US4265874A — Method of delivering drug with aid of effervescen…

Claim 1

Independent Claim 169 words

An osmotic device for delivering a drug to an environment of use, said device comprising: (a) a shaped laminated wall comprising a lamina formed of a semi-permeable material and a lamina formed of a microporous material, said wall permeable to the passage of an external fluid present in the environment of use and substantially impermeable to the passage of drug, the wall surrounding and forming; (b) a compartment containing the drug indomethacin which exhibits a limited solubility in the fluid, and a pharmaceutically acceptable compound selected from the group consisting of carbonates, bicarbonates and mixtures thereof, which compounds are capable of reactively effervescing with fluid present in the environment of use; and, (c) a passageway in the wall connecting the compartment and the exterior of the device for delivering (1) the drug in a therapeutically effective amount to the envirionment, and (2) the compound which reacts with fluid in the environment and effervesces, and thereby aids in delivering the drug to the environment over a prolonged period of time.

Claim 2

Dependent Claim 169 words

An osmotic device for delivering a drug to an environment of use, said device comprising: (a) a shaped laminated wall comprising a lamina formed of a semi-permeable material and a lamina formed of a microporous material, said wall permeable to the passage of an external fluid present in the environment of use and substantially impermeable to the passage of drug, the wall surrounding and forming; (b) a compartment containing the drug indomethacin which exhibits a limited solubility in the fluid, and a pharmaceutically acceptable compound selected from the group consisting of carbonates, bicarbonates and mixtures thereof, which compounds are capable of reactively effervescing with fluid present in the environment of use; and, (c) a passageway in the wall connecting the compartment and the exterior of the device for delivering (1) the drug in a therapeutically effective amount to the envirionment, and (2) the compound which reacts with fluid in the environment and effervesces, and thereby aids in delivering the drug to the environment over a prolonged period of time.

Claim 3

Dependent Claim 18 words

The osmotic device for delivering the drug according to claim 1 wherein the drug is sodium indomethacin trihydrate.

Claim 4

Dependent Claim 29 words

The osmotic device for delivering the drug according to claim 1 wherein the drug is delivered in a therapeutically effective amount of 2 milligrams to 15 milligrams per hour.

Claim 5

Dependent Claim 17 words

The osmotic device for delivering the drug according to claim 1 wherein the bicarbonate is potassium bicarbonate.

Claim 6

Dependent Claim 17 words

The osmotic device for delivering the drug according to claim 1 wherein the carbonate is potassium carbonate.

Claim 7

Dependent Claim 61 words

The osmotic device for delivering the drug according to claim 1 wherein the microporous lamina comprises 45% of cellulose acetate having an acetyl content of 39.8%, 27.5% of hydroxypropyl methylcellulose and 27.5% of polyethylene glycol, and the semipermeable lamina comprises 50% of cellulose acetate having an acetyl content of 39.8%, and 50% of cellulose acetate having an acetyl content of 32%.

Claim 8

Dependent Claim 60 words

The osmotic device for delivering the drug according to claim 1 wherein the microporous lamina comprises 45% of cellulose acetate having an acetyl content of 39.8%, 45% of sorbitol, and 10% of polyethylene glycol, and the semipermeable lamina comprises 50% of cellulose acetate having an acetyl content of 39.8%, and 50% of cellulose acetate having an acetyl content of 32%.

Claim 9

Dependent Claim 59 words

The osmotic device for delivering the drug according to claim 1, wherein (1) the indomethacin exhibits a limited solubility in the fluid and precipitates therein, and wherein (2) the compound reacts with the fluid in the environment and effervesces, which effervescence substantially prevents precipitation of the drug at the passageway of the device over a prolonged period of time.

Claim 10

Dependent Claim 29 words

The osmotic device for delivering the drug according to claim 1 wherein the environment of use is a human, and the device is orally admitted into the gastrointestinal tract.

Claim 11

Dependent Claim 104 words

The osmotic device for delivering the drug according to claim 1 wherein, when the device is in operation in the environment of use, fluid therefrom is imbibed through the wall into the compartment in a tendency towards osmotic equilibrium, at a rate determined by the permeability of the wall and the osmotic pressure gradient across the wall to form a solution of compound containing the drug, which solution is delivered through the passageway to the environment of use, with the compound effervescing in the environment, and the drug being delivered to the environment in a therapeutically effective amount over a prolonged period of time.

