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Cefditoren pivoxil liposome solid preparation

A technology of cefditoren and solid preparations, which is applied in the field of medicine to achieve the effects of high encapsulation rate, excellent dissolution and good sustained release effect

Inactive Publication Date: 2014-01-15
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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  • Cefditoren pivoxil liposome solid preparation
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  • Cefditoren pivoxil liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Embodiment 1 cefditoren pivoxil liposome tablet

[0080] The ingredients used are as follows:

[0081]

[0082] Adopt following production process to prepare cefditoren pivoxil liposome tablet:

[0083] (1) Accurately weigh 100g of cefditoren pivoxil, 100g of soybean phosphatidylserine, 50g of cholesterol, and 50g of polyoxyethylene alkylamine, and dissolve them in 1000ml of a mixed solvent of ethanol and chloroform with a volume ratio of 2:1, Stir to dissolve;

[0084] (2) Put the above solution in an eggplant-shaped bottle, remove ethanol and chloroform under reduced pressure in a 50°C water bath, and form a uniform transparent film on the wall of the bottle;

[0085](3) Add 1000ml of phosphate buffer solution with a pH value of 6.6 to the eggplant-shaped bottle, and continue to rotate in a water bath at 50°C under normal pressure to swell and hydrate the film;

[0086] (4) Filter the above solution with a 0.45 μm microporous membrane, place the filtrate in a ...

Embodiment 2

[0090] Embodiment 2 cefditoren pivoxil liposome tablet

[0091] The ingredients used are as follows:

[0092]

[0093] Adopt following production process to prepare cefditoren pivoxil liposomal capsules:

[0094] (1) Accurately weigh 100g of cefditoren pivoxil, 50g of soybean phosphatidylserine, 50g of cholesterol, and 80g of polyoxyethylene alkylamine, and dissolve them in 1000ml of a mixed solvent of ethanol and chloroform with a volume ratio of 2:1, Stir to dissolve;

[0095] (2) Put the above solution in an eggplant-shaped bottle, remove ethanol and chloroform under reduced pressure in a 50°C water bath, and form a uniform transparent film on the wall of the bottle;

[0096] (3) Add 1000ml of phosphate buffer solution with a pH value of 6.6 to the eggplant-shaped bottle, and continue to rotate in a water bath at 50°C under normal pressure to swell and hydrate the film;

[0097] (4) Filter the above solution with a 0.45 μm microporous membrane, place the filtrate in...

Embodiment 3

[0101] Embodiment 3 cefditoren pivoxil liposome tablet

[0102] The ingredients used are as follows:

[0103]

[0104] Adopt the following production process to prepare cefditoren pivoxil liposome dry suspension:

[0105] (1) Accurately weigh 100g of cefditoren pivoxil, 150g of soybean phosphatidylserine, 100g of cholesterol, and 100g of polyoxyethylene alkylamine, and dissolve them in 1000ml of a mixed solvent of ethanol and chloroform at a volume ratio of 2:1, Stir to dissolve;

[0106] (2) Put the above solution in an eggplant-shaped bottle, remove ethanol and chloroform under reduced pressure in a 50°C water bath, and form a uniform transparent film on the wall of the bottle;

[0107] (3) Add 1000ml of phosphate buffer solution with a pH value of 6.6 to the eggplant-shaped bottle, and continue to rotate in a water bath at 50°C under normal pressure to swell and hydrate the film;

[0108] (4) Filter the above solution with a 0.45 μm microporous membrane, place the f...

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Abstract

The invention discloses a cefditoren pivoxil liposome solid preparation and a method for preparing the same. The active ingredient namely cefditoren pivoxil and a specific combination of soybean phosphatidylserine, cholesterol, and polyoxyethylene alkylamine are prepared into liposome, so the stability, dissolution property and bioavailability of the preparation are greatly improved, and moreover, the preparation has a stable and lasting effect, small side effects and obvious efficacy.

Description

technical field [0001] The invention relates to a cefditoren pivoxil liposome solid preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cefditoren pivoxil (cefditoren pivoxil) is the third-generation cephalosporin developed in Japan, and later classified as the fourth generation. Its chemical name is: (-)-(6R,7R)-2,2-dimethyl Propionyloxymethyl 7-[(Z)-2-(2-amino-4-thiazolyl)-2-methoxyiminoacetamido]-3-[(Z)-2-(4-methyl -5-thiazolyl)vinyl]-8-oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylate, molecular formula C 25 h 28 N 6 o 7 S 3 , molecular weight 620.73, structural formula: [0003] [0004] Cefditoren pivoxil was approved by the US FDA in September 2001. Cefditoren pivoxil has potent activity against Gram-positive (GP) and Gram-negative (GN) bacteria and has now been classified as a fourth-generation oral cephalosporin. Cefditoren pivoxil itself has no antibacterial activity. As a prodrug,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/127A61K31/546A61K47/34A61P31/04
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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