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Formulation Development and evaluation of fast disintegrating tablets of Lamotrigine using liqui-solid technique

INTRODUCTION: Epilepsy is a serious neurological disorder. Lamotrigine is an alternative to lithium for the treatment of epilepsy, and its oral bioavailability is 98%; however, its poor aqueous solubility hinders its oral absorption. Among the techniques available to enhance the solubility, dissolut...

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Autores principales: Koteswari, Poluri, Sunium, Suvarnala, Srinivasababu, Puttugunta, Babu, Govada Kishore, Nithya, Pinnamraju Durga
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/PMC4241626/
https://www.ncbi.nlm.nih.gov/pubmed/25426442
http://dx.doi.org/10.4103/2230-973X.143125
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author Koteswari, Poluri
Sunium, Suvarnala
Srinivasababu, Puttugunta
Babu, Govada Kishore
Nithya, Pinnamraju Durga
author_facet Koteswari, Poluri
Sunium, Suvarnala
Srinivasababu, Puttugunta
Babu, Govada Kishore
Nithya, Pinnamraju Durga
author_sort Koteswari, Poluri
collection PubMed
description INTRODUCTION: Epilepsy is a serious neurological disorder. Lamotrigine is an alternative to lithium for the treatment of epilepsy, and its oral bioavailability is 98%; however, its poor aqueous solubility hinders its oral absorption. Among the techniques available to enhance the solubility, dissolution rate and bio availability of poorly soluble drugs, liqui-solid technique is a novel and promising approach. The objectives of the investigation are to formulate, optimize lamotrigine liqui-solid compacts using 2(3) factorial experiments, validate experimental designs statistically and to compare with the marketed tablets using similarity and difference factors. MATERIALS AND METHODS: Based on solubility studies tween 20 as nonvolatile liquid, avicel pH 101 as a carrier and aerosil 200 as a coating material were used. Liquid load factor other flow and compression characteristics were determined for different ratios of carrier and coat materials. Suitable quantities of carrier and coat materials were taken, according to the experimental designs other excipients were added, liqui-solid tablets were prepared by direct compression and evaluated. Drug excipient compatibility was determined using Fourier transform infrared spectroscopy (FTIR) analysis. The hardness, disintegration time and T75% were considered for validation of experimental designs. RESULTS: The physicochemical properties of tablets such as hardness (1.5 ± 0.8–4.95 ± 0.96 kg), in vitro disintegration time (40 ± 20–320 ± 25 s) and Friability (0.39 ± 0.5–1.45 ± 0.2% also <1%) possess all the Indian pharmacopoeal requirements. The T75% was calculated and found to be 6.62–22.8 min. The rate of drug release followed first order kinetics. f(1) and f(2) values indicated the similarity in dissolution profiles between marketed and the optimized formulation and 63.64% similar with that of the marketed fast disintegrating tablets. FTIR studies revealed the absence of drug excipient incompatibility.
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spelling pubmed-42416262014-11-25 Formulation Development and evaluation of fast disintegrating tablets of Lamotrigine using liqui-solid technique Koteswari, Poluri Sunium, Suvarnala Srinivasababu, Puttugunta Babu, Govada Kishore Nithya, Pinnamraju Durga Int J Pharm Investig Original Research Article INTRODUCTION: Epilepsy is a serious neurological disorder. Lamotrigine is an alternative to lithium for the treatment of epilepsy, and its oral bioavailability is 98%; however, its poor aqueous solubility hinders its oral absorption. Among the techniques available to enhance the solubility, dissolution rate and bio availability of poorly soluble drugs, liqui-solid technique is a novel and promising approach. The objectives of the investigation are to formulate, optimize lamotrigine liqui-solid compacts using 2(3) factorial experiments, validate experimental designs statistically and to compare with the marketed tablets using similarity and difference factors. MATERIALS AND METHODS: Based on solubility studies tween 20 as nonvolatile liquid, avicel pH 101 as a carrier and aerosil 200 as a coating material were used. Liquid load factor other flow and compression characteristics were determined for different ratios of carrier and coat materials. Suitable quantities of carrier and coat materials were taken, according to the experimental designs other excipients were added, liqui-solid tablets were prepared by direct compression and evaluated. Drug excipient compatibility was determined using Fourier transform infrared spectroscopy (FTIR) analysis. The hardness, disintegration time and T75% were considered for validation of experimental designs. RESULTS: The physicochemical properties of tablets such as hardness (1.5 ± 0.8–4.95 ± 0.96 kg), in vitro disintegration time (40 ± 20–320 ± 25 s) and Friability (0.39 ± 0.5–1.45 ± 0.2% also <1%) possess all the Indian pharmacopoeal requirements. The T75% was calculated and found to be 6.62–22.8 min. The rate of drug release followed first order kinetics. f(1) and f(2) values indicated the similarity in dissolution profiles between marketed and the optimized formulation and 63.64% similar with that of the marketed fast disintegrating tablets. FTIR studies revealed the absence of drug excipient incompatibility. Medknow Publications & Media Pvt Ltd 2014 /pmc/articles/PMC4241626/ /pubmed/25426442 http://dx.doi.org/10.4103/2230-973X.143125 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
Koteswari, Poluri
Sunium, Suvarnala
Srinivasababu, Puttugunta
Babu, Govada Kishore
Nithya, Pinnamraju Durga
Formulation Development and evaluation of fast disintegrating tablets of Lamotrigine using liqui-solid technique
title Formulation Development and evaluation of fast disintegrating tablets of Lamotrigine using liqui-solid technique
title_full Formulation Development and evaluation of fast disintegrating tablets of Lamotrigine using liqui-solid technique
title_fullStr Formulation Development and evaluation of fast disintegrating tablets of Lamotrigine using liqui-solid technique
title_full_unstemmed Formulation Development and evaluation of fast disintegrating tablets of Lamotrigine using liqui-solid technique
title_short Formulation Development and evaluation of fast disintegrating tablets of Lamotrigine using liqui-solid technique
title_sort formulation development and evaluation of fast disintegrating tablets of lamotrigine using liqui-solid technique
topic Original Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4241626/
https://www.ncbi.nlm.nih.gov/pubmed/25426442
http://dx.doi.org/10.4103/2230-973X.143125
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