Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl
Autor(a) principal: | |
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Data de Publicação: | 2020 |
Outros Autores: | , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Brazilian Journal of Pharmaceutical Sciences |
Texto Completo: | https://www.revistas.usp.br/bjps/article/view/181623 |
Resumo: | The objective of this study was to determine specific combination of pharmaceutical excipients that lead to formulation of efficient nebivolol hydrochloride SMEDDS and its subsequent formulation into IR-SET (Immediate release- Self emulsifying tablet) which will enhance its solubility and dissolution. Solubility and Pseudo-ternary phase studies were carried out to identify the excipients showing highest solubility and to identify the zone of microemulsion with selected ingredients. Liquid-SMEDDS (L‑SMEDDS) were optimized for Concentration of oil(X1) and Smix(X2) and formulated using a combination of Kollisolv GTA as oil, Tween 80 as surfactant and propylene glycol as co-surfactant which gave smaller droplet size(Y1) 55.98nm , Emulsification time (Y2) 16±1.5 s,% transmittance (Y3) 99.94±0.47%. Neusilin US2 was used as solid carrier for solidification of L-SMEDDS in to Solid-SMEDDS (S-SMEDDS) by adsorption technique. IR-SET of nebivolol were formulated with S-SMEDDS and optimized for the concentration of binder (X1) (PVP K30) and superdisintegrant (X2) (KOLLIDON CL) which showed low Disintegration time (Y1) (92±0.5s) and low Friability(Y2)(0.424±0.03%). Also the DSC and XRD data revealed the molecular state of the drug in S-SMEDDS. The extent of in-vivo drug release and ex-vivo diffusion values from L-SMEDDS and IR-SET was much higher than pure drug and marketed tablet. In conclusion, the results showed potential of SMEDDS to improve solubility and thus the bioavailability. |
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oai:revistas.usp.br:article/181623 |
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USP-31 |
network_name_str |
Brazilian Journal of Pharmaceutical Sciences |
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Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HClNebivolol hydrochlorideLiquid & Solid SMEDDSFull factorial designNeusilin US2 IR-SETThe objective of this study was to determine specific combination of pharmaceutical excipients that lead to formulation of efficient nebivolol hydrochloride SMEDDS and its subsequent formulation into IR-SET (Immediate release- Self emulsifying tablet) which will enhance its solubility and dissolution. Solubility and Pseudo-ternary phase studies were carried out to identify the excipients showing highest solubility and to identify the zone of microemulsion with selected ingredients. Liquid-SMEDDS (L‑SMEDDS) were optimized for Concentration of oil(X1) and Smix(X2) and formulated using a combination of Kollisolv GTA as oil, Tween 80 as surfactant and propylene glycol as co-surfactant which gave smaller droplet size(Y1) 55.98nm , Emulsification time (Y2) 16±1.5 s,% transmittance (Y3) 99.94±0.47%. Neusilin US2 was used as solid carrier for solidification of L-SMEDDS in to Solid-SMEDDS (S-SMEDDS) by adsorption technique. IR-SET of nebivolol were formulated with S-SMEDDS and optimized for the concentration of binder (X1) (PVP K30) and superdisintegrant (X2) (KOLLIDON CL) which showed low Disintegration time (Y1) (92±0.5s) and low Friability(Y2)(0.424±0.03%). Also the DSC and XRD data revealed the molecular state of the drug in S-SMEDDS. The extent of in-vivo drug release and ex-vivo diffusion values from L-SMEDDS and IR-SET was much higher than pure drug and marketed tablet. In conclusion, the results showed potential of SMEDDS to improve solubility and thus the bioavailability.Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2020-12-09info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/18162310.1590/s2175-97902019000418070Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18070Brazilian Journal of Pharmaceutical Sciences; v. 56 (2020); e18070Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e180702175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/181623/168583Copyright (c) 2020 Brazilian Journal of Pharmaceutical Scienceshttp://creativecommons.org/licenses/by/4.0info:eu-repo/semantics/openAccessTrivedi, Hemangi Ramesh Siriah, Tanvi Mukund Puranik, Prashant Keshao 2021-06-12T19:46:54Zoai:revistas.usp.br:article/181623Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2021-06-12T19:46:54Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false |
