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 .
Claim Status
A Requirement for Restriction/Election Office Action was mailed 17 September 2025.
In Applicant’s reply, filed 17 November 2025, Applicant elected Group I (claims 1-15 and 23-24), drawn to a composition of extended-release multiple unit pellet system, with traverse. Group II (claim 19), drawn to the profess for preparation of extended-release multiple unit pellet system, reads on an unelected invention and is hereby withdrawn from consideration.
Applicant's election with traverse of Group I, claims 1-15 and 23-24 in the reply filed on 17 November 2025 is acknowledged. The traversal is on the ground(s) that WO 2012/052834 does not specifically disclose or enable a composition of extended-release multiple unit pellet system comprising the limitations of claim 1. Further, Applicant argues the claimed composition differs from WO 2012/052834 in that WO 2012/052834 formulates tablets such that the dissolution profile of the extended-release pellets remains substantially unaffected. The instant claims, Applicant argues, do not read on this feature in WO 2012/052834. This argument is not found persuasive because instant claim 1 reads broadly on a composition that allows for picking and choosing elements, all of which are disclosed by WO 2012/052834, as suitable for use in an extended release, multiple unit pellet system that would allow for one of ordinary skill to arrive at the instantly claimed invention. Further search, as discussed further in this office action, reveals the composition of claim 1 does not make a contribution over prior art.
The requirement is still deemed proper and is therefore made FINAL. Therefore, claim 19 is withdrawn from consideration pursuant to 37 CFR § 1.142(b) as being drawn to a non-elected invention.
In addition, Applicant has elected the following species in their 17 November 2025 reply, but argues the species election requirement is inappropriate:
Core sphere active pharmaceutical ingredient: Applicant elects Metformin Hydrochloride; Venlafaxine Hydrochloride; and/or Metoprolol Succinate.
Seal coating polymer: Applicant elects hydroxypropyl methylcellulose (HMPC) and/or polyethylene glycol (PEG) 4000; and seal coating solvent: Applicant elects water.
Functional coating: Applicant elects ethyl cellulose and/or Hypromellose.
Second seal coating polymer: Applicant elects hydroxypropyl methylcellulose (HMPC) and/or polyethylene glycol (PEG) 4000; and second seal coating solvent: Applicant elects water.
Claims 1-4, 6-15, 19, and 23-24 read on the elected species. However, the species election as indicated in the 17 September 2025 Office Action is withdrawn after further consideration and search.
Therefore, claims 1-15, 19, and 23-24 are currently pending. Claim 19 is withdrawn from consideration. Claims 1-15 and 23-24 are under examination.
Priority
Applicant’s claim for the following priority is acknowledged:
PNG
media_image1.png
90
631
media_image1.png
Greyscale
Information Disclosure Statement (IDS)
The IDS (1) filed on 01 November 2023 has been considered by the examiner. A signed copy is enclosed.
Applicant is reminded of their duty to disclose to the Office all information known to the
person to be material to patentability as defined in 37 CFR 1.56. As stated therein, “[e]ach
individual associated with the filing and prosecution of a patent application has a duty of candor
and good faith in dealing with the Office, which includes a duty to disclose to the Office all
information known to that individual to be material to patentability as defined in this section.”
Claim Objections
Claim 1 is objected to as failing to establish a primary antecedent basis. Claim 1 recites: “…cores spheres containing active pharmaceutical ingredient…” This is grammatically incorrect and further fails to establish primary antecedent basis for the active pharmaceutical ingredient as recited in claims 3 and 4. The proper way to format claim 1 is: “…core spheres containing a pharmaceutical active ingredient…” See USPTO’s Claim Drafting (particularly ‘the three basic rules for claim drafting’ on pages 12-15) for further guidance: https://www.uspto.gov/sites/default/files/documents/Claim%20drafting.pdf.
Claim 8 is objected to for containing a potential typographical error. Claim 8 recites ‘Opdary,’ which is assumed to be Opadry.
Claims 1-15 and 23-24 are objected to. The claims contain several grammatical errors (e.g., matching singular and plural nouns; lacking conjunctions; lacking indefinite/definite articles to modify nouns; misspellings; and inappropriate capitalization of words). Applicant is urged to review the claims thoroughly for these errors.
Claim Rejections - 35 USC § 112(a)
Claims 1-15 and 23-24 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, because the specification, while being enabling for making a limited number of specific extended-release multiple unit pellet system compositions, does not reasonably provide enablement for the full scope of the claimed invention without undue experimentation.
The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make the invention commensurate in scope with these claims.
Enablement is considered in view of the Wands factors (MPEP 2164.01(A)).
