Ex Parte Gordon

Board of Patent Appeals and Interferences

Nov 15, 2010

10762714 (B.P.A.I. Nov. 15, 2010)

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.
10/762,714 01/22/2004 Maxwell Gordon 1360-001 5204
47888 7590 11/15/2010
HEDMAN & COSTIGAN, P.C.
1230 AVENUE OF THE AMERICAS
7th floor
NEW YORK, NY 10020
EXAMINER
CLAYTOR, DEIRDRE RENEE
ART UNIT PAPER NUMBER
1627
MAIL DATE DELIVERY MODE
11/15/2010 PAPER
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.
PTOL-90A (Rev. 04/07)

UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
__________

Ex parte MAXWELL GORDON
__________

Appeal 2010-007607
Application 10/762,714
Technology Center 1600
__________

Before DEMETRA J. MILLS, LORA M. GREEN, and
JEFFREY N. FREDMAN, Administrative Patent Judges.

FREDMAN, Administrative Patent Judge.

DECISION ON APPEAL1
This is an appeal under 35 U.S.C. § 134 involving claims to a
pharmaceutical dosage form. The Examiner rejected the claims as obvious.
We have jurisdiction under 35 U.S.C. § 6(b). We affirm.

1 The two-month time period for filing an appeal or commencing a
civil action, as recited in 37 C.F.R. § 1.304, or for filing a request
for rehearing, as recited in 37 C.F.R. § 41.52, begins to run from
the “MAIL DATE” (paper delivery mode) or the
“NOTIFICATION DATE” (electronic delivery mode) shown on
the PTOL-90A cover letter attached to this decision.
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Statement of the Case
The Specification teaches that the “invention relates to solid dosage
forms of oral analgetic drugs which are effective for pain control(or treating
diarrhea) and are not adapted for recovery of the opiate analgetic” (Spec. 1,
ll. 17-20).
The Claims
Claims 1-6, 16-18, 21 and 22 are on appeal. Claims 1, 6, and 16 are
representative. Claims 1, 6, and 16 read as follows:
1. A solid pharmaceutical dosage form which
comprises an opiate, an opiate antagonist and an
amount of hydrocolloids and other excipients
including starch, lactose, xanthan gum, locust bean
gum, monobasic calcium phosphate, dibasic
calcium phosphate, microcrystalline cellulose,
propylene glycol alginate, zein and magnesium
stearate which are effective to form a viscous, non-
injectable matrix when said dosage form is
contacted with water.

6. A solid pharmaceutical dosage form as defined
in claim 1 which includes an amount of enteric
coated opiate antagonist pellets which is effective
to reduce or eliminate the constipating effects of
oycodone, methadone, morphine, codeine,
dilaudid, pantopon, paregoric, pentazocine,
buprenorphine, fentanyl, oxymorphone,
hydromorphone, hydrocodone, propoxyphene,
nalbuphine and meperidine.

16. A solid pharmaceutical dosage form which
comprises a controlled release dosage form of an
opiate, an opiate antagonist and a hydrocolloid and
excipients as defined in claim 1, wherein said
opiate, an opiate antagonist, hydrocolloid and
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excipients are formulated into pellets (a); pellets
(b) and pellets (c) ;
pellets (a) comprise about one-third of said
opiate, opiate antagonist and hydrocolloid in an
immediate release form;
pellets (b) comprise about one-third of said
opiate, opiate antagonist, hydrocolloid and
excipients in an a delayed release form which
releases substantially all contents of the pellets in
the jejunum; and
pellets (c) comprise about one-third of said
opiate, opiate antagonist, hydrocolloid and
excipients in a delayed release form which
substantially all of the contents of the pellets in the
ileum.

The issue
The Examiner rejected claims 1-6, 16-18, 21, and 22 under 35 U.S.C.
§ 103(a) as obvious over Oshlack2 and Meissner3 (Ans. 3-5).
The Examiner finds that “Oshlack et al. teach solid dosage forms of
compositions comprised of an opiate, an opiate antagonist and a
hydrocolloid containing excipient” (Ans. 3). The Examiner finds that
“Meissner et al. teaches improved laxation during oral naloxone treatment in
opioid-associated constipation” (Ans. 5). The Examiner finds it obvious “to
formulate a composition comprised of an opiate, an opiate antagonist,
hydrocolloids and other excipients as exemplified in claim 1 because
Oshlack et al. teach the suitability of all of the hydrocolloids and excipients

