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Amoxicillin lipidosome solid preparation

A technology of amoxicillin solid and amoxicillin lipid, applied in the field of amoxicillin liposome and its preparation, can solve problems such as poor dissolution rate, poor quality stability, etc. Effects of side effects

Inactive Publication Date: 2011-05-04
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The object of the present invention is to provide a kind of amoxicillin liposome solid preparation, specifically, through the combination of certain content egg yolk lecithin, cholesterol, sodium glycocholate, Tween 80 and active ingredient amoxicillin, adopt Amoxicillin liposomes are made by film dispersion technology, and then mixed with certain excipients to make various solid preparations, which solves the problems of poor dissolution and poor quality stability, and improves the drug efficacy and bioavailability of the preparations Degree, obtained satisfactory technical effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of amoxicillin liposomes

[0043] Prescription: Amoxicillin 125g

[0044] Egg Yolk Lecithin 375g

[0045] Cholesterol 125g

[0046] Sodium Glycocholate 250g

[0047] Tween 80 62.5g

[0048] Preparation Process

[0049] (1) Dissolve 125g of amoxicillin, 375g of egg yolk lecithin, 125g of cholesterol, 250g of sodium glycocholate and 62.5g of Tween 80 in 4000ml of isopropanol, mix well, and remove isopropyl alcohol under reduced pressure on a rotary thin film evaporator. propanol, make phospholipid film;

[0050] (2) Add 2000ml of acetic acid-sodium acetate buffer solution with pH = 4.5, shake and stir to completely hydrate the phospholipid membrane, then homogenize and emulsify for 20min with a tissue masher at a speed of 15000r / min to obtain a liposome suspension liquid;

[0051] (3) The suspension is freeze-dried to prepare amoxicillin liposomes.

Embodiment 2

[0059] Example 2 Preparation of amoxicillin liposomes

[0060] Prescription: Amoxicillin 250g

[0061] Egg yolk lecithin 2000g

[0062] Cholesterol 1500g

[0063] Sodium Glycocholate 1000g

[0064] Tween 80 1250g

[0065] Preparation Process

[0066] (1) Dissolve 250g of amoxicillin, 2000g of egg yolk lecithin, 1500g of cholesterol, 1000g of sodium glycocholate and 1250g of Tween 80 in 18000ml of isopropanol, mix well, and remove isopropanol under reduced pressure on a rotary thin film evaporator Alcohol, make phospholipid film;

[0067] (2) Add 10000ml of citric acid-sodium citrate buffer solution with pH = 6.0, shake and stir to completely hydrate the phospholipid membrane, and then homogenize and emulsify for 10min with a tissue masher at a speed of 13000r / min to obtain lipid Plastid suspension;

[0068] (3) The suspension is spray-dried to prepare amoxicillin liposomes.

Embodiment 3

[0080] Example 3 Preparation of amoxicillin liposomes

[0081] Prescription: Amoxicillin 125g

[0082] Egg Yolk Lecithin 625g

[0083] Cholesterol 500g

[0084] Sodium Glycocholate 375g

[0085] Tween 80 250g

[0086] Preparation Process

[0087] (1) Dissolve 125g of amoxicillin, 620g of egg yolk lecithin, 500g of cholesterol, 375g of sodium glycocholate and 250g of Tween 80 in 7500ml of isopropanol, mix well, and remove the isopropanol under reduced pressure on a rotary thin film evaporator. Alcohol, make phospholipid film;

[0088] (2) Add pH = 5.2 sodium dihydrogen phosphate-disodium hydrogen phosphate buffer solution 3000ml, shake and stir to completely hydrate the phospholipid membrane, and then homogenize and emulsify for 20 minutes with a tissue masher at a high speed of 12000r / min to obtain liposome suspension;

[0089] (3) The suspension is spray-dried to prepare amoxicillin liposomes.

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Abstract

The invention provides an amoxicillin lipidosome solid preparation and a new application thereof. Certain amounts of yolk lecithin, cholesterin, natrium glycocholicum, tween 80 and an active ingredient amoxicillin are combined and are prepared into amoxicillin lipidosome by film dispersion technology, and the amoxicillin lipidosome is mixed with the certain accessories to prepare various solid preparations. The amoxicillin lipidosome solid preparation not only can solve the problems of poor dissolution rate and poor quality stability of the amoxicillin, increases the medical effect and the bioavailability of the preparation, can treat bacterial liver abscess and obtain good invention effect.

Description

technical field [0001] The invention relates to an amoxicillin liposome and a preparation method thereof, in particular to an amoxicillin liposome solid preparation and a preparation method thereof, and a new application of the solid preparation in treating bacterial liver abscess. Background technique [0002] Bacterial liver abscess is a common acute and severe infectious disease clinically. The main pathogenic bacteria are Escherichia coli, Klebsiella pneumoniae, Enterococcus, Staphylococcus aureus, and anaerobic bacteria. The cases were mixed infections. [0003] The liver communicates with the biliary tract and thereby communicates with the intestinal tract. The liver receives double blood supply from the hepatic artery and the portal vein. Due to these anatomical characteristics, the chances of the liver being infected by bacteria increase. The main sources of bacteria that cause liver abscess are: (1) through the biliary tract Bacterial retrograde infection of the sy...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/16A61K9/20A61K9/48A61K31/43A61K47/28A61K47/24A61K47/40A61K47/38A61K47/36A61K47/34A61K47/32A61P31/04A61P1/16A61K47/26
Inventor 邱民
Owner HAINAN MEIDA PHARMA
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