Medicine with imaging and metastatic bone tumor treatment functions as well as preparation method and application of medicine

A bone tumor and metastatic technology, applied in the field of nuclear medicine, can solve the problem of low action intensity, and achieve the effects of short reaction time, simple method and scientific design

Inactive Publication Date: 2021-04-06
THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as the first generation of nitrogen-free bisphosphonates, HEDP’s action strength is significantly lower than that of the second and third generation of nitrogen-containing bisphosphonates, such as alendronic acid and ibandronic acid.

Method used

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  • Medicine with imaging and metastatic bone tumor treatment functions as well as preparation method and application of medicine
  • Medicine with imaging and metastatic bone tumor treatment functions as well as preparation method and application of medicine
  • Medicine with imaging and metastatic bone tumor treatment functions as well as preparation method and application of medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Present embodiment 1 has investigated the consumption of stannous chloride among the present invention, specifically:

[0028] Take 15 EP tubes, add ibandronic acid (30mg / ml) 1.2mg, ascorbic acid (50mg / ml) 0.3mg to each tube in turn, and then add stannous chloride solution (0.1 molar hydrochloric acid to prepare 6mg / ml) 0.02mg, 0.04mg, 0.06mg, 0.08mg, 0.10mg, 0.12mg, 0.14mg, 0.16mg, 0.18mg, 0.20mg, 0.24mg, 0.28mg, 0.32mg, 0.36mg, 0.40mg, then add Potassium perrhenate (0.2mg / ml) 0.005mg, freshly rinsed Na 188 ReO 4 The eluent (370MBq / ml) is 37MBq, adjust the pH value to about 2 with 1 mole of sodium acetate solution and 1 mole of hydrochloric acid, shake and mix well, react in a metal bath at 95°C for 30min, after the reaction is completed and cool to room temperature, The pH value of the tube is adjusted to 6-7, and a 0.22 μm filter membrane is used for sterilization and filtration. Then it was determined by thin layer paper chromatography (TLC) 188 The radiochemic...

Embodiment 2

[0033] The present embodiment investigates the pH value among the present invention, specifically:

[0034] Take 12 EP tubes, add 1.2 mg of ibandronic acid (30 mg / ml), 0.3 mg of ascorbic acid (50 mg / ml), 0.14 mg of stannous chloride (6 mg / ml with 0.1 mole of hydrochloric acid) to each tube in turn, Potassium perrhenate (0.2mg / ml) 0.005mg, freshly rinsed Na 188 ReO 4Eluate (370MBq / ml) 37MBq, adjust the pH value to 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9 with 1 mole of sodium acetate solution and 1 mole of hydrochloric acid , shake and mix well, and react in a metal bath at 95°C for 30 minutes. After the reaction is completed and cooled to room temperature, adjust the pH value of each tube to 6-7, and use a 0.22 μm filter membrane to sterilize and filter. Then it was determined by thin layer paper chromatography (TLC) 188 The radiochemical purity of Re-ibandronic acid, the results are shown in Table 2:

[0035] Table 2 The results of radiochemical purity under different pH ...

Embodiment 3

[0040] The present embodiment investigates the dosage of ibandronic acid in the present invention, specifically:

[0041] Take 15 EP tubes, add ibandronic acid (30mg / ml) 0.2mg, 0.4mg, 0.6mg, 0.8mg, 1.0mg, 1.2mg, 1.4mg, 1.6mg, 1.8mg, 2.0mg, 2.4 mg, 2.8mg, 3.2mg, 3.6mg, 4.0mg, then add ascorbic acid (50mg / ml) 0.3mg, stannous chloride (0.1 molar hydrochloric acid to 6mg / ml) 0.14mg, potassium perrhenate (0.2mg / ml) 0.005mg, freshly rinsed Na 188 ReO 4 The eluent (370MBq / ml) is 37MBq, adjust the pH value to about 2 with 1 mole of sodium acetate solution and 1 mole of hydrochloric acid, shake and mix well, react at 95°C for 30min, after the reaction is completed and cool to room temperature, adjust each tube The pH value is 6-7, and a 0.22 μm filter membrane is used for sterilization and filtration. Then it was determined by thin layer paper chromatography (TLC) 188 The radiochemical purity of Re-ibandronic acid, the results are shown in Table 3 below:

[0042] Table 3 The resul...

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Abstract

The invention discloses a medicine with imaging and metastatic bone tumor treatment functions as well as a preparation method and application of the medicine and belongs to the technical field of nuclear medicine. The medicine disclosed by the invention is ibandronic acid marked by 188Re, namely 188Re-ibandronic acid. The preparation method comprises the following steps of: uniformly mixing an ibandronate solution, an antioxidant solution, a reducing agent solution, an auxiliary agent solution and a Na188ReO4 solution, adjusting the pH value, carrying out a reaction, adjusting the pH value, and performing sterilizing and filtering. The 188Re-ibandronic acid is high in water solubility, good in in-vitro stability at room temperature and high in plasma protein binding rate, and shows high and long-time bone uptake in in-vivo distribution in mice and development of New Zealand rabbits; and pharmacodynamic tests show that the curative effect of the 188Re-ibandronic acid is higher than that of Na188ReO4 or ibandronic acid in corresponding groups. The 188Re-ibandronic acid is an excellent bone imaging agent and a metastatic bone tumor therapeutic radiopharmaceutical.

Description

technical field [0001] The invention belongs to the technical field of nuclear medicine, and in particular relates to a drug capable of imaging and treating metastatic bone tumors, its preparation method and application. Background technique [0002] Bone is a predilection site for distant metastasis of malignant tumors, and its incidence rate is second only to lung and liver. Early diagnosis and treatment of metastatic bone tumors can effectively improve the prognosis and quality of life of patients. [0003] Current treatments for metastatic bone tumors mainly include radiotherapy, chemotherapy, radionuclide therapy, bisphosphonate therapy, analgesic therapy, and palliative surgery. Targeted radionuclide therapy for metastatic bone tumors can significantly relieve bone pain and at the same time kill tumor cells with less toxic and side effects. It is a safe and effective treatment. Currently, radiopharmaceuticals commonly used in the treatment of metastatic bone tumors i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/00A61K31/663A61K9/08A61P35/04A61K103/10
CPCA61K51/00A61K31/663A61K9/08A61P35/04A61K2300/00
Inventor 陈跃徐婷婷王映伟刘汉香陈赞杨松松赵岩刘光富刘林彭登赛
Owner THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV
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