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Vanishing Act

For drugs which are administered orally – like capsules and tablets – the bioavailability of the drug and its effectiveness are dependent on its solubility in gastrointestinal fluids. Approximately 80% of new small molecule drugs emerging from discovery pipelines can be regarded as poorly soluble. It is not only the growing number of new compounds that have this problem, it is also the extent of insolubility.

Different Approaches
There are several approaches that are commonly used to improve the drug solubility in aqueous media:

Chemical Modification
If the drug substance is a weak acid or base, it may then be possible to form a salt with a suitable counter ion. Salts are often more water-soluble than the free acid or base form of the compound. However, this approach is not appropriate for neutral molecules. Also, there is no guarantee that the water solubility of the salt will be markedly greater than the free form of the drug.

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Robert Harris is Chief Technical Officer at Juniper Pharma Services and has over 30 years’ experience in the pharma industry. His early career involved technical roles with Warner Lambert and Glaxo Wellcome before spending time in academia as a Research Fellow at the University of Manchester, UK, where he helped develop novel drug delivery systems.
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