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Triamcinolone acetonide microsphere preparation and preparation method thereof

A technology of microspheres and preparations, which is applied in the field of medicine, can solve the problems of small force, increase of solvent residues in microspheres, and pollute the environment, and achieve the effects of reducing usage, improving drug stability, and reducing residual solvents

Active Publication Date: 2019-05-03
ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, the structure of this immature turntable device has certain defects that make it very limited in application. The reason is that the force of using centrifugal force and surface tension to stretch the liquid into balls is too small. For those with high viscosity and cohesive force Strong feed liquid often cannot be broken effectively, so In the patent, in order to reduce the viscosity of the feed liquid and obtain the microspheres with the target particle size, a large amount of organic solvents are used to dissolve triamcinolone acetonide and PLGA. The use of a large amount of organic solvents not only pollutes the environment, but also increases the residual solvent in the microspheres. For those who need Drugs that avoid large amounts of organic solvents are not suitable

Method used

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  • Triamcinolone acetonide microsphere preparation and preparation method thereof
  • Triamcinolone acetonide microsphere preparation and preparation method thereof
  • Triamcinolone acetonide microsphere preparation and preparation method thereof

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Embodiment 1

[0042] 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

[0047] 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;

[0048] 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 .

[0049] 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

[0067] (1) Weigh 25g of triamcinolone acetonide and 75g of PLGA7525 (intrinsic viscosity 0.6dL / g) and disperse them in 75g of dichloromethane solvent, and the final viscosity of the obtained homogeneous solution is 374cp;

[0068] ⑵The homogeneous solution described in step ⑴ is supplied into the cup-shaped container through the liquid supply port (liquid supply speed 5mL / min), adjust the rotating drive device, set the cup-shaped container speed to 40m / s, and the speed of the first layer of disc-shaped turntable The rotational speed of the disc-shaped turntable on the second layer is 110m / s, and the rotational speed of the third-layer disc-shaped turntable is 130m / s. Under the action of centrifugal force, the material liquid in the cup-shaped container crosses the mouth of the cup and hits the opposite direction. The surface of the first layer of disc-shaped turntable is dispersed into droplets, and the formed droplets continue to hit the second layer of disc-shaped turntable r...

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Abstract

The invention provides a preparation method of a triamcinolone acetonide microsphere preparation. The method comprises the steps of: (1) dissolving PLGA in a volatile and well-soluble organic solventso as to form a homogeneous-phase solution; (2) adding triamcinolone acetonide to the homogeneous-phase solution described in the step (1) to be dissolved to obtain a homogeneous-phase solution with afinal viscosity of 5-500cp; and (3) feeding the homogeneous-phase solution described in the step (2) to a cup-shaped container in the center of a turntable device, wherein the liquid in the cup-shaped container passes over a cup rim, the solution hits a lateral disc-shaped turntable under the action of centrifugal force and gravity so as to form microdroplets, the formed microdroplets continue tohit a more lateral disc-shaped turntable, and after two or more hitting, the microdroplets fly out of the turntable and are solidified to form microspheres. The microsphere preparation obtained by the method has outstanding sustained release ability, and requires no additional release regulator, and the sustained release period can be as long as 1-3 months.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a triamcinolone acetonide microsphere preparation and a preparation method thereof. Background technique: [0002] Knee osteoarthritis (Osteoarthritis of the knee, KOA) is a chronic degenerative disease mainly manifested by recurrent joint pain and gradual joint mobility impairment. The main pathological changes are the progressive destruction of the involved articular cartilage, cartilage degeneration, and subchondral bone sclerosis, etc., and its essence is the imbalance of catabolism and anabolism of the articular cartilage matrix. KOA is a degenerative joint disease that affects more than 27 million Americans. According to Global Data, the osteoarthritis drug market is expected to grow from $1.6 billion in 2016 to $3.5 billion in 2026. According to relevant epidemiological statistics, the prevalence rate of KOA in the Chinese population is 8.1%, which seriously affects the...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/58A61K47/34A61P19/02
Inventor 于崆峒蒋朝军
Owner ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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