Controlled Release Delivery System for Bio-Active Agents

• US 20070275068A1
• Filed: 09/09/2005
• Published: 11/29/2007
• Est. Priority Date: 09/09/2004
• Status: Active Grant

• Current Assignee: KU Leuven Research & Development
• Original Assignee: KU Leuven Research & Development
• Inventors: Martens, Johan, Van Den Mooter, Guy, Van Humbeeck, Jan, Mellaerts, Randy, Aerts, Caroline
• Granted Patent: US 8,790,697 B2
• Time in Patent Office: Days
• US Class Current: 424/484
• CPC Class Codes: A61K 9/1611 Inorganic compounds
• CPC Class Codes: C01B 33/18 Preparation of finely divided silica neither in sol nor in gel form; After-treatment thereof preparation of aerogels by dehydrating gels C01B33/158; treatment to enhance the pigmenting or filling properties C09C

Abstract

The invention provides a controlled release delivery system comprising a bio-active compound and a matrix carrier, wherein said matrix carrier is an amorphous microporous non-fibrous silicon or titanium oxide being loaded with said bio-active compound and wherein the micropores of said matrix carrier have a mean size in the range of 0.4 to 2.0 nm.

Claims

1. A controlled release delivery system comprising a bio-active compound and a matrix carrier, wherein said matrix carrier is an amorphous microporous non-fibrous silicon or titanium oxide being loaded with said bio-active compound and wherein the micropores of said matrix carrier have a mean size in the range of 0.4 to 2.0 nm.

27. A controlled release delivery system according to claim 1, wherein at least 50% of said bio-active compound is molecularly dispersed in the pores of said matrix carrier.

28. Controlled release delivery system according to claim 1, wherein said bio-active compound amounts to 1 to 30% by weight of the delivery system.

29. A controlled release delivery system according to claim 1, wherein at least 50% of said bio-active compound is molecularly dispersed in the pores of said matrix carrier, and wherein said bio-active compound amounts to 1 to 30% by weight of the delivery system.

30. A controlled release delivery system according to claim 1, wherein an 80% release of said bio-active compound into an aqueous fluid at a pH between 1.0 and 8.0 is not obtained before a period of time ranging from 30 minutes to about 150 hours.

31. A controlled release delivery system according to claim 1, wherein said delivery system is for oral administration and wherein an 80% release of said bio-active compound in an aqueous fluid at a pH between 1.0 and 8.0 is not obtained before a period of time ranging from 2 hours to 12 hours.

32. A controlled release delivery system according to claim 1, wherein said amorphous microporous non-fibrous oxide is a non-erodible amorphous microporous silica or titania.

33. A controlled release delivery system according to claim 1, wherein at least 50% of said bio-active compound is molecularly dispersed in the pores of said matrix carrier, and wherein said amorphous microporous non-fibrous oxide is a non-erodible amorphous microporous silica or titania.

34. A controlled release delivery system according to claim 1, wherein said bio-active compound amounts to 1 to 30% by weight of the delivery system, and wherein said amorphous microporous non-fibrous oxide is a non-erodible amorphous microporous silica or titania

35. A controlled release delivery system according to claim 1, wherein it comprises the matrix carrier in a nano-particulate form or in a micro-particulate form.

36. A controlled release delivery system according to claim 1, characterised in that the matrix carrier has a monomodal micropore size distribution.

37. A controlled release delivery system according to claim 1, wherein the molecular size of the active compound is not higher than the mean size of the micropores of said matrix carrier.

38. A controlled release delivery system according to claim 1, wherein the matrix carrier has a micropore volume of at least 0.01 ml/g and at most 0.52 ml/g.

39. A controlled release delivery system according to claim 1, wherein the matrix carrier has a BET surface area of at least 25 m²/g and at most 1,000 m²/g.

40. A controlled release delivery system according to claim 1, being prepared by first synthesising said amorphous micro-porous non-fibrous oxide matrix carrier having micropores with a mean size in the range of 0.4 to 2.0 nm, said synthesis optionally comprising a calcination step, and then loading said bioactive agent into said matrix carrier.

41. A controlled release delivery system according to claim 1, being in the form of a tablet or capsule for oral administration.

42. A controlled release delivery system according to claim 1, being in the form of a transdermal patch, wound dressing or cosmetic cream for topical administration.

2-26. -26. (canceled)

43. A method of administration of at least one bio-active agent to a mammal, comprising the administration of a controlled release delivery system comprising said bio-active agent and a matrix carrier, wherein said matrix carrier is an amorphous microporous non-fibrous silicon or titanium oxide being loaded with said bio-active agent and wherein the micropores of said matrix carrier have a mean size in the range of 0.4 to 2.0 nm.

44. A method according to claim 43, wherein said administration to a mammal is a gastrointestinal administration.

45. A method according to claim 43, wherein said administration to a mammal is a topical administration.

46. A method according to claim 43, wherein said administration to a mammal is an oral administration

47. A method according to claim 43, wherein said administration to a mammal is via an implant.