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 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.
Claims 1-21 are rejected under 35 U.S.C. 103 as being unpatentable over Kim et al. WO 2013/154390 A1, in view of Cho et al. WO 2020/213868 A.
Kim teaches a multi-unit spheroidal tablets (MUSTs) encapsulated in a hard capsule and a method for preparing same. The inventive hard capsule composite formulation can effectively charge the MUSTs in the limited space of the capsule, which allows charging a high dose of different pharmaceutically active ingredients in a capsule with a relatively small size, to thereby increase the productivity and render it readily administered to patients. Also, the capsule has a good dissolution rate because the pharmaceutically active ingredients contained in the capsule are separated from one another; therefore, the dissolution rates of the ingredients are less affected by one another. It may also be possible to maximize the therapeutic effects of the pharmaceutically active ingredients since the composite formulation has good stability. See Abstract. MUST having diameter between 1-4 mm and the claimed volume to ratio is found in pages 6-8, and Examples and page 20. Active agents include losartan is found in page 9. Tablet excipients are found in pages 10-11. MUST further comprising film coating is found in pages 12-14. Process for preparing the tablets can be found in the Examples.
While Kim teaches active agents can include losartan, it is noted that the list of active agents is quite long. However, minitablet comprising losartan is known in the art. See for example the teaching in Cho, which teaches an oral composition comprising losartan or a pharmaceutically acceptable salt thereof in a dosing ranging between 40 to 100 mg of the salt in terms of the free acid form of losartan. See Abstract and Claims. The method for preparing ezetimibe granules is not particularly limited, but it may be preferable to prepare the granules in a wet state. Ezetimibe is a poorly soluble drug that exhibits low saturation solubility of around 1 ppm in both acidic to weakly basic body fluid conditions. The saturation solubility and dissolution rate from the start of dissolution to saturation can be important indicators for evaluating the bioavailability of poorly soluble drugs. The wet granules can reach saturated solubility at a faster rate than that of the poorly soluble drug, Eje. High bioavailability can be secured for Timibe. The method for preparing losartan granules is not particularly limited, but it may be preferable to prepare the granules by a compression granulation method. When sieving with a sieve (No. 60) having a sieve size of 250 μm, the content of ezetimibe granules (residues) having a diameter exceeding 250 μm is 15% by weight or less, preferably 10% by weight or less. I can. Losartan granules, when sieved through a sieve having a sieve size of 250 μm, the content of granules (residues) having a diameter exceeding 250 μm, are 35 to 55% by weight, preferably 40 to 50% by weight, and have a sieve size of 500 μm. When sieved with a sieve (No. 35), the content of granules (residues) having a diameter exceeding 500 μm may be 10 to 30% by weight, preferably 15 to 25% by weight. When the ezetimibe granules and losartan granules are adjusted within the above range, the elution amount of ezetimibe and losartan can be adjusted at an appropriate level. See translation Abstract. Selection of the type and content of these additives can be appropriately selected by a person skilled in the art according to the type of specific formulation to be prepared. For example, the excipient is selected from the group consisting of lactose, starch, mannitol, microcrystalline cellulose, carboxymethylcellulose, and combinations thereof, and the binder is povidone, hypromellose, hydroxypropylcellulose, copovidone, and their It is selected from the group consisting of combinations, the disintegrant is selected from the group consisting of crospovidone, croscarmellose sodium, sodium starch glycolate, low-substituted hydroxypropyl cellulose, and combinations thereof, and the lubricant is stearic acid It may be selected from the group consisting of magnesium, talc, light anhydrous silicic acid, sodium stearyl fumarate, and combinations thereof, but is not limited thereto. See English Abstract. Oral dosage includes minitablet comprising coating layer can be found in the Examples. Film coated losartan minitablet having diameter between 1-4 mm is found in Example 3.
Thus, it would have been prima facie obvious to one of ordinary skill in the art to optimize the teaching in Kim in view of the Cho with the expectation to obtain an invention useful for the delivery of losartan to a wide population of patients. This is because Cho teaches it is well known in the art to include losartan in minitablet to increase solubility of the drug, and this is because Kim teaches minitablet composition useful for a wide variety of active agents including losartan.
Correspondence
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/SUSAN T TRAN/Primary Examiner, Art Unit 1615