Formulations for Low-Dose / High Potency Drugs

Liquid and semi-solid fill or encapsulation technologies are proven methods for effective drug delivery. These technologies have long-established market precedence and are routinely employed for bioavailability enhancement, API stability improvement, and addressing food effects. Liquid and semi-solid fill technologies also offer an optimal approach for delivering high potency / low dose drugs in either liquid fill hard capsule or soft gelatin capsule formats. The percentage of drugs classified as “highly potent”- those with occupational exposure limits (OELs) at or below 10 micrograms per cubic meter—has been steadily increasing in pharmaceutical development pipelines and is estimated to be as high as 30% currently. Many high-potency molecules such as cytotoxics, hormones and steroids are frequently assigned even lower OELs. Formulations for these low-dose / high-potency compounds require specialized production and safeguards to ensure safety for formulators, production personnel and the local environment.

Capsugel specializes in liquid- or semisolid-fill technologies that are particularly suited for formulating high-potency drugs

These technologies, which are based on either liquid-filled hard capsules (LFHC) or soft gelatin capsules, offer a number of advantages over tablets or solid-fill capsules, including:

  • improving product dose uniformity facilitated by highly accurate liquid fill metering
  • minimizing product cross-contamination
  • increasing operator safety through reducing potential exposure
  • reducing processing time and costs
  • increasing filling speeds
  • removing the risk of fire or explosion due to dusting
  • improving the overall ease of handling

We utilize flexible high containment handling capability and facilities for a wide range of compound types and safety classifications, ranging from biologics and small molecules, and inhalation to oral. We can typically accommodate high potency API’s to OEB 5. Our co-located product development and manufacturing sites also are equipped to handle other challenging compounds including controlled substances, hormones and cytotoxics.

Our Capsugel Bend (Bend, OR) division has a flexible stand-alone high containment facility using the latest best practices design features. The facility is designed for safety through state-of-the-art clean room design coupled with engineering controls at the equipment level. Product development teams utilize this facility for a small and large molecule formulation development for either oral or inhaled delivery.

Capsugel offers integrated formulation and secondary manufacturing services for high-potency drugs in either LFHC or soft gelatin capsules. The choice of technology is based on the target product profile, as well as our clients’ commercial and manufacturing considerations. Our capabilities in liquid- and semisolid-fill technologies are augmented by our Bioavailability Enhancement and Modified- / Targeted-Release Suites in addressing complex formulation challenges.

Overall product development efficiency is gained by locating our product-development and production sites together in the US, UK and France. These sites, which are fully equipped to handle up to OEB-5 molecules, produce a range of high-potency drug formulations in both liquid-filled hard capsule and soft-gelatin product formats. Specialized capsule-coating expertise complements our liquid-filled hard-capsule formulation capability for targeted drug delivery.