Solubility parameter based drug delivery system and method for altering drug saturation concentration

• US 6,221,383 B1
• Filed: 05/25/1999
• Issued: 04/24/2001
• Est. Priority Date: 01/07/1994
• Status: Expired due to Term

• Current Assignee: Noven Pharmaceuticals (Hisamitsu Pharmaceutical Company Incorporated)
• Original Assignee: Noven Pharmaceuticals (Hisamitsu Pharmaceutical Company Incorporated)
• Inventors: Miranda, Jesus, Sablotsky, Steven
• Primary Examiner(s): Dodson, Shelley A.
• Assistant Examiner(s): Williamson, Michael A.
• Application Number:
  US09/318,121
• Time in Patent Office: 700 Days
• Field of Search: 424/448, 424/449
• US Class Current: 424/449
• CPC Class Codes: A61F 13/0276 Apparatus or processes for manufacturing adhesive dressings or bandages
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61K 9/7069 obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide
• CPC Class Codes: A61L 15/18 containing inorganic materials
• CPC Class Codes: A61L 15/58 Adhesives
• CPC Class Codes: A61L 15/585 Mixtures of macromolecular compounds
• CPC Class Codes: B26F 1/384 using rotating drums
• CPC Class Codes: C08L 31/04 Homopolymers or copolymers of vinyl acetate
• CPC Class Codes: C08L 33/00 Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers

Abstract

A blend of at least two polymers, or at least one polymer and a soluble polyvinylpyrrolidone, in combination with a drug provides a pressure-sensitive adhesive composition for a transdermal drug delivery system in which the drug is delivered from the pressure-sensitive adhesive composition and through dermis when the pressure-sensitive adhesive composition is in contact with human skin. According to the invention, soluble polyvinylpyrrolidone can be used to prevent crystallization of the drug, without affecting the rate of drug delivery from the pressure-sensitive adhesive composition.

Claims

1. A pressure-sensitive adhesive composition suitable for use in a transdermal drug delivery system, which composition comprises a blend of:

(a) a rubber adhesive, wherein the rubber adhesive is present in an amount from 5% to 97% by weight of the total composition;

(b) a polyacrylate in an amount from 1% to 85% by weight of the total composition, wherein the ratio of the polyacrylate to the rubber adhesive is from 2;

98 to 96;

4;

(c) a therapeutically effective amount a mixture of two or more drugs for transdermal drug delivery, wherein the drug is present in an amount weight 0.1% to 50% by weight of the total composition, and wherein said two or more drugs include an androgenic steroid and an estrogen; and

(d) a soluble polyvinylpyrrolidone, wherein the soluble polyvinylpyrrolidone is present in an amount of 1% to 20% by weight of the total composition,

wherein the ratio of the drug to the soluble polyvinylpyrrolidone is from 1;

10 to 10;

1, and

wherein the amount of soluble polyvinylpyrrolidone is sufficient to solubilize all of the drug which is present in an amount that would exceed its solubility in a composition that contains a rubber adhesive and a polyacrylate, but lacks soluble polyvinylpyrrolidone.

2. A pressure-sensitive adhesive composition suitable for use in a transdermal drug delivery system, which composition comprises a blend of:

(a) a synthetic elastomeric polymer;

(b) a soluble polyvinylpyrrolidone;

(c) a therapeutically effective amount of a drug or a mixture of two or more drugs for transdermal drug delivery, wherein said two or more drugs include an androgenic steroid and an estrogen; and

(d) optionally one or more additives selected from the group consisting of enhancers, fillers, plasticizers, tackifying agents, and co-solvents.

3. A pressure-sensitive adhesive composition suitable for use in a transdermal drug delivery system, which composition comprises a blend of

(a) a rubber;

(b) a soluble polyvinylpyrrolidone;

(c) a therapeutically effective amount of a drug or a mixture of two or more drugs for transdermal drug delivery, wherein said two or more drugs include an androgenic steroid and an estrogen; and

(d) optionally one or more additives selected from the group consisting of enhancers, fillers, plasticizers, tackifying agents, and co-solvents.

4. A pressure-sensitive adhesive composition suitable for use in a transdermal drug delivery system, which composition comprises a blend of:

(a) a rubber adhesive, wherein the rubber adhesive is present in an amount from 5% to 97% by weight of the total composition;

(b) a polyacrylate in an amount from 1% to 85% by weight of the total composition, wherein the ratio of the polyacrylate to the rubber adhesive is from 2;

98 to 96;

4;

(c) a therapeutically effective amount a drug for transdermal drug delivery, wherein the drug is present in an amount of 0.1% to 50% by weight of the total composition, and wherein said drug is selected from the group consisting of terbinafine, sumatriptan, physostigmine, loratadine, simvastatin, pravstatin, methimazole, alendranate, etidronate, ropinirole, pramipexole, fenoldopam, and nimesulide; and

(d) a soluble polyvinylpyrrolidone, wherein the soluble polyvinylpyrrolidone is present in an amount of 1% to 20% by weight of the total composition,

wherein the ratio of the drug to the soluble polyvinylpyrrolidone is from 1;

10 to 10;

1, and

wherein the amount of soluble polyvinylpyrrolidone is sufficient to solubilize all of the drug which is present in an amount that would exceed its solubility in a composition that contains a rubber adhesive and a polyacrylate, but lacks soluble polyvinylpyrrolidone.