Torasemide liposome injection

A technology of torasemide liposome, which is applied in the field of medicine, can solve the problems of poor solubility of torasemide, unsuitable for injection, and reduced drug content, so as to achieve uniform appearance, improve bioavailability, and improve The effect of stability

Inactive Publication Date: 2013-01-23
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Chinese patent CN100372534C discloses a freeze-dried preparation of torasemide and a preparation method thereof, which effectively solves the problem of poor solubility of torasemide by adding sodium bicarbonate. The solubility of torasemide is made into injections, but there is an amide bond in the structure of torasemide, which is easily hydrolyzed after being prepared into a liquid preparation, resulting in a decrease in drug content and an increase in related substances, which affects the curative effect
[0014] Chinese patent CN102078300A discloses a liposomal solid oral preparation of torasemide, which is prepared into liposomes according to specific ratios by torasemide and soybean lecithin, cholesterol, sodium glycocholate, sorbitol and soybean sterol. Plastids, whose membranes are complex and unsuitable for injectable use

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1 torasemide liposome injection

[0050]

[0051] Preparation Process:

[0052] (1) Take by weight 10g torasemide, 120g cephalin, 40g cholesterol, 50g polyoxyethylene 40 hydrogenated castor oil and 9g vitamin E and place in a pear-shaped bottle, add 6000ml n-butanol, heat and stir to make It dissolves, and then removes n-butanol under reduced pressure on a rotary evaporator, forming a uniform transparent phospholipid film on the bottle wall;

[0053] (2) Under the protection of nitrogen, add 700ml of citrate buffer solution with a pH of 6.2 to the bottle, stir to elute the phospholipid film and disperse it in the medium to swell and hydrate. Massage 4 to 6 times, filter through a 0.22 μm microporous membrane, and obtain torasemide liposomes;

[0054] (3) Dissolve 120g of trehalose in 200ml of distilled water, add it to the liposomes above, make up to 1000ml with distilled water, remove bacteria and heat source through ultrafiltration membrane, fill it ...

Embodiment 2

[0055] Embodiment 2 Torsemide liposome freeze-dried powder injection

[0056]

[0057] Preparation Process:

[0058] (1) Take by weight 20g torasemide, 200g cephalin, 70g cholesterol, 90g polyoxyethylene 40 hydrogenated castor oil and 15g vitamin E and place in a pear-shaped bottle, add 10000ml n-butanol, heat and stir to make It dissolves, and then removes n-butanol under reduced pressure on a rotary evaporator, forming a uniform transparent phospholipid film on the bottle wall;

[0059] (2) Under the protection of nitrogen, add 1500ml of citrate buffer solution with a pH of 6.2 to the bottle, stir to elute the phospholipid film and disperse it in the medium to swell and hydrate. Massage 4 to 6 times, filter through a 0.22 μm microporous membrane, and obtain torasemide liposomes;

[0060] (3) Dissolve 200g of trehalose in 300ml of distilled water, add it to the liposomes, adjust the volume to 2000ml with distilled water, remove bacteria and heat sources through ultrafi...

Embodiment 3

[0061] Embodiment 3 Torsemide liposome freeze-dried powder injection

[0062]

[0063] Preparation Process:

[0064] (1) Take by weight 20g torasemide, 180g cephalin, 60g cholesterol, 80g polyoxyethylene 40 hydrogenated castor oil and 12g vitamin E and place in a pear-shaped bottle, add 9000ml n-butanol, heat and stir to make It dissolves, and then removes n-butanol under reduced pressure on a rotary evaporator, forming a uniform transparent phospholipid film on the bottle wall;

[0065] (2) Under the protection of nitrogen, add 1500ml of citrate buffer solution with a pH of 6.2 to the bottle, stir to elute the phospholipid film and disperse it in the medium to swell and hydrate. Massage 4 to 6 times, filter through a 0.22 μm microporous membrane, and obtain torasemide liposomes;

[0066] (3) Dissolve 160g of trehalose in 200ml of distilled water, add it to the liposomes, adjust the volume to 2000ml with distilled water, remove bacteria and heat sources through an ultra...

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Abstract

The invention discloses a torasemide liposome injection. The torasemide liposome injection is prepared from torasemide, cephalin, cholesterol, polyoxyethylene (40) hydrogenated castor oil, one or more antioxidants and one or more protective agents. The torasemide liposome injection has the advantages that preparation stability is good; liposome fracture caused by dehydration and fusion is avoidedin a freeze-drying process; after hydration redissolution, the liposome still retains a good entrapment rate and good stability; and the torasemide liposome injection improves preparation product quality, reduces toxic and side effects of torasemide and is suitable for industrial production.

Description

technical field [0001] The invention relates to a new preparation of torasemide, in particular to a torasemide liposome injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Torasemide (torasemide), the chemical name is 1-isopropyl-3-[(4-m-tolylamino-3-pyridyl)sulfonyl]urea, molecular formula: C 16 h 20 N 4 o 3 S, molecular weight: 348.43, structural formula: [0003] [0004] Torsemide is a sulfonylupyridine diuretic that mainly acts on the thick ascending branch of Henle's loop of Henle, inhibiting Na + / K + / 2Cl - Carrier system that makes urine Na + 、K + , Cl - and water excretion increased but had no significant effect on glomerular filtration rate, renal plasma flow or acid-base balance in vivo. It is clinically used for patients with edema caused by congestive heart failure, renal failure and kidney disease, and can also be used for patients with essential hypertension. [0005] Since tora...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/44A61K47/44A61K47/28A61K47/24A61P7/10
Inventor 廖爱国曹仕霞
Owner HAINAN MEIDA PHARMA
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