Ex Parte Siepmann et al

Patent Trial and Appeal Board

Nov 21, 2018

13478668 (P.T.A.B. Nov. 21, 2018)

UNITED STA TES p A TENT AND TRADEMARK OFFICE
APPLICATION NO. FILING DATE
13/478,668 05/23/2012
48219 7590 11/26/2018
PA TENT DEPT.
FMC CORPORATION
2929 WALNUT STREET
PHILADELPHIA, PA 19104
FIRST NAMED INVENTOR
Juergen Siepmann
UNITED STATES DEPARTMENT OF COMMERCE
United States Patent and Trademark Office
Address: COMMISSIONER FOR PATENTS
P.O. Box 1450
Alexandria, Virginia 22313-1450
www .uspto.gov
ATTORNEY DOCKET NO. CONFIRMATION NO.
60799-USA 5030
EXAMINER
RIDER, LANCE W
ART UNIT PAPER NUMBER
1618
NOTIFICATION DATE DELIVERY MODE
11/26/2018 ELECTRONIC
Please find below and/or attached an Office communication concerning this application or proceeding.
The time period for reply, if any, is set in the attached communication.
Notice of the Office communication was sent electronically on above-indicated "Notification Date" to the
following e-mail address(es):
patents@fmc.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte JUERGEN SIEPMANN and YVONNE CUPPOK
Appeal2017-010209
Application 13/478,668
Technology Center 1600
Before RICHARD M. LEBOVITZ, JEFFREY N. FREDMAN, and
DAVID COTTA, Administrative Patent Judges.
FREDMAN, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal 1,2 under 35 U.S.C. § 134 involving claims to a solid
dose form comprising an ethanol resistant film coating. The Examiner
rejected the claims as obvious. We have jurisdiction under 35 U.S.C. § 6(b ).
We affirm.
1 Appellants identify the Real Party in Interest as the FMC Corporation (see
Br. 1. Appellants' Brief lacks page numbers. We number the pages
sequentially starting with the page with the "Real Party in Interest" heading
numbered as page 1 ).
2 We have considered and herein refer to the Specification of May 23, 2012
("Spec."); Non-Final Office Action of Nov. 10, 2015 ("Non-Final Act.");
Final Office Action of May 18, 2016 ("Final Act"); Appeal Brief of Nov. 30,
2016 ("Br."); and Examiner's Answer of May 2, 2017 ("Ans.").
Appeal2017-010209
Application 13/478,668
Statement of the Case
Background
"Controlled release dosage forms are designed to provide prolonged
and/or delayed release of an active ingredient after the administration of the
dosage form, as compared with the administration of an immediate release
dosage form" (Spec. ,r 2). "The design of controlled release dosage forms
must mitigate the risk of premature release ('dose dumping') leading to
overdose" (id. ,r 4). "The co-ingestion of alcoholic beverages with solid
dosage forms can lead to unintended high release rates and potentially fatal
side effects" (id. ,r 5). "The object of this invention was to identify a novel
polymeric film coating, which has reduced sensitivity to high concentrations
of ethanol in the surrounding bulk fluid" (id. ,r 6).
The Claims
Claims 1-3, 5-10, and 12-18 are on appeal. Independent claim 1 is
representative and reads as follows:
1. A solid dose form comprising an ethanol resistant film
coating composition encapsulating a core, wherein:
(i) said core comprises an active ingredient comprising at
least one of a pharmaceutical, veterinary, or nutraceutical active
ingredient;
(ii) said ethanol resistant film coating composition
comprises ethylcellulose and guar gum, wherein said guar gum
has an apparent viscosity 2: 151.0 cps at a shear rate of 50 s-1 in
a 1 % aqueous guar gum solution measured rotationally at 20°C
after 1 minute equilibration using a 6 cm acrylic cone (1 °) on a
cone-plate viscometer wherein the shear is ramped up linearly
from 1 to 50 s-1 in 25 steps over 29 seconds, and wherein said
guar gum is present in a weight ratio of ethylcellulose to guar
gum of from 60 :40 to 93: 7 respectively;
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(iii) said ethanol resistant film coating composition
provides controlled release of said active ingredient in both
acidic and neutral environments within the gastrointestinal
tract; and
(iv) said film coating composition is present on a dry
solids basis in an amount of from 2 to 40% by weight of the
total dose form.
