Method for the microencapsulation by phase separation of...

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A61K 9/36 (2006.01) A61K 9/16 (2006.01) A61K 9/52 (2006.01) B01J 13/02 (2006.01) B01J 13/20 (2006.01)

Patent

CA 1259567

- ? - TITLE Method for the microencapsulation by phase separation of medicamentous water-soluble substances ABSTRACT OF THE DISCLOSURE The microencapsulation of medicamentous water-soluble substances is carried out by phase separation. The opera- tions of the hardening step take place at a temperature comprised between about o and about 25°C, the non-solvent used during this step being an aliphatic fluorinated or fluorohalogenated hydrocarbon or a mixture of such hydro- carbons. Further, the non-solvent is used in an excess with respect to the volume of solvent and non-solvent re- sulting from the phase-separation step. BACKGROUND OF THE INVENTION The microencapsulation of medicamentous substances is an established technique, which in particular permits the protection and the controlled administration of medica- mentous substances having a short half-life in vivo. The resulting galenic form most often has the form of an injectable suspension of a very high efficiency. Various methods of relization are described in the literature (see for example the Patent Application EP No. 0052510, published 26 May 1982, corresponding to Canadian Patent No. 1,176,565. One of the most used methods of micro-encapsulation by phase separation can be described as follows: a) a biocompatible polymer is first dissolved in an organic solvent non-miscible with water (for example CH2Cl2) ; b) an aqueous solution of the selected medicamentous subs-

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