Ex Parte Kolter et al

Patent Trial and Appeal Board

Jul 21, 2016

12663046 (P.T.A.B. Jul. 21, 2016)

UNITED STA TES p A TENT AND TRADEMARK OFFICE
APPLICATION NO. FILING DATE
12/663,046 12/04/2009
123223 7590 07/25/2016
Drinker Biddle & Reath LLP (WM)
222 Delaware A venue, Ste. 1410
Wilmington, DE 19801-1621
FIRST NAMED INVENTOR
Karl Kolter
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.
074008-0955-US (286117) 1779
EXAMINER
CHUI, MEI PING
ART UNIT PAPER NUMBER
1616
NOTIFICATION DATE DELIVERY MODE
07/25/2016 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):
IPDocketWM@dbr.com
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PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte KARL KOLTER, MICHAEL SCHONHERR,
SILKE GEBERT, KATHRIN MEYER-BOHM,
and ANGELIKA MASCHKE
Appeal2014-006406
Application 12/663,046
Technology Center 1600
Before DONALD E. ADAMS, JEFFREY N. FREDMAN, and
JOHN G. NEW, Administrative Patent Judges.
FREDMAN, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal 1 under 35 U.S.C. § 134 involving claims to a tablet,
pharmaceutical formulation, and process for producing the formulation. The
Examiner rejected the claims as obvious. We have jurisdiction under
35 U.S.C. § 6(b). We affirm-in-part.
1 Appellants identify the Real Party in Interest as BASF SE (see
App. Br. 2).
Appeal2014-006406
Application 12/663,046
Statement of the Case
Background
"Tablets which disintegrate rapidly in the mouth and/or dissolve
rapidly are becoming increasingly important for the oral administration of
medicaments" (Spec. 1 :8-9). "Such tablets must disintegrate within a short
time, preferably within 30 seconds, in the oral cavity and have a pleasant
taste and must not leave behind a gritty sensation" (Spec. 1 :9-12).
The Claims
Claims 23--44 are on appeal. Independent claim 23 is representative
and reads as follows:
23. A pharmaceutical formulation in the form of
agglomerates comprising
A) an excipient content composed of
a. 60-97% by weight of sugar or sugar
alcohols,
b. 1-25% by weight of a disintegrant,
c. 1-15% by weight of water-insoluble, film-
forming polymers
d. 0-15% by weight of water-soluble polymers
and
e. 0-15% by weight of further pharmaceutically
customary excipients the total of the components a) to
e) being 100% by weight, and
B) at least one active ingredient.
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The Issues
The Examiner rejected claims 23--44 under 35 U.S.C. § 103(a) as
obvious over Faham,2 Kolter, 3 Tian,4 and Eliasen5 (Ans. 3-9).
The Examiner finds that
One of ordinary skill in the art would have been motivated to
modify the pharmaceutical formulation from the granular or
powder form to the agglomerates form because the prior art
Kolter and Tian teach that the agglomerated form of the
claimed polymers, i.e. polyvinyl acetate and
polyvinylpyrrolidone and the agglomerated form of the claimed
sugar alcohol (e.g. mannitol) and disintegrant can provide
beneficiaries to the rapid disintegrated tablet, such as an
improved disintegration time compared to the tablet made by
conventional compression of a dry blend, improves dissolution
of active ingredients in body fluids, higher tablet breaking
resistances and lower tablet friabilities, as well as less dusting
during handling and excellent flowability, as taught by Kolter,
Tian and Eliasen.
(Ans. 8).
The issue with respect to this rejection is: Does the evidence of
record support the Examiner's conclusion that the prior art render the claims
obvious?
2 Faham et al., WO 03/041683 A2, published May 22, 2003.
3 Kolter et al., US 6,066,334, issued May 23, 2000.
4 Tian et al., US 2005/0169986 Al, published Aug. 4, 2005.
5 Eliasen, I., US 2006/0115524 Al, published June 1, 2006.
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Application 12/663,046
Findings of Fact
1. Kolter teaches a process for producing solid pharmaceutical
presentations that "make[ s] rapid release of the active ingredients possible"
and
that this object is achieved by the use of redispersible
polymer powders or polymer granules consisting of
a) 10-95% by weight of polyvinyl acetate,
b) 5-90% by weight of an N-vinylpyrrolidone-containing
polymer,
c) 0-20% by weight of another water-soluble or water-
swellable substance and
d) 0-20% by weight of a water-insoluble dusting agent
with or without
e) other additives,
as binders for producing solid pharmaceutical
presentations, where the binder content in the presentation is
from 0.5 to 20% by weight.
(Kolter 2: 18-36).
2. Kolter teaches that it "is furthermore possible for the products
to contain other hydrophilic, water-soluble polymers such as ...
monosaccharides, disaccharides, sugar alcohols" (Kolter 4: 14--22).
3. Kolter teaches that the "product according to the invention is
mixed dry with the active ingredient and other ancillary substances, for
example ... disintegrants" (Kolter 4:59---62).
