Haksar, Priyanka Bansilal. et al.

Patent Trials and Appeals Board

Oct 18, 2019

14416171 - (D) (P.T.A.B. Oct. 18, 2019)

UNITED STA TES p A TENT AND TRADEMARK OFFICE
APPLICATION NO. FILING DATE FIRST NAMED INVENTOR
14/416,171 01/21/2015 Priyanka Bansilal Haksar
151167 7590 11/12/2019
Gruneberg and Myers PLLC
1775 Tysons Blvd
5th Floor
Tysons, VA 22102
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.
000278US 3913
EXAMINER
CHANNA V AJJALA, LAKSHMI SARADA
ART UNIT PAPER NUMBER
1611
NOTIFICATION DATE DELIVERY MODE
11/12/2019 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):
patent@gandmpatent.com
kg@gandmpatent.com
em@gandmpatent.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte PRIY ANKA BANSILAL HAKSAR,
SHRADDHA SANJEEV JOSHI, HARSH SHAH, PREETI PATIL,
and SMITHA SHETTY1
Appeal2019-000013
Application 14/416,171
Technology Center 1600
Before ERIC B. GRIMES, ULRIKE W. JENKS, and
MICHAEL A. VALEK, Administrative Patent Judges.
GRIMES, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134(a) involving claims to a
pharmaceutical or nutraceutical composition, which have been rejected as
obvious. We have jurisdiction under 35 U.S.C. § 6(b).
We AFFIRM.
1 Appellant identifies the Real Party in Interest as Evonik Rohm GmbH.
Appeal Br. 1. We use the word Appellant to refer to "applicant" as defined
in 37 C.F.R. § l.42(a).
Appeal2019-000013
Application 14/416,171
STATEMENT OF THE CASE
"Pharmaceutical or nutraceutical compositions are designed to release
the active ingredient in a manner of reproducible release curves." Spec. 1.
"[T]he release of active ingredient ... can be altered by ... the use of
ethanol or ethanol-containing drinks." Id. at 2.
[A] gastric resistant coating layer compris[ing] 10 to 100 % by
weight of one or more salts of alginic acid ... solves the
problem [ ofJ protection against the influence of ethanol.
However except for coatings which include the ammonium
alginate, coatings which employ other alginate salts, like
sodium or potassium alginate, show no resistance against the
influence of calcium ions at the same time.
Id. at 1. "[S]ituations w[h Jere considerable amounts of calcium ions are
present in the food and are ingested together with the pharmaceutical or
nutraceutical composition ... can for instance happen when diary [sic]
products such like milk or yoghurt are consumed simultaneously." Id. at 3.
The Specification discloses "a pharmaceutical or nutraceutical composition
for sustained or extended release with a release profile which is resistant
against the influence of ethanol and also resistant against the influence of
calcium ions." Id. at 4.
Claims 1-18 are on appeal. Claim 1 is the only independent claim and
reads as follows:
Claim 1. A pharmaceutical or nutraceutical composition,
compnsmg:
a) a core, comprising a pharmaceutical or a
nutraceutical active ingredient;
b) an inner coating layer comprising a salt of alginic
acid; and
2
Appeal2019-000013
Application 14/416,171
c) an outer coating layer comprising a polymer or
copolymer which is insoluble in water over a pH range of 1-14:
wherein a ratio by weight of the amount of the salt of
alginic acid in the inner coating layer to the amount of the
water-insoluble polymer or copolymer in the outer coating layer
is from 2.5: 1 to 15: 1.
OPINION
The Examiner has rejected claims 1-18 under 35 U.S.C. § I03(a) as
obvious based on Bodinge2 and Kim. 3 Ans. 3. The Examiner finds that
Bodinge discloses a composition comprising a pharmaceutical or
nutraceutical active ingredient-containing core, and a gastric-resistant
coating layer comprising a salt of alginic acid. Id. The Examiner finds that
Bodinge discloses that its gastric-resistant coating can also include water-
insoluble polymers "that are swellable but not soluble over a pH range of 1-
14," such as Eudragit NE 30D or NM 30D. Id. at 4. The Examiner finds that
"[f]or the claimed ratio of alginic acid and water-insoluble polymers, several
examples, for instance, examples 2, 4--11, include amounts that render the
claimed ratios." Id.
