DETAILED ACTION
Notice of Pre-AIA or AIA Status
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
1-7, 9-12, 14-20, 27, and 31 are pending.
Election/Restrictions
Applicant’s election without traverse of Group I, claims 1-7, 9-12, and 14-20 in the reply filed on 10/20/2025 is acknowledged.
Claims 27 and 31 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected invention, there being no allowable generic or linking claim. Election was made without traverse in the reply filed on 10/20/2025.
Claims 1-7, 9-12, and 14-20 are under current examination.
Information Disclosure Statement
Citations provided without a publication date (NPL reference 42 on the IDS filed 11/13/2023) were not considered by the examiner as indicated by a line through on the IDS. See MPEP 609.04(a):
37 CFR 1.98(b) requires that each item of information in an IDS be identified properly. U.S. patents must be identified by the inventor, patent number, and issue date. U.S. patent application publications must be identified by the applicant, patent application publication number, and publication date. U.S. applications must be identified by the inventor, the eight digit application number (the two digit series code and the six digit serial number), and the filing date. If a U.S. application being listed in an IDS has been issued as a patent or has been published, the applicant should list the patent or application publication in the IDS instead of the application. Each foreign patent or published foreign patent application must be identified by the country or patent office which issued the patent or published the application, an appropriate document number, and the publication date indicated on the patent or published application. Each publication must be identified by publisher, author (if any), title, relevant pages of the publication, and date and place of publication. The date of publication supplied must include at least the month and year of publication, except that the year of publication (without the month) will be accepted if the applicant points out in the information disclosure statement that the year of publication is sufficiently earlier than the effective U.S. filing date and any foreign priority date so that the particular month of publication is not in issue. The place of publication refers to the name of the journal, magazine, or other publication in which the information being submitted was published. See MPEP § 707.05(e), for more information on data that should be used when citing publications and electronic documents. Pending U.S. applications that are being cited can be listed under the non-patent literature section or in a new section appropriately labeled.
Claim Objections
Claim 7 is objected to because of the following informalities: Claim 7 does not end in a period. See MPEP 608.01(m), which requires claims to be a single sentence (i.e. ending with a period). Appropriate correction is required.
Claim Rejections - 35 USC § 112
The following is a quotation of 35 U.S.C. 112(b):
(b) CONCLUSION.—The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or a joint inventor regards as the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), second paragraph:
The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the applicant regards as his invention.
Claims 5-7, 9-12, and 14-17 are rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being indefinite for failing to particularly point out and distinctly claim the subject matter which the inventor or a joint inventor (or for applications subject to pre-AIA 35 U.S.C. 112, the applicant), regards as the invention.
Claim 5 recites the limitation "the biocompatible polymer" in line 2. There is insufficient antecedent basis for this limitation in the claim. Specifically, claim 1 allows for two biocompatible polymers, the first polymer in the shell and/or the second polymer in the core. As the claims are currently worded, it is unclear whether claim 5 limits one or both of the biocompatible polymers that claim 1 embraces.
Regarding claim 5, the phrase "such as" (e.g. line 2) renders the claim indefinite because it is unclear whether the limitations following the phrase are part of the claimed invention. See MPEP § 2173.05(d).
Claim 5 recites the word “phenolic” in line 5. This renders the claim indefinite because “phenolic” is an adjective, but it is unclear what polymer the word modifies. As such, the scope of the polymers that may qualify as “phenolic” is unclear.
Claim 5 recites the word “polyvinyl” in line 11. This renders the claim indefinite because “polyvinyl” is an adjective, but it is unclear what polymer the word modifies. As such, the scope of the polymers that may qualify as “polyvinyl” is unclear.
Claim 6 recites the limitation "the biocompatible polymer" in line 2. There is insufficient antecedent basis for this limitation in the claim. Specifically, claim 1 allows for two biocompatible polymers, the first polymer in the shell and/or the second polymer in the core. As the claims are currently worded, it is unclear whether claim 6 limits one or both of the biocompatible polymers that claim 1 embraces.
Claim 7 recites the limitation "the non-erodible polymer" in line 2. There is insufficient antecedent basis for this limitation in the claim. Specifically, claim 1 allows for two non-erodible polymers, the first polymer in the shell and/or the second polymer in the core. As the claims are currently worded, it is unclear whether claim 7 limits one or both of the non-erodible polymers that claim 1 embraces.
