Trials@uspto.gov
`571.272.7822
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` Paper No. 47
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` Entered: November 8, 2017
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`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`AMNEAL PHARMACEUTICALS, LLC,
`Petitioner,
`
`v.
`
`PURDUE PHARMA L.P.,
`THE P.F. LABORATORIES, INC., and
`PURDUE PHARMACEUTICALS L.P.,
`Patent Owner.
`____________
`
`Case IPR2016-01028
`Patent 9,060,976 B2
`____________
`
`
`Before LORA M. GREEN, CHRISTOPHER G. PAULRAJ, and
`JACQUELINE T. HARLOW, Administrative Patent Judges.
`
`PAULRAJ, Administrative Patent Judge.
`
`
`
`FINAL WRITTEN DECISION
`Determining That Claim 1 Has Been Shown To Be Unpatentable
`35 U.S.C. § 318(a) and 37 C.F.R. § 42.73
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`INTRODUCTION
`
`Amneal Pharmaceuticals LLC (“Petitioner”) filed a Petition
`requesting an inter partes review of claim 1 of U.S. Patent No. 9,060,976 B2
`(Ex. 1001, “the ’976 patent”). Paper 2 (“Pet.”). The P.F. Laboratories, Inc.,
`Purdue Pharma L.P., and Purdue Pharmaceuticals L.P. (collectively, “Patent
`Owner”) filed a Preliminary Response to the Petition. Paper 9 (“Prelim.
`Resp.”). We determined that the information presented in the Petition
`demonstrated that there was a reasonable likelihood that Petitioner would
`prevail in challenging claim 1 as unpatentable under 35 U.S.C. § 103(a).
`Pursuant to 35 U.S.C. § 314, the Board instituted trial on November 9, 2016,
`as to that claim of the ’976 patent. Paper 12 (“Institution Decision” or “Inst.
`Dec.”).
`Following our institution, Patent Owner filed a Response to the
`Petition (Paper 16, “PO Resp.”) and Petitioner filed a Reply to Patent
`Owner’s Response (Paper 19, “Reply”). Pursuant to our authorization,
`Patent Owner also filed a Sur-Reply (Paper 39, “PO Sur-Reply”). An oral
`hearing was held on August 2, 2017. The transcript of the hearing has been
`entered into the record. Paper 46 (“Tr.”).
`We have jurisdiction under 35 U.S.C. § 6. This Final Written
`Decision is issued pursuant to 35 U.S.C. § 318(a) and 37 C.F.R. § 42.73.
`Based on the record before us, we conclude that Petitioner has demonstrated
`by a preponderance of the evidence that claim 1 of the ’976 patent is
`unpatentable as obvious.
`Related Proceedings
`A.
`The ’976 patent is asserted against Petitioner in two civil actions
`pending in the United States District Court for the District of Delaware
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`captioned Purdue Pharma L.P. et al. v. Amneal Pharmaceuticals LLC, 15-
`cv-831, filed September 17, 2015 (Ex. 1007), and Purdue Pharma L.P. et al.
`v. Amneal Pharmaceuticals LLC, 15-cv-1152, filed December 15, 2015 (Ex.
`1008). Pet. 1.
`
`Furthermore, the claims of U.S. Patent No. 8,337,888 B2 (Ex. 1002,
`the ’888 patent), of which the ’976 patent is a continuation (Ex. 1001), were
`also asserted against Petitioner, and were held invalid in a district court
`proceeding in the Southern District of New York captioned Purdue Pharma
`L.P. et al. v. Amneal Pharmaceuticals LLC, No. 13-cv-3372 (“the SDNY
`Litigation”). The Federal Circuit upheld the invalidity of those claims on
`April 8, 2016. Ex. 1004.
`
`Additionally, Petitioner filed a separate Petition challenging the
`validity of claim 1 of the ’976 patent. See Case IPR2016-01027, Paper 1.
`IPR2016-01027 is being decided concurrently with the instant proceeding.
`The ’976 Patent (Ex. 1001)
`B.
