DETAILED ACTION
Continued Examination Under 37 CFR 1.114
A request for continued examination under 37 CFR 1.114, including the fee set forth in 37 CFR 1.17(e), was filed in this application after final rejection. Since this application is eligible for continued examination under 37 CFR 1.114, and the fee set forth in 37 CFR 1.17(e) has been timely paid, the finality of the previous Office action has been withdrawn pursuant to 37 CFR 1.114. Applicant's submission filed on 08/01/2025 has been entered.
Response to Amendment
Applicant’s response of 08/01/2025 has been received and entered into the application file. Claims 1-8, 11, and 13-14 are pending in this application.
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.
Claims 1-8, 11, and 13-14 are rejected under 35 U.S.C. 103 as being unpatentable over Lee et al. (US 2011/0142889 A1), Kodgule et al. (WO 2016/016770 A1) and Kim et al. (US 2016/003046 A1).
Lee discloses a pharmaceutical composition for oral drug delivery comprising a solid dosage form containing a core comprising: an effective amount of a therapeutic agent, a permeation enhancer (disintegrant), excipient, and a layer atop the core (Abstract). In some embodiments, the composition can be further coated with an enteric material ([0011]). The matrix can be 0-20% of hydroxypropyl methylcellulose ([0084]) as well as hydroxypropyl cellulose ([0081]). The matrix can also comprise disintegrants such as croscarmellose, crospovidone, sodium starch glycolate ([0081]). The therapeutic agent is selected from the group consisting of acetyl cysteine ([0066]), glutathione ([0070]), vitamin B12 ([0066]), ubiquinone (similar to ubiquinol) ([0066]).
Lee teaches that the invention provides a pharmaceutical composition that is capable of modulating the pharmacokinetic profile of a therapeutic agent. The release kinetics of the therapeutic agent and the disintegrant can be modulated by a different composition and/or ratio of components in the core matrix, thickness of the coating layer, to provide a burst or immediate release, or an extended or sustained profile, depending on the desired therapeutic effect ([0016]).
Lee discloses that the core can be coated with layers of hydroxypropyl methylcellulose (HPMC) and/or ethyl cellulose ([0241]) and another enteric layer of Eudragit L30D-55 (methacrylic acid-ethyl acrylate copolymer, dissolution above pH 5.5) ([0020]).
Lee does not mention specific HPMCs with different viscosities.
Kodgule discloses a novel modified release pharmaceutical composition of sitagliptin (Abstract). The modified release composition can be divided into an immediate release part and an extended-release part (page 7, last paragraph). The osmotic push layer comprises one or more osmotic agents which includes hydrophilic vinyl and acrylic polymers such as poly(methacrylic) acid (page 27, last paragraph). Kodgule discloses a modified release tablet having a core comprising Hypromellose (HPMC K4M) and Hypromellose (HPMC K100M) plus an extended-release coating (outer coating) comprising poly(methacrylic) acid polymer and HPMC E5/Povidone K30 (page 33, Table 3).
HPMC K4M has a viscosity ranging between 3.0 and 5000 mPa.s at 2% in H2O at 20 degrees Celsius and the HPMC K100M has a viscosity ranging between 13500 and 280000 mPa.s at 2% in H2O at 20 degrees Celsius, as per claim 1.
Kim teaches a formulation containing Mosapride, high-viscosity and low-viscosity HPMCs as a controlled-release matrix (Abstract). The high-viscosity and low-viscosity HPMC were mixed at a ratio of from 10:1 to 1:1, and then added with a specific ratio of povidone as a binder, microcrystalline cellulose as an excipient, lactose, low substituted hydroxypropylcellulose (HPC) ([0030]). Additionally, the formulation can comprise a disintegrating agent such as croscarmellose sodium, sodium starch glycolate, microcrystalline cellulose, crospovidone; the disintegrating agent is used in the amount of from 10 wt% to 30 wt % ([0037]). Kim explicitly teaches a matrix containing one or more HPMCs, HPC, and disintegrating agents. In an embodiment, the formulation contains about 25-30 wt% of HPMC and 15-30 wt% of HPC ([0043]).
Therefore, it would have been obvious to one of ordinary person in the art before the effective filing date of the claimed invention to have combined teachings of above to arrive at a controlled-release solid oral composition with a core comprising HPMC, HPC, disintegrant polymers, with an outer coating layer comprising HPMC and/or ethyl cellulose or a gastro-resistant layer (enteric layer) for the advantage of contributing to the release profile of the compositions. This is taking some teaching, suggestion, or motivation in the prior art that would have led one of ordinary skill to modify the prior art reference or to combine prior art reference teachings to arrive at the claimed invention.
Regarding claim 2, Lee teaches that the pharmaceutical compositions may be formulated to achieve controlled release (e.g., monolithic matrix) of the drugs ([0082]).
Regarding claim 3, Kodgule teaches that the modified release tablet contains active ingredient (e.g., sitagliptin) in the core as well as immediate release part (See Example 5).
Regarding claim 4, the coating layer comprising ethyl cellulose is discussed above in claim 1.
Regarding claim 5, a layer comprising HPMC and/or ethyl cellulose coated with gastroresistant or enteric polymers is discussed above in claim 1.
Regarding claim 6, a gastoresistant layer is discussed above.
Regarding claim 7, Lee discloses that the enteric coating polymer may be selected from Eudragit (e.g., Eudragit L30D-55, dissolution above pH 5.5), methacrylic acid copolymers, shellac ([0118]).
Regarding claim 8, pH-dependent methacrylic acid copolymer is discussed above.
Regarding claim 11, disintegrants are discussed above in claim 1.
Regarding claim 13, HPMC and/or ethyl cellulose in certain content weight is discussed above.
Regarding claim 14, Lee discloses that the therapeutic agent can be a biologically active macromolecule such as a protein, peptide, polysaccharide, nucleic acid, lipid, carbohydrate, and a combination thereof (claims 21-22). Lee also teaches acetyl cysteine as the active ingredient ([0066]).
Response to Arguments
Applicant’s arguments filed 08/01/2025 have been fully considered and new rejection is applied.
On page 8 of remarks, Applicant argues that the presently claimed invention is not a simple juxtaposition of known components but a carefully constructed system in which the interaction of each of the elements – notably the specific viscosity grades of HPMC – plays a critical role. However, the use of these HPMC components is already well-known as taught by Kodgule. Additionally, Kim discloses a controlled-release solid formulation comprising HPMCs with different viscosities, HPC, and disintegrating agents. One of ordinary skill in the art would routinely experiment with various concentrations of these routinely used ingredients within a formulation for the purpose of controlling the release rate.
Therefore, claims 1-8, 11, and 13-14 remain rejected.
Conclusion
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/JOHN SEUNGJAI KWON/Examiner, Art Unit 1615
/Robert A Wax/Supervisory Patent Examiner, Art Unit 1615