Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2000-01-21
2001-08-14
Reamer, James H. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
06274609
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to a pharmaceutical composition comprising as a main component 4-oxo-8-[4-(4-phenylbutoxy)benzoylamino]-2-(tetrazol-5-yl)-4H-1-benzopyran or its hydrate. In particular, it relates to an aqueous liquid pharmaceutical composition containing the benzopyran derivative or its hydrate in higher concentration and having good properties.
BACKGROUND OF THE INVENTION
4-Oxo-8-[4-(4-phenylbutoxy)benzoylamino]-2-(tetrazol-5-yl)-4H-1-benzopyran is an antagonist toward leukotrienes (LTC4, LTD4, LTE4) and is known to be a medicine having excellent pharmacological activities on various allergic diseases including asthma (JP-A 61-50977). Its ½ hydrate is called as “pranlukast” and is utilized as an anti-allergic medicine. Then, in the field of ophthalmology, it has been proposed to apply such a medicine to allergic eye diseases such as vernal keratoconjunctivitis, etc.
In general, for preparing an aqueous liquid pharmaceutical composition such as water-soluble eye drops, it is considered that a pharmacologically active component should be present in concentration of about 0.01 to 0.1%. However, 4-oxo-8-[4-(4-phenylbutoxy)benzoylamino]-2-(tetrazol-5-yl)-4H -1-benzopyran and its hydrate (hereinafter, they are referred to as “pranlukast” all together, unless otherwise stated) have very low water-solubility, which makes every difficult to prepare a useful aqueous liquid pharmaceutical composition thereof. Then, the use of polyvinyl pyrrolidone and &bgr;-cyclodextrin has been proposed to solubilize pranlukast (JP-A 8-73353).
However, even if polyvinyl pyrrolidone, which is a material known to have strongest solubilization power, is used, pranlukast dissolves in water in concentration of, at highest, about 0.01%.
OBJECTS OF THE INVENTION
The main object of the present invention is to promote solubilization or suspension of pranlukast in water, thereby providing an aqueous liquid pharmaceutical composition containing higher concentration of pranlukast and having good properties.
This object as well as other objects and advantages of the present invention will become apparent to those skilled in the art from the following description with reference to the attached drawings.
REFERENCES:
patent: 5976760 (1999-03-01), Sasatani et al.
patent: 0641569 (1995-03-01), None
patent: 96/41628 (1996-12-01), None
Database WPI, Section Ch, Week 9621, Derwent Publications Ltd., London, GB; Class A96, AN 96-205438, XP002081469 & JP 08 073353 A (Ono Pharmaceutical) Mar. 19, 1996.
Ii Yoshinori
Ogawa Takahiro
Terai Tadashi
Yasueda Shin-ichi
Ono Pharmaceutical Co. Ltd.
Reamer James H.
Wenderoth, Lind & Ponac L.L.P.
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