Example as a basis for modification

This decision concerns a modification of a claim relating to a tablet. The modification was based on features as disclosed in the specification in combination with a selection of ingredients disclosed in the examples without their amounts. The patent was revoked in opposition, as the omission of the relative amounts in the amended claim resulted in an unacceptable intermediate generalization. The patentee appealed, arguing that the examples are not limiting and that whether the amounts of the ingredients influenced the effect of the compositions was not an issue in the art judgment. . 123 (2) EPC. The chamber ruled in favor of the opposition division.

Claim 1 of the main request has been amended as follows:

1. Tablet or capsule comprising a pharmaceutical composition, wherein the pharmaceutical composition comprises up to 5 mg apixaban and a pharmaceutically acceptable diluent or carrier, wherein apixaban is in particulate and crystalline form and the individual apixaban particles, whether the particles exist alone or are agglomerated, have a D90 of 89 μ or lessm measured by laser light scattering, in which the composition consists of the following components:

(a) intragranular: apixaban, anhydrous lactose, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, sodium lauryl sulfate;

(b) extragranular: croscarmellose sodium, magnesium stearate; and

(c) film coating; and wherein the tablet is made using a dry granulation process.

Amended claim 1 was essentially based on the tablet compositions described in paragraph [0006] with a more precise definition of the specific components according to table 3.

Paragraph [0006] reports that tablet compositions prepared using a dry granulation process and comprising up to 5 mg Apixaban particles with an D90 less than 89 m have been shown to allow constant in vivo dissolution, constant exposure and constant inhibition of factor Xa. This report is followed by the statement that, therefore, the invention provides a pharmaceutical composition comprising crystalline apixaban particles of a size as measured by laser light scattering and an acceptable diluent or carrier.

The Commission observed that Table 3 only mentions one type of tablet, namely the “20 mg tablet”. The middle column of Table 3 refers to “5% w / w drug loaded granulation”. The Board also concluded that “100.00 mg” and “103.5 mg” are incompatible with the title of the middle column and that, given the format shown in Table 4, the ingredients actually add up to 100% and 103.5%. Therefore, one skilled in the art cannot directly and unambiguously derive a description of a 5 mg apixaban tablet from Table 3.

The Board also noted that the application as filed only reports trials on 20 mg apixaban tablets and makes no reference to experiments using 5 mg apixaban tablets.

The Board further noted that the compositions in Table 3 are presented in bioequivalence studies. As supported by the documents on the record and by para. [0008] of the application as filed, the excipients in Table 3 influence the dissolution rates of the drug. According to the Council:

This influence is relevant in the context of the assessment of modifications under Article 123 (2) EPC, since in view of the mentioned context of the disclosure of the compositions in Table 3, this influence indicates a functional relationship between the choice of components (…) and the quantities of these components (…). Regardless of the non-limiting purpose of the examples (…).

Thus, given the relevant relationship between the ingredients and their amounts listed in Table 3 as well as the fact that Table 3 does not illustrate a 5 mg tablet of apixaban, the Council affirmed that:

those skilled in the art would not infer directly and unambiguously from the application as initially filed that the disclosure in paragraph [0006] tablet compositions comprising up to 5 mg of apixaban should be associated with the characteristics of the tablet compositions of Table 3, not to mention the ingredients listed in the left column of Table 3 taken from their relative amounts.

Accordingly, the board concluded that the amendment in question did not comply with the requirement of Art. 123 (2) EPC.


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