These include:
(A) The breadth of the claims;
(B) The nature of the invention;
(C) The state of the prior art;
(D) The level of one of ordinary skill;
(E) The level of predictability in the art;
(F) The amount of direction provided by the inventor;
(G) The existence of working examples; and
(H) The quantity of experimentation needed to make or use the invention based
on the content of the disclosure
All of the Wands factors have been considered with regard to the instant claims as discussed below:
(A)/(B) The breadth of the claims/The nature of the invention:
The breadth of the claims and nature of the invention weighs strongly against enablement.
Claim 1 broadly recites an extended-release multiple unit pellet system (MUPS) composition without limiting: the active pharmaceutical ingredient, drug loading, solubility, dose, particle size, stability, coating weight, pellet size, release profile apart from the broadly claimed ‘extended release,’ release duration, release medium, or dissolution conditions. Claim 3 further expands the scope to a large genus of active pharmaceutical ingredient (API) classes ranging from hormones to hypnotic agents. Claims 4 and 5 recite numerous individual APIs having materially different physiochemical and pharmacokinetic properties.
The claimed genus of APIs includes, for example, highly soluble high-dose drugs, poorly soluble high-dose drugs, peptides, enzymes, hormones, antibiotics, antifungals, antihypertensives, steroids, and gastro-intestinal agents. These APIs differ significantly in solubility, permeability, dose, stability, hygroscopicity, compressibility, particle size, compatibility with coating solvents, sensitivity to heat or moisture, and desired release profile.
The claims also broadly encompass numerous excipient classes, polymers, and solvents. The claims do not specifically define which combinations of API, core excipients, seal coat, functional coat, second seal coat, and extra-granular excipients will successfully produce an extended-release MUPS composition across the full claim scope.
The nature of the invention weighs against enablement because the claimed subject matter concerns extended-release, multi-particulate, pharmaceutical formulation, which is highly formulation-dependent. The claimed invention is not merely the physical act of coating pellets. The claims require an extended-release multiple unit pellet system, meaning the formulation must provide controlled drug release from multi-particulate units after coating, blending, and, in some embodiments, compression into tablets or filling into capsules or sachets.
Achieving extended release from coated pellets depends on many interrelated formulation variables including:
API solubility and dose;
API particle size and distribution within the core;
Pellet size and porosity;
Seal coat composition and thickness;
Compatibility between API and coating materials;
Compression force; and
Selection of solvent, excipient, and polymer systems and their interaction with the coatings.
Because even minute changes in these variables could materially affect release rate, stability, dose dumping, pellet rupture, coat integrity, and tablet performance, the nature of the invention is unpredictable across the full scope of the claimed API and formulation genra.
(C)/(E) State of the prior art/Level of predictability in the art:
The state of the prior art, before the effective filing date of 12 February 2021, weighs only partially in favor of enablement. Examiner acknowledges that extended-release pellets, seal coatings, functional release coatings, extrusion/spheronization, ethyl cellulose coatings, Hypromellose coatings, and MUPS tablets were generally known in the art before the effective filing date. A person of ordinary skill would have understood the general techniques for preparing coated pellets and compressing multi-particulates into tablets. For instance, Tiwari (cited in prior office action as: WO 2012/052834 A2; published: 26 April 2012) contemplates extended release MUPS comprising various ingredient materials. However, where Tiwari differs from the instantly claimed invention is the API selection. Tiwari’s disclosure is very narrowly contemplated and specifically directed to a single API. Comparatively, instant claim 1 allows for any API and the dependent claims only slightly limit the extensive scope of claimed API, only magnifying just how broad Applicant’s claimed invention is.
The existence of general MUPS technology does not mean that a person of ordinary skill could make the claimed genus of the invention without undue experimentation. The claims are not limited to a specific API or narrow class of APIs. Rather, the scope of the claims covers an astronomical number of APIs and excipient systems having materially different release and stability requirements. The prior art knowledge of general coating methods would not provide a universal formulation recipe that would predictably yield extended-release MUPS compositions for each API claimed in instant claims 1, and 3-5.
Thus, while the prior art may reduce the amount of routine experimentation needed for a narrowly elected species, it does not cure the lack of commensurate guidance for the fully claimed scope.
The level of predictability of the art weighs strongly against enablement. There is no universally accepted extended-release pharmaceutical formulation across a genus encompassing every single API. A highly water-soluble, high-dose API may require a different coating thickness, polymer ratio, and pore-forming strategy than a poorly soluble high-dose drug. A peptide or protein may raise different stability and solvent-compatibility concerns than a small-molecule antibiotic or anti-hypertensive. A poorly-soluble API may require solubilizers, particle-size control, or different core architecture to achieve reproducible release. The claims do not provide objective formulation rules that would allow a person of ordinary skill to predict which API/excipient/coating combination will provide the claimed extended-release MUPS composition. Instead, the claims broadly cover an indefinite amount of combinations, only a small percentage of which may actually achieve the extended-release property required by instant claim 1. Because the art is highly dependent on API-specific and formulation-specific variables, the unpredictability factor supports a finding of non-enablement.
