(W1030-10-57) The Effect of Food Vehicle on In Vitro Performance of Mini-Tablets Formulation

Purpose: The aim of this study is to investigate the impact of different food vehicles on the in vitro performance of mini-tablets formulation. By systematically analyzing the leaching time of mini-tablets, the dissolution and release profiles of mini-tablets in various food vehicle, we aim to understand how different food matrices affect the dissolution, and drug release kinetics of the formulation. This research seeks to provide insights into optimizing mini-tablets formulation for enhanced bioavailability and therapeutic efficacy in diverse dietary conditions.

Methods: In this study, three commonly used food vehicles were selected for in vitro testing mini-tablets: Apple sauce, Yogurt and Banana Puree. Dissolution:Capsule (n=6) was opened and the mini-tablets was sprinkled on the food vehicles. The food vehicle-drug mixture was kept under room temperature for 0, 30, and 60 min before the whole food vehicle- drug mixture was placed in dissolution apparatus for in vitro dissolution testing. The dissolution parameter and condition are listed below: Apparatus: USP Apparatus II (Rotating Paddles). Dissolution Medium: 0.1M Potassium Phosphate, pH 4.0. Dissolution Medium Volume: 900 mL. Temperature: 37.0ºC ± 0.5ºC. Pull Volume: 5 mL. Flush volume: 3 mL. Sampling Times: 10, 15, 20, 30, 60, and 90 minutes. Assay: Capsule content was sprinkled on the 2 teaspoonfuls of food vehicles (Figure 1), mix mini-tablets with food vehicle and set aside for the specified exposure time at 30 and 60 min. At the end of the proposed time, separate mini-tablets from soft food using a spatula and test for the recovery of drug substance and calculate mass balance.

Results: Assay: The leaching study for assay test was performed on the three food vehicles using mini-tablets. The results of this study indicate that no significant leaching was observed in all three food types after total exposure time of 60 minutes except in apple sauce, in which 27.1% of Assay leaching was found. Dissolution: The dissolution testing of the drug release profile are not affected by 0 min, 30 min and 60 minutes of exposure in apple sauce and yogurt against control sample. Based on the results obtained from the dissolution testing of mini-tablets, by 0 min, 30 min and 60 min soaking in banana puree against control sample, %release was slow in the dissolution profile.

Conclusion: The coating materiel of the drug product contains EUDRAGIT^®E PO which is soluble below pH 5.0 and apple sauce has acidic pH around 3.5 that could be the reason to get more leaching in applesauce at 60 min. Additionally, mass balance data indicate that the desired therapeutic dose of mini-tablets would be delivered with soft food within 60 minutes of exposure time. drug release profiles are lower in banana puree and yogurt against control sample The lump was formed while dispensing banana puree with sample using syringe and mini-tablets stuck into that lump which takes time to disperse that lump and release of drug substance

Figure. 1 In-vitro dissolution studies of the mini-tablets with Apple Sauce


Figure. 2 In-vitro dissolution studies of the mini-tablets with Banana Puree


Figure. 3 In-vitro dissolution studies of the mini-tablets with Yogurt