"Bodinge also teaches that in certain embodiments, it is useful to have
two or more gastric resistant enteric coatings," but "fails to teach the inner
and outer coatings claimed in the instant invention, where the inner coating
is alginic acid and outer coating is water insoluble coating." Id. at 5. The
Examiner finds that Kim teaches "an enteric coated granule prepared by
coating lactic acid bacteria-containing seed with a water-miscible coating
2 Bodinge et al., WO 2012/022498 Al, pub. Feb. 23, 2012.
3 Kim et al., US 6,365,148 Bl, iss. Apr. 2, 2002.
3
Appeal2019-000013
Application 14/416,171
material as a first coating and a controlled-release coating material as a
second coating material." Id. The Examiner finds that Kim teaches that the
water-miscible coating material can be sodium alginate, and "Kim suggests
coating the inner water miscible coating with an enteric coating material."
Id. "Kim teaches that the above coating enables high survival rates for lactic
acid bacteria." Id.
The Examiner concludes that it would have been obvious to modify
Bodinge' s composition to "coat the core with two layers of gastric resistant
polymers i.e., salts of alginic acid as an inner coating and a pH independent
water insoluble polymer such as Eudragit NE30D or Eudragit NM 30D, as
an outer coating" because "Kim suggests providing alginic acid salts as an
inner coating and an outer coating containing controlled release polymer
coating that can include pH independent water insoluble polymers such as
ethyl cellulose." Id. at 6. The Examiner finds that a "skilled artisan would
have been able to choose to employ the polymers as separate coatings or a
single coating depending on the ease of application of the different polymers
when coating the core." Id.
Alternatively, the Examiner reasons that it would have been obvious
to modify Kim's composition
to coat with an outer water insoluble polymer layer such as
ethyl cellulose (pH independent) taught by Kim or by
employing the pH independent water insoluble polymer such as
Eudragit NE30D or Eudragit NM 30D, because Bodinge
teaches the combination of alginic acid salts and water
insoluble pH independent polymers provide protection against
inactivation of active agents at stomach pH.
Id. at 7. The Examiner finds that "a skilled artisan would have employed the
above polymers in the claimed ratios because Bodinge also teaches the
4
Appeal2019-000013
Application 14/416,171
claimed ratios for a controlled release of the active agent i.e., less release at
pH 1.2 and higher release rates at pH 6.8, which is unaffected by the
presence of ethanol or calcium ions." Id.
We agree with the Examiner that the claimed composition would have
been obvious in view of Bodinge and Kim. Bodinge discloses "a gastric
resistant pharmaceutical or nutraceutical composition, comprising a core,
comprising a pharmaceutical or nutraceutical active ingredient and a gastric
resistant coating layer onto the core, ... wherein the gastric resistant coating
layer comprises 10 to 100 % by weight of one or more salts of alginic acid."
Bodinge 3. The alginic acid salt can be sodium alginate. Id. at 6. The
disclosed dosage form is said to solve the problem of an increased release
rate of the active agent in the stomach in the presence of ethanol. Id.
Bodinge discloses that one preferred use of its composition is "for
enteric coated pharmaceutical dosage forms." Id. at 10. "Therapeutical and
chemical classes of drugs used in enteric coated pharmaceutical dosage
forms are for instance analgetics, antibiotics or anti-infectives, ...
therapeutical bacteria," etc. Id.
Bodinge discloses that, in addition to a salt of alginic acid, "[t]he
gastric resistant coating layer may comprise ... one or more water-insoluble
polymers or one or more cellulosic polymers." Id. at 6. "Water-insoluble
polymers in the sense of the invention are polymers which do not dissolve in
water or are only swellable in water over of the whole range of pH 1-14."
Id. at 7. Bodinge discloses that suitable water-insoluble polymers include
Eudragit® NE/NM or Eudragit® RL/RS polymers. Id.
5
Appeal2019-000013
Application 14/416,171
Bodinge provides examples of its coated dosage forms, several of
which have coatings with alginate contents of 75-83% (i.e., alginate:water-
insoluble polymer ratios of 3: 1 to -5: 1 ). Id. at 17 (Examples 4--11 ).
