Preparation method of PLGA (poly (lactic-co-glycolic acid)) drug sustained release microspheres

A technology for slow-release microspheres and drugs, which is applied in the production of pharmaceutical formulations, inactive medical preparations, and bulk chemicals. It can solve the problems of low PLGA concentration, long curing time, etc. The effect of easy control and shortening of time

Active Publication Date: 2022-06-07
SHANGHAI RUINING BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the traditional emulsification solvent volatilization-precipitation method is still used in this technical solution, which still cannot solve the problems of low PLGA concentration and long curing time

Method used

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  • Preparation method of PLGA (poly (lactic-co-glycolic acid)) drug sustained release microspheres
  • Preparation method of PLGA (poly (lactic-co-glycolic acid)) drug sustained release microspheres
  • Preparation method of PLGA (poly (lactic-co-glycolic acid)) drug sustained release microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1 Preparation of PLGA drug sustained-release microspheres by conventional emulsifying solvent evaporation method

[0050] The microspheres were prepared according to the recipe in Table 1.

[0051] 1. Preparing the solidified phase: Weigh a certain amount of surfactant in a beaker containing ultrapure water and wait for it to be dissolved for later use.

[0052] 2. Preparation of oil phase: Add a certain concentration of PLGA and dexamethasone small molecule drug into a beaker containing an organic solvent, and turn on the stirring device to stir the oil phase to obtain a uniform drug water-in-oil emulsion or drug particle suspension system .

[0053] 3. Under mechanical stirring, add the oil phase to the water phase to emulsify and solidify.

[0054] 4. After the solidification is completed, solid-liquid separation, centrifugation and washing are carried out by means of centrifugation to obtain concentrated microspheres.

[0055] 5. Transfer the washed conce...

Embodiment 2

[0070] Example 2 Preparation of PLGA drug sustained-release microspheres by polymer-assisted phase inversion method

[0071] Referring to Table 2, select different types of interface inversion regulators, and prepare PLGA drug sustained-release microspheres by polymer-assisted phase inversion method. The preparation process is as follows:

[0072] 1. Preparation of water phase: Weigh a certain amount of interface inversion regulator A or / and B, respectively, and dissolve them in a beaker containing ultrapure water for use.

[0073] 2. Preparation of solidified phase: prepare 10% poloxamer aqueous solution (W / V), and set aside.

[0074] 3. Oil phase: Dissolve 3g PLGA and 1.5g dexamethasone in a beaker containing 10ml of ethyl acetate solvent, turn on the stirring device, and continue stirring to obtain a uniform drug water-in-oil emulsion or drug particle suspension system.

[0075] 4. Through the peristaltic pump, the water phase is added to the oil phase at a fixed flow rate...

Embodiment 3

[0089] On the basis of Example 2, when poloxamer and mannitol with a mass ratio of 1:10 were used as interface modifiers, the concentration of PLGA in the oil phase was changed, and the preparation of PLGA drug sustained-release microspheres was carried out. The preparation steps :

[0090] 1. Preparation of water phase: Weigh 5g of poloxamer and 50g of mannitol respectively and dissolve them in a beaker of 250ml of ultrapure water, set aside.

[0091] 2. Preparation of solidified phase: prepare a 10% poloxamer aqueous solution for use.

[0092] 3. Oil phase: Dissolve a certain amount of PLGA and triamcinolone acetonide small-molecule drug in a beaker containing an organic solvent, turn on the stirring device, and continuously stir to obtain a uniform drug particle suspension system.

[0093] 4. Through the peristaltic pump, the water phase is added to the oil phase at a certain flow rate, and the semi-solidified microspheres are rapidly formed.

[0094] 5. Then add the soli...

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Abstract

The invention relates to a preparation method of PLGA (poly (lactic-co-glycolic acid)) drug sustained-release microspheres, which is characterized in that emulsification and partial curing are quickly realized by combining a polymer-assisted phase inversion method on the basis of an emulsifying solvent volatilization method. According to the preparation method, the drug loading rate exceeding 50% and the drug encapsulation rate exceeding 90% can be achieved at the same time, and the preparation method has the advantages that the particle size is easy to control, the process is easy to amplify, the solvent toxicity is low, and process equipment is simple.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a preparation method of PLGA drug sustained-release microspheres. [0002] technical background [0003] With the rapid development of biotechnology in recent years, a large number of drugs with potential therapeutic applications have appeared. However, due to the inherent physical and chemical instability of drugs, after oral administration to patients, they are hydrolyzed and degraded in the acidic environment of the stomach. Bioavailability in the gastrointestinal tract is very low. Relatively rapid inactivation can also be observed following non-intravenous injection. Therefore, despite the high pharmacological activity of these compounds, repeated frequent injections of high-dose drugs may be required to maintain long-term drug efficacy, which is a heavy burden on patients and greatly reduces patient compliance. If the frequency of dosing can be reduced, complianc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/34
CPCA61K9/1647A61K9/1682Y02P20/54
Inventor 夏海影潘震
Owner SHANGHAI RUINING BIOTECH CO LTD
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