DETAILED ACTION
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA . 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 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.
Status of the Claims
The response and amendment filed 07/20/2026 is acknowledged.
Claims 1-2, 7, 9-11, 14, 18-19, 21-24, 26 and 28-33 are pending.
Claims 29-33 are new.
Claims 18-19, 21-24, 26, and 28 remain withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected invention, there being no allowable generic or linking claim.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 09/18/2025.
Claims 1-2, 7, 9-11, 14, and 29-33 are treated on the merits in this action.
The following rejections and/or objections are either reiterated or newly applied. They constitute the complete set presently being applied to the instant application. Rejections not reiterated herein have been withdrawn.
Withdrawn
The rejection of claim 2 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subject matter which the inventor or a joint inventor, or for pre-AIA the applicant regards as the invention has been withdrawn because of Applicant’s amendment.
The rejection of claim 12 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subject matter which the inventor or a joint inventor, or for pre-AIA the applicant regards as the invention has been withdrawn because of Applicant’s amendment.
The rejection of claim 14 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subject matter which the inventor or a joint inventor, or for pre-AIA the applicant regards as the invention has been withdrawn because of Applicant’s amendment.
The rejection of claim 5 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 pre-AIA the applicant regards as the invention has been withdrawn because of Applicant’s amendment.
The rejection of claim 4 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 pre-AIA the applicant regards as the invention has been withdrawn because of Applicant’s amendment.
The rejection of claim 16 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 pre-AIA the applicant regards as the invention has been withdrawn because of Applicant’s amendment.
The previous rejection of claims 1-2, 4-5, 7-12, 14, and 16 under 35 U.S.C. 102(a)(1) and 35 U.S.C. 102(a)(2) as being anticipated by Fujii, WO 2019013310 A1 has been withdrawn because of Applicant’s amendment. However, Fujii has been reapplied using different teachings to address the amended subject matter.
The rejection of claims 1-2, 4-5, 7, 9-10, 12, 14, and 16 under 35 U.S.C. 102(a)(1) and 35 U.S.C. 102(a)(2) as being anticipated by Ecseri, WO 2015028829 A1 (cited on IDS dated 09/18/2025) has been withdrawn because of Applicant’s amendment.
The previous rejection of claims 1-2, 4-5, 7-12, 14, and 16 under 35 U.S.C. 102(a)(1) and 35 U.S.C. 102(a)(2) as being anticipated by Kurasawa, US 20150037423 has been withdrawn because of Applicant’s amendment. However, Kurasawa has been reapplied using different teachings to address the amended subject matter.
The previous rejection of claims 1-2, 4-5, 7-12, 14, and 16 under 35 U.S.C. 103 as being unpatentable over Fujii, WO 2019013310 A1 has been withdrawn because of Applicant’s amendment. However, Fujii has been reapplied using different teachings to address the amended subject matter.
Response to Arguments
Applicant’s arguments with respect to claim(s) 1-2, 7, 9-11, 14, and 29-33 have been considered but are moot because the new ground of rejection does not rely on any reference applied in the prior rejection of record for any teaching or matter specifically challenged in the argument.
Rejections Addressing Applicant’s Amendment
Claim Rejections - 35 USC § 112
The following is a quotation of 35 U.S.C. 112(a):
(a) IN GENERAL.—The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor or joint inventor of carrying out the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), first paragraph:
The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same and shall set forth the best mode contemplated by the inventor of carrying out his invention.
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.
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.
Claims 1-2, 7, 9-11, 14, and 29-33 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventor(s), at the time the application was filed, had possession of the claimed invention.
This is a new matter rejection.