Claim 7 does not recite a conjunction before the last substance in the Markush listing of polymers, therefore it is unclear whether all polymers are required or the non-erodible polymer may be only one of the recited polymers in microparticles falling within the claimed scope.
Claim 9 recites the limitation "the dispersing agent" in line 2. There is insufficient antecedent basis for this limitation in the claim. Amending claim 9 to depend from claim 2 would obviate the rejection.
Claim 11 recites the phrase “can be” both in line 7 and in line 8. This renders the claim indefinite because the phrase “can be” implies that the x and y variables could alternatively be limited something other than the scope following the phrase “can be”. Amending the claim to recite “x is” and “y is” would obviate the rejection.
Claim 14 is indefinite because the claim requires a weight percentage of active agent, which present only in the core in claim 1, without identifying whether the percentage is relative to the entire microparticle or only relative to the component containing the active agent (e.g. the core).
Claim 15 is indefinite because the claim requires a weight percentage of
dispersing agent, which present only in the shell in claim 2, without identifying whether the percentage is relative to the entire microparticle or only relative to the component containing the dispersing agent (e.g. the shell).
Claim 16 is indefinite because the claim recites a range on duration of active agent release without providing an upper or lower limit to the range. The examiner notes that any amount of time can be measured in days or weeks, whether fractions or multiples are required.
Claim 17 is indefinite because the claim recites a range on duration of drug release without providing an upper limit or lower to the range. The examiner notes that any amount of time can be measured in days or weeks, whether fractions or multiples are required.
Claim 17 recites the limitation "the drug" in line 2. There is insufficient antecedent basis for this limitation in the claim.
Claims depending from rejected claims have also been rejected because they incorporate all of the limitations of the claims from which they depend, but fail to resolve the indefiniteness concerns outlined above.
Claim Rejections - 35 USC § 103
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis (i.e., changing from AIA to pre-AIA ) for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made.
The factual inquiries for establishing a background for determining obviousness under 35 U.S.C. 103 are summarized as follows:
1. Determining the scope and contents of the prior art.
2. Ascertaining the differences between the prior art and the claims at issue.
3. Resolving the level of ordinary skill in the pertinent art.
4. Considering objective evidence present in the application indicating obviousness or nonobviousness.
This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
Claims 1, 3-5, 14, 16-20 are rejected under 35 U.S.C. 103 as being unpatentable over Bruna et al. (US20020012679; publication date: 01/31/2002) as evidenced by Chang et al. (US 20030194382 ; publication date: 10/16/2003).
With regard to claim 1, Bruna discloses polymer coated particles of gabapentin or pregabalin (abstract, title). The particles are preferably between 100 – 400 mm and are therefore microparticles (0032). In an example composition (see example 1, 0065-0075), gabapentin is combined with polyvinylpyrrolidone (PVP; a biocompatible polymer) to form a core. The examiner considers this structure to fall within the scope of “a polymeric core comprising a first polymer (PVP) and an active agent susceptible to abuse (gabapentin)”. This core is then coated with Eudragit E 100, a biocompatible polymer coating.
The example above differs from the claimed invention in that the polymer Eudragit E 100 is an aminoalkyl methacrylate copolymer (Chang: 0054), and therefore soluble in water under certain pH conditions. This does not meet the requirement set forth in the definition of the term “non-erodible” found in the instant specification (page 19): a biocompatible polymer that is water insoluble. However, Bruna discloses other polymers that may be used to coat the microparticles, including ethyl cellulose (0039; i.e. a water insoluble/non-erodible polymer, see Chang: claim 7).
It would have been prima facie obvious to coat Bruna’s microparticles with ethyl cellulose because such was within the scope of this invention.
With regard to claims 3 and 4, as noted above, the particles contain the gabapentinoids, gabapentin or pregabalin.
With regard to claim 5, as noted above the biocompatible polymer may be ethyl cellulose, which is a cellulose ether.
With regard to claim 14, Bruna discloses that the polymer [the coating] is between 60 – 80% by weight relative to the weight of gabapentin. This allows for up to approximately 40% gabapentin and this range overlaps with the range for amount of active agent recited in the instant claims. See MPEP 2144.05(I).
