WO2006129479A1

WO2006129479A1 - Gastrointestinal drug composition

Info

Publication number: WO2006129479A1
Application number: PCT/JP2006/309791
Authority: WO
Inventors: Tomohiko Nakata; Ryou Kanaya; Norikazu Yamaguchi; Akiyoshi Oohira
Original assignee: Kowa Company, Ltd.
Priority date: 2005-05-30
Filing date: 2006-05-17
Publication date: 2006-12-07
Also published as: TWI430807B; CN101141972A; JPWO2006129479A1; TW200716160A; KR20080026084A; KR101254511B1; JP5070047B2

Abstract

Disclosed is a gastrointestinal agent having a significantly enhanced effect of a gastrointestinal drug. A gastrointestinal agent composition comprising methylmethionine sulfoniumchloride and a herb Atractylodis Lanceae Rhizoma, particularly for the prevention of eructation, nausea or vomiting or the alleviation of early satiety, feeling of heavy stomach, dyspepsia, gastric or abdominal bloating or anorexia.

Description

Specification

Gastrointestinal composition

Technical field

[0001] The present invention relates to a gastrointestinal pharmaceutical composition comprising methylmethionine sulfomum chloride (MMSC) and sputum with significantly enhanced efficacy.

Background art

[0002] In general, gastrointestinal drugs are used to relieve symptoms such as overeating, heartburn, leaning, stomach pain, nausea and vomiting, and to maintain the gastrointestinal state in a healthy state. This medicine is widely used for gastrointestinal drugs, and is subdivided into digestive drugs, stomachic drugs, antacids, compound gastrointestinal drugs, gastrointestinal analgesics and antispasmodics.

[0003] Methylmethionine sulfomum chloride (MMSC) is widely used as a component of gastrointestinal drugs, particularly complex gastrointestinal drugs, because it has the action of repairing rough gastric mucosa. In addition, Sojitsu is a rhizome of Atractylodes lancea De Candolle or Atra ctylodes chinensis Koidzumi, and is recognized as an ancient biomedicine, and is mainly used as a healthy stomach-disinfectant and antistatic agent. (Non-Patent Document 1). However, so far, there is no pharmaceutical composition containing both, particularly gastrointestinal drugs.

[0004] Non-Patent Document 1: 14th Revised Japanese Pharmacopoeia, 2001, D-674-677

Disclosure of the invention

Problems to be solved by the invention

[0005] An object of the present invention is to provide a new gastrointestinal drug composition that is significantly more effective than conventional gastrointestinal drugs.

Means for solving the problem

[0006] The present inventors combined methylmethionine sulfo-muchloride (MMSC), which is known as a gastric mucosal repair agent, with sputum, which is known as a healthy gastrointestinal digestive or antistatic antienteric agent. When used, it exhibits a significant gastrointestinal motility activation, resulting in suppression of burping, scalding, nausea or vomiting, or chest gripping, leaning, indigestion, stomach bloating or loss of appetite I found out that the effect as a gastrointestinal medicine such as elimination is drastically increased. The present invention has been completed.

That is, the present invention provides a gastrointestinal composition containing MMSC and sputum. The present invention also relates to a gastrointestinal composition comprising MMSC and sputum for suppressing belching, scalding, nausea or vomiting, or holding the chest, leaning, indigestion, gastric 'abdominal bloating or loss of appetite. About.

The invention's effect

[0008] The gastrointestinal composition of the present invention has MMS C due to a synergistically enhanced gastrointestinal motility activation effect that cannot be obtained by using MMSC or sputum alone, respectively. It has the effect of significantly reducing the effects of suppressing burping, scorching, nausea or vomiting, or holding the chest, leaning, poor extinction, fullness of stomach / abdomen or loss of appetite.

