Radiolabeled compositions containing a calcific matrix and their use for treatment of arthritis

Claim 2

A therapeutic radiation ablation treatment method comprising: injecting into the synovium of a patient a therapeutically effective amount of a pharmaceutical composition consisting essentially of a radionuclide sorbed to a calcific matrix, wherein the calcific matrix is particulate, the particles being spherical or irregular in form and having an average diameter of between about 1 and about 90 microns.

Claim 3

The method of claim 1 wherein the calcific matrix is hydroxyapatite.

Claim 4

The method of claim 1 wherein the patient is suffering from rheumatoid arthritis.

Claim 5

The method of claim 1 wherein the radionuclide is Sm-153, Ho-166, Lu-177, La-140, Gd-159, Yb-175, In-115m, Y-90, Sc-47, Re-186 or Re-188.

Claim 6

The method of claim 4 wherein the radionuclide is Sm-153 or Ho-166.

Claim 7

A therapeutic radiation ablation treatment method comprising: injecting into the synovium of a patient a therapeutically effective amount of a pharmaceutical composition comprising a radionuclide sorbed to a calcific matrix, wherein the calcific matrix is particulate, the particles being spherical or irregular in form and having an average diameter of between about 1 and about 90 microns and the composition further contains a layered mixed metal hydroxide of Formula I: Li.sub.m D.sub.d T(OH).sub.(m+2d+3+na) A.sub.a.sup.n (I) wherein: m is 0 to about 1 D is a divalent metal ion selected from the group consisting of magnesium, calcium, barium, strontium, manganese, iron, cobalt, nickel, copper, and zinc or a mixture thereof; d is 0 to about 4; provided that both m and d are not 0; T is a metal ion selected from the group consisting of aluminum, gallium, chromium, and iron; A is a monovalent or polyvalent ion other than a hydroxyl ion; n is the valence of the anion A; and (m+2d+3+na) is equal to or greater than 3.

Claim 8

A therapeutic radiation ablation treatment method comprising: injecting into the synovium of a patient a therapeutically effective amount of a pharmaceutical composition comprising a radionuclide sorbed to a calcific matrix, wherein the calcific matrix is particulate, the particles being spherical or irregular in form and having an average diameter of between about 1 and about 90 microns and the composition further contains a layered mixed metal hydroxide of Formula I: Li.sub.m D.sub.d T(OH).sub.(m+2d+3+na) A.sub.a.sup.n (I) wherein: m is 0 to about 1 D is a divalent metal ion selected from the group consisting of magnesium, calcium, barium, strontium, manganese, iron, cobalt, nickel, copper, and zinc or a mixture thereof; d is 0 to about 4; provided that both m and d are not 0; T is a metal ion selected from the group consisting of aluminum, gallium, chromium, and iron; A is a monovalent or polyvalent ion other than a hydroxyl ion; n is the valence of the anion A; and (m+2d+3+na) is equal to or greater than 3.

Claim 9

The method of claim 6 wherein the patient is suffering from rheumatoid arthritis.

Claim 10

The method of claim 6 wherein the calcific matrix is hydroxyapatite.

Claim 11

The method of claim 6 wherein the radionuclide is Sm-153, Ho-166, Lu-177, La-140, Gd-159, Yb-175, In-155m, Y-90, Sc-47, Re-186 or Re-188.

Claim 12

The method of claim 9 wherein the radionuclide is Sm-153 or Ho-166.

Claim 13

The method of claim 6 wherein m is in from about 0.5 to about 0.75; D is magnesium, calcium, or a mixture thereof; d is from about 1 to about 3; and T is a halide, sulfate, or phosphate.

Claim 14

The method of claim 6 wherein the layered mixed metal hydroxide has the formula: Mg.sub.x Al.sub.y (OH).sub.z A.sub.a.sup.n wherein: x is approximately 1 to approximately 3; y is approximately 1; z is approximately 3 to approximately 5; A is a halide, sulfate, phosphate, or carbonate; n is the valence of A; and a is approximately 0.1 to 1.0.

Claim 15

The method of claim 12 wherein x is 1, y is 1, z is 4.7 and a is 0.3.

Claim 16

The method of claim 12 wherein the radionuclide is Sm-153, Ho-166, Lu-177, La-140, Gd-159, Y6-175, In-115m, Y-90, Sc-47, Re-186 or Re-188.

Claim 17

The method of claim 14 wherein the radionuclide is Sm-153 or Ho-166.

Claim 18

A therapeutic radiation ablation treatment method comprising: injecting into the synovium of a patient a therapeutically effective amount of a pharmaceutical composition consisting essentially of a chelate sorbed to a calcific matrix, wherein the chelate is a radionuclide complexed with a chelating agent wherein the calcific matrix is particulate, the particles being spherical or irregular in form and having an average diameter of between about 1 and about 90 microns.