The Issue
The Examiner rejected claims 1-3, 5-10, and 12-18 under 35 U.S.C.
§ I03(a) as obvious over Cavalcanti, 3 Oshlack, 4 Bastin, 5 and Hamed6 (Non-
Final Act. 9-12).
The Examiner finds Cavalcanti teaches "ethylcellulose films for
coating tablets comprising 90: 10, 80:20, and 70:30 ethylcellulose to guar
ratios" but does not teach "the amount of such coatings to use on tablets or
the inclusion of plasticizers or anti-tack agents in the coating formulations"
(Non-Final Act. 10). The Examiner finds Oshlack teaches "drug containing
controlled release dosage forms coated (2-25% weight gain) with dispersions
of ethyl cellulose (Aquacoat ECD-30) and a 0.1-70% or preferably 0.1-25%
of release modifying agent / hydrophilic polymer such as guar gum" (id.).
The Examiner finds Bastin teaches "abuse resistant tablet formulations
requiring gelling agents in the preparation that swell and prevent drug
release attempted through extraction in aqueous and ethanol solutions.
3 Cavalcanti et al., Characterisation of Ethyl cellulose Films containing
Natural Polysaccharides by Thermal Analysis and FTIR Spectroscopy, 23
Acta Farm. Bonaerense 53-7 (2004).
4 Oshlack et al., US 5,472,712, issued Dec. 5, 1995.
5 Bastin et al., US 6,309,668 Bl, issued Oct. 30, 2001.
6 Hamed et al., US 2013/0209560 Al, published Aug. 15, 2013.
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Application 13/478,668
These gelling agents include agents such as guar and have a viscosity of
1000 to 100,000 cp" (Non-Final Act. 11). The Examiner finds Hamed
teaches "abuse resistant dosage forms comprising a strong film former such
as ethylcellulose at 30-80%" (id.). The Examiner finds it obvious "to use a
commonly used viscosity of guar gum in the ethyl cellulose/guar coatings of
Cavalcanti and Oshlack in order to provide abuse resistance to such
sustained release dosage forms" (id.).
The issue with respect to this rejection is: Does the evidence of
record support the Examiner's conclusion that Bastin, Hamed, Cavalcanti,
and Oshlack render claim 1 obvious?
Findings of Fact
1. Hamed teaches "[s]ustained-release oral dosage forms suitable
for twice-a-day administration of hydrocodone are provided ... a dosage
form may have alcohol resistance" (Hamed ,r 7).
2. Hamed teaches a
coated granule, as described herein, can comprise a granule
comprising hydrocodone or a salt form thereof in an amount
from about O .1 to about 90 percent by weight of the granule, a
first strong film former in an amount from about 1 to about 90
percent by weight of the granule, a second viscosity modifier in
an amount from about 1 to about 90 percent by weight of the
granule, and a first fat/wax in an amount from about O to about
40 percent by weight of the granule; and a coating on the
granule, wherein the coating is present in an amount from about
20 to about 80 percent by weight of the coated granule, and
wherein the coating comprises a second strong film former in
an amount from about 10 to about 50 percent by weight of the
coated granule.
(Hamed ,r 12).
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Application 13/478,668
3. Hamed teaches in "some embodiments, the first and second
strong film formers are ethylcellulose" (Hamed ,r 13).
4. Hamed teaches a "viscosity modifier ... creates a
solution/dispersion with a viscosity of from about 100 to about 200,000
mPa· s" (Hamed ,r 41 ).
5. Hamed teaches "[ e ]xamples of viscosity modifiers include .. .
hydroxypropylmethylcellulose, hydroxyethylcellulose ... and guar gums .. .
or mixtures thereof' (Hamed ,r 41 ).
6. Bastin teaches "abuse resistant tablets comprising a plurality of
layers ... release of the drug substance from a tablet comprising a gelling
agent is improved if the drug substance and the gelling agent are present in
separate layers of the tablet" (Bastin 1 :7-31 ).
7. Bastin teaches "[ s Jui table gelling agents include, but are not
limited to, modified celluloses ... [and] guar ... gums. Mixtures of two or
more gelling agents may also be used" (Bastin 2: 1-7).
8. Bastin teaches "[p ]referably, the gelling agent will have a
viscosity within the range of about 4,000 cp to about 100,000 cp" (Bastin
2:17-18).
