DETAILED ACTION
Claims 1-19 are currently pending and under examination.
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 .
Examiner’s Note
Applicant's amendments and arguments filed 02/26/2026 are acknowledged and have been fully considered. The Examiner has re-weighed all the evidence of record. Rejections and/or objections not reiterated from previous office actions are hereby withdrawn. The following rejections and/or objections are either reiterated or newly applied. They constitute the complete set presently being applied to the instant application. In the Applicant’s response, filed 02/26/2026, it is noted that claim 1 has been amended and no new matter or claims have been added.
Modified Rejections:
The following rejections are modified based on Applicant’s claim amendments.
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.
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 1-13, 15 and 17-19 is/are rejected under 35 U.S.C. 103 as being unpatentable over US 2009/0162434 (Applicant provided) in view of US 2007/0218134 (Applicant provided), WO 2003/045356 (Applicant provided) and Dwibhashyam (Applicant provided) as evidenced by DrugBank (Applicant provided).
Regarding claims 1 and 10, the limitation of an enteric coated tablet comprising (A) a core tablet containing a medical ingredient and having a weight of 1,000 mg or more is met by the ‘434 publication teaching mesalazine tablets (abstract) wherein DrugBank evidenced mesalazine is a synonym for 5-aminosalicylic acid (page 1). The tablet core comprises mesalazine from 100 mg to about 900 mg [0026], the binder is present in the core from 60 to 100 mg [0028] and the intergranular superdisintegrant is 30 mg or more [0029], thus teaching an overlapping range with the instant claims weight of 1,000 mg or more of core weight. 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).
The limitation of (B) a coating layer containing a water-soluble polymer applied onto the surface of the core tablet wherein the water-soluble polymer coating layer (b) having no enteric property is met by the ‘434 publication teaching the first coating layer increases the adhesion of the second coating layer and includes hydroxypropyl methyl cellulose [0032], the elected water-soluble polymer, wherein no additional polymers are required.
The limitation of (C) an enteric coating layer dissolving at a pH of 7 or higher which is applied onto the surface of the coating layer containing a water-soluble polymer is met by the ‘434 publication teaching a second coating layer being methacrylic acid/methyl methacrylate copolymer [0037] such as EUDRAGIT S, which is a methacrylic acid/methyl methacrylate copolymer [0040]. The second layer is taught to be enteric [0021] wherein drug release is taught at pH 7 or higher [0020].
The limitation of wherein a sum of a polymer amount of the coating layer (B) and a polymer amount of the coating layer (C) is 10 to 18 mg/cm2 and 10-14 mg/cm2 is met by the ‘434 publication teaching the first coating layer can be about 1 to about 2 mg/cm2 [0036] and a second coating layer can be about 6 mg/cm2 to about 15 mg/cm2 [0045], leading to an overlapping amount with the claimed range wherein the combined coating weight is 7 mg/cm2 to 17 mg/cm2. 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).
The limitation of a polymer amount of coating layer (C) is 3 to 6 mg/cm2, or 3 to 4 mg/cm2 or 4-6 mg/cm2 is met by the ‘434 publication teaching about 5 mg/cm2 [0045] thus teaching an overlapping amount with the instant claims as the about allows for amounts above and below the specifically recited amount. The instant specification teaches an excess of 6 mg/cm2 results in a lag time of 60 minutes or longer [0043], therefore the ‘434 publication teaching about 5 mg/cm2 of enteric coating would necessarily result in the claimed lag time at a pH of 7.2 to releasing the medicinal ingredient of one hour or less.
Regarding the limitation of releases the medicinal ingredient in the lower gastrointestinal tract form the ileum to the colon is met by the ‘434 publication teaching the drug is released I the terminal ileum and the colon of the patient [0020].
Regarding claims 2, the limitation of wherein the core tablet (A) has a weight of 1,000 to 1,500 mg is met by the ‘434 publication teaching the tablet core comprises mesalazine from 100 mg to about 900 mg [0026], the binder is present in the core from 60 to 100 mg [0028] and the intergranular superdisintegrant is 30 mg or more [0029] and optionally includes one or more additional excipients [0030], thus teaching an overlapping range with the instant claims weight of 1,000 mg or more of core weight. 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).
