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Solid cefpodoxime proxetil liposome preparation

A technology of cefpodoxime axetil and solid preparations, which is applied in the field of medicine to achieve the effects of improving the product quality of preparations, improving the dissolution of preparations, and improving the therapeutic effect

Inactive Publication Date: 2012-01-25
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] However, the challenge in preparing liposomes lies in selecting the appropriate liposome composition and formulation

Method used

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  • Solid cefpodoxime proxetil liposome preparation
  • Solid cefpodoxime proxetil liposome preparation
  • Solid cefpodoxime proxetil liposome preparation

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preparation example Construction

[0069] On the other hand, the present invention provides the preparation method of cefpodoxime axetil liposome, the method comprises the following steps:

[0070] (a) dissolving cefpodoxime axetil, β-sitosterol, stearylamide, cholesterol, and Tween 80 in an organic solvent, stirring to dissolve it;

[0071] (b) Place the above solution in an eggplant-shaped bottle, remove the organic solvent under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0072] (c) Add buffer solution to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pressure to swell and hydrate the film;

[0073] (d) The above solution is filtered with a 0.45 microporous membrane, the filtrate is placed in a -20°C refrigerator and frozen overnight, then taken out and thawed, repeated freezing and thawing three times, and spray-dried to obtain cefpodoxime axetil liposome powder.

[0074] In a preferred embodiment of the me...

Embodiment 1

[0117] Embodiment 1 cefpodoxime axetil liposome sheet

[0118] The raw materials used are as follows:

[0119]

[0120] Adopt following production process to prepare cefpodoxime axetil liposome tablet:

[0121] (1) Accurately weigh 50g cefpodoxime axetil, 160g β-sitosterol, 40g stearamide, 100g cholesterol, 50g Tween 80, dissolve in 1200ml volume ratio of 2:1 dichloromethane and isopropanol and mix In the solvent, stir to dissolve it;

[0122] (2) Place the above solution in an eggplant-shaped bottle, remove methylene chloride and isopropanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0123] (3) Add 1200ml of phosphate buffer solution with a pH value of 6.8 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pressure to swell and hydrate the film;

[0124] (4) above-mentioned solution is filtered with 0.45 microporous membrane, and filtrate is placed in-20 ℃ of ref...

Embodiment 2

[0128] Embodiment 2 cefpodoxime axetil liposome capsule

[0129]

[0130] Adopt following production process to prepare cefpodoxime axetil liposome capsule:

[0131] (1) Accurately weigh 100g cefpodoxime axetil, 100g β-sitosterol, 25g stearamide, 150g cholesterol, 80g Tween 80, dissolve in 1000ml volume ratio of 2:1 dichloromethane and isopropanol and mix In the solvent, stir to dissolve it;

[0132] (2) Place the above solution in an eggplant-shaped bottle, remove methylene chloride and isopropanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0133] (3) Add 1000 ml of phosphate buffer solution with a pH value of 6.8 to the eggplant-shaped bottle, and continue to rotate in a 45°C water bath under normal pressure to swell and hydrate the film;

[0134] (4) above-mentioned solution is filtered with 0.45 microporous membrane, and filtrate is placed in-20 ℃ of refrigerators and freezes overnight, then takes ou...

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Abstract

The invention discloses a solid cefpodoxime proxetil liposome preparation and a preparation method thereof. The liposome is prepared with an active ingredient cefpodoxime proxetil and particular combination of beta-sitosterol, stearamide, cholesterol and Tween 80. The stability, dissolution and bioavailability of drugs can be greatly improved, stable and lasting effects can be achieved, and the curative effect is significant. The preparation product quality is improved, and toxic side effects are reduced.

Description

technical field [0001] The invention relates to a liposome solid preparation, in particular to a cefpodoxime axetil liposome solid preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cefpodoxime proxetil (Cefpodoxime proxetil), is the third-generation oral cephalosporin developed by Japan's Sankyo Company, which was first listed in Japan in 1990. The chemical name of cefpodoxime axetil is: (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)-acetamido]-3 -Methoxymethyl-8-oxo-5-thio-1-azabicyclo-[4,2,0]oct-2-ene-2-carboxylic acid isopropoxycarbonyloxyethyl ester, molecular formula: C 21 h 27 N 5 o 9 S 2 , molecular weight: 557.59, the structural formula is as follows: [0003] [0004] Cefpodoxime axetil is the prodrug of cefpodoxime, which itself has no antibacterial activity. It is absorbed through the intestinal tract after oral administration, and is hydrolyzed into cefpodoxime by non-specif...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/546A61K47/34A61P31/04
Inventor 廖爱国董林青
Owner HAINAN MEIDA PHARMA
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