9. Bastin teaches "forming the core from a suitable powder by
compressing the powder using a suitable tablet press. Thereafter, the core
may be enclosed within the active layer or surrounded by a cap of active
layer using conventional means" (Bastin 3 :48-52).
10. Cavalcanti teaches "[ e ]thylcellulose (EC) has been widely used
as a coating material for controlled release systems. Some oligo-
polysaccharides such as inulin (IN), guar gum (GG) and their derivatives
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have been proposed as biodegradable materials for site-specific releases"
(Cavalcanti, Abstract).
11. Cavalcanti teaches ethylcellulose "has been considered
promising for colon-specific delivery dosage forms" (Cavalcanti 54, col. 1 ).
12. Cavalcanti teaches guar gum "could be potentially used as a
biodegradable material for the preparation of coated dosage forms for site-
specific release. This carbohydrate is susceptible to microbial degradation in
a specific region of the gastrointestinal tract" ( Cavalcanti 54, col. 1 ).
13. Cavalcanti teaches "EC/GG [ethylcellulose/guar gum] films
were prepared in three compositions: 90/10, 80/20 and 70/30" (Cavalcanti
55, col. 1 ).
14. Cavalcanti teaches "polymeric coatings for selective drug
delivery. Polymer blends having colon specific properties and film-forming
properties have also been suggested, especially those which contain
cellulose derivatives" (Cavalcanti 53, col. 1 ).
15. Oshlack teaches "cellulose derivatives ... have been used in the
prior art to develop controlled release dosage forms. Methods of using these
polymers to develop controlled release dosage forms such as tablets ... are
to overcoat the individual dosage units" (Oshlack 1:56-61 ).
16. Oshlack teaches "the pore-formers may comprise one or more
water-soluble hydrophilic polymers in order to modify the release
characteristics of the formulation" (Oshlack 11 :62---64).
1 7. Oshlack teaches the "controlled release coatings of the present
invention can also include released modifying agents which promote erosion
(i.e., erosion promoting agents), such as ... guar" (Oshlack 12:54---63).
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18. Oshlack teaches "stabilized controlled release formulations of
the present invention slowly release the active agent, e.g., when placed in an
environmental fluid in an environment of use. By 'environmental fluid', it is
meant that the formulation is placed in an aqueous solution" (Oshlack 9:14--
18).
Principles of Law
"The combination of familiar elements according to known methods
is likely to be obvious when it does no more than yield predictable results."
KSR Int'! Co. v. Teleflex Inc., 550 U.S. 398,416 (2007).
Analysis
We adopt the Examiner's findings of fact and reasoning regarding the
scope and content of the prior art (Non-Final Act. 9--12; FF 1-18) and agree
that the claims are rendered obvious by Hamed, Bastin, Oshlack, and
Cavalcanti. We address Appellants' arguments below.
Appellants contend that: "Cavalcanti does not teach or suggest many
of the claimed limitations of the present application" (Br. 4); that "Oshlack
. . . does not provide guidance as to what characteristics are desirable for the
guar gum - used as an erosion promoter - and certainly no suggestion as to
properties for other uses" (id. at 5); that Bastin "conspicuously does not
teach a mixture of guar gum and ethylcellulose" (id.); and that "Hamed,
although introducing the problem of ethanol resistance in a tablet coating,
does not name either of the coating components claimed by the applicants"
(id.).
Appellants also contend "[ n Jo opinions were offered that would
motivate one of ordinary skill to look to combine the teaching of that
reference with the other references cited. No discussion was offered and no
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conclusions were drawn, for example, with respect to the efficacy of using
any of the films as coating materials" (Br. 6).
We find these arguments unpersuasive because it is the combination
of Hamed, Bastin, Cavalcanti, and Oshlack along with what these references
suggest, not any single reference alone, that renders the claims obvious.
"Non-obviousness cannot be established by attacking references individually
where the rejection is based upon the teachings of a combination of
references." In re Merck & Co., 800 F.2d 1091, 1097 (Fed. Cir. 1986).
In particular, Hamed teaches alcohol resistant oral dosages that
comprise hydrocodone cores (FF 1) with film forming coatings that include
cellulose (FF 2-3) as well as viscosity modifier coatings that may comprise
cellulose and guar gum "or mixtures thereof' (FF 5). Hamed teaches a
range of viscosities that was "independently used to prevent the abuse of
drugs" (Final Act. 9; see FF 4). Bastin, which also expressed interest in
abuse resistant tablets, teaches a gelling agent layer (FF 6) that may be
composed of mixtures of gelling agents including celluloses and guar gum
(FF 7) with viscosities of 4,000 to 100,000 centipoise (FF 8). Oshlack also
teaches the use of cellulose in controlled release coatings (FF 15-17).
