Ex Parte Seth

Board of Patent Appeals and Interferences

Sep 27, 2006

09583228 (B.P.A.I. Sep. 27, 2006)

The opinion in support of the decision being entered today was not written
for publication and is not binding precedent of the Board.

UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
__________

Ex parte PAWAN SETH

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Appeal No. 2006-0139
Application No. 09/583,228
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ON BRIEF
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Before SCHEINER, MILLS, and GRIMES, Administrative Patent Judges.

MILLS, Administrative Patent Judge.

DECISION ON APPEAL
This is a decision on appeal under 35 U.S.C. § 134 from the examiner's final
rejection of claims 1-4, 6, 9-14, 19-22 and 24-50.
Claims 1 and 26 read as follows:
1. A tablet composition free of food effect comprising:
a) a core comprising from 20 to 80% by weight of verapamil and from 10 to 80%
by weight of a gelling agent; and
b) a coating comprising, based on the weight of the coating, from 30 to 80% of a
gastroresistant polymer, and from 10 to 40% of a hydrophilic silicon dioxide, wherein the
gastroresistant polymer will dissolve in the intestines while withstanding the acidic
medium of the stomach and duodenum, and as the gastroresistant polymer dissolves,
verapamil is released in the intestines without the influence of food intake.

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26. A tablet composition free of food effect comprising:
a) a core comprising from 20 to 80% by weight of verapamil and from 10 to 80%
by weight of a gelling agent;
b) an intermediate coating; and
c) a coating comprising, based on the weight of the coating, from 30 to 80% of a
gastroresistant polymer, and from 10 to 40% of a hydrophilic silicon dioxide, wherein the
gastroresistant polymer will dissolve in the intestines while withstanding the acidic
medium of the stomach and duodenum, and as the gastroresistant polymer dissolves,
verapamil is released in the intestines without the influence of food intake.

The prior art references cited by the examiner are:

Morella et al. (Morella) 5,378,474 Jan. 3, 1995

Grounds of Rejection
Claims 1-4, 6, 9-14, 19-22 and 24-50 stand rejected under 35 U.S.C. § 103(a)
over Morella.
We affirm this rejection.

Claim Grouping
Appellant argues claims 26-50 separately from the other rejected claims.
Therefore, we select claims 1 and 26 as representative of the rejected claims. 37
C.F.R. ' 41.37(c)(1)(vii) (September 13, 2004).
DISCUSSION

Obviousness
Claims 1-4, 6, 9-14, 19-22 and 24-50 stand rejected under 35 U.S.C. § 103(a)
over Morella.
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In rejecting claims under 35 U.S.C. § 103, the examiner bears the initial burden
of presenting a prima facie case of obviousness. See In re Rijckaert, 9 F.3d 1531,
1532, 28 USPQ2d 1955, 1956 (Fed. Cir. 1993). A prima facie case of obviousness is
established when the teachings from the prior art itself would appear to have suggested
the claimed subject matter to a person of ordinary skill in the art. In re Bell, 991 F.2d
781, 783, 26 USPQ2d 1529, 1531 (Fed. Cir. 1993). An obviousness analysis requires
that the prior art both suggest the claimed subject matter and reveal a reasonable
expectation of success to one reasonably skilled in the art. In re Vaeck, 947 F.2d 488,
493, 20 USPQ2d 1438, 1442 (Fed. Cir. 1991). With this as background, we analyze
the prior art applied by the examiner in the rejection of the claims on appeal.
According to the examiner (Answer, pages 3-4)
Morella et al. … teaches a sustained release pharmaceutical composition
having a core element containing an antihypertensive agent such as
Verapamil Hydrochloride, binding agent, such as PVD, modified
celluloses, and other well known pharmaceutical carrier and excipients; a
coating comprising a methacrylic polymer (1-30% wt., soluble at a pH from
6-7.5 in the intestines), hydroxypropyl methylcellulose (4-20% wt.),
polyethylene glycol (15-35% wt.) and a filler such as silicon dioxide (4-30%
wt.), see, particularly, claims 1, 2, 7 and 9 as well as Col. 4, line 24.
column 11, lines 3-33. Morella … also teaches that the active ingredient
in the pharmaceutical composition reaches its maximum concentration
between about 4 and about 30 hours, col. 24, claim 1 and that the
bioavailability of the active agents in the pharmaceutical pellet is not
compromised by food, col. 7, lines 34-40. Morella discloses at least one
polymer which is substantially insoluble at acidic pH (i.e., that of the
stomach) but at least partially soluble at a less acidic to basic pH (i.e., the
pH of the intestine), see col. 6, lines 43-52[,] col. 7[,] lines 34-62 in
particular.
Morella … does not teach the particular composition containing the
specific ingredients in the amounts herein.

