Continuous flow preparation method of high drug-loading microspheres

A technology of high drug loading and microspheres, which is applied in the preparation of microspheres, pharmaceutical formulations, microcapsule preparations, etc. It can solve the problems of wide particle size distribution range, average particle size, encapsulation rate drug loading, and large differences in drug release. problems, to achieve the effects of avoiding property differences, reducing toxicity risks, and reducing production costs and risks

Pending Publication Date: 2022-03-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In addition, the batch preparation method of traditional microspheres often leads to a wide range of particle size distribution of the same batch of microspheres, and the average particle size, encapsulation efficiency, drug loading and drug release of different batches of microspheres vary greatly.

Method used

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  • Continuous flow preparation method of high drug-loading microspheres
  • Continuous flow preparation method of high drug-loading microspheres
  • Continuous flow preparation method of high drug-loading microspheres

Examples

Experimental program
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Embodiment 1

[0048] Such as figure 1 As shown, this embodiment discloses a continuous flow preparation device for highly drug-loaded microspheres, including a first reactor and a second reactor, the first reactor includes a first inlet, a second inlet and a first outlet, and the second reactor includes a first inlet, a second inlet and a first outlet. The second reactor includes a third inlet and a fourth inlet.

[0049] Optional situation 1: the first reactant and the second reactant enter the first reactor through the first inlet and the second inlet respectively, and the obtained mixture of the first reactant and the second reactant passes through the second reactor under the action of the pump. The third inlet enters the second reactor, and at the same time, the third reactant enters the second reactor through the fourth inlet, and the obtained oil-in-water emulsion can be solidified to obtain high drug-loaded microspheres. Optional situation 2: the first reactant and the second react...

Embodiment 2

[0051] Such as figure 2 As shown, this embodiment discloses a continuous flow preparation device for highly drug-loaded microspheres. The difference between this embodiment and Embodiment 1 is that there are two second inlets, which are respectively perpendicular to the straight line formed by the first reactor and the first inlet; there are two fourth inlets, which are respectively perpendicular to the second reactor and the third inlet formed straight line.

[0052] The first reactant and the second reactant enter the first reactor through the first inlet and the second inlet respectively, and the obtained mixture of the first reactant and the second reactant enters the second reactor through the third inlet under the action of the pump. In the reactor, at the same time, the third reactant enters the second reactor through the fourth inlet, and the obtained oil-in-water emulsion can be solidified to obtain high drug-loaded microspheres. The exchange of the inlet of the fi...

Embodiment 3

[0054] Such as image 3 As shown, this embodiment discloses a continuous flow preparation device for highly drug-loaded microspheres. The difference between this embodiment and embodiment 2 is that there is one second inlet, the first inlet and the second inlet both form an included angle (0-180 degrees) with the first reactor, and the rest are the same.

[0055] The first reactant and the second reactant enter the first reactor through the first inlet and the second inlet respectively, and the obtained mixture of the first reactant and the second reactant enters the second reactor through the third inlet under the action of the pump. In the reactor, at the same time, the third reactant enters the second reactor through the fourth inlet, and the obtained oil-in-water emulsion can be solidified to obtain high drug-loaded microspheres. The exchange of the inlet of the first reactant and the second reactant into the first reactor does not affect the preparation of high drug-load...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and discloses a continuous flow preparation method of high-drug-loading microspheres. The method comprises the following steps: precipitating an active drug solution by using a poor solvent in which a microsphere matrix material is dissolved to form nanoparticles, directly taking the mixture as an oil phase, mixing the oil phase with a water phase to prepare oil-in-water emulsion droplets, and curing to obtain the high-drug-loading microspheres. The nanoparticles are directly wrapped in one step in continuous flow preparation, the preparation process of the microspheres is simplified, and the application value is high. The prepared high-drug-loading microsphere comprises nanoparticles composed of active drug components and a microsphere matrix material used for controlling drug release, and the particle size is 1-2000 [mu] m; the mass of the active drug component accounts for 5-80% of the mass of the whole microsphere, and the encapsulation efficiency of the active drug is 5-100%. The microspheres prepared through a continuous flow method are high in encapsulation efficiency and drug loading capacity and free of burst release, the treatment efficiency can be effectively improved, and toxic and side effects and adverse reactions can be reduced.

Description

technical field [0001] The invention relates to a continuous flow preparation method of highly loaded polypeptide and protein microspheres, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Peptides and proteins are one of the important components of organisms, with the advantages of high activity, high specificity, and low toxicity. Since recombinant human insulin was approved for marketing by the US Food and Drug Administration in 1982, the development of peptide and protein drugs has entered the fast lane, and has been favored by researchers at home and abroad. At present, there are about 80 kinds of peptide and protein drugs used in the clinical treatment of diseases in the world, more than 150 kinds of peptide and protein drugs are in the clinical development stage, and more than 600 kinds of peptide and protein drugs are undergoing preclinical research. Compared with small molecule drugs, peptide and protein drugs occupy a ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): B01J13/02A61K9/52A61K47/38A61K47/34A61K47/36
CPCB01J13/02A61K9/5036A61K9/5031A61K9/5042
Inventor 刘东飞刘颖欣胡帅张佩孙宏斌
Owner CHINA PHARM UNIV
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