US4344934A — Therapeutic compositions with enhanced bioavailab…

Claim 1

Independent Claim 73 words

A pharmaceutical composition in dry solid form comprising a mixture of a therapeutically effective amount of a poorly water soluble drug and a non-toxic, pharmacologically acceptable, water-soluble polymer; said mixture being the product of a melt mix or of a dried solution and said mixture in dry solid form having been treated with solution comprising water and a minor amount of a wetting agent selected from anionic and cationic surfactants and then dried.

Claim 2

Dependent Claim 73 words

A pharmaceutical composition in dry solid form comprising a mixture of a therapeutically effective amount of a poorly water soluble drug and a non-toxic, pharmacologically acceptable, water-soluble polymer; said mixture being the product of a melt mix or of a dried solution and said mixture in dry solid form having been treated with solution comprising water and a minor amount of a wetting agent selected from anionic and cationic surfactants and then dried.

Claim 3

Dependent Claim 33 words

The composition of claim 1 wherein said polymer is selected from at least one of polyvinylpyrrolidone, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, methyl cellulose, block co-polymers of ethylene oxide and propylene oxide, and polyethylene glycol.

Claim 4

Dependent Claim 29 words

The composition of claim 1 wherein said wetting agent is an anionic surfactant selected from sodium lauryl sulfate, sodium laurate, dioctylsodium sulfosuccinate, sodium stearate, potassium stearate and sodium oleate.

Claim 5

Dependent Claim 21 words

The composition of claim 1 wherein said wetting agent is a cationic surfactant selected from benzalkonium chloride and bis-2-hydroxyethyl oleyl amine.

Claim 6

Dependent Claim 37 words

The composition of claim 1 or 2 wherein the concentration of said drug is from about 0.1% to about 95% by weight and the concentration of said polymer is from about 5% to about 99% by weight.

Claim 7

Dependent Claim 37 words

The composition of claim 1 or 2 wherein the concentration of said drug is from about 50% to about 90% by weight and the concentration of said polymer is from about 10% to about 50% by weight.

Claim 8

Dependent Claim 36 words

The composition of claim 1 or 2 wherein the concentration of said drug is about 50% to about 80% by weight and the concentration of said polymer is from about 20% to about 50% by weight.

Claim 9

Dependent Claim 29 words

The composition of claim 1, 2, 3 or 4 wherein the concentration of the wetting agent in the drug-polymer mixture is from about 0.025% to about 2.0% by weight.

Claim 10

Dependent Claim 29 words

The composition of claim 1, 2, 3 or 4 wherein the concentration of the wetting agent in the drug-polymer mixture is from about 0.2% to about 1.0% by weight.

Claim 11

Dependent Claim 14 words

The composition of claim 1, 2 3 or 4 wherein said drug is griseofulvin.

Claim 12

Dependent Claim 60 words

The composition of claim 1, 2, 3 or 4 wherein said drug is griseofulvin in a concentration ranging from about 0.1% to about 90% by weight; the concentration of the polymer is from about 5% to about 95% by weight; and the concentration of the wetting agent in the drug-polymer mixture is from about 0.025% to about 2.0% by weight.

Claim 13

Dependent Claim 60 words

The composition of claim 1, 2, 3 or 4 wherein said drug is griseofulvin in a concentration ranging from about 50% to about 80% by weight; the concentration of the polymer is from about 20% to about 50% by weight; and the concentration of the wetting agent in the drug-polymer mixture is from about 0.2% to about 1.0% by weight.

Claim 14

Dependent Claim 116 words

A pharmaceutical composition in solid form comprising a mixture of at least about 0.1% to about 90% by weight of griseofulvin; from about 5% to about 95% by weight of a polymer selected from polyvinylpyrrolidone, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, methyl cellulose, block copolymers of ethylene oxide and propylene oxide, and polyethylene glycol; and from about 0.025% to about 2.0% by weight of a wetting agent selected from anionic surfactants which was added to the drug-polymer mixture in dry solid form by a wet treatment from a solution comprising water; wherein said drug polymer mixture is the product of a melt mix or of a dried solution and said composition was dried following the wet treatment.

