Pharmaceutical composition for delaying senescence of lens cells and application of pharmaceutical composition

By preparing eye drops with cycloastragaloyl-3-acetate as the active ingredient, the problem of low solubility of cycloastragaloyl in water was solved, achieving the preparation of clear and stable eye drops, improving bioavailability and user experience, and ensuring the efficacy and safety of the drug.

CN121534064APending Publication Date: 2026-02-17SHENZHEN RUIYU BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202511674880.5
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-11-14
Publication Date
2026-02-17

AI Technical Summary

Technical Problem

Cycloastragalool has extremely low solubility in water, making it difficult to produce clear and stable aqueous eye drops using conventional techniques. Direct suspension in water results in an uneven, easily precipitated suspension with low bioavailability and a tendency to clog the outlet of ophthalmic preparations, leading to a poor user experience and potential safety hazards.

Method used

Using cycloastragaloyl-3-acetate as the active ingredient, combined with solubilizers, cosolvents, osmotic pressure regulators, buffer salts, and preservatives, eye drops are prepared. The process includes esterification and silica gel column chromatography purification to form a clear and stable pharmaceutical composition.

Benefits of technology

It improves the lipid solubility and cell membrane permeability of cycloastragalool, enhances bioavailability, ensures that the drug can effectively reach the target site, exhibits stronger biological activity potential, and guarantees the product's quality reliability and efficacy consistency.

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Abstract

The invention relates to the technical field of drugs for delaying senescence of lens cells, and particularly discloses a pharmaceutical composition for delaying senescence of lens cells and application thereof, the pharmaceutical composition comprises 0.05-0.1 wt% of cycloastragenol ester derivatives, 0.1-5 wt% of a solubilizer, 1.0-10.0 wt% of a cosolvent, 0.5-2.0 wt% of an osmotic pressure regulator, 0.01-0.5 wt% of a buffer salt, 0.001-0.05 wt% of a preservative, and the balance of water for injection; wherein the cycloastragenol ester derivative is cycloastragenol-3-acetate, and the structural formula of the cycloastragenol ester derivative is shown in Cycloastragenol-3-acetate is applied to delaying senescence of lens cells, compared with a parent compound cycloastragenol, the esterified derivative has significantly enhanced fat solubility and cell membrane permeability, and under the same concentration, the ability of activating the telomerase activity of lens epithelial cells is significantly superior to that of cycloastragenol; stronger biological activity potential is shown.
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