Claim 12

Dependent Claim 141 words

An osmotic device for orally delivering a drug to a human, which device comprises: (a) a shaped laminated wall comprising a semipermeable lamina and a microporous lamina, said wall permeable to the passage of an external fluid and substantially impermeable to the passage of drug, the wall surrounding and forming: (b) a compartment containing from 0.5 milligrams to 3 grams of the drug indomethacin, and from 0.5 milligrams to 3 grams of a pharmaceutically acceptable compound selected from the group consisting of carbonates, bicarbonates and mixtures thereof that are capable of effervescing in the presence of the fluid; and, (c) a passageway in the wall for delivering from the device at a controlled and continuous rate, a therapeutically effective amount of the drug, and an amount of the compound for reactively effervescing with the fluid over a prolonged period of time.

Claim 13

Dependent Claim 141 words

An osmotic device for orally delivering a drug to a human, which device comprises: (a) a shaped laminated wall comprising a semipermeable lamina and a microporous lamina, said wall permeable to the passage of an external fluid and substantially impermeable to the passage of drug, the wall surrounding and forming: (b) a compartment containing from 0.5 milligrams to 3 grams of the drug indomethacin, and from 0.5 milligrams to 3 grams of a pharmaceutically acceptable compound selected from the group consisting of carbonates, bicarbonates and mixtures thereof that are capable of effervescing in the presence of the fluid; and, (c) a passageway in the wall for delivering from the device at a controlled and continuous rate, a therapeutically effective amount of the drug, and an amount of the compound for reactively effervescing with the fluid over a prolonged period of time.

Claim 14

Dependent Claim 28 words

The osmotic device for orally delivering the drug according to claim 11 wherein the device is orally admitted into the gastrointestional tract and the fluid is gastric fluid.

Claim 15

Dependent Claim 39 words

The osmotic device for orally delivering the drug according to claim 11 wherein the carbonate is a member selected from the group consisting of lithium carbonate, sodium carbonate, potassium carbonate, ammonium carbonate, magnesium carbonate, calcium carbonate, and mixtures thereof.

Claim 16

Dependent Claim 37 words

The osmotic device for orally delivering the drug according to claim 11 wherein the bicarbonate is a member selected from the group consisting of lithium bicarbonate, sodium bicarbonate, potassium bicarbonate, magnesium bicarbonate, calcium bicarbonate, and mixtures thereof.

Claim 17

Dependent Claim 51 words

The osmotic device for orally delivering the drug according to claim 11 wherein the indomethacin is sodium indomethacin trihydrate and the compartment contains from 40 milligrams to 250 milligrams of said indomethacin, and the bicarbonate is potassium bicarbonate and the compartment contains from 50 milligrams to 300 millgrams of said bicarbonate.

Claim 18

Dependent Claim 47 words

The osmotic device for orally delivering the drug according to claim 11 wherein the indomethacin is sodium indomethacin trihydrate and the compartment contains from 85 milligrams to 125 milligrams thereof, and the bicarbonate is potassium bicarbonate and the compartment contains from 130 milligrams to 190 milligrams thereof.

Claim 19

Dependent Claim 39 words

The osmotic device for orally delivering the drug according to claim 11 wherein the indomethacin is sodium indomethacin trihydrate and the compartment contains 105 milligrams thereof, and the bicarbonate is potassium bicarbonate and the compartment contains 142 milligrams thereof.

Claim 20

Dependent Claim 39 words

The osmotic device for orally delivering the drug according to claim 11 wherein the indomethacin is sodium indomethacin trihydrate and the compartment contains 105 milligrams thereof, and the bicarbonate is potassium bicarbonate and the comparment contains 158 milligrams thereof.

Claim 21

Dependent Claim 46 words

The osmotic device for orally delivering the drug according to claim 11 wherein the microporous lamina comprises cellulose acetate, hydroxypropyl methylcellulose and polyethylene glycol, and the semipermeable lamina comprises cellulose acetate having an acetyl content of 32% and cellulose acetate having an acetyl content of 39.8%.

Claim 22

Dependent Claim 45 words

The osmotic device for orally delivering the drug according to claim 11 wherein the microporous lamina comprises cellulose acetate, sorbitol and polyethylene glycol, and the semipermeable lamina comprises cellulose acetate having an acetyl content of 39.8% and cellulose acetate having an acetyl content of 32%.

