Ex Parte Brzeczko et al

Patent Trial and Appeal Board

Jan 13, 2015

12019666 (P.T.A.B. Jan. 13, 2015)

UNITED STATES PATENT AND TRADEMARK OFFICE
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BEFORE THE PATENT TRIAL AND APPEAL BOARD
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Ex parte ALBERT W. BRZECZKO and JOHN A. DONEY
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Appeal 2012-007345
Application 12/019,666
Technology Center 1600
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Before DONALD E. ADAMS, JEFFREY N. FREDMAN, and
ROBERT A. POLLOCK, Administrative Patent Judges.

FREDMAN, Administrative Patent Judge.

DECISION ON APPEAL
This is an appeal1 under 35 U.S.C. § 134 involving claims to an
oxcarbazepine composition. The Examiner rejected the claims as
anticipated. We have jurisdiction under 35 U.S.C. § 6(b). We affirm.

1 Appellants identify the Real Party in Interest as ISP Investments
Inc. (see App. Br. 3).
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Statement of the Case
Background
“Oxcarbazepine is . . . an anticonvulsant and is currently marketed by
Novartis Pharmaceuticals under the branded name TRILEPTAL®” (Spec. 2
¶ 2).
The Claims
Claims 1–9 are on appeal. Independent claim 1 is representative and
reads as follows:
1. A composition comprising a solid solution wherein
the solid solution comprises oxcarbazepine and one or more
solubility-enhancing polymer(s) wherein said oxcarbazepine
is substantially amorphous and exhibits enhanced
bioavailability compared to a control composition without
the solubility-enhancing polymer.

The issue
The Examiner rejected claims 1–9 under 35 U.S.C. § 102(e) as
anticipated by Blau2 (Ans. 5–7).
The Examiner finds that “Blau teaches a pharmaceutical composition
comprising, a) spray granulated oxcarbazepine, and b) at least one
pharmaceutical excipient” (Ans. 5). The Examiner finds that “Blau teaches
spray-granulated oxcarbazepine is a product of spraying a dispersion of
oxcarbazepine particles on air–fluidized excipient particles” (Ans. 6).
The issue with respect to this rejection is: Does the evidence of record
support the Examiner’s conclusion that Blau anticipates the claims?

2 Blau, S., US 2007/0178164 A1, published Aug. 2, 2007.
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Findings of Fact
1. Blau teaches “a pharmaceutical composition comprising
oxcarbazepine and at least one pharmaceutical excipient, wherein the
oxcarbazepine in the composition has a broad particle size distribution and
an enhanced oxcarbazepine dissolution rate” (Blau, abstract).
2. The Specification teaches that the
[T]erm “solid solution” as used herein refers to a type of
solid dispersion wherein one component is molecularly
dispersed throughout another component such that the
system is chemically and physically uniform and
homogeneous throughout. These systems do not contain any
significant amounts of active ingredients in their crystalline
or microcrystalline state as evidenced by thermal analysis or
x-ray diffraction

(Spec. 6–7 ¶ 22).
3. The Specification teaches that the “invention includes other
methods described herein that are also useful in converting oxcarbazepine to
the amorphous state and corresponding enhanced bioavailability. Those
methods include, without limitation . . . granulation” (Spec. 7 ¶ 24).
4. Blau teaches “the production of the pharmaceutical composition
comprising a broad particle size distribution of oxcarbazepine comprises
spray granulation of at least one population of oxcarbazepine particles, either
from small drug particles or from large drug particles” (Blau 6 ¶ 89).
5. The Specification teaches that “[s]olubility-enhancing polymers
that are suitable for use in the mixtures of the present invention should result
in conversion of at least some of the crystalline oxcarbazepine to the
amorphous state . . . examples of useful polymers include, but are not limited
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to . . . hydroxypropylmethyl cellulose . . . [and] polyvinylpyrrolidone”
(Spec. 12 ¶ 36).
6. Blau teaches that the “oxcarbazepine is milled in a
liquid dispersion by a homogenizer. . . . Preferably, such reduction of the
particle size of oxcarbazepine by wet milling is carried out in the presence of
a hydrophilic polymer or stabilizer. A preferred hydrophilic polymer or
stabilizer is a hypromellose (Hydroxypropylmethylcellulose, HPMC)” (Blau
5 ¶ 86).
7. Blau teaches that the “oxcarbazepine pharmaceutical
compositions comprising a broad particle size distribution as in the present
invention further may contain excipients such as . . . hydroxypropyl methyl
cellulose and Povidone [i.e. polyvinylpyrrolidone]” (Blau 5 ¶ 76).
8. Blau teaches that “[s]olid pharmaceutical compositions that are
compacted into a dosage form, such as a tablet, may include excipients
whose functions include helping to bind the active ingredient and other
excipients together after compression. Binders for solid pharmaceutical
compositions include . . . hydroxypropyl methyl cellulose . . . povidone”
(Blau 5 ¶ 79).
9. Blau teaches that “[o]xcarbazepine raw material . . . was
dispersed in a solution of 240 g hypromellose (Pharmacoat 603) in 4800 g of
purified water. The Pharmacoat was added to the water and mixed until a
clear mixture was obtained” (Blau 7 ¶ 104). Blau then teaches performance
of a series of granulation and spraying steps, concluding with a step where
the oxcarbazepine and hypromellose “mixture was subsequently pressed into
tablets” (Blau 8 ¶ 110).
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Principles of Law
“A single prior art reference that discloses, either expressly or
inherently, each limitation of a claim invalidates that claim by anticipation.”
Perricone v. Medicis Pharm. Corp., 432 F.3d 1368, 1375 (Fed. Cir. 2005).
Where, as here, the claimed and prior art products are
identical or substantially identical, or are produced by
identical or substantially identical processes, the PTO can
require an applicant to prove that the prior art products do
not necessarily or inherently possess the characteristics of
his claimed product. . . . Whether the rejection is based on
“inherency” under 35 U.S.C. § 102, on “prima facie
obviousness” under 35 U.S.C. § 103, jointly or alternatively,
the burden of proof is the same, and its fairness is evidenced
by the PTO’s inability to manufacture products or to obtain
and compare prior art products.

