009423.0lOUSl
`
`CLAIMS
`
`What is claimed is:
`
`1.
`
`A solid composition comprising sincalide, wherein the composition does not contain a
`
`dibasic potassium phosphate buffer, and wherein the composition is stable in storage.
`
`2.
`
`The solid composition of claim 1, wherein the composition does not contain any
`
`phosphate buff er.
`
`3.
`
`The solid composition of claim 1, wherein the composition also does not contain
`
`polysorbate 20 and/or polysorbate 80.
`
`4.
`
`The solid composition of claim 3, wherein the composition does not contain any
`
`surfactant/solubilizer.
`
`5. The solid composition of claim 1, wherein the composition does not contain dibasic
`
`potassium phosphate and does not contain either or both polysorbate 20 and polysorbate 80.
`
`6.
`
`The solid composition of claim 1, wherein the composition further comprises a stabilizer
`
`and/or a bulking agent/tonicity adjuster.
`
`7.
`
`The solid composition of claim 6, wherein the stabilizer is selected from the group
`
`consisting of pentetic acid, arginine hydrochloride, L-methionine, L-lysine hydrochloride,
`
`sodium metabisulfite, and a combination thereof, and
`
`wherein the bulking agent/tonicity adjuster comprises mannitol.
`
`8.
`
`The solid composition of claim 1, wherein the composition maintains total impurities of
`
`less than 5% and/or a sincalide level of at least 90% after 15 months of storage at 25°C, 60%
`
`relative humidity when tested by a sincalide-specific assay.
`
`32
`
`Bracco Ex. 2012
`Maia v. Bracco
`IPR2019-00345
`
`1
`
`
`
`CLAIMS
`
`What is claimed is:
`
`1.
`
`A solid composition comprising sincalide, wherein the composition does not contain a
`
`dibasic potassium phosphate buffer, and wherein the composition is stable in storage.
`
`2.
`
`The solid composition of claim 1, wherein the composition does not contain any
`
`phosphate buff er.
`
`3.
`
`The solid composition of claim 1, wherein the composition also does not contain
`
`polysorbate 20 and/or polysorbate 80.
`
`4.
`
`The solid composition of claim 3, wherein the composition does not contain any
`
`surfactant/solubilizer.
`
`5. The solid composition of claim 1, wherein the composition does not contain dibasic
`
`potassium phosphate and does not contain either or both polysorbate 20 and polysorbate 80.
`
`6.
`
`The solid composition of claim 1, wherein the composition further comprises a stabilizer
`
`and/or a bulking agent/tonicity adjuster.
`
`7.
`
`The solid composition of claim 6, wherein the stabilizer is selected from the group
`
`consisting of pentetic acid, arginine hydrochloride, L-methionine, L-lysine hydrochloride,
`
`sodium metabisulfite, and a combination thereof, and
`
`wherein the bulking agent/tonicity adjuster comprises mannitol.
`
`8.
`
`The solid composition of claim 1, wherein the composition maintains total impurities of
`
`less than 5% and/or a sincalide level of at least 90% after 15 months of storage at 25°C, 60%
`
`relative humidity when tested by a sincalide-specific assay.
`
`32
`
`Bracco Ex. 2012
`Maia v. Bracco
`IPR2019-00345
`
`1
`
`
`
`009423.0lOUSl
`
`9.
`
`The solid composition of claim 1, comprising:
`
`(a) a therapeutically effective amount of sincalide,
`
`(b) I to 4 mg pentetic acid,
`
`(c) 15 to 45 mg arginine hydrochloride,
`
`(d) 2 to 8 mg methionine,
`
`(e) 7.5 to 30 mg lysine hydrochloride,
`
`(f) 0.02 to I mg sodium metabisulfite,
`
`(g) 85 to 340 mg mannitol, and
`
`(e) a pH from 6.5 to 7.5 when reconstituted in a pharmaceutically acceptable diluent; and
`
`wherein the composition does not contain a buffer having a pKa within one unit of the pH, and
`
`wherein the composition is storage stable.
`
`10.
`
`The solid composition of claim 1, wherein the composition is a lyophilized powder.
`
`11.
`
`A method for the treatment, prevention, and/or diagnosis of gall bladder- and/or
`
`pancreatic disorders, or other diagnostic imaging of a patient in need thereof comprising
`
`administering a therapeutically or diagnostically effective amount of the composition of claim I
`
`in reconstituted form to the patient.
`
`12.
`
`The method of claim 11, wherein the composition comprises:
`
`(a) a chelator comprising pentetic acid,
`
`(b) a stabilizer comprising a combination of L-arginine hydrochloride, L-methionine, L(cid:173)
`
`lysine hydrochloride, and sodium metabisulfite,
`
`( c) a bulking agent/tonicity adjuster comprising mannitol, and
`
`wherein the composition further lacks dibasic potassium phosphate, and wherein the composition
`
`further lacks polysorbate 20.
`
`13.