Claim 23

Dependent Claim 138 words

An osmotic device for orally delivering a drug to a human, which device comprises: (a) a shaped semipermeable, wall said wall permeable to the passage of an external fluid and substantially impermeable to the passage of drug, the semipermeable wall surrounding and forming: (b) a compartment containing from 0.5 milligrams to 3 grams of the drug indomethacin, and from 0.5 milligrams to 3 grams of a pharmaceutically acceptable compound selected from the group consisting of carbonates, bicarbonates and mixtures thereof that are capable of reactively effervescing in the presence of the fluid; and, (c) a passageway in the wall for delivering from the device to the human at a controlled and continuous rate, a therapeutically effective amount of the drug, and an amount of the compound for reactively effervescing with the fluid over a prolonged period of time.

Claim 24

Dependent Claim 138 words

An osmotic device for orally delivering a drug to a human, which device comprises: (a) a shaped semipermeable, wall said wall permeable to the passage of an external fluid and substantially impermeable to the passage of drug, the semipermeable wall surrounding and forming: (b) a compartment containing from 0.5 milligrams to 3 grams of the drug indomethacin, and from 0.5 milligrams to 3 grams of a pharmaceutically acceptable compound selected from the group consisting of carbonates, bicarbonates and mixtures thereof that are capable of reactively effervescing in the presence of the fluid; and, (c) a passageway in the wall for delivering from the device to the human at a controlled and continuous rate, a therapeutically effective amount of the drug, and an amount of the compound for reactively effervescing with the fluid over a prolonged period of time.

Claim 25

Dependent Claim 28 words

The osmotic device for orally delivering the drug according to claim 21 wherein the device is orally admitted into the gastrointestional tract, and the fluid is gastric fluid.

Claim 26

Dependent Claim 40 words

The osmotic device for orally delivering the drug according to claim 21 wherein the carbonate is a member selected from the group consisting essentially of lithium carbonate, sodium carbonate, potassium carbonate, ammonium carbonate, magnesium carbonate, calcium carbonate, and mixtures thereof.

Claim 27

Dependent Claim 37 words

The osmotic device for orally delivering the drug according to claim 21 wherein the bicarbonate is a member selected from the group consisting of lithium bicarbonate, sodium bicarbonate, potassium bicarbonate, magnesium bicarbonate, calcium bicarbonate, and mixtures thereof.

Claim 28

Dependent Claim 52 words

The osmotic device for orally delivering the drug according to claim 21 wherein the indomethacin is sodium indomethacin trihydrate and the compartment contains from 40 milligrams to lb 250 milligrams of said indomethacin, and the bicarbonate is potassium bicarbonate and the compartment contains from 50 milligrams to 300 milligrams of said bicarbonate.

Claim 29

Dependent Claim 47 words

The osmotic device for orally delivering the drug according to claim 21 wherein the indomethacin is sodium indomethacin trihydrate and the compartment contains from 85 milligrams to 125 milligrams thereof, and the bicarbonate is potassium bicarbonate and the compartment contains from 130 milligrams to 190 milligrams thereof.

Claim 30

Dependent Claim 42 words

The osmotic device for orally delivering the drug according to claim 21 wherein the semipermeable material comprises a selectively permeable polymer selected from the group consisting of cellulose acylate, cellulose diacylate, cellulose triacylate, cellulose acetate, cellulose diacetate, cellulose triacetate, and mixtures thereof.

Claim 31

Dependent Claim 34 words

The osmotic device for orally delivering the drug according to claim 21 wherein the semipermeable wall comprises cellulose acetate having an acetyl content of 32% and cellulose acetate having an acetyl content of 39.8%.

Claim 32

Dependent Claim 37 words

The osmotic device for orally delivering a drug according to claim 21 wherein semipermeable wall comprises 50% of cellulose acetate having an acetyl content of 32%, and 50% of cellulose acetate having an acetyl content of 39.8%.

Annuity Stage	Window Opens	Payment Deadline	Surcharge Period Until	Estimated Fee	Status
3.5 Years (Year 4)	1984-05-04	1984-11-03	1985-05-05	$2000.00	Window Closed / Lapsed
7.5 Years (Year 8)	1988-05-04	1988-11-03	1989-05-05	$3760.00	Window Closed / Lapsed
11.5 Years (Year 12)	1992-05-04	1992-11-03	1993-05-05	$7700.00	Window Closed / Lapsed

Method of delivering drug with aid of effervescent activity generated in environment of use

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