2 Oshlack et al., US 7,144,587 B2, issued Dec. 5, 2006.
3 Meissner et al., Oral naloxone reverses opioid-associated
constipation, 84 PAIN 105-109 (2000).
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in a composition of coated beads with an opiate and an opiate antagonist”
(Ans. 5).
Appellant contends that it “is not seen how a reference can make
obvious a formulation having ingredients that are not disclosed by the
reference. Oshlack teaches the use of sequestered aversive agents that impart
a bitter, irritant or gelling effect when the dosage form is not used for its
intended use” (App. Br. 4). Appellant argues that an “opiate antagonist that
is sequestered or non-available may be added to the Oshlack teachings but
such a sequestered agent can have no role in reducing or prevent
constipation according to composition claim 6 and method claim 22 which
both utilize an enteric” (App. Br. 4-5).
Appellant contends that “[c]laim 16 points out a specific three pellet
formulation where the pellets are formulated to release the drugs in specific
anatomical locations of the small intestine. This formulation is also not made
obvious by Oshlack and/or Meissner” (App. Br. 5).
The issue with respect to this rejection is: Does the evidence of record
support the Examiner’s conclusion that Oshlack and Meissner render
obvious the claimed solid pharmaceutical dosage forms?
Findings of Fact
1. Oshlack teaches “preventing or deterring of the abuse of opioid
analgesics by the inclusion of an opioid antagonist and at least one aversive
agent in the dosage form with the opioid analgesic” (Oshlack, col. 6, ll. 17-
20).
2. Oshlack teaches that “various gelling agents can be employed
including . . . starch and starch derivatives, cellulose derivatives, such as
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microcrystalline cellulose, . . . xanthan gum, . . . polyethylene glycol, . . .
mixed surfactant/wetting agent systems, emulsifiers, other polymeric
materials, and mixtures thereof” (Oshlack, col. 7, ll. 23-36).
3. Oshlack teaches that when “being formulated as a tablet, the
aversive agent and opioid agonist and opioid antagonist may be combined
with one or more inert, non-toxic pharmaceutical excipients which are
suitable for the manufacture of tablets. Such excipients include, for example,
an inert diluent such as lactose” (Oshlack, col. 16, ll. 50-55).
4. Oshlack teaches that “[o]ther gelling agents such as . . .
alginates . . . locust bean gum . . . could also be used as gelling agents”
(Oshlack, col. 35, ll. 26-32).
5. Oshlack teaches a formulation in Example 6 which comprises
dicalcium phosphate (see Oshlack, Example 6, col. 39, l. 34).
6. Oshlack teaches that in “certain embodiments of the dosage
forms of the present invention may also include a surfactant. Surfactants
useful in accordance with the present invention, include for example . . .
propylene glycol” (Oshlack, col. 32, ll. 48-65).
7. Oshlack teaches that in “certain embodiments, a sustained
release coating is applied to the sustained release spheroids, granules, or
matrix multiparticulates. In such embodiments, the sustained-release coating
may include . . . zein” (Oshlack, col. 25, ll. 4-9).
8. Oshlack teaches a formulation in Example 1 which comprises
magnesium stearate (see Oshlack, Example 1, col. 35, l. 50).
9. Oshlack teaches that the “aversive agent can be combined with
an enteric carrier to delay its release or combined with a carrier to provide a
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sustained release of the aversive agent” (Oshlack, col. 4, ll. 12-15). Oshlack
also teaches that “the antagonist . . . can be an antagonist with minimal oral
activity such as naloxone in releasable or ‘non-sequestered’ form” (Oshlack,
col. 4, ll. 35-37).
10. Oshlack teaches that the formulation “can be formulated as an
immediate release formulation or controlled release oral formulation in any
suitable tablet, coated tablet or multiparticulate formulation known to those
skilled in the art” (Oshlack, col. 17, ll. 12-17).
11. The Examiner finds that “the teaching of dicalcium phosphate
renders the monocalcium phosphate obvious because the compounds are
similar and have similar properties of being excipients” (Ans. 4)).
12. Meissner teaches that “[o]pioid-related constipation is one of
the most frequent side effects in chronic pain patients, sometimes to the
extent that treatment with morphine and other opioids must be reduced”
(Meissner 105, col. 1).
13. Meissner teaches that “[p]atients preferred naloxone to the
previously used laxatives because of the stronger effect, the rapid onset of
laxation, and the unpleasant taste of lactulose” (Meissner 108, col. 2).
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’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. Moreover, an “[e]xpress suggestion to substitute
one equivalent for another need not be present to render such substitution
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obvious.” In re Fout, 675 F.2d 297, 301 (CCPA 1982). As noted by the
Court in KSR, “[a] person of ordinary skill is also a person of ordinary
creativity, not an automaton.” 550 U.S. at 421.
Analysis
Claim 1
