Ligand used together with protein type medicinal active component and oral protein type medicine preparation

Abstract

The invention relates to ligand used together with a protein type medicinal active component. The ligand is composed of taurocholic acid and glycocholic acid. The invention further provides an oral protein type medicine preparation. Specifically, the preparation is composed of a combined substance of the ligand and the protein type medicinal active component as a center which is wrapped with nano-liposomes. Due to the adoption of a nano-liposome wrapping layer, protection on a core structure can be improved, in addition, when the active component is insulin, phosphorus ions can be provided forself phosphorylation when insulin plasmid is in contact with a receptor. The oral protein type medicine preparation which is provided by the invention and has the insulin as the active component is capable of regulating blood sugar and blood fat, mainly has the effect of preventing complications of type-II diabetes, has bioavailability higher than that of injected insulin, causes no hypoglycemia,and in addition causes no brain death because of hypoglycemia; due to an orally taken mode, the preparation is convenient to administrate, the blood sugar is stable after administration, the inner environment of a body is stabilized, and good and wide application prospects can be achieved.

Description

technical field

[0001] The invention relates to the field of protein drugs, in particular to a ligand used in combination with protein drug active ingredients and an oral protein drug preparation. Background technique

[0002] At present, protein drugs are widely used in the diagnosis and treatment of diseases, but if they are administered orally, they are easily metabolized by enzymes in the digestive tract and lose their activity. Therefore, at present, most protein drugs are difficult to be made into oral preparations, and are mostly used in the form of injections.

[0003] Among them, oral insulin has been developed for nearly half a century, but no one has been listed yet. There are two main reasons: 1. As a protein, insulin cannot pass through the powerful protease degradation system in the digestive tract; 2. Insulin cannot enter the blood through the small intestine wall. Therefore, it is considered that the development of an oral formulation of insulin is extremel...

Examples

Embodiment 1

[0034] This example provides a ligand used in combination with protein-based pharmaceutical active ingredients, the ligand is composed of taurocholic acid and glycocholic acid at a mass ratio of 1:1.

Embodiment 2

[0036] This example provides a ligand used in combination with protein-based pharmaceutical active ingredients, the ligand is composed of taurocholic acid and glycocholic acid at a mass ratio of 1:2.

Embodiment 3

[0038] This example provides a ligand used in combination with protein-based pharmaceutical active ingredients, the ligand is composed of taurocholic acid and glycocholic acid at a mass ratio of 1:4.

technical field

[0001] The invention relates to the field of protein drugs, in particular to a ligand used in combination with protein drug active ingredients and an oral protein drug preparation. Background technique

[0002] At present, protein drugs are widely used in the diagnosis and treatment of diseases, but if they are administered orally, they are easily metabolized by enzymes in the digestive tract and lose their activity. Therefore, at present, most protein drugs are difficult to be made into oral preparations, and are mostly used in the form of injections.

[0003] Among them, oral insulin has been developed for nearly half a century, but no one has been listed yet. There are two main reasons: 1. As a protein, insulin cannot pass through the powerful protease degradation system in the digestive tract; 2. Insulin cannot enter the blood through the small intestine wall. Therefore, it is considered that the development of an oral formulation of insulin is extremel...

Examples

Embodiment 1

[0034] This example provides a ligand used in combination with protein-based pharmaceutical active ingredients, the ligand is composed of taurocholic acid and glycocholic acid at a mass ratio of 1:1.

Embodiment 2

[0036] This example provides a ligand used in combination with protein-based pharmaceutical active ingredients, the ligand is composed of taurocholic acid and glycocholic acid at a mass ratio of 1:2.

Embodiment 3

[0038] This example provides a ligand used in combination with protein-based pharmaceutical active ingredients, the ligand is composed of taurocholic acid and glycocholic acid at a mass ratio of 1:4.

Images