EP0327295A2 — Tetracycline dosage form

Claim 1

Independent Claim 82 words

A pharmaceutical composition including a core element including at least one active ingredient including at least one tetracycline antibiotic; and a core coating for the core element which is partially soluble at an acidic pH and which, in use, generates a dissolution profile for the pellet composition which is equal to or greater than the minimum dissolution profile required to provide bioequivalence with a capsule or tablet containing an equal amount of the at least one active ingredient in an uncoated form.

Claim 2

Dependent Claim 82 words

A pharmaceutical composition including a core element including at least one active ingredient including at least one tetracycline antibiotic; and a core coating for the core element which is partially soluble at an acidic pH and which, in use, generates a dissolution profile for the pellet composition which is equal to or greater than the minimum dissolution profile required to provide bioequivalence with a capsule or tablet containing an equal amount of the at least one active ingredient in an uncoated form.

Claim 3

Dependent Claim 26 words

A pharmaceutical composition according to claim 1 wherein the at least one tetracycline antibiotic is selected from tetracycline, chlortetracycline, demeclocycline, methacycline, oxytetracycline, minocycline and mixtures thereof.

Claim 4

Dependent Claim 86 words

A pharmaceutical composition according to claim 1 wherein a first dissolution profile is measured at a pH level approximating that of the stomach and a second dissolution profile is measured at a pH level approximately that of at least one point in the small intestine; the first and second dissolution profiles for the pharmaceutical composition each being equal to or greater than the minimum dissolution required to provide substantial bioequivalence with a capsule or tablet containing the at least one active ingredient in an uncoated form.

Claim 5

Dependent Claim 42 words

A pharmaceutical composition according to claim 2 wherein the pellet composition generates a total dissolution, in use a total dissolution of greater than 10% dissolved in one hour at pH 1.2 and greater than 50% dissolved after 30 minutes at pH 5.5.

Claim 6

Dependent Claim 53 words

A pharmaceutical composition including a core element including at least one active ingredient including at least one tetracycline antibiotic; and a core coating for the core element which is partially soluble at an acidic pH; and wherein the active ingredient is available for substantially complete absorption substantially immediately after entering the small intestine.

Claim 7

Dependent Claim 53 words

A pharmaceutical composition including a core element including at least one active ingredient including at least one tetracycline antibiotic; and a core coating for the core element which is partially soluble at an acidic pH; and wherein the active ingredient is available for substantially complete absorption substantially immediately after entering the small intestine.

Claim 8

Dependent Claim 44 words

A pharmaceutical composition according to claim 5 wherein the core coating is a hybrid core coating which coating provides a controlled low rate of release at an acidic pH and allows a more rapid rate of release at a less acidic to basic pH.

Claim 9

Dependent Claim 51 words

A pharmaceutical composition according to claim 6 wherein the hybrid core coating includes at least one polymer which is substantially insoluble at an acidic pH and at least partially soluble at a less acidic to basic pH; at least one component which is at least partially soluble at an acidic pH.

Claim 10

Dependent Claim 23 words

A pharmaceutical composition according to claim 7 wherein the tetracycline antibiotic is selected from tetracycline, chlortetracycline, demeclocyline, methacycline, oxytetracycline, minocycline and mixtures thereof.

Claim 11

Dependent Claim 18 words

A pharmaceutical composition according to claim 7 wherein the core element is a pellet, tabletted pellet or tablet.

Claim 12

Dependent Claim 13 words

A pharmaceutical composition according to claim 8 wherein the tetracycline antibiotic includes minocycline.

Claim 13

Dependent Claim 32 words

A pharmaceutical composition according to claim 7 wherein the core element includes an effective amount of at least one tetracycline antibiotic; at least one core seed; and at least one binding agent.

Claim 14

Dependent Claim 31 words

A pharmaceutical composition according to claim 7 wherein the core element includes an effective amount of at least one tetracycline antibiotic; at least one binding agent; and at least one filler.

Claim 15

Dependent Claim 26 words

A pharmaceutical composition according to claim 7 wherein the core element includes at least one tetracycline antibiotic; at least one lubricant; and at least one filler.

Claim 16

Dependent Claim 62 words

A pharmaceutical composition according to claim 11 wherein the at least one tetracycline antibiotic is present in amounts of approximately 5 to 95% by weight based on the total weight of the core element; and the at least one core seed is present in amounts of from approximately 5.0 to 25% by weight based on the total weight of the core element.

Claim 17

Dependent Claim 29 words

A pharmaceutical composition according to claim 14 wherein the core element has a formulation: minocycline powder 25 - 94% sugar seeds 5 - 74% hydroxypropyl cellulose 0.1 - 20%

Claim 18

Dependent Claim 28 words

A pharmaceutical composition according to claim 14 wherein the core element has a formulation: minocycline powder 25 - 94% sugar seeds 5 - 74% povidone 0.1 - 20%

Claim 19

Dependent Claim 29 words

A pharmaceutical composition according to claim 12 wherein the core element has a formulation: minocycline powder 25 - 94% microcystalline cellulose 1 - 40% Hydroxypropyl cellulose 1.0 - 10%

Claim 20

Dependent Claim 114 words

A pharmaceutical pellet composition according to claim 7 wherein the hybrid core coating includes approximately 15 to 85% by weight, based on the total weight of the hybrid core coating, excluding filler, of at least one acid insoluble polymer selected from cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, polyvinyl acetate phthalate, methacrylic acid copolymer type A, methacrylic acid: acrylic acid methyl ester copolymer, hydroxypropyl methylcellulose acetate succinate, shellac, cellulose acetate trimellitate or mixtures thereof; and approximately 1 to 50% by weight, based on the total weight of the hybrid core coating, excluding filler, of an at least partially acid soluble component selected from polyvinylpyrrolidine, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, sugars and mixtures thereof.

