Authors :
Lixin Gong, MS – Aucta Pharmaceuticals, Inc.
Anil Patel, MS – Aucta Pharmaceuticals, Inc.
Ha Nguyen, MS – Aucta Pharmaceuticals, Inc.
Gloria Macalintal, BA – Aucta Pharmaceuticals, Inc.
Presenting Author: Erika Torres, PharmD, MHS, RPh – Aucta Pharmaceuticals, Inc.
Rationale:
Lacosamide Extended-Release Capsules, MOTPOLY XR, was approved by FDA in May 2023 for oral use of anti-seizure treatment by taking whole capsules once daily with or without food. Lacosamide Extended-Release (ER) Capsules with a novel formulation contain Lacosamide Extended-Release (ER) beads. To assess the additional use of the approved labeling for patient populations who are unable to swallow the whole capsules, an alternate option of sprinkling the Lacosamide ER beads from one whole capsule onto the proposed soft food Applesauce, the in vitro study was performed according to FDA draft guidance on soft foods. Methods:
The compatibility and suitability of the proposed sprinkle vehicle, Applesauce, was evaluated by the assessment of critical quality attributes of Lacosamide ER beads, especially potency (Assay), dissolution and stability when the beads were sprinkled onto applesauce. Lacosamide ER Capsules, 200 mg, lot # 4530661 used in bioequivalence study and stored under controlled room-temperature condition for over 36 months, were used in the in vitro soft food study. Carefully opened the whole capsule, emptied and sprinkled the entire contents of capsule, Lacosamide ER beads, onto about 15 g (equivalent to approximate 15 mL) of applesauce. The validated stability indicating analytical method for Assay and validated Dissolution method were used for the testing at initial sprinkling mixture, and again two hours (2 Hrs) after incubating the ER beads with the applesauce under both room temperature (RT) and refrigerator (RF) conditions. Refer to Table 1 for Assay results that demonstrated no significant change in Assay from the original value and Dissolution results that compared with original dissolution results showing the similarity. Refer to Figure 1 for comparison of dissolution profiles. Size of Lacosamide ER beads was also evaluated to meet FDA requirements of beads size for sprinkle in drug product labelling to be proposed.Results:
Results: Table 1 Assay and Dissolution Results
Figure 1 Comparison of Dissolution Profiles
Conclusions:
The above in vitro soft food study demonstrated that applesauce is suitable for being used as sprinkle delivery vehicle for Lacosamide ER Capsules by opening the whole capsule and sprinkling the internal beads onto up to 15 mL of applesauce for immediate drug administration in addition to the approved labeling (Reference: FDA draft guidance, Use of Liquids and/or Soft Foods as Vehicles for Drug Administration, effective in July 2018). This alternative sprinkling oral administration option for Lacosamide ER capsules is very important for patients with swallowing difficulties as it supports medication adherence and overall treatment success.
Funding:
This study was funded by Aucta Pharmaceuticals, Inc.