Regarding claim 3, the limitation of wherein the water-soluble polymer is one or more members selected from the group consisting of water soluble cellulose ethers is met by the ‘434 publication teaching the first coating layer increases the adhesion of the second coating layer and includes hydroxypropyl methyl cellulose [0032], the elected water soluble polymer.
Regarding claim 4, the limitation of wherein the enteric coating layer dissolving at pH 7 or higher is a coating formed of one or more polymer selected from the group consisting of methacrylic acid copolymer is met by the ‘434 publication teaching a second coating layer being methacrylic acid/methyl methacrylate copolymer [0037] such as EUDRAGIT S, which is a methacrylic acid/methyl methacrylate copolymer [0040]. The instant specification evidences methacrylic acid-methyl methacrylate copolymer is an enteric polymer [0021], and the elected copolymer. The second layer is taught to be enteric [0021] wherein drug release is taught at pH 7 or higher [0020].
Regarding claim 5, the limitation of wherein a total weight of the enteric coating tablet is 1,200 to 1,600 mg is met by the ‘434 publication teaching the active agent present at about 900 mg [0026], the superdisintegrant at 30 mg or more [0029], the binder is taught to be 50 to 140 mg [0028], the first coating is taught to be 0.6 mg per tablet [0035], the second coating layer is taught to be about 50 mg [0038], which leads to a tablet weight of 1120.6. MPEP 2144.05(I) teaches “a prima facie case of obviousness exists where the claimed ranges and prior art ranges do not overlap but are close enough that one skilled in the art would have expected them to have the same properties. Titanium Metals Corp. of America v. Banner, 778 F.2d 775, 227 USPQ 773 (Fed. Cir. 1985).”
Regarding claim 1 and 6-8, the limitation of wherein the medicinal ingredient is a therapeutic agent for a colonic disease, an inflammatory bowel disease, specifically 5-aminosalicylic acid is met by the ‘434 publication teaching mesalazine tablets (abstract). DrugBank evidenced mesalazine is a synonym for 5-aminosalicylic acid (page 1). The elected drug is taught and thus would be capable of the intended use of treatment of colonic disease and inflammatory bowel disease.
The ‘434 publication does not specifically teach a polymer amount of the coating layer (B) is 6 to 12 mg/cm2 (claim 1).
The ‘434 publication does not specifically teach a ratio by polymer mass (B/C) of the coating layer (B) to coating layer (C) of 1.0 to 2.5 (claim 9) and 1.5 to 2.5 (claim 11-19 and 17).
The ‘134 publication teaches pharmaceutical compositions for sustained release comprising as active ingredient a drug, said composition comprising a core consisting of an inner phase and outer phase. The core is taught as first coated with a non-functional film coat and then with an enteric coat (abstract). The enteric film coat is taught to include copolymerized methacrylic acid/methacrylic acid methyl esters (e.g., Eudragit) [0081]. The non-functional film coat is taught to include hydroxypropylmethyl cellulose [0084]. The non-functional coat is taught to be about 4 mg of film coat per cm2 and the enteric coating is taught to be 4 to 6 mg polymer per cm2 ([0103]-[0104]), thus teaching the claimed ratio of (B) to (C) required by the instant claim 10, such as a 1:1 ratio. The core is first coated with the non-functional coating and then an enteric coating [0107].
The ‘356 publication teaches pharmaceutical composition in a solid unit dosage form for oral administration comprising a therapeutically active agent, an inner coating comprising polymethylacrylic acid, methyl methacrylic and an outer coating layer of an enteric polymer film coating material (abstract). The drug is taught to be selected from a group including 5-amino salicylic acid (page 3, last paragraph). The outer coating layer is selected from a group including hydroxypropyl methyl cellulose (page 6, second paragraph). The total coating thickness is taught to be from about 5 mg/cm2 to about 40 mg/cm2 (page 7, 4th paragraph). The inner layer is taught to be 9.2 mg/cm2 and the outer layer is taught to be 4.1 mg/cm2 (page 11, 5-6th paragraph).
