There are many possible reasons why a drug may require modified or targeted release. Some of these are related to the characteristics of the product itself, such as its pharmacodynamic or pharmacokinetic profile and the need to avoid degradation in specific areas of the gastrointestinal tract, or a desire to manage a product’s life cycle in the market. Others arise from clinical considerations like the importance of taking a drug to the precise site in the gut where the release will be most effective or improving patient compliance.

At Quay Pharma, we have world-leading expertise in the science of modified release technologies, and a wealth of experience covering a wide range of modified and targeted release projects. We can provide you with a vast range of options to modify the rate at which an API is released, and for ensuring that it is delivered only to a specific, predetermined site within the gastrointestinal tract. All of the formulations we develop are provided to clients with full Intellectual Property rights, and on a royalty-free basis.

Solubility and bioavailability are overwhelming challenges in drug development. We have a range of practical, proven approaches for overcoming these barriers. Approximately 40% of all drugs currently on the market, and 90% of the compounds at present in development for future use, are reported to show poor solubility in water. This leads to difficulties in obtaining adequate, reproducible absorption from the gastrointestinal tract after oral administration. Poor solubility and variable drug absorption are associated with low bioavailability, and ultimately affect the efficacy and safety of the product.

Class 1 (High Solubility) High Solubility, High Permeability, Rapid Dissolution. Class 1 drugs do not normally exhibit bioavailability problems. However, from a pharmacokinetic perspective, a slower but longer-lasting release would sometimes be preferable.

Class 2 (Low Solubility) Low Solubility, High Permeability. Class 2 includes the majority of NCEs in the development pipelines. Their solubility in the gastrointestinal tract has to be increased to allow them to be formulated into marketable products

Class 3 (High Solubility) High Solubility, Low Permeability. Class 3 drugs are soluble in the gastrointestinal tract but not readily taken up by the body. Permeation enhancing techniques are required to to turn them into clinically effective products

Class 4 (Low Solubility) High Solubility, Low Permeability. Class 4 contains substances that neither dissolve nor penetrate physiological barriers to enter the body. They are not usually developed further, although they may have some application when used with pro-drugs.

Our unparalleled range of technologies designed to increase the solubility or permeability of drug compounds have applications throughout the development process, from the earliest stages to commercialisation. Provided on a royalty-free basis, they include:

While lipophilic systems, solid dispersions, particle size reduction and pH control are the principal techniques used to overcome solubility difficulties, we have a wide range of other approaches, such as the ones below, which we use where they will offer results that more closely meet the needs of our clients.