Preparation of pharmaceutical or cosmetic dispersions

• US 4,996,004 A
• Filed: 03/15/1989
• Issued: 02/26/1991
• Est. Priority Date: 08/14/1982
• Status: Expired due to Term

• Current Assignee: Bayer AG
• Original Assignee: Bayer AG
• Inventors: Klinksiek, Bernd, Koglin, Bernd, Bucheler, Manfred, Gehringer, Hans
• Primary Examiner(s): Lovering, Richard D.
• Application Number:
  US07/324,985
• Time in Patent Office: 713 Days
• Field of Search: 252/312, 252/314, 514/941, 514/942, 514/943
• US Class Current: 424/401
• CPC Class Codes: A61K 8/06 Emulsions
• CPC Class Codes: A61K 8/062 Oil-in-water emulsions
• CPC Class Codes: A61K 9/107 Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00
• CPC Class Codes: A61Q 17/04 Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin
• CPC Class Codes: B01F 23/41 Emulsifying
• CPC Class Codes: B01F 25/45 Mixers in which the materials to be mixed are pressed together through orifices or interstitial spaces, e.g. between beads B01F25/44 takes precedence
• CPC Class Codes: B01F 25/4521 the components being pressed through orifices in elements, e.g. flat plates or cylinders, which obstruct the whole diameter of the tube
• CPC Class Codes: B01F 25/45211 the elements being cylinders or cones which obstruct the whole diameter of the tube, the flow changing from axial in radial and again in axial
• CPC Class Codes: Y10S 516/925 Phase inversion

Abstract

The invention relates to a process for the preparation of fine-particled, stable, pharmaceutical or cosmetic dispersions consisting of an aqueous phase and an organic phase which is insoluble or not completely soluble in water (oily phase) in which a pre-emulsion is prepared from the two phases by known emulsifying methods and in then pumped through a jet disperser, the temperature, the proportion of the aqueous and organic phases, and the pressure at the jet disperser being adjusted so that phase inversion of the emulsion is effected in the jet disperser at the same time as homogenization and fine dispersion, and in the course of which all the pressure energy is consumed in the dispersing zone and the dispersion leaves as a non-directional stream.

Claims

1. Process for the preparation of fine-particled, stable, pharmaceutical or cosmetic dispersions consisting of an aqueous phase and an organic oily phase which is insoluble or not completely soluble in water, characterized in that a pre-emulsion is pumped through a jet disperser which consists of one or more jets, which are designed as capillary bores with a diameter of 0.5 to 0.8 mm and have a length to diameter ratio of 1.5 to 2 the temperature, the proportions of the aqueous phase and the organic phase and the pressure at the jet disperser being adjusted so that phase inversion of the emulsion is effected in the jet disperser at the same time as homogenization and fine dispersion, and in the course of which all the pressure energy is consumed in the dispersing zone and the dispersion leaves the dispersing zone as a non-directional stream.

2. A process according to claim 1, wherein to prepare the pre-emulsion, the organic phase is initially introduced as the external phase and the aqueous phase is emulsified therein as the internal phase.

3. A process according to claim 2, wherein the phase inversion is carried out as a concentration of 50 to 70% by weight of the organic phase.

4. A process according to claim 1, wherein the pre-emulsion is pumped through the jet disperser under a pressure of 2 to 50 bar.

5. A process according to claim 1, wherein the organic phase contains a mixture of glycerol esters or fatty acid esters and/or liquid, semi-solid and solid hydrocarbons, as well as polyhydric alcohols, non-ionic emulsifiers and fat-soluble pharmaceutical or cosmetic active compounds, and the aqueous phase contains an aqueous solution of glycerol, glycols, low-molecular monohydric alcohols and cosmetic or pharmaceutical active compounds, with the addition of substances which increase the viscosity and preservatives.

6. A process according to claim 1, wherein the pre-emulsion is pumped through the jet disperser under a pressure of 10 to 50 bar.