Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification
Autor(a) principal: | |
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Data de Publicação: | 2017 |
Outros Autores: | , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNIFESP |
Texto Completo: | https://repositorio.unifesp.br/handle/11600/58251 http://dx.doi.org/10.14227/DT240417P6 |
Resumo: | Intrinsic dissolution testing allows characterizing drug substances through its dissolution rate when exposed to a specified surface area in a specific dissolution media, This can be used to determine if a drug substance is highly or poorly soluble. In this work. DDDPlus version 4.0 (Simulations Plus, Inc.) was used to simulate intrinsic dissolution experiments for pyrimethamine and metronidazole. These drugs have low and high solubility properties. Predicted intrinsic dissolution rates (IDR) were compared to observed in vitro IDR. Physicochemical parameters from literature and the experimental conditions of the intrinsic dissolution tests for each drug were used as input data into the software. The program was able to predict the IDR of pyrimethamine and metronidazole within a pH range of 1.0 to 7.2. Observed and predicted IDR values for both drugs showed high correlations (R-2 > 0.9424), The IDR values from simulations showed the pH-dependent solubility of pyrimethamine and metronidazole, allowing us to classify the solubility according to the Biopharmaceutics Classification System (BCS). Intrinsic dissolution test simulations using DDDPlus can be used to obtain a BCS solubility classification of a drug substance, helping to reduce the number of laboratory experiments. |
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Duque, Marcelo Dutra [UNIFESP]Issa, Michele GeorgesSilva, Daniela AmaralSakamoto Kakuda, Beatriz Ayumi [UNIFESP]Carpentieri Rodrigues, Leticia Norma [UNIFESP]Lobenberg, RaimarFerraz, Humberto Gomes2020-09-01T13:21:25Z2020-09-01T13:21:25Z2017Dissolution Technologies. Hockessin, v. 24, n. 4, p. 6-11, 2017.1521-298Xhttps://repositorio.unifesp.br/handle/11600/58251http://dx.doi.org/10.14227/DT240417P6WOS000416133600001.pdf10.14227/DT240417P6WOS:000416133600001Intrinsic dissolution testing allows characterizing drug substances through its dissolution rate when exposed to a specified surface area in a specific dissolution media, This can be used to determine if a drug substance is highly or poorly soluble. In this work. DDDPlus version 4.0 (Simulations Plus, Inc.) was used to simulate intrinsic dissolution experiments for pyrimethamine and metronidazole. These drugs have low and high solubility properties. Predicted intrinsic dissolution rates (IDR) were compared to observed in vitro IDR. Physicochemical parameters from literature and the experimental conditions of the intrinsic dissolution tests for each drug were used as input data into the software. The program was able to predict the IDR of pyrimethamine and metronidazole within a pH range of 1.0 to 7.2. Observed and predicted IDR values for both drugs showed high correlations (R-2 > 0.9424), The IDR values from simulations showed the pH-dependent solubility of pyrimethamine and metronidazole, allowing us to classify the solubility according to the Biopharmaceutics Classification System (BCS). Intrinsic dissolution test simulations using DDDPlus can be used to obtain a BCS solubility classification of a drug substance, helping to reduce the number of laboratory experiments.National Council of Scientific and Technological Development (CNPq/Brazil)Univ Sao Paulo, Fac Pharmaceut Sci, Dept Pharm, Sao Paulo, BrazilUniv Fed Sao Paulo UNIFESP, Inst Environm Chem & Pharmaceut Sci, Dept Exact & Earth Sci, Sao Paulo, BrazilUniv Alberta, Ctr Pharm & Hlth Res, Fac Pharm & Pharmaceut Sci, Edmonton, AB, CanadaUniv Fed Sao Paulo UNIFESP, Inst Environm Chem & Pharmaceut Sci, Dept Exact & Earth Sci, Sao Paulo, BrazilCNPq: 400455/2014-5Web of Science6-11engDissolution Technologies, IncDissolution Technologiespyrimethaminemetronidazoleintrinsic dissolution rateBCSDDDPlusdissolutionIntrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classificationinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleHockessin244info:eu-repo/semantics/openAccessreponame:Repositório Institucional da UNIFESPinstname:Universidade Federal de São Paulo (UNIFESP)instacron:UNIFESPORIGINALWOS000416133600001.pdfapplication/pdf640690${dspace.ui.url}/bitstream/11600/58251/1/WOS000416133600001.pdf63973d8e976a509280ab259b9475b524MD51open accessTEXTWOS000416133600001.pdf.txtWOS000416133600001.pdf.txtExtracted texttext/plain26170${dspace.ui.url}/bitstream/11600/58251/8/WOS000416133600001.pdf.txt2b2338fd4f69fae92a59f456f51b04e2MD58open accessTHUMBNAILWOS000416133600001.pdf.jpgWOS000416133600001.pdf.jpgIM Thumbnailimage/jpeg8515${dspace.ui.url}/bitstream/11600/58251/10/WOS000416133600001.pdf.jpg51c6a7bc246f0d7fd897e6279ea6f106MD510open access11600/582512023-06-05 19:35:20.718open accessoai:repositorio.unifesp.br:11600/58251Repositório InstitucionalPUBhttp://www.repositorio.unifesp.br/oai/requestopendoar:34652023-06-05T22:35:20Repositório Institucional da UNIFESP - Universidade Federal de São Paulo (UNIFESP)false |