(D) Level of one of ordinary skill:
The level of ordinary skill in the art weighs somewhat in favor of enablement, but does not overcome the breadth and unpredictability of the claims. One having ordinary skill in the art would have an advanced degree in bioorganic and medicinal chemistry such as a PhD and/or a pharmaceutical or medical doctor degree. Therefore, the level of skill is high.
However, even a skilled formulation scientist would need to conduct substantial API-specific experimentation to determine whether a given API could be successfully formulated into the claimed extended-release MUPS architecture. The claims encompass APIs with widely different solubility, dose, stability, permeability, and release requirements. The specification does not provide sufficient predictive guidance or representative examples showing one of ordinary skill how to adapt the claimed system across those materially different APIs.
(F) The amount of direction provided by the inventor/(G) The existence of working
examples:
This factor weighs against enablement. The claims and disclosure provide broad lists of possible APIs, coating polymers, release-controlling polymers, plasticizers, anti-adherents, disintegrants, glidants, lubricants, binders, diluents, and solvents. Arriving at a composition having extended-release properties would require picking and choosing from materials across each of these lists without any guidance on how to select and combine these ingredients to obtain extended-release. While instant claim 23 provides a more specific formulation framework, it does not demonstrate enablement across the full scope of claims 1-15 because the claims are not limited to that particular formulation or to a specific API for which that formulation has been shown to work.
The specification only provides limited working examples and therefore, this factor weighs against enablement. Applicant has disclosed 14 working examples using only three total APIs: metformin hydrochloride, metoprolol succinate, and venlafaxine hydrochloride.
CORE SPHERES
APIs (3):
Metformin hydrochloride is an antidiabetic drug used for the treatment of type 2 diabetes. Metformin has a molecular weight of 129.167 g/mol and is highly soluble in water. Metoprolol succinate is a beta-blocker used to treat high blood pressure, angina, heart failure, and arrythmias. Metoprolol succinate has a molecular weight of 652.82g/mol and is highly soluble in water. Venlafaxine hydrochloride is an antidepressant medication and used to treat major depressive disorder, anxiety disorders, and panic disorders. Venlafaxine hydrochloride has a molecular weight of 277.408 g/mol and is highly soluble in water. Therefore, Applicant has provided working examples of two small molecule drugs and one large molecule drug used to treat various disease and all three of which are highly water soluble.
Excipients (4):
Chosen from the group consisting of: microcrystalline cellulose, povidone K-30, hydroxy propyl cellulose, and copovidone.
SEAL COATING
Polymers (5):
Chosen from the group consisting of: PEG-4000, Hypromellose E5 LV, Eudragit NM 30 D, Opadry Clear, and Povidone.
Solvent (1):
Only one used: purified water.
FUNCTIONAL COATING
Release Controlling Polymers (3):
Chosen from the group consisting of: ethyl cellulose, Hypromellose ES LV, and Surelease E-&-19040.
Excipients (5):
Chosen from the group consisting of: triethyl citrate, talc, isopropyl alcohol, water, and dibutyl sebacate.
SECOND SEAL COATING
Polymers (4):
Chosen from the group consisting of: PEG-4000, Hypromellose E5 LV, PEG-6000, and Opadry Clear.
Solvent (1):
Only one used: purified water.
TABLET EXCIPIENTS
Tablet Excipients (6):
Chosen from the group consisting of: microcrystalline cellulose, copovidone, colloidal silicon dioxide, magnesium stearate, sodium stearyl fumarate, and water.
The release profile was only tested in three of the 14 examples using only two of the three APIs (specification, p. 39-40).
The claims encompass a broad genus of APIs and ingredient combinations, but the specification appears to provide, at most, limited examples directed to a few formulations using only three APIs and a handful of other material combinations. Even if the specification enables a particular elected API/polymer/excipient species, such examples are not representative of the full genus recited in claims 1-15 and 23-24.
For a genus as broad as what is claimed, representative working examples would be expected across materially different API types, such as: highly soluble, high-dose; poorly-soluble, high-dose; unstable; peptides/proteins; APIs requiring organic solvent avoidance; APIs requiring high drug loading; and APIs formulated into both tablets and capsules/sachets. The claims cover numerous materially different APIs and formulation systems without sufficient representative examples showing the claimed MUPS architecture universally provides an extended-release profile across the scope of the claims. Thus, the working examples are not commensurate in scope with the breadth of the claims.
