College of Pharmacy
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HelixTalk Episode #138 - Hidden Pharmaceutics: The Fascinating Science Behind Dosage Formulations
Date posted: October 26, 2021, 6:00 am
In this episode, we discuss the fascinating science of pharmaceutics with Dr. Kristen Ahlschwede and Dr. Rahul Deshmukh. We explore how dosage forms and excipients play an important role in how a drug product behaves in the human body with a particular focus on fentanyl patches, osmotic tablets (with laser-drilled holes), Depakote Sprinkles, and IV amiodarone.
- Fentanyl patches were reformulated from a drug-in-a-reservoir system to an adhesive matrix system to prevent abuse and misuse. The new formulation prevents fentanyl from "leaking" out when cut.
- Osmotic tablet systems, such as Procardia XL, Glucotrol XL, and Concerta, use an "active" layer (containing drug) adjacent to a "push" layer that is osmotically active. When the push layer is exposed to water in the GI tract, it swells and pushes the active layer through a small laser-drilled precision hole.
- "Sprinkle" dosage forms typically involve small pellets inside a capsule, such as Depakote Sprinkles. The capsule itself does not delay or extend release; instead, the pellets themselves are involved in prolonging the absorption profile of the drug.
- Amiodarone IV is commercially available in two formulations -- the conventional formulation (Cordarone) contains benzyl alcohol and tween 80 to solubilize the drug but these excipients are associated with hypotension. A newer formulation (Nexterone) uses cyclodextrin as a solubilizing agent and is not associated with hypotension (although has a risk of nephrotoxicity, especially at higher cumulative doses).