Brookhaven Science Associates, Lcc

The United States of America As Represented by the United States

The State University of New York

George E Meinken

Suresh C Srivastava

Leonard F Mausner

Powell Richards

Harold L Atkins

Radoslav R Adzic

Barry S Coller

Gilbert R Gonzales

Zizhong Li

Methods for preparing an implant coated with a conversion electron emitting source (CEES) are disclosed. The typical method includes cleaning the surface of the implant; placing the implant in an activating solution comprising hydrochloric acid to activate the surface; reducing the surface by Hevolution in HSOsolution; and placing the implant in an electroplating solution that includes ions of the CEES, HCl, HSO, and resorcinol, gelatin, or a combination thereof. Alternatively, before tin plating, a seed layer is formed on the surface. The electroplated CEES coating can be further protected and stabilized by annealing in a heated oven, by passivation, or by being covered with a protective film. The invention also relates to a holding device for holding an implant, wherein the device selectively prevents electrodeposition on the portions of the implant contacting the device.

Method of electroplating a conversion electron emitting source on implant

Novel methods are provided for the manufacture of Sn(Sn ) DTPA. The method allows the use of DTPA, a toxic chelating agent, in an approximately 1:1 ratio to Sn(Sn ) via either aqueous conditions, or using various organic solvents, such as methylene chloride. A pharmaceutical composition manufactured by the novel method is also provided, as well as methods for treatment of bone tumors and pain associated with bone cancer using the pharmaceutical composition of the invention.

Process for the manufacture of 117Sn diethylenetriaminepentaacetic acids

The invention provides a method for the palliation of bone pain due to cancer by the administration of a unique dosage of a tin-117m (Sn-117m) stannic chelate complex in a pharmaceutically acceptable composition. In addition, the invention provides a method for simultaneous palliation of bone pain and radiotherapy in cancer patients using compositions containing Sn-117m chelates. The invention also provides a method for palliating bone pain in cancer patients using Sn-117m-containing compositions and monitoring patient status by imaging the distribution of the Sn-117m in the patients. Also provided are pharmaceutically acceptable compositions containing Sn-117m chelate complexes for the palliation of bone pain in cancer patients.

Therapeutic tin-117m compositions

Radiopharmaceutical compositions including Sn labeled stannic (Sn ) chelates are provided. The chelates are preferably polyhydroxycarboxylate, such as oxalates, tartrates, citrates, malonates, gluconates, glucoheptonates and the like. Methods of making Sn-labeled (Sn ) polyhydroxycarboxylic chelates are also provided. The foregoing pharmaceutical compositions can be used in methods of preparing bone for scintigraphical analysis, for radiopharmaceutical skeletal imaging, treatment of pain resulting from metastatic bone involvement, treatment of primary bone cancer, treatment of cancer resulting from metastatic spread to bone from other primary cancers, treatment of pain resulting from rheumatoid arthritis, treatment of bone/joint disorders and to monitor radioactively the skeletal system.

Radiopharmaceutical compositions

Radiopharmaceutical compositions including,Sn labeled stannic (Sn,) chelates are provided. The chelates are preferably polyhydroxycarboxylate, such as oxalates, tartrates, citrates, malonates, gluconates, glucoheptonates and the like. Methods of making,Sn-labeled (Sn,) polyhydroxycarboxylic chelates are also provided. The foregoing pharmaceutical compositions can be used in methods of preparing bone for scintigraphical analysis, for radiopharmaceutical skeletal imaging, treatment of pain resulting from metastatic bone involvement, treatment of primary bone cancer, treatment of cancer resulting from metastatic spread to bone from other primary cancers, treatment of pain resulting from rheumatoid arthritis, treatment of bone/joint disorders and to monitor radioactively the skeletal system.

Radiopharmaceutical stannic Sn-117m chelate compositions and methods of use

The invention provides improved formulations of .sup.117m Sn (Sn.sup.4+) DTPA which allow higher doses of .sup.117m Sn (Sn.sup.4+) to be administered than were previously possible. Methods for making pharmaceutical compositions comprising .sup.117m Sn (Sn.sup.4+) DTPA in which the amount of unchelated DTPA is minimized are disclosed along with methods of using the improved formlulations, both for palliation of bone pain associated with cancer and for treatment of osseous tumors.

Formulation for Tin-.sup.117m /diethylenetriaminepentaacetic acids

Method for palliation of pain in human bone cancer using therapeutic

There is provided a radiolabeled monoclonal antibody of the class IgG.sub.1 which reacts readily with both normal human and dog blood platelets while failing to react with thrombasthenic human platelets. This antibody has the property of completely blocking interaction of fibrinogen with platelets induced by ADP, and the ability to detect fresh thrombi in vivo.

Radiolabeled antiplatelet monoclonal antibody for imaging in-vivo thrombi

A radiopharmaceutical composition comprising a radioactive isotope of lead (Pb-203) in combination with a pharmaceutical or an antibody or antibody fragment and a bifunctional chelating agent. These compositions are especially useful in the imaging and diagnosis of tumors and tumor metastases.

Lead-203 as a label for radioimaging

The radiopharmaceutical reagents of this invention and the class of Tin-117m radiopharmaceuticals are therapeutic and diagnostic agents that incorporate gamma-emitting nuclides that localize in bone after intravenous injection in mammals (mice, rats, dogs, and rabbits). Images reflecting bone structure or function can then be obtained by a scintillation camera that detects the distribution of ionizing radiation emitted by the radioactive agent. Tin-117m-labeled chelates of stannic tin localize almost exclusively in cortical bone. Upon intravenous injection of the reagent, the preferred chelates are phosphonate compounds, preferable, PYP, MDP, EHDP, and DTPA. This class of reagents is therapeutically and diagnostically useful in skeletal scintigraphy and for the radiotherapy of bone tumors and other disorders.

Tin-117m-labeled stannic (Sn.sup.4+) chelates

A novel Ruthenium-transferrin complex, prepared by reacting iron-free human transferrin dissolved in a sodium acetate solution at pH 7 with ruthenium by heating at about 40.degree. C. for about 2 hours, and purifying said complex by means of gel chromotography with pH 7 sodium acetate as eluent. The mono- or di-metal complex produced can be used in nuclear medicine in the diagnosis and/or treatment of tumors and abscesses. Comparative results with Ga-67-citrate, which is the most widely used tumor-localizing agent in nuclear medicine, indicate increased sensitivity of detection and greater tumor uptake with the Ru-transferrin complex.

Growing community of inventors

Middle Island, NY, United States of America

George E Meinken