Appeal No. 2002-0783 Page 5
Application No. 09/268,957
Rashidy,
the apomorphine dose required to achieve a significant erectile response
is usually accompanied by nausea or other serious undesirable side
effects such as hypertension, flushing and diaphoresis. [El-Rashidy,
Background of the Invention, column 2, lines 24-27]
and
The present invention provides compositions that release water-
soluble drugs relatively slowly over an extended time period. The
composition is suitable for dosage forms that deliver drugs by the
sublingual or buccal routes. In the practice of this invention with its
application to the pharmacological agent, apomorphine, a sublingual
tablet formulation that includes particular constituents permits the drug to
achieve its effective therapeutic plasma concentration which is below a
plasma concentration where undesirable side effects such as nausea and
vomiting occur. In addition to this major improvement arising from the
present invention, the added benefit of drug release over a longer period
of time from the tablet can increase the duration of the therapeutic activity
for the drug.
The composition, in the form of a tablet, delivers the
pharmacological agent, such as apomorphine, at a controlled rate to
produce the desired physiological effect of the drug while preventing or
diminishing the side effects such as hypotension, nausea and vomiting
that have been associated with apomorphine. Such a composition thus
provides the therapeutic benefits of apomorphine, as for example, in the
treatment of Male Erectile Dysfunction . . . with minimal side effects.
[El-Rashidy, Summary of the Invention, column 3, lines 17-40].
We agree with the examiner that it would have been well within the skill of the art
and obvious to a person having ordinary skill to apply the teachings of El-Rashidy to the
active ingredient sildenafil. In his specification, page 6, lines 15 and 16, applicant
describes sildenafil as water soluble. Further, at the time the invention was made, the
oral use of the citrate salt of sildenafil had been approved by the U.S. Food and Drug
Administration (FDA) for treating male erectile dysfunction (specification, page 2, lines
30-33). In dose-response studies, increasing doses of sildenafil (25 to 100 mg)
Page: Previous 1 2 3 4 5 6 7 8 9 10 Next
Last modified: November 3, 2007