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Analysis and optimization of drug solubility to improve pharmacokinetics

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Abstract

Solubility measurement is one of the key elements that need to be considered in drug discovery and development process. Hence, its appropriate analysis and optimization is necessary to enhance the drug’s pharmacokinetic and therapeutic effects. In this article, different methods used for solubility analysis and optimization such as shake flask, potentiometric, turbidimetric, computational, miniature device and high throughput automated methods have been summarized. Additionally, the effect of solubility optimization methods (physical, chemical and carrier technology modifications) on pharmacokinetic enhancement has also been elucidated. New fast, feasible and automated methods of solubility analysis are necessary for its accurate measurement as well as for minimization of errors posed by traditional methods. Among the physical, chemical and carrier modification methods; higher potential is exhibited by nanoparticulate drug delivery carriers for optimization of drug solubility and enhancement of pharmacokinetics. Based on the drug characteristics and delivery requirement, appropriate method can be chosen for efficient solubility and pharmacokinetics enhancement of lipophilic drugs, especially of BCS class II and class IV.

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  1. College of Pharmacy, Yeungnam University, 214-1 Dae-dong, Gyeongsanbuk-do, Gyeongsan-si, 712-749, South Korea

    Raj Kumar Thapa, Jong Oh Kim & Chul Soon Yong

  2. College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Ansan, Sangnok-gu, 426-791, South Korea

    Han-Gon Choi

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  1. Raj Kumar Thapa
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Correspondence to Jong Oh Kim or Chul Soon Yong.

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All authors (R.K. Thapa, H.G. Choi, J.O. Kim, C.S. Yong) declare that they have no conflict of interest.

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Thapa, R.K., Choi, HG., Kim, J.O. et al. Analysis and optimization of drug solubility to improve pharmacokinetics. Journal of Pharmaceutical Investigation 47, 95–110 (2017). https://doi.org/10.1007/s40005-016-0299-z

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  • Issue Date:

  • DOI: https://doi.org/10.1007/s40005-016-0299-z

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