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Oral insulin nanometer granular preparation and method for preparing same

A nanoparticle and insulin technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of low bioavailability of insulin and easy to be trapped, and achieve good results. Hypoglycemic effect, blood sugar control, high bioavailability effect

Inactive Publication Date: 2018-08-07
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the strong interaction between mucus-adsorbing particles and mucus, the particles are easily trapped in the mucus layer, and are quickly cleared by the mucus layer, and cannot reach the epithelium of the small intestine, resulting in low bioavailability of insulin
Currently, there is still a lack of an insulin delivery system that can effectively overcome the mucus layer barrier in the small intestine

Method used

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  • Oral insulin nanometer granular preparation and method for preparing same
  • Oral insulin nanometer granular preparation and method for preparing same
  • Oral insulin nanometer granular preparation and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1 Synthesis of chitosan quaternary ammonium salt (HTCC)

[0061] 2g chitosan was dissolved in 100mL of 2wt% acetic acid solution, heated to 80 o After C, slowly drop 5mL glycidyltrimethylammonium chloride (GTMAC) aqueous solution into the solution, 80 o The reaction was carried out at C for 24 h, and the resulting solution was cooled and precipitated twice in 10 times the volume of acetone. The precipitate was redissolved in double distilled water, dialyzed against water for 3 days, and freeze-dried to obtain the final product HTCC. Among them, the mass concentration of GTMAC aqueous solution is 20%, and the degree of quaternization of HTCC is 43%. In addition, by adjusting the volume of GTMAC to 2mL or 4mL, HTCC with quaternization degrees of 12% and 23% could be obtained, respectively.

Embodiment 2

[0062] Example 2 Synthesis of thiolated hyaluronic acid (HA-SH)

[0063] 1. Dissolve hyaluronic acid (HA) in double distilled water at a concentration of 5mg / mL, add ion exchange resin (the mass ratio of resin to hyaluronic acid is 3:1), stir for 0.5h, filter off the resin, and use tetrabutylhydrogen The pH value of the solution was adjusted to 7.04 with ammonium oxide, and lyophilized to obtain the product HA-TBA.

[0064] 2. Dissolve HA-TBA (1.5g) in DMSO at a concentration of 0.5mg / mL, and add 4-dimethylaminopyridine (0.35g), dithiodipropionic acid (2.4g), di-tert-dicarbonate Butyl ester (0.2mL), react at 45°C for 20h. After cooling to room temperature, dialyze against double distilled water to remove DMSO, then precipitate twice in 10 times volume of acetone, dissolve in double distilled water, dialyze against water for 3 days, and freeze-dry. Dissolve the lyophilized product (0.5g) in double distilled water, adjust the pH to 8.5, add dithiothreitol (0.5g), react for 3h,...

Embodiment 3

[0065] Example 3 Preparation of nanoparticles using FNC technology

[0066] FNC technology is a technology for preparing drug-loaded nanoparticles through electrostatic interaction in water phase (recorded in the inventor's previous patent application number PCT / US2017 / 014080), and the preparation process is mainly carried out in a multi-entrance vortex mixer , with the characteristics of high throughput and strong controllability, the prepared nanoparticles are evenly distributed and small in particle size, and the difference between batches is small. Since there is no organic solvent involved in the whole process, it is especially suitable for the preparation of biological macromolecules such as proteins and nucleic acids. The multi-inlet vortex mixer ( figure 1 A, figure 1 B) comprising a first part at the top, a second part at the middle and a third part at the bottom, the first part, the second part and the third part are cylinders with the same diameter; the first part...

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Abstract

The invention belongs to the technical field of medicines, and particularly discloses an oral insulin nanometer granular preparation and a method for preparing the same. The oral insulin nanometer granular preparation is provided with core-shell structures. Cores of the oral insulin nanometer granular preparation are nanometer composite cores which comprise chitosan quaternary ammonium salt and insulin, and shells of the oral insulin nanometer granular preparation are hyaluronic acid or sulfhydrylation hyaluronic acid which is coated on the surfaces of the cores. The oral insulin nanometer granular preparation and the method have the advantages that nanometer grains are high in entrapment efficiency and / or medicine-loading rate and have small intestine mucus adhesion and penetration functions, accordingly, absorption of the insulin at small intestine positions can be improved, and the oral insulin nanometer granular preparation is high in oral bioavailability; blood glucose can be effectively controlled after the oral insulin nanometer granular preparation is orally taken, blood glucose change is stable as compared with subcutaneous injection, excellent blood glucose reducing effects can be realized by the oral insulin nanometer granular preparation, and the oral insulin nanometer granular preparation is high in bioavailability; the blood glucose can be effectively controlled,accordingly, unnecessary suffering of diabetes mellitus patients can be relieved to a great extent, and the oral insulin nanometer granular preparation is safe and convenient.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and more specifically relates to an oral insulin nanoparticle preparation and its preparation method and application. Background technique [0002] Insulin has been the drug of choice for patients with insulin-dependent diabetes since its inception. Insulin is mainly administered through the subcutaneous route, and long-term repeated administration is required, which causes great pain and low compliance for patients, and also causes a series of safety problems, such as allergic reactions, subcutaneous fat atrophy or hyperplasia, resistance Receptivity and so on. Compared with a series of problems caused by subcutaneous injection, oral administration is considered to be a more suitable route of administration. Oral administration can effectively reduce hyperinsulinemia, prevent body weight gain associated with systemic insulin therapy, and reduce the risk of hypoglycemia. At the same time, o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K9/51A61K47/36A61P3/10
CPCA61K38/28A61K9/0053A61K9/5161A61K9/5192A61K47/36A61P3/10
Inventor 刘志佳田厚宽陈永明毛海泉梁锦荣刘利新何治宇孙成新
Owner SUN YAT SEN UNIV
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