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A kind of hydrophilic drug sustained-release microsphere with high encapsulation efficiency and preparation method thereof

A technology of hydrophilic drugs and slow-release microspheres, applied in the field of medicine, can solve the problems of high cost, difficult to achieve linear amplification, and increased production cost, and achieve the effect of improving the encapsulation rate and avoiding the burst release effect.

Active Publication Date: 2021-02-12
ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the industrialization of this kind of process is still early, and it is difficult to achieve linear scale-up, and the cost is high
[0006] The method of preparing microspheres by gradual precipitation in the continuous phase, the drug molecules in the inner aqueous phase will be subjected to various forces, such as interfacial tension, osmotic pressure, mechanical shear force, and will diffuse to the surface of the microspheres with the solvent removal process , eventually dissolved in the external aqueous phase, thus increasing drug loss
Therefore, the precipitation of microspheres in the liquid phase cannot theoretically achieve a 100% drug encapsulation efficiency, and the yield of microspheres is limited. The rate is usually not high, and the generation cost is increased
These problems restrict the industrialization of hydrophilic drug microspheres in my country, and a new microsphere preparation technology is needed to completely improve the problems of low encapsulation efficiency, low yield and serious burst release of water-soluble drugs.

Method used

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  • A kind of hydrophilic drug sustained-release microsphere with high encapsulation efficiency and preparation method thereof
  • A kind of hydrophilic drug sustained-release microsphere with high encapsulation efficiency and preparation method thereof
  • A kind of hydrophilic drug sustained-release microsphere with high encapsulation efficiency and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] like Figure 1-3 As shown, a turntable device for producing droplets from liquid materials, the device is a turntable structure, a cup-shaped container 24 and its first driving device 33 are arranged in the center of the turntable structure, and the outside of the cup-shaped container 24 At least two layers of butterfly turntables are sequentially nested, and each layer of butterfly turntables is equipped with a corresponding driving device. Two layers of butterfly turntables are provided in the accompanying drawings, that is, the first layer of butterfly turntables 26 and the second layer of butterfly turntables 28, the first layer of butterfly turntables 26 are driven to rotate by the second drive device 34, and the second layer of butterfly turntables 28 is driven to rotate by the third driving device 35, and the first driving device 33, the second driving device 34 and the third driving device 35 can be high-speed rotary motors, or strong magnetic high-speed motors....

Embodiment 2

[0055] like Figure 4 Shown, a kind of equipment for making microsphere, described equipment comprises main tank body 23 and embodiment 1 and is used for producing the turntable device of liquid material droplet, the bottom of described turntable device is supported by auxiliary structure 39 is installed in the main tank body 23;

[0056] The main tank 23 is an inverted tapered stainless steel double-layer tank capable of withstanding positive pressure, and a first temperature control element 40 that can adjust temperature is installed on the side wall of the tank. The first temperature control element 40 may be a temperature control water bath placed outside the jacket layer of the main tank body 23 .

[0057] The minimum inner diameter of the main tank body 23 is preferably more than 80 cm. When the longest diameter disc-shaped turntable rotates at the highest rotational speed, the droplets that fly out do not contact the inner wall of the main tank body 23 . Any target pa...

Embodiment 3

[0072] (1) Weigh 1.20g of triptorelin acetate and dissolve it in 1.80ml water to make a hydrophilic drug solution; take 20.00g of PLGA7525 and dissolve it in 33.30g of dichloromethane to make an organic solution; Emulsify on the disperser to form the first emulsion, after cooling, the viscosity of the first emulsion obtained is 954cp.

[0073] (2) the cup-shaped container 24 that the first emulsion described in step (1) is supplied into the turntable device, the cup-shaped container 24 rotating speeds are set to 60m / s, and the rotating speed of the first layer of dish-shaped turntable is 105m / s, and the second layer of dish-shaped The rotation speed of the turntable is 135m / s, and the rotation speed of the third disc-shaped turntable is 160m / s. When the turntable drive device is started, the colostrum is accelerated by the cup-shaped container and passes over the cup mouth, and hits the first layer of disc-shaped turntable under the action of centrifugal force and gravity to di...

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Abstract

The invention discloses a hydrophilic drug slow-release microsphere with a high encapsulation rate and a preparation method thereof. The preparation method is to supply the primary emulsion into a cup-shaped container in the center of a turntable device, start the turntable drive device, and put the The colostrum is accelerated over the mouth of the cup, and hits the outer disc-shaped turntable under the action of centrifugal force and gravity to disperse into fine droplets. The small droplets are accelerated by the disc-shaped turntable and continue to escape from the mouth of the cup to hit the outer disc-shaped turntable. After multiple impacts and dispersion, the microdroplets fly out of the turntable and are highly dispersed in the main tank, solidifying to form microspheres during the downward movement. The preparation method can be used to produce microspheres in a continuous and large-scale production mode, and the prepared microspheres have high encapsulation efficiency, high yield, low organic solvent residue, uniform and controllable particle size, and low burst release efficiency.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a hydrophilic drug slow-release microsphere with high encapsulation efficiency and a preparation method thereof. Background technique [0002] In microsphere drug delivery systems, the properties of the carrier material are the main factors that determine the drug release behavior. Polyester polymer materials are by far the best biosafety and most widely used biodegradable synthetic polymer carrier materials. Its degradation mechanism is hydrolysis and deesterification in the body, the molecular weight decreases continuously, and finally produces lactic acid monomers. Lactic acid is oxidized to pyruvate under the action of lactate dehydrogenase, and through the tricarboxylic acid cycle in the body, it is finally metabolized into water and carbon dioxide. At present, polylactic acid (PLA) and poly(lactic-co-glycolic acid) (PLGA) have been approved by the US FDA and are used as d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K9/52A61K47/34A61K38/22A61K38/09A61J3/00
Inventor 于崆峒蒋朝军
Owner ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD