Process for the production of morphologically uniform...

Details Process for the production of morphologically uniform... Process for the production of morphologically uniform...

A - Human Necessities

61

K

A61K 9/50 (2006.01) A61K 9/16 (2006.01) A61K 38/00 (2006.01) A61K 38/09 (2006.01) A61K 38/21 (2006.01) A61K 38/28 (2006.01) A61K 38/38 (2006.01) A61K 47/34 (2006.01) B01J 13/02 (2006.01)

Patent

CA 2238352

The invention concerns a method of producing morphologically uniform microcapsules containing peptides, proteins or other water-soluble biologically active substances as active substance, and microcapsules produced by this method with a charging degree of between 3 and 30 wt.% and a diameter of <= 8 µm. According to the invention, biodegradable polymers are dissolved in a halogen-free solvent or solution mixture and the buffered active substance solution, which has a pH of between 6.0 and 8.0, is dispersed in this solution. An aqueous solution containing a surfactant is then added to this W/O emulsion (W/O/W emulsion) and the solvent removed. The microcapsules produced by this method display no tendency to agglomerate. The encapsulation efficiency of the method is between 90 and 95 %.

L'invention concerne un procédé pour la production de microcapsules à morphologie uniforme, contenant comme principe actif des peptides, des protéines ou d'autres substances actives biologiquement hydrosolubles, ainsi que les microcapsules obtenues, présentant un degré de charge compris entre 3 et 30 % en poids et un diamètre </= 8 mu m. Des polymères biodégradables sont dissous dans un solvant ou un mélange de dissolution dépourvu d'halogène, et la solution de principe actif tamponnée, laquelle présente un pH compris entre 0,6 et 8,0, est dispersée dans cette solution. Une solution aqueuse renfermant un tensioactif est alors ajoutée à cette émulsion d'eau dans l'huile, donnant ainsi une émulsion eau/huile/eau, et le solvant est éliminé. Les microcapsules ainsi produites ne présentent aucune tendance à l'agglomération. L'efficacité d'encapsulation obtenue avec ce procédé se situe entre 90 et 95 %.

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