Solid preparation of Torasemide liposome

A technology of torasemide fat and solid preparations, which is applied in the field of medicine, can solve the problems of no improvement in the solubility and stability of torasemide, the increase of related substances, and the decrease of drug content, so as to improve bioavailability and reduce toxic and side effects Low, the effect of improving stability

Inactive Publication Date: 2011-06-01
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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

Examples

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preparation example Construction

[0070] On the other hand, the present invention provides the preparation method of above-mentioned torasemide liposome, and 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) placing the above-mentioned lipid solution in a flask, in a constant temperature water bath at 35-40 °C, removing ethanol by rotary evaporation, and forming a uniform lipid film on the bottle wall;

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

[0074] (4) The above suspension is filtered through a microporous filter membrane with a pore size of 0.45 μm, and spray-dried to obtain torasemide proliposome powder.

[0075] The torasemide liposome prepared by the method provi...

Embodiment 1

[0099] Example 1 Preparation of torasemide liposome tablet

[0100] The raw 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] Sodium Carboxymethyl Starch 10g

[0110] Povidone K30 10g

[0111] Magnesium Stearate 4g

[0112] Preparation Process:

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

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

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

Embodiment 2

[0120] Example 2 Preparation of torasemide liposome tablets

[0121] The raw 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] Sodium Carboxymethyl Starch 5g

[0131] Povidone K30 5g

[0132] Magnesium Stearate 2g

[0133] Preparation Process:

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

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

[0136] (3) 20g of sorbitol was dissolved in 200ml of water, slowly poured into the flask and shaken gently, so that the lipid film was eluted and dispersed in a hydrated m...

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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 torasemide liposome solid preparation 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 is 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 sulfonylurea pyridine diuretic, which mainly acts on the thick ascending branch of the loop of Henry's loop and inhibits Na + / K + / 2Cl - carrier system to make urinary Na + , K + , Cl - and water excretion but had no significant effect on glomerular filtration rate, renal plasma flow, or acid-base balance in the body. It is clinically used in patients with congestive heart failure, renal failure and edema caused by renal disease, an...

Claims

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Application Information

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Patent Type & Authority Applications(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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