Process for the preparation of liposomal medicaments

Details Process for the preparation of liposomal medicaments Process for the preparation of liposomal medicaments

1982-01-07

1988-03-15

Lovering, Richard D.

Plastic and nonmetallic article shaping or treating: processes

Encapsulating normally liquid material

Liquid encapsulation utilizing an emulsion or dispersion to...

264 41, 264 46, 424450, 4284022, 436829, A61K 952, B01J 1302

Patent

active

047312106

ABSTRACT:
Associates of at least one amphiphilic bilayer-forming substance and a solubilizing agent are formed in an aqueous phase. The bilayer-forming substance itself can be a pharmaceutical substance, or pharmaceutical substances and/or pharmaceutical auxiliaries may be added. The equilibrium conditions for the molar ratio of bilayer-forming substance to solubilizing agent in the associates are then changed in the aqueous phase containing the associates, in order to remove solubilizing agent from the associates, so that the associates combine to form liposomes. In particular, the solubilizing agent concentration in the aqueous phase is reduced, for example by dilution with additional aqueous phase. The change is effected at a rate which is sufficiently high for formation of liposomes having a predefined number of double layers. Furthermore, the rate of change in the aqueous phase is kept virtually constant with respect to location and time. The liposomes thereby achieve a predefined, virtually homogeneous size.

REFERENCES:
patent: 3932657 (1976-01-01), Rahman
patent: 3957971 (1976-05-01), Oleniacz
patent: 3993754 (1976-11-01), Rahman et al.
patent: 4310506 (1982-01-01), Baldeschwieler et al.
Rhoden et al.: "Formation of Unilamellar Lipid Vesicles . . . ", Biochemistry, vol. 18, No. 19, 1979, pp. 4173-4176.

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