Dwibhashyam teaches that thicker coatings offer better resistance to frictional forces (abstract). Thus, it was well known to a person of ordinary skill at the time the invention was made that the use of a thicker coating, such as the coating amounts taught by the ‘356 publication, would result in more impact resistance.
It would have been prima facie obvious to one of ordinary skill in the art before the filing date of the claimed invention to increase the thickness of the first coating layer taught by the ‘434 publication because the ‘134 publication teaches pharmaceutical formulations containing a first coating layer of hydroxypropyl methyl cellulose wherein the coating thickness is about 4mg/cm2 and teaches an enteric coating layer of about 4 to 6 mg/cm2 to obtain release in the intestinal track ([0081], [0084], [0103]-[0104], [0077]), and the ‘434 publication is directed to compositions which release active agent in the intestinal tract of a patient [0020] containing hydroxypropyl methyl cellulose as the first coating layer and an enteric methacrylate coating layer as the second coating. Thus it would have been obvious to one of ordinary skill in the art before the filing date of the instant invention that amounts of coating layers of the first and second film as taught by the ‘134 publication could be used by the ‘434 publication to obtain a functional coating to release the drug in intestinal track of a patient. Further it would have been prima facie obvious to one of ordinary skill in the art before the filing date of the claimed invention that coating thickness of the hydroxypropyl methyl cellulose first coating layer could be optimized as the ‘434 publication teaches the first coating layer hydroxypropyl methyl cellulose is used to increase adhesion of the second coating layer and remove any incompatibility between the tablet core and second coating layer [0032] and teaches the first coating layer can be any suitable loading [0036], which would result in an optimizable parameter and the ‘134 publication teaches about 4 mg of film coat per cm2, thus teaching amounts above and below the specifically recited 4 mg/cm2 can be utilized. Additionally, Dwibhashyam teaches that thicker coatings offer better resistance to frictional forces (abstract). Thus, it was well known to a person of ordinary skill at the time the invention was made that the use of a thicker coating, such as the coating amounts taught by the ‘356 publication, would result in more impact resistance and optimize to obtain the desired effect. As MPEP 2144.05 recites “where the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine optimization”.
One of ordinary skill in the art before the filing date of the claimed invention would have a reasonable expectation of success as the ‘356 publication teaches a dual layer coating of a 5-amino salicylic acid solid dosage form (page 4, 3rd paragraph) with an inner and outer coating layer (page 4, 5th paragraph) wherein a broad range of combined coating thickness is taught (5mg/cm2 to about 40 mg/cm2) (page 7, 5th paragraph) and inner coating layers are specific taught to be 9.2 mg/cm2 and outer coating layers are taught to be 4.1 mg/cm2 (example 1), thus teaching the concentration of the first and second coating layer are known to be utilized on a 5-amino salicylic acid solid dosage form and one of ordinary skill in the art would have a reasonable expectation of success of using such coating concentrations for the inner and outer coating layer taught by the ‘434 publication using the hydroxypropylmethyl cellulose inner layer and methacrylic acid copolymer outer layer.
Regarding claim 1 and 15, the limitation of which has improved impact resistance compared to an enteric coated tablet comprising less than 6mg/cm2 of the polymer in the coating layer (B) as measured by a drop test from a height of 30 cm is met by the ‘356 publication teaching the outer coating layer is selected from a group including hydroxypropyl methyl cellulose (page 6, second paragraph). The total coating thickness is taught to be from about 5 mg/cm2 to about 40 mg/cm2 (page 7, 4th paragraph). The inner layer is taught to be 9.2 mg/cm2 and the outer layer is taught to be 4.1 mg/cm2 (page 11, 5-6th paragraph). Dwibhashyam teaches that thicker coatings offer better resistance to frictional forces (abstract). Thus, it was well known to a person of ordinary skill at the time the invention was made that the use of a thicker coating, such as the coating amounts taught by the ‘356 publication, would result in more impact resistance.