Bodinge discloses that "[i]n certain embodiments it may be useful to
have two or more different gastric resistant coatings layers." Id. at 16.
Bodinge states that its Example 40 composition includes an inner layer
comprising a disintegrant and an outer layer lacking a disintegrant: "In this
case the inner coating accelerates the drug release in pH 6.8 buffer without
affecting the enteric properties at pH 1.2. The outer coating alone would not
show th[is] combination of properties." Id.
Kim states that "ingested lactic acid bacteria prevent the abnormal
fermentation of food and activate the function of intestine." Kim 1: 16-17.
Kim discloses that "when lactic acid bacteria are first coated with a specific
water-miscible coating material and then, if desired, second coated with a
conventional controlled-release coating material, ... the coated granule ...
safely protect[ s] lactic acid bacteria from the attack of gastric juice." Id. at
2: 15-26. "[SJ odium alginate is preferably used as the water-miscible first
coating material." Id. at 3 : 16-18.
Kim discloses that "the first coated granule of lactic acid bacteria ...
is sufficiently effective by itself, but it can be more effectively used after
second coating with a conventional controlled-release coating material." Id.
at 3:34--37. Kim states that suitable materials for the second coating include
"sodium alginate, alginic acid, polymethylmethacrylate, for example,
Eudragit L30D, Eudragit LS30D, Kollicoat MAE 3DP (manufactured by
BASF Co.), etc." Id. at 3:48-51.
6
Appeal2019-000013
Application 14/416,171
The composition of claim 1 would have been obvious to a person of
ordinary skill in the art in view of these teachings. Bodinge discloses a
dosage form comprising a core comprising a pharmaceutical active agent,
which can be therapeutical bacteria. Similarly, Kim discloses a dosage form
comprising lactic acid bacteria, to improve digestion.
Bodinge discloses that coating its active agent with a layer comprising
10-100% of an alginate salt, such as sodium alginate, prevents increased
release of the active agent in the presence of ethanol. Kim discloses that
coating lactic acid bacteria, preferably with sodium alginate, protects the
bacteria from attack by gastric acid.
Bodinge discloses that its gastric-resistant coating can also comprise
water-insoluble polymers such as Eudragit® NE/NM or Eudragit® RL/RS
polymers. Bodinge exemplifies coatings that comprise 75-83% sodium
alginate and 25-17% of a Eudragit® polymer. Bodinge also suggests that "it
may be useful to have two or more different gastric resistant coating[]
layers." Bodinge 16.
Kim discloses that, in addition to the first coating layer of (preferably)
sodium alginate, its composition is "more effectively used after second
coating with a conventional controlled-release coating material." Kim 3:34--
37. Among the polymers that Kim suggests for its second coating layer are
Eudragit L30D and Eudragit LS30D.
Thus, it would have been obvious to formulate Bodinge's dosage form
to include lactic acid bacteria (therapeutical bacteria) as the active agent, an
inner layer comprising 7 5-83 % sodium alginate and 25-17% Eudragit
polymer, and an outer layer comprising 75-83% sodium alginate and 25-
7
Appeal2019-000013
Application 14/416,171
17% Eudragit polymer. Bodinge exemplifies coating having these amounts
of sodium alginate and Eudragit polymers, and expressly suggests including
more than one coating layer in its dosage form. In addition, Kim discloses
that a second coating of, for example, sodium alginate or a Eudragit polymer
increases the effectiveness of a lactic acid bacteria-containing dosage form.
The layers exemplified by Bodinge, and combined as suggested by
both Bodinge and Kim, result in a ratio of sodium alginate in the inner layer
to Eudragit polymer in the outer layer of between 3:1 (two layers of75%
sodium alginate, 25% Eudragit) and -5: 1 ( two layers of 83 % sodium
alginate, 17% Eudragit). The cited references thus would have made obvious
the ratios recited in instant claims 1 and 18.
