Il 178249 to Astellas Pharma Inc is a patent application titled “PHARMACEUTICAL COMPOSITION FOR USE IN SOLID FORMULATION CRYSTALLINE SOLIFENACIN OR SALT THEREOF AND A PROCESS FOR ITS PREPARATION”. On allowance, back in 2012, it was opposed.
Following the Statement of Claims, Astellas requested various claim amendments, some of which were allowed and some were opposed. The Applicant requested a further amendment and the Opposer did not object, so the amended claims published for Opposition purposes.
This amended claims set (version 5) is now subject to a judicial decision under Section 34. Based on her analysis, the Deputy Commissioner, Ms Jacqueline Bracha considers the claimed invention as lacking novelty and inventive step, and therefore provisionally refuses it under Sections 4 and 5 of the Israel Patent Law 1967. The Applicant has 30 days to appeal this decision.
The claimed invention is a pharmaceutical preparation that includes solid formulation crystalline solifenacin or a salt thereof in a concentration of up to 77% as measured by NMR. The relevant date is the filing date of the priority document which is 25 March 2004.
The specification itself states that this preparation was known, as was its crystalline state and its method of manufacture, and its effectiveness in treating urinary diseases. The amorphous state was present in tablets on sale prior to the priority date, and the Applicant is requested to answer whether this amorphous phase is indeed inherently present and if so,how and why it affects the novelty of the invention as claimed.
The Applicant claims that the percentage amorphous material in the tablet affects the efficacy and moisture during manufacture affects the amount of amorphous material in the pills. PEG is used as a binder but this is not claimed and so is not part of the claimed preparation. Apendix IX of the Statement of Opposition shows that exposure of pharmaceuticals to moisture degrades them, and this occurs more in amorphous regions. as stated in reference:
“What we can conclude from this analysis is that medium effects due to residual water in the amorphous state can be significant, but that the direction and extent of this effect will depend on the nature (e.g., polarity, specific solvation) of the transition state for the particular reaction causing degradation.”
Reference 10 states that wet granulation affects the degradation rate.
From the above, it is clear that persons of the art would expect the amount of amorphous active material to affect the rate of degradation, the extent of degradation over time and to reduce degradation one should protect from moisture. Consequently the claimed invention is obvious.
The Statement of Opposition shows that the pill was on sale before the priority date.
The Application is therefore provisionally refused, and the Applicant has 30 days to respond.