Appeal No. 2001-2157 Page 7
Application No. 08/918,741
answer that question in the negative.
The examiner argues that there is reason, suggestion, or motivation stemming
from the prior art to prepare raloxifene in an amorphous form. According to the
examiner, a person having ordinary skill would have recognized that an amorphous
form of raloxifene would possess improved physical characteristics, e.g., increased
solubility, compared with its known crystalline form. It follows, according to the
examiner, that an amorphous form of raloxifene would possess improved bioavailability
compared with its crystalline form; and that this would have been recognized by a
person having ordinary skill in the art.
We shall not belabor the record on this point, because applicants concede that
the prior art provides adequate reason, suggestion, or motivation to prepare raloxifene
in an amorphous form. Applicants concede that
when the ordinarily skilled artisan is faced with a pharmaceutical that has
poor oral-bioavailability properties [crystalline raloxifene], one technique
for improving dissolution rates, and thus, hopefully, oral bioavailability, is
to administer an amorphous form of that pharmaceutical. Once it is
determined that an amorphous form is obtainable, Appellants have also
conceded that it is well know [sic] in the art that preparing that amorphous
form may be done by spray drying the material as taught, e.g., in
Takeuchi. [Paper No. 12, page 4, 3rd full paragraph]
In other words, applicants do not controvert the examiner's position that the cited prior
art suggests the desirability of preparing raloxifene in an amorphous form. Applicants
also acknowledge that spray drying is a conventional technique, known in the art for
preparing amorphous products.
Applicants do not concede, however, that spray-drying was known for preparing
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