Ex Parte Holton et al

Patent Trial and Appeal Board

Nov 1, 2016

13240500 (P.T.A.B. Nov. 1, 2016)

United States Patent and Trademark Office
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
APPLICATION NO. FILING DATE FIRST NAMED INVENTOR ATTORNEY DOCKET NO. CONFIRMATION NO.
13/240,500 09/22/2011 Darrell Holton JR. N64138 1020US.1 (0006.2) 2564
26158 7590 11/03/2016
WOMBLE CARLYLE SANDRIDGE & RICE, LLP
ATTN: IP DOCKETING
P.O. BOX 7037
ATLANTA, GA 30357-0037
EXAMINER
AHMED, HASAN SYED
ART UNIT PAPER NUMBER
1615
NOTIFICATION DATE DELIVERY MODE
11/03/2016 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):
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PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte DARRELL HOLTON, JR.,
NELLY FRANSEN, and MATT REDDICK1
Appeal 2015-003194
Application 13/240,500
Technology Center 1600
Before MELANIE L. McCOLLUM, JEFFREY N. FREDMAN, and
JOHN G. NEW, Administrative Patent Judges.
McCOLLUM, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134 involving claims to
pharmaceutical compositions and methods. The Examiner has rejected the
claims as obvious. We have jurisdiction under 35 U.S.C. § 6(b). We affirm.
STATEMENT OF THE CASE
Claims 1—27 and 48—52 are pending and on appeal (App. Br. 2 & 17—
18). Claims 1, 4, and 48 are representative and read as follows:
1. A nicotine-containing pharmaceutical composition, comprising:
a. a nicotinic compound;
1 Appellants identify the real party in interest as Niconovum USA, Inc.
(App. Br. 1).
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b. a sugar substitute in an amount of at least about 80% by
weight; and
c. a sugar alcohol syrup,
wherein the sugar substitute is a non-hygroscopic sugar alcohol
capable of forming a glassy matrix and wherein the composition is in a
pharmaceutically acceptable form adapted for oral delivery of the
composition.
4. The pharmaceutical composition of claim 1, wherein the nicotinic
compound is sorbed onto a porous particulate carrier.
48. A nicotine-containing pharmaceutical composition, comprising:
a. a nicotinic compound;
b. a first non-hygroscopic sugar alcohol capable of forming a
glassy matrix in an amount of at least about 80% by weight; and
c. a second sugar alcohol in an amount of at least about 4.5% by
weight and up to about 20% by weight,
wherein the composition is in a pharmaceutically acceptable form
adapted for oral delivery of the composition.
Claims 1, 2, 6—14, 48—50, and 52 stand rejected under 35 U.S.C.
§ 103(a) as obvious over Dam et al. (US 2007/0081949 Al, Apr. 12, 2007)
(“Dam”) in view of Chan et al. (US 2005/0123502 Al, June 9, 2005)
(“Chan”) (Final Act. 2).
Claims 1—3, 6—20, and 51 stand rejected under 35 U.S.C. § 103(a) as
obvious over Dam in view of Chan (Final Act. 4—5).
Claims 1—27 stand rejected under 35 U.S.C. § 103(a) as obvious over
Dam in view of Chan and Hansson (US 2004/0191322 Al, Sept. 30, 2004)
(Final Act. 6).
I
In the first two rejections, the Examiner relies on Dam for disclosing
“a lozenge that has stable pH and stable levels of active ingredient over
time” (Final Act. 2). In particular, the Examiner finds:
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Dam discloses a nicotine containing pharmaceutical composition
comprising: (a) a nicotine compound . . . ; (b) a sugar substitute
(e.g. isomalt)... at a concentration of up to 60% by weight.. . ;
and a sugar alcohol syrup .... The sugar substitute is a non-
hygroscopic sugar (e.g., isomalt...) which forms a glassy matrix
composition pharmaceutically acceptable for oral delivery.
(Id. at 2—3.)
