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Solid preparation of Torasemide liposome

A technology of torasemide lipid and rice liposome, which is applied in the field of medicine, can solve the problems of no improvement in the solubility and stability of torasemide, reduced drug content, and low bioavailability, so as to improve bioavailability , low toxic and side effects, and high bioavailability

Inactive Publication Date: 2012-01-11
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Torsemide is insoluble in water, and currently listed preparations include tablets, capsules and injections. Chinese patent CN101632665A discloses a torasemide oral pharmaceutical composition, which consists of torasemide, gelatin, mannitol, aspen Patan made a taste-masking composition, and then made dispersible tablets with other excipients. This patent improved the taste of dispersible tablets to a certain extent, but the solubility and stability of torasemide did not improve, resulting in Low bioavailability, affecting drug efficacy
Chinese patent CN100372534C discloses a freeze-dried preparation of torasemide and its preparation method. The solubility of torasemide is effectively increased by adding sodium bicarbonate. The solubility of Semide can be made into injections, but there is an amide bond in the structure of Torsemide, 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
[0010] However, the challenge in preparing liposomes lies in selecting the appropriate liposome composition and formulation

Method used

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  • Solid preparation of Torasemide liposome
  • Solid preparation of Torasemide liposome
  • Solid preparation of Torasemide liposome

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preparation example Construction

[0070] On the other hand, the present invention provides the preparation method of above-mentioned torasemide liposome, this method comprises the following steps:

[0071] (1) dissolving torasemide, soybean lecithin, cholesterol, sodium glycocholate and soybean sterol in an appropriate amount of ethanol to obtain a lipid solution;

[0072] (2) Place the above-mentioned lipid solution in a flask, in a constant temperature water bath at 35-40°C, remove ethanol by rotary evaporation, and form a uniform lipid film on the bottle wall;

[0073] (3) Dissolve sorbitol in water, slowly pour it into a flask and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution, to obtain a liposome suspension;

[0074] (4) Filter the above suspension with a microporous filter membrane with a pore size of 0.45 μm, and spray dry to obtain torasemide proliposome powder.

[0075] The torasemide liposome prepared by the method provided by the invention has hi...

Embodiment 1

[0099] The preparation of embodiment 1 torasemide liposome tablet

[0100] The raw and auxiliary materials used are as follows:

[0101] Torsemide 5g

[0102] Soy Lecithin 40g

[0103] Cholesterol 5g

[0104] Sodium Glycocholate 7.5g

[0105] Sorbitol 40g

[0106] Soy Sterol 4g

[0107] Lactose 50g

[0108] Starch 65g

[0109] Carboxymethyl Starch Sodium 10g

[0110] Povidone K30 10g

[0111] Magnesium Stearate 4g

[0112] Preparation Process:

[0113](1) 5g torasemide, 40g soybean lecithin, 5g cholesterol, 7.5g sodium glycocholate and 4g soybean sterol are dissolved in 800ml ethanol to obtain lipid solution;

[0114] (2) Place the above-mentioned lipid solution in a flask, and remove ethanol by rotary evaporation in a constant temperature water bath at 40°C, and a uniform lipid film is formed on the bottle wall;

[0115] (3) 40g sorbitol was dissolved in 400ml water, slowly poured into the flask and shaken gently, the lipid film was eluted and dispersed in the hyd...

Embodiment 2

[0120] The preparation of embodiment 2 torasemide liposome tablet

[0121] The raw and auxiliary materials used are as follows:

[0122] Torsemide 2.5g

[0123] Soy Lecithin 12g

[0124] Cholesterol 5g

[0125] Sodium Glycocholate 4g

[0126] Sorbitol 20g

[0127] Soy Sterol 1.5g

[0128] Lactose 26g

[0129] Starch 32g

[0130] Carboxymethyl Starch Sodium 5g

[0131] Povidone K30 5g

[0132] Magnesium Stearate 2g

[0133] Preparation Process:

[0134] (1) 2.5g torasemide, 12g soybean lecithin, 5g cholesterol, 4g sodium glycocholate and 1.5g soybean sterol are dissolved in 400ml ethanol to obtain lipid solution;

[0135] (2) The above-mentioned lipid solution is placed in a flask, placed in a constant temperature water bath at 40°C, and the ethanol is removed by rotary evaporation, and a uniform lipid film is formed on the bottle wall;

[0136] (3) Dissolve 20g of sorbitol in 200ml of water, slowly pour it into a flask and shake gently, so that the lipid film is el...

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Abstract

The invention provides a solid preparation of Torasemide liposome, which is prepared from the following raw materials and auxiliaries in parts by weight: 10 parts of Torasemide, 40 to 100 parts of soybean lecithin, 5 to 40 parts of cholesterin, 4 to 20 parts of sodium glycocholate, 60 to 200 parts of sorbitol and 5 to 20 parts of soyasterol. The solid preparation provided by the invention has high dissolubility, high stability, simple preparation method, high envelope rate, uniform particle size and long remaining time in body, thus the quality of preparation product is enhanced, the bioavailability is raised and the toxic and side effects are reduced.

Description

technical field [0001] The invention relates to a liposome solid preparation, in particular to a liposome solid preparation of torasemide and a preparation method thereof, including tablets, capsules, granules and dispersible tablets, belonging to the technical field of medicine. Background technique [0002] Torsemide, chemical name N-[[(1-methylethyl)amino]carbonyl]-4-[(3-methylphenyl)amino]-3-pyridinesulfonamide, 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 c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/00A61K9/20A61K9/16A61K9/48A61K31/44A61K47/28A61P7/10
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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