Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Patent
1995-12-20
1998-02-03
Mullis, Jeffrey C.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
424484, 424486, A61K 9113
Patent
active
057141541
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to a process for the production of multiple w/o/w emulsions in which a w/o pre-emulsion is initially prepared with intensive shearing from water, an oil and an emulsifier I and the w/o pre-emulsion thus formed is subsequently treated with an aqueous emulsifier II with gentle shearing, to multiple w/o/w emulsions obtainable by this process and to the use of these multiple w/o/w emulsions for the production of cosmetic and pharmaceutical products.
2. Statement of Related Art
Multiple emulsions are emulsions of emulsions. Depending on their production process, they are either multiple water/oil/water (w/o/w) or oil/water/oil (o/w/o) emulsions. The most important application of multiple emulsions lies in the processing of active substances, which would otherwise be immiscible with one another, in a single formulation. Another advantage is that the active substances can be released under control over a prolonged period. Accordingly, multiple emulsions are of particular significance for the production of cosmetic and pharmaceutical
A particularly suitable process for the production of multiple emulsions is described by S. Matsumoto in J. Coll. Interf. Sci. 57, 353 (1976). In this process, a pre-emulsion is initially prepared with intensive shearing at elevated temperature and is subsequently introduced into an aqueous solution of a hydrophilic emulsifier with gentle shearing at ambient temperature. Sorbitan monooleate and a polyethylene glycol derivative are used as the pair of emulsifiers.
In addition, it is known from the extensive prior art that, basically, monoglycerides, sorbitan esters, polysorbates and highly ethoxylated fatty alcohols may be used as hydrophilic emulsifiers for the production of multiple emulsions, cf. the articles in Pharm. Acta. Helv. 66, 343 (1991), and by Seiller and Luca in Bull. Tech./Gattefosse Rep. 80, 27 (1987), S. T. P. Pharma 4, 679 (1988) and Int. J. Cosmet. Sci. 13, 1 (1991).
In addition, w/o/w emulsions containing glycerol trifatty acid esters as oil component and hydrophilic polymers, such as gelatine for example, as stabilizer are known from Yakugaku Zasshi 112, 73 (1992). The use of albumin and polyacrylates as stabilizers for the water phase and nonionic surfactants for the oil phase is known from J. Controlled Release 3, 279 (1986). Unfortunately, formulations such as these have proved to be inadequately stable in storage, particularly in the event of variations in temperature.
Accordingly, a particular problem in the production of multiple emulsions lies in the choice of suitable pairs of emulsifiers which provide for adequate thermal stability, even in the event of prolonged storage. Another disadvantage is that mineral oils showing unfavorable biodegradability are normally used as the oil component.
Accordingly, the problem addressed by the present invention was to provide a new process for the production of multiple w/o/w emulsions which would be free from the disadvantages mentioned above.
DESCRIPTION OF THE INVENTION
The present invention relates to a process for the production of multiple w/o/w emulsions, in which glycerol and/or oligoglycerol or polyglycerol fatty acid esters is initially processed with intensive shearing to form a w/o pre-emulsion A and emulsifier II from the group of adducts of ethylene oxide with fatty alcohols and/or sterols and, optionally, fatty alcohols, the treatment being accompanied by gentle shearing.
It has surprisingly been found that the multiple w/o/w emulsions obtainable by the process according to the invention remain stable in storage for long periods, even in the event of significant variations in temperature. The invention includes the observation that multiple emulsions with distinctly improved biodegradability in relation to the prior art can be made available through the choice of the oils mentioned and the absence of polymeric stabilizers.
Oils
Suitable oils for the production of the multiple w/o/w emulsions according to the invention are
REFERENCES:
De Luca, et al., "A Stable w/o/w Multiple Emulsion", Cosmetics & Toiletries, vol. 105, Nov., 1990, pp. 65,66 and 69 only.
Matsumoto, et al., "An Attempt at Preparing Water-in-Oil-in-Water Multiple-Phase Emulsions", Journal of Colloid and Interface Science, vol. 57, No. 2, Nov., 1976, pp. 353-361.
Lin, et al., "Physical Parameters and Release Behaviors of W/O/W Multiple Emulsions Containing Cosurfactants and Different Specific Gravity of Oils", Pharm. Acta. Helv., 66, Nr. 12 (1991), pp. 342-347.
Dupinay, et al., "Mise en Gelule et Liberation D'un Principe Actif en Milieu Pateux", Bull. Tech./Gattefosse, Reg. 80, 27-31 (1987).
DeLuca, et al., "Les emulsions mutiples", International Journal of Cosmetic Science, 13, (1991), pp. 1-21.
Zhang, et al., "Preparation of Stable W/O/W Type Multiple Emulsion Containing Water-Soluble Drugs and in Vitro Evaluation of Its Drug-Releasing Properties", Yakugaku Zasshi 112 (1) (1992) pp. 73-80.
Law, et al., "Stabilisation of W/O/W Multiple Emulsions By Interfacial Complexation of Macromolecules and Nonionic Surfactants", Journal of Controlled Release, 3 (1986) pp. 279-290.
R. Perron et C. Paquot, "Preparation des ethers-oxydes symetriques derives des alcools aliphatiques satures a longue chaine", Bull Soc. Chim. France, No. 72, pp. 333-337.
ROEMPP Chemie Lexikon, vol. 5, 1992, pp. 4302-4303.
DeLuca et al. "A Stable W/O/W Multiple Emulsion", Cosmetics & Toiletries, vol. 105, pp. 65-66 (1990).
Henkel KGA (Oct.-1991), translation of WO 9115184.
Grossiord Jean-Louis
Le Hen-Ferrenbach Catherine
Magnet Armelle
Puisieux Francis
Seiller Monique
Drach John E.
Henkel Kommanditgesellschaft auf Aktien
Jaeschke Wayne C.
Millson Jr. Henry E.
Mullis Jeffrey C.
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