Site-specific adhesion within the GI tract using nanoparticles stabilized by high molecular weight, linear poly (ethylene oxide) polymers
AssigneeNano Systems L.L.C.
InventorsStephen B. Ruddy, W. Mark Eickhoff, Gary Liversidge
Life of this patent
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Abstract
Nanoparticulate crystalline therapeutic or diagnostic substances formulated with stabilizers and high molecular weight, linear poly(ethylene oxide) polymers, enhance contact between the crystalline therapeutic or diagnostic substances and the gastrointestinal tract providing site-specific and extended therapeutic or diagnostic effect.
Claims15
An orally/rectally administerable therapeutic or diagnostic X-ray formulation comprising:
- (A) of from about 0.1% to about 45% of an essentially water insoluble particulate radiopaque crystalline material or drug having an effective average particle size of less than about 2000 nm;
- (B) of from about 0.1 to about 10.0% w/v of a bioadhesive polymeric stabilizer selected from the group consisting of:
- (i) polyethylene-polypropylene oxide tri-block co-polymers of the formula;
- (polyethylene oxide).sub.a -(polypropylene oxide).sub.b -(polyethylene oxide).sub.c wherein
- a is 46, 52, 62, 75, 97, 98, 122, or 128;
- b is 16, 30, 35, 39, 47, 54, or 67;
- and
- c is 46, 52, 62, 75, 97, 98, 122, or 128;
- (ii) polyvinyl alcohol,
- (iii) polyvinyl pyrrolidone,
- (iv) hydroxypropyl methylcellulose, and
- (v) polyoxyethylene sorbitan mono-oleate;
- (C) of from about 0.1 to about 5.0 w/v of a long chain linear poly (ethylene oxide) polymer having a molecular weight of from about 100,000 to about 2,000,000 daltons;
- and
- (D) water to make 100% w/v.
An orally/rectally administerable gastrointestinal diagnostic X-ray formulation comprising:
- (A) of from about 0.1% to about 45% of an essentially water insoluble particulate radiopaque crystalline material having an effective average particle size of less than about 2000 nm;
- (B) of from about 0.1 to about 10.0% w/v of a bioadhesive polymeric stabilizer selected from the group consisting of:
- (i) polyethylene-polypropylene oxide tri-block co-polymers of the formula;
- (polyethylene oxide).sub.a -(polypropylene oxide).sub.b -(polyethylene oxide).sub.c wherein
- a is 46, 52, 62, 75, 97, 98, 122, or 128;
- b is 16, 30, 35, 39, 47, 54, or 67;
- and
- c is 46, 52, 62, 75, 97, 98, 122, or 128;
- (ii) polyvinyl alcohol,
- (iii) polyvinyl pyrrolidone,
- (iv) hydroxypropyl methylcellulose, and
- (v) polyoxyethylene sorbitan mono-oleate;
- (C) of from about 0.1 to about 5.0 w/v of a long chain linear poly (ethylene oxide) polymer having a molecular weight of from about 100,000 to about 2,000,000 daltons;
- and
- (D) water to make 100% w/v.
A method of carrying out X-ray examination of the gastrointestinal tract of a patient, the method comprising orally/rectally administering to the patient an X-ray contrast composition comprising:
- (A) of from about 0.1% to about 45% of an essentially water insoluble particulate radiopaque crystalline material having an effective average particle size of less than about 2000 nm;
- (B) of from about 0.1 to about 10.0% w/v of a bioadhesive polymeric stabilizer selected from the group consisting of:
- (i) polyethylene-polypropylene oxide tri-block co-polymers of the formula;
- (polyethylene oxide).sub.a -(polypropylene oxide).sub.b -(polyethylene oxide).sub.c wherein
- a is 46, 52, 62, 75, 97, 98, 122, or 128;
- b is 16, 30, 35, 39, 47, 54, or 67;
- and
- c is 46, 52, 62, 75, 97, 98, 122, or 128;
- (ii) polyvinyl alcohol,
- (iii) polyvinyl pyrrolidone,
- (iv) hydroxypropyl methylcellulose, and
- (v) polyoxyethylene sorbitan mono-oleate;
- (C) of from about 0.1 to about 5.0 w/v of a long chain linear poly (ethylene oxide) polymer having a molecular weight of from about 100,000 to about 2,000,000 daltons;
- and
- (D) water to make 100% w/v.
Dependencies are inferred from the claim text.