`The ’976 patent issued on June 23, 2015, with Curtis Wright,
`
`Benjamin Oshlack, and Christopher Breder as the listed co-inventors.
`Ex. 1001. The ’976 patent is a continuation of application number
`13/349,449, which issued as the ’888 patent. Id. The ’976 patent claims
`priority to a non-provisional application (No. 10/214,412) filed August 6,
`2002 and a provisional application (No. 60/310.534) filed August 6, 2001.
`Id.
`The ’976 patent relates generally to a controlled release formulation of
`
`oxycodone, which has been marketed by Patent Owner under the tradename
`“OxyContin.” Id. at 1:46–48. As noted in the SDNY Litigation,
`OxyContin, which was originally approved in 1995, has been at the center of
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`the current national opioid abuse epidemic, and Patent Owner stopped
`selling the original formulation in 2010 because it was susceptible to
`tampering and abuse. Ex. 1003, 28–29. The invention claimed in the ’976
`patent stems from Patent Owner’s efforts to develop an abuse-deterrent
`alternative to the original formulation.
`In this respect, the ’976 patent notes that “[o]pioid analgesics are
`sometimes the subject of abuse.” Ex. 1001, 1:17. According to the ’976
`patent, the opioid analgesic may be more potent when injected after mixing
`with a suitable vehicle, or when crushed and administered orally or nasally.
`Id. at 1:18‒29. The ’976 patent discloses that “[o]pioid antagonists have
`been combined with certain opioid agonists in order to deter the parenteral
`abuse of opioid agonists,” but states that there is still a need of opioid dosage
`forms that are less subject to abuse Id. at 1:32‒34, 2:9‒11.
`
`Thus, the ’976 patent discloses “oral dosage forms . . . comprising an
`opioid analgesic; and an aversive agent or agents as a component(s) of the
`dosage form helps to prevent injection, inhalation, and/or oral abuse by
`decreasing the ‘attractiveness’ of the dosage form to a potential abuser.” Id.
`at 2:42‒47. The ’976 patent defines “aversive agent” as “a bittering agent,
`an irritant, a gelling agent, or combinations thereof.” Id. at 4:12‒14.
`
`According to the ’976 patent:
`In certain embodiments of the present invention, the
`dosage form comprises an aversive agent such as a gelling agent
`to discourage an abuser from tampering with the dosage form
`and thereafter inhaling, injecting, and/or swallowing the
`tampered dosage form. Preferably, the gelling agent is released
`when the dosage form is tampered with and provides a gel-like
`quality to the tampered dosage form which slows the absorption
`of the opioid analgesic such that an abuser is less likely to obtain
`a rapid “high”. In certain preferred embodiments, when the
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`dosage form is tampered with and exposed to a small amount
`(e.g., less than about 10 ml) of an aqueous liquid (e.g., water),
`the dosage form will be unsuitable for injection and/or inhalation.
`Upon the addition of the aqueous liquid, the tampered dosage
`form preferably becomes thick and viscous, rendering it
`unsuitable for injection.
`Id. at 2:64‒3:11. Moreover, upon contact with the mucous membranes of
`the nasal passages the gelling agent may also become a gel, which sticks to
`the nasal passage, minimizing absorption of the opioid. Id. at 3:25‒30.
`
`The ’976 teaches as to the gelling agent:
`In certain embodiments of the present invention wherein
`the dosage form includes an aversive agent comprising a gelling
`agent, various gelling agents can be employed including, for
`example and without limitation, sugars or sugar derived alcohols,
`such as mannitol, sorbitol, and the like, starch and starch
`derivatives, cellulose derivatives, such as microcrystalline
`cellulose, sodium cahoxymethyl cellulose, methylcellulose,
`ethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose,
`and hydroxypropyl methylcellulose, attapulgites, bentonites,
`dextrins, alginates, carrageenan, gum tragacanth, gum acacia,
`guar gum, xanthan gum, pectin, gelatin, kaolin, lecithin,
`magnesium aluminum silicate, the carbomers and carbopols,
`polyvinylpyrrolidone, polyethylene glycol [PEG], polyethylene
`oxide [PEO], polyvinyl alcohol, silicon dioxide, surfactants,
`mixed surfactant/wetting agent systems, emulsifiers, other
`polymeric materials, and mixtures thereof, etc. In certain
`preferred embodiments, the gelling agent is xanthan gum. In
`other preferred embodiments, the gelling agent of the present
`invention is pectin.
