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Ganciclovir compound as well as preparation method and pharmaceutical composition thereof

A technology of ganciclovir and composition, applied in the field of ganciclovir compound, preparation method and pharmaceutical composition thereof, can solve the problems of drug physics, chemistry and stability reduction, drug agglomeration, easy oxidation of drug, etc. Achieve the effect of good product stability, low moisture absorption, smooth and delicate appearance

Active Publication Date: 2014-11-19
北京科创鼎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

[0009] However, the ganciclovir of the prior art has hygroscopicity, so that there are certain problems in storage, and the hygroscopicity can also cause drug caking, fluidity reduction, deliquescence, crystal form change, etc., and then cause color changes, content reduction or Compatibility changes between components; after moisture absorption, the drug is more likely to be oxidized, hydrolyzed, and mildewed, thereby reducing the physical, chemical and stability of the drug

Method used

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  • Ganciclovir compound as well as preparation method and pharmaceutical composition thereof
  • Ganciclovir compound as well as preparation method and pharmaceutical composition thereof
  • Ganciclovir compound as well as preparation method and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1, the preparation of ganciclovir compound

[0042] (1) Prepare A solution: Sterile filter 600L of a mixed solvent of methanol and acetone (the volume ratio of methanol and acetone is 5:1) into a crystallization tank, cool down to 12°C and wait for use, which is A solution;

[0043](2) Preparation of solution B: Add 60kg of water for injection into the dissolving tank, control the temperature at 70°C, add 30kg of crude ganciclovir, add 0.45kg of activated carbon after dissolving, stir for 30min to decolorize, filter aseptically, and use 10kg of water for injection Washing, collecting filtrate and washing liquid, obtains B solution;

[0044] (3) Add solution B to solution A, lower the temperature to 15°C, precipitate crystals, grow crystals for 2 hours, filter, wash, and vacuum dry at 45°C until the water content is less than 0.5%.

[0045] The X-ray powder diffraction pattern obtained by measuring the obtained ganciclovir compound using Cu-Kα rays is shown i...

Embodiment 2-9

[0048]

[0049] The X-ray powder diffraction pattern obtained by measuring the ganciclovir obtained in Examples 2-9 using Cu-Kα rays is similar to Example 1.

preparation Embodiment 1

[0050] Preparation Example 1, Ganciclovir for Injection

[0051] prescription:

[0052]

[0053] Preparation:

[0054] (1) Weigh the prescribed amount of dextran 40, add appropriate amount of water for injection to dissolve, and obtain dextran 40 solution;

[0055] (2) Take the ganciclovir compound prepared in Example 1 of the prescription amount, add equimolar sodium hydroxide solution, stir to dissolve; then add the dextran 40 solution obtained in step (1), add water for injection to the total 4 / 5 of the volume, and adjust the pH value to 10.5-11.5, add water for injection to the full amount;

[0056] (3) Add 0.1% activated carbon, keep warm at 60°C, stir for 30 minutes, decarburize the liquid through a 0.8μm microporous membrane; then fine filter through a 0.22μm microporous membrane;

[0057] (4) Filling, plugging, intermediate detection, freeze-drying, and capping of the filtered medicinal solution; wherein, the freeze-drying is carried out according to the followin...

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PUM

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Abstract

The invention belongs to the technical field of the medicine, and specifically relates to a ganciclovir compound as well as a preparation method and a pharmaceutical composition thereof. The ganciclovir compound has a structural formula as shown in a formula (I); the compound is measured by using Cu-K alpha rays so that an X-ray powder diffraction pattern as shown in a figure 1 can be obtained. Hygroscopicity tests indicate that compared with the prior art, the ganciclovir compound provided by the invention has low hygroscopicity; a freeze-dried powder injection prepared from the ganciclovir compound provided by the invention is bright, clean, fine and even in appearance, and excellent in product stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a ganciclovir compound, a preparation method and a pharmaceutical composition thereof. Background technique [0002] Ganciclovir (ganciclovir) has broad-spectrum antiherpes virus activity and is the first effective antiviral drug for the treatment of human cytomegalovirus (CMV) infection. The inhibitory effect on cytomegalovirus is one of the most active antiviral drugs approved for use so far, and the incidence of adverse reactions is low. It is currently recognized as the first choice drug for the treatment of cytomegalovirus, and it is also an indispensable prevention of organ transplantation. and therapeutic drugs. Ganciclovir is widely distributed in various tissues in the body, and can pass through the placenta. The concentration in the cerebrospinal fluid is 7%-67% of the plasma concentration in the same period; it can also enter the intraocular tissue, and t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D473/18A61K31/522
Inventor 李琦杨磊
Owner 北京科创鼎诚医药科技有限公司