Novartis Ag

Novartis Corporation

Sandoz Gmbh

Birgit Hauer

Ulrich Posanski

Armin Meinzer

Friedrich Richter

Jacky Vonderscher

Lorenz Hahn

Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva]-Ciclosporin, in 'microemulsion pre-concentrate' and microemulsion form. The compositions typically comprise (1.1) a Calkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.

Pharmaceutical compositions comprising cyclosporins

Pharmaceutical compositions comprising a cyclosporin in a novel galenic formulations for oral administration. The compositions typically comprise a cyclosporin, 1,2-propylene glycol, a mixed mono-, di- and tri-glyceride and a hydrophilic surfactant. Further a refined glycerol-transesterified corn oil is provided representing a mixed mono-, di- and tri-glyceride suitable for the novel formulation. Dosage forms include in particular oral dosage forms.

Pharmaceutical Composition

Pharmaceutical compositions containing cyclosporin as the active agent

Pharmaceutical compositions comprising a cyclosporin in a novel galenic formulations for oral administration. The compositions typically comprise a cyclosporin, 1,2-propylene glycol, a mixed mono-,di- and tri-glyceride and a hydrophilic surfactant. Further a refined glycerol-transesterified corn oil is provided representing a mixed mono-, di- and tri-glyceride suitable for the novel formulation. Dosage forms include in particular oral dosage forms.

Pharmaceutical composition

Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva].sup.2 -Ciclosporin, in 'microemulsion pre-concentrate' and microemulsion form. The compositions typically comprise (1.1) a C.sub.1-5 -alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.

Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva].sup.2 -Ciclosporin, in 'microemulsion pre-concentrate' and microemulsion form. The compositions typically comprise (1.1) a C.sub.1-5 alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.

Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or �Nva!.sup.2 -Ciclosporin, in 'microemulsion pre-concentrate' and microemulsion form. The compositions typically comprise (1.1) a C.sub.1-5 alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.

A combination of a pharmacologically active compound and a water soluble monoester of a saturated or unsaturated (C.sub.6-18) fatty acid and a polyol, especially a saccharide, particularly as a solid solution of the active compound in the monoester. The solid solution is especially suitable for substantially water insoluble active compounds, particularly such polypeptides, e.g. ciclosporins and is in all desirable weight ratios miscible with water. The invention also, in particular, provides pharmaceutical compositions comprising a cyclosporin as active ingredient together with a fatty acid saccharide monoester.

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Lahr, Germany

Birgit Hauer