1. Patent Claim (Patent No. 3563036)
“A pharmaceutical composition comprising one or more orally deliverable dose units, each comprising particulate celecoxib in an amount of about 10 mg to about 1000 mg …having a distribution of celecoxib particle sizes such that D90 of the particles is less than 200µm, in the longest dimension of said particles.”
2. An excerpt from the Judgment
It can be said that…descriptions [in the specification]…indicate that bioavailability of celecoxib is improved when unformulated celecoxib was milled and “the D90 particle size of the celecoxib” was “less than about 200µm”, and that impact milling such as pin milling of the celecoxib provides improved blend uniformity to the final composition relative to other types of milling. However, in Exhibit A-1, there is no description indicating methods for preparation of “celecoxib” in an invention of Exhibit A-1, “oral capsules containing 300 mg of celecoxib”, and there is neither description nor suggestion for using celecoxib that is micronized through a mill, or for setting a condition for micronizing celecoxib by “the D90 particle size of the celecoxib”…
…[I]n Exhibits A-9 and A-10, there is no description or suggestion that in the case of powder which produces an effect with a smaller particle size than the specified size, it is common for raw powder for medicinal products to identify a particle size distribution “by a percentage of powder having a smaller size than a desired size in the entire powder”, but not by an average particle diameter, and moreover, there is no description or suggestion for setting a condition for micronizing celecoxib by “the D90 particle size of the celecoxib”, nor description or suggestion that bioavailability of celecoxib is improved when “the D90 particle size of the celecoxib’ was ‘less than about 200µm”. In addition, there is no sufficient evidence to find that in the case of powder which produces an effect with a smaller particle size than the specified size, it is common for raw powder for medicinal products to identify a particle size distribution “by a percentage of powder having a smaller size than a desired size to the whole powder”, but not by average particle diameter. Then, even if a person skilled in the art who came in contact with Exhibit A-1 would conceive an idea of reducing the particle size of celecoxib contained as a medicinal ingredient in the invention of Exhibit A-1, oral capsules containing 300 mg of celecoxib, to improve the oral absorbability (bioavailability) and the uniformity of the content of medicinal ingredient, it cannot be acknowledged that there is motivation for the person skilled in the art to adopt, as a condition for micronization of celecoxib, a composition…“having a distribution of celecoxib particle sizes such that D90 of the particles is less than 200µm, in the longest dimension of said particles”.
3. Consideration of this case (Case No. 2019 [Gyo-ke] 10137)
In recent relevant cases, the court generally judged an inventive step of an invention by adopting a framework under which a parameter or a numerical value range is regarded as the matters used to specify the invention, and whether a person skilled in the art would easily arrive at the parameter or the numerical value range is questioned, and when the person skilled in the art would not easily arrive at the same, the invention is considered as having an inventive step.
In this case, the Court questioned whether a person skilled in the art would easily conceive a parameter or a numerical value, that is, “celecoxib particle sizes such that D90 of the particles is less than 200µm”, then denied that the invention could be easily conceived, and found, without entering into discussion on remarkable effect and the like, that the invention has an inventive step.
Writer: Hideki TAKAISHI
Supervising editor: Kazuhiko YOSHIDA
Contact information for inquiries: h_takaishi@nakapat.gr.jp
Hideki TAKAISHI
Attorney at Law & Patent Attorney
Nakamura & Partners
Room No. 616, Shin-Tokyo Building,
3-3-1 Marunouchi, Chiyoda-ku
Tokyo 100-8355, JAPAN