JPH03246221A - Rearing promoter - Google Patents

Abstract

PURPOSE:To obtain an animal and human rearing promoter containing l- carnitine, acyl-l-carnitine or salt thereof as an active ingredient, extremely weak in toxicity and free from side effects by administration. CONSTITUTION:The aimed rearing promoter containing at least one kind of compound selected from l-carnitine, acyl-l-carnitine and physiologically acceptable salt thereof as an active ingredient and capable of exhibiting excellent effects in prevention and treatment of disorder of patient poor in weight increase or animal such as cattle deficient in growth or necessary for promotion of growth. The doze of the active ingredient compound is 5-100mg/time adult, preferably 10-50mg/time adult in the number of times of about three times per day in the case of oral administration.

Description

[Detailed description of the invention]

[0001]

[Industrial application field]

The present invention relates to growth promoters for animals and humans. [0002]

[Conventional technology]

In recent years, a variety of experiments have been conducted regarding the physiological effects of di-carnitine, the main ones of which are improving digestive motility, enhancing secretion of digestive juices, and promoting bone growth. . However, dl-carnitine cannot be expected to have the above-mentioned effects or is ineffective in animals, and currently does not have sufficiently satisfactory effects in humans. [0003]

[Problem to be solved by the invention]

The present invention can be used not only for patients suffering from poor weight gain, but also for healthy people.
Furthermore, the aim was to provide a drug that has excellent ameliorating effects and growth promotion for animals. [0004]

[Means to solve the problem]

The above purpose is achieved by using at least one type of active ingredient selected from 1-carnitine (i.e., el-carnitine), acyl-1-carnitine (i.e., acyl-el-carnitine), and physiologically acceptable salts thereof. Achieved by growth promoters. [0005] Carnitine, which is an active ingredient in the present invention, was first introduced in 1905 by Gulewisch.
) This is a compound discovered from meat extracts by Krimberg and Kutscher. In 1947, Fraenkel and R1ewet
T) discovered that an unknown substance contained in yeast or liver extract is essential for the growth of brown rice beetle, and named it vitamin Br. After that, 195
In 2 years, Carter et al.
Active crystals were isolated and confirmed to be the same substance as carnitine. Carnitine is distributed in a wide range of organisms, from humans to microorganisms, and is known to be particularly present in large amounts in muscle and pancreatic juice. Regarding its physiological and biochemical significance, Frit
A series of studies have been reported by Frits et al.
1. B, et al., J., Lipid Res.
, 4 279 1963). Carnitine + C(CH) N CH2CH(OH)CH3COO-
] present in living cells promotes the uptake of Acyl-CoA, an active fatty acid, into the mitochondria during β-oxidation of fatty acids in mitochondria. That is, carnitine is Acyl-CoA
is converted to Acyl-CoA carnitine through the action of Acyl-CoA carnitine transferase, and the barrier (B
It is said that the enzymes rapidly pass through the endothelial tract (Arrier) and participate in β-oxidation in the endometrial system, thereby aiding in the production of energy. Therefore, carnitine can be expected to have various pharmacological effects by utilizing its physiological effects, but there have been no reports of actual prevention or treatment of poor weight gain, etc. using the active ingredient of the present invention. [0006] The present invention provides a drug containing 1-carnitine, acyl-1-carnitine, and a physiologically acceptable salt thereof as an active ingredient. It was discovered and completed that the above-mentioned symptoms can be effectively prevented and treated by administering it to animals such as livestock that require growth promotion. [0007] The carnitine used as an active ingredient in the present invention can be in the form of a physiologically acceptable salt. [0008] Next, 1-carnitine, acyl-1- used in the present invention
The toxicity of carnitine is explained using a table. Acute toxicity (LD5o) [0009]

[Table 1] (1) monocarnitine betaine (mg/kg) [0010]

[Table 2] (2) Monocarnitine hydrochloride (mg/kg)

