Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1995-05-09
1997-12-16
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424458, 424489, 424470, A61K 920
Patent
active
056982216
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a water-dispersible tablet formulation containing 4-amino-2-(4-methylpiperazin-1-yl)-5-(2,3,5-trichlorophenyl)pyrimidine.
European Patent Specification No. 372934 discloses the compound 4-amino-2-(4-methylpiperazin-1-yl)-5-(2,3,5-trichlorophenyl)-pyrimidine (hereinafter referred to as "AMTP") and their use in the treatment of neurodegenerative and other neurological disorders of the central nervous system, the aetiology of which includes excessive release of neurotransmitter glutamate, including Alzheimer's disease, cerebral ischemic damage, chronic pain and epilepsy.
In order to be able to administer AMTP to patients to achieve the optimum therapeutic benefit from the drug, it would be desirable to present the drug in a pharmaceutical formulation that is capable of rapid dispersion in water.
Following extensive research and investigation, we have now discovered a tablet formulation for AMTP that is capable of rapid dispersion in water.
According to one aspect of the present invention there is provided a water-dispersible tablet comprising within the granules of the tablet AMTP together with a pharmaceutically acceptable swellable clay disintegrating agent to provide a tablet which is capable of dispersing in water within a period of 3 minutes to provide a dispersion which is capable of passing through a sieve screen with a mesh aperture of 710 .mu.m in accordance with the test for dispersible tablets defined in the British Pharmacopoeia, 1988, Volume II, page 895 which disclosure is herein incorporated by reference.
According to a further aspect of the present invention there is provided a water-dispersible tablet comprising within the granules of the tablet AMTP together with a pharmaceutically acceptable swellable clay disintegrating agent and a further pharmaceutically acceptable disintegrating agent to provide a tablet which is capable of dispersing in water within a period of 3 minutes to provide a dispersion which is capable of passing through a sieve screen with a mesh aperture of 710 .mu.m in accordance with the test for dispersible tablets defined in the British Pharmacopoeia, 1988, Volume II page 895 which disclosure is herein incorporated by reference.
The above-mentioned test for dispersion time is carried out using the following apparatus and method:
(a) A rigid basket-rack assembly supporting six cylindrical glass tubes 75.0 to 80.0 mm long, 21.5 mm in internal diameter and with a wall thickness of about 2 mm.
(b) A cylindrical disc for each tube, each 20.55 to 20.85 mm in diameter and 9.35 to 9.65 mm thick, made of transparent plastic with a relative density of 1.18 to 1.20, pierced with five holes, each 2 mm in diameter, one in the centre and the other four spaced equally on a circle of radius 6 mm from the centre of the disc. Four equally spaced grooves are cut in the lateral surface of the disc in such a way that at the upper surface of the disc they are 9.5 mm wide and 2.55 mm deep and at the lower surface 1.6 mm square.
(c) The tubes are held vertically by two superimposed transparent plastic plates 90 mm in diameter and 6 mm thick, perforated by six holes having the same diameter as the tubes. The holes are equidistant from the centre of the plate and are equally spaced from one another. Attached to the underside of the lower plate is a piece of woven gauze made from stainless steel wire 0.635 mm in diameter and having nominal mesh apertures of 2.00 mm.
(d) The plates are held rigidly in position and 77.5 mm apart by vertical metal rods at the periphery and a metal rod is also fixed to the centre of the upper plate to enable the assembly to be attached to a mechanical device capable of raising and lowering it smoothly through a distance of 50 to 60 mm at a constant frequency of between 28 and 32 cycles per minute.
(e) The assembly is suspended in the liquid medium in a suitable vessel, preferably a 1000-ml beaker. The volume of liquid is such that when the assembly is in the highest position the wire mesh is at least 15 mm below the surface of the liqu
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Salo et al, P
Fielden Krystyna Elzbieta
Gamlen Michael John Desmond
Patel Suryakant Dahyabhai
Benston, Jr. William E.
Page Thurman K.
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