Vesifact Ag

Ciba Specialty Chemicals Corporation

Other

Ciba-geigy Corporation

Novartis Corporation

Hans Georg Weder

Andreas Supersaxo

Dietmar Hüglin

Joachim Röding

Marc Antoine Weder

Peter Van Hoogevest

Ute Isele

Matthias Mutsch

The invention relates to compositions in the form of microemulsion preconcentrates that contain (a) a mixture that consists of a medium-chain triglyceride and an omega-9 fatty acid and/or an omega-6 fatty acid; and (b) a surface-active component that contains a polyoxethylene tenside. When contacted with water or with an aqueous medium these microemulsion preconcentrates form microemulsions. The microemulsions of the O/W type have an average particle size below 150 nm, preferably below 100 nm. The inventive microemulsion preconcentrates and microemulsions are suitable for use as vehicles for substances, namely active agents, that are hardly soluble in water, but soluble in components (a) and/or (b). In the aqueous phase, said microemulsions may contain water-soluble substances.

Microemulsion preconcentrate, microemulsion and use thereof

A nanodispersion comprises The nanodispersions prepared according to this invention are suitable as transport vehicles for pharmaceutical active agents.

Use of nanodispersions in pharmaceutical end formulations

A description is given of the use of a nanodispersion, which comprises The nanodispersions used according to this invention can be easily prepared and are suitable as carrier systems for a very wide range of cosmetic active agents and oil-soluble dyes.

Use of nanodispersions in cosmetic end formulations

A description is given of the use of a nanodispersion, which comprises The nanodispersions used according to this invention are suitable as transport vehicles for pharmaceutical active agents.

The cosmetic preparation contains: (a) an oil-soluble active ingredient that is suitable for skin cosmetics, (b) a partial fatty acid ester of polyoxyethylene sorbitan, (c) at least one phospholipid, (d) ethanol, and (e) water as a carrier liquid. The phospholipid is dissolved in ethanol, and then the partial fatty acid esters of polyoxyethylene sorbitan and the active ingredient are added. The oil phase that is obtained is added to water and stirred. The preparation is obtained in the form of a nanodispersion.

Cosmetic preparations

The present invention relates to a pharmaceutical composition for the intravenous administration of the sparingly soluble staurosporin derivative N-benzoyl-staurosporin. The composition comprises the following preferred components: a) the therpeutic agent N-benzoyl-staurosporin; b) a polyoxyethylene/polyoxypropylene block copolymer; c) ethanol and water as carrier liquids; and d) purified lecithin from soybeans and e) as water-soluble excipients glycerol and sorbitol.

Nanosuspensions for intravenous administration

The invention relates to a novel advantageous dosage form for sparingly soluble staurosporin derivatives, especially N-benzoyl-staurosporin. The dosage form is administrable intravenously in the form of a nanoemulsion and comprises as solubilisers a combination of phospholipids, triglycerides and partial fatty acid esters of polyoxyethylene sorbitan.

Intravenous solutions for a derivative of staurosporine

An aqueous phase, an oil of a triglyceride or fatty acid ester, and, per part by weight of oil 0.05 to 0.4 part by weight of an amphoteric emulsifier are mixed together and processed in a high-pressure homogenizer into a nanoemulsion of less than 200 nm sized oil particles. The emulsifier, exhibiting in the aqueous phase a lamellar liquid-crystalline structure, is preferably a glycerophosphatide of the formula: ##STR1## wherein, R.sub.1 and R.sub.2 mean acyloxy and/or alkyl or alkenyl ether. R.sub.3 is a tri-lower-alkyl ammonio or amino-substituted lower alkyl. The resultant nanoemulsion is stable for a period of several months and does not contain any toxic emulsifier materials. Therefore, it can be advantageously utilized as a vehicle for active agents, for example medicines and/or cosmetic ingredients.

Growing community of inventors

Rüschlikon, Switzerland

Hans Georg Weder