Oshlack teaches “preventing or deterring of the abuse of opioid
analgesics by the inclusion of an opioid antagonist and at least one aversive
agent in the dosage form with the opioid analgesic” (Oshlack, col. 6, ll. 17-
20; FF 1). Meissner teaches that “[o]pioid-related constipation is one of the
most frequent side effects in chronic pain patients, sometimes to the extent
that treatment with morphine and other opioids must be reduced” (Meissner
105, col. 1; FF 12). Meissner teaches that “[p]atients preferred naloxone to
the previously used laxatives because of the stronger effect, the rapid onset
of laxation, and the unpleasant taste of lactulose” (Meissner 108, col. 2; FF
13).
Applying the KSR standard of obviousness to the findings of fact, we
conclude that the person of ordinary creativity would have predictably
incorporate naloxone into the opioid analgesic of Oshlack to reduce any
opioid related constipation taught as a problem by Meissner (FF 12-13).
Further, the ordinary practitioner would have used components taught or
rendered obvious by Oshlack for the composition (FF 1-8, 11). Such a
combination is merely a “predictable use of prior art elements according to
their established functions.” KSR, 550 U.S. at 417.
Appellant contends that it “is not seen how a reference can make
obvious a formulation having ingredients that are not disclosed by the
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reference. Oshlack teaches the use of sequestered aversive agents that impart
a bitter, irritant or gelling effect when the dosage form is not used for its
intended use” (App. Br. 4).
We are not persuaded. Oshlack teaches, or renders obvious, each of
the components of Claim 1 for use in opioid compositions, specifically
teaching the use of starch (FF 2), lactose (FF 3), xanthum gum (FF 2), locust
bean gum (FF 4), monobasic calcium phosphate (FF 11), dibasic calcium
phosphate (FF 5), microcrystalline cellulose (FF 2), propylene glycol (FF 6),
alginate (FF 4), zein (FF 7) and magnesium stearate (FF 8).
While we are fully aware that hindsight bias often plagues
determinations of obviousness, Graham v. John Deere Co., 383 U.S. at 36,
we are also mindful that the Supreme Court has clearly 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 401. This reasoning is applicable, since the instant invention simply
combines components taught or rendered obvious by Oshlack and Meissner
for their predictable functions (FF 1-13). Appellant has provided no
evidence of any secondary consideration (see App. Br. 4-5).
Claims 6 and 22
Appellant argues that an “opiate antagonist that is sequestered or non-
available may be added to the Oshlack teachings but such a sequestered
agent can have no role in reducing or prevent constipation according to
composition claim 6 and method claim 22 which both utilize an enteric”
(App. Br. 4-5).
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We are not persuaded. Oshlack specifically teaches that the “aversive
agent can be combined with an enteric carrier to delay its release or
combined with a carrier to provide a sustained release of the aversive agent”
(Oshlack, col. 4, ll. 12-15; FF 9). Oshlack also teaches that in “certain
embodiments, a sustained release coating is applied to the sustained release
spheroids, granules, or matrix multiparticulates. In such embodiments, the
sustained-release coating may include . . . zein” (Oshlack, col. 25, ll. 4-9; FF
7). We also agree with the Examiner that “Oshlack teaches that the
antagonist can be in a sequestered form as well as a non-sequestered form
(see Col. 4, lines 35-45). Therefore, an antagonist such as naloxone will be
available to reduce constipation” (Ans. 6; see FF 4).
Claim 16
Appellant argues that “[c]laim 16 points out a specific three pellet
formulation where the pellets are formulated to release the drugs in specific
anatomical locations of the small intestine. This formulation is also not made
obvious by Oshlack and/or Meissner” (App. Br. 5).
We are not persuaded. Oshlack teaches that the formulation “can be
formulated as an immediate release formulation or controlled release oral
formulation in any suitable tablet, coated tablet or multiparticulate
formulation known to those skilled in the art” (Oshlack, col. 17, ll. 12-17; FF
10). Thus, Oshlack specifically suggests multiparticulate formulations
which may be composed of immediate and controlled release particles (FF
10). Appellant does not explain why claim 16 would have been unobvious
over Oshlack’s teaching by showing some unobvious result or secondary
consideration.
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Conclusion of Law
The evidence of record support the Examiner’s conclusion that
Oshlack and Meissner render obvious the claimed solid pharmaceutical
dosage forms.
SUMMARY
In summary, we affirm the rejection of claims 1, 6, 16, and 22 under
35 U.S.C. § 103(a) over Oshlack and Meissner. Pursuant to 37 C.F.R. §
41.37(c)(1)(vii)(2006), we also affirm the rejection of claims 1-5, 17, 18,
and 21, 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)(1)(iv)(2006).

AFFIRMED

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HEDMAN & COSTIGAN, P.C.
1230 AVENUE OF THE AMERICAS
7th floor
NEW YORK NY 10020