Appellant argues that Kim "is not from the same field of endeavor as
the claimed invention nor is it reasonably pertinent to the problem faced by
the inventor and is non-analogous art." Appeal Br. 3. Appellant argues that
"[t]he field of endeavor of Kim et al. is to deliver acid sensitive lactic acid
bacteria to the intestine, avoiding the acidic gastric environment," whereas
"the object of the claimed invention is a pharmaceutical or nutraceutical
composition designed to release the active ingredient in a manner of
reproducible release curves." Id. at 4. Appellant also argues that Kim "is
not reasonably pertinent to the problem of sustained release under conditions
of simulated gastric fluid since the object of Kim et al. is to avoid release of
lactic acid [bacteria] in the stomach." Id. at 6 (emphasis omitted).
This argument is not persuasive. "In order to rely on a reference as a
basis for rejection of the applicant's invention, the reference must either be
in the field of the applicant's endeavor or, if not, then be reasonably
8
Appeal2019-000013
Application 14/416,171
pertinent to the particular problem with which the inventor was concerned."
In re Oetiker, 977 F.2d 1443, 1447 (Fed. Cir. 1992). In this case, Kim,
Bodinge, and the instant claims are all pertinent to the problem of delivering
therapeutical bacteria, such as lactic acid bacteria, to a subject. See Kim
2:17-27; Bodinge 10; Spec. 18-19. Thus, Kim is reasonably pertinent to the
problem with which Appellant and Bodinge were concerned, and is therefore
analogous art.
Appellant argues that deriving the ratios required by the claims from
Bodinge requires "cherry pick[ing]" from Bodinge's working examples,
because only nine of the twenty-nine examples include alginate:polymer
ratios within the claimed range. Appeal Br. 9. Appellant also argues that
Bodinge "provides no guidance of a ratio of alginic acid salt in an inner
coating to water-insoluble polymer in an outer coating." Id. Similarly,
Appellant argues that claim 18 requires a ratio between 4: 1 and 12: 1, and
"[ o ]f the 29 illustrative inventive examples, 27 examples fail to illustrate a
mixture ratio of 4--12: 1. Given the lack of suggestion of two separate layers
and the breadth of disclosure outside the range of 4--12: 1, the claimed ratio
of 4--12:1 would not have been obvious." Id. at 12.
These arguments are not persuasive. As discussed above, Kim states
that a lactic acid bacteria-containing dosage form is more effective if a
coating of sodium alginate is covered with a second coating of, for example,
sodium alginate or a Eudragit polymer. Bodinge expressly suggests using
multiple coating layers on its dosage form, and exemplifies coatings having
mixtures of 75-83% sodium alginate and 25-17% Eudragit. When
considered together, these teachings would have provided a reason to coat a
9
Appeal2019-000013
Application 14/416,171
therapeutical bacteria active agent (e.g., lactic acid bacteria) with two of the
coating layers exemplified by Bodinge, which would result in a ratio of
alginate in the inner layer to water-insoluble polymer in the outer layer
between 3: 1 (75%:25%) and -5: 1 (83%: 17%).
Finally, Appellant argues that
the Examiner asserts that one of skill in the art would have
expected, after modification of the coating with an outer layer
of a water-insoluble polymer, to achieve release of active agent
at gastric pH within the first 2 hours which is less than at pH
6.8 after 2 hours.
Contrary to the Examiner's assertion, one of ordinary skill in
the art would have expected an outer coating of a water-
insoluble polymer to alter the desired release characteristics of
not more than 15% at pH 1.2 for 2 hours and at least 50% at pH
6.8 for one hour, such that there would have been no motive to
provide a separate coating of a water-insoluble polymer
overlying the gastric resistant coating of Bodinge et al.
Appeal Br. 10.
This argument is not persuasive because, regardless of the rate of
release that would have been expected at different pHs, Kim provides a
reason to include an outer coating layer in Bodinge' s dosage form for
therapeutical bacteria, because Kim teaches that the additional coating layer
( e.g., of sodium alginate or a Eudragit polymer) increases the effectiveness
of administering lactic acid bacteria.
Claims 2-17 were not argued separately and therefore fall with claims
1 and 18. 37 C.F.R. § 4I.37(c)(l)(iv).
10
Appeal2019-000013
Application 14/416,171
In summary:
DECISION SUMMARY
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). See 37 C.F.R.
§ 1.136(a)(l )(iv).
AFFIRMED
11