Formulation development: which is the direction?

We are in the era of controlled release formulations, but new emerging technologies are coming, such as fixed dose combinations or those with dual release profile.

The former use multiparticolates with variable coating or two- or three-layer tablets, while in the latter case two or more active ingredients are formulated in the same dosage form. According to Blessed Vladovicova, R & D manager of Saneca Pharma, also the solution of the solubility problems that characterize many new active ingredients will be at the center of the formulators’ priorities in the new year.

The advantages of controlled release formulations

Less risk of dose changes, constant concentrations in the blood and lower toxicity are, for Vladovicova, the main benefits of controlled release formulations. Formulation development is often outsourced – explained Vladovicova – and it is important that the chosen supplier has proven experience and technological ability in the development of this type of complex products. One of the emerging technologies in this sense is the pelletization, which often allows to solve the problems related to the formulation of active ingredients that are not stable or that have compatibility problems.

Formulate the opiates

Another hot topic reported by Vladovicova, especially in the United States where FDA has issued last year a new guideline dedicated to the development of generic abuse-deterrents, is the formulation of opiate drugs used to treat pain. A double-edged sword, because the abuse or misuse of this category of drugs can lead to dependence, and this kind of effect is the basis of the “opium epidemic” which currently represents a health emergency in the US. The abuse-deterrent formulations, explained Vladovicova, contain physical barriers that prevent breaking the tablets to extract the active ingredient. Another approach involves the use of opioid antagonists that are activated in case of wrong use of the medicine by inhibiting the action on the central nervous system, or substances that are unwelcome to the user who tries to alter the dosage form.