Selected polyols as co-formers for pharmaceutical solid dispersions

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Date

2024

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Publisher

Universty of the Western Cape

Abstract

Poor aqueous solubility is a major concern for most new chemical entities (NCEs) developed for oral drug delivery as well as for almost 70% of registered and already marketed drugs. Solid-state alterations such as solid dispersions (SDs), co-amorphous and co-crystal systems have taken the lead over the past two decades, in an effort to address the challenge of poor drug solubility. One of the common factors amongst these techniques, that play a significant role in solubility enhancement, is the type of carrier or co-former used. Low molecular weight excipients such as amino acids, citric acid and a few sugars were studied as potential co-formers. However, the efforts made in identifying new low molecular weight excipients were modest. Given their low molecular weight, safety, hydrophilic nature and having high hydrogen bonding propensity makes polyols an interesting option to be explored as carriers.

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Keywords

Solid dispersions, solubility enhancement, increased dissolution rate, membrane permeation, isoniazid

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