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 § 112
The following is a quotation of 35 U.S.C. 112(b):
(b) CONCLUSION.—The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or a joint inventor regards as the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), second paragraph:
The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the applicant regards as his invention.
Claim 18 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 applications subject to pre-AIA 35 U.S.C. 112, the applicant), regards as the invention.
The phrase “perfectly” in line 2 of claim 18 renders the claim indefinite because it is not entirely unclear how spherical is considered perfectly spherical in shape. This is further in view of the present specification. There is no disclosure in the specification to define or determine the perfect shape.
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.
Claims 1-14, 17 and 18 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Yoon et al. WO 2020/080806 A1.
Yoon teaches a method for preparing injectable microparticles comprising naltrexone. The microparticles are prepared by solvent extraction/evaporation of an oil-in-water emulsion, the dispersed oil phase being solutions formed by using an organic solvent, including mainly of naltrexone and biodegradable, biocompatible polymer. See Abstrac, Claims and page 4. The methods according to embodiments of the present invention are described in detail with reference to FIG.1. In the present disclosure, the use of the term "first" or "second" is only intended to explain the present disclosure more conveniently, but these terms do not represent or imply that there is a particular order or degree of importance between them. In addition, a singular form of expression throughout the present disclosure includes a plural meaning as well unless it is contextually clear there is a difference. The mixing of the first phase and the second phase is performed in any order. In one aspect, but not limited to, the first phase may be added to the top of the second phase and then mixed to prepare the mixture. This process may be emulsification, and the mixture is an oil-in-water emulsion of polymer, naltrexone, and one or more solvents. Oil particles in the mixture (emulsion) become microparticles through a follow-up process of the present disclosure. The mixing may be a process to form microparticles of desired size range, which may depend on the mixing conditions such as rotation speed, power and the like. The first phase may be also called a continuous phase in the present disclosure. The first phase comprises poly(vinyl alcohol) and the first solvent, wherein the first solvent comprises at least one selected from the group consisting of water, dichloromethane (DCM), benzyl alcohol (BA), and ethyl acetate (EA). In one aspect, the first solvent must comprise water. For example, the first solvent may be water and the first phase may be formed by addition PVA into water. In another aspect, the first solvent may further comprise an organic solvent, which is at least one selected from the group consisting of dichloromethane, benzyl alcohol, and ethyl acetate. When the first solvent comprises water and one or more organic solvents, the organic solvent could be mixed together with poly(vinyl alcohol) and water when preparing the first phase. In other aspects, when the first solvent comprises water and one or more organic solvents, the organic solvent could be mixed with a solution including poly(vinyl alcohol) and water immediately after mixing poly(vinyl alcohol) and water when preparing the first phase. In another aspect, when the first solvent comprises water and one or more organic solvents, the organic solvent could be mixed with the solution comprising poly(vinyl alcohol) and water immediately before mixing the first phase with the second phase. Preferably, one or more organic solvents may be mixed with a solution comprising poly(vinyl alcohol) and water immediately before mixing with the second phase. In one aspect, the continuous phase (first phase) comprises about 0.1~5% (w/v) poly(vinyl alcohol) (PVA) in water. In another aspect, the continuous phase may further comprise 0 to 1.8% (w/v) dichloromethane (DCM) and/or 0 to 3.3% (w/v) benzyl alcohol. See pages 5-6. Dissolving naltrexone and a biodegradable polymer in dichloromethane and a cosolvent is found in page 6. The second phase may be also called an organic phase in the present disclosure. The second phase comprises biodegradable polymer, naltrexone and the second solvent, wherein the second solvent comprises at least one selected from the group consisting of dichloromethane, benzyl alcohol, and ethyl acetate. In one aspect, the second solvent comprises dichloromethane and benzyl alcohol, ethyl acetate or a combination thereof. In another aspect, for the preparation of the microparticles, the second phase comprises about 1~40% (w/w) biodegradable polymer dissolved in an organic solvent, such as dichloromethane (DCM), also known as methylene chloride, and 1~50% (w/w) naltrexone dissolved in another organic solvent, such as benzyl alcohol. The naltrexone could be used in the method in the form of free base, salt, solvate, cocrystal or combinations thereof. Biodegradable polymer may be a homopolymer, copolymer, or terpolymer or repeating monomeric units linked by groups such as ester groups. The polymer may be a polyester that may be composed of units of about one or more hydroxycarboxylic acid residues, where the distribution of units may be random, blocked, paired, or distributed sequentially. When the biodegradable polymer is a polyester, the polyesters include polylactide, polyglycolide, and PLGA. In one aspect, the biodegradable polymer is a polylactide, PLGA, or combinations thereof. Preferably, the suitable biodegradable polyester has the lactide:glycolide (L:G) (molar) ratio of 50:50 to 100:0, preferably 65:35 to 90:10, more preferably 75:25 to 85:15. Preferably, the suitable biodegradable polyester is a 60:40 to 95:5 PLGA. More preferably, the suitable biodegradable polyester is a 70:30 to 90:10 PLGA. Even more preferably, the biodegradable polyester is a 75: 25 to 85:15 PLGA. The most preferably, the biodegradable polyester is an 85:15 PLGA. In one aspect, the biodegradable polymer has an average molecular weight of 50,000 to 150,000 Daltons. See pages 6-7. Aqueous phase comprising water and surfactant such as polyvinyl alcohol is found in page 7.
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 15 and 16 are rejected under 35 U.S.C. 103 as being unpatentable over Yoon et al. WO 2020/080806 A1, in view of Kim KR 20190004189 A and Kim KR 20180018985 A.
Yoon is relied upon for the reasons stated above. Yoon does not teach the claimed stirring steps as recited in claims 15 and 16.
Kim teaches a solvent removal method including steps: stirred at 500 rpm at room temperature, followed by stirring at 300 rpm at 35°C for 16 hours, then the solvent is removed by filtration under reduced pressure, and the microcapsules are washed. The washed microcapsules are dried in an oven at 40°C to completely remove water. See Examples.
Kim teaches a solvent removal method including steps such as solution and network silica to the reaction tank and stirring at 5 to 200 rpm for 12 to 36 hours at room temperature to prepare a rubber-silica suspension, the solvent is removed with stirring at ~ 200 rpm. At this time. The absolute pressure is preferably adjusted to 0.005 to 0.2 bar. When this operation is operated for about 3 to 8 hours, WMB is obtained. When the solvent is removed, the surface becomes soft like popcorn. When it is pressurized at a high temperature, it becomes a plate which is easy to carry and handle. See Examples.
Thus, it would have been prima facie obvious to one of ordinary skill in the art to, by routine experimentation select the stirring parameters that fall within the claimed range in view of the teaching of the Kim references. This is because the Kim references teach a solvent removing can include steps that fall within the claimed range is known in the art. This is because Yoon teaches the desirability to remove solvent and washing the microparticle to remove all residual organic solvent with the expectation to obtain a microparticle useful for the delivery of a wide variety of water-insoluble active agents.
Correspondence
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/SUSAN T TRAN/Primary Examiner, Art Unit 1615