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Salmon calcitonin-phospholipid complex and its lipid nanoparticle and preparation method

A technology of calcitonin phospholipid and salmon calcitonin, which is applied in the field of medicine, can solve the problems of poor fat solubility, low encapsulation rate, and low transmission rate, and achieve long-term storage and transportation and good long-term stability. Effect

Active Publication Date: 2016-09-07
CHENGDU UNIV
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Problems solved by technology

However, because salmon calcitonin is easily soluble in water and poor in fat solubility, the permeability on the cell membrane is low, and the encapsulation efficiency is low when it is directly prepared into nanoparticles
So far, there has been no report of making salmon calcitonin into phospholipid complexes and then making lipid nanoparticles to improve the oral bioavailability of salmon calcitonin

Method used

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Embodiment Construction

[0046] The above-mentioned content of the present invention will be further described in detail below through specific implementation in the form of examples, to illustrate but not limit the present invention.

[0047] Given that salmon calcitonin has poor fat solubility, poor transmembrane absorption, is easily degraded by proteolytic enzymes in the gastrointestinal tract, and is sensitive to the pH of the gastrointestinal tract, its oral bioavailability is low. The inventors overcome the problem by making lipid nanoparticles from salmon calcitonin into phospholipid complexes, lipid materials, surfactants and water through thin film dispersion. The above-mentioned defects have obtained salmon calcitonin-phospholipid complex lipid nanoparticles with advantages such as high oil-water partition coefficient of the drug, high mucosal permeability, good stability, and protection from protease degradation, which can improve oral bioavailability and purpose of clinical efficacy.

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Abstract

The invention belongs to the technical field of medicines and relates to a salmon calcitonin-phospholipid complex and its lipid nanoparticle and preparation method. The salmon calcitonin-phospholipid complex and its lipid nanoparticle can improve drug lipid solubility, have a certain intestinal adhesion, can be easily absorbed through intestinal mucosa and can prevent drug degradation caused by gastrointestinal tract protease. The lipid nanoparticle of the salmon calcitonin-phospholipid complex comprises the salmon calcitonin-phospholipid complex, a lipid material, a surfactant and water and is prepared through a film dispersion method. The water-soluble drug nanoparticle obtained through the preparation method has a high drug oil-liquid distribution coefficient and good membrane permeability and improves oral bioavailability. The preparation method has simple processes.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a salmon calcitonin-phospholipid complex, lipid nanoparticles and a preparation method thereof. Background technique [0002] Calcitonin (calcitonin) is a hormone secreted by parafollicular cells in the thyroid gland. It is a polypeptide composed of 32 amino acids. It was first discovered and proved by Hirsh that it has the function of regulating calcium and phosphorus metabolism. Calcitonin takes bone as the target cell, and it can inhibit the proliferation of osteoclasts and prevent osteolysis after binding to the receptors on the surface of osteoclasts. According to different sources, calcitonin is divided into human, pig, salmon and eel calcitonin, among which salmon calcitonin has the highest specific activity, which is about 30 times that of human calcitonin, and has a long acting time and good stability , long half-life, small side effects, so salmon calciton...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K38/23A61K47/48A61K47/24A61P5/22A61P19/10A61P5/16A61P25/00A61P39/02
CPCA61K9/5123A61K38/23A61K47/24
Inventor 张颖王彩云高燕杜伟宏符海娟李佳
Owner CHENGDU UNIV
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