JPH04112823A - Remedy for dementia - Google Patents

Abstract

PURPOSE:To obtain a remedy for dementia effective against dementia, especially Alzheimer-type dementia and Alzheimer disease by using a chalybeate known as a remedy for sideropenic anemia in combination with coenzyme Q10 and vitamin B6. CONSTITUTION:The objective remedy for dementia contains vitamin B6, a chalybeate and coenzyme Q10 as active components. The addition of the chalybeate is effective not only to develop the dementia-amelioration effect in a short period but also to decrease the amounts of coenzyme Q10 and vitamin B6. The remedy for dementia may be a mixture of three components consisting of coenzyme Q10, vitamin B6 and the chalybeate, a mixture of two components consisting of coenzyme Q10 and vitamin B6 or coenzyme Q10 and the chalybeate, or a simple preparation containing coenzyme Q2. In the case of two-component preparation or a simple preparation, it is necessary to separately administer the other components. The remedy exhibits remarkable effect and has no side action.

Description

[Detailed Description of the Invention] [Industrial Field of Application] The present invention provides a therapeutic agent for dementia, more specifically, coenzyme Q I
The present invention relates to a dementia therapeutic agent containing Q as an active ingredient or one of the active ingredients.

[Conventional technology]

It is well known that coenzyme Q10 used in the present invention is widely distributed in many human tissues and plays an important role as a coenzyme in the respiration process of cells and tissues. It is said to be involved in the transmission system (MORTENR, A,: Nat
ure, 182.1764 (1958), Ca1
eP, HlArch, Biochem, Biop
hys, 9.3.211 (1961)].

It is known that deficiency of coenzyme Q10 is observed in conditions such as myocardial insufficiency, myocardial ischemia, and cerebral ischemia, arteriosclerosis, hypertension, and muscle malnutrition (Folk
ner K: Int, J, Vit, Res,
, 40°380 (1970)].

On the other hand, clinically, administration of coenzyme Q IG has been shown to have an ameliorating effect on various pathological conditions, such as myocardial failure, hypertension, post-infectious symptoms, myobasis due to malnutrition, chronic periodontitis, and mental instability. It has been reported that (
Yamazawa, Y.: Biomedical
and C11nical Aspects of
Coenzyme Q, Elsevier Dutch Ed, Vol, II, 333 (198
0)].

In addition, coenzyme Q 1 is also used for cerebral anoxia.
It has been reported that the administration of 0 or in combination with phospholipids can bring about an improvement effect [JP-A-61-33118
issue〕. Coenthyme Q is used for such oxygen-deficient and energy-deficient conditions. It is predicted that Coenthyme 010 has a clinically improving effect based on its pharmacological action of regulating respiratory processes in cells and tissues.

However, in recent years, as the population ages, the number of dementia patients has increased significantly, and this has become a major social problem. Dementia is a syndrome in which a normally developed brain exhibits various mental and emotional symptoms, mainly progressive intellectual and behavioral disorders, due to acquired organic brain damage.

Among these, clinically important dementias occurring after old age are Alzheimer's type dementia and cerebrovascular dementia caused by brain parenchymal damage caused by changes in blood vessels in the brain. Alzheimer's dementia causes atrophy of the entire brain, even though there is no noticeable damage to the cerebral blood vessels, and dementia progresses along with changes such as neurological loss and degeneration (for example, the appearance of amyloid and senile plaques). It is something to do.

Research on the symptoms and etiology of dementia, as well as neuropathological research, has become active in recent years, and various drug treatments for dementia have been tested. Drugs that have been used to treat dementia are mainly cerebral circulation improving agents and cerebral metabolism activators. However, these drugs do not show the expected effect on intellectual decline, and the reality is that they are unable to prevent the progression of dementia.

Furthermore, in Alzheimer's dementia, various neurotransmitters are reduced, and therefore, treatment with various neurotransmitter-related compounds has been performed, and improvement in intellectual function is extremely insufficient.

The present inventor has become interested in drug therapy for dementia, and as a result of conducting intensive research, has already discovered that a remarkable therapeutic effect on dementia can be obtained by using coenzyme Q10 in combination with vitamin B6 (patent application) Hei 1-3
2318).

[Invention or problem to be solved]

However, in this treatment method, since it is necessary to use a larger amount than usual on both sides, there remained concerns about side effects in actual treatment.