With regard to claims 16 and 17, in view of the indefiniteness rejection above, the examiner interprets claims 16 and 17 not to clearly limit the amount of time over which the active agent/drug is released. Given this broadest reasonable interpretation claims 16 and 17 read on Bruna’s immediate release formulation because an immediate release profile could be measured in fractions of a day or week.
With regard to claims 18-20, Bruna discloses that the microparticles may be incorporated into pharmaceutical compositions such as tablets, which contain tableting excipients such as diluents (i.e. dispersing agents; 0050; 0051; limitation of instant claim 20). The preambles to claims 18 and 19 limit the claimed compositions to those that are capable of use for localized delivery or abuse-resistance, respectively. As the compositions meet all the structural requirements of the claim and could be delivered locally (e.g. to a certain portion of the gastrointestinal tract using enteric coatings or to resist abuse, due to the presence of the water insoluble polymer coating of ethyl cellulose) the compositions disclosed by Bruna could be used for both purposes required by the claims.
Claims 2, 7, 9-12, and 15 are rejected under 35 U.S.C. 103 as being unpatentable over Bruna et al. (US20020012679; publication date: 01/31/2002) as evidenced by Chang et al. (US 20030194382 ; publication date: 10/16/2003) as applied to claims 1, 3-5, 14, 16-20 above, and further in view of Ghosh et al. (US 20120202838; publication date: 08/09/2012).
The relevant disclosure of Bruna is set forth above.
Bruna does not disclose a dispersing agent and required by instant claims 2, 9-12, and 15.
Bruna discloses that the shell may further comprise a plasticizer (0039).
Ghosh discloses that poloxamers, such as poloxamer 407, function as plasticizers (0016, claim 20, 0068).
It would have been prima facie obvious to use poloxamer 407 (limitations of instant claims 9-12) as the plasticizer in Bruna’s invention because this substance was known to serve the same purpose as the plasticizers disclosed by Bruna (see MPEP 2144.06(I)).
With regard to the limitation of instant claim 2 requiring a dispersing agent, the examiner notes that poloxamer 407 also functions as a dispersing agent (see claims 9-12) and as such this limitation is inherently met by the substance poloxamer 407 (see MPEP 2112).
With regard to the amount of dispersing agent required by instant claim 15, Ghosh discloses an example composition comprising poloxamer 407 at 6.4% of the formulation (table 4, page 16). This falls within the scope of the range required by instant claim 15 and would have given the artisan of ordinary skill a starting point to optimize plasticizing effect. The examiner does not consider the range recited in instant claim 15 to patentably define over the cited prior art as substances falling within the term “dispersing agent” (i.e. poloxamer 407) were known for use in the field within the claimed range. Absent evidence establishing criticality of the claimed range in dispersing agent to an unexpectedly superior property, this limitation is considered prima facie obvious. See MPEP 2144.05(II).
Bruna does not disclose the specific polymers listed in instant claim 7.
Bruna discloses that polyvinylpyrrolidone, the polymer present in the element of Bruna’s invention corresponding to the instant core, functions as a binder (table following 0067).
Ghosh discloses that both polyvinylpyrrolidone and polyvinyl alcohol were known in the pharmaceutical arts to function as binders as of the instant effective filing date (0093).
It would have been prima facie obvious to use polyvinyl alcohol as the binder in Bruna’s invention because this substance was known to serve the same purpose as the binder disclosed by Bruna (see MPEP 2144.06(I)).
Claim 7 limits either the non-erodible first polymer or the non-erodible second polymer because claim 1 permits either the first (core) or the second (shell) polymer to be non-erodible. As such, claim 7 reads on microparticles in which the first or second polymers are non-erodible and selected from polysulfone, poly(ethylene-co-vinyl-acetate), or polyvinyl alcohol (see rejection under 35 USC 112(b) above).
Claims 6 and 7 are rejected under 35 U.S.C. 103 as being unpatentable over Bruna et al. (US20020012679; publication date: 01/31/2002) as evidenced by Chang et al. (US 20030194382 ; publication date: 10/16/2003) as applied to claims 1, 3-5, 14, 16-20 above, and further in view of Lee et al. (US 20160326325; publication date: 11/10/2016).
The relevant disclosure of Bruna is set forth above.
As noted above, Bruna discloses that the coating may be formed from ethyl cellulose but Bruna does not disclose the specific polymers listed in instant claims 6 and 7.