Claim(s) 14 and 16 is/are rejected under 35 U.S.C. 103 as being unpatentable over US 2009/0162434 in view of US 2007/0218134, WO 2003/045356 and Dwibhashyam as evidenced by DrugBank as applied to claims 1-13, 15 and 17-19 above, and further in view of US 2004/0142035 (Applicant provided).
As mentioned in the above 103(a) rejection, all the limitations of claims 1-13, 15 and 17-19 are taught by the combination of the ‘434 publication, the ‘134 publication, the ‘356 publication and Dwibhashyam.
The combination of references does specifically teach wherein the enteric coated tablet has a hardness in the longitudinal direction of 250 to 500 N (claim 14).
The combination of references does not teach wherein medicinal ingredient begins release from the tablet in 60 minutes or less (claims 16).
The ‘035 publication teaches oral dosage forms comprising two or more enteric coating materials. The composition is characterized by having a sustained release profile at lower pH and an accelerated dissolution profile at higher pH (abstract). The pharmaceutical composition displays sustained release profile at lower pH and an accelerated dissolution profile at high pH [0009]. The dissolution profile of the beads coated with Eudragit delayed the drug release in the acidic medium and provided sustained release profiles (about 20% drug release per hour) after exposure to pH 6 medium. Under high pH testing conditions (e.g. pH 6.5, 7 or 7.5) it resulted in the acceleration of the drug release, for example using pH 6.5 dissolution medium the drug release was sped up significantly compared to the dissolution profile at pH 6.0 [0058]. The blend is compressed into tablets with a tablet hardness of 15 to 20 kp [0074] which is 147 N to 196 N.
It would have been prima facie obvious to one of ordinary skill in the art before the filing date of the claimed invention that the drug release rate is tied to the pH of when enteric polymers are used as coating materials and hardness, wherein the ‘434 publication teaches using an enteric coating layer, methacrylic acid/methyl methacrylate copolymer [0037] such as EUDRAGIT S [0040]. It would have been prima facie obvious to one of ordinary skill in the art that the drug may be released within 60 minutes or less when exposed to a high pH and hardness of 250-500N as the ‘035 publication teaches the pH to which the composition is exposure effects the release time and wherein enteric polymers release the active agent within 60 minutes when exposure to high pH and compression force results in the tablet hardness range. Thus, one of ordinary skill in the art before the filing date of the claimed invention would expect release rate within the hour when exposure to high pH environment in the compositions comprising an EUDRAGIT enteric polymer as taught by the ‘434 publication and have an optimizable hardness based on the compression force of the tablet blend based on the teachings of the ‘035 publication. As MPEP 2144.05 recites “where the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine optimization”.
37 CFR 1.132 Declaration
The examiner acknowledges receipt of the Declaration under 37 CFR 1.132 by Akia Ryu filed on 02/26/2026.
The Declaration under 37 CFR 1.132 filed 02/26/2026 is insufficient to overcome the rejection of claims 1-13, 15 and 17-19 based upon obviousness over US 2009/0162434 in view of US 2007/0218134, WO 2003/045356 and Dwibhashyam as evidenced by DrugBank as set forth in the last Office action because:
Declarant argues the ‘434 publication teaches a first coating layer having an amount of 1 to 2 mg/cm2; a second coating layer having an amount of 6 to 16 mg/cm2 and a sum of coating amounts of the first coating layer and the second coating layer is 7 to 17 mg/cm2. As shown in the data of Example of the application I see that when a polymer amount of coating layer (B) was decreased impact resistance was reduced although enteric property was obtained. These improvements were unexpected. In Declarants view the ‘434 suggests that if impact resistance was sought to improve the tablet the increase would be a sum of coating amounts, not the first coating layer only.