Claim 1 includes the limitations of:
(b) a first coating layer surrounding the core which comprises a polymer selected from gelatins, ovalbumin, gum arabic, polyethylene glycol (PEG), polyethylene oxides, polyoxyalkylene derivatives, poly(vinyl pyrrolidone) (PVP), polyvinyl alcohol (PVA), a vinylpyrrolidone-vinyl acetate copolymer, sodium carboxymethyl cellulose, sodium alginate, xantham gum, a polyvinylalcohol-polyethyleneglycol-copolymer and mixtures thereof; and
(c) a second coating layer surrounding the first coating layer, the second coating layer comprising particles of a sugar, a sugar alcohol, or any mixture thereof;
wherein no further coating layer is present between the first coating layer and the second coating layer; and
wherein, if the first coating layer comprises two or more discrete sublayers, the outermost sublayer comprises a polymer selected from gelatins, ovalbumin, gum arabic, polyethylene glycol (PEG), polyethylene oxides, polyoxyalkylene derivatives, poly(vinyl pyrrolidone) (PVP), polyvinyl alcohol (PVA), a vinylpyrrolidone-vinyl acetate copolymer, sodium carboxymethyl cellulose, sodium alginate, xantham gum, a polyvinylalcohol-polyethyleneglycol-copolymer and mixtures thereof.
The claim presents a combination of limitations which were not disclosed in the specification at the time of filing. Claim 1 requires that there be no further coating layer present between the first coating layer and the second coating layer. Claim 1 also requires that if the first coating layer comprises two or more discrete sublayers, the outermost sublayer comprises a polymer selected from gelatins, ovalbumin, gum arabic, polyethylene glycol (PEG), polyethylene oxides, polyoxyalkylene derivatives, poly(vinyl pyrrolidone) (PVP), polyvinyl alcohol (PVA), a vinylpyrrolidone-vinyl acetate copolymer, sodium carboxymethyl cellulose, sodium alginate, xantham gum, a polyvinylalcohol-polyethyleneglycol-copolymer and mixtures thereof.
Claim 1 encompasses a granule which comprises a first coating layer having two or more discrete sublayers, the outermost sublayer comprises a polymer selected from gelatins, ovalbumin, gum arabic, polyethylene glycol (PEG), polyethylene oxides, polyoxyalkylene derivatives, poly(vinyl pyrrolidone) (PVP), polyvinyl alcohol (PVA), a vinylpyrrolidone-vinyl acetate copolymer, sodium carboxymethyl cellulose, sodium alginate, xantham gum, a polyvinylalcohol-polyethyleneglycol-copolymer and mixtures thereof and wherein the granule has no further coating layer between the first coating layer and the second coating layer
The specification states that the outermost sublayer of the first coating layer is a further coating layer (Specification, e.g., pg. 35:15-20). On this basis the specification does not support a claim to a granule having no further coating layer between the first coating layer and the second coating layer, and a first coating layer comprising two or more discrete sublayers. These limitations in combination appear to be contradictory according to the disclosure. A granule comprising a coating layer comprising a sublayer and an outermost sublayer under a second coating layer necessarily has a first layer and a further layer between the first coating layer and the second coating layer. See additional discussion below in the 112(b) rejection.
Further, Applicant has not pointed out, and the examiner cannot find, support for a granule which comprises a first coating layer having two or more discrete sublayers, the outermost sublayer comprising a selected polymer, and wherein the granule has no further coating layer between the first coating layer and the second coating layer.
Applicant states support for these amendments may be found, for instance, at paragraph [0084] of the published specification, at original Claim 4, at original Claim 5, Example 2 (examples that do not contain any further coating layer between the first and second coating layers), and at paragraph [0139] of the published specification.
However, ¶ 0084 is silent to a granule which comprises a first coating layer having two or more discrete sublayers, the outermost sublayer comprising a selected polymer, and wherein the granule has no further coating layer between the first coating layer and the second coating layer.
Original claims 4 and 5 are silent to a granule which comprises a first coating layer having two or more discrete sublayers, the outermost sublayer comprising a selected polymer, and wherein the granule has no further coating layer between the first coating layer and the second coating layer.
Example 2 includes embodiments which do not contain any further coating layer between the first and second coating layers. However, the embodiments of Example 2 do not have a first coating layer having two or more discrete sublayers wherein the outermost layer comprises a polymer selected from those listed in claim 1. Therefore, Example 2 does not support a granule which comprises a first coating layer having two or more discrete sublayers with an outermost sublayer comprising a selected polymer and wherein the granule has no further coating layer between the first coating layer and the second coating layer.
The specification does not convey with reasonable clarity to those skilled in the art that, as of the filing date sought, the inventor was in possession of the invention as now claimed. See, e.g., Vas-Cath, Inc., 935 F.2d at 1563-64, 19 USPQ2d at 1117.
Claims 1-2, 7, 9-11, 14, and 29-33 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 pre-AIA the applicant regards as the invention.
