Claims
- 1. An intraoral quickly disintegrating tablet comprising a cyclic GMP phosphodiesterase inhibitor and a saccharide selected from the group consisting of mannitol, xylitol, and erythritol,wherein the saccharide is present in a ratio of 4 to 30 parts by weight to 1 part by weight of the cyclic GMP phosphodiesterase inhibitor.
- 2. The tablet as claimed in claim 1, which further comprises a binder.
- 3. A method for manufacturing the tablet defined in claim 1, which comprises mixing a cyclic GMP phosphodiesterase inhibitor with a saccharide, kneading the mixture with an organic solvent, water or an aqueous organic solvent and subjecting it to a compression-molding.
- 4. The method as claimed in claim 3, which comprises filling the kneaded mixture in a mold and subjecting it to a compression-molding with a film.
- 5. The tablet as claimed in any one of claims 1 or 2, wherein the cyclic GMP phosphodiesterase inhibitor is selected from the group consisting of:5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one represented the formula (I) 1,3-dimethyl-6-(2-propoxy-5-methanesulfonamidophenyl)-1,5-dihydropyrazolo[3,4-d]pyrimidin-4-one represented by the formula (II) 2-(4-carboxypiperidino)-4-(3,4-methylenedioxybenzyl)amino-6-chloroquinazoline represented by the formula (III) (6R,12aR)-2,3,6,7,12,12a-hexahydro-2-methyl-6-(3,4-methylenedioxyphenyl)-pyrazino[2′, 1′:6,1]pyrido[3,4-b]-indol-1,4-dione represented by the formula (IV) (3S,6R,12aR)-2,3,6,7,12,12a-hexahydro-2,3-dimethyl-6-(3,4-methylenedioxyphenyl)-pyrazino[2′, 1′:6,1]pyrido[3,4-b]-indol-1,4-dione shown by the formula (V) or a pharmacologically acceptable salt thereof.
- 6. The tablet as claimed in any one of claims 1 or 2, wherein the cyclic GMP phosphodiesterase inhibitor is a compound selected from the group consisting of:4-(3-chloro-4-methoxybenzyl)amino-6-cyano-1-(4-hydroxypiperidino)phthalazine hydrochloride represented by the formula (IX) 4-(3-chloro-4-methoxyphenethyl)amino-6-cyano-1-(4-hydroxypiperidino)phthalazine hydrochloride represented by the formula (X) 4-[(3-chloro-4-methoxybenzyl)amino]-1-(2-hydroxy-7-azaspiro[3,5]non-7-yl)-6-phthalazine carbonitrile hydrochloride represented by the formula (XI) 1-(2-hydroxy-7-azaspiro[3,5]non-7-yl)-4-[(4-methoxy-3-methylbenzyl)amino]-6-phthalazine carbonitrile hydrochloride represented by the formula (XII) 1-[4-fluoro-4-(hydroxymethyl)piperidino]-4-[(4-methoxy-3-methylbenzyl)amino]-6-phthalazine carbonitrile hydrochloride represented by the formula (XIII) 4-[(3-chloro-4-methoxyphenethyl)amino]-1-(2-hydroxy-7-azaspiro[3,5]non-7-yl)-6-phthalazine carbonitrile hydrochloride shown by the formula (XIV) 4-[(3-chloro-4-methoxybenzyl)amino]-1-(3-oxo-2-oxa-8-azaspiro[4,5]decen-8-yl)-6-phthalazine carbonitrile represented by the formula (XV).
- 7. The method for manufacturing as claimed in any one of claims 3 or 4, wherein the cyclic GMP phosphodiesterase inhibitor is selected from the group consisting of:5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one represented by the formula (I), and a compound represented by the formula (VI), or pharmacologically acceptable salts thereof.
Priority Claims (2)
Number |
Date |
Country |
Kind |
10-282378 |
Oct 1998 |
JP |
|
10-295947 |
Oct 1998 |
JP |
|
Parent Case Info
This application is the national phase under 35 U.S.C. §371 of PCT International Application No. PCT/JP99/05298 which has an International filing date of Sep. 28, 1999, which designated the United States of America.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
PCT/JP99/05298 |
|
WO |
00 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO00/20033 |
4/13/2000 |
WO |
A |
US Referenced Citations (9)
Foreign Referenced Citations (33)
Number |
Date |
Country |
0521310 |
Jan 1993 |
EP |
A2521310 |
Jan 1993 |
EP |
0636626 |
Feb 1995 |
EP |
A1636626 |
Feb 1995 |
EP |
A1779887 |
Jun 1997 |
EP |
0807433 |
Nov 1997 |
EP |
A1807433 |
Nov 1997 |
EP |
A5622725 |
Mar 1981 |
JP |
56022725 |
Mar 1981 |
JP |
58183615 |
Oct 1983 |
JP |
5914446 |
Apr 1984 |
JP |
05271054 |
Oct 1993 |
JP |
06218028 |
Aug 1994 |
JP |
770128 |
Mar 1995 |
JP |
0819589 |
Jan 1996 |
JP |
08310969 |
Nov 1996 |
JP |
A8310969 |
Nov 1996 |
JP |
0948726 |
Feb 1997 |
JP |
9503996 |
Apr 1997 |
JP |
10114657 |
May 1998 |
JP |
A10167966 |
Jun 1998 |
JP |
10167966 |
Jun 1998 |
JP |
2807346 |
Jul 1998 |
JP |
A1937124 |
Apr 1993 |
WO |
9307124 |
Apr 1993 |
WO |
9319742 |
Oct 1993 |
WO |
A1-9319742 |
Oct 1993 |
WO |
9428902 |
Dec 1994 |
WO |
9703070 |
Jan 1997 |
WO |
A1973675 |
Feb 1997 |
WO |
9703675 |
Feb 1997 |
WO |
A1987430 |
Feb 1998 |
WO |
9807430 |
Feb 1998 |
WO |
Non-Patent Literature Citations (1)
Entry |
M. Boolell et al., British Journal of Urology, 78, pp. 257-261 (1996). |