Ultrasonic technology-based method for preparing microsphere and device thereof

A technology for preparing devices and microspheres, applied in the fields of microsphere preparation, microcapsule preparations, chemical instruments and methods, etc., can solve the problems of restricting large-scale production, large consumption of water phase, small particle size of microspheres, etc. Industrialization prospect, good dispersion, small particle size effect

Active Publication Date: 2010-04-14
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the commonly used methods such as emulsification method, precipitation method, spray drying method or phase separation method produce microspheres with small particle size and wide particle size distribution, which is difficult to scale up and is not conducive to industrial production.
[0003] The microsphere preparation device disclosed in Chinese patent (patent number: 200420081682.5) has many advantages compared with common methods, but its water phase consumption is extremely large, which limits the possibility of further large-scale production

Method used

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  • Ultrasonic technology-based method for preparing microsphere and device thereof
  • Ultrasonic technology-based method for preparing microsphere and device thereof
  • Ultrasonic technology-based method for preparing microsphere and device thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] use figure 1 A device for preparing drug-containing microspheres, the effective height of the microsphere forming tube 4 is 50 cm, and the aperture of the small hole 302 is 50 μm;

[0037] First, the polyvinyl alcohol (PVA) aqueous solution with a concentration of 1 g / L is filled into the microsphere forming tube 4 and the microsphere solidifier 5, and the end of the nozzle 303 is inserted in the polyvinyl alcohol (PVA) aqueous solution;

[0038] Take 20g of donepezil (the second-generation acetylcholinesterase inhibitor, used for the treatment of Alzheimer's disease) and 80g of poly(lactic-co-glycolic acid) (PLGA), and dissolve them in methylene chloride to form a 50g / L drug-carrier material composite The substance solution is transported to the mold sleeve by the peristaltic pump, and the ultrasonic driving power is turned on. Under the action of ultrasonic vibration, the solution sprays and disperses into droplets in the PVA aqueous solution through small holes, and ...

Embodiment 2

[0046] use figure 1 A device for preparing drug-containing microspheres, the effective height of the microsphere forming tube 4 is 200 cm, and the diameter of the small holes 302 is 100 μm;

[0047] First, the polyvinyl alcohol (PVA) aqueous solution with a concentration of 50 g / L is filled into the microsphere forming tube 4 and the microsphere solidifier 5, and the end of the nozzle 303 is inserted in the polyvinyl alcohol (PVA) aqueous solution;

[0048] Weigh 30g of aconitin (analgesic and anti-inflammatory drug) and 120g of PLGA, dissolve in ethyl acetate to form a 200g / L drug-carrier material complex solution, transport it to the mold sleeve by a peristaltic pump, turn on the ultrasonic drive power supply, Under the action of ultrasonic vibration, the solution is sprayed and dispersed into micro-droplets in the PVA aqueous solution through the small holes. At 55°C, the flow rate of 5L / min is continuously circulated for 300 minutes until the microspheres are initially sol...

Embodiment 3

[0054] use figure 1 A device for preparing drug-containing microspheres, the effective height of the microsphere forming tube 4 is 100 cm, and the aperture of the small hole 302 is 500 μm;

[0055] At first the hydroxypropyl methylcellulose (HPMC) aqueous solution that concentration is 2.5g / L is filled into microsphere forming tube 4 and microsphere solidifier 5, and the end of nozzle 303 is inserted in polyvinyl alcohol (PVA) aqueous solution middle;

[0056] Get 30g naltrexone (opioid receptor antagonist, used for drug rehabilitation, prevent relapse) and 70g PLA, dissolve in chloroform, form 300g / L drug-carrier material complex solution, deliver to stainless steel by peristaltic pump In the mold sleeve, turn on the ultrasonic driving power supply, and the solution is sprayed and dispersed into microdroplets in the HPMC aqueous solution through small holes under the action of ultrasonic vibration. Stir continuously at a stirring speed of 400r / min for 30min, and keep the tem...

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Abstract

The invention provides an ultrasonic technology-based method for preparing microsphere and a device thereof. The preparation device comprises an ultrasonic vibration generation system, a tool head with two open ends, a mold sleeve, a microsphere forming pipe and a microsphere solidifying device; the upper end of the tool head is communicated with the ultrasonic vibration generation system; one side of the mold sleeve is provided with a duct; the lower end of the mold sleeve is provided with a pore and an spraying pipe that is connected with the pore and extends downwards; the mold sleeve is sheathed outside the tool head; the lower end of the tool head extends downwards to the pore; the duct is connected with a pump by a pipeline; the upper end of the microsphere forming pipe is connected with the lower end of the mold sleeve; the spraying pipe is inserted in the microsphere forming pipe; and the microsphere solidifying device is communicated with the lower end of the microsphere forming pipe. The device adopts the ultrasonic as the driving force to disperse the solution into micro drops, thus obtaining better dispersion; and the obtained microsphere has small particle size, the microsphere has high yield, and the device and the method have good industrialization prospect.

Description

technical field [0001] The invention relates to a preparation device and a preparation method of drug-containing microspheres. Background technique [0002] In the past ten years, biodegradable polymer microspheres have become one of the important research fields of new drug delivery systems. It can be used as a carrier for long-acting preparations to release the drug slowly and maintain the curative effect in the body for a week or longer. At present, the commonly used methods such as emulsification, precipitation, spray drying, or phase separation methods produce microspheres with small particle size and wide particle size distribution, which is difficult to scale up and is not conducive to industrial production. [0003] The microsphere preparation device disclosed in the Chinese patent (Patent No.: 200420081682.5) has many advantages compared with common methods, but its water phase consumption is extremely large, which limits the possibility of further large-scale prod...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): B01J13/02B01J19/10B01F17/00C09K23/00
Inventor 王浩皮佳鑫栾瀚森张惠平
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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