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Application of Cyclodextrin in the Preparation of Radioactive Iodine Labeled Hypericum Drug Preparations

The technology of a pharmaceutical preparation and radioactive iodine is applied in the application field of cyclodextrin in the preparation of radioactive iodine-labeled hypericum drug preparations, and can solve the problems of not obtaining and the like, and achieve low cost, high preparation efficiency and fast blood removal. Effect

Inactive Publication Date: 2021-02-12
南京成至诚医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent CN201310111593.4 uses cholate to solubilize radioactive iodine-labeled Hypericum drugs, but cholate is used as an adjuvant drug for intravenous injection and has not yet obtained relevant adjuvant approval documents

Method used

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  • Application of Cyclodextrin in the Preparation of Radioactive Iodine Labeled Hypericum Drug Preparations
  • Application of Cyclodextrin in the Preparation of Radioactive Iodine Labeled Hypericum Drug Preparations
  • Application of Cyclodextrin in the Preparation of Radioactive Iodine Labeled Hypericum Drug Preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Traditional formulations (DMSO- 131 I-Hyp is diluted with equal proportions of PEG and propylene glycol) Drug preparation:

[0031] First, weigh 0.01-13mg of Hyp (1 mg is the best), and add 1 mL of DMSO in proportion to obtain 0.01-13 mg / mL DMSO-Hyp solution drug (1 mg / mL is the best). Apply the catalyst Iodogen to the 1.5mL EP tube in advance (the best ratio is 3-10ug Iodogen:1mCi Na 131 1), add about 1mL of DMSO-Hyp solution, then add about 1-100μL of Na 131 I solution (the specific activity is 20-1000mCi / mL, the half-life of the isotope from production to use is not more than 1, and the best treatment is 100μL), vortex and mix continuously and check the labeling rate until the labeling rate reaches more than 98%. Dilute with 1mL PEG and 1mL propylene glycol to obtain DMSO- 131 PEG, Propylene Glycol Diluent of I-Hyp.

[0032] Improved formulation 1 (cyclodextrin- 131 I-Hyp solution) drug preparation:

[0033] First weigh 0.01-1mg of Hyp, add 1mL of 50% mass volu...

Embodiment 2

[0037] Comparison experiment of labeling rate between traditional preparation and improved preparation

[0038] The traditional preparation, improved preparation 1, and improved preparation 2 described in Example 1 were compared for labeling rate within 7 days; Solution to cyclodextrin-saturated Hyp solution, 0.01-10mg / mL DMSO-Hyp solution by adding Na 131 I solution, after mixing for a period of time under the catalyst lodogen, adopt thin-layer chromatography (Thin-layer chromatography, TLC), coordinate gamma counter to detect the concentration of solution 131 I mark rate.

[0039] Then add 0.01-13mg / mL DMSO- 131 I-Hyp solution was diluted with equal volume of PEG and propylene glycol to obtain traditional preparations; 0.01-10mg / mL DMSO- 131 I-Hyp is diluted with at least 15 times of 50% mass volume fraction of hydroxypropyl-β-cyclodextrin solution to obtain improved formulation 2, and with improved formulation 1 (cyclodextrin- 131 I-Hyp solution) for stability testing o...

Embodiment 3

[0042] Traditional preparation and improved preparation 1, improved preparation 2 used in rat experiments 131 I-Hyp biodistribution and necrosis targeting comparison experiment

[0043] Model building:

[0044] Male SD rats (250-300 g) began to take 0.5% KI solution instead of drinking water 24 hours before operation to block the thyroid uptake of free iodine. On the day of the operation, a laparotomy was performed under anesthesia for necrosis and reperfusion of the right liver lobe. Within 24 hours, an MRI scan was performed to detect whether there was local necrosis of the liver.

[0045] Selected 18 hepatic necrosis-reperfusion model rats and randomly divided them into 3 groups, 6 rats per group.

[0046] Prepare traditional preparation, improved preparation 1, and improved preparation 2 according to the best (optimum) concentration of embodiment 1, and inject about various preparations (Hyp dosage is 0.1mg / Kg) about 100 μ Ci respectively in penis vein, before putting to...

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Abstract

The invention belongs to the field of pharmaceutical preparations, in particular to the application of cyclodextrin in the preparation of radioactive iodine-labeled hypericum drug preparations. For the first time, cyclodextrin is applied to the preparation of "radioactive iodine-labeled hypericum drug" preparations. Dextrin is an oligocyclic compound of glucose, which is basically non-toxic to the human body. Hydroxypropyl-β-cyclodextrin is an excipient approved for intravenous injection in China. At the same time, compared with other solvents, it can ensure the efficiency of iodine labeling Under the premise, the water solubility of hypericin can be greatly mentioned, and the blood clearance of radioactive iodine-labeled hypericum drugs dissolved in cyclodextrin is fast, and there is no difference in necrosis targeting compared with traditional preparations, so cyclodextrin As a substitute for DMSO, it can be applied to radioactive iodine-labeled hypericum drug preparations; the method for preparing iodine-labeled hypericum drug preparations has simple process, low cost and high preparation efficiency, and is suitable for industrial operation.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to the application of cyclodextrin in the preparation of radioactive iodine-labeled hypericum drug preparations. Background technique [0002] Hypericin (hypericin, abbreviated as Hyp) is an active ingredient extracted from Hypericum perforatum. Herpes virus, varicella virus, influenza and other viral infections have a therapeutic effect. In addition, studies have shown that hypericin has no genotoxicity and systemic toxicity to the human body, and is an antitumor drug with less toxic and side effects. Hypericin has affinity for necrosis, and 80% of solid tumors have spontaneous necrosis inside, so it can be 131 I mark hypericin ( 131 I-Hyp) for tumor necrosis targeted internal irradiation. nuclide 131 I can emit short-range high-energy β particles, and can perform radiation therapy on residual living tumors, so as to achieve the therapeutic effect of tumors. Using th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/40A61K31/122A61K9/08A61K51/06A61P35/00A61K101/02
CPCA61K9/0019A61K9/08A61K31/122A61K47/40A61K51/06
Inventor 倪以政李玥朱孝云张健孙自平蒋维平
Owner 南京成至诚医药科技有限公司
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