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The examiner concludes (Answer, page 4)

It would have been obvious to one of ordinary skill in the art at the
time the invention was made to make the particular composition
containing the specific ingredients herein in amounts herein.
One of ordinary skill in the art would have been motivated to make
the composition [c]laimed herein since a substantially similar composition
is taught in the prior art.

We find the examiner has provided sufficient evidence to support a prima facie
case of obviousness. In particular, with respect to claim 1, Morella describes a core
element which contains a drug and further includes a filler of as much as 10% by weight
of hydroxypropylmethyl cellulose1 or polyvinylpyrollidone. Morella, column 11, lines
24-50. Morella further describes a coating layer including an enteric polymer such as a
methacrylic acid copolymer or "a cellulose" (column 9, lines 17-31) and 0-75% of a filler
such as silicon dioxide (column 10, lines 4-9). The pharmaceutical pellet of Morella
may be in tableted form. Column 13, lines 32-34.
We further note that appellant's claims are broad and are not limited to a specific
dissolution profile. Morella discloses that the desired dissolution profile of the drug can
be selected by adjusting the amounts of ingredients in the coating layers. Morella
discloses (Column 8, line 63 to column 9, line 1) that "[t]he rate of dissolution at highly
acidic pH of the hybrid core coating will depend on the amount of the at least one

1 Specification, page 3, lists hydroxypropylmethylcellulose as a gelling agent.
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partially acid soluble component, the pH dependent and pH independent polymers, and
the thickness of the coating." "Once a minimum amount of the at least partially acid
soluble component, and/or the maximum thickness of the coating to achieve the
minimum dissolution profile at an highly acidic pH has been established, then it is simply
a matter of design choice to adjust the composition and /or thickness of the coating as
desired." Column 9, lines 5-10. In addition, Morella further describes that, "[i]t has been
found that the dissolution rate of the soluble drug at various pH's can be modified at will
by altering the ratio of polymers." Column 9, lines 11-14. Therefore, we agree with the
examiner that it would have been obvious to one of ordinary skill in the art to adjust the
thickness and amounts of the coatings described in Morella to achieve a desired
dissolution profile.
Moreover, with respect to claim 26, Morella particularly describes a hybrid
coating having more than one layer, such as a layer soluble at less acidic pH and a
layer soluble at acidic pH. Column 8, lines 34-67. Thus, Morella evidences that it is
within the skill of one of ordinary skill in the art to adjust the drug dissolution rate based
upon the coating thickness and amounts of coating ingredients, and adjust the location
of drug dissolution, either the stomach or intestine, based on the pH of the tablet
coating.

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Where the prior art, as here, gives reason or motivation to make the claimed
invention, the burden then falls on an appellant to rebut that prima facie case. Such
rebuttal or argument can consist of any other argument or presentation of evidence that
is pertinent. In re Dillon, 919 F.2d 688, 692-93, 16 USPQ2d 1897, 1901 (Fed. Cir.
1990) (en banc).
In response to the examiner's prima facie case of obviousness, appellant
contends that Morella describes additional components in the core coating and that,
"[t]here is no suggestion nor any motivation to modify this composition and eliminate the
other two components." Brief, page 10. However, in the present case appellant's
claims do not limit coating components to those recited in the claim due to the open
ended language "comprising", as would be the case if the claimed components were
limited by the use of a transitional phrase such as "consisting of" or possibly, "consisting
essentially of." Thus appellant's claim 1, as interpreted in accordance with claim
interpretation precedent, reads on the prior art coated tablets disclosed in Morella.
Appellant additionally argues that, "the claims recite that the coating includes
from 30 to 80% of a gastroresistant polymer soluble at a pH above 5.5. On the other
hand, Morella teaches an analogous component at a level of 1-30%, preferably 2-20%."
Brief, page 11. We are not persuaded by this argument. Appellant mischaracterizes
the teachings of Morella. In particular, Morella teaches "[t]he at least one enteric
polymer may be present in the coating in an amount of from approximately 1 to 60% by
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weight…" and thus is not limited to the preferred embodiment of 1-30% as argued by
appellant. Column 9, line 27-30.
As evidence of non-obviousness, appellant also proffers the Declaration of Dr.
Seth. The Declaration compares the dissolution profile of a selected tablet and coating
of the claimed invention with the tablet and coating of selected example 3 of Morella.
The Declarant argues at numbered paragraph 9 of the Declaration, that the evidence
shows that, the "compositions of Morella and of the invention are different and will
exhibit different behaviour in the gastrointestinal (GI) tract," and the "coated formulation
of the invention has different profiles at different pH." Id., at paragraph 10.
We do not find appellant's Declaration evidence to be convincing or to overcome
the rejection before us. To begin, appellant's Declaration compares the tablet and
coating of Morella example 3, an example in which the components were selected to
"illustrate a prolongation of release" of the active agent. Col. 16, line 8-12. Example 3,
Table 5 of Morella shows that at pH 7.5, at 180 minutes, 28.12 mg of drug was
released. However, the teachings of Morella are not limited solely to those of example
3. For example, if appellant had compared the dissolution profile of the claimed tablet
with that of Morella example 1 (Table 2, pH 7.5, at 180 minutes) a faster release rate of
35.39 mg of drug would have been found. Similarly, example 2 (Table 4, pH 7.5 at 180
and 240 minutes) shows a much greater release of 33.66 mg of drug and 42.7 mg of
drug, respectively.
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As the other embodiments of Morella also reflect relevant prior art teachings, we
agree with the examiner that the Declaration is not sufficiently comparative with either
the full breadth of the teachings of Morella, or indicative of the full scope of the pending
claims. We find the Board's determination in Ex parte Winters2 to be instructive here.
In Winters we stated:
... appellant is not required to test each and every species within
the scope of the appealed claims and compare same with the closest prior
art species. Rather patentability is established by a showing of
unexpected superiority for representative compounds within the scope of
the appealed claims. What is representative is a factual question which is
decided on a case-by-case basis.