`Id. at 6:45‒63 (emphasis added).
`
`The ’976 patent teaches further:
`A gelling agent may be added to the formulation in a ratio of
`gelling agent to opioid agonist of from about 1:40 to about 40:1
`by weight, preferably from about 1:1 to about 30:1 by weight,
`and more preferably from about 2:1 to about 10:1 by weight of
`the opioid agonist. In certain alternative embodiments, the
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`gelling agent may be present in a ratio to the opioid agonist of
`from about 1:15 to about 15:1, preferably in a ratio of from about
`1:8 to about 8:1, and more preferably from about 1:3 to about 3:1
`by weight of the opioid agonist.
`Id. at 7:12‒20.
`
`The ’976 patent teaches:
`The opioid analgesic formulation in combination with one
`or more aversive agents 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. The controlled release dosage
`form may include a controlled release material which is
`incorporated into a matrix along with the opioid analgesic. In
`addition, the aversive agent may be separate from the matrix, or
`incorporated into the matrix.
`Id. at 12:29‒37.
`
`According to the ’976 patent, the matrix may contain suitable
`quantities of other materials, such as lubricants “that are conventional in the
`pharmaceutical art.” Id. at 16:18‒21. The ’976 patent teaches that
`“[e]xamples of lubricants include but are not limited to magnesium stearate,
`sodium stearate, stearic acid, calcium stearate, magnesium oleate, oleic acid,
`potassium oleate, caprylic acid, sodium stearyl fumarate, and magnesium
`palmitate.” Id. at 25:34‒37.
`C. District Court Proceeding Involving the ’888 patent
`According to the district court in the SDNY Litigation, the ’888 patent
`relates to “a controlled release oral dosage form containing oxycodone that
`forms a gel when dissolved in an aqueous liquid,” wherein the “gelling
`properties . . . enable it to resist abuse by injection, snorting, and oral
`ingestion.” Ex. 1003, 1. Claim 1 of the ’888 patent is reproduced below:
`
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`A controlled release oral dosage form comprising:
`1.
`from about 2.5 mg to about 320 mg oxycodone or a
`pharmaceutically acceptable salt thereof; and
`a gelling agent comprising polyethylene oxide in an effective
`amount to impart a viscosity of at least about 10 cP when the
`dosage form is subjected to tampering by dissolution in from
`about 0.5 to about 10 ml of an aqueous liquid;
`the dosage form providing a therapeutic effect for at least about
`12 hours when orally administered to a human patient.
`Ex. 1002, 40:22‒32.
`
`The district court concluded that the ’888 patent was invalid as
`obvious. Ex. 1003, 40. Specifically, the district court found that the prior
`art teaches that gelling agents prevent potential abuse (id. at 41), and that the
`prior art teaches that PEO acts both as an agent to control the rate of release
`in sustained release dosage forms and as a gelling agent (id. at 43).
`
`The Court of Appeals for the Federal Circuit, our reviewing court,
`affirmed the decision of the district court in a short per curium order. Ex.
`1004. Specifically, the Federal Circuit held:
`The judgment of the United States District Court for the Southern
`District of New York is affirmed on the ground that the court did
`not err in concluding that the asserted claims of U.S. Patent No.
`8,337,888 would have been obvious.
`Id. at 2.
`
`Challenged Claim
`D.
`Petitioner challenges claim 1, the only claim of the ’976 patent, which
`is reproduced below:
`1.
