Use of copolymers as solubilizers for slightly water-soluble compounds

• US 8,158,686 B2
• Filed: 10/25/2006
• Issued: 04/17/2012
• Est. Priority Date: 11/04/2005
• Status: Active Grant

• Current Assignee: BASF AG (BASF SE)
• Original Assignee: BASF SE
• Inventors: Bouillo, Nathalie, Pierobon, Marianna, Widmaier, Ralf, Dobrawa, Rainer, Lange, Ronald Frans-Maria, Meyer-Boehm, Kathrin
• Primary Examiner(s): Vivlemore, Tracy
• Assistant Examiner(s): Levin, Miriam A.
• Application Number:
  US12/092,676
• Publication Number:
  US 20080293828A1
• Time in Patent Office: 2,001 Days
• Field of Search: 514/183, 514/772.3
• US Class Current: 514/772.3
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61K 8/86 Polyethers
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin
• CPC Class Codes: C08F 218/08 Vinyl acetate
• CPC Class Codes: C08F 220/06 Acrylic acid; Methacrylic acid; Metal salts or ammonium salts thereof

Abstract

The use of copolymers obtained by free-radical polymerization of a mixture of

• • i) 30 to 80% by weight of N-vinyllactam,
  • ii) 10 to 50% by weight of vinyl acetate, and
  • iii) 10 to 50% by weight of a polyether,
    with the proviso that the total of components i), ii) and iii) equals 100% by weight,
    as solubilizers for slightly water-soluble substances.

Claims

1. A method comprising solubilizing a slightly water soluble substance with a copolymer wherein the copolymer solubilizes the slightly water-soluble substance and wherein the copolymer is obtained by free-radical polymerization of a mixture of

i) 30 to 80% by weight of N-vinylcaprolactam, N-vinylpyrrolidone, or a mixture thereof,

ii) 10 to 50% by weight of vinyl acetate, and

iii) 10 to 50% by weight of a polyethylene glycol,

with the proviso that the total of components i), ii) and iii) equals 100% by weight.

2. The method according to claim 1, where the copolymer is obtained from

i) 30 to 70% by weight of N-vinylcaprolactam, N-vinylpyrrolidone, or a mixture thereof,

ii) 15 to 35% by weight of vinyl acetate, and

iii) 10 to 35% by weight of a polyethylene glycol.

3. The method according to claim 1, where N-vinylcaprolactam is employed as component i).

4. The method according to claim 1, where the copolymer comprises a polyethylene glycol having a molecular weight of from 1000 daltons to 10 000 daltons as component iii).

5. The method according to claim 1, where the copolymer has a K value from 10 to 60 and wherein the K value is measured in a 1% by weight ethanolic solution.

6. The method according to claim 4, where the copolymer has a K value of from 15 to 40 and wherein the K value is measured in a 1% by weight ethanolic solution.

7. The method according to claim 1, where the slightly water-soluble substance is a bioactive substance.

8. The method according to claim 1 for producing a pharmaceutical preparation for the treatment of diseases.

9. The method according to claim 1 for producing cosmetic preparations.

10. The method according to claim 1 for producing-agrochemical preparations.

11. The method according to claim 1 for producing-dietary supplements or dietetic compositions.

12. The method according to claim 1 for producing food products.

13. The method according to claim 1 for producing colorant preparations.