11 USPQ2d at 1388. We do not find appellant has provided a sufficient showing of
nonobviousness or unexpected results, commensurate with the pending claim scope.
In addition, appellant is reminded that when relying on comparative testing, the
most effective comparison is between the claimed invention and the closest prior art.
See, In re Burckel, 592 F.2d 1175, 201 USPQ 67 (CCPA 1979); In re Merchant, 575
F.2d 865, 197 USPQ 785 (CCPA 1978); Ex parte Beck, 9 USPQ2d 2000, 2002 (Bd.
Pat. App. & Int. 1987) (Acomparative evidence, to be effective, must compare the
claimed subject matter with the closest prior art''); Ex parte Meyer, 6 USPQ2d 1966,
1968 (Bd. Pat. App. & Int. 1988) (AAn applicant relying upon a comparative showing to
rebut a prima facie case of obviousness must compare his claimed invention with the

2 Ex parte Winters, 11 USPQ2d 1387 (Bd Pat App Int 1989).

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closest prior art.''). For the reasons indicated above, we do not find the results put forth
in the Declaration of Seth to be comparative.
Furthermore, Morella discloses that the dissolution profile of a drug is a result
effective variable dependent upon the coating thickness and amounts of ingredients in
the coating composition. In In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA
1955), a predecessor of our appellate reviewing court set out the rule that the discovery
of an optimum value of a variable in a known process is normally obvious. See also, In
re Boesch, 617 F.2d 272, 276, 205 USPQ 215, 219 (CCPA 1980). Our reviewing court
has found an exception to this general rule where Athe parameter optimized was not
recognized to be a result effective variable,@ In re Antonie, 559 F.2d 618, 621, 195
USPQ 6, 8 (CCPA 1977). Exceptions to this rule have also been found in cases where
the results of optimizing a variable, which was known to be result effective, were
unexpectedly good. In re Waymouth, 499 F.2d 1273, 1276, 182 USPQ 290, 293 (CCPA
1974). However, neither of these exceptions to the art recognized principles of
optimization and result effective variables are found in the present case.
In our view, for the reasons indicated herein, we agree that the examiner has
presented a prima facie case of obviousness which has not been convincingly rebutted
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by appellant. In view of the above, the rejection of the claims for obviousness in view of
Morella is affirmed.
CONCLUSION
The rejection of claims 1-4, 6, 9-14, 19-22 and 24-50 under 35 U.S.C. § 103(a)
over Morella is affirmed.
No time period for taking any subsequent action in connection with this appeal
may be extended under 37 CFR ' 1.136(a).

AFFIRMED

)
Toni R. Scheiner )
Administrative Patent Judge )
)
)
) BOARD OF PATENT
Demetra J. Mills )
Administrative Patent Judge ) APPEALS AND
)
) INTERFERENCES
)
Eric Grimes )
Administrative Patent Judge )

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