BEST MODE FOR CARRYING OUT THE INVENTION

[0009] MMSC is a drug that was launched in 1959 and has been used mainly as a gastric mucosal repair agent or for improving liver function in chronic liver disease. However, when used in combination with MMSC and sputum, it exhibits significant gastrointestinal motility activity, resulting in the suppression of burping, scalding, nausea or vomiting, or chest gripping, leaning, and extinguishing. There has been no report or suggestion so far that the effect of resolving poor malformation, stomach bloating or loss of appetite can be significantly improved compared to using MMSC alone.

[0010] In addition, with regard to sputum, the function that enhances motility of the digestive tract has been known (Non-patent Document 1), but the function that can be used in combination with MMSC is synergistically enhanced. As a result, M MSC There has been no report or suggestion so far about the synergistic enhancement of the effect as a gastrointestinal composition containing gut and sputum.

[0011] The present invention provides a gastrointestinal composition having a synergistically enhanced effect that cannot be achieved by using each of the MMSC and sputum, which has not been used in combination in the past. Is.

[0012] The gastrointestinal composition of the present invention has an action of activating the motion of the digestive tract represented by the intestinal tract transport rate, as shown in Examples described later. The effect is MMSC, られる It is recognized that the activity of the gastrointestinal tract is activated by a synergistic effect that is significantly higher than the sum of the effects observed when each is used alone.

[0013] Although not bound by the following reasoning, in the present invention, the synergistic activation of such gastrointestinal motility results in burping, peeling, Symptoms such as vomiting, chest gripping, leaning, indigestion, stomach and abdominal bloating and loss of appetite, especially those symptoms caused by excessive drinking or eating too much compared to using MMSC or sputum alone It is inferred that this has been improved. In addition, synergistic activation of gastrointestinal motility eliminates the retention of intestinal contents and promotes the promotion of digestion more strongly.

[0014] The MMSC used in the present invention may be, for example, commercially available from Yonezawa Hamari Chemical Co., Ltd., or synthesized according to the method described in JP-B 36-13209. May be used. As for koji, it is only necessary to obtain and use those widely distributed and used as herbal ingredients.

[0015] The combination ratio of MMSC and koji and their synergistic effect! / In terms of weight ratio, MMSC: koji (in terms of drug substance) 9 parts: 8 parts to 3 parts: 500 parts, especially 1 part: 2 parts to 1 part: In the case of 5 parts, the synergistic effect of the combined use can be exhibited particularly strongly. In addition, the blending amounts in the MMSC and salmon compositions may be determined and used in amounts that satisfy the blending ratio of the previous period from the range of amounts that can be blended as the gastrointestinal composition.

[0016] In addition to MMSC and sputum, the gastrointestinal composition of the present invention includes a pharmaceutically acceptable carrier and other pharmaceutical ingredients, excipients, binders, disintegrants, lubricants, colorants, It can also be used in the form of a pharmaceutical composition containing a corrigent and the like.

[0017] Examples of the excipient include lactose, starches, crystalline cellulose, sucrose, mannitol, light anhydrous hydrous key acid and the like. Examples of the binder include hydroxypropylmethylcellulose, hydroxypropylcellulose, gelatin, alpha-monified starch, polybulurpyrrolidone, polybullic alcohol, and pullulan. Examples of the disintegrant include carmellose, carmellose calcium, croscarmellose sodium, crospovidone, corn starch, and low-substituted hydroxypropylcellulose. Examples of lubricants include magnesium stearate and talc. Coloring agents include tar pigments and iron sesquioxide Etc. Examples of the corrigent include stevia, aspartame, and fragrances.

[0018] The gastrointestinal composition of the present invention is a dosage form such as powder, granule, tablet, wearable tablet, film-coated tablet, sugar-coated tablet, drink, soft capsule, hard capsule, jelly, etc., depending on the purpose. Can be manufactured and used. In particular, it is preferable to manufacture and use powders, granules, tablets, and film-coated tablets.

