Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1989-07-28
1991-07-23
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424428, 424659, 424660, 514914, 514269, A61F 200, A61K 908
Patent
active
050342304
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
This invention offers ophthalmics which are useful for treatment of allergic eye diseases such as allergic conjunctivitis.
BACKGROUND OF THE INVENTION
Japanese Patent Publication ( Publication No. Sho 60-50197 ) discloses that the compound of the formula [I] and salts thereof ( hereinafter called as Compound [I]) are excellent anti-allergic drugs. ##STR2##
But, ophthalmic application of Compound [I] has not been studied, so, it is necessary to examine preparation methods of ophthalmic formulations and study the effect on allergic eye diseases.
As the result of our precise studies on preparation methods of ophthalmic formulations and the effect on allergic eye diseases, we found that Compound [I] has an excellent anti-allergic effect in eyes and has a possibility to be applied to stable and low irritative ophthalmics.
DISCLOSURE OF THE INVENTION
This invention relates to the anti-allergic ophthalmics containing the compound of the formula [I] or salts thereof ( hereinafter called as Compound [I]) as a main ingredient. ##STR3##
Examples of the salts of the compound [I] are metal salts such as potassium, sodium, calcium and magnesium and organic amine salts.
Compound [I] is already known to have an excellent anti-allergic effect However, the application to ophthalmics and its effect on allergic eye diseases have not been known.
Topical diseases such as eye diseases are efficiently treated by topical application of a drug and it is necessary to study a topical application of oral drug to ophthalmics
Especially, the potassium salt of Compound[I], that is 9-methyl-3-(1H-tetrazole-5-yl)-4H-pyrido[1,2-a]pyrimidine-4-one potassium salt ( hereinafter called as Compound A ), is an excellent anti-allergic drug, so we studied mainly an application of the potassium salt to ophthalmics.
Important factors for ophthalmics are not only to have excellent efficacy, but also low irritation because ophthalmics are administered directly to the eye, which is a highly sensitive organ.
Particularly, patients with allergic diseases complain of a strong pain in the eye, so less irritative ophthalmics are desired to treat such patients
As the result of the experiment using eye drops of Compound A as one of the examples, the details of which are described later in the article of the irritation test, we found that the eye drops cause little eye irritation and the ophthalmics of this invention are well applicable to anti-allergic ophthalmics.
Furthermore, in the case of eye drops, stability in solution is required, which is different from an oral drug, because the ingredients should be dissolved. We examined the stability of the eye drops of compound A. As the result of a preservation test during 6 months in the condition at 40.degree. C. and 75% of relative humidity, a notable change was not observed and the eye drops proved to have good stability.
These properties cannot be presumed from the properties of oral preparations and can be found only from the application study to ophthalmics.
We examined the efficacy of ophthalmics, which is the most important property, and found that Compound A showed strong anti-allergic effect by topical application, the details of which and described later in the disclosure of the pharmacological test using eye drops of Compound A, and the ophthalmics of this invention were very useful for treatment of allergic eye diseases, such as allergic conjunctivitis.
Furthermore, to apply a medical substance to eye drops, the solubility of the substance is an important factor.
If a substance is easily soluble in water, any particular consideration is not necessary.
But, if a medical substance is hardly soluble in water, or if a substance, once dissolved in water, is readily crystallized while storing, many kinds of studies are required to formulate such substance in eye drops.
Compound A, which is an excellent anti-allergic drug, is a water soluble substance, but, readily precipitates as crystals after being dissolved in water. So, such problem about soluability has to be solved to fo
REFERENCES:
patent: 4122274 (1978-10-01), Juby
Hikida Mitsushi
Iso Tadashi
Kawashima Youichi
Morita Takakazu
Page Thurman K.
Santen Pharmaceutical Co. Ltd.
Spear James M.
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