Spontaneously dispersible concentrates and aqueous microemulsions with steryl retinates having anti-tumor activity
AssigneeMarigen S.A.
InventorsCarl Eugster, Conrad H. Eugster, Walter Haldemann, Giorgio Rivara
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Abstract
There are described spontaneously dispersible agents containing sterolester and/or sterolphosphor compounds having a pronounced antitumour activity. Novel sterolesters and sterolphosphor compounds, their use for treating tumors, and processes for their preparation are disclosed.
Claims9
A spontaneously dispersible concentrate which forms an ultramicroemulsion when diluted with water or a glucose solution comprising:
- 0.001 to 15% by weight of one or a combination of steryl ester compounds selected from the group consisting of compounds of formulae (I) to (XII):
- ##STR31## wherein R.sub.1 represents a C.sub.1-10 alkyl or a C.sub.2-10 alkenyl group and R.sub.2 represents a member selected from the group consisting of formulae (XVI) and (XVII):
- ##STR32## wherein n is 1, 2, 3, 4, or 5, and R.sub.5 represents a radical selected from the group consisting of ##STR33## 0to 40% by weight of a pharmaceutically acceptable solvent or solvent mixture which acts as a hydrotropic agent or co-emulsifier;
- 0. 001 to 90% by weight of a pharmaceutically acceptable surfactant or surfactant mixture;
- 0 to 10% by weight of a vitamin or provitamin,
- up to 10% by weight of a free fatty acid, and
- a pharmaceutically acceptable carrier or diluent.
A composition which inhibits the growth of tumor cells comprising 25 parts by weight of a spontaneously dispersible concentrate as claimed in claim 4, 44 parts by weight of a core material for granules or pellets, and 31 parts by weight of an enteric coating comprising hydroxypropyl methyl acetate succinate.
A steryl ester selected from the group consisting of compounds of formulae (I) to (XII):
- ##STR36## wherein R.sub.1 represents a C.sub.1-10 alkyl or a C.sub.2-10 alkenyl group and R.sub.2 represents a member selected from the group consisting of formulae (XVI) and (XVII):
- ##STR37## wherein n is 1, 2, 3, 4, or 5, and R.sub.5 represents a radical selected from the group consisting of ##STR38## or R.sub.5 represents a group of formula (XX) or (XXII):
- ##STR39## with the proviso that the ester is not cholest-5-en-3-all trans retinate.
Dependencies are inferred from the claim text.