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Enhanced solubilisation using complexing agents, co-solvents lipids and surfactants

The solubility of the API may be increased by mixing it with a number of solubility enhancing reagents. Typically the IPI would undertake an initial screen of reagents which would include investigating the use of co-solvents, cyclodextrins, lipids and surfactants.

Our Approach:
Phase 1-Initial screen
Typically about 15 simple systems will be screened to identify those in which the solubility of the API is significantly enhanced. The solubility of the API will be assessed by visual and microscopic inspection.

Phase 2- Designing a liquid formulation for preclinical studies
Following analysis of the data from the initial screen, IPI scientists will design a small number, typically three, of liquid formulations at the customer’s desired concentration of API. The main concern with the prototype formulations is whether the API remains in solution over a period of time, a range of pH and a range of temperatures. To determine this, the prototype formulations will be stored at a range of temperature conditions over a 1 week period. The samples will be observed visually to determine the affects on solubility. In addition, samples of the prototype formulations will be diluted into buffer solutions over a range of pH values to determine the affect of pH on solubility of the API; again samples will be visually inspected.

Phase 3-Development and stability testing of selected formulation(s)
If positive short term stability/solubility results are obtained from the testing of prototype formulations then typically one will be selected for additional stability/solubility testing. This will involve more detailed analytical methodology, for example an HPLC assay method will be used to determine maximum solubility, as well as solubility and chemical stability over time at a range of temperatures.