Delayed Release, Enteric Protection and Colonic Delivery
Capsugel has multiple technologies and approaches for modifying the behavior of drug compounds within the body to achieve:
- Effective targeted drug delivery in the upper gastro-intestinal tract
- Protection of acid-sensitive drugs from acidic stomach conditions
- Protection of the stomach lining from irritating drug actives
- Effective drug delivery to the colon
We have an extensive track record using various polymers and polymer combinations to achieve enteric protection, delayed release, and targeted delivery in the GI tract. The technologies used for targeted delivery are often employed in conjunction with other enabling technologies – such as solubility enhancement – in the development of complex dosage forms:
- Intrinsically enteric capsule technologies – full enteric protection / delayed release without the use of coatings. Capsules are designed for gastric protection, stomach protection against gastric-irritating compounds, and/or protection of the API from stomach acidity.
- Timed-release technologies – using erodible polymer coatings for multiparticulates, tablet matrices and capsules; diffusion / erosion approaches using matrices; or osmotic approaches for zero order release
- pH-controlled-release technologies– using polymer coatings that degrade at specific pH levels for multiparticulates and capsules
- Combination of pH-triggered and enzyme-triggered coatings for reaching the colon
Intrinsically enteric capsule technologies represent a significant breakthrough in providing enteric protection and targeted delivery. By incorporating biopharmaceutically-approved enteric polymers into the hard capsule shell, the technologies eliminate the need for enteric / delayed release coatings, and offer a number of benefits:
- Product development functionality for rapid prototype development and testing of performance in patients
- Speed to clinic – by minimizing the amount of work needed during process development, scale-up and validation programs
- Branding and life cycle management opportunities due to the uniqueness of the capsule functionality
Intrinsically enteric capsule technologies include:
- Vcaps® Enteric – capsules incorporating a polymer blend that enables effective delayed release, gastric protection, and protection of compounds with mild-to-moderate acid sensitivity
- enTRinsic Drug Delivery Technology – capsule technologies incorporating a polymer blend that provides enteric protection to small and large molecules that are highly acid-sensitive.,
In additional to intrinsically enteric capsule technologies, Capsugel offers a full range of finished dosage forms focused on delayed, controlled and targeted release. These can range from single or multi-layer tablets, osmotic tablets, drug-layered or matrixed multiparticulates, capsules-in-capsules, and coated or uncoated capsules including liquid filled hard capsules (LFHC). LFHCs using either pH 6.8-7.2-triggered coatings or a combination of high pH-triggered and enzymatic-triggered coatings are typically used for effective colonic delivery.
Capsugel utilizes a range of lab-scale through commercial-scale equipment to produce finished dosage forms based on its targeted delivery technologies.