(H) The quantity of experimentation needed to make or use the invention based on the
content of the disclosure:
In view of the foregoing analysis, the quantity of experimentation to practice the full
scope of the invention would be undue. The skilled artisan would be required to perform extensive API-specific experimentation. This experimentation would need to be repeated for many APIs and excipient combination covered by the claims. Such experimentation would not amount to routine optimization of a known working formulation, but rather would be necessary to determine which combinations within the broadly claimed genus actually produced an extended-release MUPS composition.
The quantity of experimentation that amounts to far more than routine optimization supports a conclusion that the specification does not enable the full scope of the claims.
Considering the Wands factors as a whole, the currently claimed invention lacks scope of enablement. A significant amount of undue experimentation would be required to make the composition under the full scope of the claimed invention. Although the specification may enable a limited number of extremely specific MUPS formulations, the claims broadly encompass extended-release multi-particulate compositions for a large and diverse genus of APIs and materials. The specification does not provide sufficient representative examples, predictive guidance, or formulation rules commensurate with the broad scope of the claims.
Claim Rejections - 35 USC § 112(b)
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 1-15 and 23-24 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 1 is rejected as being indefinite for the following reasons:
Claim 1 recites “…extra-granular portion containing tableting excipients at least one or more selected from categories of diluent, disintegrant, binder, glidant, and lubricant.” This claim wording is ambiguous because a lack of proper grammar. It is unclear whether the extra-granular portion must include at least one excipient selected from any one of the listed categories, or whether it must include at least one excipient from each listed category.
Furthermore, claim 1 recites the terminology “tabletting.” This term is not defined or even mentioned in the specification and therefore, one of ordinary skill could not determine the metes and bounds of the claim.
Additionally, claim 1 contains many improper dependencies that lack antecedent basis within the claim. For instance, (a) recites “core spheres,” but (b) only refers to the “core.” Similarly, (c) recites “functional coating over seal coated pellets” and pellets is not mentioned previously in the claim. Furthermore, (c) recites “functional coating,” but (d) refers to “functional coated pellets.”
Claim 1 also recites “(c)…other excipients…” It is unclear what the term ‘other’ is meant to clarify. Does this indicate the excipient in (c) is different from that of (a)? Is it meant to imply the release controlling polymer contains an excipient? Do parts (a) and (c) require multiple excipients (as indicated by the plural writing of excipient)? So, one would not be infringing upon part (c) of the claim if only one excipient was added with the release controlling polymer?
Claims 3, 7, and 9 are included in this rejection because of their dependency on, and requiring all the limitations of, instant claim 1.
Claim 2 is rejected as being indefinite for the following reasons:
Claim 2 recites “[t]he composition as claimed in claim 1, where excipients are…” Excipients are recited twice in claim 1 under core spheres and functional coating. Claim 1 fails to provide primary antecedent basis for excipients and claim 2 fails to provide secondary antecedent basis for excipients. It is unclear whether ‘excipients’ refers to the excipients in the core spheres, the functional coating, or both.
Furthermore, claim 2 recites a list “wherein the excipients are…” The list contains multiple materials separated by the conjunction ‘and,’ thereby requiring that the excipients are all of the recited materials of the list. Applicant is strongly urged to refer to USPTO’s guidance on claim drafting and thoroughly review claims for grammatical errors prior to filing.
For purposes of compact prosecution, this claim will be read as excipients selected from the list, instead of requiring every single material recited in the list.
Claims 4 and 5 are rejected as being indefinite for the following reasons:
Claim 4 recites the active pharmaceutical ingredient (API) is a “high soluble high dose.” It is unclear what ‘high soluble’ is (highly soluble?) and Applicant has not defined this terminology in the specification. Similarly, claim 5 recites the API is a “low soluble high dose” (poorly soluble?).
Applicant has not defined the parameters of ‘high soluble,’ ‘low soluble,’ or ‘high dose’ in the specification and these terms are so broad that one of ordinary skill in the art would not know what constitutes the metes and bounds of the claim.
In addition, claim 5 recites the phrase “and the like” which renders the scope of the claimed genus unclear. The claim does not provide objective boundaries for determining which additional active pharmaceutical ingredients could be included by the phrase “and the like.”
Claim 6 is rejected as being indefinite for the following reason:
As described above under claim 2, claim 6 recites a list “wherein the diluent is…” The list contains multiple materials separated by the conjunction ‘and,’ thereby requiring that the diluent is all of the recited materials of the list.
For purposes of compact prosecution, this claim will be read as diluents selected from the list, instead of requiring every single material recited in the list.
