Direct compression tablet formulation of trimetazidine through systematic screening of oxalate salts.

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Tác giả: Yuebin Ge, Xianju Huang, Yuan Ming, Changquan Calvin Sun, Chenguang Wang, Zhangyaoyu Yuan, Mingzhen Zhang

Ngôn ngữ: eng

Ký hiệu phân loại: 271.6 *Passionists and Redemptorists

Thông tin xuất bản: Netherlands : International journal of pharmaceutics , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 160669

Salt formation has been extensively used to modulate and improve the properties of active pharmaceutical ingredients (API), such as solubility, stability and mechanical properties. Tablets of the anti-angina drug, trimetazidine (TMZ) are currently manufactured using the wet granulation process, rather than the more cost-effective direct compression method. In an effort to address the two main challenges associated with the commercial dihydrochloride salt (TMZ-2HCl), i.e., poor flowability and high hygroscopicity, we have screened and prepared three new oxalate (Oxa) salts of TMZ, i.e., TMZ:Oxa 2:1 (hemi-salt), 1:1 (mono-salt), and 1:2 (di-salt). All of the three salts exhibited improved solid-state properties over TMZ-2HCl, including flow, tabletability, and stability against high humidity. Among the three salts, the TMZ-Oxa (1:2) di-salt demonstrates overall superior properties, establishing it as the most promising alternative crystal form. Consequently, using the di-salt, we developed a direct compression tablet formulation that shows potential for commercial manufacturing.
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