API Solubility Enhancement

APIs with poor solubility characteristics can often present significant challenges during early preclinical pharmacokinetic (PK) and toxicology investigations, which often leads to high dose formulations being administered to obtain the required exposure levels.

In order to help overcome this problem, Pharmaterials has developed a rational screening platform aimed at finding quick and cost-effective solutions to support such studies. We are well-equipped to work with limited API supplies and are sensitive to the tight timelines and the need for flexibility during such investigations, therefore, all study plans are individually tailoured depending on each clients specific requirements and goals. A recommended systematic approach is described below.

• Step 1: API Evaluation
  
  1. Solubility screening
  2. pKa determination
  3. Crystallinity assessment
  
  
• Step 2: Solubility Enhancement
  
  1. Co-solvents (GRAS approved)
  2. Lipid-based systems (solutions, emulsions)
  3. Additives/complexes (surfactants, polymers, cyclodextrins)
  4. Solid-state modification (particle size reduction, salt formation, solid-state stabilisation of the amorphous state)

• Step 3: Prototype Evaluation
  
  1. Chemical stability
  2. Physical stability (precipitation, form transformation)
  3. Physical and chemical stability in Simulated Gastric Fluid
  4. Dosing properties (drug loading, content uniformity, ease of administration)

This process typically takes 4-6 weeks, requiring ca. 5-10 g of active material. For more information or to arrange a meeting to discuss your company's own requirements, please contact us at: enquiries@pharmaterials.co.uk.

Pharmaterials can take you seemlessly from concept to clinical supply.