TREA

Oral DTPA for radionuclide chelation

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Information

  • Patent Application
  • 20070196273
  • Publication Number
    20070196273
  • Date Filed
    February 14, 2007
    17 years ago
  • Date Published
    August 23, 2007
    17 years ago
Information
Abstract
A composition for oral radionuclide chelation therapy comprises a DTPA chelate selected from Zn-DTPA and Ca-DTPA and a permeation enhancer that preferentially increases jejunal uptake of the DTPA chelate. The composition has a DTPA chelate bioavailability of at least 10% of the chelate when orally administered to a mammal.
Description
Claims
  • 1. A composition for oral radionuclide chelation therapy, said composition comprising: a DTPA (diethylenetriaminepentaacetate) chelate selected from the group consisting of calcium-DTPA (Ca-DTPA) and zinc-DTPA (Zn-DTPA); anda permeation enhancer that preferentially increases jejunal uptake of the DTPA chelate, wherein the composition has a DTPA chelate bioavailability of at least 10% when orally administered to a mammal.
  • 2. The composition of claim 1 wherein the intestinal permeation enhancer is selected from the group consisting of medium-chain glycerides, macrogolglycerides, polyglycols, and mixtures thereof.
  • 3. The composition of claim 1 wherein the intestinal permeation enhancer comprises less than 40 wt % of the composition.
  • 4. The composition of claim 1 wherein the intestinal permeation enhancer is caprylocaproyl macrogol-8-glycerides.
  • 5. The composition of claim 1 wherein the DTPA chelate comprises at least 20% by weight of the composition.
  • 6. The composition of claim 1 in an enteric-coated unit dosage form.
  • 7. The composition of claim 1 further comprising a P glycoprotein (Pgp) inhibitor.
  • 8. The composition of claim 1 in the form of extruded beads contained within a capsule.
  • 9. The composition of claim 1 in the form of extruded beads contained within a capsule, wherein the beads have an average diameter between 0.1-1 mm.
  • 10. The composition of claim 1 in a thixotropic form contained within a capsule.
  • 11. The composition of claim 1 wherein the DTPA chelate bioavailability is at least 20%.
  • 12. The composition of claim 1 in a unit dosage form comprising at least 250 mg of the DTPA chelate.
  • 13. The composition of claim 1 in a unit dosage form comprising at least 250 mg of the DTPA chelate, wherein the DTPA chelate bioavailability is at least 25%.
  • 14. A method for chelating radionuclides in a mammal, the method comprising: administering to the mammal the composition of claim 1.
  • 15. The method of claim 14 wherein the intestinal permeation enhancer is selected from medium-chain glycerides, macrogolglycerides, polyglycols, and mixtures thereof.
  • 16. The method of claim 14 wherein the DTPA chelate comprises at least 20% by weight of the composition.
  • 17. The method of claim 14 wherein the composition is in an enteric-coated unit dosage form.
  • 18. The method of claim 14 wherein prior to the administering step, the mammal is administered a Pgp inhibitor.
  • 19. A kit comprising the composition of claim 1.
  • 20. The kit of claim 17 further comprising a Pgp inhibitor.
Provisional Applications (1)
Number Date Country
60774935 Feb 2006 US