Claim 1 includes the limitations of
(a) a core comprising an active pharmaceutical ingredient (API), food supplement or vitamin;
(b) a first coating layer surrounding the core which comprises a polymer selected from gelatins, ovalbumin, gum arabic, polyethylene glycol (PEG), polyethylene oxides, polyoxyalkylene derivatives, poly(vinyl pyrrolidone) (PVP), polyvinyl alcohol (PVA), a vinylpyrrolidone-vinyl acetate copolymer, sodium carboxymethyl cellulose, sodium alginate, xantham gum, a polyvinylalcohol-polyethyleneglycol-copolymer and mixtures thereof; and
(c) a second coating layer surrounding the first coating layer, the second coating layer comprising particles of a sugar, a sugar alcohol, or any mixture thereof;
wherein no further coating layer is present between the first coating layer and the second coating layer; and
wherein, if the first coating layer comprises two or more discrete sublayers, the outermost sublayer comprises a polymer selected from gelatins, ovalbumin, gum arabic, polyethylene glycol (PEG), polyethylene oxides, polyoxyalkylene derivatives, poly(vinyl pyrrolidone) (PVP), polyvinyl alcohol (PVA), a vinylpyrrolidone-vinyl acetate copolymer, sodium carboxymethyl cellulose, sodium alginate, xantham gum, a polyvinylalcohol-polyethyleneglycol-copolymer and mixtures thereof.
1) There is no antecedent basis for “the outermost sublayer.” It is not clear where this layer is or which previously established layer this refers to.
Clarification is required.
2) Claim 1 recites a first coating layer, and wherein no further coating layer is present between the first coating layer and the second coating layer, and also states the first coating layer may comprise two or more discrete sublayers. This arrangement is unclear. If there are sublayers under/within the “first coating layer” then the skilled artisan would reasonably consider the first sublayer coating the “first coating layer”. The outermost sublayer would be a “further coating layer” on the first sublayer coating layer between the first coating layer and the second coating layer. It is not clear how the skilled artisan would determine which coating layer is “a first coating layer.” It is not clear how the skilled artisan would determine which coating layer is an “outermost sublayer” rather than a “further coating layer.” The elements/layers making up the first coating layer, further coating layer, and second coating layer are arbitrary and confusing. Naming a layer an outermost sublayer or further coating layer is arbitrary. The skilled artisan cannot determine where “the first layer” begins and ends. The skilled artisan cannot determine where the second coating layer begins.
This is illustrated in the specification which states embodiments in which a “further” coating layer as described above is present between the first coating layer and the second coating layer are equivalent to embodiments in which no “further” coating layer is present, but wherein the first coating layer comprises two or more sublayers … i.e., wherein the outermost sublayer of the first coating layer is a “further” coating layer. See published application, e.g., 0141 or pp. 34:18-pg. 36:2.
The distinction between a first coating layer having two or more sublayers and a first coating layer having a further coating layer is semantic rather than structural since the “further” layer may also be called an outermost sublayer. There is no reasonable way for the skilled artisan to distinguish between a granule comprising a first coating layer containing two or more sublayers and a granule comprising a first coating layer and a further coating layer.
Further, since the skilled artisan understands from the specification that an embodiment which comprises a first coating layer comprising two or more discrete sublayers is an embodiment which comprises a first coating layer and a further coating layer, the limitation of wherein no further coating layer is present between the first coating layer and the second coating layer doesn’t make sense in the current claim when the first coating layer comprises two or more discrete sublayers.
If there is no further layer between the “first coating” and the “second coating,” as required by claim 1, then there cannot be two or more sublayers in the “first coating” because the specification indicates the outermost sublayer (of the first coating layer containing sublayers) is also known as a “further” coating layer between the first coating layer and the second coating layer.
Clarification is required
3) The term “substantially” in claim 1 is a relative term which renders the claim indefinite. The term “substantially” is not defined by the claim, the specification does not provide a standard for ascertaining the requisite degree, and one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. In this case, the term substantially is used in the phrase wherein said granules are substantially spherical. It is not clear how spherical a granule must be, or how or nonspherical a granule can be, to meet the limitations of the claim. There is no quantified threshold for sphericality presented in the application or well understood standard for comparison.
