Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1998-08-12
2000-05-02
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424465, 424468, 424470, 424477, 424481, 424500, A61K 920
Patent
active
060569743
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a rapid-release tablet of (+)-(Z)-calcium 7-[(1R,2S,3S,4S)-3-benzenesulfonamidobicyclo[2.2.1]hept-2-yl]-5-heptenoate dihydrate (hereinafter referred to as S1452). S1452 has been known to possess an antagonistic activity to thromboxane A.sub.2 (TXA.sub.2) receptor, thus the present preparation is useful as a medical preparation for diseases concerned with TXA.sub.2.
BACKGROUND ART
Japanese Laid-Open Patent Publication No. 63-139161 describes that a series of bicycle sulfonamide derivatives including S1452 possess an antagonistic activity to TXA.sub.2 receptor and is effective for the prevention or treatment of inflammation, hypertension, thrombosis, cerebral apoplexy, myocardial infarction, angina pectoris, cerebral infarction, asthma, and the like.
Japanese Laid-Open Patent Publication No. 2-160758 discloses the lysine salt corresponding to S1452.
Japanese Laid-Open Patent Publication No. 3-17054 describes that S1452 is stable crystal.
However, no embodiment of the preparation of S1452 is described in any of the above patent publications. Therefore, it has been desired to develop a medical preparation, especially tablets, with which S1452 can be suitably utilized as a medicine.
Additionally, a preparation containing silica (silicon dioxide) is described, for example, in Japanese Laid-Open Patent Publication Nos. 60-209518 and 2-178222, wherein the purpose of adding silica is to make tablets stabler in high-temperature storage, to prevent granules from adhering each other before coating them and the like, and so it is not related directly to the solubility of a principal agent in tablets. Namely, those technologies do not suggest the present invention at all.
DISCLOSURE OF INVENTION
Considering the above problems, the present inventors have studied on formulating S1452 into tablets. Usually, in order to enhancing the solubility of a principal agent in tablets, it is generally carried out to allow the principal agent to release at once by quickly disintegrating the tablets through the addition of disintegrators thereto. However, the present inventors have found that in the case of S1452 being formulated into tablets by merely adding disintegrator as usual, the solubility is well high at pH around neutral condition but remarkably low in an acidic solution. Therefore, it has been concerned that the dissolving of S1452 might be delayed in stomach when orally administered.
Then, the present inventors have further examined to find that the solubility of S1452 can be improved by adding, as an additive in preparing tablets, a dispersant in an amount enough to disperse the principal agent after the disintegration in a body.
BRIEF DESCRIPTION OF DRAWINGS
FIG. 1 shows, as to the tablet containing 25 mg of S1452, the relation between the amount of dispersants and the dissolving rate in an acidic solution. The axis of ordinate shows the dissolving rate (%) and the axis of abscissa shows the time (minute).
FIG. 2 shows, as to the tablet containing 50 mg of S1452, the relation between the amount of dispersants and the dissolving rate in an acidic solution The axis of ordinate shows the dissolving rate (%) and the axis of abscissa shows the time (minute).
BEST MODE FOR CARRYING OUT THE INVENTION
The present invention provides a rapid-release tablet of S1452 (hereinafter referred to as a tablet of the present invention ), which is characterized by at least containing the following components "a" and "b": 7-[(1R,2S,3S,4S)-3-benzenesulfonamidobicyclo[2.2.1]hept-2-yl]-5-heptenoate dihydrate (S1452), and the disintegration of the tablet.
The preferred embodiments of a tablet of the present invention are exemplified below. is 0.05 to 9 parts by weight to 100 parts by weight of the tablet. is 0.1 to 7 parts by weight to 100 parts by weight of the tablet. is 0.3 to 5 parts by weight to 100 parts by weight of the tablet. is 0.5 to 30 parts by weight to the principal agent. 0.3 to 5 parts by weight of silica to 100 parts by weight of the tablet. disintegrator. of the inte
REFERENCES:
patent: 4665018 (1987-05-01), Vold
patent: 4666703 (1987-05-01), Kopf
patent: 4861913 (1989-08-01), Narisada et al.
patent: 5168101 (1992-12-01), Arai et al.
patent: 5270055 (1993-12-01), Moest
Derwent, World Patent Index, Abstract 90-149201/20.
Derwent, World Patent Index, Abstract 85-250478/41.
Kadota Hitoshi
Suzuki Yoshikazu
Wakamiya Eizo
Page Thurman K.
Shionogi & Co. Ltd.
Tran Susan
LandOfFree
Rapid-release S1452 tablets does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Rapid-release S1452 tablets, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Rapid-release S1452 tablets will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1592056