The Examiner relies on Chan for teaching “an oral composition
comprising a nicotine active” wherein the “composition may be formulated
as a lozenge or candy” and “may comprise up to 99% fillers” (id. at 4). The
Examiner also finds that Chan teaches that “[s]uitable fillers include non-
hygroscopyic [sic] sugar alcohols such as mannitol and sorbitol” (id.) The
Examiner concludes that the claimed composition would have been obvious
in view of Dam and Chan (id.).
Findings of Fact
1. The Specification discloses: “[T]he present invention relates to
a nicotine-containing composition intended to be employed for therapeutic
purposes. The composition is typically in a pharmaceutically acceptable
form adapted for oral delivery of the composition. The composition
incorporates at least one nicotinic compound, a sugar substitute, and a sugar
alcohol syrup.” (Spec. 4.)
2. The Specification also discloses: “In some embodiments, the
sugar substitute is isomalt. In certain embodiments, the sugar alcohol syrup
is maltitol syrup or xylitol syrup.” (Id.)
3. In addition, the Specification discloses:
“Sugar alcohol syrup” as used herein is intended to refer to a
thick solution of sugar alcohol in water, e.g., having greater than
about 40% solids ... by weight. Typically, the solid content of
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Application 13/240,500
the sugar alcohol syrup primarily comprises the named sugar
alcohol (i.e., maltitol syrup typically comprises greater than
about 80% ... by weight maltitol on a dry basis). Sugar alcohol
syrups are generally prepared by heating a solution of the sugar
alcohol in water and cooling the mixture to give a viscous
composition. The resulting syrup is typically characterized by a
relatively high concentration of sugar alcohol and relatively high
stability (i.e., the sugar alcohol typically does not crystallize from
solution, e.g., at room temperature).
(Id. at 15-16.)
4. Dam discloses “a glassy lozenge for buccal drug delivery
comprising: a) a matrix; b) an active agent; [and] c) water; . . . wherein the
matrix comprises (i) at least one gum and (ii) at least one non-crystallising
sugar or non-crystallising sugar alcohol” (Dam H 17—22 (paragraphs and
paragraph numbers removed)).
5. Dam also discloses that “[according to an embodiment of the
invention the lozenge provides for controlled release of the active agent” (id.
144).
6. In addition, Dam discloses:
The release profile of the active agent or the dissolution profile
of the lozenge is governed by the matrix composition and
lozenge size and can be varied according to the nature of the
active agent and the desired effect. Thus, the dissolution profile
can be altered, whilst retaining the same amount of the active
agent, by varying the lozenge size and/or the proportion of gum
in the lozenge. A smaller overall lozenge size will result in faster
dissolution. Similarly a reduced gum content will result in faster
lozenge dissolution.
(Id. 145.)
7. Dam also discloses: “The ratio of matrix components can be
varied to vary the dissolution profile. Typically, the matrix comprises from
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Application 13/240,500
40-90% of the gum component and from 60-10% of the non-crystallising
sugar or non-crystallising sugar alcohol component.” {Id. 147.)
8. In addition, Dam discloses that the active ingredient may be
nicotine {id. 1 69).
9. Dam also discloses “preferred lozenges of the invention
containing water, gum acacia, non-crystalizing sorbitol, non-crystallising
xylitol, non-crystallising maltitol, non-crystallising isomalt or other non­
crystallizing sugar alcohol derivatives, homologues or associated sugars”
{id. 196).
10. In Example 1, Dam discloses:
Dispense 276 kg of water, purified into the batch mixing
container. Heat to 70° C. and thermostatically maintain the
temperature. Add the sorbitol liquid (non-crystallizing), acacia
(spray dried) and xylitol. Heat the pre-mix slurry with stirring
for between 30 and 40 minutes maintaining a temperature of
between 68° C. and 72° C.
{Id. 1107.)
11. Chan “provides an oral composition that comprises a nicotine
active, alginic acid, or a salt thereof, and a polycarbophil component, or a
salt thereof’ (Chan 19).
12. Chan discloses:
Suitable fillers for use in the present composition include, but are
not limited to, those conventionally used in the art, such as . . .
microcrystalline cellulose; acacia gum; gum arabic;... mannitol;
sorbitol; inositol;... and any combinations thereof. When incor­
porated, fillers are generally present in the present compositions
from about 50% to about 99%.
