JPS5938203B2 - A therapeutic agent for cerebral circulation disorders whose main ingredient is coenzyme Q. - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a therapeutic agent for cerebral circulation disorder containing coenzyme Q represented by the following general formula (wherein n represents an integer of 7 to 10) as a main component.

Coenzyme Q was discovered by Crane in 1957 from the mitochondrial lipids of cow heart.

In nature, coenzyme Q exists with various numbers of n in the above general formula.

Although its action in vivo is not fully known, it is thought to be involved in the electron transport system.

As for the medical use of coenzyme Q, coenzyme Qto is currently used as a therapeutic agent for congestive heart failure.

The present inventor has discovered that this coenzyme Q is responsible for various symptoms caused by cerebral circulation disorders (
It was found that it has a therapeutic effect on patients with various complaints (complaints).

Therefore, coenzyme Q is effective in improving symptoms (complaints) such as headache, dizziness, olfactory abnormality, numbness of limbs, and disturbance of consciousness, which are observed in stroke, cerebral arteriosclerosis, and sequelae of head trauma.

Coenzyme Q is a highly safe substance, and the acute and chronic toxicity of coenzyme QIO is as follows.

Acute and chronic toxicity 0 Acute toxicity (~/to) 0 Chronic toxicity To male and female Wistar rats, 6,60.60Or”9
/ Kp was administered for 7 days consecutively for 26 weeks, and general conditions, blood and urine tests, and morphological observations (macroscopic,
Histologically, no difference was observed from the control group.

The daily dose of coenzyme Q for adults is approximately 101,119-5
00~.

The dosage form may be oral or injection, and the dosage form may be any powder, granule, tablet, capsule, injection, etc.

These can be produced by conventional methods using conventional excipients.

Next, the present invention will be explained in more detail with reference to Examples.

Example 1 A woman (68 years old) lost consciousness for 2 months due to a skull base fracture caused by a traffic accident and was in a vegetative state.

The patient had paralysis of his left upper and lower limbs, showed no interest in eating, and had difficulty taking medication.

In contrast, administration of a central stimulant citicoline preparation,
Although there was an improvement in the clinical symptoms and electroencephalogram findings, both the symptoms and electroencephalogram findings returned to their original state after 3 months.

When the drug was injected into the mouth every two weeks at a dose of coenzyme Q1o20q x 2/day (injection), clinical symptoms and electroencephalogram findings showed significant improvement, and the improved condition was maintained even after more than 3 months had passed. .

Symptoms include interest in the outside world and ability to respond easily.

Example 2 Female (54 years old), upper and lower limb motor paralysis due to cerebral thrombosis After a sudden loss of consciousness, motor paralysis of the upper and lower limbs occurred as a sequela.

After 3 months, I visited the hospital and immediately started coenzyme Q1o 20 ”'i.
f1 day (injection) for 20 consecutive days, and then 2 doses per week.
Similar administration has been carried out ~3 times.

Three months after coming to the hospital, a significant improvement in brain waves, which is one of the indicators of treatment effectiveness, was observed, and a reduction in paralysis was also observed.

Next, treatment examples will be described as examples.

Next, examples of formulations will be described.

Example 14 Capsule Coenzyme Q1o5g Microcrystalline cellulose 80g Corn starch 209 Lactose
229 Polyvinylpyrrolidone 3g Total amount 130g The above ingredients were granulated by a conventional method and then filled into hard gelatin capsules.

Example 15 Powder Coenzyme QIO 5゜g Microcrystalline cellulose 400g Corn starch 550g Total
Amount: 1,000 g of coenzyme Q1o was dissolved in acetone, and then adsorbed onto microcrystalline cellulose, followed by drying.

This was mixed with corn starch and made into a powder using a conventional method.

Example 16 Tablet coenzyme Q1o5g Corn starch 1 (Hi'
Refined white sugar 20g Carboxymethylcellulose calcium 10g Microcrystalline cellulose 40g Polyvinylpyrrolidone 5g Talc
10g total amount
After dissolving 100g coenzyme Q1o in acetone and adsorbing it onto microcrystalline cellulose,
Dry.

Corn starch, refined sucrose, and carboxymethyl cellulose calcium were mixed therein, and then an aqueous solution of polyvinylpyrrolidone was added as a binder and granulated by a conventional method.

After adding talc as a lubricant and mixing, 1 tablet
It was compressed into 00rIIL1 tablets.

Example 17 Injection coenzyme Q1o10g Nikkol HCO-6037g Sesame oil 2g Sodium chloride 9g Propylene glycol 40g Phosphate buffer (
0.1M, pH 6.0) 100r/ll distilled water Total amount 1,000rll Coenzyme Q10. Mix N1kkol HCO-60, sesame oil, and half the amount of propylene glycol, heat and dissolve at about 80°C, add phosphate buffer, sodium chloride, propylene glycol, and distilled water in advance to about 80°C.
Warm to 0°C and add total amount i, oo.

ml aqueous solution.

After dispensing this aqueous solution into 1 ml ampoules and sealing them,
Heat sterilized.

Claims (1)

[Claims] 1. A therapeutic agent for cerebral circulation disorder containing coenzyme Q as a main component. 2 Claim 1 in which coenzyme Q is coenzyme QIO
A therapeutic agent for cerebral circulation disorders as described in Section 1.