Semaglutide liposome and preparation method thereof

A technology of samoglutide fat and samoglutide, which is applied in the field of medicine, can solve the problems of low bioavailability, strong side effects, instability of samoglutide, etc., and achieve the effect of reducing permeability, high encapsulation rate and avoiding aggregation

Inactive Publication Date: 2014-09-24
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, samoglutide is unstable in the human bod...

Method used

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  • Semaglutide liposome and preparation method thereof
  • Semaglutide liposome and preparation method thereof
  • Semaglutide liposome and preparation method thereof

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preparation example Construction

[0063] The preparation method of the samoglutide liposome provided by the invention can adopt the film dispersion method.

[0064] The preparation method of the samoglutide liposome provided by the invention comprises the following steps: after taking phospholipids and cholesterol and dissolving them in chloroform, removing the chloroform by rotary evaporation, adding PBS buffer solution containing samoglutide, and mixing with pharmaceutically acceptable The aqueous solution of the lyoprotectant is mixed and freeze-dried to obtain the product.

[0065] The particle size of the samorutate liposome prepared by the film dispersion method is 50nm-200nm.

[0066] The mass ratio of phospholipids, samoglutide, cholesterol and pharmaceutically acceptable cryoprotectant in the PBS buffer containing samoglutide prepared by the thin film dispersion method is (0.001~5): (0.1~ 500): (0.01~50): (0.01~100).

[0067] The molar-volume concentration of phosphate is 0.01 mol / L, and the pH valu...

Embodiment 1

[0100] Embodiment 1 film dispersion method prepares Samolutai liposome

[0101] Weigh each component:

[0102] Samorutai

7mg

Dipalmitoylphosphatidylcholine (DPPC)

700mg

cholesterol

70mg

Mannitol

70mg

[0103] Take 700mg of dipalmitoylphosphatidylcholine (DPPC) and 70mg of cholesterol in a round bottom flask, add 10mL of chloroform and stir to dissolve, then remove the chloroform by vacuum evaporation, and form a uniform and transparent film on the wall; under the protection of nitrogen, in Add 200 μL of isotonic PBS buffer solution (pH6.5, 0.01mol / L phosphate) into the round bottom flask, containing 7 mg of samoglutide, stir for 4 minutes, and place it at 25 °C for 2 hours to make the film fully swell; Stir at 25°C for 2 hours to obtain a large unilamellar liposome suspension; pass the resulting large unilamellar liposome suspension through a high-pressure milk homogenizer twice, and filter through a 0.20 μm microporous me...

Embodiment 2

[0105] Embodiment 2 thin film dispersion method prepares Samolutai liposome

[0106] Weigh each component:

[0107] Samorutai

70mg

Dipalmitoylphosphatidylcholine (DPPC)

2g

cholesterol

200mg

Mannitol

100mg

[0108] Take 2 g of dipalmitoylphosphatidylcholine (DPPC) and 200 mg of cholesterol in a round-bottomed flask, add 50 mL of chloroform and stir to dissolve, remove the chloroform by vacuum evaporation, and form a uniform and transparent film on the wall; under the protection of nitrogen, in Add 2mL of isotonic PBS buffer solution (pH6.5, 0.01mol / L phosphate) into the round bottom flask, containing 70mg of samoglutide, stir for 4min, and place it at 25°C for 2 hours to make the film fully swell; Stir at 25°C for 2 hours to obtain a large unilamellar liposome suspension; pass the obtained liposome suspension twice through a high-pressure homogenizer, and filter through a 0.20 μm microporous filter membrane to obtain a smal...

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Abstract

The invention relates to the technical field of medicine, and especially relates to semaglutide liposome and a preparation method thereof. The semaglutide liposome provided in the invention comprises phospholipid, semaglutide, cholesterol and a pharmaceutically-acceptable cryoprotectant, and has a particle size of 50 nm-200 nm. The semaglutide liposome provided in the invention adopts phospholipid and cholesterol as membrane materials, and semaglutide is wrapped in the membrane materials to form liposome with negative charges. Therefore, the damage of semaglutide to pancreas and kidney is reduced; the gastrointestinal reaction after semaglutide administration is alleviated; and the stability and bioavailability of semaglutide are improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a liposome of samoglutide and a preparation method thereof. Background technique [0002] Diabetes can be divided into 4 types: Type I diabetes, Type II diabetes, other types of diabetes, and gestational diabetes. Among them, type II diabetes is the most common, also known as non-insulin-dependent diabetes, and the causes of type II diabetes are low B cell function, relative lack of insulin and insulin resistance. In recent years, the prevalence of type II diabetes has gradually increased. According to the World Health Organization's forecast, by 2030, there will be 300 million type II diabetes patients worldwide. [0003] At present, the therapeutic drugs for type II diabetes mainly include insulin and oral hypoglycemic agents, such as metformin, acarbose, glipizide, and repaglinide. Although these drugs can effectively lower blood sugar and improve patients' symptoms, these ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K38/17A61P3/10
Inventor 徐春莲郑春莲刘建马亚平袁建成
Owner HYBIO PHARMA
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