Bioavailability enhancement – the key to success for pharmaceutical drug products

Poor bioavailability is a hot topic in the pharmaceutical sector. While novel APIs, including biological molecules such as proteins and peptides, are particularly prone, API reformulations can also be affected. As for innovators, more than 40% of all novel APIs never leave the pipeline because they fail to achieve the concentration levels needed for optimal efficacy at the site of action.

Key factors in API bioavailability include drug solubility in an aqueous environment and drug permeability through biological membranes. Another important factor is API stability; this means keeping formulations stable during storage, but also protecting APIs from environmental influences such as gastric acid or humidity.

Current techniques for modifying these factors include counterions, solubilizers, stabilizers, drug carriers, API modification, and hydrogels. These techniques can be used for enhanced solubility, modifying pharmacokinetic/pharmacodynamic profiles, tissue-specific drug targeting, controlled release, and appropriate formulations for optimized bioavailability. New approaches include phytosomes, oral synchronous drug delivery systems, and transient permeability enhancer technology.

With so many techniques and products available to enhance bioavailability, manufacturers need to select the method that will ensure maximum efficacy for their specific molecule – and maximum safety in terms of excipient biocompatibility.

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