JP2003095934A - Analgesic agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an analgesic agent having an excellent analgesic effect and reduced adverse effects. SOLUTION: This analgesic agent contains ethenzamide and dicyclomine hydrochloride.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an analgesic.

[0002]

2. Description of the Related Art Ethenzamide has an excellent antipyretic and analgesic effect and is used as a single agent and also as a drug for general colds. However, etenzamid has side effects such as hypersensitivity such as rash and anorexia, heartburn, stomach pain, nausea and vomiting, and there is a problem that the dose cannot be increased to obtain a sufficient analgesic effect.

[0003]

SUMMARY OF THE INVENTION It is, therefore, an object of the present invention to provide a medicine which has reduced side effects and can exert the excellent analgesic effect of etenzamid.

[0004]

In view of the above situation, the present inventors have earnestly studied and, as a result, have surprisingly found that the combined use of etenzamid and the anticonvulsant dicyclomine hydrochloride synergistically enhances the analgesic effect. The present inventors have completed the present invention by discovering that even at a low dose, it exhibits excellent analgesic action and side effects can be reduced. That is, the present invention provides an analgesic containing ethenamide and dicyclomine hydrochloride.

[0005]

BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, dicyclomine hydrochloride used in combination with etenzamid has an excellent antispasmodic action,
It is mainly used as a therapeutic drug for alleviating tension of visceral smooth muscles associated with digestive system diseases, cholelithiasis, urolithiasis, dysmenorrhea and the like. However, dicyclomine hydrochloride has side effects such as hypersensitivity such as rash, headache, nausea, vomiting, loss of appetite, malaise, weakness, etc., and thus the dose cannot be increased. So far, no examples have been known in which both etenzamid and dicyclomine hydrochloride are used in combination.

The content ratio of ethenamide and dicyclomine hydrochloride in the analgesic of the present invention is preferably 1: 0.00033 to 1: 0.75 by weight, more preferably 1: 0. 0008 to 1: 0.4.

The analgesic agent of the present invention is effective for symptoms such as headache, toothache, menstrual pain, stomach pain, abdominal pain and joint pain. The analgesic of the present invention is an antipyretic analgesic such as acetaminophen, aspirin, and isopropylantipyrine, and a hypnotic sedative such as bromvalerylurea and allylisopropylacetylurea, caffeine, and vitamin agents as components other than ethenamide and dicyclomine hydrochloride. An antacid such as aminoacetic acid, or a crude drug (earth dragon, liquorice, cinnamon, salamander, etc.) can be added. Also, pharmaceutically acceptable carriers such as excipients, binders, fillers, disintegrants,
Surfactants, lubricants, dispersants, buffers, preservatives, corrigents, flavors and the like can be used in appropriate combination. Examples of the dosage form include oral administration by tablets, capsules, granules, powders, solutions, syrups and the like, and parenteral administration by suppositories and the like.

The dose of the analgesic of the present invention depends on age, body weight,
Depending on the symptoms, administration form, number of administrations, etc., for example, in the case of oral administration to an ordinary adult, once as an active ingredient (total amount of ethenamide and dicyclomine hydrochloride),
mg to 630 mg is preferred. The single oral dose of etenzamid is preferably 40 to 600 mg for adults, and 0.2 to 30 mg for dicyclomine hydrochloride.
In the case of oral administration, it can be administered once to several times a day.

[0009]

The present invention will be described in detail below with reference to examples, but the present invention is not limited thereto.

EXAMPLE 1 A test drug dissolved or suspended in physiological saline was intraperitoneally administered to male ICR mice that had been fasted overnight in a volume of 20 mL / kg. After 5 minutes, 16 mg / 10 mL / kg of acetylcholine was intraperitoneally administered, and the number of times of licing observed for 10 minutes immediately after the administration was measured. In each group, 15 animals were tested. The results are shown in Table 1.

[0011]

[Table 1]

By intraperitoneal administration of acetylcholine, 8.4 ± 1.02 times of licing were observed.
In contrast, intraperitoneal administration of etenzamid 40 mg / kg and dicyclomine hydrochloride 3 mg / kg was 49% and 8%, respectively.
Showed an inhibitory effect on. On the other hand, when both drugs are used together, 58%
It showed a suppressive effect on the, and a significant effect was recognized as compared with the control group. When this result was examined by the bulge method, the relative index (0.42) of the combination group was smaller than the product of the relative indices alone (0.51 × 0.92 = 0.47), and A synergistic effect was observed.

Production Example 1 1200 parts by weight of etenzamid, 50 of acetaminophen
0 parts by weight, bromvalerylurea 600 parts by weight, caffeine 150 parts by weight, hydroxypropyl cellulose 94.
5 parts by weight, low-substituted hydroxypropyl cellulose 15
An aqueous solution prepared by dissolving 450 parts by weight of water in 30 parts by weight of dicyclomine hydrochloride is added to a mixed powder consisting of 7.5 parts by weight and crystalline cellulose of 386.5 parts by weight, and wet granulation is performed.
After drying, 31.5 parts by weight of magnesium stearate was added, and the mixture was compression-molded with a tableting machine (Kikusui Seisakusho Collect 19TU) to give tablets of 350 mg each.

[0014]

[Table 2]

[0015]

INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide an analgesic agent having an excellent analgesic effect and reduced side effects.

Claims (3)

[Claims] 1. An analgesic containing etenzamid and dicyclomine hydrochloride. 2. The analgesic according to claim 1, wherein the content ratio by weight of ethenamide and dicyclomine hydrochloride is 1: 0.00033 to 1: 0.75. 3. The analgesic according to claim 1, wherein the content ratio by weight of ethenamide and dicyclomine hydrochloride is 1: 0.0008 to 1: 0.4.