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Poorly Soluble Compounds

Poor solubility is a major issue in the development of new drugs. A common strategy in this situation is to increase the dissolution rate of the drug. Poor dissolution often results in low and highly variable bioavailability.Improving the dissolution rate of a poorly soluble compound leads to improved bioavailability and reduced side effects. This enables better control of the therapeutic dose. Such improvements can lead to lower doses and lower cost of goods.

RightSize Particle technology can improve the dissolution rate of drug substances through various strategies. These include nanoparticle production, generation of solid dispersions and formation of cocrystals or salts.
  • Improve dissolution rate
  • Improve bioavailability
  • Lower dose requirements
  • Reduce formulation development time

Nanoparticles

Increasing the particle surface area to mass ratio through the production of nanoparticles is an attractive method to improve dissolution rates. RightSize Particle technology is able to produce nanoparticles with consistent size below 200 nm. Adjusting process parameters, such as temperature, pressure and solvent choice, allows easy control of particle size and size distribution.

Amorphous or Crystalline
Nanoparticles can be produced from biomolecules as well as small organic molecules. Moderate temperatures are used in the process, making it ideal for thermolabile compounds. Both amorphous and highly crystalline particles can be formed.

High Drug Load
RightSize Particle technology is compatible with a wide range of excipients. Excipients can, for example, be added to increase stability and/or wettability in amounts from >50% down to trace amounts. The API can also be processed without any excipients, generating a drug product with high drug load.

RightSize produced crystalline Budesonide.

Solid Dispersions

RightSize Particle technology is well suited to the production of solid dispersions, as demonstrated by Itraconazole-HPMCP particles. A wide variety of solid dispersion systems have been successfully tested resulting in enhanced solubility.

Amorphous product with good stability can be produced through the tuning of process parameters. In the graph, PXRD shows that the product is still amorphous after six months storage at ambient conditions.

Another inherent benefit of the technology is minimal residual solvent. A supercritical extraction step ensures the effective removal of solvent.

SEM picture of Itraconazole - HPMC P55

Cocrystal & Salt

RightSize Particle technology enables particle and crystal properties to be chosen rather than constrained by the production technology.

It is well suited for co-precipitation. Cocrystals and salts can be easily formed in a single-step process. Highly crystalline particles can be produced and polymorph selection is simple to control.