Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification

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dc.citation.issue4
dc.citation.volume24
dc.contributor.authorDuque, Marcelo Dutra [UNIFESP]
dc.contributor.authorIssa, Michele Georges
dc.contributor.authorSilva, Daniela Amaral
dc.contributor.authorSakamoto Kakuda, Beatriz Ayumi [UNIFESP]
dc.contributor.authorCarpentieri Rodrigues, Leticia Norma [UNIFESP]
dc.contributor.authorLobenberg, Raimar
dc.contributor.authorFerraz, Humberto Gomes
dc.coverageHockessin
dc.date.accessioned2020-09-01T13:21:25Z
dc.date.available2020-09-01T13:21:25Z
dc.date.issued2017
dc.description.abstractIntrinsic 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.en
dc.description.affiliationUniv Sao Paulo, Fac Pharmaceut Sci, Dept Pharm, Sao Paulo, Brazil
dc.description.affiliationUniv Fed Sao Paulo UNIFESP, Inst Environm Chem & Pharmaceut Sci, Dept Exact & Earth Sci, Sao Paulo, Brazil
dc.description.affiliationUniv Alberta, Ctr Pharm & Hlth Res, Fac Pharm & Pharmaceut Sci, Edmonton, AB, Canada
dc.description.affiliationUnifespUniv Fed Sao Paulo UNIFESP, Inst Environm Chem & Pharmaceut Sci, Dept Exact & Earth Sci, Sao Paulo, Brazil
dc.description.sourceWeb of Science
dc.description.sponsorshipNational Council of Scientific and Technological Development (CNPq/Brazil)
dc.description.sponsorshipIDCNPq: 400455/2014-5
dc.format.extent6-11
dc.identifierhttp://dx.doi.org/10.14227/DT240417P6
dc.identifier.citationDissolution Technologies. Hockessin, v. 24, n. 4, p. 6-11, 2017.
dc.identifier.doi10.14227/DT240417P6
dc.identifier.fileWOS000416133600001.pdf
dc.identifier.issn1521-298X
dc.identifier.urihttps://repositorio.unifesp.br/handle/11600/58251
dc.identifier.wosWOS:000416133600001
dc.language.isoeng
dc.publisherDissolution Technologies, Inc
dc.relation.ispartofDissolution Technologies
dc.rightsAcesso aberto
dc.subjectpyrimethamineen
dc.subjectmetronidazoleen
dc.subjectintrinsic dissolution rateen
dc.subjectBCSen
dc.subjectDDDPlusen
dc.subjectdissolutionen
dc.titleIntrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classificationen
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