(Id. 125.)
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13. Chan also discloses that “[s]uitable sweeteners include, but are
not limited to, . . . isomalt, . . . maltitol, . . . xylitol, and any combinations
thereof’ (id. 126).
14. In addition, Chan discloses:
The rate or level of controlled or sustained release will vary,
depending upon the ratio of the components employed, the
particular active composition, the method of incorporation, the
order of mixing of the components, and the like. Additional
additives may also be present that may modify the characteristics
of the matrix and its release properties.
(Id. 147.)
15. Chan also discloses that its compositions “are designed for oral
administration in the form of a pill, a lozenge, candy, an orally dissolving
film or similar product form, which [is] retained in the oral cavity for a
sufficient period to dissolve[] or disintegrate therein” (id. 1 50).
16. Chan exemplifies compositions containing 86.26 wt.% and
85.45 wt.% mannitol, respectively, as well as compositions containing
97.684 wt.%, 93.952 wt.%, and 96.452 wt.% isomalt, respectively (id.
11 58-59 & 65).
Analysis
In our analysis of the first two rejections, we will initially focus on
independent claim 1. We will separately discuss claim 48, which is also
independent, below.
Claim 1
Dam discloses “a glassy lozenge for buccal drug delivery comprising:
a) a matrix; b) an active agent[, such as nicotine]; [and] c) water; . . .
wherein the matrix comprises (i) at least one gum and (ii) at least one non-
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crystallising sugar or non-crystallising sugar alcohol” (Finding of Fact (FF)
4 & 8). Dam also discloses that the “ratio of matrix components can be
varied to vary the dissolution profile” (FF 7). In particular, Dam discloses
that “a reduced gum content will result in faster lozenge dissolution” (FF 6).
In addition, Dam discloses that, “[tjypically, the matrix comprises from 40-
90% of the gum component and from 60-10% of the non-crystallising sugar
or non-crystallising sugar alcohol component” (FF 7).
Chan “provides an oral composition that comprises a nicotine active,
alginic acid, . . . and a polycarbophil component” (FF 11). Chan also
discloses that “fillers for use in [its] composition include, but are not limited
to, those conventionally used in the art, such as . . . acacia gum; gum arabic;
. . . mannitol; sorbitol; inositol; . . . and any combinations thereof,” and “are
generally present. . . from about 50% to about 99%” (FF 12). Chan
exemplifies compositions containing more than 80% by weight mannitol or
isomalt (FF 16). In view of Chan, we agree with the Examiner that it would
have been prima face obvious to include at least about 80% by weight sugar
alcohol in Dam’s composition in order to obtain the desired release profile
(Ans. 7).
Appellants argue, however, “that one of skill in the art would not be
led to modify the composition disclosed in Dam to arrive at a composition
comprising the recited components, including a sugar substitute in an
amount of at least about 80% by weight” (App. Br. 6). We are not
persuaded.
We understand Appellants’ position that this modification requires a
significant increase in the amount of sugar alcohol, and therefore a
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significant decrease in the amount of gum, than Dam describes as typical
(FF 7). However, as noted by the Examiner (Ans. 4), Dam makes clear that
these amounts are result effective variables (FF 6—7). See In re Antonie,
559, F.2d 618, 620 (CCPA 1977); In reAller, 220 F.2d 454, 456 (CCPA
1955). In addition, Chan specifically discloses nicotine compositions
containing the claimed amount of sugar alcohol (FF 16). Thus, we conclude
that the Examiner has the better position.
We also acknowledge Appellants’ argument that “the Dam and Chan
references are directed to entirely different goals” and that “there is nothing
in Chan that would lead one of skill in the art to predict that modifying the
teachings of Dam to include a sugar substitute in an amount of at least about
80% by weight would provide a desirable result” (App. Br. 11). However,
Dam and Chan are both directed to the buccal delivery of nicotine, such as
through a lozenge (FF 4, 8, 11, & 15). Thus, we do not agree with
Appellants that these references are directed to entirely different goals. In
addition, both references suggest that the ratio of the matrix components can
be varied to achieve the desired release profile (FF 6—7 & 14). Moreover,
Chan discloses that it was known in the art to use the claimed amount of
sugar alcohol (FF 16). Thus, we conclude that the evidence supports the
Examiner’s position that it would have been obvious to include the claimed
amount of sugar alcohol.
