Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1987-09-23
1990-08-28
Griffin, Ronald W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514546, 514533, 514826, A61K 3112, A61K 3135
Patent
active
049525646
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel antiallergic agent
BACKGROUND ART
It has been reported that isoliquiritigenin, contained in an extract of Glycyrrihiza, exhibits an antiulcerous activity, and is used in the treatment of gastric ulcers (Japanese Patent Publication No. 8485/1973). However, it has previously been not known at all that isoliquiritigenin has the activity of ameliorating allergosis.
DISCLOSURE OF INVENTION
As a result of earnest investigations, the inventors of the present invention newly discovered that isoliquiritigenin has an excellent antiallergic activity and produces few side effects when administered for a long time, leading to the achievement of the present invention.
In other words, the present invention relates to an antiallergic agent containing isoliquiritigenin as an effective component.
Isoliquiritigenin according to the present invention can be provided as its salt, if necessary.
In accordance with the present invention, isoliquiritigenin can be orally or parenterally administered as an anti I-type allergic agent (e.g., by venous injection, hypodermic administration, or rectal administration) in order to cure, treat, and prevent asthma, allergic dermal diseases, ectopic and atopic dermatitis, allergic rhinitis, urticaria, and food allergies and can be prepared in a form suitable for each of these administration method. For example, such a medicine can be prepared by a known method with the addition of additives such as an atoxic excipient, binder, lubricant, disintegrator, antiseptic agent, isotonizing agent, stabilizer, dispersant, antioxidant, coloring agent, flavoring agent, or buffer.
Such a medicine can be prepared in any preparation form, such as a tablet, a capsule, granules, powder, fine granules, a pill, a troche, a suppository, an ointment, an injection agent, an emulsion, a suspension, or a syrup, corresponding to the use thereof. Examples of the above-described usable atoxic additives include starch, gelatine, glucose, lactose, fructose, maltose, magnesium carbonate, talc, magnesium stearate, methyl cellulose, carboxymethyl cellulose, gum arabic, polyethyleneglycol, propyleneglycol, petrolatum, Carbowax, glyceline, ethanol, simple syrup, i.e., concentrated sucrose solution in water, sodium chloride, sodium sulfite, sodium phosphate, citric acid, polyvinyl pyrolidone, and water. This preparation can include other medicines which are therapeutically useful
The content of isoliquiritigenin in this medicine depends upon the form thereof, but it is preferable that the medicine generally contains it in a concentration of 0.1 to 100 wt %.
It is possible to widely vary the dosage of the medicine of the present invention in accordance with the kind of warm-blooded animal including humans, to which the medicine is applied, the severity of symptoms, and the diagnosis of the doctor, but the dosage can generally be determined to be 0.01 to 300 mg/kg per day. However, it is possible to change the dosage range to correspond to the severity of the symptoms of the patient and the diagnosis of the doctor. The above-described dosage can be divided into one or more portions so that the medicine can be administered one or more times a day.
BEST MODE FOR CARRYING OUT THE INVENTION
The present invention is described below on the basis of examples of the pharmaceutical effects thereof and of prescription. However, as a matter of course, these examples do not limit the present invention.
EXAMPLE 1
(Toxicity)
Isoliquiritigenin was orally or intra-peritoneally administered to five 5-week-old ddY male mice. Consequently, it was determined that the minimum lethal dose was not less than 3000 mg/kg (oral administration) or not less than 1000 mg/kg (intra-peritoneal administration).
EXAMPLE 2
(Antiallergic Activity)
The Schultz-Dale test and the inhibition effect of the compound of the present invention on the liberation of histamines by a compound 48/80 indicate that isoliquiritigenin has an antiallergic activity.
1. Schultz-Dale reaction
(1) Active sens
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Matsumoto Hitoshi
Sato Toshio
Dainippon Ink and Chemicals Inc.
Griffin Ronald W.
Nippon Hypox Laboratories Incorporated
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