Radiolabeled tumor imaging agent and method of preparation

Claim 1

A method of labeling porphyrin compounds, analogs, derivatives and substances containing porphyrin with the radionuclide of indium at physiologic pH 7-8 condition which comprises the sequential steps of: (a) reacting an acidic solution of radioactive trichloride of indium with a water soluble sodium salt; (b) raising the pH of the admixture of step (a) to 7.4 with a solution of dilute alkali; (c) adding to the neutralized solution of step (b) 0.5-10 ml of an aqueous solution of a porphyrin compound desired to be labeled; (d) heating the admixture of step (c) at 110°-120° C. for 15 minutes and allowing it to cool to room temperature for 10-30 minutes.

Claim 2

A method of labeling porphyrin compounds, analogs, derivatives and substances containing porphyrin with the radionuclide of indium at physiologic pH 7-8 condition which comprises the sequential steps of: (a) reacting an acidic solution of radioactive trichloride of indium with a water soluble sodium salt; (b) raising the pH of the admixture of step (a) to 7.4 with a solution of dilute alkali; (c) adding to the neutralized solution of step (b) 0.5-10 ml of an aqueous solution of a porphyrin compound desired to be labeled; (d) heating the admixture of step (c) at 110°-120° C. for 15 minutes and allowing it to cool to room temperature for 10-30 minutes.

Claim 14

A method of labeling hematoporphyrin derivative (HPD) with 111 In at physiologic pH 7-8 condition based on the bicarbonate reaction with 111 InCl 3 producing a diagnostic composition suitable for radiologic imaging of neoplasms in man or in animal comprising the sequential steps of: (a) converting 111 InCl 3 to 111 In-bicarbonate by neutralizing 0.5-5 ml(1-10 mCi) 111 InCl 3 solution to pH 7.4 with a sufficient amount of a 7.5% sodium bicarbonate solution and mixing the admixture for 1-5 minutes; (b) adding 0.5-1 ml(5-10 mg) HPD solution to the neutralized radioactive solution of step (a) and mixing it for 1-5 minutes; (c) heating the radioactive admixture of step (b) at 110°-120° C. for 15 minutes and allowing it to cool to room temperature for 10-30 minutes.

Claim 15

A method of labeling hematoporphyrin derivative (HPD) with 111 In at physiologic pH 7-8 condition based on the bicarbonate reaction with 111 InCl 3 producing a diagnostic composition suitable for radiologic imaging of neoplasms in man or in animal comprising the sequential steps of: (a) converting 111 InCl 3 to 111 In-bicarbonate by neutralizing 0.5-5 ml(1-10 mCi) 111 InCl 3 solution to pH 7.4 with a sufficient amount of a 7.5% sodium bicarbonate solution and mixing the admixture for 1-5 minutes; (b) adding 0.5-1 ml(5-10 mg) HPD solution to the neutralized radioactive solution of step (a) and mixing it for 1-5 minutes; (c) heating the radioactive admixture of step (b) at 110°-120° C. for 15 minutes and allowing it to cool to room temperature for 10-30 minutes.

Claim 16

A method of labeling HPD with 111 In at physiologic pH 7-8 condition based on the citrate or acetate reaction with 111 InCl 3 producing a diagnostic composition suitable for radiologic imaging of neoplasms in man or in animal comprising the sequential steps of: (a) reacting 0.5-5 ml(1-10 mCi) 111 InCl 3 solution with 1-2 ml of an aqueous solution of either 5% sodium citrate or 5% sodium acetate to form the corresponding soluble indium salt and mixing the admixture for 1-5 minutes; (b) raising the pH of the admixture of step (a) to 7.4 with a sufficient amount of 0.1N NaOH solution; (c) adding 0.5-1 ml(5-10 mg) HPD solution to the neutralized radioactive solution of step (b) and mixing it for 1-5 minutes; (d) heating the radioactive admixture of step (c) at 110°-120° C. for 15 minutes and allowing it to cool to room temperature for 10-30 minutes.

Claim 17

A method of labeling HPD with 111 In at physiologic pH 7-8 condition based on the citrate or acetate reaction with 111 InCl 3 producing a diagnostic composition suitable for radiologic imaging of neoplasms in man or in animal comprising the sequential steps of: (a) reacting 0.5-5 ml(1-10 mCi) 111 InCl 3 solution with 1-2 ml of an aqueous solution of either 5% sodium citrate or 5% sodium acetate to form the corresponding soluble indium salt and mixing the admixture for 1-5 minutes; (b) raising the pH of the admixture of step (a) to 7.4 with a sufficient amount of 0.1N NaOH solution; (c) adding 0.5-1 ml(5-10 mg) HPD solution to the neutralized radioactive solution of step (b) and mixing it for 1-5 minutes; (d) heating the radioactive admixture of step (c) at 110°-120° C. for 15 minutes and allowing it to cool to room temperature for 10-30 minutes.