dc.title.none.fl_str_mv |
Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
title |
Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
spellingShingle |
Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl Trivedi, Hemangi Ramesh Nebivolol hydrochloride Liquid & Solid SMEDDS Full factorial design Neusilin US2 IR-SET |
title_short |
Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
title_full |
Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
title_fullStr |
Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
title_full_unstemmed |
Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
title_sort |
Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
author |
Trivedi, Hemangi Ramesh |
author_facet |
Trivedi, Hemangi Ramesh Siriah, Tanvi Mukund Puranik, Prashant Keshao |
author_role |
author |
author2 |
Siriah, Tanvi Mukund Puranik, Prashant Keshao |
author2_role |
author author |
dc.contributor.author.fl_str_mv |
Trivedi, Hemangi Ramesh Siriah, Tanvi Mukund Puranik, Prashant Keshao |
dc.subject.por.fl_str_mv |
Nebivolol hydrochloride Liquid & Solid SMEDDS Full factorial design Neusilin US2 IR-SET |
topic |
Nebivolol hydrochloride Liquid & Solid SMEDDS Full factorial design Neusilin US2 IR-SET |
description |
The objective of this study was to determine specific combination of pharmaceutical excipients that lead to formulation of efficient nebivolol hydrochloride SMEDDS and its subsequent formulation into IR-SET (Immediate release- Self emulsifying tablet) which will enhance its solubility and dissolution. Solubility and Pseudo-ternary phase studies were carried out to identify the excipients showing highest solubility and to identify the zone of microemulsion with selected ingredients. Liquid-SMEDDS (L‑SMEDDS) were optimized for Concentration of oil(X1) and Smix(X2) and formulated using a combination of Kollisolv GTA as oil, Tween 80 as surfactant and propylene glycol as co-surfactant which gave smaller droplet size(Y1) 55.98nm , Emulsification time (Y2) 16±1.5 s,% transmittance (Y3) 99.94±0.47%. Neusilin US2 was used as solid carrier for solidification of L-SMEDDS in to Solid-SMEDDS (S-SMEDDS) by adsorption technique. IR-SET of nebivolol were formulated with S-SMEDDS and optimized for the concentration of binder (X1) (PVP K30) and superdisintegrant (X2) (KOLLIDON CL) which showed low Disintegration time (Y1) (92±0.5s) and low Friability(Y2)(0.424±0.03%). Also the DSC and XRD data revealed the molecular state of the drug in S-SMEDDS. The extent of in-vivo drug release and ex-vivo diffusion values from L-SMEDDS and IR-SET was much higher than pure drug and marketed tablet. In conclusion, the results showed potential of SMEDDS to improve solubility and thus the bioavailability. |
publishDate |
2020 |
dc.date.none.fl_str_mv |
2020-12-09 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/181623 10.1590/s2175-97902019000418070 |
url |
https://www.revistas.usp.br/bjps/article/view/181623 |
identifier_str_mv |
10.1590/s2175-97902019000418070 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/181623/168583 |
dc.rights.driver.fl_str_mv |
Copyright (c) 2020 Brazilian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/4.0 info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Copyright (c) 2020 Brazilian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/4.0 |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
dc.source.none.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18070 Brazilian Journal of Pharmaceutical Sciences; v. 56 (2020); e18070 Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18070 2175-9790 1984-8250 reponame:Brazilian Journal of Pharmaceutical Sciences instname:Universidade de São Paulo (USP) instacron:USP |
instname_str |
Universidade de São Paulo (USP) |
instacron_str |
USP |
institution |
USP |
reponame_str |
Brazilian Journal of Pharmaceutical Sciences |
collection |
Brazilian Journal of Pharmaceutical Sciences |
repository.name.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP) |
repository.mail.fl_str_mv |
bjps@usp.br||elizabeth.igne@gmail.com |
_version_ |
1800222915109584896 |