Entwicklung und Charakterisierung von gefriergetrockneten Tabletten mittels Lyoc® Technologie

Abstract

The goal of this dissertation was to characterize and optimize the formulation of lyophilized Orally Disintegrating Tablets (ODTs), by using more specifically the patented Lyoc® technology.

ODTs have several advantages in comparison to conventional tablets, since they allow the patient to have a convenient administration (no need of water, discreet treatment, does not leave any residue in the mouth after administration). This dosage form is thus adapted for patients who have swallowing difficulties (such as pediatric use, geriatric use, and patients suffering from dysphagia), and has a great area of interest for the psychiatric use.

A Lyoc® formulation is based on a suspension system containing mainly a diluent, a binder, Active Pharmaceutical Ingredient (API) and water.

In the frame of the formulation development, a Design of Experiment study was performed on a Mannitol / Dextran / Water formulation and revealed that even if the studied systems were quite complex due to the broad ranges of IPCs and the high variability possibility of each compound, an optimum could still be successfully determined.

The API solubility also has an influence on the Lyocs® not only on the macroscopic but also on the microscopic structure of the Lyocs®. Using X-Ray and DSC Analysis, it could be stated that water-soluble APIs tended to get partially amorphous after lyophilization, leading to a structure loss. On the contrary, less water-soluble APIs stays crystalline after lyophilization, which imparts elegance to the Lyoc® structure.