An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device
Autor(a) principal: | |
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Data de Publicação: | 2022 |
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/203357 |
Resumo: | Chemotherapy induced nausea and vomiting (CINV) is an issue, which usually occurs in cancer patient. Despite high bioavailability of oral and intravenous administration, these have some drawbacks. The oral route causes hepatic first pass metabolism and intravenous route is invasive in nature. Hence, antiemetic drug by means of transdermal route is necessary to administer in such cases. The aim of the present investigation is to develop suitable Transdermal Therapeutic System (TTS) with an objective to enhance solubility and skin permeability properties of metoclopramide base. Preformulation study begins with an approach to enhance solubility of 40 metoclopramide base by solid dispersion technique. transdermal films were prepared with 41 the solid dispersion as well as with pure drug. Phase solubility study at various temperatures reveals binding constants (Ka, 95-350 M-1 for PVP K30; 56-81 M-1 for HPβCD). Spontaneity of solubilization was justified by AL type linear profiles. The films showed satisfactory diffusion (%), permeation rate and flux after 8 h study. The transdermal patches as prepared were analyzed under FTIR, DSC and SEM. Both solubility and permeability rate in this investigation have been enhanced. So, it can be affirmed that this route would effectively enhance bioavailability. |
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Brazilian Journal of Pharmaceutical Sciences |
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An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal deviceSolid dispersion. Solubility. Metoclopramide base. Transdermal device. Permeation. Bioavailability.Chemotherapy induced nausea and vomiting (CINV) is an issue, which usually occurs in cancer patient. Despite high bioavailability of oral and intravenous administration, these have some drawbacks. The oral route causes hepatic first pass metabolism and intravenous route is invasive in nature. Hence, antiemetic drug by means of transdermal route is necessary to administer in such cases. The aim of the present investigation is to develop suitable Transdermal Therapeutic System (TTS) with an objective to enhance solubility and skin permeability properties of metoclopramide base. Preformulation study begins with an approach to enhance solubility of 40 metoclopramide base by solid dispersion technique. transdermal films were prepared with 41 the solid dispersion as well as with pure drug. Phase solubility study at various temperatures reveals binding constants (Ka, 95-350 M-1 for PVP K30; 56-81 M-1 for HPβCD). Spontaneity of solubilization was justified by AL type linear profiles. The films showed satisfactory diffusion (%), permeation rate and flux after 8 h study. The transdermal patches as prepared were analyzed under FTIR, DSC and SEM. Both solubility and permeability rate in this investigation have been enhanced. So, it can be affirmed that this route would effectively enhance bioavailability.Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2022-11-09info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttps://www.revistas.usp.br/bjps/article/view/20335710.1590/s2175-97902020000418910Brazilian Journal of Pharmaceutical Sciences; Vol. 57 (2021)Brazilian Journal of Pharmaceutical Sciences; v. 57 (2021)Brazilian Journal of Pharmaceutical Sciences; Vol. 57 (2021)2175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/203357/187336Copyright (c) 2022 Brazilian Journal of Pharmaceutical Scienceshttps://creativecommons.org/licenses/by/4.0info:eu-repo/semantics/openAccessKahali, NancyKhanam, JasminaGhosh, Nondita2022-11-09T18:34:12Zoai:revistas.usp.br:article/203357Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2022-11-09T18:34:12Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false |
dc.title.none.fl_str_mv |
An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device |
title |
An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device |
spellingShingle |
An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device Kahali, Nancy Solid dispersion. Solubility. Metoclopramide base. Transdermal device. Permeation. Bioavailability. |
title_short |
An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device |
title_full |
An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device |
title_fullStr |
An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device |
title_full_unstemmed |
An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device |
title_sort |
An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device |
author |
Kahali, Nancy |
author_facet |
Kahali, Nancy Khanam, Jasmina Ghosh, Nondita |
author_role |
author |
author2 |
Khanam, Jasmina Ghosh, Nondita |
author2_role |
author author |
dc.contributor.author.fl_str_mv |
Kahali, Nancy Khanam, Jasmina Ghosh, Nondita |
dc.subject.por.fl_str_mv |
Solid dispersion. Solubility. Metoclopramide base. Transdermal device. Permeation. Bioavailability. |
topic |
Solid dispersion. Solubility. Metoclopramide base. Transdermal device. Permeation. Bioavailability. |
description |
Chemotherapy induced nausea and vomiting (CINV) is an issue, which usually occurs in cancer patient. Despite high bioavailability of oral and intravenous administration, these have some drawbacks. The oral route causes hepatic first pass metabolism and intravenous route is invasive in nature. Hence, antiemetic drug by means of transdermal route is necessary to administer in such cases. The aim of the present investigation is to develop suitable Transdermal Therapeutic System (TTS) with an objective to enhance solubility and skin permeability properties of metoclopramide base. Preformulation study begins with an approach to enhance solubility of 40 metoclopramide base by solid dispersion technique. transdermal films were prepared with 41 the solid dispersion as well as with pure drug. Phase solubility study at various temperatures reveals binding constants (Ka, 95-350 M-1 for PVP K30; 56-81 M-1 for HPβCD). Spontaneity of solubilization was justified by AL type linear profiles. The films showed satisfactory diffusion (%), permeation rate and flux after 8 h study. The transdermal patches as prepared were analyzed under FTIR, DSC and SEM. Both solubility and permeability rate in this investigation have been enhanced. So, it can be affirmed that this route would effectively enhance bioavailability. |
publishDate |
2022 |
dc.date.none.fl_str_mv |
2022-11-09 |
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/203357 10.1590/s2175-97902020000418910 |
url |
https://www.revistas.usp.br/bjps/article/view/203357 |
identifier_str_mv |
10.1590/s2175-97902020000418910 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/203357/187336 |
dc.rights.driver.fl_str_mv |
Copyright (c) 2022 Brazilian Journal of Pharmaceutical Sciences https://creativecommons.org/licenses/by/4.0 info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Copyright (c) 2022 Brazilian Journal of Pharmaceutical Sciences https://creativecommons.org/licenses/by/4.0 |
eu_rights_str_mv |
openAccess |
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. 57 (2021) Brazilian Journal of Pharmaceutical Sciences; v. 57 (2021) Brazilian Journal of Pharmaceutical Sciences; Vol. 57 (2021) 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_ |
1800222915631775744 |