The need:

BCS Class II (low solubility, high permeability) and Class IV (low solubility, low permeability) drugs are frequently associated with low bioavailability, nonlinear PK and high variability. These drugs classes represent a very significant segment in the pharmaceutical industry:

  1. Around  30- 45% of drugs on the market are poorly soluble
  2. In 2006 Around 90% of drugs in development were either BCS Class II  or Class IV drugs

The Accordion Pill™ solution:

The Accordion Pill™ enhances the drug’s absorption as follows:

By retaining the dosage form in the stomach and releasing the drug gradually towards the upper part of the GI tract, the available drug at the site of absorption can be consistently increased due to:

  1. Enhanced exposure of the drug to bile salts.
  2. Effective exposure of the drug to a relative larger volume of GI media.
  3. Solubility increase of drugs with pH-dependent solubility.

An example:

A designated Accordion Pill™ was developed for a BCS class IV (poor solubility, poor permeability)  drug. The PK of the drug’s current marketed formulation shows limited bioavailability with nonlinear exposure with increasing dose.

The Accordion Pill™ formulation significantly extended the absorption phase of the drug. The bioavailability of the drug was doubled. In addition, The AUC and Cmax achieved with one Accordion Pill™ and two Accordion Pills were found proportional, whereas the commercial formulation does not show dose proportionality in these ranges:

poor-solubility-graph