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Issue: April 2015, Posted Date: 3/30/2015
FORMULATION DEVELOPMENT - A QbD Approach to Develop Extended Release Softgels
INTRODUCTION
Soft gelatin capsules (softgels) continue to be the oral solid dosage form preferred by consumers.1 Understandably, as they are easy to swallow and digest, effectively mask unpleasant tastes and smells, and have a pleasing appearance. Softgels also offer formulation and marketing benefits. They can accommodate a wide variety of compounds filled as liquids, solids, semi-solids, suspensions, or emulsions. They can also address a broad range of formulation challenges, such as improving the absorption and bioavailability of poorly water-soluble APIs. Softgels are particularly well suited for formulating low melting point APIs, which require additional processes for tablet forms. They also allow low- and ultra-low-dose precision for highly potent compounds. To extend product lifecycle with added patent protection, softgels can be developed in various dosage forms, such as chewables, controlled release, and softgels from non-animal materials.
Developing drug delivery systems with a targeted drug-release profile can be challenging, especially with dosages that require timed release, high dose, limited volume, and abuse deterrence simultaneously. Wisely choosing and efficiently modulating a release system for the aforementioned purpose is a head-scratching task that requires deep understanding of formulation science and softgel expertise. Formulation scientists must know the most efficient and effective ways to develop the softgel fill medicine and capsule shell to ensure quality and mitigate risk, saving formulation time and costs. Following Quality by Design (QbD) is the most appropriate approach for every aspect of pharmaceutical development.
This paper reviews the fundamentals and technologies for formulating sustained-release softgel capsules, presents a study by Banner Life Sciences to develop an extended-release matrix of softgel capsule fill that has the aforementioned characteristics for highly soluble drugs, and demonstrates the general approach of applying QbD methodology to extended-release softgel product development.
ACHIEVING CONTROLLED RELEASE SOFTGELS
For many medical conditions, such as metabolic disorder, allergy, cancer, autoimmune, and neurodegenerative diseases, it is desirable for the drug to reach its targeted site of action at a therapeutically effective level and for the drug concentration to remain at that level over a sufficient period of time.2 These requirements can be met by applying controlled-release technologies to the oral solid dosage form through matrix swelling, erosion, or...