Galenic form for oral administration and its method of preparation by lyophilization of an oil-in-water emulsion

Claim 1

A method for preparing a galenic form for oral administration by lyophilization of an oil-in-water emulsion containing at least one pharmaceutically active ingredient and obtained from a lipid phase and an aqueous phase, wherein said method comprises: (a) preparing the lipid phase by stirring at a temperature lower than or equal to 80° C. so as to mix all the lipid-phase components, whereby said lipid phase is liquid, (b) preparing the aqueous phase, by stirring at a temperature lower than or equal to 80° C. so as to mix the water and the other components of said aqueous phase, said aqueous phase including an organic filler selected from the group consisting of lactose, whole milk powder, semi-skimmed milk powder, skimmed milk powder, glycocoll, mannitol, maltodextrins, and mixtures thereof; said aqueous phase also containing a thickening agent selected from the group consisting of natural natural and synthetic gums, cellulose derivatives, pectins, bentonites, colloidal silicas, polyvinyl alcohol, polyvinylpyrrolidone, acrylic polymers and copolymers, and mixtures thereof, said organic filler and thickening agent constituting from 10 to 85% by weight of the total aqueous phase, not counting the pharmaceutically active substance present; (c) preparing an emulsion under stirring at a temperature within the range of 10° C. to 80° C. by introducing the liquid lipid phase into the aqueous phase in order to obtain a homogeneous emulsion, (d) distributing the resulting mixture into alveolar packs, (e) freezing the contents of said alveolar packs at a temperature within the range of -20° C. to -50° C., then lyophilizing said contents under a pressure within the approximate range of 80 Pa to 0.13 Pa, with a heat supply such that the temperature of the treated mass is always lower than the starting melting temperature of said mass, the pharmaceutically effective material being incorporated before step (d).

Claim 2

A method for preparing a galenic form for oral administration by lyophilization of an oil-in-water emulsion containing at least one pharmaceutically active ingredient and obtained from a lipid phase and an aqueous phase, wherein said method comprises: (a) preparing the lipid phase by stirring at a temperature lower than or equal to 80° C. so as to mix all the lipid-phase components, whereby said lipid phase is liquid, (b) preparing the aqueous phase, by stirring at a temperature lower than or equal to 80° C. so as to mix the water and the other components of said aqueous phase, said aqueous phase including an organic filler selected from the group consisting of lactose, whole milk powder, semi-skimmed milk powder, skimmed milk powder, glycocoll, mannitol, maltodextrins, and mixtures thereof; said aqueous phase also containing a thickening agent selected from the group consisting of natural natural and synthetic gums, cellulose derivatives, pectins, bentonites, colloidal silicas, polyvinyl alcohol, polyvinylpyrrolidone, acrylic polymers and copolymers, and mixtures thereof, said organic filler and thickening agent constituting from 10 to 85% by weight of the total aqueous phase, not counting the pharmaceutically active substance present; (c) preparing an emulsion under stirring at a temperature within the range of 10° C. to 80° C. by introducing the liquid lipid phase into the aqueous phase in order to obtain a homogeneous emulsion, (d) distributing the resulting mixture into alveolar packs, (e) freezing the contents of said alveolar packs at a temperature within the range of -20° C. to -50° C., then lyophilizing said contents under a pressure within the approximate range of 80 Pa to 0.13 Pa, with a heat supply such that the temperature of the treated mass is always lower than the starting melting temperature of said mass, the pharmaceutically effective material being incorporated before step (d).

Claim 18

A method for preparing a galenic form for oral administration by lyophilization of an oil-in-water emulsion containing at least one pharmaceutically active ingredient and obtained from a lipid phase and an aqueous phase, wherein said method comprises: (a) preparing the lipid phase by stirring at a temperature lower than or equal to 80° C. so as to mix all the lipid-phase components, whereby said lipid phase is liquid, (b) preparing the aqueous phase by stirring at a temperature lower than or equal to 80° C. so as to mix the water and the other components of said aqueous phase, said aqueous phase containing milk powder as an organic filler and a thickening agent selected from the group consisting of natural and synthetic gums, cellulose derivatives, pectins, bentonites, collidal silicas, polyvinyl alcohol polyvinylpyrrolidone, acrylic polymers and copolymers, and mixtures thereof, said organic filler and thickening agent representing about 10 to 85% by weight of the aqueous phase, not counting the weight of said pharmaceutically active ingredient present; (c) preparing an emulsion under stirring at a temperature within the range of 10° C. to 80° C. by introducing the liquid phase into the aqueous phase in order to obtain a homogeneous emulsion, the weight ratio of lipid phase to aqueous phase being within the range of 1:100 to 1:4, and the temperature of said lipid and aqueous phases on mixing being substantially equal; (d) distributing the resulting mixture into alveolar packs, (e) freezing the contents of said alveolar packs at a temperature within -20° to -50° C., and then lyophilizing said contents under a pressure within the approximate range of 80 Pa to 0.13 Pa, with a heat supply such that the temperature of the treated mass is always lower than the starting melting temperature of said mass, the pharmaceutically effective material being incorporated before step (d).

Claim 19

A method for preparing a galenic form for oral administration by lyophilization of an oil-in-water emulsion containing at least one pharmaceutically active ingredient and obtained from a lipid phase and an aqueous phase, wherein said method comprises: (a) preparing the lipid phase by stirring at a temperature lower than or equal to 80° C. so as to mix all the lipid-phase components, whereby said lipid phase is liquid, (b) preparing the aqueous phase by stirring at a temperature lower than or equal to 80° C. so as to mix the water and the other components of said aqueous phase, said aqueous phase containing milk powder as an organic filler and a thickening agent selected from the group consisting of natural and synthetic gums, cellulose derivatives, pectins, bentonites, collidal silicas, polyvinyl alcohol polyvinylpyrrolidone, acrylic polymers and copolymers, and mixtures thereof, said organic filler and thickening agent representing about 10 to 85% by weight of the aqueous phase, not counting the weight of said pharmaceutically active ingredient present; (c) preparing an emulsion under stirring at a temperature within the range of 10° C. to 80° C. by introducing the liquid phase into the aqueous phase in order to obtain a homogeneous emulsion, the weight ratio of lipid phase to aqueous phase being within the range of 1:100 to 1:4, and the temperature of said lipid and aqueous phases on mixing being substantially equal; (d) distributing the resulting mixture into alveolar packs, (e) freezing the contents of said alveolar packs at a temperature within -20° to -50° C., and then lyophilizing said contents under a pressure within the approximate range of 80 Pa to 0.13 Pa, with a heat supply such that the temperature of the treated mass is always lower than the starting melting temperature of said mass, the pharmaceutically effective material being incorporated before step (d).