dc.title.en.fl_str_mv |
Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification |
title |
Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification |
spellingShingle |
Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification Duque, Marcelo Dutra [UNIFESP] pyrimethamine metronidazole intrinsic dissolution rate BCS DDDPlus dissolution |
title_short |
Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification |
title_full |
Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification |
title_fullStr |
Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification |
title_full_unstemmed |
Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification |
title_sort |
Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification |
author |
Duque, Marcelo Dutra [UNIFESP] |
author_facet |
Duque, Marcelo Dutra [UNIFESP] Issa, Michele Georges Silva, Daniela Amaral Sakamoto Kakuda, Beatriz Ayumi [UNIFESP] Carpentieri Rodrigues, Leticia Norma [UNIFESP] Lobenberg, Raimar Ferraz, Humberto Gomes |
author_role |
author |
author2 |
Issa, Michele Georges Silva, Daniela Amaral Sakamoto Kakuda, Beatriz Ayumi [UNIFESP] Carpentieri Rodrigues, Leticia Norma [UNIFESP] Lobenberg, Raimar Ferraz, Humberto Gomes |
author2_role |
author author author author author author |
dc.contributor.author.fl_str_mv |
Duque, Marcelo Dutra [UNIFESP] Issa, Michele Georges Silva, Daniela Amaral Sakamoto Kakuda, Beatriz Ayumi [UNIFESP] Carpentieri Rodrigues, Leticia Norma [UNIFESP] Lobenberg, Raimar Ferraz, Humberto Gomes |
dc.subject.eng.fl_str_mv |
pyrimethamine metronidazole intrinsic dissolution rate BCS DDDPlus dissolution |
topic |
pyrimethamine metronidazole intrinsic dissolution rate BCS DDDPlus dissolution |
description |
Intrinsic dissolution testing allows characterizing drug substances through its dissolution rate when exposed to a specified surface area in a specific dissolution media, This can be used to determine if a drug substance is highly or poorly soluble. In this work. DDDPlus version 4.0 (Simulations Plus, Inc.) was used to simulate intrinsic dissolution experiments for pyrimethamine and metronidazole. These drugs have low and high solubility properties. Predicted intrinsic dissolution rates (IDR) were compared to observed in vitro IDR. Physicochemical parameters from literature and the experimental conditions of the intrinsic dissolution tests for each drug were used as input data into the software. The program was able to predict the IDR of pyrimethamine and metronidazole within a pH range of 1.0 to 7.2. Observed and predicted IDR values for both drugs showed high correlations (R-2 > 0.9424), The IDR values from simulations showed the pH-dependent solubility of pyrimethamine and metronidazole, allowing us to classify the solubility according to the Biopharmaceutics Classification System (BCS). Intrinsic dissolution test simulations using DDDPlus can be used to obtain a BCS solubility classification of a drug substance, helping to reduce the number of laboratory experiments. |
publishDate |
2017 |
dc.date.issued.fl_str_mv |
2017 |
dc.date.accessioned.fl_str_mv |
2020-09-01T13:21:25Z |
dc.date.available.fl_str_mv |
2020-09-01T13:21:25Z |
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.citation.fl_str_mv |
Dissolution Technologies. Hockessin, v. 24, n. 4, p. 6-11, 2017. |
dc.identifier.uri.fl_str_mv |
https://repositorio.unifesp.br/handle/11600/58251 http://dx.doi.org/10.14227/DT240417P6 |
dc.identifier.issn.none.fl_str_mv |
1521-298X |
dc.identifier.file.none.fl_str_mv |
WOS000416133600001.pdf |
dc.identifier.doi.none.fl_str_mv |
10.14227/DT240417P6 |
dc.identifier.wos.none.fl_str_mv |
WOS:000416133600001 |
identifier_str_mv |
Dissolution Technologies. Hockessin, v. 24, n. 4, p. 6-11, 2017. 1521-298X WOS000416133600001.pdf 10.14227/DT240417P6 WOS:000416133600001 |
url |
https://repositorio.unifesp.br/handle/11600/58251 http://dx.doi.org/10.14227/DT240417P6 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.ispartof.none.fl_str_mv |
Dissolution Technologies |
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info:eu-repo/semantics/openAccess |
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openAccess |
dc.format.none.fl_str_mv |
6-11 |
dc.coverage.none.fl_str_mv |
Hockessin |
dc.publisher.none.fl_str_mv |
Dissolution Technologies, Inc |
publisher.none.fl_str_mv |
Dissolution Technologies, Inc |
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