Solubility and Oral Bioavailability Enhancement of Pharmaceuticals: Challenges and Opportunities
Rakesh Bhasin, Senior Vice President, Cadila Pharmaceuticals
It has been estimated that around 60-70% of drug molecules in drug discovery program are poorly soluble in aqueous media and/or have very low permeability to allow for their adequate and reproducible absorption from the gastrointestinal tract (GIT) following oral administration. In recent years drug bioavailability has become a subject of interest not only in drug development, but also in the early stages of drug discovery. Most of the candidate drugs that failed in clinical trials did so because of problems with ADME (absorption, distribution, metabolism, excretion) and toxicology, rather than through lack of efficacy. Efforts are made in pharmaceutical industry to improve success rates by improving bioavailability. Here, attention is focused to briefly discuss factors affecting bioavailability and poor performance of actives, technologies that alter these factors like pharmaceutical factors, dosage form characteristics. Here techniques for improving oral bioavailability like nanosuspension, microemulsion, self micro emulsifying drug delivery system (SMEDDS), solid lipid nanoparticles (SLNs), polymeric nanoparticles, vesicular delivery systems such as liposomes and other technology like Cocrystals etc has been discussed. At the same time, various regulatory challenges and Opportunities associated with drug development program has been discussed.
|
|