IN THE UNITED STATES RATENT AN TRADEMRRK OFFICE
`
`Docket No. 200 4_1o1 6A
`
`Group Art Unit 1611
`
`Examineri Rae, Charlesworth E
`
`In re application of
`
`Masayo HIGASHIYAMA
`
`
`
`
`,/r C
`' as. :s»
`‘~~”
`.
`
`Filed on June 30, 2004
`
`For: AQUEOUS LIQUID PREPARATIONS AND LIGHT-STABILIZED AQUEOUS
`LIQUID PREPARATIONS
`
`DECLARATION UNDER 37 CFR §1.132
`
`Honorable Commissioner of
`Patents,
`P.O. Box 1450
`
`Alexandria, Virginia 22313-1450
`
`Sirs:
`
`I, Masayo HIGASHIYAMA, citizen of Japan and residing in
`
`Suita—shi, Osaka, Japan, sincerely declare;
`
`That my education and employment history is as follows:
`
`1.
`
`I graduated from Nagoya City University, Japan,
`
`Graduate School of Pharmaceutical Sciences,
`
`in March 1995,
`
`2.
`
`I received a Doctor's degree in Engineering from
`
`Kyushu Institute of Technology, Japan,
`
`in September 2007,
`
`and
`
`A
`
`3. since April 1995 up to this time, I have been an
`
`employee of Senju Pharmaceutical Co., Ltd., and engaged
`
`in the pharmaceutical research of ophthalmic formulation;
`
`That I am a member of the Pharmaceutical Society of Japan
`
`since.November 1993, and the Controlled Release Society
`
`since January 2002;
`
`That I am a co—author of the following papers:
`
`1. Yasueda S, Higashiyama M, Yamaguchi M,
`
`Isowaki A,
`
`Ohtori A; Corneal critical barrier against the
`
`penetration of dexamethasone and lomefloxacin
`hydrochloride: evaluation by the activation energy for
`
`drug partition and diffusion in cornea, Drug Dev Ind
`
`H Pharm., 2007, 33(8), 805-11,
`
`2. Higashiyama M,
`
`Inada K, Ohtori A, Kakehi K; NMR
`
`1
`
`MYLAN EX. 1022, Page1
`
`MYLAN Ex. 1022, Page1
`
`
`
`Docket No. 200 4_1o1 6A
`
`Group Art Unit 1611
`
`Examineri Rae, Charlesworth E
`
`In re application of
`
`Masayo HIGASHIYAMA
`
`
`
`
`,/r C
`' as. :s»
`‘~~”
`.
`
`Filed on June 30, 2004
`
`For: AQUEOUS LIQUID PREPARATIONS AND LIGHT-STABILIZED AQUEOUS
`LIQUID PREPARATIONS
`
`DECLARATION UNDER 37 CFR §1.132
`
`Honorable Commissioner of
`Patents,
`P.O. Box 1450
`
`Alexandria, Virginia 22313-1450
`
`Sirs:
`
`I, Masayo HIGASHIYAMA, citizen of Japan and residing in
`
`Suita—shi, Osaka, Japan, sincerely declare;
`
`That my education and employment history is as follows:
`
`1.
`
`I graduated from Nagoya City University, Japan,
`
`Graduate School of Pharmaceutical Sciences,
`
`in March 1995,
`
`2.
`
`I received a Doctor's degree in Engineering from
`
`Kyushu Institute of Technology, Japan,
`
`in September 2007,
`
`and
`
`A
`
`3. since April 1995 up to this time, I have been an
`
`employee of Senju Pharmaceutical Co., Ltd., and engaged
`
`in the pharmaceutical research of ophthalmic formulation;
`
`That I am a member of the Pharmaceutical Society of Japan
`
`since.November 1993, and the Controlled Release Society
`
`since January 2002;
`
`That I am a co—author of the following papers:
`
`1. Yasueda S, Higashiyama M, Yamaguchi M,
`
`Isowaki A,
`
`Ohtori A; Corneal critical barrier against the
`
`penetration of dexamethasone and lomefloxacin
`hydrochloride: evaluation by the activation energy for
`
`drug partition and diffusion in cornea, Drug Dev Ind
`
`H Pharm., 2007, 33(8), 805-11,
`
`2. Higashiyama M,
`
`Inada K, Ohtori A, Kakehi K; NMR
`
`1
`
`MYLAN EX. 1022, Page1
`
`MYLAN Ex. 1022, Page1
`
`
`
`analysis of ion pair formation between timolol and sorbic
`
`acid in ophthalmic preparations, J Pharm Biomed Anal.,
`
`2007, 43(4), 1335-42,
`
`3. Higashiyama M, Tajika T,
`
`Inada K, Ohtori A;
`
`Improvement of the ocular bioavailability of carteolol by
`
`ion pair, J'Ocul Rharmacol Ther., 2006, 22(5), 333-9,
`
`Inada K, Ohtori
`4. Yasueda S, Higashiyama M, Shirasaki Y,
`A; An HPLC method to evaluate purity of a steroidal drug,
`
`loteprednol etabonate, J'Rharm Biomed Anal., 2004, 36(2),
`
`g
`309-16, and
`Improvement
`Inada K, Ohtori A, Tojo K:
`,
`5. Higashiyama
`of the ocular bioavailability of timolol by sorbic acid,
`
`Int J Pharm., 2004, 272(l—2), 91-8;
`
`That I am the sole inventor of the above-identified U.S.
