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Oral insulin micelle nanoparticles and preparation method thereof

A micellar nano-insulin technology, applied in the direction of capsule delivery, microcapsules, nanocapsules, etc., can solve the problems of inconvenient drug delivery, hypertrophic malnutrition of subcutaneous fat, etc., and achieve obvious acid-base sensitivity, critical glue Low beam concentration, avoiding the effect of release absorption

Inactive Publication Date: 2018-09-04
XIANGTAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method of administration is extremely inconvenient, and it needs to be administered several times a day. Long-term injection will bring great pain to the patient, and complications such as hypoglycemia reaction, atrophy of subcutaneous fat, and hypertrophic malnutrition will occur. Drugs can avoid these problems, and it is convenient to adjust the dosage according to the patient's condition

Method used

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  • Oral insulin micelle nanoparticles and preparation method thereof
  • Oral insulin micelle nanoparticles and preparation method thereof
  • Oral insulin micelle nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 1. Preparation of Insulin Micellar Nanoparticles

[0036] Polymer P(MMA30 -co-MAA 35 )-b-PPEGMA 19 (average molecular weight 91792) 30mg was dissolved in 20ml of organic solvent N,N-dimethylformamide, mixed and stirred at 25°C for 15h according to the mass ratio of 0.005:1 to form a polymer solution; 5mg of insulin was dissolved in a concentration of 0.0001mol 10ml of medicinal hydrochloric acid solution per L was made into insulin acid solution at a mass ratio of 0.001:1; under stirring at 25°C, the insulin solution and the polymer solution were fully mixed for 30 minutes, and then the polymer micelle solution was transferred into In the dialysis bag (molecular weight cut-off MWCO=7000D), dialyze with the acetic acid-sodium acetate buffer solution of pH=5.0 for 24h, to remove the organic solvent and unloaded free drug in the micelle solution, wherein polymer micelle solution and acetic acid - The volume ratio of sodium acetate buffer solution is 1:50. During the dial...

Embodiment 2

[0052] Embodiment 2 operation steps are with embodiment 1, polymer P (MMA 30 -co-MAA 35 )-b-PPEGMA 19 (Average molecular weight=91792) 100mg is dissolved in organic solvent N, N-dimethylformamide 20ml when preparing according to the mass ratio of 0.0105:1, the polymer appears a large amount of coagulation, can not form micelles and particle diameter reaches 1586nm, potential -40mV.

Embodiment 3

[0053] Example 3 The operation steps are the same as in Example 1, the dialysis bag is replaced with a dialysis bag with a molecular weight cut-off of 14000D, the potential of the obtained insulin-loaded nanomicelle is -20.2mV, the particle size is 172.6nm, the mass percentage of drug loading is 9.2%, the mass The encapsulation efficiency is 87.4%.

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Abstract

The invention discloses oral insulin micelle nanoparticles and a preparation method thereof. The preparation method comprises the following steps: dissolving an amphiphilic block copolymer with pH (Potential of Hydrogen) sensitivity, i.e., [poly(methyl methacrylate-co-methacrylate)-b-monomethoxypolyethylene glycol polymethacrylate P(MMA-co-MAA)-b-PPEGMA], into an organic solvent; dissolving insulin into a diluted acid solution with the concentration of 0.0001mol / L; then slowly dropwise adding an insulin solution into a polymer solution; sufficiently stirring; then transferring a mixed solutioninto a dialysis bag and dialyzing for 24 to 48h in the environment with the pH (Potential of Hydrogen) of 4.5 to 6.0; removing an organic solvent to form a polymer drug-loading micelle; centrifuging,freeing and drying to obtain the oral insulin micelle nanoparticles which have relatively uniform sizes, are micro-spherical and have the remarkable pH sensitivity and the quality entrapment rate of85 percent or above.

Description

technical field [0001] The invention relates to an oral insulin micelle nanoparticle and a preparation method thereof. Background technique [0002] Insulin is a protein peptide drug commonly used to treat diabetic patients. Direct oral administration will be hydrolyzed by protease in the human stomach, and it is difficult to reach the intestinal tract and enter the blood through the intestinal mucosa to play a role. Therefore, at present, subcutaneous injections are used clinically for administration. However, this method of administration is extremely inconvenient, and it needs to be administered several times a day. Long-term injection will bring great pain to the patient, and complications such as hypoglycemia reaction, atrophy of subcutaneous fat, and hypertrophic malnutrition will occur. Medicine can avoid these problems, and it is convenient to adjust the dosage according to the patient's condition. At present, oral insulin drugs have become a research hotspot. [...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K9/51A61K47/34A61P3/10
Inventor 吴志民陆腾飞熊迪刘跃进潘浪胜喻超段鳗珍李蓉
Owner XIANGTAN UNIV
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