Compound Profiling

Physicochemical Profiles

 

Ionization – Pion instrumentation and expertise can determine the pKa values of compounds with extremely low-aqueous solubility, high molecular weight, and multiple, overlapping ionization constants. pKa measurements are performed by either spectrophotometric or potentiometric methods. Drug ionization profiles explain the behavior of drug molecules. As a drug molecule ionizes into species with different charges, its physical, chemical and biological properties are also affected.  

 

Solubility - Equilibrium and kinetic solubility measurements are performed using Pion’s patented methods and instrumentation. Measurements can be done across a range of pH values using buffers or biorelevant media like SGF, FaSSIF and FeSSIF.  Utilizing in situ techniques the kinetic solubility or dissolution can be characterized as quickly as every second.

 

Dissolution - Pion utilizes advanced fiber optics for in situ kinetic solubility and supersaturation UV monitoring for dissolution testing to determine the rate of release of a drug substance over time. From pure API, to formulations, to finished QC drug product, Pion can meet the need of every scientist along the drug development cycle.

 

Absorption – Pion has pioneered reliable methods for predicting the absorption potential of finished dosage products prior to clinical trials. New testing technology allows Pion to combine traditional dissolution testing with repeatable methods for assessing the absorption potential of APIs, API/ingredient combinations, or finished dosage products. As a result, Pion can more reliably and realistically test and model IVIVC (in vitro-in vivo correlation). Pion’s approach allows potential problems with the permeability and absorption potential of a promising compound to be identified far earlier in the development process. In addition, Pion can accurately predict the absorption potential and bioequivalence of various finished dosage products earlier in development. This capability facilitates better decision-making and resource allocation by pharmaceutical developers.

 

Permeability – Pion’s Double-Sink™ PAMPA assay is commonly performed across a range of pH values anywhere from pH 3-10. The compound’s permeability when compared to standard compounds can be used to predict human intestinal, blood-brain or skin permeability depending on the model.

 

Lipophilicity - The octanol-water partition coefficient logP (lipophilicity as a function of pH) is used in combination with the pKa to predict the distribution of a drug compound in a biological system. Factors such as absorption, excretion and penetration of the CNS may be related to the log P of a drug.