`An extended release abuse deterrent dosage form
`comprising:
`a. a core matrix comprising a blended mixture of:
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`(a) PEO having a molecular weight of from about 300,000
`daltons to about 5,000,000 daltons;
`(b) magnesium stearate; and
`(c) oxycodone or a pharmaceutically acceptable salt thereof;
`wherein the core matrix is heated to melt at least a portion of the
`PEO included in the core matrix during preparation of the dosage
`form; and
`b. PEG applied onto the core matrix;
`wherein the dosage form provides extended release of the drug.
`Ex. 1001, 40:35–48.
`Instituted Grounds of Unpatentability
`E.
`We instituted inter partes review in this proceeding based on the
`following patentability challenges:
`a) obviousness of claim 1 under 35 U.S.C. § 103 based on
`Palermo,1. the Handbook,2 and McGinity;3
`b) obviousness of claim 1 under 35 U.S.C. based on McGinity,
`Joshi,4 Bastin,5 and the PDR.6
`
`1 Palermo et al, WO 99/32120, published Jul. 1, 1999 (Ex. 1011)
`(“Palermo”).
`2 HANDBOOK OF PHARMACEUTICAL EXCIPIENTS, 399‒400, 655
`(Arthur H. Kibbe, Ph.D., ed., Am. Pharm. Ass’n & Pharm. Press 3rd ed.
`2000) (Ex. 1012) (“Handbook” or “HPE-3rd”). Patent Owner refers to this
`reference as “HPE-3rd,” whereas Petitioner refers to it as the “Handbook.”
`We use the terms interchangeably in this Decision.
`3 McGinity et al, WO 97/49384, published Dec. 31, 1997 (Ex. 1013)
`(“McGinity”).
`4 Joshi et al., Pub. No. US 2002/0187192 A1, published Dec. 12, 2002
`(Ex. 1014) (“Joshi”).
`5 Bastin et al., WO 95/20947, published August 10, 1995 (Ex. 1015)
`(“Bastin”).
`6 PHYSICIANS’ DESK REFERENCE®, PRODUCT INFORMATION, OXYCONTIN®,
`2569–74 (53rd ed. 1999) (Ex. 1016) (“the PDR”).
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`Petitioner relies on the Declarations of Anthony Palmieri III, Ph.D.
`(Ex. 1009), Robert J. Timko, Ph.D. (Ex. 1040), and Thomas D. Vander Veen
`(Ex. 1042) to support its Petition and Reply.
`Patent Owner relies on the Declarations of Stephen Byrn, Ph.D. (Ex.
`2007; Ex. 2096), Benjamin Oshlack (Ex. 2097), Curtis Wright IV, M.D.,
`M.P.H. (Ex. 2098), and Eric M. Gaier, Ph.D. (Ex. 2041) to support its
`Response and Sur-Reply.
`
`
`
`DISCUSSION
`Level of Skill in the Art
`A.
`Petitioner contends that a person of ordinary skill in the art for the
`’976 patent would have “a degree in one or more fields of medicine,
`chemical engineering, chemistry, pharmaceutical science, polymer
`chemistry, pharmaceutics, pharmaceutical technology, pharmacokinetics,
`and/or pharmacology, and/or a number of years of industry training or
`experience in one or more of those fields.” Pet. 22–23 (citing Ex.1009 ¶ 17).
`Patent Owner agrees with Petitioner’s proposed level of skill in the art. PO
`Resp. 25. We, therefore, apply that skill level in our analysis, with the
`understanding that the level of skill is also reflected in the prior art of record.
`See Okajima v. Bourdeau, 261 F.3d 1350, 1355 (Fed. Cir. 2001).
`Claim Construction
`B.
`In an inter partes review, claim terms in an unexpired patent are
`interpreted according to their broadest reasonable construction in light of the
`specification of the patent in which they appear. See 37 C.F.R. §42.100(b);
`Cuozzo Speed Techs., LLC v. Lee, 136 S. Ct. 2131, 2144–45 (2016)
`(upholding the use of the broadest reasonable interpretation standard).
