TAK-438 liposome and preparation method and application thereof

A TAK-438, liposome technology, applied in the directions of liposome delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve problems such as inability to use TAK-438 tablets, and achieve good antacid effect, Ease of operation, high solubility and bioavailability

Active Publication Date: 2015-11-25
SHOUGUANG FUKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present invention aims at the problem that patients with gastric acid-related diseases cannot use TAK-438 tablets, and provides a TAK-438 liposome

Method used

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  • TAK-438 liposome and preparation method and application thereof

Examples

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Embodiment 1

[0038] The present embodiment provides a TAK-438 liposome, comprising the following raw materials in parts by mass: lecithin 60mg, cholesterol 10mg, film-forming solvent 10mL, TAK-4381mg, buffer 40mL, the film-forming solvent is chloroform, the The buffer solution is a phosphate buffered saline solution, and the pH value of the phosphate buffered saline solution is 7.4.

[0039] Specifically include the following steps:

[0040] (1) Add 60mg lecithin and 10mg cholesterol into the reactor;

[0041] (2) Add 10mL of film-forming solvent and methanol solution containing TAK-4381mg to the above reactor to obtain a mixed solution, in which the mass ratio of TAK-438 to methanol is 1:1;

[0042] (3) Evaporate the solvent in the mixed solution to form a film, then add 40 mL of buffer solution, and rotate for 20 minutes with a rotary evaporator to obtain TAK-438 liposomes;

[0043] (4) Stir the TAK-438 liposomes for 3 hours, sonicate for 3 minutes; then filter through a 0.8um filter m...

Embodiment 2

[0055] This embodiment provides a TAK-438 liposome, the preparation method of which is similar to that of Example 1, the only difference being that the mass parts of raw materials are as follows: 25 parts of soybean lecithin, 5 parts of cholesterol, and 8 parts of film-forming solvent , 0.5 parts of TAK-438, 20 parts of buffer.

Embodiment 3

[0057] This embodiment provides a TAK-438 liposome, the preparation method of which is similar to that of Example 1, the only difference being that the mass parts of raw materials are as follows: 80 parts of soybean lecithin, 25 parts of cholesterol, and 258 parts of film-forming solvent , 2.5 parts of TAK-438, 60 parts of buffer.

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Abstract

The invention provides a TAK-438 liposome which comprises the following raw materials in parts by mass: 25-80 parts of lecithin or soybean lecithin, 5-25 parts of cholesterol, 8-25 parts of a film forming solvent, 0.5-2.5 parts of TAK-438 and 20-60 parts of a buffer solution. The raw materials used by the TAK-438 liposome provided by the invention are non-toxic and easy to obtain, the TAK-438 liposome has high stability, the solubility and bioavailability of medicines in the liposome are high, and the anti-acid effect of TAK-438 in the liposome can be better exerted. The TAK-438 liposome provided by the invention is simple in preparation method, simple and convenient to operate, and easy to realize industrial production. The TAK-438 liposome provided by the invention is suitable for inhibiting gastric acid related diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a TAK-438 liposome and its preparation method and application. Background technique [0002] Acid-related diseases (ARDs) are upper gastrointestinal diseases whose pathogenesis is closely related to gastric acid, and can be divided into the following categories according to the types of onset: food reflux to the gastrointestinal tract, indigestion, gastrointestinal inflammatory symptoms, Zollinger-Ellison syndrome (also known as "Zollinger-Ellison syndrome") and gastrointestinal diseases caused by non-steroidal anti-inflammatory drugs. The incidence of ARDs is increasing year by year, especially in my country, such diseases have become very serious diseases, which greatly reduce the quality of life of patients with gastric acid-related diseases, and cause economic losses to ARDs patients. It's a big burden. [0003] Proton pump inhibitors-PPIs have some ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4439A61P1/04
Inventor陈大全宋成刚王中华秦杰子王伟郝冠华宋伟国李金艳王福洲朱素美
OwnerSHOUGUANG FUKANG PHARMA