High-surface-area lyophilized composition containing arsenic for oral administration to patients
The development of an oral lyophilized arsenic trioxide formulation addresses the limitations of intravenous administration by providing comparable bioavailability and convenience, enhancing solubility and stability for treating hematological malignancies.
JP7885288B2Active Publication Date: 2026-07-06ケツァール·セラピューティクス·リミテッド·ライアビリティ·カンパニー
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Patent Information
- Application Number
- JP2024135193
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Priority Date
- 2015-04-03
- Filing Date
- 2024-08-14
- Publication Date
- 2026-07-06
- Estimated Expiration
- 2036-02-01
AI Technical Summary
Technical Problem
Conventional arsenic treatments for hematological malignancies require daily intravenous administration, which is inconvenient, risky, and costly, and there is no FDA-approved oral formulation available.
Method used
A lyophilized composition containing arsenic trioxide is developed, which can be administered orally, enhancing bioavailability and solubility through a process involving solubilization and freeze-drying, and optionally incorporating fillers and lubricants.
Benefits of technology
The oral formulation provides systemic bioavailability comparable to intravenous administration, offers a convenient and less dangerous method, and maintains stability for over three months, with improved solubility and bioavailability.
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Abstract
To address the issues of the insolubility of As2O3 and the lack of bioavailability and provide a lyophilized composition comprising arsenic that makes it bioavailable, and further to provide methods for production thereof, and methods for treating malignancies such as tumor or cancer by orally administering the lyophilized composition comprising arsenic.SOLUTION: A method for preparing a lyophilized composition comprising arsenic (LCCA) comprises the steps for: (A) solubilizing As2O3 powder in an aqueous medium to form an As2O3 solution; and (B) lyophilizing the As2O3 solution.SELECTED DRAWING: None
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