United States Patent:  5,958,876

Assignee:  Novartis AG (Basel, CH)

Filed:  March 12, 1998

The present invention relates to a cyclosporin-containing soft capsule preparation which contains a composition containing cyclosporin as an active ingredient; a non-hydrophilic component propylene carbonate or a mixture of propylene carbonate and a hydrophilic component polyethylene glycol, one or a mixture of two or more selected from the group consisting of an esterified compound of fatty acid and primary alcohol, medium chain fatty acid triglyceride and fatty acid monoglyceride as an oil component; and a surfactant having an HLB (Hydrophilic Lipophilic Balance) value of 8 to 17.

SUMMARY OF THE INVENTION

Therefore, it is an aspect of the present invention to provide a composition suitable for formulation into soft capsules, which comprises cyclosporin as an active ingredient; a second component selected from the group consisting of propylene carbonate as a non-hydrophilic substance and a mixture of propylene carbonate as a non-hydrophilic substance and polyethylene glycol as a hydrophilic substance; an oil component as defined below, and a surfactant. It is a further aspect of the present invention to provide a soft capsule preparation comprising a composition which contains cyclosporin as an active ingredient; a second component selected from the group consisting of propylene carbonate and a mixture of propylene carbonate and polyethylene glycol; one or a mixture of two or more selected from the group consisting of an esterified compound of fatty acid and primary alcohol, medium chain fatty acid triglyceride (if desired) and fatty acid monoglyceride as an oil component; and a surfactant having an HLB (Hydrophilic Lipophilic Balance) value of 8 to 17. Further it is another aspect of the present invention to provide a process for preparing the soft gelatin capsule preparation as defined above.

Even though the present invention is described herein particularly with respect to soft gelatine capsules, it is to be appreciated that the invention covers the composition itself, which may be used as such e.g. as a drink solution, e.g. as Sandimmun Neoral, or be in other unit dosage forms.

Claim 1 of 24 Claims

1. A pharmaceutical composition, comprising:

(1) pharmacologically effective amounts of cyclosporin,

(2) propylene carbonate,

(3) an oil component selected from the group consisting of an esterified compound of fatty acid and primary alcohol, medium chain fatty acid triglyceride and fatty acid monoglyceride; and

(4) a surfactant having HLB (Hydrophilic-lipophilic balance) value of 8 to 17,

wherein said cyclosporin, said propylene carbonate, said oil component and said surfactant are present in a ratio of 1:0.1-10:1-10:1-10, respectively, on the basis of weight.

____________________________________________
If you want to learn more about this patent, please go directly to the US Patent and Trademark Office web site to access the full patent.