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Method for preparing calibrated biodegradable microspheres

A kind of microsphere, biological technology, applied in the field of pharmaceutical industry, to achieve the effect of simple method

Active Publication Date: 2007-04-25
埃法尔姆具有监督和管理委员会的有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this approach is only aimed at providing lipid emulsions and non-complex systems in which the organic phase comprises a polymer and organic solvent

Method used

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  • Method for preparing calibrated biodegradable microspheres
  • Method for preparing calibrated biodegradable microspheres
  • Method for preparing calibrated biodegradable microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach 1

[0121] General procedure for preparing microspheres from single emulsions:

[0122] This method can be used to prepare biodegradable polymer microspheres, which are especially useful for the delivery of lipophilic active ingredients.

[0123] The active ingredient to be encapsulated is dispersed or dissolved in an organic phase consisting of PLGA dissolved in vinyl acetate.

[0124] Then, the organic phase is emulsified in an aqueous phase containing water and a hydrophilic surfactant such as PVA in an amount of 0.1-10%, preferably 1-4%, and a viscosity agent such as poly Ethylene glycol or poloxamer, the content is 10-50%.

[0125] To optimize shear efficiency, the viscosity ratio of the two phases can be adjusted. Preferably the viscosity ratio of the organic phase to the aqueous phase is 0.1-10, more precisely 3-8.

[0126] The so-called "coarse" emulsions thus obtained are then subjected to laminar shear. This step is preferably carried out in a Couette apparatus, as...

Embodiment approach 2

[0135] Preparation of 2.5 µm microspheres from a single emulsion:

[0136] In a flask, the continuous aqueous phase was prepared by dissolving 0.9 g of PVA in 14.14 g of demineralized water (3%) at vinyl acetate saturation under magnetic stirring at 70°C. After cooling, 15 g of PEG 400 was added thereto. The aqueous phase therefore contained 3% PVA, 50% PEG 400 and was saturated with vinyl acetate.

[0137] The organic phase was prepared in a sealed bottle by dissolving 2.6 g of PLGA 75 / 25 in 17.39 g of a water-saturated vinyl acetate solution (3%) under magnetic stirring. The organic phase thus contained 13% PLGA dissolved in water-saturated vinyl acetate.

[0138] All these organic phases were then emulsified in 20 g of the above aqueous phase by manual stirring using a spatula. The emulsion contains 50% by mass of the dispersed organic phase.

[0139] The premix thus obtained was placed in a Couette apparatus and sheared at 400 rpm in a gap of 100 μm with a piston upf...

Embodiment approach 3

[0143] Preparation of 6.5 µm microspheres from a single emulsion:

[0144] In a flask, the continuous aqueous phase was prepared by dissolving 1.2 g of PVA in 35.25 g of demineralized water (3%) at vinyl acetate saturation under magnetic stirring at 70°C. After cooling, 4.02 g of PEG 2000 was added thereto. The aqueous phase therefore contained 3% PVA, 10% PEG 2000 and was saturated with vinyl acetate.

[0145] The organic phase was prepared in a sealed flask by dissolving 2.67 g of PLGA 75 / 25 in 17.89 g of a water-saturated vinyl acetate solution (3%) under magnetic stirring. The organic phase thus contained 13% PLGA dissolved in water-saturated vinyl acetate.

[0146] All these organic phases were then emulsified in 20 g of the above aqueous phase by manual stirring using a spatula. The emulsion contains 50% by mass of the dispersed organic phase.

[0147] The premix thus obtained was placed in a Couette apparatus and sheared at 300 rpm in a gap of 100 μm with a piston...

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Abstract

The invention relates to a method for preparing monodispersed biodegradable microspheres consisting in a) preparing an emulsion containing at least one polymeric phase and at least one aqueous phase at a viscosity ratio between the dispersed polymeric phase and the aqueous phase ranging from 0.12 to 10, b) exposing the thus obtained emulsion to a controlled laminar shear strength, c) removing a solvent from the polymeric phase and in d) isolating the thus obtained microspheres. The use of the prepared microspheres is also disclosed.

Description

field of invention [0001] The present invention relates to the pharmaceutical industry. More precisely, the present invention relates to the preparation of monodisperse biodegradable microspheres, in particular for the administration of pharmaceutically active ingredients. Background of the invention [0002] It is known (we) to encapsulate active pharmaceutical ingredients in microspheres in order to facilitate their administration or to prevent their decay in living organisms. [0003] Microencapsulation involves the encapsulation of solid or liquid substances into particles varying in size from 0.1 to 1000 μm. [0004] In this context, the application of biodegradable microspheres for the delivery of active ingredients over longer periods of time is particularly envisioned. [0005] Various techniques for preparing biodegradable microspheres are known. [0006] Thus, US Pat. No. 5,643,607 discloses microcapsules for prolonged administration of hydrophilic active ingred...

Claims

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Application Information

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IPC IPC(8): B01J13/12B01J13/04
CPCB01J13/04B01J13/12B01J13/06
Inventor A·鲁瓦埃D·巴齐勒J·比贝
Owner 埃法尔姆具有监督和管理委员会的有限公司
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