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A kind of chitosan nanoparticle and preparation method for improving oral colonic absorption of insulin

A technology of chitosan nanoparticles and insulin, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problems of insulin oral bioavailability, unstable nanoparticles, Inability to protect substances and other issues, to achieve good physical and chemical stability, protective activity, and increased interaction

Active Publication Date: 2018-06-15
江西省药物研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Literature (Journal of Applied Polymer Science, 1997, 63 (1): 125-132. International Journal of Pharmaceuticals, 2002, 249 (1-2): 139-147) reported that the shell wrapped with insulin was prepared by ion cross-linking Glycan nanoparticles, the nanoparticles prepared by this method are unstable in the gastric acid environment and cannot protect the substances they encapsulate
The literature (Journal of Shenyang Pharmaceutical University, 2006,23(2):65-69) reported that hydroxypropyl methylcellulose phthalate (HP55) was used to prepare chitosan nanoparticles loaded with Ins by ion cross-linking. enteric-coated capsules to improve the oral colonic absorption of insulin, but the oral bioavailability of insulin needs to be improved

Method used

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  • A kind of chitosan nanoparticle and preparation method for improving oral colonic absorption of insulin
  • A kind of chitosan nanoparticle and preparation method for improving oral colonic absorption of insulin
  • A kind of chitosan nanoparticle and preparation method for improving oral colonic absorption of insulin

Examples

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Embodiment 1

[0080] Take by weighing 8 mg of chitosan powder whose molecular weight is 100,000 Daltons and have a deacetylation degree of 95%, dissolve it in 0.2% acetic acid solution of 4 ml, adjust the pH value to 5.5 with 1mol / L sodium hydroxide solution, and call it Solution A. 2 mg of Tat (amino acid sequence GRKKRRQRRRP) was weighed, dissolved in solution A and called solution B, and solution B was stirred on a magnetic stirrer at room temperature. Weigh 4.2 mg of insulin, dissolve it in 2 mL of 0.1 mol / L hydrochloric acid solution, adjust the pH value to 8.0 with 1 mol / L sodium hydroxide solution, and call it solution C. Solution C was slowly added to solution B under stirring at room temperature, and stirring was continued for 1 hour to form solution D. Weigh 2.3 mg of sodium tripolyphosphate and dissolve it in 2 mL of distilled water and call it solution E. Slowly add solution E to solution D while stirring at room temperature, and continue stirring for 0.5 hours to form nanopart...

Embodiment 2

[0082]Take by weighing 8 mg of chitosan powder with a molecular weight of 50,000 Daltons and a degree of deacetylation of 85%, dissolve it in 0.2% acetic acid solution of 4 ml, adjust the pH value to 6.0 with 1mol / L sodium hydroxide solution, called Solution A. 2.3 mg of Tat (amino acid sequence GRKKRRQRRRP) was weighed, dissolved in solution A and called solution B, and solution B was stirred on a magnetic stirrer at room temperature. Weigh 4 mg of insulin, dissolve it in 2 mL of 0.1 mol / L hydrochloric acid solution, adjust the pH value to 8.0 with 1 mol / L sodium hydroxide solution, and call it solution C. Solution C was slowly added to solution B under stirring at room temperature, and stirring was continued for 1 hour to form solution D. Weigh 2 mg of sodium tripolyphosphate and dissolve it in 2 mL of distilled water and call it solution E. Slowly add solution E to solution D while stirring at room temperature, and continue stirring for 0.5 hours to form nanoparticle suspe...

Embodiment 3

[0084] Take by weighing 8 mg of chitosan powder whose molecular weight is 100,000 Daltons and whose degree of deacetylation is 85%, dissolve it in 4 ml of 0.2% acetic acid solution, adjust the pH value to 5.5 with 1mol / L sodium hydroxide solution, called Solution A. 2 mg of Tat (amino acid sequence GRKKRRQRRRP) was weighed, dissolved in solution A and called solution B, and solution B was stirred on a magnetic stirrer at room temperature. Weigh 4 mg of insulin, dissolve it in 2 mL of 0.1 mol / L hydrochloric acid solution, adjust the pH value to 8.0 with 1 mol / L sodium hydroxide solution, and call it solution C. Solution C was slowly added to solution B under stirring at room temperature, and stirring was continued for 1 hour to form solution D. Weigh 2.3 mg of sodium tripolyphosphate and dissolve it in 2 mL of distilled water and call it solution E. Slowly add solution E to solution D while stirring at room temperature, and continue stirring for 0.5 hours to form nanoparticle ...

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Abstract

The invention relates to a chitosan nanoparticle coated with an enteric-coated material and wrapped with insulin and a cell-penetrating peptide Tat and a preparation method thereof. prepared from chitosan. After oral administration of the prepared enteric-coated insulin-chitosan nanoparticles, the protective effect of the enteric-coated material Eudragit S100 can greatly reduce the release of the loaded contents of the chitosan nanoparticles in the stomach and upper small intestine. quantity. When the chitosan nanoparticles reach the lower end of the digestive tract, due to the rise of the pH value, the enteric coating material on the surface of the chitosan nanoparticles begins to dissolve and expose the chitosan nanoparticles. It is destroyed under certain conditions, thereby releasing the cell-penetrating peptide and insulin inside. Cell-penetrating peptides promote the absorption of insulin by colonic epithelial cells, thereby increasing the oral bioavailability of insulin.

Description

technical field [0001] The invention relates to nanometer particles that can be used in the technical field of biomedicine and a preparation method thereof, in particular to a chitosan nanoparticle that improves oral colonic absorption of insulin and a preparation method thereof. Background technique [0002] Insulin is widely used clinically to treat type Ⅰ diabetes, and its main mode of administration is subcutaneous injection. Diabetic patients need to inject insulin (Ins) multiple times a day in order to control their blood sugar levels, which brings great pain to the patient's body and mind and many inconveniences in daily life. The oral drug delivery system is considered to be the most compliant, natural and safest drug delivery method for patients, but the oral bioavailability of insulin is very low and basically has no pharmacological effect. The main reasons are: first, insulin is easily degraded and inactivated by acid and enzymes in the digestive tract; second, i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/28A61K47/38A61K9/51A61K47/32A61P5/48A61K38/08
Inventor 钟海军陈双喜罗荣余华邓泽元
Owner 江西省药物研究所
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