Gossypol acetic acid suspension, its preparation method and application

By using a gossypol acetate suspension formulation, controlling particle size, and employing stabilizers and dispersants, the problems of low solubility and gastrointestinal irritation of gossypol acetate have been solved, achieving sustained release and high bioavailability for injection, and significantly improving the safety and efficacy of tumor treatment.

CN122097261APending Publication Date: 2026-05-29HANGZHOU INSTITUTE OF MEDICAL SCIENCES CHINESE ACADEMY OF SCIENCES

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HANGZHOU INSTITUTE OF MEDICAL SCIENCES CHINESE ACADEMY OF SCIENCES
Filing Date
2026-03-05
Publication Date
2026-05-29

AI Technical Summary

Technical Problem

Gossypol acetate has poor solubility in water, low bioavailability, and significant irritation to the gastrointestinal mucosa when taken orally, which limits its clinical application.

Method used

The formulation uses a gossypol acetate suspension, which overcomes solubility limitations through microparticle dispersion. Injection avoids the first-pass effect and mucosal irritation in the gastrointestinal tract. The particle size is controlled within 0.1~100μm. Stabilizers and dispersants are used to ensure formulation stability. It is suitable for subcutaneous/intramuscular injection.

Benefits of technology

It achieves stable and long-lasting sustained release of gossypol acetate, reduces the frequency of administration, improves bioavailability, enhances formulation stability, has a wide range of applicable populations, has a significant antitumor effect, and reduces the risk of toxic side effects.

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Abstract

The application discloses a gossypol acetic acid suspension, a preparation method and application thereof. The suspension takes gossypol acetic acid as an effective component, which is stably dispersed in a dispersion medium containing stabilizers, dispersants and other accessories in the form of microparticles. The preparation method comprises preparation of the dispersion medium, and dispersion of gossypol acetic acid in the medium by means of dry grinding, wet micronization, high shear or ultrasonic and the like. The application effectively solves the defects of low solubility in water, poor bioavailability and large gastrointestinal stimulation of gossypol acetic acid, and realizes smooth and long-acting release of the drug by forming a crystal drug library at an injection site through subcutaneous or intramuscular injection, reduces the frequency of drug administration of patients, and has excellent preparation stability, high drug loading rate and good biocompatibility. The suspension has a significant tumor inhibition effect in the treatment of various tumors, provides a safe, effective and convenient treatment option for tumor patients, and has good industrialization prospect and clinical application value.
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