Formulating Highly Potent Drugs

New drug compounds, especially those for the proposed use in oncology, have become more selective in their interaction with biological targets, with pharmacological activity usually attained with small amounts of the drug. The production of highly potent drug substances alongside their products needs special attention and care to guarantee the safety of those who manage the materials.

Furthermore, as products having highly potent drugs usually contain minute quantities of the drug per unit dose, it is crucial that during the processing stage, excellent uniformity of dose across an entire batch is attained.

Safe Management of Highly Potent Materials

For the safe management of highly potent materials, production practices have moved away from dependence on safety equipment alone. Modern practices focus on suppression at source, with the use of isolator technologies to prevent the exposure of operators to such compounds all through processing. So given a new drug unit, how do we classify it based on its potency and thus decide what measures are needed to handle it.

Today, many systems have been anticipated for classifying drug substances according to their potency level based on the utilization of occupational exposure bands or occupational exposure limits.

Categorizing Highly Potent Drugs

Usually, a compound can be considered as highly potent when the therapeutic dose is less than one milligram. Some examples of commercial products that fall into the category of highly potent drugs are alprazolam (Xanax tablets, 250 µg per tablet) and digoxin (Linoxin capsules, 100 µg per capsule). An exceptionally highly powerful compound with regard to pharmacological activity is calcitriol.

The safe management of highly potent drug substances is not the only problem associated with manufacturing and development activities. Consideration must also be given to the practicalities of manufacturing a homogeneous group of products with unit doses having small quantities of the drug. In addition, there may be challenges in discovery limits for samples of swabs taken for the cleaning verification of equipment.

This means that, given the responsibility of manufacturing an oral dosage form for a new oncology medicine at a dose of ten micrometers per unit dose, what is the most appropriate formulation tactic. An excellent starting point is to consider implementing the medicine in a liquid vehicle and encapsulating the formulation in a soft gel or hard shell capsule.

Generally, it should be possible to dissolve the low concentration of the drug in a suitable vehicle appropriate for encapsulation.

 

Benefits of Liquid Encapsulation

Below are some of the advantages of the liquid encapsulation approach:

1. Conspicuous limitation of risk of exposure to the operator if the drug is dispersed/dissolved in a liquid vehicle. Here, no airborne dust is generated because it is very common during the process stage of the manufacturing of drugs.

2. Dissolving the tablet in a liquid provides the most excellent opportunity to attain a satisfactory dose consistency for low-dose products.

3. Alternatively, if a liquid-in-capsule presentation is impossible, then a granule formulation can be considered for compression into tablets or encapsulation.

Reach out to AbbVie contract manufacturing for your potent drug contract manufacturing.