JPS58216119A - Antiulcer agent - Google Patents

Abstract

PURPOSE:To provide an antiulcer agent containing capsimycin as an active component. CONSTITUTION:The capsimycin of formula is used as an active component and is combined properly with a vehicle, a binder, a disintegrant, a lubricant, a fluidity improving agent, etc. to obtain an antiulcer agent for oral administration in the shape of tablet, capsule, granule, syrup, etc. Dose; 0.01-100mg/kg daily for adult in one or several divided doses.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a novel anti-ulcer agent containing casocimycin as an active ingredient. Kabushimycin is a compound that has only been known as an antibiotic effective against gray late blight and damping-off of cucumbers, but its pharmacological effects were completely unknown.

The present inventors have conducted extensive studies on the pharmacological activity of this kabushimycin, and have discovered that this compound exhibits an extremely excellent anti-ulcer effect, and have completed the present invention.

That is, the present invention provides an anti-ulcer agent containing kabushimycin represented by the following formula (1) as an active ingredient.

Kabushimycin of the present invention is a colorless needle-like crystal with a molecular formula of C, oH,, N20°, a molecular weight of 524.64, and a melting point of 186°C (min ps), and is soluble in chloroform, pyridine, ether, benzene, n-hexane, and water. It is an acidic compound that is insoluble in, and can be easily produced, for example, by the N1# method disclosed in JP-A No. 55-310.

The anti-ulcer effect of Kabushimaren is shown below.

(1) Effect of indomethacin on ulcer weight 180
A group of 6 male Donryu rats, aged ~200 y and 7 weeks old, were used, and after fasting for 48 hours, Kabushima Ren was dissolved in physiological saline containing 5 g of dimethyl sulfoxide to prepare a sample, and a predetermined amount of the sample was orally administered. .

One hour later, indomethacin was orally administered using a No. 25 tube, and 5 hours later, a 2-tibrilliant blue solution was administered intravenously, and the stomach was removed. The helmet was incised, the long axis of the generated ulcer site was measured, and the total value (in) was taken as the ulcer coefficient.

The results are shown in Table 1.

(2) Effect on stress ulcers A group of eight 5-week-old ddY male mice weighing 23 to 26 g were used as a sample by dissolving them in a physiological saline solution containing 5% dimethyl sulfoxide and a predetermined amount of the sample. was administered orally. The mice were held vertically and submerged up to their necks in a water bath with a water temperature of 26°C for 8 hours. 2 chips IJ 1
After intravenously administering the 7antoplue solution, the stomachs were removed and examined for the presence or absence of ulcer formation. The results are shown in Table 2.

As mentioned above, Kabushima Ren has an extremely excellent preventive effect on experimental ulcers. It's a drug.

Next, the administration method and dosage of the anti-ulcer agent of the present invention will be shown.

As for the administration method, oral administration using tablets, capsules, granules, syrups, etc. is preferred.

The dosage is usually o, as an oral dose in adults.
o i~100η/匈 is suitable.・Take this once a day or in divided doses.

Oral preparations can be manufactured according to conventional manufacturing methods. That is, test preparations of starch, lactose, mannitol, etc.
Binders such as carboxymethyl cellulose sodium and hydroxypropyl cellulose, disintegrants such as crystalline cellulose and carboxymethyl cellulose calcium, Merck,
Tablets, capsules, granules, etc. can be manufactured by appropriately combining and formulating a lubricant such as magnesium stearate, a fluidity improver such as light anhydrous silicic acid, and the like.

Next, the antiulcer agent of the present invention will be explained with reference to Examples.

Example 1 Tablet One tablet with the following ingredients and quantities was manufactured by a conventional method.

Kabushimiren 1009D-Ma/21
・-Rule 150 crystalline cellulose
50 de/def 28 carboxymethylcellulose 16 calcium talc 4 total ml 350■Example 2
CapsulesProduce granules with the following ingredients and amounts using a conventional method.
A capsule was manufactured by filling one No. 1 capsule.

Kabushimiren 259 Crystalline cellulose 17 types Light anhydrous silicone M 79

Claims (1)

[Claims] An anti-ulcer agent whose active ingredient is kabushimycin represented by the following formula.