Claim 8 is rejected as being indefinite for the following reasons:
As described above under claim 2, claim 8 recites a list “wherein the coating polymer is…” The list contains multiple materials separated by the conjunction ‘and,’ thereby requiring that the coating polymer is all of the recited materials of the list.
For purposes of compact prosecution, this claim will be read as a coating polymer selected from the list, instead of requiring every single material recited in the list.
Claim 8 is further considered indefinite because within the list of available coating polymers, Applicant claims celluloses and also many types of celluloses such as ethyl cellulose. The claimed celluloses would include ethyl cellulose, so it is unclear why Applicant has claimed specific types of cellulose and the broad category of celluloses. In addition, it is unclear why specific compounds are claimed in the plural such as ethyl celluloses, hydroxypropyl celluloses, etc. This is especially unclear considering the claim recites “the coating polymer is…” implying a singular material, but then lists the materials in plural form.
Claim 8 further indicates the coating polymer can be selected from sugars. However, some sugars are not polymers (e.g., glucose, fructose). Applicant is required to claim their invention so that one of ordinary skill could determine the metes and bounds of the claim. It is unclear if the use of glucose in the seal coating step would constitute infringement under this claim because it is a sugar, but not polymer.
Claim 10 is rejected as being indefinite for the following reason:
As described above under claim 2, claim 10 recites a list “wherein the plasticizer is…” The list contains multiple materials separated by the conjunction ‘and,’ thereby requiring that plasticizer is all of the recited materials of the list.
For purposes of compact prosecution, this claim will be read as a plasticizer selected from the list, instead of requiring every single material recited in the list.
Claim 11 is rejected as being indefinite for the following reason:
Claim 11 recites a list “…wherein the anti-adherent or anti-tacking agent is…” There is no conjunction in the recited list and therefore, it is unclear if the claim requires all recited materials of the list or selected from a single recited material of the list.
For purposes of compact prosecution, this claim will be read as a plasticizer selected from the list, instead of requiring every single material recited in the list.
Claim 12 is rejected as being indefinite for the following reason:
As described above under claim 2, claim 12 recites a list “wherein the disintegrant is…” The list contains multiple materials separated by the conjunction ‘and,’ thereby requiring that disintegrant is all of the recited materials of the list.
For purposes of compact prosecution, this claim will be read as a disintegrant selected from the list, instead of requiring every single material recited in the list.
Claim 13 is rejected as being indefinite for the following reason:
As described above under claim 2, claim 13 recites a list “wherein the glidant is…” The list contains multiple materials separated by the conjunction ‘and,’ thereby requiring that glidant is all of the recited materials of the list.
For purposes of compact prosecution, this claim will be read as a glidant selected from the list, instead of requiring every single material recited in the list.
Claim 14 is rejected as being indefinite for the following reason:
As described above under claim 2, claim 14 recites a list “wherein the lubricant is…” The list contains multiple materials separated by the conjunction ‘and,’ thereby requiring that lubricant is all of the recited materials of the list.
For purposes of compact prosecution, this claim will be read as a lubricant selected from the list, instead of requiring every single material recited in the list.
Claim 15 is rejected as being indefinite for the following reasons:
Claim 15 recites “[t]he composition as claimed in claim 1, wherein the solvent is…” Solvents are recited twice in claim 1 under seal coating and second seal coating. It is unclear whether ‘the solvents’ refers to the solvents in the seal coating, the second seal coating, or both.
As described above under claim 2, claim 15 recites a list “wherein the solvent is…” The list contains multiple materials separated by the conjunction ‘and,’ thereby requiring that solvent is all of the recited materials of the list.
For purposes of compact prosecution, this claim will be read as a solvent selected from the list, instead of requiring every single material recited in the list.
The lack of proper grammar in claim 23 is so severe it exceeds the threshold of a claim objection because one of ordinary skill in the art cannot ascertain the metes and bounds of the claim.
As an example, claim 23 recites, in part, “…extragranular portion containing microcrystalline cellulose, copovidone, colloidal silicon dioxide and sodium stearyl fumarate or magnesium stearate for lubricating and compressing…” It is impossible to ascertain which materials are intended to be included in the extragranular portion because the claim lacks proper grammar (e.g., appropriate use of commas). Does the extragranular portion comprise microcrystalline cellulose, copovidone, colloidal silicon dioxide, and sodium stearyl fumarate? Could the extragranular portion comprise only magnesium stearate? Similarly, the coating polymer is PEG, Hypromellose, Eudragit, or requiring Opadry and water together? Or, does the coating polymer require a selection from PEG, Hypromellose, Eudragit, or Opadry, and whatever selection of polymer chosen also requires water? In addition, the conjunctions used to modify the lists contained within claim 23 are inappropriate if applicant did not intend for every material listed to be included in the phases of preparation (see discussion of the conjunction ‘and’ in the rejections above).
