JPS5938204B2 - Aplastic anemia treatment agent - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a therapeutic agent for aplastic anemia containing coenzyme Q represented by the following general formula (%) 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 Q1o is currently used as a therapeutic agent for congestive heart failure.

The present invention has discovered that this coenzyme Q is effective as a therapeutic agent for aplastic anemia.

Traditionally, treatment for aplastic anemia has included adrenocortical hormones,
Although administration of anabolic hormones, ACTH, folic acid, etc., and blood transfusions have been carried out, an appropriate treatment method has not yet been established.

When the coenzyme Q of the present invention was administered to aplastic anemia patients whose symptoms had not improved even after the above-mentioned treatments, the therapeutic effect, particularly an increase in the number of red blood cells, was obvious.

In the present invention, the daily dose of coenzyme Q for adults is approximately 1
0rI11 to 2001rL9.

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.

The toxicity of coenzyme Q is extremely low as shown below.

Acute toxicity (■/2) Coenzyme Q10 administration 0 Chronic toxicity Coenzyme Q, 0 was administered to male and female Rice Coues rats at 6.60°6.
00■/2/days for 26 consecutive weeks, general condition, facial fluid, urine test, morphological observation (macroscopic,
Histologically, no difference was observed from the control group.

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

Example 1 Aplastic anemia patient trial 1 The following cases 1 to 3 of the aplastic anemia patients received a combination of oral administration of coenzyme Q1o30q and intramuscular injection of 10 ml per day.

In the fourth case, coenzyme Q1o30rIl was administered orally for one day.

Case 1: The patient, a 25-year-old man, has been hospitalized for about a year, receiving blood transfusions, adrenocortical hormones, ACTH, folic acid, anabolic hormones, and vitamin B1□
This patient did not see any improvement in his anemia despite using the drug.

When coenzyme QIO was administered to this patient while continuing conventional treatment, the anemia improved, and the red blood cell count remained at 3 million even after reducing and even discontinuing the blood transfusion.

However, no increase in white blood cells or platelets was observed.

Case 2: 62-year-old man This case is a patient who, like the previous case, has been undergoing the same treatment process for about a year.

When coenzyme QIO was administered at the same time as conventional treatment was continued, the number of red blood cells increased slightly, and even when the amount of blood transfusion was halved, the number of red blood cells did not decrease.

No increase in white blood cells was observed, but the number of platelets increased.

Case 3: 60-year-old man This patient also had no improvement for about 2 years despite a combination of blood transfusions, adrenocortical hormones, anabolic hormones, and other treatments.

When coenzyme QIO was administered at the same time as conventional treatment was continued, the number of red blood cells increased significantly at the beginning of administration.

No increase in white blood cells or platelets was observed. Fourth example 64
In this case, the patient's symptoms recovered to some extent after admission to the hospital, but after the blood transfusion was discontinued, the symptoms worsened despite the administration of vitamin B1□ drugs.

Therefore, blood transfusion was performed again, and when the number of red blood cells reached 3,020,000, the blood transfusion was stopped, and coenzyme QIO was subsequently administered.

After administration, the number of red blood cells decreased temporarily, but increased again and is now maintained at 3 million.

White blood cells also decreased temporarily, but have increased again.

The progress of the above four cases is shown in the table below.

Example 2 Capsule Coenzyme Q1o5g Microcrystalline cellulose 80g Corn starch 21 Lactose
22g Polyvinylpyrrolidone 3g Total amount 130g The above ingredients were granulated by a conventional method and then filled into hard gelatin capsules.

Example 3 Powder coenzyme Q1o 50g 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 4 Tablet Coenzyme Q1o5g Corn starch 10g Refined white sugar 20g Carboxymethyl cellulose calcium 10g Microcrystalline cellulose
409 Polyvinylpyrrolidone
5g talc
10g total amount
Dissolve 100g coenzyme Qio in acetone,
Next, this was adsorbed onto microcrystalline cellulose and then dried.

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 mixing this with talc as a lubricant, one tablet weighs 100172. It was compressed into tablets.

Example 5 Injection coenzyme Q1o10g Nikkol HCO-6037,! i' sesame oil
2g sodium chloride
9g propylene glycol
40g phosphate buffer (0.1M,
pH6,0) 100mA! Distilled water
Total amount 1,000ml Coenzyme Q10. N1
Mix kkol HCO-60, sesame oil and half the amount of propylene glycol, heat and dissolve at about 80°C, add distilled water in which phosphate buffer, sodium chloride and the remaining half of the propylene glycol have been dissolved in advance at about 80°C. The mixture was heated and added to make an aqueous solution with a total volume of 1,000 ml.

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

Claims (1)

[Scope of Claims] 1. A therapeutic agent for aplastic anemia containing coenzyme Q represented by the general formula (wherein n is an integer of 7 to 10) as a main component. 2 Claim 1 in which coenzyme Q is coenzyme QIO
A therapeutic agent for aplastic anemia as described in .