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58Fe hemin, preparation method and application of 58Fe hemin to study of pharmacokinetics

A technology of hemin and ferrous chloride, which is applied in the fields of drug synthesis and pharmacokinetics research, and can solve the problems of not finding research methods and the like

Inactive Publication Date: 2013-11-06
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Many scholars have also made various attempts to this, but have not yet found an effective research method

Method used

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  • 58Fe hemin, preparation method and application of 58Fe hemin to study of pharmacokinetics
  • 58Fe hemin, preparation method and application of 58Fe hemin to study of pharmacokinetics
  • 58Fe hemin, preparation method and application of 58Fe hemin to study of pharmacokinetics

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Experimental program
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Effect test

Embodiment 1

[0035] 1. Weigh 0.240g isotope 58 Fe powder (ISOFLEX USA, San Franciso, No.26-01-58-4030) was transferred to a single-necked flask, 25ml of anaerobic water was added, and HCl gas (generated by chlorine sodium chloride / ammonium chloride and concentrated sulfuric acid), heated in an oil bath until 58 Fe powder completely disappeared. Under the protection of nitrogen, evaporate the water in the reaction solution on a rotary evaporator to obtain isotopic ferrous chloride solid; dry in a vacuum oven for 12 hours to obtain isotopic ferrous chloride crystals.

[0036] 2. Add 2.0918g disodium protoporphyrin in a 500ml three-necked round bottom flask with a stirring bar, a thermometer and an air reflux condenser (Tokyo Chemical Industry Co., Ltd., 6-15-9, Toshima, Kita-ku, Tokyo, Lot. GG01), dissolved in about 220ml DMF as solvent, acidified by adding 770ul concentrated hydrochloric acid, fully dissolved by ultrasonic vibration, and the pH value of the system was 6-7 at this time. A...

Embodiment 2

[0050] 1. Weigh 0.8589g isotope 58 Fe powder (ISOFLEX USA, San Franciso, No.26-01-58-4030) was transferred to a single-necked flask, 20ml of anaerobic water was added, and HCl gas (generated by chlorine) was introduced below the liquid level of the single-necked flask. sodium chloride / ammonium chloride and concentrated sulfuric acid), heated in an oil bath until 58 Fe powder completely disappeared. Under the protection of nitrogen, evaporate the water in the reaction solution on a rotary evaporator to obtain isotopic ferrous chloride solid; dry in a vacuum oven for 12 hours to obtain isotopic ferrous chloride crystals.

[0051] 2. Add 0.4652g disodium protoporphyrin in a 100ml three-neck round bottom flask with a stirring bar, a thermometer and an air reflux condenser (Tokyo Chemical Industry Co., Ltd., 6-15-9, Toshima, Kita-ku, Tokyo, Lot. GG01), dissolved in about 50ml DMF as solvent, acidified by adding 130ul concentrated hydrochloric acid, fully dissolved by ultrasonic v...

Embodiment 3

[0059] Repeat the process of Example 2, the change is to control the reaction molar ratio of isotopic iron powder and disodium protoporphyrin to be 1:10 and 1:15 respectively. The pure products of isotope hemin with the purity of 91.89% and 94.85% can be obtained respectively.

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Abstract

The invention relates to the fields of the synthesis of medicines and pharmacokinetics, in particular to hemin containing stable isotope 58Fe and a method for synthesizing the hemin. The method comprises the following steps of: (a), oxidizing isotope 58Fe powder by using excess diluted hydrochloric acid to generate an isotope ferrous chloride solution, evaporating to remove moisture, and drying under vacuum to prepare an isotope ferrous chloride crystal; (b), reacting the prepared isotope ferrous chloride crystal with acidified protoporphyrin disodium, and controlling the pH value of a system before reaction to be 5 to 7; and (c), evaporating to remove most of reaction solvents, washing, adding an inorganic acid, regulating the pH value of the system to be 1 to 2, performing ultrasound oscillation, standing and performing suction filtration to obtain the 58Fe hemin. The invention provides a high-accuracy and high-sensitivity study method for the study of the intracorporal process of an endogenous substance, namely a core skeleton of the endogenous substance is marked by an isotope marking method, and the intracorporal process of the endogenous substance is studied quantitatively by measuring the content of the marked endogenous substance.

Description

technical field [0001] The invention relates to the fields of drug synthesis and pharmacokinetics research, in particular to a stable isotope-containing 58 Hemin of Fe and its synthesis method. Background technique [0002] Hemin is a stable form of heme (iron porphyrin). It is internationally recognized as the most effective drug for preventing and treating iron deficiency anemia. Its main features are high iron content, no gastrointestinal irritation, easy absorption by the human body, good bioavailability, directly absorbed in the gastrointestinal tract in molecular form after entering the human body, fast absorption rate, and obvious iron supplementation effect ; Therefore, many researchers regard it as the optimal choice to replace the inorganic iron supplements currently dominant in the market. In addition, hemin is also widely used in the food industry, as an additive of various foods, and plays a functional role in the treatment of iron deficiency anemia. [0003...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/22G01N33/60
Inventor 陈西敬张永杰唐明清赵娣韩德恩王越
Owner CHINA PHARM UNIV
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