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Vol. 24, Art. 74 (pp. 1087-1096)    |    2023       

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Approaches to the development of prodrugs on examples of successful strategies for increasing oral bioavailability of drugs (Literature review)

Orlova A.B., Ivanov I.M., Nikiforov A.S., Kolesnikov A.M.

FSBI «State Research Testing Institute of Military Medicine» of the Ministry of Defense of the Russian Federation

Brief summary

The review considers approaches to increasing the oral bioavailability of physiologically active substances (PAS) through their chemical modification aimed at optimizing the physicochemical and pharmacological properties. For poorly soluble substances, using the example of tedizolid phosphate and isavuconazonium sulfate, the approach of adding polar functional groups is considered. A modification aimed at improving passive permeability was implemented when creating prodrugs of oseltamivir carboxylate and dabigatran etexilate. The transfer of polar exogenous molecules by facilitated diffusion has been demonstrated in the development of valaciclovir and valganciclovir. The strategy of modifying the molecule to protect it from first pass metabolism was applied in the development of bambutirol, a prodrug of terbutaline.


Key words

prodrugs, oral bioavailability, chemical modification

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