`
`A method of making a storage stable solid sincalide composition comprising:
`
`(1) mixing:
`
`(a) sincalide, and
`
`33
`
`2
`
`
`
`009423.0lOUSl
`
`(b) an excipient consisting essentially of (i) a stabilizer, (ii) a bulking
`
`agent/tonicity adjuster, (iii) a chelator, or (iv) any combination of (i), (ii) and (iii), and
`
`(c) water
`
`(2) adjusting the pH of the mixture to 6.5 to 7.5, and
`
`(3) lyophilizing the pH-adjusted mixture,
`
`wherein the storage stable sincalide composition does not contain a buffer having a pKa within
`
`one unit of the pH.
`
`14. The method of claim 13, wherein the storage stable solid sincalide composition does not
`
`contain a surfactant/solubilizer.
`
`15.
`
`A liquid composition comprising sincalide and a pharmaceutically acceptable carrier,
`
`wherein the composition is storage stable.
`
`16.
`
`The liquid composition of claim 15, wherein the composition further comprises a
`
`stabilizer and/or a bulking agent/tonicity adjuster.
`
`17.
`
`The liquid composition of claim 16, wherein the stabilizer is selected from the group
`
`consisting of pentetic acid, arginine hydrochloride, L-methionine, L-lysine hydrochloride,
`
`sodium metabisulfite, and a combination thereof, and
`
`wherein the bulking agent/tonicity adjuster comprises mannitol.
`
`18.
`
`The liquid composition of claim 15, wherein the composition lacks a phosphate buffer.
`
`19.
`
`The liquid composition of claim 18, wherein the composition lacks any buffer.
`
`20.
`
`The liquid composition of claim 15, wherein the composition does not contain
`
`polysorbate 20 and/or polysorbate 80.
`
`21.
`
`The liquid composition of claim 20, wherein the composition does not contain any
`
`surfactant/solubilizer.
`
`34
`
`3
`
`
`
`009423.0lOUSl
`
`22.
`
`The liquid composition of claim 15, wherein the composition does not contain dibasic
`
`potassium phosphate and does not contain either or both polysorbate 20 and polysorbate 80.
`
`23.
`
`The liquid composition of claim 15, wherein the composition maintains total impurities
`
`of less than 5% and/or a sincalide level of at least 90% after
`
`i) 6 month of storage at 25°C, 65% relative humidity, or
`
`ii) 12 months of storage at 2-8°C,
`
`when tested by a sincalide-specific assay.
`
`24.
`
`The liquid composition of claim 15, comprising:
`
`(a) a therapeutically effective amount of sincalide,
`
`(b) I to 4 mg pentetic acid,
`
`(c) 15 to 45 mg arginine hydrochloride,
`
`(d) 2 to 8 mg methionine,
`
`(e) 7.5 to 30 mg lysine hydrochloride,
`
`(f) 0.02 to I mg sodium metabisulfite, and
`
`(g) 85 to 340 mg mannitol;
`
`wherein the pH of the composition is 6.5 to 7.5, and
`
`wherein the composition does not contain a buffer having a pKa within one unit of the
`
`pH, and wherein the composition is storage stable.
`
`25.
`
`A method for the treatment, prevention, and/or diagnosis of gall bladder- and/or
`
`pancreatic disorders, or other diagnostic imaging of a patient in need thereof administering a
`
`therapeutically or diagnostically effective amount of the liquid composition of claim 15 to the
`
`patient.
`
`26.
`
`The method of claim 25, further comprising diluting the composition prior to
`
`administering it.
`
`27.
`
`The method of claim 26, wherein the liquid composition comprises:
`35
`
`4
`
`
`
`009423.0lOUSl
`
`(a) a therapeutically effective amount of sincalide,
`
`(b) I to 4 mg pentetic acid,
`
`(c) 15 to 45 mg arginine hydrochloride,
`
`(d) 2 to 8 mg methionine,
`
`(e) 7.5 to 30 mg lysine hydrochloride,
`
`(f) 0.02 to I mg sodium metabisulfite,
`
`(g) 85 to 340 mg mannitol, and
`
`(e) a pH from 6.5 to 7.5.
`
`28.
`
`The method of claim 27, wherein the composition does not contain a buffer having a pKa
`
`within one unit of the pH.
`
`29.
`
`The method of claim 28, wherein the composition further does not contain a
`
`surfactant/solubilizer.
`
`30.
`
`A method of making a storage stable liquid sincalide composition comprising:
`
`(1) mixing:
`
`(a) sincalide, and
`
`(b) an excipient, wherein the excipient consists essentially of (i) a stabilizer, (ii) a
`
`agent/tonicity adjuster, (iii) a chelator, or (iv) any combination of (i), (ii)
`
`bulking
`
`and (iii), and
`
`(c) water, and
`
`(2) adjusting the pH of the mixture to 6.5 to 7.5,
`
`wherein the storage stable sincalide composition maintains total impurities of less than 5%,
`
`and/or a sincalide level of at least 90% after
`
`i) 6 month of storage at 25°C, 65% relative humidity, or
`
`ii) 12 months of storage at 2-8°C,
`
`when tested by a sincalide-specific assay.
`
`36
`
`5
`
`
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