In response, the ‘434 publication teaches first coating layer comprises a cellulose derivative (abstract) wherein the first coating layer can be of any suitable loading, e.g. a loading of about 0.8 mg/cm2 or more, specifically loading of about 1mg/cm2 to about 2 mg/cm2 [0036]. The ‘356 publication teaches the outer layer is selected from a group including hydroxypropyl methyl cellulose (page 6, second paragraph). The ‘356 publication additionally teaches the inner coating layer is 9.2 mg/cm2 and the outer coating layer is 4.1 mg/cm2 (page 11, Example 1). Thus the ‘434 publication teaches the hydroxypropyl cellulose layer to be the inner layer and can be from 0.8 mg/cm2 and above, thus teaching an overlapping range and the ’356 publication further teaching coating layer which may be HPMC which are present at 4.1 and 11.9 mg/cm2, thus teaching that coating layers of HPMC in oral dosage forms releasing the same active ingredients (5-aminosalicylic acid) are known to have thickness of HPMC which overlaps with the instant claim range and used as a coating layer over the tablet. Thus increasing the thickness of the second coating is prima facie obvious as the ‘434 publication does not limit to a specific number disclosed in the preferable range but rather teaches any suitable loading may be used.
Declarant argues the ‘134 related to a pharmaceutical composition for sustained release, wherein said composition comprising a core which is first coated with a non-functional film coat and then an enteric coat. The composition has a dosage weight from about 5 to about 300 mg, which is small composition relative to the composition of the present claims and thus there is no nexus to use the teaching of large tablets of the ‘434 and the teachings of the ‘134 publication.
In response, the ‘434 publication and the ‘134 publication are both directed to oral pharmaceutical formulations comprising a coating layer of hydroxypropyl methyl cellulose and an enteric coating, and thus there is a nexus between the teachings.
Declarant points to Table 4 and Fig 1 shows the impact resistance of enteric coated tablets when the amount of water-soluble polymer coating layer and the enteric coating layers were varied. It is evidence that when the amount of enteric polymer was 4mg/cm2, when the amount of water-soluble polymer was 6 mg/cm2 or more good impact resistance was the result. Where the amount of entering polymer was 3 mg/cm2 and the amount of the water-soluble polymer was 8 mg/cm2 or more good impact resistance was the result. It is evidence that a tablet with lower amount of water-soluble polymer, like that described in the ‘434 publication, the resulting tablet would have poor impact resistance.
In response, Dwibhashyam teaches thicker coatings offer better resistance to frictional forces (abstract). Thus, it was well known to a person of ordinary skill at the time the invention was made that use of thicker coating, such as the coating amounts taught by the ‘356 publication, would result in more impact resistance as is tested and demonstrated in the instant specification. Thus, the results are not unexpected, as thicker coatings are known to have resistance to frictional forces.
Declarant argues Table 5 shows the acid resistance of enteric coated tablets when the amount of the two coating polymers were varied. When the water soluble and the enteric polymers were presented in an amount of 5 mg/cm2 good acid resistance required for enteric drug products was the result. While the resultant composition has good acid resistance it is shown in table 4 that when the amount of the two coating polymer was in sum less than 10 mg/cm2 the impact resistance suffered. This serves to highlight the point that is not one or even two variables that are important but the combination of three that effect impact resistance, acid resistance, enteric performance and spraying time. Declarant argues Figure 2 shows the lag time at a pH of 7.2 when the amount of the enteric polymer was varied. The lag time of the coated tablet was prolonged considerably depending on the amount of the enteric polymer but when the amount exceeded 6mg/cm2 the lag time was more than 60 minutes delay that was too long for delivery of the drug and sets the limit on the amount enteric polymer at 3 to 6 mg/cm2. Declarant argues the spraying time required for forming the layer is too long if the upper limit is not less than the water-soluble polymer at 12 mg/cm2. If the composition does not meet the three requirements for the enteric and water-soluble coating layers the careful balance of impact resistance, acid resistance, enteric performance and spraying time could not have been achieved. None of the cited references by the USTPO would have suggested to that such a combination of results would be expected results. The data shows the criticality of the amounts of the coating layers and the ratios thereof.