[Table 3] (3) Acyl-1-carnitine hydrochloride (mg/kg) The pharmacological effects will be detailed in the Examples below. By administering an appropriate amount of the above carnitine,
We were able to demonstrate that weight gain became noticeable and daily life became more comfortable. The reason for such a remarkable effect is currently not clear, but it is thought to be related to the fact that the administered carnitine or its salt has the effect of promoting an increase in free hydrochloric acid and an increase in gastric juice acidity [0012] In any case, the above-mentioned carnitine or its salts are highly effective in preventing and treating these symptoms in patients with poor weight gain, or in livestock and other animals that lack growth or require growth promotion, and are also an indicator of safety. It has extremely low toxicity and no side effects upon administration, making it extremely effective as a growth promoter. [0013] The growth promoter of the present invention is usually formulated into a pharmaceutical composition depending on the administration method using a pharmaceutical carrier together with the active ingredient compound. Examples of carriers include fillers, extenders, binders, wetting agents, and
Diluents or excipients such as disintegrants, surfactants, and lubricants can be used. There are no particular restrictions on the administration method,
Although various methods such as oral administration, intravenous administration, subcutaneous administration, and intraperitoneal administration can be employed, oral administration is most preferred. Examples of dosage forms suitable for oral administration include tablets, gunpowders, powders, liquids, granules, capsules, and drinks. Further, as a formulation suitable for intravenous administration, it is preferable to use an injection such as an aqueous solution or suspension. [0014] The amount of the active ingredient in the pharmaceutical composition formulated into a dosage unit form is not particularly limited and may be appropriately selected within a wide range, but it is usually 1 to 70% by weight of the total composition. In addition, the dosage of each preparation depends on various conditions such as the patient's age, sex, weight, severity of disease, etc., and the method of administration. 5mg~1
A pharmaceutical composition containing 00 mg, preferably in the range of 10 mg to 50 mg, may be administered, and the frequency of administration may be increased or decreased depending on the severity of the patient, with the standard of administration being 3 times a day. [0015]

【Example】

Next, examples for formulating the drug of the present invention will be shown.The composition is not necessarily limited to the following composition.

[Example 1] Crystalline cellulose 266mg Carboxymethylcellulose 266mg Light silicic anhydride 50mg Macrogol 600
Granules, fine granules, and powders are produced by adding 20 to 500 mg of at least one selected from 1-carnitine, acyl-I-carnitine, or salts thereof to 50 mg of the additive.

[Example 2] Crystalline cellulose 100mg Magnesium stearate 4mg Tart
Capsules are prepared by adding 50 to 500 mg of at least one selected from 1-carnitine, acyl-1-carnitine, or salts thereof to 8 mg of additives.

[Example 3] Crystalline cellulose 44mg carboxymethyl cellulose 44mg milk
Sugar 89mg Magnesium stearate 3mg Tarri 5mg
Tablets (uncoated tablets, film-coated tablets, sugar-coated tablets) are prepared by containing 20 to 500 mg of at least one selected from 1-carnitine, acyl-1-carnitine, or salts thereof.

[Example 4] Citric acid 2 mg/
m 1 glucose 100
Additives consisting of mg/ml of l-lunithine, acyl-
An oral liquid preparation containing 100 to 500 mg/ml of at least one selected from 1-carnitine or a salt thereof and adding a sufficient amount of sterile purified water is prepared in a 10 to 100 ml ampoule, glass bottle, or synthetic resin container. .

[Example 5] 1-carnitine, acyl-
Contains 5 to 250 mg/ml of at least one selected from 1-carnitine or salts thereof.
Manufacture injections in 0ml ampoules, vials, or plastic containers for infusion. [0016] Next, specific effects of the present invention will be explained in detail using experimental examples. 1 Animal experiment example Wistar rats were used as animals. Male rat rat pups weighing around 45 g were test-reared for one week, and those with similar weight increases were divided into two groups, each group containing five rats. The target group was given the following various feeds, and ■-carnitine, acyl-1-
The carnitine group further contains these at 10-45 mg/
kg was administered daily. The breeding period was 26 to 43 days, and during this period, body weight was measured every other day. On the day after breeding, the animals were autopsied under ether anesthesia to determine serum protein level (Hitachi protein needle), A/G ratio (Yoshikawa and Saito method), liver weight, liver water content, liver fat content (S0hlt fat extractor), liver Glycogen content (Somgy 1 method) Liver air mass (KJ eldahl-Ner method) Liver nucleic acid image (Br Feed: Basic solid food Oriental solid food Basic synthetic room casein 15%, soybean oil 5%, potato Shiyo starch 74%, Matsuriki lamb salt 5%, Panvitan 1% [0017]

[Table 4]

[Table 5]

[Table 6] As is clear from the clothes 4, Tables 5 and 6 above, the clothes of the present invention showed a significant weight gain compared to the control group, and a very significant difference in growth was confirmed. 2 Clinical experiment subjects were subjects (7 males,
(16 females) Their ages ranged from 2 months to 10 years old, 11 were infants, young children, and 12 were school children. The drug is 10-25 m
The daily dose was 2 to 3 g/kg per month. [0020] Judgment was made based on the effect on appetite, observation by the mother or nurse, or amount of leftover food. Regarding body weight, those whose weight increase (daily dose) for one month after administration was 10 g more than before administration were considered effective (+), and those whose weight increase was 50 g or more were considered excellent response (++). The results are shown in Table 7. [0021]

[Table 7]

Claims (1)

[Claims] 1. A growth promoter comprising at least one selected from 1-carnitine, acyl-1-carnitine, and physiologically acceptable salts thereof as an active ingredient.