Appellants also argue “that the Dam reference does not teach or
suggest incorporating a sugar alcohol in the form of a syrup into the
compositions described therein” (App. Br. 11). We are not persuaded.
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The Specification states that the term “‘[s]ugar alcohol syrup’ ... is
intended to refer to a thick solution of sugar alcohol in water” (FF 3). Dam
discloses:
Dispense 276 kg of water, purified into the batch mixing
container. Heat to 70° C. and thermostatically maintain the
temperature. Add the sorbitol liquid (non-crystallizing), acacia
(spray dried) and xylitol. Heat the pre-mix slurry with stirring
for between 30 and 40 minutes maintaining a temperature of
between 68° C. and 72° C.
(FF 10.) We conclude that Appellants have not adequately explained why
Dam’s slurry is not within the scope of the definition of a sugar alcohol
syrup provided in Appellants’ Specification.
We note Appellants’ argument that the “Dam reference does not
disclose or suggest that the ‘pre-mix slurry’ is heated at a sufficient
temperature or for a sufficient period of time to result in the formation of a
‘syrup,’ as is clearly defined by the present specification” (App. Br. 12). In
addition, the Specification does states that “[s]ugar alcohol syrups are
generally prepared by heating a solution of the sugar alcohol in water and
cooling the mixture to give a viscous composition” (FF 3 (emphasis added)).
However, we agree with the Examiner that the definition of sugar alcohol
syrup does not require that the syrup be formed in this way (Ans. 11).
In addition, Appellants argue:
To achieve the stated goals of the reference, one of skill in the art
would have no reasonable expectation of success in modifying
the teachings of the Dam reference by incorporating a
significantly higher percentage of sugar substitute meeting the
recitation in the present claims of a product comprising a sugar
substitute in an amount of at least about 80% by weight (which
would obviously result in a significantly lower percentage of
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gum component). Such a significantly lower percentage of gum
component would not be expected to be capable of achieving the
desirable dissolution and release characteristics of the products
described in the Dam reference.
(App. Br. 14.) We are not persuaded.
We do not disagree with Appellants’ argument that Dam suggests
advantages of relatively slow release profiles {id. at 13—15). However, Dam
does state that “[according to an embodiment of the invention the lozenge
provides for controlled release of the active agent” (FF 5 (emphasis added)).
Thus, we agree with the Examiner that the teachings of Dam are not limited
to those compositions that provide relatively slow release (Ans. 8). In
addition, although the claimed higher amount of sugar alcohol, and therefore
a lower amount of gum, than Dam describes as typical (FF 7) may result in a
product that does not achieve all of the advantages described in Dam, we do
not agree with Appellants that there would not have been a reasonable
expectation for success, particularly in view of the disclosure in Chan.
Claim 48
Our analysis regarding claim 1 generally applies to claim 48 as well.
However, we note that claim 48 does not recite that either sugar alcohol is a
syrup. Thus, Appellants’ argument regarding a syrup does not apply to
claim 48.
Appellants additionally argue, with regard to claim 48, that “the
references ... do not teach or suggest a second sugar alcohol in an amount
of at least about 4.5% by weight and up to about 20% by weight in the
compositions described therein” (App. Br. 17). We are not persuaded.
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Dam discloses “a glassy lozenge for buccal drug delivery comprising:
a) a matrix; b) an active agent; [and] c) water; . . . wherein the matrix
comprises (i) at least one gum and (ii) at least one non-crystallising sugar or
non-crystallising sugar alcohol” (FF 4 (emphasis added)). In addition, Dam
exemplifies a composition containing both sorbitol and xylitol (FF 10).
