TOPICS

“Pharmaceutical Preparation”

 Overview:

A case where the IP High Court upheld the decision in a trial for patent invalidation, finding a lack of inventive step.

► Summary of Judgment and Link to Full Text (Japanese)

 Main Issue:

Whether containing a ripasudil aqueous composition in a container that blocks light in the 300 to 335 nm wavelength range involves an inventive step.

Corrected claim 1 (Corrected Invention 1)

1.   A pharmaceutical preparation comprising an aqueous composition comprising ripasudil, a salt thereof, or a solvate of ripasudil or a salt thereof, the aqueous composition being contained in a primary container,

              wherein the content of ripasudil, a salt thereof, or a solvate of ripasudil or a salt thereof in the aqueous composition is 0.05 to 5 w/v%, calculated as the free form, based on the total volume of the aqueous composition,

              wherein 50% or more of the total inner surface area of the primary container blocks light having a wavelength of 300 to 335 nm such that an average transmittance of the light is 10% or less, and

              wherein the average transmittance is determined by measuring a light transmittance of the container in air at 0.5 nm intervals within the wavelength range of 300 to 335 nm using a spectrophotometer, and then calculating an average of the measured values.

Difference 2

Corrected Invention 1 is a “pharmaceutical preparation” in which a composition “is contained in a primary container, wherein 50% or more of the total inner surface area of the primary container blocks light having a wavelength of 300 to 335 nm such that an average transmittance of the light is 10% or less, and wherein the average transmittance is determined by measuring a light transmittance of the container in air at 0.5 nm intervals within the wavelength range of 300 to 335 nm using a spectrophotometer, and then calculating an average of the measured values.” However, Invention 1 of Reference 2 does not specify any corresponding features.

Summary:

(2) Concerning Difference 2

i) Since ripasudil was a chemical substance intended for use as an ophthalmic solution as an anti-glaucoma drug (Reference 2), and since, in order to obtain regulatory approval for a formulation of an ophthalmic solution containing ripasudil as an active ingredient, it is necessary to repeatedly change the container and conduct stability tests until it can be demonstrated that the formulation is not affected by exposure to light (References 7 to 9), it is recognized that a person skilled in the art would have been motivated to select a container for an ophthalmic preparation that enables demonstration that ripasudil is not affected by exposure to light.

(3) Remarkable Effect

…the above effect that containing the preparation in a container capable of blocking, to some extent, light having a wavelength of 300 nm or more can suppress degradation caused by light compared with containing it in a transparent container is an effect that a person skilled in the art could have predicted, and merely confirms a property that would naturally become apparent through the photostability testing of the preparation that a person skilled in the art would inevitably conduct.

Comments:

The court held that an effect that merely reflects a property that would naturally be confirmed through tests (photostability tests) that are inevitably conducted to obtain approval to manufacture and market a pharmaceutical product, i.e., an effect that is “naturally revealed” under regulations of the Pharmaceuticals and Medical Devices Act, cannot serve as a basis for affirming inventive step as a “remarkable effect.”

Akiteru Tamura