Ganciclovir sodium monohydrate and preparation method thereof

A technology of ganciclovir sodium and monohydrate, which is applied in the field of ganciclovir sodium monohydrate and its preparation, can solve the problem that the moisture absorption capacity of ganciclovir sodium monohydrate is weakened, the product quality is affected, and the product quality is affected. Reduce the content of ingredients and other problems, to achieve the effects of low production cost, easy control, and mild reaction conditions

Pending Publication Date: 2022-04-22
ANHUI POLY PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Ganciclovir sodium has strong hygroscopicity, and placing it in the air will lead to a decrease in the main component content of the product, thereby affecting product quality. Relatively speaking, the relative moisture absorption capacity of the prepared ganciclovir sodium monohydrate will be weakened.

Method used

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  • Ganciclovir sodium monohydrate and preparation method thereof
  • Ganciclovir sodium monohydrate and preparation method thereof
  • Ganciclovir sodium monohydrate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Add 20.0g of ganciclovir to 33mL of purified water, stir at room temperature, dissolve 3.2g of sodium hydroxide in 15mL of purified water and add to the system, stir for 3 hours, then add 120mL of 95% ethanol, grow crystals at room temperature for 1h, then filter, and then Add 120mL of 95% ethanol to the crude wet product, heat up to 78°C and stir for 2 hours, filter while hot, then add 200mL absolute ethanol to the crude wet product, heat up to 78°C and stir for 2 hours, filter while hot, vacuum dry to control the internal temperature ≤60°C, vacuum degree ≤0.08Mpa, dry under reduced pressure. 17.5 g of ganciclovir sodium monohydrate was obtained.

Embodiment 2

[0027] Add 20.0g of ganciclovir into 25mL of purified water, stir at room temperature, dissolve 3.2g of sodium hydroxide in 15mL of purified water and add to the system, stir for 2 hours, then add 100mL of 95% ethanol, grow crystals at room temperature for 0.5h, then filter, and then Add 100mL of 95% ethanol to the crude wet product, raise the temperature to 75°C and stir for 1.5 hours, filter while hot, then add 150mL absolute ethanol to the crude wet product, raise the temperature to 75°C and stir for 1.5 hours, filter while hot, and vacuum-dry Dry under reduced pressure at temperature ≤60°C and vacuum degree ≤0.08Mpa.

Embodiment 3

[0029] Add 20.0g of ganciclovir into 40mL of purified water, stir at room temperature, dissolve 3.2g of sodium hydroxide in 20mL of purified water and add to the system, stir for 4 hours, then add 140mL of 95% ethanol, grow crystals at room temperature for 1.5h, then filter, and then Add 140mL of 95% ethanol to the crude wet product, raise the temperature to 80°C and stir for 2.5 hours, filter while hot, then add 250mL absolute ethanol to the crude wet product, raise the temperature to 80°C and stir for 2.5 hours, filter while hot, and vacuum-dry Dry under reduced pressure at temperature ≤60°C and vacuum degree ≤0.08Mpa.

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Abstract

The invention provides ganciclovir sodium monohydrate, which is radiated by Cu-K alpha, and an X-ray powder diffraction pattern of the ganciclovir sodium monohydrate comprises the following diffraction peaks expressed by angle 2 theta: 4.2 degrees + / -0.1 degrees, 18.1 degrees + / -0.1 degrees, 23.2 degrees + / -0.1 degrees, 8.44 degrees + / -0.1 degrees, 15.28 degrees + / -0.1 degrees, 20.381 degrees + / -0.1 degrees, 21.24 degrees + / -0.1 degrees, 24.441 degrees + / -0.1 degrees, 30.98 degrees + / -0.1 degrees and 31.96 degrees + / -0.1 degrees. The X-ray powder diffraction pattern of the ganciclovir sodium monohydrate is basically as shown in Figure 1. According to the preparation method provided by the invention, water and ganciclovir react, 95% ethanol is added for crystallization after the reaction is finished, and the monohydrate crystal form of ganciclovir sodium is prepared; operation is simple, and reaction conditions are mild and easy to control.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a ganciclovir sodium monohydrate and a preparation method thereof. Background technique [0002] Ganciclovir (Ganciclovir) is an antiviral drug synthesized in 1980 by Julien Verheyden and John Martin of Syntex Research. It has strong activity against cytomegalovirus, HSV-I, HSV-II, varicella-zoster virus (VZV), Epstein-Barr virus (EBV) and human herpesvirus type 6 (HHV-6) in vivo and in vitro, among which The inhibitory activity against cytomegalovirus and Epstein-Barr virus is 10-20 times stronger than that of acyclovir, and 15-19 times stronger than that of foscarnet. Ganciclovir and its salts can inhibit the synthesis of cytomegalovirus DNA, slow down the extension of viral DNA and inhibit the replication of cytomegalovirus, so as to achieve its antiviral activity. [0003] At present, ganciclovir and ganciclovir sodium salt are mainly listed at home and abroad. Compared w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/18
CPCC07D473/18C07B2200/13
Inventor 范敏华聂良邓周学来周胜军周燕宝戴昕锐
Owner ANHUI POLY PHARM CO LTD
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