A New Instrument to Support Drug Formulation

Our goal is to build a new instrument that can be used by pharmaceutical scientists to
investigate formulations of “small molecule” drugs.
The active pharmaceutical ingredients (APIs) in most drugs on the market today are organic
compounds with molecular weight of 500 or less which interact with receptors in the human
body to produce a desired therapeutic effect. Only a few milligrams of these APIs are required
for a single dose. On their own, these doses would look like a few specks of white powder, so
they must be mixed with inert ingredients called excipients to create tablets or capsules which
are of a manageable size for the patient. As well as providing bulk, formulations are used to
modify the behaviour of APIs. Two common procedures are to control the release of API in
order to prolong the effect of the drug over a long period, and to enhance the solubility of
poorly soluble APIs to improve their bioavailability.
Controlled release can be investigated by dissolution experiments, and solubility enhancement
is often achieved by taking advantage of supersaturation. We have developed a new technique
for investigating dissolution under changing pH conditions and in the presence of a lipid
phase to mimic the GI tract. We also hold a patent on a technique for measuring solubility and
supersaturation. We have demonstrated the value of these techniques to customers of our
analytical service. We now seek to develop an automated instrument that we will design
specifically for formulation scientists to exploit this newly developed technology.
Modifying the behaviour of APIs requires clever chemistry. In the past, new compounds were
often shelved because of poor solubility, but recent efforts of formulation scientists have
managed to make some extremely poorly soluble APIs into successful drugs. Formulation is
an important aspect of drug development. All large pharmaceutical companies have
formulation departments, as do generics manufacturers and many subcontractors.