In response, Dwibhashyam teaches thicker coatings offer better resistance to frictional forces (abstract). Thus it was well known to a person of ordinary skill at the time the invention was made that the use of a thicker coating, such as the coating amounts taught by the ‘356 publication, would result in more impact resistance as is tested and demonstrated in the instant specification. Thus the results are not unexpected, as thicker coatings are known to have resistance to frictional forces. Further with regards to Tables 4 and 5, Appellant provides test data to indicate that within the ranges there is good impact resistance, but nothing outside the claimed ranges indicating poor impact resistance. Figure 1 likewise shows that increasing coating thickness affects impact resistance, which was known previously as demonstrated by Dwibhashyam. Further the applied art demonstrates the total coating thickness is taught (see the ‘434 publication).
The ‘434 publication teaches methacrylic copolymer coating in the claimed range and thus would have the same lag release rate.
Appellant has not demonstrated how this is an unexpected result. It would be clear to one of ordinary skill that additional coating material being applied would take additional time. Appellant has not established that the additional coating time is unobvious, and additionally the total coating thickness is taught by the primary reference, the ‘434 publication.
It is well known in the art at the time of the invention to vary coating thickness to obtain desired results, such as is demonstrated the ‘434 publication teaching a range for each coating layer and teaching the first coating layer to increase adhesion and remove incompatibility and teaching varying the amount of enteric coating to cause different dissolution profiles [0056].
The ‘434 publication teaches first coating layer comprises a cellulose derivative (abstract) wherein the first coating layer can be of any suitable loading, e.g., a loading of about 0.8 mg/cm or more, specifically a loading of about 1 mg/cm2 to about 2 mg/cm2 [0036]. The '356 publication teaches the outer layer is selected from a group including hydroxypropyl methylcellulose (page 6, second paragraph). The ‘356 publication additionally teaches the inner coating layer is 9.2 mg/cm2 and the outer coating layer is 4.1 mg/cm2 (page 11, Example 1) and embodiments wherein the outer coating layer is 11.9 mg/cm2 (Example 2). Thus the ‘434 publication teaches the hydroxypropyl cellulose layer to be the inner layer and can be from 0.8 mg/cm2 and above, thus teaching an overlapping range, and the ‘356 publication further teaches coating layers which may be HPMC which are present at 4.1 and 11.9 mg/cm2, thus teaching that coating layers of HPMC in oral dosage forms releasing the same active ingredient (5-aminosalicylic acid) are known to have thickness of HPMC which overlap with the instant claimed range (‘356 publication) and are used as the coating layer over the tablet (‘434 publication). Thus, the methacrylic acid thickness and total coating thickness is taught by the ‘434 publication. Appellant has not provided evidence demonstrating the thickness of the coating layer provides the unexpected results presented. Further those results that are presented are not commensurate in scope with the instant claims, as the claims are broadly directed to a coating layer and an enteric coating layer, wherein only a single specific polymer was tested for each layer.
In addition to the facts provided above, the examiner notes that the Affiant is the same as the Inventor of the instant application. Therefore, the Affiant has an interest in the outcome of the instant application.
In assessing the weight to be given expert testimony, the examiner may properly consider, among other things, the nature of the fact sought to be established, the strength of any opposing evidence, the interest of the expert in the outcome of the case, and the presence or absence of factual support for the expert’s opinion. See Ex parte Simpson, 61 USPQ2d 1009 (BPAI 2001), Cf. Redac Int’l. Ltd. v. Lotus Development Corp., 81 F.3d 1576, 38 USPQ2d 1665 (Fed. Cir. 1996), Paragon Podiatry Lab., Inc. v. KLM Lab., Inc., 948 F.2d 1182, 25 USPQ2d 1561, (Fed. Cir. 1993).
Affidavits or declarations are provided as evidence and must set forth facts, not merely conclusions. In re Pike and Morris, 84 USPQ 235 (CCPA 1949).
Upon consideration of the facts taught by the prior art and the information submitted by the Affiant, the balance of evidence indicates that the prior art teaches the instantly claimed inventions.
