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Curcumin dicaprate suspension injection and preparation method and application thereof

A technology of dicaprate and injection, which is applied in the field of medicine, can solve the problems of low solubility, difficulty in injection, and low solubility of curcumin dicaprate, and achieve the effects of simple prescription, great practical value, and easy process

Inactive Publication Date: 2013-05-29
北京鼎国昌盛生物技术有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

From the physical and chemical properties of curcumin dicaprate, it can be seen that the solubility of curcumin dicaprate in water is much lower than that of curcumin in water, and the solubility of curcumin dicaprate in various organic solvents is not very high. It is very difficult to make injections

Method used

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  • Curcumin dicaprate suspension injection and preparation method and application thereof
  • Curcumin dicaprate suspension injection and preparation method and application thereof
  • Curcumin dicaprate suspension injection and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0021] The preparation of embodiment 1 curcumin dicaprate nanosuspension

[0022] The planetary ball mill of the present invention uses water for injection as the solvent for wet grinding, weighs 1.00 g of CurDD during grinding, adds 25 g of balls, adds 1 ml of aqueous solution containing 50 mg of poloxamer 401, and grinds for 1 hour at a rotating speed of 650 rpm in a parallel planetary ball mill Grind, add water after completion, transfer to clean vials several times, seal with tin foil, store at -80°C for 24 hours, and then put it in a freeze dryer. Program freeze-drying: pre-freeze at -45°C for 6 hours; Operate at -30°C for 18 hours, at -20°C for 5 hours, and at 0°C for 4 hours; perform secondary drying at 20°C for 4 hours to obtain a lyophilized powder. The obtained lyophilized powder is a yellow powdery solid with a good appearance, no collapse or shrinkage on the surface, and some small cracks. Accurately weigh 500 mg of freeze-dried nano-suspension particles, disperse...

Embodiment 2

[0024] Embodiment 2 curcumin dicaprate nanoparticles particle size distribution

[0025] Firstly, the optical path is calibrated before the experiment (for the light, the detection pool of the instrument is water), so that the background has no large interference peaks, and the laser intensity is detected (greater than 70). The grinding particles of the ball mill are evenly dispersed in the dispersant, and the particles are dispersed with each other by ultrasonic waves, and then added dropwise into the particle size distribution instrument that is ready to be measured until the shading degree reaches 5-10. After mixing and stirring for a period of time, press the Start key to start the instrument to measure the particle size distribution. The measurement principle is that the particles pass through the laser beam at a certain flow rate. Different particle sizes have different diffraction angles. The diffracted light is collected by a detector and the received signal is conve...

Embodiment 3

[0026] Embodiment 3 Curcumin Dicaprate Nanoparticle Morphological Observation

[0027] The particle morphology and particle size distribution observation of the curcumin dicaprate nano freeze-dried powder prepared in Experimental Example 1 was carried out with a scanning electron microscope. Particles were immobilized on metal sample pans and sprayed with gold (3nm). Depend on figure 2 It can be seen that the freeze-dried powder nanoparticles are spherical, and the particle size range is concentrated between 300-700nm, which is consistent with the particle size distribution measurement results.

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Abstract

The invention discloses curcumin dicaprate and a derivative nano suspension agent, a preparation method of freeze-dried powder thereof and an application in the treatment of depression and tumor. A surfactant serves as a main pharmaceutical adjunct, particularly poloxamer, and curcumin dicaprate nano granulation is successfully realized by employing the wet grinding combined freeze drying technology. The curcumin dicaprate is prepared into a pharmaceutically acceptable oil diluent, and the reconstructed curcumin dicaprate and derivative nano suspension agent can be prepared into a nano suspension agent for injection with the particle size of about 500nm. The nano suspension agent consists of the following components: curcumin dicaprate and / or derivatives thereof and the surfactant. The nano suspension agent preparation can be applied to treating depression and tumors. The nano suspension agent preparation is simple in composition, high in stability, high in needle penetration, economic and reliable in preparation method and easy to industrialize.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a curcumin dicaprate suspension injection capable of long-acting sustained release, a preparation method and an application thereof. Background technique [0002] Nanosuspension refers to a suspension formed by dispersing nanoparticles with an average particle size of less than 1 μm in a liquid medium. Nanosuspensions are mainly used in water-insoluble drugs, especially those that are insoluble in both water and organic solvents, and nanosuspensions have long-term targeting effects. At present, the methods for preparing nanosuspensions at home and abroad can be divided into two categories according to the different particle formation methods: bottom-up method and top-down method. Bottom-up mainly refers to the aggregation of nanoparticles after drug dissolution, such as Precipitation method, etc.; while top-down is to crush large particles of drugs into nanoparticles by mechani...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/12A61K31/22A61P25/24A61P35/00
Inventor 廖永红魏晓兰韩英瑞刘春雨权丽辉姚广印
Owner 北京鼎国昌盛生物技术有限责任公司
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