Download: The Oral Dosage Drug Delivery Market

Challenges in Oral Formulations

Poor solubility of a drug substance is a major challenge in early oral formulation development. When a drug candidate has poor or low solubility, this can have a major impact on the ability of a drug to be absorbed into a patient’s gastrointestinal tract. The development process needs to be focused on improving the rate of dissolution and maintaining the supersaturated solubility state at the site of absorption. If it is not, it can lead to delays in development or even clinical trial failures, leading to added costs.

Improving the bioavailability of a compound requires extensive knowledge and experience in oral solid dose development. If a company does not have the capabilities in-house to do this successfully, they will need to find a competent partner with the appropriate resources to help bring their drug to market.

Soft Gels are an Art

While oral solids continue to dominate the oral delivery landscape, soft gels are growing in popularity among certain patient population thanks to their ease in swallowing, improved absorption, enhanced bioavailability, and high atmospheric stability. And, due to the flexibility of the substance, soft gels can perform well for complex formulations, including DEA-controlled substances, hormones, and products with multiple APIs.

Creating a soft gel capsule that performs as intended is extremely complicated and difficult, and truly is an art form. Skilled scientists will perform early development studies, such as gel film evaluations, gel fill compatibility, solubility evaluations, and forced degradation studies to simulate what will happen under cGMP conditions.

Trends to Watch for in OSDs

Innovation is being driven by the need to differentiate and to deliver sustainable, advanced products in a crowded pharmaceutical space. Some of these trends include:

• Developing and manufacturing highly potent active pharmaceutical ingredients (HPAPIs);
• Bi-layered tablets for reducing the bill burden;
• Extended release rates;
• 3D printing for customization; and
• Plant-based coating materials.

Why work with a CDMO?

Pharma companies recognize that experienced science based contract development and manufacturing organizations (CDMOs) can have a profound impact on solving OSD formulation and development challenges by providing invaluable pharmaceutical know-how to overcome these difficult-to-formulate drug obstacles. Ideally, you will want to work with a CDMO that provides multiple process capabilities — from small-scale R&D to commercial scale — and has expertise in solubility enhancement, the ability to address challenges for developing, and take your project through to commercialization.

Having a team with decades of experience in developing dosage forms can be invaluable in the early stages of development, as they also have the foresight to look down the road and anticipate any potential future challenges, such as physical instability of the dosage form (i.e., crystallization of amorphous API, particle size growth of wet milled material, or crashing out of API from the supersaturated lipidic formulation). Hence, selection of the right CDMO that has the overall Pharmaceutics Know-How™ to bring the product to the market will dictate the final success of the project.