`Under the broadest reasonable construction standard, claim terms are
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`presumed to have their ordinary and customary meaning, as would be
`understood by one of ordinary skill in the art in the context of the entire
`disclosure. In re Translogic Tech., Inc., 504 F.3d 1249, 1257 (Fed. Cir.
`2007).
`Petitioner and Patent Owner have offered constructions for the
`following claim terms: “extended release,” “abuse deterrent,” “core matrix
`comprising a blended mixture,” “core matrix is heated to melt at least a
`portion of the PEO included in the core matrix during preparation of the
`dosage form,” and “PEG applied onto the core matrix.” Pet. 23–27; PO
`Resp. 26–30. For purposes of our Institution Decision, we construed the
`terms “extended release,” “abuse deterrent,” and “PEG applied onto the core
`matrix.” Inst. Dec. 8–11. We have considered anew those claim
`constructions in this Final Written Decision based on the full record in this
`proceeding. In addition, in view of the arguments presented, we asked the
`parties during the oral hearing whether they were in agreement as to the
`construction to be given to the terms “core matrix” and “wherein the core
`matrix is heated to melt at least a portion of the PEO included in the core
`matrix during preparation of the dosage form.” Tr. 30:20–32:19. In
`response, the parties sent an email to the Board memorializing their agreed-
`upon constructions for those terms. Ex. 3001.
`On the present record, we determine that the following claim terms
`require explicit construction for purposes of this Decision. See, e.g.,
`Wellman, Inc. v. Eastman Chem. Co., 642 F.3d 1355, 1361 (Fed. Cir. 2011)
`(“[C]laim terms need only be construed ‘to the extent necessary to resolve
`the controversy.’”) (quoting Vivid Techs, Inc. v. Am. Sci. & Eng’g, Inc., 200
`F.3d 795, 803 (Fed. Cir. 1999)).
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`“extended release”
`i.
`Petitioner contends that the term “extended release” does not appear
`in the Specification, but rather the Specification uses the terms “sustained
`release” and “controlled release.” Pet. 24. The Specification, Petitioner
`asserts, defines “sustained release” as “release of the opioid analgesic from
`the oral dosage form at a rate such that blood (e.g., plasma) concentrations
`(levels) are maintained within the therapeutic range but below toxic levels
`over an extended period of time.” Id. (quoting Ex.1001, 4:56–60).
`Petitioner asserts further that although the Specification provides examples
`of 12 to 24 hours, it “does not suggest that such a period of release defines
`the concept.” Id. (citing Ex. 1001, 4:61‒62). Thus, Petitioner argues that
`“the broadest reasonable interpretation of extended release is the above
`phrase wherein ‘over an extended period of time’ means a period of time
`other than that of an immediate release of the opioid analgesic.” Id. (citing
`Ex. 1009 ¶ 23).
`Patent Owner responds that Petitioner’s definition “fails to provide a
`time period over which the drug must be maintained within the therapeutic
`window.” PO Resp. 26. Patent Owner contends that Petitioner’s “expert
`could not specify how to determine what release would have been ‘longer
`than that of an immediate release of the opioid analgesic.’” Id. (citing Ex.
`2099, 169:16–173:15). As such, Patent Owner requests the Board to adopt
`the exemplary teaching in the patent specification and incorporate a
`requirement that extended release must be “from about 12 to about 24
`hours.” Id. at 27 (citing Ex. 1001, 4:61).
`The Specification teaches the following:
`The term “sustained release” is defined for purposes of
`the present invention as the release of the opioid analgesic from
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`the oral dosage form at such a rate that blood (e.g., plasma)
`concentrations (levels) are maintained within the therapeutic
`range but below toxic levels over an extended period of time,
`e.g., from about 12 to about 24 hours as compared to an
`immediate release product. Preferably the sustained release is
`sufficient to provide a twice-a-day or a once-a-day formulation.
