QbD-Based Formulation Development of Amiodarone Hydrochloride Tablet

基于质量源于设计(QbD)的盐酸胺碘酮片剂制剂开发

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Abstract

Background/Objectives: We conducted this study to develop a generic amiodarone tablet pharmaceutically equivalent to the reference drug. This development is crucial for securing a stable supply chain for this orphan drug, which currently faces domestic market instability. Amiodarone, a national essential medicine, often experiences unstable supply due to its limited profitability. Methods: To secure this stable supply chain, we employed a factorial design, utilizing a Quality by Design (QbD) approach, to create the most suitable formulation. Initially, we observed a limitation where the formulation exhibited a flowability of 25% based on the Carr's Index, which exceeded the target of 20%. To address this challenge, we incorporated lactose monohydrate during the pre-mixing stage rather than the post-mixing stage. Subsequently, we identified the binder content and the amount of granulation solvent as Critical Material Attributes (CMAs), and we performed a Design of Experiments (DoE). Result: Based on these investigations, we determined that the optimal prescription utilizes 5.71% povidone K25 and 40 mg/T of purified water. The final formulation successfully achieved an excellent flowability of 15.8%. Furthermore, this formulation showed a dissolution and bioequivalence PK profile equivalent to the reference drug in pH 1.2, 4.0, and 6.8 buffer solutions, each containing 1% Tween 80. Conclusions: Ultimately, the developed formulation is anticipated to establish a stable domestic supply chain and concurrently reduce national healthcare costs. These research findings also establish the groundwork for future continuous manufacturing implementation.

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