Claim 15

Dependent Claim 116 words

A pharmaceutical composition in solid form comprising a mixture of at least about 0.1% to about 90% by weight of griseofulvin; from about 5% to about 95% by weight of a polymer selected from polyvinylpyrrolidone, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, methyl cellulose, block copolymers of ethylene oxide and propylene oxide, and polyethylene glycol; and from about 0.025% to about 2.0% by weight of a wetting agent selected from anionic surfactants which was added to the drug-polymer mixture in dry solid form by a wet treatment from a solution comprising water; wherein said drug polymer mixture is the product of a melt mix or of a dried solution and said composition was dried following the wet treatment.

Claim 16

Dependent Claim 60 words

The composition of claim 13 wherein the concentration of the griseofulvin is from about 50% to about 80% by weight; from about 20% to about 50% by weight of a polymer selected from polyvinylpyrrolidone and hydroxypropyl cellulose; and from about 0.2% to about 1.0% by weight of an anionic surfactant selected from sodium lauryl sulfate, sodium sulfate and dioctylsodium sulfosuccinate.

Claim 17

Dependent Claim 29 words

A compressed pharmaceutical tablet comprising the composition of claim 1, 2, 3, 4, 13 or 14 wherein said drug is in the form of ultramicrocrystals and pharmaceutically acceptable excipients.

Claim 18

Independent Claim 76 words

A method of preparing a pharmaceutical composition with increased bioavailability in mammals from a poorly water soluble or water insoluble drug, which comprises: (a) forming a solution of the drug with a pharmacologically acceptable, water soluble polymer; (b) drying the drug-polymer solution; (c) treating the dried drug-polymer solution with a wetting sufficient amount of a solution comprising water and a wetting agent selected from anionic and cationic surfactants; and (d) drying the mixture of step (c).

Claim 19

Independent Claim 76 words

A method of preparing a pharmaceutical composition with increased bioavailability in mammals from a poorly water soluble or water insoluble drug, which comprises: (a) forming a solution of the drug with a pharmacologically acceptable, water soluble polymer; (b) drying the drug-polymer solution; (c) treating the dried drug-polymer solution with a wetting sufficient amount of a solution comprising water and a wetting agent selected from anionic and cationic surfactants; and (d) drying the mixture of step (c).

Claim 20

Dependent Claim 48 words

The method of claim 16 wherein said polymer is selected from polyvinylpyrrolidone, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, polyethylene glycol and block co-polymers of ethylene oxide and propylene oxide and said wetting agent is an anionic surfactant selected from sodium lauryl sulfate, sodium laurate and dioctyl sodium sulfosuccinate.

Claim 21

Dependent Claim 63 words

The method of claim 16 or 17 wherein the solution of the drug and polymer is formed in a mutual solvent; the drug is griseofulvin and wherein the concentration of griseofulvin in the dried mixture of step (d) is from about 0.1% to about 90% by weight and the concentration of the wetting agent in the dried mixture is about 0.025-2.0% by weight.

Claim 22

Dependent Claim 30 words

The method of claim 18 wherein the grisefulvin concentration is from about 50% to about 80% and the concentration of said wetting agent is from about 0.2% to about 1.0%.

Claim 23

Dependent Claim 11 words

The product prepared by the method of claim 16 or 17.

Claim 24

Dependent Claim 22 words

A method for treating fungal diseases in mammals which comprises orally administering to said mammal the composition of claim 13 or 14.

Claim 25

Dependent Claim 9 words

The product prepared by the method of claim 18.

Claim 26

Dependent Claim 9 words

The product prepared by the method of claim 19.

Annuity Stage	Window Opens	Payment Deadline	Surcharge Period Until	Estimated Fee	Status
3.5 Years (Year 4)	1985-08-16	1986-02-15	1986-08-17	$2000.00	Window Closed / Lapsed
7.5 Years (Year 8)	1989-08-16	1990-02-15	1990-08-17	$3760.00	Window Closed / Lapsed
11.5 Years (Year 12)	1993-08-16	1994-02-15	1994-08-17	$7700.00	Window Closed / Lapsed

Therapeutic compositions with enhanced bioavailability

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