Clarification is required.
Claims 10 and 31 are 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 10 does not include all the limitations of claim 1 from which it depends. Claim 1 includes the limitation of wherein no further coating layer is present between the first coating layer and the second coating layer. Claim 10 has a first coating layer (first sublayer) and a further coating layer (at least a second discrete sublayer) which is between the first coating layer (first sublayer) and the second coating layer surrounding the first coating layer.
Claim 31 depends from claim 10.
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 31 is 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 pre-AIA the applicant regards as the invention.
There is a lack of antecedent basis for the sublayer closest to the core. The core is not structurally defined, e.g., it is not clear where the first layer ends and the core begins. Due at least in part to the lack of clarity regarding the “first coating layer” explained above, the relationship between the first layer, the sublayer closest to the core, and the core is not sufficiently defined. Therefore, the location of the sublayer closest to the core is defined by an unknown. This may refer to the first layer on the core or it may refer to any intermediate layer below the outermost sublayer or it may refer to any intermediate layer below the second coating layer.
A claim may be rendered indefinite when a limitation of the claim is defined by reference to an object and the relationship between the limitation and the object is not sufficiently defined. See MPEP 2173.05(b), II.
Clarification is required.
Claim Rejections - 35 USC § 102
The following is a quotation of the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action:
A person shall be entitled to a patent unless –
(a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale or otherwise available to the public before the effective filing date of the claimed invention.
(a)(2) the claimed invention was described in a patent issued under section 151, or in an application for patent published or deemed published under section 122(b), in which the patent or application, as the case may be, names another inventor and was effectively filed before the effective filing date of the claimed invention.
Claims 1-2, 7, 9, 10, 11, 14, and 29-30, and 32 are rejected under 35 U.S.C. 102(a)(1) and 35 U.S.C. 102(a)(2) as being anticipated by Fujii, WO 2019013310 A1.
Fujii teaches granules comprising a substantially spherical core containing an active pharmaceutical agent (API) and comprising multiple coatings, e.g. first and second coating layers. See Fujii, entire document, pg. 75, Table 1-4, reference example 3. The claimed core reads on Compound A containing particles. First coating layer reads on dissolution controlling substance coating layer comprising polysorbate 80. Second layer reads on the water insoluble polymer coating layer and coagulation inhibiting substance coating layer comprising mannitol directly on the first layer.
Polyoxyalkylene derivative reads on polysorbate 80.
Alternatively, core reads on Compound A containing particles. First coating sublayer reads on water soluble polymer coating layer and first coating layer outermost sublayer reads on dissolution controlling substance coating layer comprising polysorbate 80 (outermost sublayer comprises a polyoxyalkylene derivative). Second layer reads on the water insoluble polymer coating layer and coagulation inhibiting substance coating layer comprising mannitol directly on the first layer.
Mannitol outer coating layer is taught as a coagulation inhibiting substance (Fujii, e.g., 0025-0027, 0069, e.g., Table 1-2, 0071, e.g., Table 1-4, claims). Coagulation inhibiting substance may be saccharides or sugar alcohol, e.g., mannitol erythritol, trehalose, maltitol (Fujii, e.g., 0025, e.g., pg. 14:26-pg. 15:3, tables 1-2 and 1-4). Coagulation inhibiting substance may be applied as a suspension, i.e., resulting in particles on the outer layer, i.e., rough surface (Fujii, e.g., ¶ spanning pp. 19-20). Thus, the skilled artisan would have at once envisaged API granules comprising a core and having first and second coatings including a second coating layer containing an outer coagulating inhibiting substance coating containing saccharides or sugar alcohol in the form of particles. Even if applied as a solution, particles of mannitol having some size will be present, particularly after the coating is dried. Coagulation inhibiting substance may be applied with a binder (Fujii, e.g., 0025-0027, 0069, e.g., Table 1-2, 0071, e.g., Table 1-4, claims). Coagulation inhibiting substance is effective for taste masking (Fujii, e.g., 0095, experimental example 7, Table 3, pg. 106).