Cavalcanti teaches that ethylcellulose and guar gum are widely used
as film coatings for controlled release dosage forms (FF 10-12). Cavalcanti
further teaches three specific ethylcellulose/ guar gum formulations that fall
within the weight ratio required by claim 1 (FF 13).
These teachings would therefore have provided reason to consider
known cellulose and guar gum coatings for use in the dosages of Hamed and
Bastin, and select the particular ethylcellulose/guar gum formulations of
Cavalcanti for selective drug delivery because "[p ]olymer blends having
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colon specific properties and film-forming properties have also been
suggested, especially those which contain cellulose derivatives" (FF 14). "If
a person of ordinary skill can implement a predictable variation, § 103 likely
bars its patentability." KSR, 550 U.S. at 417.
Appellants contend
there is no evidence or data presented in Cavalcanti that would
fairly suggest that the films obtained therein are ethanol
resistant. The examiner has previously relied on an inherency
argument to support this conclusion, but Cavalcanti cannot
provide support for an 'inherency' argument since it is not an
anticipatory reference.
(Br. 6).
We find this argument unpersuasive for several reasons. First, both
Hamed and Bastin suggest that cellulose coating mixtures that may include
guar gum may be ethanol resistant (FF 1, 5-7) and Cavalcanti exemplifies a
cellulose/guar gum coating (FF 13). Second, inherency is relevant to
obviousness, as the Federal Circuit noted, "[ w ]e have recognized that
inherency may supply a missing claim limitation in an obviousness analysis"
when that limitation is necessarily present. Par Pharm., Inc. v. TWI
Pharms., Inc., 773 F.3d 1186, 1194--95 (Fed. Cir. 2014).
We recognize that the limitation must be "the natural result of the
combination of elements explicitly disclosed by the prior art." Par, 773 F.3d
at 1196. In the current case, the Examiner has provided evidence that
selecting the ethylcellulose/guar gum coating of Cavalcanti consistent with
the teachings of Hamed and Bastin would "have the same required ratios of
ethylcellulose to guar and the same viscosity of guar required by the instant
claims" (Ans. 8) and "[p ]roducts of identical chemical composition can not
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have mutually exclusive properties." In re Spada, 911 F.2d 705, 708 (Fed.
Cir. 1990).
We think the Examiner has therefore provided a fact-based prima
facie case of obviousness and has shifted the burden to Appellants to
demonstrate that the coating of Cavalcanti, when used on tablets as
suggested by Hamed and Bastin, would not have necessarily had the alcohol
resistant properties desired by Hamed and Bastin (FF 1, 6).
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).
Appellants contend that the "erosion promoting function of guar in the
coatings of Oshlack does not highlight or suggest guar gum as potentially
useful to impart ethanol resistance to the coatings of the presently claimed
invention. This teaching of Oshlack can be considered a teaching away
from the claimed invention" (Br. 7).
We are not persuaded. A teaching away requires a reference to
actually criticize, discredit, or otherwise discourage the claimed solution.
See In re Fulton, 391 F.3d 1195, 1201 (Fed. Cir. 2004) ("The prior art's
mere disclosure of more than one alternative does not constitute a teaching
away from any of these alternatives because such disclosure does not
criticize, discredit, or otherwise discourage the solution claimed").
Appellants' citation to Oshlack does not criticize, discourage or otherwise
discredit the use of guar gum as a coating.
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More importantly, Oshlack teaches that release agents include "water-
soluble hydrophilic polymers" (FF 16) and that controlled release coatings
allow erosion in the aqueous environment of the intestine (FF 18). Thus,
Oshlack does not suggest coatings in general that are alcohol/ethanol
soluble, nor does Oshlack teach that guar gum in particular is
alcohol/ethanol soluble (FF 17), but rather Oshlack suggests that these
coatings must be water-soluble to some degree (FF 16, 18). Therefore,
contrary to Appellants' arguments, Oshlack supports the Examiner's
reasoning because Oshlack teaches that guar gum is water-soluble, not
alcohol-soluble, and would therefore be expected to have some degree of
ethanol resistance because it dissolves in water, not alcohol (FF 16-18).