Therefore, it has been desired to develop a safe dementia therapeutic agent that has high therapeutic effects in treatment using coenzyme Q10 and vitamin B6 and is less likely to cause side effects in terms of quantity.

The purpose of the present invention is precisely in this respect, and is to provide a therapeutic agent for dementia that has excellent therapeutic effects with little risk of side effects.

[Means to solve the problem]

The present inventor has conducted intensive research in order to solve the above problem, and found that by using an iron preparation used as a therapeutic agent for iron deficiency anemia in combination with the above-mentioned coenzyme Q10 and vitamin B, a surprising result was found. The present inventors have found that the present invention has excellent therapeutic effects on dementia, particularly Alzheimer's type dementia and Alzheimer's disease, and is extremely useful as a therapeutic agent for dementia, leading to the completion of the present invention.

That is, the gist of the present invention is as follows: (1) A dementia treatment agent containing vitamin B6, an iron preparation, and coenzyme Q as active ingredients; (2) A therapeutic agent for dementia containing vitamin B, an iron preparation, and coenzyme Q to as active ingredients, intended for patients receiving vitamin B. (3) A dementia therapeutic agent containing vitamin B6 and coenzyme Q 10 as active ingredients, intended for patients receiving iron preparations, and (4) Coenzyme Q z+, intended for patients receiving vitamin B6 and iron preparations. The present invention relates to a dementia treatment agent having an active ingredient.

The dementia therapeutic agent of the present invention may be coenzyme Q 10 alone or in combination with vitamin B6 and/or iron, and it is substantially necessary to administer these three drugs. In the present invention, the effect of adding the iron supplement used is not only that the improvement effect appears in a shorter period of time, but also has the effect of reducing the amount of coenzyme 010 and vitamin B6 used.

That is, when administering only coenzyme Q to and vitamin B6, it usually takes 1 to 2 months for the improvement effect to appear, but by adding an iron supplement in the present invention, a remarkable improvement effect is usually observed in about 1 week. The effect can be seen in an extremely short period of time.

In addition, the amount of coenzyme Q10 and vitamin B6 used is approximately 1/3 of that when only these two drugs are administered.
An improvement effect is observed at about 1/2, about 273.

The dementia to be treated in the clinical trial using the dementia therapeutic agent of the present invention is Alzheimer's type dementia or Alzheimer's disease. For this reason, it is effective not only for Alzheimer's type dementia but also for dementia in general, including cerebrovascular dementia.

The excellent clinical effects of the present invention were determined based on Hase's Simple Intelligence Test and the diagnostic criteria for dementia in DSM-III-R. As shown in Tables 1 to 4 of the clinical test examples described below, remarkable improvement effects were observed as early as one week after treatment.

Coenzyme Q 10 used in the present invention is a known compound that is already commonly used as a pharmaceutical (Japanese Patent Publication No. 39-14220.39-17513.39-175).
Publication No. 14), known as a ubidecarenone preparation (Dictionary of Health Drugs, April 1990 edition, published by Yakugyo Jihosha, No. 68)
page).

Vitamin B6 is already commonly used as a medicine, and is known as a pyridoxal phosphate preparation (Dictionary of Health Drugs, April 1990 edition, published by Yakugyo Jihosha, p. 175)
.

Iron supplements are also already commonly used as medicines,
For example, there is a sodium ferrous citrate preparation (Ferromia) used for iron deficiency anemia (Dictionary of Health Drugs, April 1990 edition, published by Yakugyo Jihosha, p. 187).

In addition, the dementia therapeutic agent of the present invention is a three-drug combination of coenzyme Q10, vitamin B6 and an iron supplement as described above, or a two-drug combination of coenzyme Q10 and vitamin B6, or coenzyme Q to and an iron supplement. Alternatively, it may be a preparation of coenzyme Q10 alone. However, in the case of a two-drug combination, it will be effective as a dementia treatment if the remaining ingredients, i.e. iron supplements or vitamin B6, are taken separately, and in the case of coenzyme Q10 alone, it will be effective. It is necessary to take vitamin B6 and iron supplements separately.

Thus, the dementia therapeutic agent of the present invention contains coenzyme Q t
This is a combination or combination of O, vitamin B6, and an iron preparation, but in either case, it can be administered orally at a dosage that is adapted to individual needs. Thus, the therapeutic dosage can be administered orally in conventional dosage forms such as tablets, capsules, granules, syrups, suspensions, and the like.