Response to Arguments:
Applicant’s arguments have been fully considered and are not deemed to be persuasive.
Applicant argues they are the first to solve the problem of producing enteric coated tablets having a weight of 1,000 mg or more having a core coated with a water-soluble polymer and an outer layer of an enteric coating where the coating does not crack during the coating process from impact with the walls of the coating container with the loss of resistance needed to surface the stomach acidic environment. The prior art cited by the Examiner does not address the problem of formulating a unit dose of a drug coated with an enteric coating and water-soluble coating having a size of 1000 mg or more where ethe coating survives the coating process without cracking and a coating thickness compatible with the desired drug release characteristics. They do not recognize the interrelationship between the coating thickness, release properties and durability of the coating during the coating process.
In response to applicant's argument that the interrelationship between the coating thickness, release properties and durability of the coating during the coating process, the fact that the inventor has recognized another advantage which would flow naturally from following the suggestion of the prior art cannot be the basis for patentability when the differences would otherwise be obvious. See Ex parte Obiaya, 227 USPQ 58, 60 (Bd. Pat. App. & Inter. 1985). , Dwibhashyam teaches thicker coatings offer better resistance to frictional forces (abstract). Thus it was well known to a person of ordinary skill at the time the invention was made that the use of a thicker coating, such as the coating amounts taught by the ‘356 publication, would result in more impact resistance as is tested and demonstrated in the instant specification. Thus the results are not unexpected, as thicker coatings are known to have resistance to frictional forces. The ‘434 publication teaching mesalazine tablets comprising a first coating layer comprising cellulose derivative and a second coating layer comprising methacrylic acid/methyl methacylate copolymer with the release of the active agent starting at pH 6.8 (abstract). The tablet core comprises 100 mg binder [0028], 30 mg superdisintegrant [0029] and the drug present at 300 mg to 900 mg [0026], thus teaching an overlapping range with the instant claims weight of 1,000 mg or more of core weight. The first coating layer is taught to be at 0.8 mg/cm2 to about 2 mg/cm2 [0036] and the second coating layer is taught to be about 5 to 15 mg/cm2 [0045], thus teaching overlapping amounts of the enteric polymer (second coating) and sum of polymer and enteric coating layer amount. Thus the ‘434 publication teaches the claimed core tablet, water soluble polymer layer, enteric laying layer and overlapping amounts of the enteric polymer layer and total coating amount. The ‘434 publication teaches any amount of the water-soluble polymer coating may be used, wherein Dwibhashyam and the ‘356 publication provide the amount of water-soluble polymer and motivation to use the higher amounts. As MPEP 2144.05 recites “where the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine optimization”. It is further noted that ‘434 publication teaches varying the amount of coating on the core different dissolution profiles of the tablets are obtained [0056], thus varying the amounts of coating ingredients to obtain the desired release rate was well known in the art at the time the invention as made, as well as the thickness to obtain the desired resistance to frictional forces. Applicant has presented data on optimizing well known parameters in coating formulations to obtain the desired resistance to frictional forces and release rate, which is not considered unexpected.
Applicant argues the Ryu declaration.
The Ryu declaration is addressed above in the declaration section.
Applicant argues the rejection does not explain where in the ‘434 publication the thickness of (B) is taught. Only a fraction of the thickness is suggested. Applicant argues the examiner ignored both the claim limitation and the results of Table 4 when making the rejection.
In response to applicant's arguments against the references individually, one cannot show nonobviousness by attacking references individually where the rejections are based on combinations of references. See In re Keller, 642 F.2d 413, 208 USPQ 871 (CCPA 1981); In re Merck & Co., 800 F.2d 1091, 231 USPQ 375 (Fed. Cir. 1986). The ‘356 publication teaches the total coating thickness is taught to be from about 5 mg/cm2 to about 40 mg/cm2 (page 7, 4th paragraph). The inner layer is taught to be 9.2 mg/cm2 and the outer layer is taught to be 4.1 mg/cm2 (page 11, 5-6th paragraph). Applicant is referred to the declaration section above wherein Table 4 is discussed.