[0019] The dose of a gastrointestinal composition containing MMSC and sputum to humans depends on factors such as the dosage form, the degree of disease, the age of the patient, etc., but is usually based on MMSC for adults. The dose of sputum can be determined according to the dose that should be sufficient if it is administered about 30 to 3000 mgZ days, particularly about 100 to 225 mgZ days.

[0020] Hereinafter, the present invention will be specifically described with reference to examples, but the present invention is not limited thereto.

Example 1

[0021] Five-week-old male ddY mice fasted the day before the test were treated with methylmethioninesulfo-um chloride (1000 mgZkg, hereinafter referred to as M) suspended in 0.5% methylcellulose (hereinafter referred to as MC), dried dried juicy extract. S (300 mgZkg, 3000 mgZkg as the bulk drug substance, hereinafter referred to as S) and a mixture thereof (hereinafter referred to as M + S) were orally administered, and 15 minutes later, the activated carbon powder suspension was orally administered. 30 minutes later, the animal was killed by cervical dislocation, and the intestine from the pylorus to the ileocecal region was removed. The intestinal transport ability of the test substance was expressed as the intestinal transport rate by dividing the distance of carbon powder from the pylorus by the total length of the intestinal tract.

[0022] The test results are shown in Table 1.

[table 1]

Group fli ^ ifi ^ rate (%) ratio ¹ )

(Naoshi Hiraiso SE)

Conte '48. 5 ± 3.5. 5 1. 00

M 69.0 ± 1. 1 1.42

S 53.0 ± 3. 1 1. 09

M + S 76.2 ± 2.8 1. 57

M: Methinolemethionine Norehonum Chloride

S: Souju dried extract S

1): Ratio of intestinal transport rate when the intestinal transport rate of the control mouth group is 1.

[0023] The intestinal transport rate was 48.5% in the control group administered MC, 69.0% in the M group, 53.0% in the S group, and 76.2% in the M + S group. When the intestinal transport rate of the control group is 1, the ratio of the intestinal transport rate of the M + S group is 1.57, which is judged to have a large synergistic effect compared with the simple group product of 1.55 (1.42 X 1.09). It was. From this, the present invention promotes the gastrointestinal motility function, and as a result, suppresses burping, scalding, nausea or vomiting, or chest hold, leaning, indigestion, stomach / abdominal bloating or loss of appetite, etc. Thus, it was revealed that the composition was extremely useful as a gastrointestinal composition that was significantly enhanced.

Example 2

[0024] Using lactose as an excipient, granules containing MMSC were granulated by a conventional wet granulation method, and then compression-molded by a conventional method to produce tablet A containing 25 mg of MMSC per tablet. . Similarly, Tablet B containing 25 mg of MMSC and 12 mg (in terms of drug substance) per tablet was produced.

[0025] Ten volunteer men in their 20s and 50s who complained of abdominal indefinite complaints were randomly selected and divided into two groups (group A and group B) of five. Questionnaire format of changes in symptoms of indefinite complaints before, during and after taking tablets A for group A and tablets B for group B for 3 consecutive days after each meal I was asked to answer. The results are shown in Table 2.

[Table 2]

As is apparent from Table 2, in Group B which took the gastrointestinal composition of the present invention, a marked improvement effect on the symptoms of abdominal indefinite complaints was confirmed.

Claims

The scope of the claims

[1] A gastrointestinal drug composition comprising methylmethionine sulfo-um chloride and sputum.

[2] The gastrointestinal medicinal composition according to claim 1, for suppressing belching, scalding, nausea or vomiting, or for relieving chest gripping, leaning, indigestion, stomach-abdominal bloating or loss of appetite.

[3] The gastrointestinal composition according to claim 2, wherein belching, scalding, nausea, vomiting, chest gripping, leaning, indigestion, stomach / abdominal bloating and loss of appetite are caused by overdrinking or overeating. object.

[4] The gastrointestinal composition according to claim 1, for promoting digestion.

[5] The gastrointestinal composition according to claim 1, which activates the motor function of the digestive tract.