`Ex. 1001, 4:56–64. The use of “e.g.” in the above definition for “sustained
`release” plainly indicates that a 12 to about 24 hour time period is
`exemplary. Thus, we decline to limit the claim term as Patent Owner would
`have us do. Rather, we construe “extended release” as “release of the opioid
`analgesic from the oral dosage form at a rate such that blood (e.g., plasma)
`concentrations (levels) are maintained within the therapeutic range but
`below toxic levels over a period of time longer than that of an immediate
`release of the opioid analgesic.”
`“abuse deterrent”
`ii.
`Petitioner contends that the claim term “abuse deterrent” appears only
`in the preamble, and, thus, should not be limiting. Pet. 24–25. Specifically,
`Petitioner asserts “the preamble term ‘abuse deterrent’ should be nonlimiting
`because the claim body describes a structurally complete pharmaceutical
`dosage form and does not attribute abuse deterrence to any particular
`element.” Id. at 25 (citing Ex. 1009 ¶ 24).
`Patent Owner responds that “abuse deterrent” in the preamble should
`be limiting, as it “describes a fundamental characteristic of the claimed
`invention that informs [a skilled artisan] as to the structure required by the
`claim.” PO Resp. 27 (quoting Deere & Co. v. Bush Hog, LLC, 703 F.3d
`1349, 1358 (Fed. Cir. 2012). According to Patent Owner, the “abuse
`deterrent” language imparts a functional limitation on the amount of the
`PEO gelling agent that must be present to practice the invention. Id. at 28
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`(citing Ex. 2096 ¶¶ 97–101). Additionally, Patent Owner contends that “the
`phrase ‘extended release abuse deterrent dosage form’ is limiting because it
`provides an antecedent basis for the term ‘the dosage form’ that appears
`elsewhere in the claim.” Id. (citing Electro Sci. Indus., Inc. v. Dynamic
`Details, Inc., 307 F.3d 1343, 1348 (Fed. Cir. 2002)). Patent Owner also
`contends that that the specification and prosecution history confirm that
`abuse deterrence is the “raison d’etre” or “fundamental characteristic of the
`claimed invention.” Id. at 28–29 (citing Ex. 1001, 1:1–2, 1:15–31, 2:9–11,
`2:15–47, 2:64–3:36, 7:4–34;. Ex. 1030, 5; Ex. 1032, 7; Ex. 1036, 7).
`
`We are unpersuaded by Patent Owner’s arguments. Claim 1 is drawn
`to a dosage form—a composition. Patent Owner does not point out how the
`recitation of “abuse deterrent” in the preamble modifies the structurally
`complete dosage form recited in the body of claim 1. See Catalina Mktg.
`Int'l, Inc. v. Coolsavings.com, Inc., 289 F.3d 801, 808 (Fed. Cir. 2002) (“[A]
`preamble is not limiting ‘where a patentee defines a structurally complete
`invention in the claim body and uses the preamble only to state a purpose or
`intended use for the invention.’”) (quoting Rowe v. Dror, 112 F.3d 473, 478
`(Fed. Cir. 1997)). We conclude, therefore, that the term “abuse deterrent” is
`a goal of the invention, that is, it is merely a statement of intended use that is
`not entitled to patentable weight.
`“PEG applied onto the core matrix”
`iii.
`Petitioner argues that the ordinary artisan “would understand this term
`to mean the [polyethylene glycol, ‘PEG’] is placed on or in contact with the
`core matrix,” which “can occur before, during, or after the core matrix is
`heated.” Pet. 27 (citing Ex.1009 ¶ 28).
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`Patent Owner contends that the broadest reasonable construction of
`this claim term is “PEG coating the core matrix.” PO Resp. 26. According
`to Patent Owner, Petitioner’s construction of “in contact” with the core
`matrix suggests that the PEG may be contained within the core matrix. Id.
`
`We agree with Patent Owner that the broadest reasonable construction
`of “PEG applied onto the core matrix” is a “PEG coating of the core matrix.”
`Petitioner’s proposed construction would read “applied onto the core matrix”
`(emphasis added) out of the claim, which we decline to do. See Bicon, Inc.