Applicant argues the ‘356 publication and Dwibhashyam do not remedy the deficiencies noted previously in the rejection. Ryu testified was not simply making the coatings thicker but rather in making the outer coating thinner and the inner one thicker a concept that is not taught by the combined references. The ’356 publication limits he composition of his layer to both enteric coatings on page 4 and 5, thus omitting the water-soluble coating required by the claimed for the claimed (B) layer. The examiner provides not reason for omitting the enteric coating for (B) in ‘356 and substituting a water-soluble layer.
In response, one of ordinary skill in the art before the filing date of the claimed invention would have a reasonable expectation of success as the ‘356 publication teaches a dual layer coating of a 5-amino salicylic acid solid dosage form (page 4, 3rd paragraph) with an inner and outer coating layer (page 4, 5th paragraph) wherein a broad range of combined coating thickness is taught (5mg/cm2 to about 40 mg/cm2) (page 7, 5th paragraph) and inner coating layers are specific taught to be 9.2 mg/cm2 and outer coating layers are taught to be 4.1 mg/cm2 (example 1), thus teaching the concentration of the first and second coating layer are known to be utilized on a 5-amino salicylic acid solid dosage form and one of ordinary skill in the art would have a reasonable expectation of success of using such coating concentrations for the inner and outer coating layer taught by the ‘434 publication using the hydroxypropylmethyl cellulose inner layer and methacrylic acid copolymer outer layer.
Applicant argues the thickness of the ‘434 publication of 1-2 mg/cm2 for layer B does not overlap with that of the claimed 6-12 mg/cm2 range of the claims which ahs been shown to result effective regarding the coating integrity and the resulting acid resistance of the claimed tablets.
In response, It would have been prima facie obvious to one of ordinary skill in the art before the filing date of the claimed invention to increase the thickness of the first coating layer taught by the ‘434 publication because the ‘134 publication teaches pharmaceutical formulations containing a first coating layer of hydroxypropyl methyl cellulose wherein the coating thickness is about 4mg/cm2 and teaches an enteric coating layer of about 4 to 6 mg/cm2 to obtain release in the intestinal track ([0081], [0084], [0103]-[0104], [0077]), and the ‘434 publication is directed to compositions which release active agent in the intestinal tract of a patient [0020] containing hydroxypropyl methyl cellulose as the first coating layer and an enteric methacrylate coating layer as the second coating. Thus it would have been obvious to one of ordinary skill in the art before the filing date of the instant invention that amounts of coating layers of the first and second film as taught by the ‘134 publication could be used by the ‘434 publication to obtain a functional coating to release the drug in intestinal track of a patient. Further it would have been prima facie obvious to one of ordinary skill in the art before the filing date of the claimed invention that coating thickness of the hydroxypropyl methyl cellulose first coating layer could be optimized as the ‘434 publication teaches the first coating layer hydroxypropyl methyl cellulose is used to increase adhesion of the second coating layer and remove any incompatibility between the tablet core and second coating layer [0032] and teaches the first coating layer can be any suitable loading [0036], which would result in an optimizable parameter and the ‘134 publication teaches about 4 mg of film coat per cm2, thus teaching amounts above and below the specifically recited 4 mg/cm2 can be utilized. Additionally, Dwibhashyam teaches that thicker coatings offer better resistance to frictional forces (abstract). Thus, it was well known to a person of ordinary skill at the time the invention was made that the use of a thicker coating, such as the coating amounts taught by the ‘356 publication, would result in more impact resistance and optimize to obtain the desired effect. As MPEP 2144.05 recites “where the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine optimization”.
Applicant argues the ‘035 publication does not cure the deficiencies of the other prior art.
In response, Applicant’s arguments regarding the ‘434 publication, the ‘134 publication, the ‘356 publication and Dwibhashyam are addressed above as first presented.
Conclusion
No claims are 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.
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/LYNDSEY M BECKHARDT/Examiner, Art Unit 1613
/BRIAN-YONG S KWON/Supervisory Patent Examiner, Art Unit 1613