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Anti-virus sustained-release drug capable of being subjected to intraocular injection, preparation method and applications thereof

A technology of reaction, foscarnet, applied in the field of antiviral sustained-release drugs and their preparation, can solve the problems of high dosage of drugs, inability to apply the degradable microsphere sustained-release system, etc., and achieve the effect of good health

Active Publication Date: 2018-07-13
BEIJING CHAOYANG HOSPITAL CAPITAL MEDICAL UNIV +1
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the dosage of foscarnet sodium is much higher than that of ganciclovir, and the long-term sustained release in the eye requires a specially designed system with a drug loading close to 100%, which is technically very challenging; second, intravitreal injection The needle type is 27G or finer, and its inner diameter is only 210 μm, which requires that the particles of the sustained-release system have an appropriate size and are not easy to aggregate; third, the intraocular environment requires strict sterile materials, and the materials used for injection must pass through strict disinfection
These requirements make the conventional degradable microsphere sustained-release system unapplicable, and a new system needs to be invented to solve the on-the-spot demand for intraocular sustained release of foscarnet sodium

Method used

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  • Anti-virus sustained-release drug capable of being subjected to intraocular injection, preparation method and applications thereof
  • Anti-virus sustained-release drug capable of being subjected to intraocular injection, preparation method and applications thereof
  • Anti-virus sustained-release drug capable of being subjected to intraocular injection, preparation method and applications thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Embodiment 1, the preparation of foscarnet insoluble salt micro-crystal

[0035] according to figure 1 The preparation flow chart shown is to prepare micro-crystals of foscarnet insoluble salt.

[0036] Prepare 2mg / mL sodium foscarnet aqueous solution and 2mg / mL calcium chloride solution, pour the two solutions with a volume ratio of 1:1 and mix them under magnetic stirring, and continue stirring for 1 hour after mixing; stop stirring, and let it stand for 10 minutes. Slowly pour off the supernatant; wash the sample 3 times with pure water; freeze-dry the suspension to obtain product a.

[0037] According to the above method, by adjusting the concentration of foscarnet sodium solution and calcium chloride solution, or by adjusting the mixing volume ratio of foscarnet sodium solution and calcium chloride solution, foscarnet insoluble salt micron crystal slow-release medicines of different sizes can be prepared.

[0038] According to the above preparation method, a 6 mg...

Embodiment 2

[0040] Embodiment 2, in vitro performance characterization of foscarnet insoluble salt micro-crystals

[0041] Scanning electron microscopy characterization: the freeze-dried powder samples a, b, and c of the micro-crystals of foscarnet refractory salt prepared in Example 1 were evenly sprinkled on the sample stage with conductive glue, and the excess samples on the surface were blown off. Scanning electron microscope observation. See the experimental results figure 2 .

[0042] figure 2 (a), (b) and (c) are the scanning electron microscope pictures of the micro-crystals a, b, and c of the refractory salt of foscarnet respectively, and the average sizes are estimated to be 10 μm, 60 μm, and 100 μm in diameter, respectively, and the crystals can be seen Both grow lamellar crystals radially from the center to form spherical crystals of micron size.

[0043] Plasma mass spectrometry characterization: Weigh 50 mg of foscarnet insoluble salt micron crystal freeze-dried powder...

Embodiment 3

[0050] Embodiment 3, animal intraocular sustained release experiment of foscarnet insoluble salt micro-crystal

[0051] In the experiment, 13 New Zealand white rabbits were selected, and both eyes were injected with slow-release drugs.

[0052] The animal experiment steps are as follows:

[0053] 1. The formulation of the injection suspension: 180mg of foscarnet insoluble salt slow-release drug (product a) was dissolved in 1.8mL 1% CMV solution (carboxymethylcellulose), before vortex mixing, slow-release drug and CMV solution All should be irradiated with ultraviolet light for 60 minutes to carry out disinfection and sterilization.

[0054] 2. New Zealand white rabbits were anesthetized by intravenous injection of pentobarbital.

[0055] 3. Inject foscarnet insoluble salt / CMV suspension into the vitreous cavity of both eyes of white rabbits with a 29G insulin needle. After the injection, a white substance was observed in the vitreous cavity, confirming that the injection was...

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Abstract

The invention provides an anti-virus sustained-release drug capable of being subjected to intraocular injection, a preparation method and applications thereof, wherein the anti-virus sustained-releasedrug is a foscarnet insoluble salt micro-crystal, and the foscarnet insoluble salt is the polyvalent metal salt of foscarnet. The preparation method comprises: carrying out a reaction on the monovalent metal salt of foscarnet and the soluble salt of a polyvalent metal in water to obtain the system containing the foscarnet insoluble salt micro-crystal. According to the present invention, based onthe special requirement of the controlled-release and slow-release intraocular injection, the foscarnet insoluble salt micro-crystal slow-release system is designed, wherein the nominal drug loading can be more than 100%; the foscarnet insoluble salt micro-crystal slow-release drug can be lastingly, stably and slowly released in the vitreous cavity of rabbit eyes, the concentration of the foscarnet in the vitreous cavity is always maintained above the effective therapeutic concentration of sodium foscarnet, the sustained release period is up to 12 weeks, and the drug does not have obvious toxic effects and inflammatory reaction; and the foscarnet insoluble salt can be used as the anti-virus sustained-release drug capable of being injected into the vitreous cavity.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to an antiviral slow-release medicine which can be used by intraocular injection and its preparation method and application. Background technique [0002] Viral retinal diseases are eye diseases with high risk of visual damage and blindness, and there are various diseases, including cytomegalovirus retinitis, acute retinal necrosis, progressive outer retinopathy, etc. The incidence of viral retinal diseases has been increasing in recent years under the joint action of various factors such as population aging, the spread of AIDS, the use of new immunosuppressants, unhealthy living habits, and increased stress. [0003] Intravitreal injection of antiviral drugs is an important way for clinical treatment of viral retinal diseases, including foscarnet sodium and ganciclovir. The half-life of foscarnet sodium in the eye is very short, and after 12 hours, the concentration of foscarn...

Claims

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Application Information

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IPC IPC(8): C07F9/38A61K31/662A61K9/08A61P31/12A61P27/02
CPCA61K9/08A61K31/662A61P27/02A61P31/12C07F9/38C07F9/3808A61K9/0002A61K9/0019A61K9/0048C07B2200/13
Inventor 陶勇黄延宾孙玉玲曹庆辰
Owner BEIJING CHAOYANG HOSPITAL CAPITAL MEDICAL UNIV
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