Appellants provide no evidence that guar gum would have been expected to
be ethanol soluble based on Oshlack or other references. 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
In selecting certain features from the references and
ignoring others that teach away, the examiner has chosen to
disregard disclosures from the references that do not fit the
narrative for rejecting the claims. There is no guidance from
the other references that would lead the examiner to selectively
assemble the teachings from the references in the precise
manner that would lead to the claimed invention. This is
clearly an impermissible use of hindsight.
(Br. 8).
We are not persuaded. While we are fully aware that hindsight bias
may plague determinations of obviousness, Graham v. John Deere Co., 383
U.S. 1, 36 (1966), we are also mindful that the Supreme Court has clearly
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stated that the "combination of familiar elements according to known
methods is likely to be obvious when it does no more than yield predictable
results." KSR, 550 U.S. at 416.
Here, the Examiner has provided specific reasoning based on evidence
disclosed in the prior art for obtaining the obvious combination (see, e.g.,
Non-Final Act. 10-12). In particular, we agree that the ordinary artisan,
interested in drug tablets with alcohol resistant coatings and controlled
release coatings (FF 1, 6, 10), and aware that cellulose and guar gum were
routine components of controlled release coatings (FF 5, 7, 10, 17) would
have reasonably selected the controlled release coating of Cavalcanti for use
with the tablets of Hamed and Bastin in order to allow gastrointestinal tract
or colon specific drug release (FF 11, 12). We also agree with the Examiner
that
Bastin and Hamed are provided to teach the use of both
ethylcellulose and guar in dosage forms in order to prevent
abuse of drugs within them. Though the combination of
Cavalcanti and Oshlack alone would generally teach the dosage
forms claimed the further art of Bastin and Hamed provide that
these agents were known to be used for preventing abuse. Thus
their use for that function is not particularly novel or
unexpected. This prior art provides further motivation as to
why one would select ethylcellulose or guar with particular
viscosities for preventing abuse of such dosage forms by
alcohol extraction.
(Ans. 13).
Appellants contend
At best the examiner has asserted that it may be obvious to
experiment. "Obvious to experiment to experiment is not a
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proper standard for obviousness." In re Dow Chemical Co.,
837 F.2d 469, 5 USPQ2d 1529 (Fed. Cir. 1988).
Given that there are numerous ways that ethylcellulose
and guar gum can be combined to form a film -- particularly in
view of the wide range of materials that broadly constitute
"ethylcellulose" and "guar gum" -- it is hardly an inherent
feature that ethanol resistance would be obtained simply by
mixing the two components in some haphazard manner.
(Br. 9).
We find this argument unpersuasive. Insofar as Appellants imply "the
obviousness inquiry cannot consider that the combination of the claim's
constituent elements was 'obvious to try,' the Supreme Court in KSR
unambiguously discredited that holding." In re Kubin, 561 F.3d 1351, 1358
(Fed. Cir. 2009). The instant case falls into neither of the situations where
"obvious to try" is erroneously equated with obviousness. See id. at 1359.
Here, the prior art gives much more than general guidance regarding
controlled release coatings with Cavalcanti suggests controlled release
coatings that are composed of cellulose and guar gum in the same weight
ratios as required by claim 1 (FF 13).
Also, because Cavalcanti provides a controlled release coating with
the identical structure as that required by claim 1, no variation of parameters
would have necessarily been required to obtain a successful result.
Moreover, both Hamed and Bastin identify ethanol resistance as a critical
parameter (FF 1, 6) and teach that cellulose and guar gum are coating
components likely to be successful (FF 5, 7). Therefore, the Examiner's
obviousness position reasonably is consistent with "the Supreme Court's
statement in KSR that where a skilled artisan merely pursues 'known
options' from a 'finite number of identified, predictable solutions,'
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obviousness under§ 103 arises." Kubin, 561 F.3d at 1359 (citing KSR, 550
U.S. at 421 ).
Conclusion of Law
The evidence of record supports the Examiner's conclusion that
Bastin, Hamed, Cavalcanti, and Oshlack render claim 1 obvious.
SUMMARY
In summary, we affirm the rejection of claim 1 under 35 U.S.C.
§ 103(a) as obvious over Cavalcanti, Oshlack, Bastin, and Hamed. Claims
2, 3, 5-10, and 12-18 fall with claim 1.
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
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