`
`patent application SN 10/500,354; and
`
`That I conducted the following experiment to demonstrate
`
`the unexpected superior effect of the present invention that
`
`(+)—
`
`(S)—4—[4—[(4—chlorophenyl)(2—pyridyl)methoxylpiperidino]butyric
`
`acid and a pharmacologically acceptable acid addition salt
`
`thereof, particularly bepotastine besilate, can be light-
`
`stabilized in water by adding water—soluble metal chloride,
`
`the
`
`results of which follow hereunder.
`
`ggpgriment
`
`Effect of water—soluble metal chloride on light—stability of
`
`bepotastine besilate in aqueous solution as compared to the
`effect of glucose or mannitol
`.
`Test method
`
`The aqueous liquid preparations (Formulations 7, 18 and 19)
`
`shown in the following Table 1, which contained bepotastine
`
`besilate, were prepared according to conventional methods and
`
`filled in glass ampoules by 5 mL each. Using the Xenon long—life
`
`fade meter
`
`(FAL-25AX—Ec manufactured by SUGA TEST INSTRUMENTS Co.,
`
`Ltd.), a light corresponding to not less than 200 W-h/n3 in a
`
`total near—ultraviolet radiation energy was irradiated
`
`MYLAN EX.-1022, Page2
`
`MYLAN Ex. 1022, Page2
`
`
`
`(irradiation time: 23-34 hr), and the appearance of each
`
`formulated liquid preparation was observed. The amount of light
`
`exposure was measured by a quinine chemical actinometry system
`
`described in the Drug Approval and Licensing Procedures in Japan
`2001.
`
`Formulation
`
`bepotastine besilate
`
`sodium dihydrogen
`phosphate dihydrate
`sodium chloride
`
`glucose — 3-3
`mannitol —
`benzalkonium chloride
`o_oo5 .
`o_oo5 .
`sodium hydroxide
`S:;:::ie
`suitable amount
`total ‘amount
`100 mL
`
`o_oo5 .
`suitable amount
`
`irradiation
`
`appearance after ligh
`
`tpale—yellow black green,
`and
`containing
`precipitate
`
`black green,
`containing
`precipitate
`
`Test results
`
`The appearance after light irradiation did not change from
`
`that immediately after preparation and was pale yellow and clear
`
`for Formulation 7, comprising 0.6 w/v% sodium chloride. Meanwhile,
`the appearance after light irradiation turned black green for
`
`Formulation 18 and Formulation 19, comprising 3.3 w/v% glucose
`
`and 3.3 w/v% mannitol, and a precipitate was observed. The
`
`results indicate that a water—soluble metal chloride in a light
`
`stabilizing effective amount
`
`improves light—stability of
`
`bepotastine besilate, and saccharides such as glucose and
`
`mannitol do not improve light—stability of bepotastine besilate.
`
`I further declare that all statements made herein of my own
`
`knowledge are true and that all statements made on information
`
`and belief are believed to be true; and further that these
`
`statements were made with the knowledge that willful false
`
`MYLAN EX. 1022, Page3
`
`MYLAN Ex. 1022, Page3
`
`
`
`statements and the like so made are punishable by fine or
`imprisonment, or both, under Section 1001 of Title 18 of the
`
`United States Code and that such willful false statements may
`
`jeopardize the validity of the application or any patent issuing
`thereon.
`
`Signed at.C%qAh Japan on this «K2 day of December, 2008
`
`.' .
`
`.
`
`.
`
`.
`
`.
`
`.
`
`.
`
`Masayo HIGASHIYAMA
`
`MYLAN Ex; 1022, Page4
`
`MYLAN Ex. 1022, Page4
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