`v. Straumann Co., 441 F.3d 945, 951 (Fed. Cir. 2006) (noting that claim
`language “should not [be] treated as meaningless”).
`“core matrix”
`iv.
`The parties agree that the broadest reasonable construction of “core
`matrix” is “a blended mixture having: (a) PEO having a molecular weight of
`from about 300,000 to about 5,000,000 daltons, (b) magnesium stearate, and
`(c) oxycodone or a pharmaceutically acceptable salt of oxycodone.” Ex.
`3001. We adopt that agreed-upon construction for purposes of this Decision.
`“wherein the core matrix is heated to melt at least a portion of
`v.
`the PEO included in the core matrix during preparation of the dosage
`form”
`The parties agree that the broadest reasonable construction for
`“wherein the core matrix is heated to melt at least a portion of the PEO
`included in the core matrix during preparation of the dosage form”7 is:
`
`
`7 Although this phrase would appear to be a “product-by-process”
`limitation, neither Patent Owner nor Petitioner have argued that it should not
`be considered in our patentability analysis. See Tr. 17:9–18:2 (Petitioner’s
`counsel acknowledging that Petitioner has not stated the position that the
`limitation is a product-by-process limitation); but see Amgen Inc. v. F.
`Hoffman-La Roche Ltd., 580 F.3d 1340, 1370 n 14, (Fed. Cir. 2009)
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`heating the blended mixture having (a) PEO having a molecular
`weight of from about 300,000 to about 5,000,000 daltons, (b)
`magnesium stearate, and (c) oxycodone or a pharmaceutically
`acceptable salt of oxycodone, during preparation of the dosage
`form sufficient to melt at least part of the PEO. Heating occurs
`at any time during or after preparation of the blended mixture
`of PEO, magnesium stearate, and oxycodone.
`Ex. 3001 (emphasis added).
`
`Notwithstanding the parties’ apparent agreement that heating may
`occur “at any time during” preparation of the blended mixture of PEO,
`magnesium stearate, and oxycodone, there nevertheless continues to be a
`dispute about whether this claim limitation requires all three components of
`the blended mixture (i.e., PEO, magnesium stearate, and oxycodone) to be
`heated together only after the core matrix is formed. For example, Petitioner
`asserts in its Reply that “[t]he claim does not require heating or high-shear
`mixing of” magnesium stearate. Reply 8. Patent Owner, in its Sur-Reply,
`contends that “[t]his interpretation of claim 1 flies in the face of the plain
`and ordinary meaning of the claim and all of the other evidence in these
`proceedings.” PO Sur-Reply 6. In support, Patent Owner points out that
`Petitioner’s original expert, Dr. Palmieri, explained at his deposition that
`“the claim takes the core mixture of the three ingredients [i.e., PEO,
`oxycodone, and magnesium stearate] and then heats it.” Id. (citing Ex. 2099,
`197:4–7, 199:20–200:5). Patent Owner further points out that Petitioner’s
`other expert, Dr. Timko, also agreed at his deposition, confirming that “in
`order to practice claim 1. . . you have to mix PEO, magnesium stearate, and
`
`
`(“Because validity is determined based on the requirements of patentability,
`a patent is invalid if a product made by the process recited in a product-by-
`process claim is anticipated by or obvious from prior art products, even if
`those prior art products are made by different processes.”).
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`oxycodone together before you heat it” and that “if I heat something and I
`don’t have the magnesium stearate in it, I have not heated the core matrix.”
`Id. (citing Ex. 2147, 35:2–5, 37:2–6).
