Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel
Autor(a) principal: | |
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Data de Publicação: | 2010 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1590/s1984-82502010000300010 http://hdl.handle.net/11449/231973 |
Resumo: | The solubility behavior of drugs remains one of the most challenging aspects in formulation development. Solid Dispersion (SD) has tremendous potential for improving drug solubility. Although praziquantel (PZQ) is the first drug of choice in the treatment of schistosomiasis, its poor solubility has restricted its delivery oral route. In spite of its poor solubility, PZQ is well absorbed in the gastrointestinal tract, but large doses are required to achieve adequate concentration at the target sites. The aim of this study was to improve the solubility and dissolution rate of PZQ and to evaluate its intestinal absorption. SDs were formulated with PEG-60 castor oil hydrogenated (CR-60) using a fusion and evaporation method. Pure PZQ and physical mixtures (PM) and PZQ-CR-60 (2:1; 1:1; 1:2 ratios) were compared as regards their solubility, dissolution and intestinal absorption. The experimental results demonstrated the improvement in the solubility, dissolution rate and intestinal absorption. In addition, the solubility behavior showed pH dependency and that the solubility of PZQ was slower in acidic medium than in neutral and basic mediums. The increase in PZQ solubility of the SD with the CR-60 could be attributed to several factors such as improved wettability, local solubilization, drug particle size reduction and crystalline or, interstitial solid solution reduction. |
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Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantelPraziquantel/dissolution ratesPraziquantel/intestinal absorptionPraziquantel/solubilitySolid dispersionThe solubility behavior of drugs remains one of the most challenging aspects in formulation development. Solid Dispersion (SD) has tremendous potential for improving drug solubility. Although praziquantel (PZQ) is the first drug of choice in the treatment of schistosomiasis, its poor solubility has restricted its delivery oral route. In spite of its poor solubility, PZQ is well absorbed in the gastrointestinal tract, but large doses are required to achieve adequate concentration at the target sites. The aim of this study was to improve the solubility and dissolution rate of PZQ and to evaluate its intestinal absorption. SDs were formulated with PEG-60 castor oil hydrogenated (CR-60) using a fusion and evaporation method. Pure PZQ and physical mixtures (PM) and PZQ-CR-60 (2:1; 1:1; 1:2 ratios) were compared as regards their solubility, dissolution and intestinal absorption. The experimental results demonstrated the improvement in the solubility, dissolution rate and intestinal absorption. In addition, the solubility behavior showed pH dependency and that the solubility of PZQ was slower in acidic medium than in neutral and basic mediums. The increase in PZQ solubility of the SD with the CR-60 could be attributed to several factors such as improved wettability, local solubilization, drug particle size reduction and crystalline or, interstitial solid solution reduction.Department of Pharmaceutical Sciences University of Sorocaba - UNISODepartment of Pharmacy Faculty of Health Sciences Methodist University of PiracicabaDepartment of Drugs and Pharmaceutical Faculty of Pharmaceutical Sciences of Araraquara São Paulo State University Júlio de Mesquita FilhoDepartment of Pharmaceutical Sciences of Ribeirão Preto University of São PauloDepartment of Drugs and Pharmaceutical Faculty of Pharmaceutical Sciences of Araraquara São Paulo State University Júlio de Mesquita FilhoUniversity of Sorocaba - UNISOMethodist University of PiracicabaUniversidade Estadual Paulista (UNESP)Universidade de São Paulo (USP)Chaud, Marco ViniciusTamascia, Pollyannade Lima, Andreäa Cristina [UNESP]Paganelli, Maria OndinaGremiäo, Maria Palmira Daflon [UNESP]de Freitas, Osvaldo2022-04-29T08:48:23Z2022-04-29T08:48:23Z2010-01-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article473-481http://dx.doi.org/10.1590/s1984-82502010000300010Brazilian Journal of Pharmaceutical Sciences, v. 46, n. 3, p. 473-481, 2010.2175-97901984-8250http://hdl.handle.net/11449/23197310.1590/s1984-825020100003000102-s2.0-78651068892Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengBrazilian Journal of Pharmaceutical Sciencesinfo:eu-repo/semantics/openAccess2024-06-24T13:46:33Zoai:repositorio.unesp.br:11449/231973Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T23:40:46.080222Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel |
