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Cefpiramide, sodium benzoate, sodium bicarbonate pharmaceutical composite lipidosome injection

A technology of sodium benzoate and sodium bicarbonate, which is applied in the field of medicine, can solve the problems of low bioavailability and poor stability, and achieve the effects of cheap and easy to obtain, stable properties, and improved pharmaceutical properties

Inactive Publication Date: 2010-07-07
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] For the shortcoming of poor stability and low bioavailability of this product currently on the market, the object of the present invention is to provide a kind of cefpiramide / sodium benzoate / sodium bicarbonate pharmaceutical composition liposome injection, by carrying out liposome injection to cefpiramide body encapsulation to change its pharmaceutical properties, greatly improving the stability of cefpiramide and ensuring the safety of medication

Method used

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  • Cefpiramide, sodium benzoate, sodium bicarbonate pharmaceutical composite lipidosome injection
  • Cefpiramide, sodium benzoate, sodium bicarbonate pharmaceutical composite lipidosome injection
  • Cefpiramide, sodium benzoate, sodium bicarbonate pharmaceutical composite lipidosome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Prescription (specification 0.1g)

[0043] Cefpiramide 10g

[0044] Sodium Benzoate 0.54g

[0045] Sodium bicarbonate 6.8g

[0046] Soy Lecithin 16g

[0047] Cholesterol 16g

[0048] Tween 80 8g

[0049] Glucose 18g

[0050] Vitamin E 7g

[0051] Preparation Process:

[0052] (1) Dissolve 16g soybean lecithin, 16g cholesterol, 7g vitamin E and 8g Tween 80 in 200ml methanol, mix well, remove the organic solvent under reduced pressure on a rotary thin film evaporator, and obtain a phospholipid film;

[0053] (2) add 200mlpH value to the sodium dihydrogen phosphate-disodium hydrogen phosphate buffer solution of 6.0 in the prepared phospholipid film, shake, stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, microporous membrane filtration, Prepare blank liposome suspension;

[0054] (3) Dissolve 10g of cefpiramide in 100ml of water for injection, filter through a microporous membrane, add the filtrate to the blank liposome sus...

Embodiment 2

[0057] Prescription (specification 0.2g)

[0058] Cefpiramide 20g

[0059] Sodium Benzoate 1.2g

[0060] Sodium bicarbonate 12g

[0061] Egg yolk lecithin 60g

[0062] Cholesterol 40g

[0063] Tween 80 20g

[0064] Sodium chloride 22g

[0065] Sodium sulfite 6g

[0066] Preparation Process:

[0067] (1) 60g egg yolk lecithin, 40g cholesterol, 6g sodium sulfite and 20g Tween 80 were dissolved in 400ml isopropanol, mixed uniformly, and the organic solvent was removed under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0068] (2) Add 300mlpH value to the citric acid-sodium citrate buffer solution of 6.2 in the prepared phospholipid film, shake, stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, microporous membrane filtration, preparation Obtain blank liposome suspension;

[0069] (3) 20g cefpiramide is dissolved in 200ml water for injection, filtered through a microporous membrane, the filtrate ...

Embodiment 3

[0072] Prescription (specification 0.05g)

[0073] Cefpiramide 5g

[0074] Sodium Benzoate 0.25g

[0075] Sodium bicarbonate 4g

[0076] Egg yolk lecithin 10g

[0077] Cholesterol 20g

[0078] Tween 80 10g

[0079] Mannitol 34g

[0080] Thiourea 10g

[0081] Preparation Process:

[0082] (1) 10g egg yolk lecithin, 20g cholesterol, 10g thiourea and 10g Tween 80 were dissolved in 600ml isopropanol, mixed uniformly, and the organic solvent was removed under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0083] (2) Add 500ml of sodium dihydrogen phosphate-disodium hydrogen phosphate buffer solution with a pH value of 5.8 to the prepared phospholipid film, shake and stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, and microporous membrane filtration to prepare Obtain blank liposome suspension;

[0084] (3) 5g cefpiramide is dissolved in 100ml water for injection, filters through microporous membra...

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Abstract

The invention discloses a cefpiramide, sodium benzoate, sodium bicarbonate pharmaceutical composite lipidosome injection and a preparation method thereof. The cefpiramide, sodium benzoate, sodium bicarbonate pharmaceutical composite lipidosome injection includes cefpiramide, sodium benzoate, sodium bicarbonate, lipidosome matrix, osmotic pressure regulator and antioxidant, wherein, the lipidosome matrix is the mixture of phospholipids, cholesterin and Tween-80. Preferentially, the mass ratio of the phospholipids, the cholesterin and the Tween-80 in the lipidosome matrix is 1-3:2:1; the mass ratio of the cefpiramide and the lipidosome matrix is 1:2-11, preferentially as 1:2-11; the mass ratio of the cefpiramide, the sodium benzoate and the sodium bicarbonate is 1:0.05-0.06:0.6-0.8.

Description

technical field [0001] The invention relates to a western medicine preparation, in particular to a cefpiramide / sodium benzoate / sodium bicarbonate pharmaceutical composition liposome injection, which belongs to the technical field of medicine. technical background [0002] Cefpiramide, its chemical name is: (6R,7R)-7-[(R)-2-(4-hydroxy-6-methyl-3-pyridinecarbonylamino)-2-(p-hydroxyphenyl)acetyl Amino]-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4,2,0] Oct-2-ene-2-carboxylic acid, molecular formula: C 25 h 24 N 8 0 7 S 2 , molecular weight: 612.63, structural formula: [0003] [0004] Cefpiramide has a broad antibacterial spectrum, good pharmacokinetic characteristics, good stability to β-lactamase, strong antibacterial activity against Gram-positive bacteria, and also antibacterial activity against Gram-negative bacteria. It has broad-spectrum antibacterial activity and a perfectly balanced antibacterial spectrum. Applicable to Staphylococ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/546A61K47/28A61K47/24A61K47/34A61P31/04A61K47/26
Inventor 王明
Owner HAINAN LINGKANG PHARMA CO LTD
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