Claim 23 is so unclear that the metes and bounds of the claimed invention cannot be reasonably determined. In particular and as discussed above, claim 23 recites lists of materials but due to the lack of proper comma placement, the scope of the claim cannot be ascertained. The examiner cannot determine what subject matter must be searched or compared to the prior art. Accordingly, examination on the merits under 35 U.S.C. §102 and §103 is not practicable until the claim is amended to clearly define the invention. Therefore, examination of claim 23 is limited to the fundamental defects under 35 U.S.C. §112(b). See 37 CFR §1.104(b) and MPEP §2173.06 (II).
Claims 8, 23, and 24 contain the trademark/trade name Opadry. Claim 23 contains the trademark/trade name Eudragit.
Where a trademark or trade name is used in a claim as a limitation to identify or describe a particular material or product, the claim does not comply with the requirements of 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph. See Ex parte Simpson, 218 USPQ 1020 (Bd. App. 1982). The claim scope is uncertain since the trademark or trade name cannot be used properly to identify any particular material or product. A trademark or trade name is used to identify a source of goods, and not the goods themselves. Thus, a trademark or trade name does not identify or describe the goods associated with the trademark or trade name. In the present case, the trademark/trade name is used to identify/describe materials within a composition and, accordingly, the identification/description is indefinite because the company could change the formulation of the trademarked material, thus changing the scope of the claim with which the trademarked ingredient is recited. Therefore, one of ordinary skill would be unable to ascertain the scope of the claims recited the trademarked material.
Claim 24 recites the limitation “tablet” in claim 1. There is insufficient antecedent basis for this limitation in the claim. Claim 1 does not recite a tablet.
Claim Rejections - 35 USC § 112(d)
The following is a quotation of 35 U.S.C. 112(d):
(d) REFERENCE IN DEPENDENT FORMS.—Subject to subsection (e), a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
The following is a quotation of pre-AIA 35 U.S.C. 112, fourth paragraph:
Subject to the following paragraph [i.e., the fifth paragraph of pre-AIA 35 U.S.C. 112], a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
Claim 24 is rejected under 35 U.S.C. 112(d) or pre-AIA 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for failing to further limit the subject matter of the claim upon which it depends, or for failing to include all the limitations of the claim upon which it depends.
Claim 24, depending from the composition of claim 1, recites a tablet that is optionally coated with Opadry® ready to use film coating. However, claim 1 does not expressly recite a tablet and the phrase “optionally coated” does not require the presence of a coating because it encompasses both coated and uncoated embodiments. Therefore, claim 24 does not clearly add a further limitation to the composition of claim 1. Applicant may cancel the claim(s), amend the claim(s) to place the claim(s) in proper dependent form, rewrite the claim(s) in independent form, or present a sufficient showing that the dependent claim(s) complies with the statutory requirements.
Claim Rejections - 35 USC § 103
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, 6-11, 13-15, and 24 are rejected under 35 U.S.C. 103 as being unpatentable over Deshpande (WO 2020/044314 A1; published 05 March 2020).
Deshpande teaches modified release dosage forms of vitamin D compounds (abstract).
Regarding claim 1 –
Claim 1 recites:
“A composition of extended release multiple unit pellet system comprising…”
Deshpande teaches extended-release multi-particulate dosage forms ([0033]).
Claim 1 further recites:
“(a) core spheres containing active pharmaceutical ingredient and optionally excipients…”
Deshpande teaches API-containing seeds/pellets in a layered formulation, including a starter seed having a layer of API ([0087]).
Claim 1 further recites:
“(b) seal coating over the core containing coating polymer and one or more solvents…”
Deshpande teaches a seal-coating over the API-containing pellet/seed, such as low-viscosity Hypromellose) to smooth the seed surface after API layering/coating and to achieve uniform coatings at subsequent stages ([0087]).
Claim 1 further recites:
“(c) functional coating over seal coated pellets containing release controlling polymers and other excipients…”
Deshpande teaches that over the seal coating is an extended-release polymer coating containing a water-insoluble polymer with a pore former ([0087]).
Claim 1 further recites:
“(d) second seal coating over the functional coated pellets containing coating polymer and one or more solvents…”
Deshpande teaches that over the functional coating is an optional seal coating containing a polymer and solvent ([0087]).
Claim 1 further recites:
“(e) extra-granular portion containing tabletting (sic) excipients at least one or more selected from categories of diluent, disintegrant, binder, glidant, and lubricant.”
Deshpande teaches that the dried pellets can be optionally coated with a lubricant ([0099]).