Chan also teaches combinations of fillers and sweeteners (FF 12—13). In
addition, Chan teaches including more than 80% by weight plus 4.5% by
weight sugar alcohol (FF 16). We conclude that it would have been prima
facie obvious to apportion this amount of sugar alcohol between the claimed
first and second sugar alcohols.
Conclusion
The evidence supports the Examiner’s conclusion that Dam and Chan
suggest the compositions of claims 1 and 48. We therefore affirm the
obviousness rejections of claims 1 and 48. Claims 2, 3, and 6—20 have not
been argued separately and therefore fall with claim 1. Claims 49—52 have
not been argued separately from claim 48 and therefore fall with claim 48.
37 C.F.R. §41.37(c)(l)(iv).
II
In the third rejection, the Examiner relies on “Dam and Chan [as]
discussed above” (Final Act. 6). However, the Examiner finds that these
references “do not teach a porous particulate carrier,” as recited in, for
example, representative claim 4 {id.).
The Examiner relies on Hansson for teaching “a nicotine-containing
particulate material for release of nicotine the material comprising a
combination of nicotine or a pharmaceutically acceptable salt, complex or
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solvate thereof and a microcrystalline cellulose” (id.). In particular, the
Examiner finds that “Hansson teaches sorption of nicotine in the form of a
solution containing nicotine as a base on a microcrystalline cellulose” and
“explains that sorption of nicotine on microcrystalline cellulose particles is
beneficial because it results in a physical and chemically stable dry
particulate material with a very fast and complete release” (id.). The
Examiner concludes that “one of ordinary skill in the art at the time the
invention was made would have been motivated to sorb nicotine onto porous
particulate carriers because it results in a physical and chemically stable dry
particulate material with a very fast and complete release” (id. at 7).
Findings of Fact
17. Hansson discloses “that sorption of nicotine ... on a
microcrystalline cellulose (MCC) results in physical and chemical stable dry
particulate material with a very fast and complete release in vitro” (Hansson
110).
18. Hansson also discloses:
[Different release may be obtained in different ways. . . . [T]he
particulate material can be incorporated into compositions such
as, e.g., pharmaceutical compositions and dependent on the
specific formulation and formulation technology applied
different release patterns can be obtained. In other words, the
present invention provides a particulate material that can be
formulated to provide fast, medium and slow release of a
nicotine, and combinations of such releases.
(Id. 142.)
19. In addition, Hansson discloses: “As mentioned above, the
pharmaceutical composition may ... be designed to release the nicotine in a
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more controlled or delayed manner. . . . [M]any different release patterns
can be obtained.” {Id. 1 63.)
Analysis
In our analysis of this rejection, we will focus on claim 4. Appellants
argue that “one of skill in the art would not be led to modify the teachings of
the Dam reference based on the teachings of Hansson” (App. Br. 16). In
particular, Appellants argue: “[0]ne of skill in the art would understand that
incorporation of MCC is designed for fast release. As such, one of skill in
the art would not be led to incorporate MCC in the design of a composition
for controlled delivery of a drug.” {Id. at 16—17.) We are not persuaded.
As discussed above, we agree with the Examiner that the teachings of
Dam are not limited to those compositions that provide relatively slow
release (Ans. 8). In addition, as noted by Appellants (App. Br. 16), Hansson
discloses that “many different release patterns can be obtained” (FF 19). In
particular, Hansson discloses that its particulate material “can be formulated
to provide fast, medium and slow release of a nicotine” (FF 18). Thus, we
do not agree with Appellants that one of skill in the art would not have been
led to incorporate MCC in Dam’s composition.
Conclusion
The evidence supports the Examiner’s conclusion that Dam, Chan,
and Hansson suggest the composition of claim 4. We therefore affirm the
obviousness rejection of claim 4. Claims 1—3 and 5—27 have not been
argued separately and therefore fall with claim 4. 37 C.F.R.
§ 41.37(c)(l)(iv).
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SUMMARY
We affirm the obviousness rejections of claims 1, 2, 6—14, 48—50, and
52 over Dam and Chan; of claims 1—3, 6—20, and 51 over Dam and Chan;
and of claims 1—27 over Dam, Chan, and Hansson.
TIME PERIOD FOR RESPONSE
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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