The appropriate dosage forms also include acceptable conventional carriers,
They can also be manufactured by incorporating the active compound with excipients, binders, stabilizers, and the like.

The dosage and frequency of administration vary depending on the severity of the dementia condition requiring treatment.
0 to 180 mg, preferably 60 to 120 mg. Also, vitamin B6 used in combination or as a combination is 120 to 210 mg, preferably 18 (1-2
10mg, iron supplement is 50~250cm, preferably 100cm
˜250 μ is a suitable daily dose.

Incidentally, the coenzyme Q10, vitamin B6, and iron preparation used in the present invention are all already commercially available as pharmaceuticals, as described above, and can be used with confidence without worrying about toxicity.

〔Example〕

Hereinafter, the present invention will be specifically explained with reference to Examples and clinical test examples, but the present invention is not limited by these Examples and the like.

Example: A capsule containing the following ingredients was prepared and used as a therapeutic agent for dementia.

Coenthyme Q, 20 ■ Hitamine 86 60 ■ Iron preparation 50 ■ Example 2 Capsules containing the following ingredients were prepared and used as a therapeutic agent for dementia.

Coenzyme Q, 40 ■ Vitamin 86 60 mg Iron preparation 50 ■ Clinical test example Coenzyme 10, vitamin B6, and iron preparation were administered to 18 cases of Alzheimer's type dementia and 9 cases of Alzheimer's disease at the daily doses listed in Table 1. The effect on dementia, which will be described later, was evaluated before administration and at 1 week, 2 weeks, 4 weeks, 6 weeks, and 8 weeks after the start of administration.

When evaluating the effectiveness of drugs for dementia, it is important to evaluate the nature of the dementia, and it is necessary to quantify dementia as objectively as possible. When making a diagnosis, we perform a diagnosis of exclusion.
Alzheimer's dementia or Alzheimer's disease was determined, and the Hasegawa simple intelligence test, which is considered the most common among various testing methods, was selected, and the test was conducted as described in Kazuo Hasegawa et al., Psychiatry, 16965-969 (1974). The therapeutic effect of the dementia therapeutic agent of the present invention was determined according to the method described in the following. The dementia scale determined by the Hasegawa Simple Intelligence Test is usually 0 to 21.5 in the case of dementia, and if there is a treatment effect, these evaluation scores will increase, and in normal people, it is usually 3.
It indicates a value of 1.0 or more.

For daily life, The American Ps.
Determination was made using the DSM-I [IR, the diagnostic criteria for dementia created by the ychiatric association (translated by Mibe Takahashi et al. pp. 72-73, Igaku Shoin, 1988).

According to the DSM-I-R standards, normality is defined as 0, and the grades of dementia are classified into ■ to ■.The details are as follows.

0: (Normal) No impairment in occupational or social activities;
They also have the ability to live independently.

■ (Mild) Occupational or social activities are clearly impaired, but the person still has the ability to live independently, maintain personal hygiene, and make relatively normal decisions.

■ (Moderate) Living independently is difficult and requires some level of supervision.

■ = (Severe) Impaired activities of daily living and requires constant supervision. For example, they are unable to maintain personal hygiene, and their speech is either limited or not spoken at all.

The clinical test results for Alzheimer type dementia or Alzheimer's disease in the present invention are summarized in Tables 1 to 4.

[Margin below]

As shown in Tables 1 to 4, the therapeutic effect of the present invention is remarkable, with a significant increase in Hase's score in most cases; A marked improvement was observed after one week. Further, regarding DSM-III-R, an improvement was also observed with a significant difference. No noteworthy side effects were observed during the treatment.

Claims (5)

[Claims] (1) Vitamin B_6, iron supplements and coenzyme Q_1_
A dementia treatment agent containing 0 as an active ingredient. (2) A dementia treatment agent containing iron supplements and coenzyme Q_1_0 as active ingredients, intended for patients receiving vitamin B_6. (3) A dementia treatment agent containing vitamin B_6 and coenzyme Q_1_0 as active ingredients, intended for patients receiving iron supplements. (4) A dementia treatment agent containing coenzyme Q_1_0 as an active ingredient, intended for patients receiving vitamin B_6 and iron preparations. (5) The dementia therapeutic agent according to claim (1), (2), (3) or (4), wherein the dementia is Alzheimer's type dementia or Alzheimer's disease.