Regarding claims 2 and 10, Deshpande teaches excipients for seed and coating materials can be selected from those generally known in the art, which include: plasticizers ([0090]). Deshpande further teaches the plasticizers are selected from: polyethylene glycol, triethyl citrate, and dibutyl sebacate ([0090]).
Regarding claim 3, Deshpande teaches the API used in the invention, vitamin D, is administered to treat a vitamin-D responsive condition or disease ([0107]). These vitamin-D responsive conditions or diseases include type I diabetes, inflammatory bowel disease, and cardiovascular diseases ([0108]). Under the broadest reasonable interpretation of claim 3, vitamin D/vitamin D analogs can be treated as anti-diabetic agents, anti-hypertensive agents, or anti-inflammatory agents because Deshpande teaches vitamin D/vitamin D analogs have anti-diabetic, anti-hypertensive, and anti-inflammatory properties.
Regarding claim 6, Deshpande teaches diluent excipients may be utilized ([0099]) and such diluent excipients include: celluloses such as microcrystalline cellulose and starch ([0069]).
Regarding claim 7, Deshpande teaches the formulation can include one or more binders selected from a list that includes: hydroxypropyl methyl cellulose, starch, gelatin, and sodium alginate ([0071]).
Regarding claim 8, Deshpande teaches the formulation can include coating materials such as water-soluble polymers like Hypromellose (hydroxypropyl methylcellulose) or polyvinylpyrrolidone ([0073]).
Regarding claim 9, Deshpande teaches the formulation can include an extended-release polymer such as ethyl cellulose and Eudragit® (p. 62, claim 17).
Regarding claims 11, 13, and 14, Deshpande teaches the formulation includes talc and refers to talc as a lubricant. Deshpande further teaches the addition of talc in the final stages of pellet formulation ([0099]). The claimed lists of claims 11, 13, and 14 contain overlapping compounds. It is unclear how talc added as an anti-adherent or anti-tacking agent (claim 11) differs in structure from the talc added as a glidant (claim 13) or from the talc added as a lubricant (claim 14). Applicant’s specification fails to indicate which structure of talc is necessary to achieve and differentiate between the claimed properties of anti-adherent/anti-tacking, lubricant, or glidant. Therefore, since Deshpande adds talc to the formulation during the same claimed extra-granular portion, it is assumed the talc disclosed by Deshpande meets the limitations of the instantly claimed talc in claims 11, 13, and 14.
Regarding claim 15, Deshpande teaches the suitable solvents of the invention include: acetone, methanol, or water (p. 21 and 22 – Table 4).
Claim 24 only requires the optional addition of Opadry® as a tablet coating. Deshpande teaches Opadry® coating as a final coating product ([0090]).
Deshpande therefore teaches embodiments of extended-release multiple unit pellet systems. The difference between the applied reference and the claimed invention is that the
applied reference may not teach the instantly claimed method with particularity so as to amount
to anticipation. See MPEP “[t]he identical invention must be shown in as complete detail as is
contained in the ... claim.” Richardson v. Suzuki Motor Co., 868 F.2d 1226, 1236, 9 USPQ2d
1913, 1920 (Fed. Cir. 1989). The elements must be arranged as required by the claim, but this is
not an ipsissimis verbis test, i.e., identity of terminology is not required. In re Bond, 910 F.2d
831, 15 USPQ2d 1566 (Fed. Cir. 1990). Deshpande discloses various embodiments of an extended-release dosage form, excipients solvents, coating polymers, release controlling polymers, diluents, binders, glidants, and lubricants requiring the skilled artisan to choose from those embodiments to arrive at the currently claimed invention.
With that said, the applied reference discloses the elements of the claimed composition
with sufficient guidance, particularity, and with a reasonable expectation of success for the
skilled artisan, that the invention would have been prima facie obvious to one of ordinary skill in
the art, prior to the effective filing date. Deshpande discloses the claim limitations of instant claims 1-3, 6-11, 13-15, and 24 with a reasonable expectation of success –it would have been obvious to pick and choose from the disclosed components, together forming embodiments of extended-release dosage forms, because Deshpande discloses successful creation of compositions from those disclosed components. Therefore, Deshpande makes obvious that which is currently claimed in instant claims 1-3, 6-11, 13-15, and 24.
Claims 4 and 12 are rejected under 35 U.S.C. 103 as being unpatentable over Deshpande as applied to claims 1-3, 6-11, 13-15, and 24 above, and further in view of Tiwari (cited in previous office action).
While Deshpande discloses extended-release dosage formulations containing the composition of claims 1-3, 6-11, 13-15, and 24 as discussed above, Deshpande does not expressly teach APIs as recited in instant claims 4 and 12. However, this feature is made obvious over Tiwari.
