Mesh for dissolution test

Inventors

Horiuchi, Kensuke • MATSUURA, Satoyo • OKABE, MAKI

Assignees

Shionogi and Co Ltd

Abstract

When the mesh is placed under the bottom of a blade and over the bottom of a vessel in the dissolution test assembly equipped with either a vessel specified in the dissolution test method of the Japanese Pharmacopoeia, the United States Pharmacopoeia or the European Pharmacopoeia or a vessel used for the dissolution test, and a paddle formed from a blade and a shaft, and the suspensions and the solid dosage forms are added to or placed at the said mesh, a drug dissolves from the said dosage forms and the dissolution ratio variation between the said multiple same dosage forms can be small.

Core Innovation

A dissolution-test mesh is positioned under a paddle blade and above the bottom of a vessel in a dissolution test assembly, such that coning of a suspension or a solid dosage form is prevented. The method uses one single-layer mesh for the test, and the suspension or the solid dosage form is placed on the one single-layer mesh. This arrangement is applied in a dissolution test assembly comprising the vessel used in the dissolution test and a paddle comprising the blade and a shaft.

The paddle has a rotating speed of 10 to 30 rpm, and the mesh placement is defined relative to the paddle blade and the bottom of the vessel. The described mesh is positioned 5 to 35 mm under the blade and 1 to 30 mm above the vessel bottom. The mesh geometry is circular, with a diameter of 10 to 95 mm and a sieve opening of 2 to 200 mesh, and structural features such as an edge part and legs/step are described for the dissolution-test mesh.

Dissolution-test assemblies are described using vessels that comply with Japanese Pharmacopoeia, United States Pharmacopoeia, or European Pharmacopoeia, together with blade and shaft paddles. Experimental results reported for drugs such as Lipitor, Baxocapsule, Celecox, and Tegretol indicate improved dissolution behavior and suppression of coning. The reported dissolution ratio variation at low paddle speeds is reduced, and dissolution-test data based on the mesh approach is used to obtain PK simulation matching improvement in GastroPlus PK simulation software.

Claims Coverage

The independent claim specifies a coning-preventing dissolution test method using one single-layer mesh placed between the paddle blade and the vessel bottom, with the suspension or solid dosage form positioned on the mesh. Across the dependent claims, multiple inventive features refine the mesh placement distances, mesh geometry, sieve opening range, and mesh structural configuration, while the paddle rotating speed range remains a core element.

The claim coverage centers on preventing coning in dissolution tests by using a single-layer mesh placed under the paddle blade and above the vessel bottom, with the suspension or solid dosage form resting on the mesh, under a paddle rotating speed of 10 to 30 rpm. Dependent claims further constrain mesh placement distances relative to the blade and vessel bottom, define circular mesh diameter, define a sieve opening range, and add mesh structural features such as an edge part.

Stated Advantages

Documented Applications