Lee discloses that polysulfone was known to function as an encapsulating (i.e. coating) agent as of the instant effective filing date.
It would have been prima facie obvious to replace the ethyl cellulose disclosed as a coating polymer with polysulfone because these two substances were known to serve the same purpose as of the instant effective filing date (see MPEP 2144.06(I)).
The examiner notes that in view of the indefiniteness rejection above, neither claim 6 nor claim 7 clearly limits the first (core) or second (shell) polymers recited in instant claim 1. Claim 6 reads on microparticles in which the first or second polymers are biocompatible and selected from polysulfone, polycaprolactone, or a combination thereof because the unclear antecedent basis of “biocompatible” is not clear. As explained in the indefiniteness rejection above, the claim is interpreted to further limit either the biocompatible first polymer or the biocompatible second polymer or both biocompatible first and second polymers. Similarly, claim 7 limits either the non-erodible first polymer or the non-erodible second polymer because claim 1 permits either the first or the second polymer to be non-erodible. As such, claim 7 reads on microparticles in which the first or second polymers are non-erodible and selected from polysulfone, poly(ethylene-co-vinyl-acetate), or polyvinyl alcohol.
Claims 16-20 are rejected under 35 U.S.C. 103 as being unpatentable over Bruna et al. (US20020012679; publication date: 01/31/2002) as evidenced by Chang et al. (US 20030194382 ; publication date: 10/16/2003) as applied to claims 1, 3-5, 14, 16-20 above, and further in view of Rimawi et al. (Scientific reports, 9(1), p 11675; publication date: 2019; cited in the IDS filed 11/20/2024) and Venkatesh et al. (US 20060246134; publication date: 11/02/2006).
The relevant disclosure of Bruna is set forth above.
Although the claims are considered obvious over Bruna itself as set forth above, in the interest of compact prosecution, the examiner also rejects claims 16-20 as obvious as the claims read on sustained, extended, or delayed release compositions.
Bruna’s composition is intended for immediate release rather than a composition that releases gabapentin or pregabalin over multiple days or weeks.
Rimawi discloses an extended release formulation of gabapentin for increasing bioavailability and decreasing dosing frequency (abstract, title).
Venkatesh discloses pulsatile release multiparticulate formulations in which several populations of drug-containing microparticles having different release profiles combined for highly tunable drug release profiles (title, abstract, figures). More specifically, immediate release particles are combined with delayed and/or sustained release particles to provide an effective dose shortly after administration and also provide continued effective plasma drug concentrations over a longer period of time allowing for e.g. once or twice daily dosing (abstract, 0008). The different release rates are achieved by polymer selection for coatings and cores of the microparticles (abstract).
It would have been prima facie obvious to combined the immediate release formulation for gabapentin or pregabalin disclosed by Bruna with additional populations of beads to form a pharmaceutical composition capable of delivering these agents over the course of days or weeks. The skilled artisan would have been motivated to do so in order to decrease dosing frequency and improve bioavailability as disclosed by Rimawi. The artisan of ordinary skill would have had reasonable expectation of success because Venkatesh provides extensive detail on how to optimize a desired drug release profile. The examiner considers the requirement of providing zero-order drug release as required by claim 16 to have been optimizable in view of the extended teachings of Venkatesh, as well.
With regard to claims 18-20, Bruna discloses that the microparticles may be incorporated into pharmaceutical compositions such as tablets, which contain tableting excipients such as diluents (i.e. dispersing agents; 0050; 0051; limitation of instant claim 20). The preambles to claims 18 and 19 limit the claimed compositions to those that are capable of use for localized delivery or abuse-resistance, respectively. As the compositions meet all the structural requirements of the claim and could be delivered locally (e.g. to a certain portion of the gastrointestinal tract using enteric coatings or to resist abuse, due to the presence of the water insoluble polymer coating of ethyl cellulose) the compositions disclosed by Bruna could be used for both purposes required by the claims.
Conclusion
No claims are allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to KATHERINE PEEBLES whose telephone number is (571)272-6247. The examiner can normally be reached Monday through Friday: 9 am to 3 pm.
Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Ali Soroush can be reached at (571)272-9925. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000.
/KATHERINE PEEBLES/Primary Examiner, Art Unit 1617