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PH response insulin slow release nanoparticle, and preparation method and application thereof

A technology of insulin and nanoparticles, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients. The effect of reducing the amount of drug release and reducing the number of injections

Inactive Publication Date: 2017-04-26
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Huynh et al. used the characteristics of polyurethane to form cations at low pH and low temperature combined with negatively charged INS, and easily lose protons to form insoluble blocks at high pH and high temperature, and prepared a temperature-controlled slow-release injection gel with pH sensitivity. Gel, the drug-loaded gel can be sustained release in vitro for 15 days, a single injection can maintain the normal level of blood sugar in rats within a week, but its encapsulation rate is low and the injection process is easy to cause blockage

Method used

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  • PH response insulin slow release nanoparticle, and preparation method and application thereof
  • PH response insulin slow release nanoparticle, and preparation method and application thereof
  • PH response insulin slow release nanoparticle, and preparation method and application thereof

Examples

Experimental program
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Embodiment 1 3

[0045] Synthesis of embodiment 1 triblock polymer mPEG-PCL-PDEAEMA

[0046] 1. Synthesis of mPEG-PCL-OH

[0047] By ring-opening polymerization. Accurately weigh an appropriate amount of mPEG5000 and ε-CL (w:w, 1:2-2.6), place it in a 50ml dry round bottom flask, and add 1% ε-CL molar mass of Sn(oct) 2 As a catalyst, react in a nitrogen environment at 130°C for 24 hours. After the reaction, add an appropriate amount of DCM to dilute, precipitate in excess glacial ether, filter with suction, collect the precipitate, and add an appropriate amount of DCM to re-dissolve. The above operation was repeated twice to obtain a white powdery product, which was vacuum-dried at 40° C. to constant weight.

[0048] 2. Synthesis of macromolecular initiator mPEG-PCL-Br

[0049] Accurately weigh an appropriate amount of the above product mPEG-PCL-OH in a 50ml dry round bottom flask, add an appropriate amount of DCM to dissolve, and add TEA and BiBB in proportion to the ice-water bath (w:w:w,...

Embodiment 2

[0052] The characterization of embodiment 2 polymer

[0053] 1 Fourier Transform Infrared Spectroscopy (FT-IR) Characterization

[0054] Grind an appropriate amount of the product to be tested and dried potassium bromide into powder at room temperature, take an appropriate amount of powder for tableting, and scan 400-4 000 cm -1 Wavenumber Absorption Spectrum.

[0055] Analysis of FT-IR spectrum results

[0056] figure 2 All spectra in 1109cm -1 There is a stretching vibration peak of the C-O bond of the mPEG segment at 1724cm -1 There is a stretching vibration peak of the C=O bond of the PCL chain segment at 2878cm -1 There are mPEG segments and PCL segments at -CH 2 The stretching vibration peak of - indicates the successful synthesis of mPEG and PCL. Due to the small proportion of -C-Br- in mPEG5k-PCL10k-Br, the figure 2 -A and figure 2 -B difference is not obvious. figure 2 -C at 2776cm -1 and 2834cm -1 The unique methyl and methylene stretching peaks of PD...

Embodiment 3

[0067] Example 3 Preparation of polymer-loaded INS nanoparticles

[0068] Polymer nanoparticles were prepared by nanoprecipitation technique. Accurately weigh an appropriate amount of INS and dissolve it in 6ml of 0.01mol / L HCl solution, and adjust its pH value to 6.0 with 1mol / L NaOH solution under the detection of a pH meter. Fully dissolve 6 mg of the polymer in 0.6 ml of tetrahydrofuran, slowly add it dropwise into the above solution under stirring, and stir overnight in a fume hood at room temperature to evaporate the tetrahydrofuran. Centrifuge at 14,000 rpm for 30 min at 4°C, collect the precipitate, wash with deionized water three times, and freeze-dry to obtain polymer-loaded INS nanoparticles. Polymer blank nanoparticles were prepared in the same way.

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Abstract

The invention relates to a pH response insulin slow release nanoparticle, and a preparation method and an application thereof, and concretely discloses a triblock copolymer. The triblock copolymer is an A-B-C block copolymer, wherein the A block is biodegradable polyethylene glycol monomethyl ether, and the molecular weight is 4000-6000; the B block is polycaprolactone, and the molecular weight is 8000-15000; and the C block is N,N-diethylaminoethyl polybasic polymethacrylate, and the molecular weight is 8000-12000. The pH response insulin slow release nanoparticle is formed by a nanocapsule formed by self-assembling the triblock polymer and insulin loaded on the nanocapsule. The nanoparticle can accurately deliver drugs according to different pH values, and can simultaneously reach sustained and controlled release effects.

Description

technical field [0001] The invention belongs to the technical field of preparation of pharmaceutical dosage forms and nano medicines, in particular to a medicine loaded with insulin by a triblock polymer. Background technique [0002] Insulin (INS) is the drug of choice for the treatment of type 1 diabetes. However, INS has defects such as fast metabolism and elimination in the body, easy to be destroyed and degraded by strong acids, alkalis, and digestive enzymes in the gastrointestinal tract, and low bioavailability. If the fluctuation is too large, it will bring life danger to the patient. In recent years, in order to achieve the purpose of increasing the gastrointestinal stability of INS, improving bioavailability, prolonging the hypoglycemic time in vivo, and reducing the number of administrations, natural biodegradable polymer materials with good biocompatibility such as alginate , hyaluronic acid, chitosan and its derivatives, and synthetic biodegradable polymer mat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K47/69A61K47/59A61P3/10C08F293/00C08F220/34C08G63/664
CPCA61K38/28C08F220/34C08F293/00C08G63/664
Inventor 曾庆冰吴蕾朱雯婷王俊刘杰
Owner SOUTHERN MEDICAL UNIVERSITY
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