Controlled Release


Developing long-acting oral medications for poorly soluble drugs is particularly challenging. The formulation design has to take into account the transit time in the gastrointestinal tract, the pH of the stomach and intestine (both with and without food), salinity and interaction with bile salts, and many other considerations. Ascendia has expertise developing matrix tablets, coated particles, nano particles or molecularly dispersed systems that can overcome these challenges. Our dosage forms solubilize the drug in small particles that when disseminated in the GI tract allow the drug to dissolve more readily. The particles contain coatings that are time and pH sensitive so that a controlled release effect is simultaneously achieved as the particles transit the GI tract.

Controlled release of an oral dosage form is achieved by using either a membrane-diffusion mechanism (where the drug release is controlled by applying an insoluble coating to pellets or tablets), or by a matrix-erosion mechanism (where drug release from pellets or tablets is controlled by the erosion of slow dissolving and high molecular weight polymers). Solubilization agents and/or lipophilic excipients are combined with the drug to increase its solubility as needed. Ascendia uses fluid-bed coating techniques to prepare controlled release beads for encapsulation, and granulation techniques to prepare compression blends for tableting.

A typical project begins with modeling and simulation to obtain the target product release profile, followed by development of analytical methods and a formulation composition. Prototype formulations are tested in-vitro to ascertain their performance under different simulated gastrointestinal conditions. Once a lead formulation is selected, Ascendia conducts stability studies, and manufactures materials for an animal or human PK study under GLP and GMP environments. If necessary, formulation optimization and iteration may be conducted before the formulation is progressed to a human trial.

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