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Oral insulin liposome hydrogel and application thereof

An insulin and liposome technology, applied in the field of insulin pharmacy, can solve the problems of easy degradation, poor absorption, and low bioavailability of oral insulin, and achieve the effects of high stability, improved protection, and prolonged residence time.

Pending Publication Date: 2022-07-22
HEFEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a kind of oral insulin liposome hydrogel and preparation method, in order to solve the technical problem that oral insulin is easily degraded, absorbs poorly, and bioavailability is low

Method used

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  • Oral insulin liposome hydrogel and application thereof
  • Oral insulin liposome hydrogel and application thereof
  • Oral insulin liposome hydrogel and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Preparation of modified sodium alginate

[0049] Dissolve 1 g of sodium alginate (Alg) in deionized water at a concentration of 20 mg / mL, add NHS and EDC to activate the carboxyl group for 10 min according to the ratio in Table 1, then add cysteine ​​hydrochloride, and stir for 5 After the reaction, the insulin complex was put into a dialysis bag, dialyzed twice with 5 mM HCl solution, 5 mM HCl solution containing 0.9 wt% NaCl, and 1 mM HCl at 4 °C in the dark, and then the pH was adjusted to 4.5 and then freeze-dried. , to obtain modified sodium alginate (cysteine-sodium alginate modification) (Cys-Alg for short).

[0050] Table 1

[0051]

Embodiment 1

[0053] The modified sodium alginate (Cys-Alg) obtained in Example 1 was subjected to Fourier transform infrared spectroscopy, hydrogen nuclear magnetic resonance spectroscopy, elemental analysis and sulfhydryl content determination:

[0054] Fourier transform infrared spectroscopy: Sodium alginate (Alg), cysteine ​​(Cys) and modified sodium alginate (Cys-Alg) were lyophilized and analyzed by ATR-FTIR (Waltham, MA, USA). The frequency range of ATR-FTIR is 4000cm -1 -600cm -1 , the resolution is 4cm -1 , a total of 16 scans, the results are as follows figure 1 shown.

[0055] Hydrogen nuclear magnetic resonance spectrum: Dissolve Alg, Cys-Alg modification and Cys in deuterium oxide (D2O), use AgilentVNMRS600 600Hz 1H NMR instrument to measure 1H nuclear magnetic resonance spectrum, the number of scans is 256 times, its structure is as follows figure 1 shown.

[0056] Depend on figure 1 and 2 It can be seen that after sodium alginate is modified by cysteine, at 3284cm -1 ...

Embodiment 3-1

[0064] Preparation of insulin-loaded liposome hydrogels:

[0065] Step 1. Dissolve insulin in 10 mM HCl at a concentration of 2 mg / mL, and adjust the pH of the solution to 7.4 to obtain solution A; dissolve arginine in deionized water at a concentration of 6 mg / mL, and adjust the pH of the solution to 7.4 , to obtain solution B; filter solution A and solution B with 0.22 μm filter membrane respectively, and then mix the two solutions obtained after filtration according to the volume ratio of 1:1 to obtain insulin complex;

[0066] Step 2. Dissolve 10 mg of phosphatidylethanolamine and 3 mg of cholesterol in 10 mL of chloroform to obtain solution C, take 2 mL of chloroform and add 4 mL of insulin complex to obtain solution D; after solution C and solution D are mixed uniformly in a volume ratio of 1:1 , carried out rotary evaporation under reduced pressure, after the completion, the liposome solution was ultrasonicated for 2 minutes and squeezed with a 0.22 μm filter membrane f...

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Abstract

The invention discloses oral insulin liposome hydrogel and application thereof, and belongs to the technical field of insulin pharmacy. The oral insulin liposome hydrogel comprises an insulin-loaded liposome and a hydrogel with a core-shell structure formed by modified sodium alginate, the core is the insulin-loaded liposome, and the shell is a hydrogel framework formed by the modified sodium alginate; the insulin-loaded liposome is formed by mixing an insulin compound, phosphatidyl ethanolamine and cholesterol in an organic solvent, the particle size of the insulin-loaded liposome is 100-200 nm, and the PD I value of the insulin-loaded liposome is 0.1-0.4; the modified sodium alginate is obtained by reacting sulfydryl-containing amino acid with sodium alginate. Comprising the oral insulin liposome hydrogel prepared by the invention can be orally administered to a patient, and compared with injection, the oral insulin liposome hydrogel has the advantages that the pain of the patient is small, repeated administration is not needed, and the blood sugar control is stable; the hypoglycemic effect is good, the hypoglycemic duration is long, the effect is remarkable, and the bioavailability of insulin is high.

Description

technical field [0001] The invention belongs to the technical field of insulin pharmacy, in particular to an oral insulin liposome hydrogel and its application. Background technique [0002] At present, insulin is the most effective way to lower blood sugar levels. The most common route of administration is injection, but it also brings side effects such as injection pain, wound ulceration, and lipoatrophy. Oral administration of insulin is preferable to injection because oral administration is more acceptable and avoids serious side effects and complications. Although oral administration is a better route for insulin delivery in vivo, it still faces challenges such as the acidic environment in the stomach, digestive enzymes in the gastrointestinal tract, mucus layer penetration, and epithelial cell absorption. Changes in pH in the gastrointestinal tract, and various digestive enzymes, including the acidic environment in the stomach (pH 1.2-2.0) and pepsin and trypsin in th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K9/06A61K9/127A61K9/00A61K47/54A61K47/24A61K47/28A61K47/36A61K47/18A61P3/10
CPCA61K38/28A61K9/06A61K9/127A61K9/0053A61K47/542A61K47/24A61K47/28A61K47/36A61K47/183A61P3/10
Inventor 李井雷吴海山程浩然国婷南剑张温清
Owner HEFEI UNIV OF TECH
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