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Cidofovir liposome and preparation method thereof

A liposome and lipid membrane technology, applied in the field of medicine, can solve the problems of limited application, toxic and side effects of cidofovir, etc.

Inactive Publication Date: 2005-11-23
山东特瑞林医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug is significantly better than the marketed drugs ganciclovir and foscarnet sod

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1 cidofovir liposome, the components are as follows:

[0017] Cidofovir 1g

[0018] Lecithin 40g

[0019] Cholesterol 10g

[0020] Sodium deoxycholate 0.5g

[0021] Sucrose 48.5g

[0022] The preparation method is as follows:

[0023] Weigh 40g of lecithin, add 500ml of absolute ethanol, add 10g of cholesterol, stir to dissolve, evaporate under reduced pressure with a rotary evaporator to form a film. Weigh 1g of cidofovir, add 300ml pH6.86 phosphate buffer to dissolve, add 0.5g sodium deoxycholate and 48.5g sucrose and mix with lecithin to prepare a suspension, high-pressure homogenate and mix well to prepare lipid Plastids, gel column separation liposome solution, after clarification and filtration, filter with 0.22um microporous membrane, canned, freeze-dried to obtain cidofovir liposomes.

Embodiment 2

[0024] Embodiment 2 cidofovir liposomes, the components are as follows:

[0025] Cidofovir 5g

[0026] Lecithin 52g

[0027] Cholesterol 12g

[0028] Sodium deoxycholate 1g

[0029] Sucrose 30g

[0030] Preparation method is with embodiment 1,

Embodiment 3

[0031] Embodiment 3 cidofovir liposomes, the components are as follows:

[0032] Cidofovir 10g

[0033] Lecithin 68g

[0034] Cholesterol 17g

[0035] Sodium deoxycholate 3g

[0036] Sucrose 2g

[0037] The preparation method is the same as in Example 1.

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Abstract

The invention relates to a cidofovir liposome and preparation method wherein the cidofovir liposome comprises the following constituents (by weight percentage), cidofovir 1-10%, lecithin 40-68%, cholesterin 10-17%, sodium deoxycholate 0.5-3%, cane sugar 2-48.2%. The preparation comprises weighing prescription amount of lecithin and cholesterin, dissolving with anhydrous alcohol and mixing, evaporating with rotary evaporator to obtain lipid film, then dissolving cidofovir into phosphoric acid buffer, charging deoxysodium cholate and cane sugar as required by prescription, charging into prepared lipid film and mixing, disintegrating with high pressure homogenizer to obtain liposome, then carrying out microporous film filtering, degerming, canning, and freeze drying.

Description

(1) Technical field [0001] The invention relates to cidofovir liposome and a preparation method thereof, belonging to the technical field of medicine. (2) Background technology [0002] Cidofovir (cidofovir, HPMPC, GS-504) is a ring-opening nucleotide analog that can inhibit viral DNA polymerase, has a strong inhibitory effect on human CMV, and has a strong inhibitory effect on other herpes viruses such as herpes simplex virus (HSV) Types I and II, varicella-zoster virus (VZV), E-B virus, herpes 6 virus (HHV-6), adenovirus, and human papillomavirus (HPV) also have strong activity. Cidofovir injection was developed by Gilead Company and was approved by the US FDA on May 15, 1996. The trade name is Vistide, which is used to treat retinitis caused by cytomegalovirus in AIDS patients. The drug is significantly better than the marketed drugs ganciclovir and foscarnet sodium in terms of curative effect, tolerance and therapeutic index. clinical application. (3) Contents of the...

Claims

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Application Information

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IPC IPC(8): A61K31/7052
Inventor 肖广常张颖孙锦光王淑娟
Owner 山东特瑞林医药科技发展有限公司
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