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European Biopharmaceutical Review

Dispersions Deliver Results

 

Low-solubility, high-permeability compounds make up nearly one-third of all active pharmaceutical ingredients (APIs) in early development. For many compounds in this class, oral absorption can be achieved by enhancing solubility using solubilisation technologies. This article is an overview of current options in solid form solubilisation technologies, including several novel platforms that are based on nanocrystals and drug/polymer solid amorphous dispersions. The platforms discussed are spray-dried dispersions (SDDs), nanoadsorbates and crystallised spray-dried dispersions (CSDDs). Strategies are described to guide rational selection of the optimum technology for solubility enhancement.

Poor oral bioavailability due to the low aqueous solubility of potential drug candidates is an increasingly common challenge facing the pharmaceutical industry (1). Nearly one-third of compounds in early development have poor bioavailability due to low solubility, representing a significant loss in economic and therapeutic opportunity (2). Although they may not fit the ‘rule of five’, many of these low-solubility compounds – which fall into Class II of the Biopharmaceutics Classification System (BCS) – have the potential to be safe and efficacious, so it is critical that further development is not halted by solubility limitations (3).

In response to this problem, multiple drug-delivery technologies have been advanced in an attempt to solubilise such molecules in order to enhance their oral bioavailability. Solubilisation technologies can improve oral absorption of BCS Class II compounds by:

  • Increasing dissolution rate
  • Increasing concentration of dissolved drug (above the equilibrium concentration of the solubility of bulk crystalline drug)
  • Maintaining the enhanced dissolved drug concentration

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Dr David T Vodak is a Senior Research Chemist and Group Leader at Bend Research Inc, a private research and development laboratory in Bend, Oregon. David holds a PhD in materials chemistry from the University of Michigan-Ann Arbor and a BA in Chemistry from Willamette University in Salem, Oregon. After completing his post-doctoral work at the Scripps Research Institute in La Jolla, California, David joined Bend Research Inc, where he has worked on novel technology development. His areas of expertise are the research and development of novel pharmaceutical drug-delivery systems for the delivery of low-solubility compounds.

Dr Dwayne T Friesen is the Vice President of Research at Bend Research Inc. Dwayne holds a PhD in physical chemistry from Oregon State University in Corvallis, Oregon, and a BS in Chemistry from California State College – Bakersfield. He holds 44 US patents and has 15 scientific publications. Dwayne directs the research and development for novel drug-delivery systems and pharmaceutical formulations.

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David T Vodak
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Dwayne T Friesen
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