Preparation method of stable nanometer suspensions of mederate hydrophobic medicine

A nanosuspension, hydrophobic drug technology, applied in pharmaceutical formulations, medical preparations of inactive ingredients, capsule delivery, etc., can solve the problems of high particle load and high stability of particle size that cannot be satisfied at the same time. , to achieve the effect of long dimensional stability, small average particle size and good stability

Active Publication Date: 2017-09-01
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, for small solute molecules with moderate or low hydrophobicity, the high loading capacit

Method used

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  • Preparation method of stable nanometer suspensions of mederate hydrophobic medicine
  • Preparation method of stable nanometer suspensions of mederate hydrophobic medicine
  • Preparation method of stable nanometer suspensions of mederate hydrophobic medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Preparation of 30 mL end-aminated mPEG- b -Suspension of PLGA-stabilized curcumin nanoparticles (containing 3 mgmPEG- b -PLGA and 3 mg curcumin):

[0026] At room temperature, take 3 mg of mPEG- b -PLGA, 3 mg curcumin (LogP is 3) and 3 mL tetrahydrofuran were thoroughly mixed to obtain a mixed solution, which was inhaled into a syringe.

[0027] Draw 3 mL of pH 9 water into another syringe of the same size.

[0028] Connect the two syringes and the two inlets of the mixer respectively, inject the two liquids into the mixer at a speed of 0.1 m / s at the same time, and the volume of the closed cavity of the mixer is about 30uL. The two-phase liquid is fully turbulently mixed in the mixer cavity, and the resulting emulsion flows out from the outlet of the mixer. Mixing takes about 3 seconds in total and the suspension is collected in a container.

[0029] Be that the water dilution suspension of 9 is to 5 times with pH, ​​and measure the particle size and di...

Embodiment 2

[0031] Example 2: Preparation of 30 mL hydroxyl-terminated mPEG- b - PLGA-stabilized suspension of curcumin nanoparticles (containing 3 mgmPEG- b -PLGA and 3 mg curcumin):

[0032] At room temperature, take 3 mg of hydroxyl-terminated mPEG- b -PLGA, 3 mg curcumin and 3 mL tetrahydrofuran were mixed thoroughly and inhaled into a syringe.

[0033] Draw 3 mL of pH 9 water into another syringe of the same size.

[0034] Connect the two syringes and the two inlets of the mixer with screw-on heads respectively, and inject the two liquids into the mixer at the same speed at the same time. The two-phase liquid is fully turbulently mixed in the mixer cavity, and the resulting emulsion flows out from the outlet of the mixer. Mixing took about 3 seconds in total. Collect the suspension in a container.

[0035] Be that the water dilution suspension of 9 is to 5 times with pH, ​​and measure the particle size and distribution of suspension with dynamic light scattering method, the res...

Embodiment 3

[0037] Example 3: Comparison of 30 mL end-aminated mPEG- b - Temporal stability of PLGA-stabilized curcumin nanoparticle suspension (containing 3 mg terminally aminated mPEG- b -PLGA, 3 mg curcumin or 3 mg aminated mPEG- b -PLGA, 0.6 mg curcumin)

[0038] At room temperature, take 3 mg of mPEG- b - PLGA, 3 mg or 0.6 mg curcumin and 3 mL tetrahydrofuran are thoroughly mixed and inhaled into a syringe.

[0039] Draw 3 mL of water of different pH values ​​into another syringe of the same size.

[0040] Connect the two syringes to the two inlets of the mixer, and simultaneously inject the two liquids into the mixer at a speed of 0.1 m / s. The two-phase liquid is fully turbulently mixed in the mixer cavity, and the resulting suspension flows out from the mixer outlet. Mixing took about 3 seconds in total. Collect the suspension in a container.

[0041] Dilute the suspension to 5 times with water of the same pH, and use the dynamic light scattering method to analyze the partic...

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Abstract

The invention relates to a preparation method of a nanometer suspensions of a moderate hydrophobic medicine, and belongs to the technical field of production of nanometer medicine agents. The preparation method comprises the following steps of dissolving the moderate hydrophobic medicine and a hydrophobic end functionalizing type amphiphilic block copolymer into an organic solvent which is mutually dissolved into water; quickly jetting and blending the solution and water with certain pH (potential of hydrogen) value, and enabling the medicine and the block copolymer to generate ionizing to produce opposite charges, so as to form a complex, thereby greatly reducing the apparent hydrophobic property of the medicine; instantaneously separating out together with the block copolymer, so as to prepare the nanometer suspensions of the medicine. The nanometer suspensions has the characteristics that the average particle size is small, the medicine carrying amount is overhigh, the size stabilizing time is long, and the single dispersivity is good.

Description

technical field [0001] The invention belongs to the technical field of production of nanomedicine. Background technique [0002] The preparation of nanoscale carriers with stable dimensions over time is a topic of common concern in many fields, especially some nanoscale carriers with ultra-high loading capacity. For example, in the field of pharmaceuticals, more than 40% of newly discovered organic drug small molecules have extremely low water solubility. Most of these hydrophobic drugs had to be abandoned due to the difficulty of administration. People often try to make these small molecules into nano-formulations to improve their dispersibility in water and increase their dissolution rate, thereby increasing their bioavailability. [0003] For common nanoscale carriers, such as micelles, vesicles, liposomes, etc., although they have good dimensional stability over time, due to the low thermodynamic solubility of hydrophobic drug molecules in the hydrophobic region inside...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/51A61K47/34A61K31/12
CPCA61K9/10A61K9/5153A61K31/12A61K47/34
Inventor 朱正曦徐鹏
Owner YANGZHOU UNIV
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