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

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

Author Duque, Marcelo Dutra Autor UNIFESP Google Scholar
Issa, Michele Georges Google Scholar
Silva, Daniela Amaral Google Scholar
Sakamoto Kakuda, Beatriz Ayumi Autor UNIFESP Google Scholar
Carpentieri Rodrigues, Leticia Norma Autor UNIFESP Google Scholar
Lobenberg, Raimar Google Scholar
Ferraz, Humberto Gomes Google Scholar
Abstract 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.
Keywords pyrimethamine
intrinsic dissolution rate
xmlui.dri2xhtml.METS-1.0.item-coverage Hockessin
Language English
Sponsor National Council of Scientific and Technological Development (CNPq/Brazil)
Grant number CNPq: 400455/2014-5
Date 2017
Published in Dissolution Technologies. Hockessin, v. 24, n. 4, p. 6-11, 2017.
ISSN 1521-298X (Sherpa/Romeo, impact factor)
Publisher Dissolution Technologies, Inc
Extent 6-11
Access rights Open access Open Access
Type Article
Web of Science ID WOS:000416133600001

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