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US 4,071,623 AGranted
Pharmaceutical preparation adapted for oral administration
AssigneeAkzona Incorporated
InventorJohannes van der Vies
Life of this patent
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Abstract
The invention relates to a novel pharmaceutical preparation with oestrogenic activity adapted for oral administration comprising an oestradiol-17.beta.-ester, the ester group of which has been derived from aliphatic carboxylic acids having 9-16 carbon atoms, in combination with a non-steroidal lipoid. The preparation may additionally contain a progestational steroid or an androgen. The invention also relates to novel oestradiol-17.beta.-esters.
Claims32
A pharmaceutical preparation with oestrogenic activity adapted for oral administration comprising
- an oestrogenically effective amount when orally administered of at least one 17.beta.-ester of oestradiol having the formula ##STR2## the ester group thereof being derived from an aliphatic carboxylic acid having 9 to 16 carbon atoms, and
- a pharmaceutically acceptable non-steroid lipoid carrier, wherein said 17-.beta. ester of oestradiol constitutes from 0.01 to 50% by weight of said preparation and said non-steroid lipoid carrier is present in an amont of at least equal to the amount of said 17.beta.-ester of oestradiol.
A 17.beta.-ester of oestradiol having the formula:
- ##STR3## wherein n = 0, 1 or 2;
- R.sub.1 = alkyl having 1-10 carbon atoms;
- R.sub.2 = h or alkyl having 1-10 carbon atoms;
- R.sub.3 = an aliphatic group having 1-18 carbon atoms, which group may contain a ring having 5-12 carbon atoms;
- or R.sub.1 and R.sub.3 form together with the carbon atom to which they are attached and a cycloaliphatic group having 7-12 carbon atoms, said cycloaliphatic group optionally being substituted by an aliphatic group having 1-6 carbon atoms, with the proviso that the total number of carbon atoms in the ester group is in the range of 8-20 carbon atoms.
2 more elements
Dependencies are inferred from the claim text.