolmitriptan
title Preparation and evaluation of sublingual tablets of zolmitriptan
title_full Preparation and evaluation of sublingual tablets of zolmitriptan
title_fullStr Preparation and evaluation of sublingual tablets of zolmitriptan
title_full_unstemmed Preparation and evaluation of sublingual tablets of zolmitriptan
title_short Preparation and evaluation of sublingual tablets of zolmitriptan
title_sort preparation and evaluation of sublingual tablets of zolmitriptan
topic Original Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3944614/
https://www.ncbi.nlm.nih.gov/pubmed/24678459
http://dx.doi.org/10.4103/2230-973X.127737
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