Bioavailability Enhancement
Bioavailability is the rate and extent to which the active pharmaceutical ingredient (API) or drug is absorbed from a drug product and becomes available at the drug action site. This depends on the physical and chemical properties of the drug molecule and how it interacts with the body upon administration. Route of administration also plays a factor in bioavailability.
In oral dosage forms, bioavailability provides an estimate of the relative fraction amount of dose that’s been absorbed into systemic circulation. However, an increasing number of newly discovered drugs have poor oral bioavailability. At Vici, our highly qualified, experienced formulation development scientists can offer strategies to enhance bioavailability.
Reasons for low bioavailability include poor drug solubility, drug degradation in low pH environments such as the stomach, digestive enzyme activity in the intestinal membranes, or first pass metabolism by the liver immediately post absorption.
The biopharmaceutics classification system (BCS) is a useful tool to pinpoint the root causes of poor bioavailability and how to go about solving them through formulation improvements:
- Poor solubility can sometimes be overcome by micronization or co-processing with solubility enhancers
- Degradation in the stomach is relatively easy to address by using enteric formulations that protect the drug from the stomach pH
- Permeability enhancers to solve low bioavailability of drugs due to poor permeability
- More advanced techniques such as self-emulsifying drug delivery systems (SEEDS) can be used for drugs that have poor solubility and undergo first pass metabolism by the liver
Altering the material properties of a drug in a formulation is another method to increase solubility for poorly soluble drugs. This can be done by maintaining the drug in its amorphous state where its solubility remains high. Amorphous solid dispersion technologies have existed for many years and we at Vici have a deep understanding of these systems.
Vici Health Sciences is partnered with universities to perform full crystal nature characterization of formulations (XRD and DCS). With a thorough analysis of the drug attributes, our formulation specialists can identify the key properties to ensure stability and maximize bioavailability.
In addition to drug characterization, Vici is experienced in formulating dosage forms for various routes of administration. If a drug has poor oral bioavailability, we can formulate the product into a dosage form more suitable for systemic absorption – such as a buccal dosage form – which can bypass the stomach and intestinal route of administration entirely.
Contact one of our formulation experts at Vici Health Sciences to learn more about the different services we offer to help speed up your drug development timeline.
