Anti-androgenic preparation for oral cavity administration

Claim 1

A pharmaceutical preparation comprising an anti-androgenically active compound represented by the formula [I]: wherein the bond at the 10-position indicates a carbon-carbon single bond or a carbon-carbon double bond and A indicates a hydrogen atom or an ether or ester residue, and other appropriate components so that the preparation is in the form of an administration unit which is intended to be placed in the oral cavity of a patient to enable the anti-androgenically active compound of formula [I] to be absorbed through the oral mucous membrane, whereby said administration unit has a disintegration time of 30 minutes or longer as measured by the disintegration test defined below: Disintegration Test An administration unit is adhesively bonded to the interior of an auxiliary tube as defined in (c) below and the tube loaded with the administration unit is put into a vessel as defined in (a) below which contains 1000 ml of water at 37 + 0.5°C. An agitator as defined in (b) below is provided such that its paddle is disposed at the level 5.0 cm above the bottom of said vessel. The agitator is driven at a rate of 100 rpm and time required for disintegration of said administration unit is measured visually at 37 + 0.5°C. In the test: (a) the vessel, made of a transparent plastics, is a 1000 ml cylinder with a round bottom, 160-175 mm in height and 50-52.5 mm in radius; the upper mouth thereof defines a peripheral flat flange to hold a lid and said lid, transparent and circular with 140 mm diameter and 4 mm thick, has a groove-like break extending with 12 mm wide from its periphery to the center defining a hole with 16 mm diameter; (b) the agitator: the journal portion of the shaft is 6.0-10.5 mm in diameter and the portion for submersion in water 9.5-10.5 mm in diameter and 370-400 mm long in total; the paddle, mounted at the shaft bottom edge, is geometrically shaped from a circular plate having 83 mm in diameter and 3.0-5.0 mm thick, by two different parallel chords, a chord of 75 + 1 mm and of 42 + 1 mm; the intermediate portion between the above two parallel chords defines the dimension of said paddle and is mounted with the 42 mm chord being down side and through the shaft center; (c) the auxiliary tube: a transparent plastics tube, having a 17 mm outer and a 12 mm inner diameter and being 20 mm long, is tipped with screw thread on both outer ends; two short tubes with the same diameters and 2.5 mm long are likewise tipped with screw thread on either inner end to be couplable with the 20 mm tube ends; and two acid-resistant nets, 0.29 mm wire and 0.42 mm opening, are tightly closed with screws at both end-mounts of the 20 mm tube.