Claim 19

A therapeutic radiation ablation treatment method comprising: injecting into the synovium of a patient a therapeutically effective amount of a pharmaceutical composition consisting essentially of a chelate sorbed to a calcific matrix, wherein the chelate is a radionuclide complexed with a chelating agent wherein the calcific matrix is particulate, the particles being spherical or irregular in form and having an average diameter of between about 1 and about 90 microns.

Claim 20

The method of claim 16 wherein the patient is suffering from rheumatoid arthritis.

Claim 21

The method of claim 16 wherein the calcific matrix is hydroxyapatite.

Claim 22

The method of claim 16 wherein the radionuclide is Sm-153, Ho-166, Lu-177, La-140, Gd-159, Y6-175, In-115m, Y-90, Sc-47, Re-186 or Re-188.

Claim 23

The method of claim 19 wherein the radionuclide is Sm-153 or Ho-166.

Claim 24

The method of claim 16 wherein the chelating agent is a polyaminophosphonate.

Claim 25

The method of claim 21 wherein the chelating agent is 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylenephosphonic acid or ethylenediaminetetramethylenephosphonic acid.

Claim 26

The method of claim 21 wherein the radionuclide is Ho-166 or Sm-153.

Claim 27

The method of claim 16 wherein the chelating agent is a diphosphonate.

Claim 28

The method of claim 24 wherein the chelating agent is methylenediphosphonic acid, hydroxyethanediphosphonic acid or hydroxymethylenediphosphonic acid.

Claim 29

The method of claim 24 wherein the radionuclide is Re-186 or Re-188.

Claim 30

The method of claim 16 wherein the composition further contains a layered mixed metal hydroxide of Formula I: Li.sub.m D.sub.d T(OH).sub.(m+2d+3+na) A.sub.a.sup.n (I) wherein: m is 0 to about 1; D is a divalent metal ion selected from the group consisting of magnesium, calcium, barium, strontium, manganese, iron, cobalt, nickel, copper, and zinc or a mixture thereof; d is 0 to about 4; provided that both m and d are not 0; T is a metal ion selected from the group consisting of aluminum, gallium, chromium, and iron; A is a monovalent or polyvalent ion other than a hydroxyl ion; n is the valence of the anion A; a is the number of anions A in the formula; and (m+2d+3+na) is equal to or greater than 3.

Claim 31

The method of claim 27 wherein the patient is suffering from rheumatoid arthritis.

Claim 32

The method of claim 27 wherein m is in from about 0.5 to about 0.75; D is magnesium, calcium, or a mixture thereof; d is from about 1 to about 3; and T is a halide, sulfate, or phosphate.

Claim 33

The method of claim 27 wherein the radionuclide is Sm-153, Ho-166, Lu-177, La-140, Gd-159, Y6-175, In-115m, Y-90, Sc-47, Re-186 or Re-188.

Claim 34

The method of claim 27 wherein the chelating agent is a polyaminophosphonate.

Claim 35

The method of claim 31 wherein the polyaminophosphonate is 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylenephosphonic acid or ethylenediaminetetramethylenephosphonic acid.

Claim 36

The method of claim 31 wherein the radionuclide is Ho-166 or Sm-153.

Claim 37

The method of claim 27 wherein the chelating agent is a diphosphonate.

Claim 38

The method of claim 34 wherein the chelating agent is methylenediphosphonic acid, hydroxyethanediphosphonic acid or hydroxymethylenediphosphonic acid.

Claim 39

The method of claim 35 wherein the radionuclide is Re-186 or Re-188.

Claim 40

The method of claim 27 wherein the layered mixed metal hydroxide has the formula: Mg.sub.x Al.sub.y (OH).sub.z A.sub.a.sup.n wherein: x is approximately 1 to approximately 3; y is approximately 1; z is approximately 3 to approximately 5; A is a halide, sulfate, phosphate, or carbonate; n is the valence of A; and a is approximately 0.1 to 1.0.

Claim 41

The method of claim 37 wherein x is 1, y is 1, z is 4.7 and a is 0.3.

Claim 42

The method of claim 38 wherein the radionuclide is Sm-153, Ho-166, Lu-177, La-140, Gd-159, Y6-175, In-115m, Y-90, Sc-47, Re-186, or Re-188.

Claim 43

The method of claim 39 wherein the radionuclide is Sm-153 or Ho-166.

Claim 44

The method of claim 37 wherein the chelating agent is a polyaminophosphonate.

Claim 45

The method of claim 41 wherein the polyaminophosphonate is 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylenephosphonic acid or ethylenediaminetetramethylenephosphonic acid.

Claim 46

The method of claim 42 wherein the radionuclide is Ho-166 or Sm-153.

Claim 47

The method of claim 37 wherein the chelating agent is a diphosphonate.

Claim 48

The method of claim 44 wherein the chelating agent is methylenediphosphonic acid, hydroxyethanediphosphonic acid or hydroxymethylenediphosphonic acid.

Claim 49

The method of claim 45 wherein the radionuclide is Re-186 or Re-188.