4. Kolter teaches that "[i]t is also possible to employ FSD
(fluidized spray drying) technology, in which initial spray-drying is
immediately followed by agglomeration in a fluidized bed" (Kolter 4:7-9).
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Application 12/663,046
5. Tian teaches
a fast disintegrating tablet comprising an active ingredient and
one or more disintegrants characterised in that the tablet
comprises agglomerates having an agglomerated particle size of
at least 50 µm, said agglomerates comprising at least 10% by
weight of a superdisintegrant selected from croscarmellose
cellulose, crospovidone and sodium starch glycollate and being
free of active ingredient.
(Tian ii 27).
6. Tian teaches that the "agglomerates comprise at least 10%,
preferably at least 25% ... by weight disintegrant. The remainder of the
agglomerates may comprise known tabletting ingredients including water-
soluble and water insoluble fillers and/or diluents, binder, flavouring agents
etc." (Tian ii 35).
7. Tian teaches "mixing the agglomerates from step (I) with an
active ingredient" (Tian ii 30).
8. Eliasen teaches that "[i]t is usually preferred to prepare
agglomerates comprising active compounds before these are manufactured
into pharmaceutical composition" (Eliasen ii 32).
9. Faham teaches "orodispersible tablets comprising coated
granules of fexofenadine" further comprising a "mixture of excipients
comprising: at least one disintegrating agent, a soluble diluent agent, a
lubricant, and optionally a permeabilising agent, a swelling agent, an
antistatic agent sweeteners, flavoring agents and colors" (Faham 1: 1-2 and
4:25 to 5:2).
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Application 12/663,046
10. Faham teaches that the "binder is selected from the group
consisting of ... sucrose and its derivatives" (Faham 7: 15-20).
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!nt'l Co. v. Teleflex Inc., 550 U.S. 398, 416 (2007). "If a person of
ordinary skill can implement a predictable variation, § 103 likely bars its
patentability." Id. at 417.
Analysis
We adopt the Examiner's findings of fact and reasoning regarding the
scope and content of the prior art (Ans. 3-9; FF 1-10). We address
Appellants' arguments below.
Claims 23 and 40
Appellants contend that:
Faham neither teaches nor suggests forming particles of
any kind from fexofenadine, binder, disintegrating agent, and
soluble diluent agent as individual components, let alone an
agglomerate of these components, prior to compression into
tablet form ....
Kolter does not disclose agglomerates with the
component makeup presently recited in the claims. The
agglomeration discussed in Kolter refers only to the production
of the binder itself ....
Tian's disclosure referring to Example 1 and the comparative
examples disclose agglomerated disintegrant (i.e., Polyplasdone
XL-1) and mannitol (not an active ingredient), but is clearly
suggested to agglomerate them separately. There is definitely
no recommendation in Tian to agglomerate the tablet excipients
and drug together ....
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Application 12/663,046
Eliasen discloses a melt agglomeration process, the
agglomerates produced have a complete different composition
compared to the present invention which is not properly
combinable with the remaining references.
(App. Br. 6-8).
We find these arguments unpersuasive because they fail to address the
combined teachings of the references. "The test for obviousness is not
whether the features of a secondary reference may be bodily incorporated
into the structure of the primary reference . . . . Rather, the test is what the
combined teachings of the references would have suggested to those of
ordinary skill in the art." In re Keller, 642 F.2d 413, 425 (CCPA 1981).
Moreover, "[ n ]on-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 the instant case, each of the references teaches delivery of active
pharmaceutical agents (FF 3, 5, 8, 9) using various excipients (FF 1, 6, 8,
10). In particular, Kolter teaches excipients including sugars and sugar
alcohols (FF 2), disintegrants (FF 3), water-insoluble and water soluble
polymers (FF 1) and other additives (FF 1 ), as well as an active ingredient
(FF 1, 3).
In addition to suggesting all of the components, Kolter suggests the
use of agglomeration technology (FF 4), a technology also taught by Tian
and Eliason (FF 7-8). Eliason specifically suggests that "[i]t is usually
preferred to prepare agglomerates comprising active compounds before
these are manufactured into pharmaceutical composition" (FF 8).
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Thus, we agree with the Examiner that the combined teachings of
Kolter, Tian, Eliason, and Faham reasonably suggest pharmaceutical
formulations of claim 23 with an active ingredient included in the
agglomeration process (FF 1-10).
Appellants specifically argue that "Tian teaches away from the
present invention" because "the entirety of the disclosure of Tian makes it
clear that agglomerates are formed which do not contain active ingredient.
These agglomerates are then dry blended and put into a tableting device with
active ingredient without further agglomeration" (App. Br. 7-8).
We find the teaching away arguments unpersuasive. A teaching away
requires a reference to actually criticize, discredit, or otherwise discourage
the claimed solution. See In re Fulton, 391F.3d1195, 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 do not identify, and we do not find, any teaching in
Tian that discredits or discourages agglomeration of the active ingredient
with the other components, only a teaching of a particular approach to
tableting (FF 7).