Tiwari teaches extended-release pellets, comprising an inert core, drug layer, and an extended-release polymer layer, compressed into tablets (abstract).
While Deshpande teaches vitamin D forms, such as calcifediol, as the API within the pellet composition, Tiwari comparatively teaches metoprolol as an API suitable for use in multiple unit pellet system (MUPS) comprising extended-release polymer-coated pellets and tablet excipients (p. 1, lines 9-15).
Tiwari discloses metoprolol is a selective beta-blocker used in the treatment of cardiovascular disorders such as hypertension, i.e., an anti-hypertensive agent (p. 1, lines 15-16).
Regarding claim 4, Tiwari discloses the metoprolol or its salts, such as succinate, may be used in the invention (p. 7, lines 7-9). As previously mentioned, it is unclear what is meant by the ‘high soluble high dose’ limitation in claim 4. Therefore, under the broadest reasonable interpretation of this claim, since metoprolol succinate is a claimed API, it is assumed it meets the ambiguous ‘high soluble high dose’ limitation.
Regarding claim 12, Deshpande teaches the formulation can include additional functional additives such as release modifiers ([0064]). Such release modifiers include disintegrants ([0066]). However, Deshpande does not disclose specific disintegrants. Tiwari cures this deficiency by providing specific disintegrants suitable for use in an extended-release MUPS which include croscarmellose sodium (p. 11, lines 19-21). Thus, Tiwari provides evidence of specific disintegrants known in the art as capable for use in the genus of disintegrants disclosed by Deshpande.
It would have been obvious to one of ordinary skill, before the effective filing date of the claimed invention, to use metoprolol succinate, a known highly soluble API, in the extended-release multi-particulate dosage form system disclosed by Deshpande. One would be motivated to do so because Tiwari teaches metoprolol succinate was a known candidate for extended-release particulate formulations and teaches conventional coating and extra-granular tableting approaches for that API. Since both Deshpande and Tiwari disclose similar MUPS architecture for API, one of ordinary skill could predict success in substituting the vitamin D API in Deshpande with metoprolol succinate disclosed by Tiwari. This is a simple substitution of one known element for another to obtain predictable results. Therefore, claims 4 and 12 are made obvious over Deshpande in further view of Tiwari.
Claim 5 is rejected under 35 U.S.C. 103 as being unpatentable over Deshpande as applied to claims 1-3, 6-11, 13-15, and 24 above, and further in view of Bhavarisetti (WO 2009/087690 A2; published 16 July 2009).
While Deshpande discloses extended-release dosage formulations containing the composition of claims 1-3, 6-11, 13-15, and 24 as discussed above, Deshpande does not expressly teach APIs as recited in instant claim 5. However, this feature is made obvious over Bhavarisetti.
Bhavarisetti teaches extended-release tablets having a core comprising carbamazepine and extended-release polymers (abstract).
While Deshpande teaches vitamin D forms, such as calcifediol, as the API within the pellet composition, Bhavarisetti comparatively teaches carbamazepine as an API suitable for use in multiple unit pellet system (MUPS) comprising extended-release polymer-coated pellets (p. 1, lines 4-8; p. 2, lines 16-21).
Regarding claim 5, Bhavarisetti discloses the Carbamazepine is contained within the core (p. 9, lines 11-15). As previously mentioned, it is unclear what is meant by the ‘low soluble high dose’ limitation in claim 5. Therefore, under the broadest reasonable interpretation of this claim, since Carbamazepine is a claimed API, it is assumed it meets the ambiguous ‘low soluble high dose’ limitation.
It would have been obvious to one of ordinary skill, before the effective filing date of the claimed invention, to use Carbamazepine, a known poorly soluble API, in the extended-release multi-particulate dosage form system disclosed by Deshpande. One would be motivated to do so because Bhavarisetti teaches Carbamazepine was a known candidate for extended-release particulate formulations and teaches conventional coating and extra-granular tableting approaches for that API. Since both Deshpande and Bhavarisetti disclose similar MUPS architecture for API, one of ordinary skill could predict success in substituting the vitamin D API in Deshpande with Carbamazepine disclosed by Bhavarisetti. This is a simple substitution of one known element for another to obtain predictable results. Therefore, claim 5 is obvious over Deshpande in further view of Bhavarisetti.
Conclusion
Claims 1-15 and 23-24 are rejected. No claim is allowed.
Communication
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Julia A. Rossi whose telephone number is (571)272-0138. The examiner can normally be reached M-Th 7:30-5:30 (MST).
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, Robert A. Wax can be reached at (571)272-0623. 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.
/JULIA A. ROSSI/Examiner, Art Unit 1615
/Robert A Wax/Supervisory Patent Examiner, Art Unit 1615
Prosecution Insights