Fujii does not expressly teach wherein at least 90% of the granules by number have a diameter of greater than 200 µm and in which at least 90% of the granules by number have a diameter of less than 1400 µm
However, Fujii teaches particle sizes which substantially overlap with the range recited in claim 11, e.g., about 75 micron to about 750 micron (Fujii, e.g., claim 7). Further, Fujii teaches 350 micron sieved particles which is a clearly disclosed value within the claimed range and specifically points to particles sized within the claimed range. The degree of overlap and additional guidance offers sufficient specificity to anticipate the range recited in claim 11. Inert cores are found in Fujii, e.g., 0036, pp. 21-22.
Separately, and applicable to claim 1, Fujii teaches outer layer granules comprising cellulose and hydroxypropylcellulose (food supplements) which granules also contain solid mannitol (particles of a sugar alcohol) and crospovidone (a polyvinylpyrrolidone). The process appears to result in a granule core which would contain mannitol particles in at least the outermost coating layer surrounding the granule core (second coating layer as claimed). Since the binder liquid is sprayed over a period of time, the coating grows as particles agglomerate and further binder is applied. Thus, it can be said that the coating comprises many layers, e.g., first and second and so forth, and wherein the first coating layer comprises a polyvinylpyrrolidone. See Fujii, e.g., pg. 99:16-30. This embodiment applies to claims 1-2, 7, 9, 10, 14, 29, 30, and 32.
Product by process limitations “in a high shear mixer” and “wet coating method,” and “fluid bed coating or high shear melt coating” do not imply any structural limitations beyond those expressly recited in the claims. Further, the prior art teaches wet coating methods including spraying of a binder solution on the granules.
Fujii anticipates the subject matter of instant claims 1-2, 7, 9, 10, 11, 14, and 29-30, and 32.
Claims 1-2, 7, 9, 10, 11, 14, and 29-30, and 32 are rejected under 35 U.S.C. 102(a)(1) and 35 U.S.C. 102(a)(2) as being anticipated by Kurasawa, US 20150037423.
Kurasawa teaches granules comprising a core and API, which granules also comprise a mannitol (water soluble sugar alcohol) outer coating. The claimed core reads on fine granules containing a drug layer (Kurasawa, e.g., 0308). The claimed first layer reads on the intermediate and polymer coatings of Kurasawa, e.g., 0309-0310 wherein the layer comprises polysorbate 80 which is a polyoxyalkylene derivative. The claimed second layer reads on the mannitol coating of Kurasawa, e.g., 0312 directly on the first layer. The particle size range for the granules is entirely within the claimed range, e.g., 250-425 microns (Kurasawa, entire document, e.g., examples, e.g., 0308-0314, production examples 28-34 and claims). Since the particle size is entirely within the claimed range, the limitation of wherein at least 90% of the granules by number have a diameter of greater than 200 µm and in which at least 90% of the granules by number have a diameter of less than 1400 µm is met. The water-soluble sugar alcohol may be mannitol, erythritol, maltitol and combinations may be used in particle form as the outer coating layer (Kurasawa, e.g., 0228). The water-soluble sugar alcohol outer layer prevents coagulation of the granules (Kurasawa, e.g., 0179). Particles of the coagulation inhibiting water soluble sugar alcohol, e.g., mannitol, would appear to be present, particularly after the coating is dried.
Further with respect to the claimed second coating layer, Kurasawa teaches the mannitol coated API granules are further mixed with outer layer granules containing solid mannitol particles to give a solid preparation containing mannitol coated API granules further comprising an outer layer of granules containing solid mannitol particles. See Kurasawa, e.g., 0275 and 0315.
Separately, and applicable to claim 1, Kurasawa teaches granules comprising cellulose and hydroxypropylcellulose (food supplements) which granules also contain solid mannitol (particles of a sugar alcohol) and a mannitol binder. The process appears to result in a granule core which would contain mannitol particles in at least one coating layer surrounding the granule core. Since the binder liquid is sprayed over a period of time, the coating grows as particles agglomerate and further binder is applied. Thus, it can be said that the coating comprises many layers, e.g., first and second and so forth.
Product by process limitations “in a high shear mixer” and “wet coating method,” and “fluid bed coating or high shear melt coating” do not imply any structural limitations beyond those expressly recited in the claims. Further, the prior art teaches wet coating methods including spraying of a binder solution on the granules.
Kurasawa anticipates the subject matter of instant claims 1-2, 7, 9, 11, 14, and 29-30, and 32.
