Ursolic acid preparations and uses thereof

Inventors

GERK, Phillip

Assignees

Virginia Commonwealth University

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Publication Number

US-12643922-B2

Patent

Publication Date

2026-06-02

Expiration Date


Abstract

Ursolic acid (UA) preparations and a self-nanoemulsifying drug delivery system (SNEDDS) composition containing at least one UA preparation selected from monopotassium ursolate (UAK), dipotassium ursolate (UAK2), monocholine ursolate (UAmC), dicholine ursolate (UAdC), pharmacological salts thereof, and mixtures thereof are provided. Methods for synthesizing UA preparations and delivering UA preparations to subjects in need thereof are also provided.

Core Innovation

The invention describes ursolic acid preparations comprising dipotassium ursolate (UAK2), ursolic acid dicholine complex (UAdC-O), and ursolic acid dicholine hydroxide hydrated complex (UAdC-W), together with self-nanoemulsifying drug delivery system (SNEDDS) compositions containing at least one such preparation and at least two emulsifying agents. UAdC-W is described as a hydrated complex containing 2–10 associated water molecules.

The described preparations and SNEDDS formulations are intended to improve ursolic acid solubility and oral bioavailability. The partial content reports increased aqueous solubility for UAdC-O and UAdC-W, and describes UAdC-W as stable. The background section is not included in the supplied partial content, so the problem identified in that section is not explicitly described in patent.

Claims Coverage

The independent claims cover five inventive features across three ursolic acid preparations, a SNEDDS composition, and a method for synthesizing UAdC-W.

Dipotassium ursolate

An ursolic acid salt identified as dipotassium ursolate (UAK2).

Ursolic acid dicholine complex

An ursolic acid complex identified as ursolic acid dicholine complex (UAdC-O).

Ursolic acid dicholine hydroxide hydrated complex

An ursolic acid dicholine hydroxide hydrated complex (UAdC-W) containing between 2 and 10 complexed water molecules.

Self-nanoemulsifying drug delivery system composition

A composition comprising at least one ursolic acid preparation selected from UAK2, UAdC-O, UAdC-W, pharmacological salts thereof, complexes thereof, and mixtures thereof, and at least two emulsifying agents.

Synthesis of UAdC-W

A method directed to synthesizing and isolating UAdC-W; [procedural detail omitted for safety].

The independent claims cover the specified ursolic acid salt and complexes, a SNEDDS composition incorporating specified ursolic acid preparations and emulsifying agents, and a method for synthesizing UAdC-W.

Stated Advantages

UAdC-O is reported to have water solubility of 18.2 mg/g, about 33.7-fold above monocholine ursolate.

UAdC-W is reported as stable and about sixfold more water-soluble than UAdC-O.

The SNEDDS formulations are intended to improve ursolic acid solubility and oral bioavailability; a dependent claim describes oral administration to increase bioavailability of a ursolic acid preparation.

Documented Applications

SNEDDS compositions containing specified ursolic acid preparations and emulsifying agents, including for oral administration to increase bioavailability of a ursolic acid preparation.

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