Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-01-06
2000-11-14
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514455, 514912, A61K 31435
Patent
active
061470813
DESCRIPTION:
BRIEF SUMMARY
This is a 371 of International Patent Application No. PCT/JP97/03444, with an international filing date of Sep. 26, 1997, now pending.
TECHNICAL FIELD
This invention relates to an ophthalmic preparation comprising sodium cromoglycate, an antihistaminic, and menthol, which does not produce unpleasant irritating sensation on instillation and produces a prompt action and a strong antipruritic effect immediately after instillation.
BACKGROUND ART
Mechanisms of onset of typical allergy are known to include the following steps. First, antigens foreign to the organism invade organisms. When exposed to these antigens, the organisms produce IgE antibodies against the antigens. Produced IgE adheres to the surface of mast cells to form IgE-bound mast cells. On renewed invasion of the antigens to the organisms with IgE-bound mast cells, antigen-antibody reactions occur at the surface of IgE-bound mast cells. As a result, various chemical mediators, such as histamine or leucotrienes, are released through degranulation of the IgE-bound mast cells. Allergic reactions occur by the actions of these chemical mediators.
To suppress these allergic reactions various drugs have been developed. For example, sodium cromoglycate is an antiallergic agent that suppresses the degranulation of mast cells and the release of chemical mediators such as histamine. It is used clinically as inhalant, nasal drops, ophthalmic preparations, and drugs for internal use as a superb preventive antiallergic agent. Especially, in the ophthalmologic field, it is used as ophthalmic preparations for allergic conjunctivitis and vernal conjunctivitis in Japan. However, since the mechanism of action of sodium cromoglycate lies in the inhibition of degranulation of mast cells, it cannot block the effects of chemical mediators already released. It is inferior in prompt action and must be administered about 4 weeks ahead of the onset of symptoms. Another drawback of sodium cromoglycate ophthalmic preparations is that it may produce eye-ache (irritating pain) at the time of instillation (Allergy Immunological and Clinical Aspects, A Wiley Medical Publication and JP-A-Sho 61-246117). Thus, sodium cromoglycate ophthalmic preparations are not satisfactory from the viewpoint of eye irritation.
Consequently, in order to add an effect of prompt onset to antiallergic ophthalmic preparations containing sodium cromoglycate, combination ophthalmic preparations have been developed in which sodium cromoglycate is formulated together with an antihistaminic that blocks released histamine. For example, a combination ophthalmic preparation containing 1.0% of sodium cromoglycate and 0.015% of chlorpheniramine maleate, an antihistaminic, has been subjected to clinical test in Japan (Igaku to Yakugaku 34(3) 507, 1995). Combination ophthalmic preparations containing sodium cromoglycate and chlorpheniramine maleate, an antihistaminic, are being used abroad (MARTINDALE The Extra Pharmacopoeia 30th Edition, The Pharmaceutical Press, 1993). These combination ophthalmic preparations containing sodium cromoglycate and an antihistaminic can produce a prompt antipruritic effect due to the antihistaminic, even when applied after the onset of allergic symptoms. However, the antipruritic effect of these ophthalmic preparations are not so strong as to prevent patients from scratching eyes due to severe itchiness, which results in development of inflammation of eye mucosa. Furthermore, since alleviation of the eye-irritating action was not taken into consideration, patients had to endure the pain upon use.
JP-A-Sho 61-246117 discloses that it is desirable to dissolve sodium cromoglycate in a solvent containing sodium bicarbonate and boric acid and adjust pH to neutral in order to alleviate the eye-ache at the time of instillation of the antiallergic ophthalmic preparation. However, sodium cromoglycate ophthalmic preparations having preventive antiallergic effects with prompt onset of action could not be obtained by the method described in the above publication. Furthermore, a supplemen
REFERENCES:
M.H. Lessof et al., "Allergy," pp. 354-357 (1984).
James E.F. Reynolds et al., "Martindale," pp. 1145, 1534, 1804, 1898 (1993).
Research Disclosure, p. 914 (Dec., 1990).
Etsuko Takamura et al., "Igaku to Yakugaku" 34(3):507-513 (1995) with English Language descriptors attached).
Aramaki, T. and Taniguchi, Igaku To Yakugaku, 34(4):693-699, 1995.
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Rikagaku Jiten (Physicochemical Dictionary), 4th ed., p. 1288, 1989.
Hirokawa Yakukagakudaijiten (Pharmaceutical Dictionary), 2nd ed., p. 1396, 1990.
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Carpenter et al., "Chemical Burns of the Rabbit Cornea," Am. J. Ophthal. 29:1363-1372, 1949.
Noyori Sachiko
Takagi Noriko
Fay Zohreh
Rohto Pharmaceutical Co. Ltd.
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