Appellants also specifically argue that "Eliasen discloses a melt
agglomeration process, the agglomerates produced have a complete different
composition compared to the present invention which is not properly
combinable with the remaining references" (App. Br. 8).
We find this argument unpersuasive because Eliasen generically
teaches that "[i]t is usually preferred to prepare agglomerates comprising
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Application 12/663,046
active compounds before these are manufactured into pharmaceutical
composition" (FF 8). Eliasen discusses this in the context of a general
discussion of agglomerates and does not limit this teaching to the particular
melt agglomeration process used in the Eliasen patent (cf Eliasen i-fi-132, 36).
The test for non-analogous art is first whether the art is within the
field of the inventor's endeavor and, if not, whether it is "reasonably
pertinent to the particular problem with which the inventor was involved."
In re Wood, 599 F.2d 1032, 1036 (CCPA 1979). "A reference is reasonably
pertinent if, even though it may be in a different field" of endeavor, it
logically would have commended itself to an inventor's attention in
considering his problem "because of the matter with which it deals." In re
Clay, 966 F.2d 656, 659 (Fed. Cir. 1992). Here, Eliasen's teaching appears
to satisfy both prongs of the analogous art test, as related to the same field of
endeavor of pharmaceutical tableting and pertinent to agglomeration for
producing such tablets (FF 8). Appellants provide no evidence that
Eliasen's teaching regarding pharmaceutical tablet preparation would not
have been understood to apply to any agglomeration process in the art of
pharmaceutical tableting or that Eliasen would not have been pertinent to
that art.
Claim 28
Appellants contend that:
While hydroxypropylcellulose is mentioned generically in
Faham (page 7, lines 15-16 & 19), there is nothing in that
reference, or any other reference, to suggest in particular
hydroxypropylcellulose with 5 to 16% hydroxypropoxy groups.
Therefore, as every limitation of claim 28 is not disclosed or
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Application 12/663,046
suggested by the art cited by the Examiner, the Examiner has
not provided a prima facie case for the obviousness
(App. Br. 9).
The Examiner responds that "there is no clear indication from claim
23 and claim 28 that the hydroxypropylcellulose, which having such
particular 5-16 % hydroxypropoxy groups, is an essential element for the
formulation and, thus, it is not critical to the claimed invention" (Ans. 10).
We find that Appellants have the better position. Whether a limitation
is "critical" or trivial, the initial burden of demonstrating that claimed
elements are taught in, or rendered obvious by, the prior art rests on the
Examiner. The Examiner "bears the initial burden ... of presenting a prima
facie case ofunpatentability." In re Oetiker, 977 F.2d 1443, 1445 (Fed. Cir.
1992). The Examiner has not satisfied this burden by finding a prior art
teaching or reason to select 5-16 % hydroxypropoxy groups as required by
claim 28.
Claim 43
Appellants contend that
neither Faham nor Kolter ... disclose or suggest the
combination of a first step in which excipients are first
agglomerated and a second step wherein the active ingredient is
further agglomerated with the agglomerated excipient
composition .... Tian clearly does not teach or suggest a
second step in which active ingredients are agglomerated with
an excipient composition. . . . [I]n the "melt agglomeration"
process of Eliasen, the active ingredient is simply mixed with
the remainder of components in a melt. There is no first step in
which excipients are agglomerated, followed by a second step
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in which the active ingredient is agglomerated with the
agglomerates formed in the first step
(App. Br. 11 ).
We do not find this argument persuasive because Tian suggests
combining the agglomerate with the active compound (FF 7) and Eliasen
teaches that "[i]t is usually preferred to prepare agglomerates comprising
active compounds" (FF 8). Thus, because Tian suggests the particular order
of addition of components and Eliasen teaches agglomeration before
pharmaceutical tableting (FF 7-8), we agree with the Examiner that it would
have been "routine experimentation and would have been obvious for one of
ordinary skill in the art to change in sequence of adding the ingredients as
claimed in any order, as suggested by Faham and Tian, that the tablet can be
prepared by combining the particular ingredients in stepwise manner" (Ans.
8). Therefore, "[t]here is no merit in [Appellants] point here in the absence
of any proof in the record that the order of performing the steps produces
any new and unexpected results." In re Burhans, 154 F.2d 690, 692 (CCPA
1946). Appellants provide no evidence of unexpected results for the specific
order of agglomeration steps.
Conclusions of Law
The evidence of record supports the Examiner's conclusion that the
prior art render claims 23, 40, and 43 obvious.
The evidence of record does not support the Examiner's conclusion
that the prior art renders claim 28 obvious.
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SUMMARY
In summary, we affirm the rejection of claims 23, 40, and 43 under
35 U.S.C. § 103(a) as obvious over Faham, Kolter, Tian, and Eliasen.
Claims 24--27, 29-39, 41, 42, and 44 fall with claims 23, 40, and 43.
We reverse the rejection of claim 28 under 35 U.S.C. § 103(a) as
obvious over Faham, Kolter, Tian, and Eliasen.
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-IN-PART
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