title |
Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel |
spellingShingle |
Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel Chaud, Marco Vinicius Praziquantel/dissolution rates Praziquantel/intestinal absorption Praziquantel/solubility Solid dispersion |
title_short |
Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel |
title_full |
Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel |
title_fullStr |
Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel |
title_full_unstemmed |
Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel |
title_sort |
Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel |
author |
Chaud, Marco Vinicius |
author_facet |
Chaud, Marco Vinicius Tamascia, Pollyanna de Lima, Andreäa Cristina [UNESP] Paganelli, Maria Ondina Gremiäo, Maria Palmira Daflon [UNESP] de Freitas, Osvaldo |
author_role |
author |
author2 |
Tamascia, Pollyanna de Lima, Andreäa Cristina [UNESP] Paganelli, Maria Ondina Gremiäo, Maria Palmira Daflon [UNESP] de Freitas, Osvaldo |
author2_role |
author author author author author |
dc.contributor.none.fl_str_mv |
University of Sorocaba - UNISO Methodist University of Piracicaba Universidade Estadual Paulista (UNESP) Universidade de São Paulo (USP) |
dc.contributor.author.fl_str_mv |
Chaud, Marco Vinicius Tamascia, Pollyanna de Lima, Andreäa Cristina [UNESP] Paganelli, Maria Ondina Gremiäo, Maria Palmira Daflon [UNESP] de Freitas, Osvaldo |
dc.subject.por.fl_str_mv |
Praziquantel/dissolution rates Praziquantel/intestinal absorption Praziquantel/solubility Solid dispersion |
topic |
Praziquantel/dissolution rates Praziquantel/intestinal absorption Praziquantel/solubility Solid dispersion |
description |
The solubility behavior of drugs remains one of the most challenging aspects in formulation development. Solid Dispersion (SD) has tremendous potential for improving drug solubility. Although praziquantel (PZQ) is the first drug of choice in the treatment of schistosomiasis, its poor solubility has restricted its delivery oral route. In spite of its poor solubility, PZQ is well absorbed in the gastrointestinal tract, but large doses are required to achieve adequate concentration at the target sites. The aim of this study was to improve the solubility and dissolution rate of PZQ and to evaluate its intestinal absorption. SDs were formulated with PEG-60 castor oil hydrogenated (CR-60) using a fusion and evaporation method. Pure PZQ and physical mixtures (PM) and PZQ-CR-60 (2:1; 1:1; 1:2 ratios) were compared as regards their solubility, dissolution and intestinal absorption. The experimental results demonstrated the improvement in the solubility, dissolution rate and intestinal absorption. In addition, the solubility behavior showed pH dependency and that the solubility of PZQ was slower in acidic medium than in neutral and basic mediums. The increase in PZQ solubility of the SD with the CR-60 could be attributed to several factors such as improved wettability, local solubilization, drug particle size reduction and crystalline or, interstitial solid solution reduction. |
publishDate |
2010 |
dc.date.none.fl_str_mv |
2010-01-01 2022-04-29T08:48:23Z 2022-04-29T08:48:23Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.1590/s1984-82502010000300010 Brazilian Journal of Pharmaceutical Sciences, v. 46, n. 3, p. 473-481, 2010. 2175-9790 1984-8250 http://hdl.handle.net/11449/231973 10.1590/s1984-82502010000300010 2-s2.0-78651068892 |
url |
http://dx.doi.org/10.1590/s1984-82502010000300010 http://hdl.handle.net/11449/231973 |
identifier_str_mv |
Brazilian Journal of Pharmaceutical Sciences, v. 46, n. 3, p. 473-481, 2010. 2175-9790 1984-8250 10.1590/s1984-82502010000300010 2-s2.0-78651068892 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
473-481 |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
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1808129542480461824 |