Claims 1-2, 7, 9, 10, 11, 14, and 29-32 are rejected under 35 U.S.C. 102(a)(1) and 35 U.S.C. 102(a)(2) as being anticipated by Shimizu, US 20020142034.
Shimizu teaches spherical granules (Shimizu, e.g., 0014) comprising a core, a plural enteric film layer, and an outer layer comprising mannitol particles directly on the plural enteric layer (Shimizu, e.g., examples 5-8). The plural enteric layer corresponding to the claimed “first coating layer” comprises three sublayers wherein the sublayer closest to the core is an enteric coating layer comprising a methacrylate copolymer (Shimizu, e.g., 0284). The outermost sublayer comprises polyethylene glycol (Shimizu, e.g., 0284-0285, enteric film coating liquid (A) containing polyethylene glycol). The claimed granule comprising a core, a first coating layer comprising two or more discrete sublayers, the outermost sublayer comprising polyethylene glycol and a second coating layer comprising particles of a sugar, sugar alcohol or mixture thereof, reads on examples 5-8 of Shimizu. The first coating layer is a physical barrier coating and/or a taste masking agent as claimed.
Applicable to claim 11: the particle sizes range from 250 µm to 450 µm with an average size of 333.7 µm (Shimizu, e.g., 0287-0288).
Product by process limitations, e.g., “in a high shear mixer” and “wet coating method,” and “fluid bed coating or high shear melt coating” do not imply any structural limitations beyond those expressly recited in the claims. Further, the prior art teaches wet coating methods including spraying of on the granules.
Shimizu anticipates the subject matter of instant claims 1-2, 7, 9, 10, 11, 14, and 29-32
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 of this title, 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.
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 1-2, 7, 9, 10, 11, 14, and 29-33 are rejected under 35 U.S.C. 103 as being unpatentable over Shimizu, US 20020142034 and Fujii, WO 2019013310 A1.
All of the teachings of Shimizu enumerated above apply here.
Shimizu teaches wherein the second layer comprises a sugar alcohol, e.g., mannitol, maltitol, erythritol (Shimizu, e.g., 0117). Shimizu does not expressly teach the second coating layer comprising maltitol, trehalose, or a mixture thereof an erythritol.
Fujii teaches mannitol, maltitol, trehalose and erythritol were known coagulation inhibiting substances which, when present in an outer layer on granules, improves handling and storage stability (Fujii, e.g., 0025-0026).
It would have been obvious to one of ordinary skill in the art before the effective filing date of the presently claimed invention to modify granules, e.g., examples 5-8, of Shimizu, by incorporating maltitol and erythritol in the outer layer with a reasonable expectation of success. Since the granules of Shimizu already have mannitol, the skilled artisan would have been motivated to include other sugar alcohols, e.g., maltitol and erythritol to improve the granules in the same way suggested by Fujii. The skilled artisan would have had a reasonable expectation of success because Shimizu’s granules already contain mannitol, and because Fujii teaches mannitol, maltitol and erythritol offer similar benefits when formulated as an outer layer on granules.
Accordingly, the subject matter of claims 1-2, 7, 9, 10, 11, 14, and 29-33 would have been prima facie obvious before the effective filing date of the presently claimed invention, absent evidence to the contrary.
Claims 1-2, 7, 9, 10, 11, 14, and 29-30, and 32-33 are rejected under 35 U.S.C. 103 as being unpatentable over Fujii, WO 2019013310 A1.
All of the teachings of Fujii enumerated above apply here.
This rejection is made in the alternative in the event the disclosure of Fujii is found insufficient to allow the skilled artisan to at once envisage a granule containing a core with a pharmaceutically active ingredient (API), additional layers, and a coagulating inhibiting substance coating containing saccharides or sugar alcohol in the form of particles.
Fujii clearly teaches coagulation inhibiting substance, e.g., sugar alcohols, may be applied as a solution or a suspension (Fujii, e.g., ¶ spanning pp. 19-20). Applying a suspension will necessarily result in particles on the outer layer, i.e., rough surface. Fujii also clearly teaches water soluble sugar alcohols may have a particle size of less than 50 mesh (Fujii, e.g., ¶ spanning pp. 23-24).
