Comparison of laser nephelometric and HPLC techniques for efficient determination of solubility of ibuprofen and its 2-hydroxypropyl-cyclodextrin inclusion.
Ssengooba, Frank Marimuthu, Thashree Olivier, Eugene Ivan Denama, Patrick Hulisani Choonara, Yahya E.
Ssengooba, Frank
Marimuthu, Thashree
Olivier, Eugene Ivan
Denama, Patrick Hulisani
Choonara, Yahya E.
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Abstract
High-throughput screening (HTS) is an important method in the pharmaceutical industry for discovering hits that will be further developed into leads, clinical candidates, and eventually into medicines. After an HTS campaign, solubility studies of the discovered hits are an important means to judge the validity of the pharmacological result and to prioritize them for further studies. In the present paper, different methods for determination of kinetic solubility were compared that are able to provide sufficient throughput and that consume only small amounts of compound. In particular nephelometric determination, UV-spectroscopic determination, and determination of kinetic solubility by HPLC have been investigated. These three assays have been compared with regard to their detection limit, information content, and speed/throughput. Further on, parameters influencing solubility in the specific HTS assay which may vary for different HTS assays are discussed. These include formation of different salt forms, time used for incubation during the assay, and concentration of cosolvent. Finally, a comparison of the results and purpose of kinetic and thermodynamic solubility is given.
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Date
2021-09-03
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Publisher
South African Chemical Institute
Research Projects
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Keywords
Cyclodextin, Ibuprofen, Inclusion complex, Laser nephelometry, Solubility