In re Best, 562 F.2d 1252, 1255 (CCPA 1977).
Analysis
We adopt the Examiner’s findings of fact and reasoning regarding the
scope and content of the prior art (Ans. 5–15; FF 1–8) and agree that claim 1
is anticipated by Blau. We address Appellants’ arguments below.
Appellants contend that “Blau fails to disclose or suggest a
composition containing the active and a solubility-enhancing polymer in the
form of a solid solution as set forth in claim 1. Furthermore, Blau fails to
disclose compositions wherein the oxcarbazepine is substantially
amorphous” (App. Br. 9). Appellants contend that “[s]praying
oxcarbazepine from a polymer solution (as in Blau example 1) would result
in polymer coated active particles but not solid solutions” (App. Br. 10).
Appellants contend that “the homogenous granulate of Blau is not a solid
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solution since one component is not molecularly dispersed throughout
another component” (App. Br. 10).
We are not persuaded. The Specification defines a “solid solution” as
“a type of solid dispersion wherein one component is molecularly dispersed
throughout another component such that the system is chemically and
physically uniform and homogeneous” (Spec. 6–7 ¶ 22; FF 2). Blau teaches
that “[o]xcarbazepine raw material . . . was dispersed in a solution of 240 g
hypromellose (Pharmacoat 603) in 4800 g of purified water. The
Pharmacoat was added to the water and mixed until a clear mixture was
obtained” (Blau 7 ¶ 104; FF 9). Blau then teaches performance of a series of
granulation and spraying steps, concluding with a step where the
oxcarbazepine and hypromellose “mixture was subsequently pressed into
tablets” (Blau 8 ¶ 110; FF 9).
We agree with the Examiner that when Blau forms a clear mixture of
the oxcarbazepine and hypromellose (FF 9), the evidence supports the
Examiner’s position that oxcarbazepine “would be molecularly dispersed
[throughout] the hypromellose (HPMC) to provide a system that is
chemically and physically uniform and homogeneous throughout” (Ans. 10).
After Blau’s mixture is homogenized, sprayed, granulated and pressed into
tablets, the Examiner reasonably finds that the resultant solid tablet
inherently satisfies the requirement for a “solid solution” of oxcarbzepine
and the solubility enhancer hypromellose (FF 5, 6). Best, 562 F.2d at 1255.
While Appellants repeatedly argue that the process of Blau would not
result in a “solid solution,” Appellants have provided no evidence supporting
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this argument. See In re Pearson, 494 F.2d 1399, 1405 (CCPA 1974)
(“Attorney’s argument in a brief cannot take the place of evidence.”).
Appellants contend that the “significant differences between the
sprayed dispersion in Blau and the solid solution set forth in claim 1 of the
pending application clearly indicate that it is improper to assume that this
property would be inherent” (App. Br. 11).
We are not persuaded. We find that the instant facts are precisely the
type of situation envisioned by Best where an Examiner should properly
apply an inherency argument. Blau teaches a composition comprising the
same drug, oxcarbazepine, as required by claim 1 (FF 1), combined with a
solubility enhancer, hydroxypropylmethyl cellulose (FF 6) identified in
Appellants’ Specification (FF 5) and required by Appellants’ claim 3.
Blau further teaches producing the composition by dissolving the
components together (FF 9) and granulation of the particles (FF 4), and
Appellants’ Specification teaches that methods “useful in converting
oxcarbazepine to the amorphous state and corresponding enhanced
bioavailability . . . include, without limitation . . . granulation” (Spec. 7 ¶ 24;
FF 3). Thus, Blau teaches a product composed of identical components
made using a process identified by Appellants’ Specification as achieving an
amorphous state and enhanced bioavailability (FF 1–9). Appellants provide
no evidence in rebuttal.
Conclusion of Law
The evidence of record supports the Examiner’s conclusion that Blau
anticipates the claims.

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SUMMARY
In summary, we affirm the rejection of claim 1 under 35 U.S.C.
§ 102(b) as anticipated by Blau. Pursuant to 37 C.F.R. § 41.37(c), claims 2–
9 fall with claim 1, as these claims were not argued separately.

No time period for taking any subsequent action in connection with
this appeal may be extended under 37 C.F.R. § 1.136(a).

AFFIRMED

cdc