Use of Polyvinyl Lactam-Polyalkylene Block Copolymers as Solubilisers for Poorly Water-Soluble Compounds

• US 20080300320A1
• Filed: 11/30/2006
• Published: 12/04/2008
• Est. Priority Date: 12/09/2005
• Status: Abandoned Application

• Current Assignee: BASF AG (BASF SE)
• Original Assignee: BASF SE
• Inventors: Dobrawa, Rainer, Mathauer, Klemens, Bouillo, Nathalie, Meyer-Bohm, Kathrin, Munster, Ingo, Lange, Ronald Frans Maria
• Application Number:
  US12/096,544
• Publication Number:
  US 20080300320A1
• Time in Patent Office: Days
• US Class Current: 514/772.1
• CPC Class Codes: A01N 25/02 containing liquids as carriers, diluents or solvents
• CPC Class Codes: A01N 25/30 characterised by the surfactants
• CPC Class Codes: A23L 29/00 Foods or foodstuffs containing additives containing additives for modifying the nutritive qualities A23L33/10; containing substantially indigestive additives, e.g. dietary fibres, A23L33/21; Preparation or treatment thereof
• CPC Class Codes: A23L 29/288 Synthetic resins, e.g. polyvinylpyrrolidone
• CPC Class Codes: A61K 2800/54 Polymers characterized by specific structures/properties
• 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 8/90 Block copolymers A61K8/89 takes precedence
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin

Abstract

Use of polyvinyllactam-polyalkylene oxide block copolymers as solubilizers for sub-stances which are sparingly soluble in water.

Claims

1. A composition comprising polyvinyllactam-polyalkylene oxide block copolymers as solubilizers for substances which are sparingly soluble in water.

2. The composition according to claim 1, wherein the block copolymers are prepared by coupling polyvinyllactams that are terminated at one or both chain ends with hydroxyl groups with polyalkylene oxides via reaction with diisocyanates.

3. The composition according to claim 1 wherein the polyvinyllactams have K values of from 6 to 20.

4. The composition according to claim 1 wherein the polyvinyllactam used is polyvinylpyrrolidone.

5. The composition according to claim 1 wherein the polyalkylene oxides have molecular weights of from 300 to 10,000 daltons.

6. The composition according to claim 1 wherein the polyalkylene oxides are chosen from the group consisting of polyethylene glycols, polypropylene glycols, polytetrahydrofurans, polybutylene glycols and the monoalkoxylated derivatives of said polyalkylene oxides.

7. The composition according to where claim 1 wherein the polyalkylene oxides used are polyoxyethylene-polyoxypropylene block copolymers.

8. The composition according to where claim 1 wherein the coupling of the polyalkylene oxide side chains takes place via diisocyanates.

9. The composition according to claim 1 wherein the polyalkylene oxides are functionalized by reaction with a diisocyanate prior to the reaction with the vinyllactam copolymer.

10. The composition according to claim 1, wherein the polyalkylene oxides are used in equimolar amounts, based on the hydroxyl groups of the vinyllactam copolymer.

11. The composition according to claim 1 wherein the diisocyanate used is isophorone diisocyanate.

12. The composition according to claim 1, wherein the polyvinyllactam-polyalkylene oxide block copolymers have an A-B, A-B-A or B-A-B structure.

13. The composition according to claim 1, wherein the copolymers have molecular weights M_w of from 700 to 20,000 g/mol.

14. The composition according to claim 1, wherein the substances which are sparingly soluble in water are biologically active substances.

21. A preparation of substances which are sparingly soluble in water, obtainable using polyvinyllactam-polyalkylene oxide block copolymers as solubilizers according to claim 1.

25. The preparation according to claim 21, comprising a cosmetic active ingredient as a biologically active substance which is sparingly soluble in water.

26. The preparation according to claim 21, comprising an agrochemical active ingredient as a biologically active substance which is sparingly soluble in water.

27. The preparation according to claim 21, comprising a food supplement or a dietetic active ingredient as a biologically active substance which is sparingly soluble in water.

28. The preparation according to claim 21, comprising a dye as a substance which is sparingly soluble in water.

29. A pharmaceutical preparation for the treatment of illnesses comprising the composition according to claim 1.

30. A cosmetic preparation comprising the composition according to claim 1.

31. An agrochemical preparation comprising the composition according to claim 1.

32. A food supplement or dietetic agent comprising the composition according to claim 1.

33. A food comprising the composition according to claim 1.

34. A dye preparation comprising the composition according to claim 1.

15-20. -20. (canceled)

22. The preparation according to claim 22, comprising a biologically active substance as a substance which is sparingly soluble in water.

23. The preparation according to claim 22, comprising a pharmaceutical active ingredient as a biologically active substance which is sparingly soluble in water.

24. The preparation according to claim 23 in the form of orally applicable administration forms.