Thus, to the extent that Fujii may not clearly disclose sugar or sugar alcohol particles in the outer layer on a granule core containing a pharmaceutically active ingredient, these teachings in Fujii represents express teachings which would have prompted the skilled artisan to configure the coagulation inhibiting substance, specifically saccharide and/or sugar alcohols as particles in the outer coating corresponding to the second coating layer as claimed with a reasonable expectation of success. Fujii teaches applying a suspension of coagulation inhibiting substance (Fujii, e.g., pg. 77:14-19).
It would have been obvious before the effective filing date of the presently claimed invention to modify any of the saccharide and/or sugar alcohol coatings exemplified in Fujii on granule core containing a pharmaceutically active ingredient by formulating the saccharide and/or sugar alcohol in the outer layer as particles with a reasonable expectation of success. Since Fujii teaches the outer layer containing sugar and/or sugar alcohol may be applied as a suspension, the skilled artisan understood from Fujii that the outer layer may contain sugar and/or sugar alcohol particles which protrude from the surface to achieve coagulation inhibiting effect and taste masking. The skilled artisan would have had a reasonable expectation of success because Fujii also clearly teaches applying a suspension of coagulation inhibiting substance.
This rejection is also made in the alternative in the event it is determined that Fujii does not describe the claimed range with sufficient specificity to anticipate the subject matter of claim 11.
Acknowledging that Fujii does not expressly teach wherein at least 90% of the granules by number have a diameter of greater than 200 µm and in which at least 90% of the granules by number have a diameter of less than 1400 µm, it is noted that Fujii does teach a general particle size range which overlaps significantly with the claimed range. For example, Fujii teaches granules having a size ranging from 50 µm to 1000 µm preferably about 75 μm - about 750 μm, more preferably about 80 μm - about 500 μm, further preferably about 100 μm - about 400 μm (Fuji, e.g., pg. 6:25-30). Further, Fujii exemplifies a number of granules having a size overlapping significantly with the claimed range, e.g., 132 µm – 355 µm (Fujii, e.g., pg. 99:2-14).
In the case where the claimed ranges “overlap or lie inside ranges disclosed by the prior art” a prima facie case of obviousness exists. In re Wertheim, 541 F.2d 257, 191 USPQ 90 (CCPA 1976); In re Woodruff, 919 F.2d 1575, 16 USPQ2d 1934 (Fed. Cir. 1990). MPEP 2144.05.
It would have been obvious before the effective filing date of the presently claimed invention to optimize the size of the granules taught by Fujii within the general range, e.g., a size ranging from 50 µm to 1000 µm suggested therein with a reasonable expectation of success since the reference suggests sizes in this range are effective for rapid pharmacological effect.
Applicable to claim 33: Fujii teaches mannitol, maltitol, erythritol, and trehalose may be used as a coagulation inhibiting agent (Fujii, e.g., 0025-0026). It would have been obvious to one of ordinary skill in the art before the effective filing date of the presently claimed invention to modify Fujii formulation example 3 by using maltitol, trehalose and erythritol for the mannitol in the outer layer with a reasonable expectation of success. The skilled artisan would have seen this modification as a combination of equivalent coagulating substances to achieve predictable results. The skilled artisan would have been motivated use these coagulation inhibiting substances for improved handling of the granules and storage stability. The skilled artisan would have had a reasonable expectation of success because each of the named excipients were expressly taught as useful with or instead of mannitol.
Accordingly, the subject matter of claims 1-2, 7, 9, 10, 11, 14, and 29-30, and 32-33 would have been prima facie obvious before the effective filing date of the presently claimed invention, absent evidence to the contrary.
Conclusion
No claim is allowed.
Applicant's amendment necessitated the new ground(s) of rejection presented in this Office action. Accordingly, THIS ACTION IS MADE FINAL. See MPEP § 706.07(a). Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any nonprovisional extension fee (37 CFR 1.17(a)) pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the mailing date of this final action.
Correspondence
Any inquiry concerning this communication or earlier communications from the examiner should be directed to WILLIAM A CRAIGO whose telephone number is (571)270-1347. The examiner can normally be reached on Monday - Friday, 9am - 6pm, PDT.
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/WILLIAM CRAIGO/Examiner, Art Unit 1615
/SUSAN T TRAN/Primary Examiner, Art Unit 1615
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