Claim 27

A method of preparing 111 In- or 113m In-labeled HPD injection at physiologic pH 7-8 condition based on the bicarbonate reaction with 111 InCl 3 or 113m InCl 3 suitable for use in radiologic imaging of neoplasms in mammal which comprises the sequential steps of: (a) reconstituting the lyophilized sodium bicarbonate reagent with 1-5 ml Water for Injection until completely dissolved; (b) injecting 0.5-50 ml(1-100 mCi) of either 111 InCl 3 or 113m InCl 3 solution into a sterile serum vial; (c) raising the pH of the radioactive indium trichloride solution to 7.4 with a sufficient amount of the reconstituted sodium bicarbonate solution and mixing the radioactive admixture for 1-5 minutes; (d) adding to the neutralized solution of step (c) 0.5-1 ml(5-10 mg) of the HPD solution slowly and mixing it for 1-5 minutes; (e) heating the contents of the reaction vial at 110°-120° C. for 15 minutes and allowing it to cool to room temperature for 10-30 minutes.

Claim 28

A method of preparing 111 In- or 113m In-labeled HPD injection at physiologic pH 7-8 condition based on the bicarbonate reaction with 111 InCl 3 or 113m InCl 3 suitable for use in radiologic imaging of neoplasms in mammal which comprises the sequential steps of: (a) reconstituting the lyophilized sodium bicarbonate reagent with 1-5 ml Water for Injection until completely dissolved; (b) injecting 0.5-50 ml(1-100 mCi) of either 111 InCl 3 or 113m InCl 3 solution into a sterile serum vial; (c) raising the pH of the radioactive indium trichloride solution to 7.4 with a sufficient amount of the reconstituted sodium bicarbonate solution and mixing the radioactive admixture for 1-5 minutes; (d) adding to the neutralized solution of step (c) 0.5-1 ml(5-10 mg) of the HPD solution slowly and mixing it for 1-5 minutes; (e) heating the contents of the reaction vial at 110°-120° C. for 15 minutes and allowing it to cool to room temperature for 10-30 minutes.

Claim 38

A method of preparing 111 In- or 113m In-labeled HPD injection at physiologic pH 7-8 condition based on the citrate or acetate reaction with 111 InCl 3 or 113m InCl 3 suitable for use in radiologic imaging of neoplasms in mammal which comprises the sequential steps of: (a) reconstituting the lyophilized sodium salt reagent(sodium citrate or sodium acetate) with 1-5 ml Water for Injection until completely dissolved; (b) reconstituting the lyophilized dilute alkali with 1-5 ml Water for Injection until completely dissolved; (c) injecting 0.5-50 ml (1-100 mCi) of either 111 InCl 3 or 113m InCl 3 solution into a sterile serum vial; (d) adding 1-2 ml of the sodium salt solution to the radioactive indium trichloride solution and mixing the admixture for 1-5 minutes; (e) raising the pH of the admixture of step (d) to 7.4 with a sufficient amount of 0.1N NaOH solution. (f) adding to the neutralized solution of step (e) 0.5-1 ml(5-10 mg) of the HPD solution slowly and mixing it for 1-5 minutes; (g) heating the contents of the reaction vial at 110°-120° C. for 15 minutes and allowing it to cool to room temperature for 10-30 minutes.

Claim 39

A method of preparing 111 In- or 113m In-labeled HPD injection at physiologic pH 7-8 condition based on the citrate or acetate reaction with 111 InCl 3 or 113m InCl 3 suitable for use in radiologic imaging of neoplasms in mammal which comprises the sequential steps of: (a) reconstituting the lyophilized sodium salt reagent(sodium citrate or sodium acetate) with 1-5 ml Water for Injection until completely dissolved; (b) reconstituting the lyophilized dilute alkali with 1-5 ml Water for Injection until completely dissolved; (c) injecting 0.5-50 ml (1-100 mCi) of either 111 InCl 3 or 113m InCl 3 solution into a sterile serum vial; (d) adding 1-2 ml of the sodium salt solution to the radioactive indium trichloride solution and mixing the admixture for 1-5 minutes; (e) raising the pH of the admixture of step (d) to 7.4 with a sufficient amount of 0.1N NaOH solution. (f) adding to the neutralized solution of step (e) 0.5-1 ml(5-10 mg) of the HPD solution slowly and mixing it for 1-5 minutes; (g) heating the contents of the reaction vial at 110°-120° C. for 15 minutes and allowing it to cool to room temperature for 10-30 minutes.