`
`The specification of the ’976 patent does not indicate that the
`magnesium stearate should be added to the core matrix during the heating/
`melt-extrusion step. Rather, it states that “[t]he preparation of a suitable
`melt-extruded matrix according to the present invention may, for example,
`include the steps of blending the opioid analgesic and at least one aversive
`agent, together with a sustained release material and preferably a binder
`material to obtain a homogeneous mixture,” and “[t]he homogenous mixture
`is then heated to a temperature sufficient to at least soften the mixture
`sufficiently to extrude the same.” Ex. 1001, 17:4–11. As such, the melt
`extrusion process described in the specification only indicates that the opioid
`analgesic, an aversive agent (to deter abuse), and the sustained release
`material are heated together. Although the specification further states that
`lubricants, such as magnesium stearate, “may be used during the
`manufacture of the dosage form to prevent sticking to die wall or punch
`faces,” this statement also does not suggest that the lubricant must
`necessarily be added during the heating/melt-extrusion step. Id. at 25:31–35.
`
`Furthermore, during prosecution, the Applicants for the ’976 patent
`stated the following:
`Applicants respectfully submit that the element “wherein
`the core matrix is heated to melt at least a portion of the PEO
`included in the core matrix during preparation of the dosage
`form” does encompass the core matrix prepared by melt
`extrusion or melt-granulation but is not limited as such.
`Applicants further respectfully submit that the element does
`encompass heating during preparation of the core matrix but is
`not limited as such as the claim recites “during preparation of
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`the dosage form.” Thus the claim also encompasses heating,
`e.g., after preparation of the core matrix; or e.g., before or after
`PEG is applied onto the core matrix.
`Ex. 2009, 2 (Applicants’ communication in response to Examiner’s Reasons
`for Allowance). As set forth above by Applicants through its use of “e.g.,”
`heating after preparation of the core matrix is only one example of when the
`dosage form may be heated. As such, Applicants plainly indicated during
`prosecution that heating can occur at any point during preparation of the
`dosage form, which would include before all the required components are
`incorporated into the core matrix.
`Given the parties’ agreement, as well as the clear statements made in
`the specification and during prosecution, we give little weight to the expert
`testimony cited by Patent Owner to support a contrary interpretation. See
`Phillips v. AWH Corp., 415 F.3d 1303, 1318 (Fed. Cir. 2005) (en banc)
`(“[A] court should discount any expert testimony ‘that is clearly at odds with
`the claim construction mandated by the claims themselves, the written
`description, and the prosecution history, in other words, with the written
`record of the patent.’”) (quoting Key Pharms. v. Hercon Labs. Corp., 161
`F.3d 709, 716 (Fed. Cir. 1998)).
`
`Accordingly, we adopt the parties’ agreed-upon construction with the
`further clarification, consistent with the parties’ construction, that the
`heating step can occur before the magnesium stearate is included in the core
`matrix.
`
`Prior Art Relied Upon
`C.
`Petitioner relies upon the following prior art teachings for its
`patentability challenges in this proceeding:
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`Overview of Palermo (Ex. 1011)
`i.
`Palermo discloses an opioid oral dosage form that is less subject to
`
`potential parenteral or oral abuse. Ex. 1011, 6:1‒9. The potential for abuse
`is reduced by “combining an analgesically effective amount of an opioid
`agonist together with an opioid antagonist into an oral dosage form.” Id. at
`6:10‒16. The opioid may be oxycodone hydrochloride, with the antagonist
`being naltrexone hydrochloride. Id. at 6:25‒28.
`
`Palermo discloses further that the dosage form may be a sustained
`release formulation, which may be accomplished by incorporating a
`sustained release carrier into the matrix containing the opioid and its
`antagonist, as well as using a sustained release coating. Id. at 8:1‒6.
`Specifically, Palermo teaches that the “tablets may be uncoated or they may
`be coated by known techniques for elegance or to delay release of the active
`ingredients.” Id. at 18:3‒5.
`
`Palermo teaches that in preferred embodiments the substrate, that is
`the matrix particle, is coated with a hydrophobic material. Id. at 22:6‒9.
`According to Palermo, the inclusion of a plasticizer in the aqueous
`dispersion of the hydrophobic material used in the coating will improve the
`physical properties of the sustained release coating. Id. at 24:25‒29. An
`example of a plasticizer that may improve the elasticity of a