Claim 21

Dependent Claim 93 words

A pharmaceutical composition according to claim 18 wherein the hybrid core coating further includes 0 to approximately 50% by weight based on the total weight of the hybrid core coating, excluding filler, of a plasticizer at least one plasticizer selected from diethyl phthalate, triethyl citrate, triethyl acetyl citrate, triacetine, tributyl citrate, polyethylene glycol and glycerol; and 0 to approximately 50% by weight based on the total weight of the hybrid core coating of at least one filler selected from silicon dioxide, talc, alumina, starch, calcium, potassium, powdered cellulose, microcrystalline cellulose and mixtures thereon.

Claim 22

Dependent Claim 31 words

A pharmaceutical composition according to claim 19 wherein the hybrid core coating has a formulation: hydroxypropyl methyl cellulose phthalate 50 - 80% polyvinylpyrrolidone 10 - 40% diethyl phthalate 1 - 30%

Claim 23

Dependent Claim 87 words

A pharmaceutical product including a plurality of pellets including a core element including at least one active ingredient including at least one tetracycline antibiotic; a core coating for the core element which is partially soluble at an acidic pH and which, in use, generates a dissolution profile for the pellet composition which is equal to or greater than the minimum dissolution profile required to provide substantial bioequivalence with a capsule or tablet containing an equal amount of the at least one active ingredient in an uncoated form.

Claim 24

Dependent Claim 87 words

A pharmaceutical product including a plurality of pellets including a core element including at least one active ingredient including at least one tetracycline antibiotic; a core coating for the core element which is partially soluble at an acidic pH and which, in use, generates a dissolution profile for the pellet composition which is equal to or greater than the minimum dissolution profile required to provide substantial bioequivalence with a capsule or tablet containing an equal amount of the at least one active ingredient in an uncoated form.

Claim 25

Independent Claim 62 words

A method for preparing a pharmacutical composition which method includes providing at least one active ingredient including at least one tetracycline antibiotic; at least one core seed; at least one binding agent in a granulating solution; and contacting the core seed with the active ingredient and simultaneously adding the binding agent solution thereto in a spheronization process to form a core element.

Claim 26

Independent Claim 62 words

A method for preparing a pharmacutical composition which method includes providing at least one active ingredient including at least one tetracycline antibiotic; at least one core seed; at least one binding agent in a granulating solution; and contacting the core seed with the active ingredient and simultaneously adding the binding agent solution thereto in a spheronization process to form a core element.

Claim 27

Dependent Claim 86 words

A method according to claim 22 which method further includes providing a hybrid core coating composition including a solution or dispersion of at least one polymer which is substantially insoluble at an acidic pH and at least partially soluble of a less acidic to basic pH; and at least one component which is at least partially soluble at an acidic pH; and a fluidized bed reactor; introducing the core element into the fluidized bed reactor; and spraying the hybrid core coating composition onto the core element.

Claim 28

Independent Claim 101 words

A method of treating bacterial infections in patients requiring such treatment which method includes administering to a patient an effective amount of a pharmaceutical composition including a core element including at least one active ingredient including at least one tetracycline antibiotic; and a core coating for the core element which is partially soluble at a highly acidic pH and which, in use, generates a dissolution profile for the pellet composition which is equal to or greater than the minimum dissolution required to provide substantial bioequivalence with a capsule or tablet containing the at least one active ingredient in an uncoated form.

Claim 29

Independent Claim 101 words

A method of treating bacterial infections in patients requiring such treatment which method includes administering to a patient an effective amount of a pharmaceutical composition including a core element including at least one active ingredient including at least one tetracycline antibiotic; and a core coating for the core element which is partially soluble at a highly acidic pH and which, in use, generates a dissolution profile for the pellet composition which is equal to or greater than the minimum dissolution required to provide substantial bioequivalence with a capsule or tablet containing the at least one active ingredient in an uncoated form.

Claim 30

Dependent Claim 59 words

A method according to claim 24 wherein the pharmaceutical composition includes a core element including at least one active ingredient including at least one tetracycline antibiotic; and a core coating for the core element which is partially soluble at acidic pH; and wherein the active ingredient is available for substantially complete absorption substantially immediately after entering the small intestine.

Claim 31

Dependent Claim 25 words

A method according to claim 25 wherein the at least one tetracycline antibiotic is selected from tetracycline, chlortetracycline, demeclocyline, methocycline, oxytetracycline, minocycline and mixtures thereof.

Tetracycline dosage form

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