JPS5867621A - Analgesic and sedative - Google Patents

Abstract

PURPOSE:An analgesic and sedative comprising uracil as an active ingredient. CONSTITUTION:Uracil has low toxicity and shows analgesic and sleep prolonging action, so it is useful as an analgesic and sedative. It is also useful for remedying various kinds of diseases caused by stress as an antistress agent. When it is prepared as a drug, uracil may be in the form of a salt with an organic or inorganic acid, and is medicated orally or parenterally. Tablets, capsules, pills, powder, granules, etc. for oral medication are pharmaceutically prepared by using properly starch, talc, gelatin, etc., and injections, etc. for parenteral medication are pharmaceutically prepared in the presence of sodium acetate, sodium benzoate, ethylenediamine, etc. It can also be used as suppositories and ointments. A daily dose for adult is 100-5,000mg by oral medication and 10-1,500mg by parenteral medication.

Description

[Detailed description of the invention] The present invention provides an analgesic agent containing uracil as an active ingredient,
Concerning sedatives.

Bases such as uracil, adenine, guanine, cytosile, and thymine are important compounds as constituents of nucleic acids, and nucleotide derivatives of these compounds are used as high-energy storage and carriers in living organisms. ,
Alternatively, it plays an important role as a coenzyme. However, although the pharmacological effects of these substances have been known, such as the thyroid function inhibition effect of the related substance thiouracil and the antitumor effect of 5-fluorouracil, there are no studies regarding pharmaceuticals containing uracil itself as an active ingredient. There are no reports.

While researching the pharmacological effects of uracil, the present inventor discovered that it has remarkable medicinal effects, particularly analgesic, sedative, and sleep prolonging effects, and completed the present invention.

The details are shown below.

1. Acutely toxic uracil was administered intraperitoneally to 10 ICR mice per group, and the number of deaths within 72 hours was determined using the Coxon method (Lttchfield-Witcox method).
, on) to determine the 50% lethal dose (LD, .).

LD: >2.000 mg/kgG2, 5ART (Specif 1ca
alternation of rhythm
Temperature) Stressed animals were treated using the method of Kita et al.
). 5ART raised by the method
Stressed animals are an animal model that exhibits a type of stress state, such as suppressed weight gain, increased heart rate, and prolonged QR3 time, which is similar to autonomic nervous system imbalance in humans caused by sudden changes in temperature. Because it is sensitive to pain, it is suitable for screening for analgesic effects.

2.1 Analgesic effect Using a group of 10 ddY male mice loaded with 5ART stress, Randall Sellitto (Randa)
1-3s I it to) Pressure stimulation was applied to the ridge using a pressure stimulation analgesic effect measuring device. The analgesic coefficient is calculated by dividing the pressurized weight in which the mouse exhibits an escape response after repeated administration of the test by the pressurized weight before administration, and the dose at which the analgesic coefficient is 1.5 (E D 1.') is determined. I asked for it.・E-
D,−,(p,o,): 56 w/hit(i
, p, ) = 7.6 ■/- 2,2 Effect of hexoparvicur on sleep effect Using a group of 10 ddY male Theseus (20-22 g),
Uracil was administered intraperitoneally, and hexoparbital sodium ω■/- was administered intraperitoneally over a period of □□□ minutes. Thereafter, sleep time was measured using the righting reflex extinction time as an index. Mice whose am time was longer than twice the average am time of the control group were considered positive, and ED, ) was calculated.

ED50: 25 47 kg According to the results of the pharmacological tests mentioned above, uracil has low toxicity (has analgesic effect, sleep prolonging effect,
Therefore, it is useful as an analgesic and sedative, and furthermore, it can be used as an anti-stress agent to treat various diseases caused by stress.

When prescribed as a medicine, uracil is inorganic! It can be formulated into tablets, capsules, pills, powders, granules, etc., and can be formulated using conventional methods with appropriate excipients such as starch and lactose, as well as lubricants such as magnesium stearate and talc, gelatin,
A binder such as cellulose, a disintegrant such as carboxymethylcellulose, etc. are used as necessary to formulate a formulation. For parenteral use, it can be made into an aqueous or non-aqueous solution as an injection. In this case, it can be formulated in the presence of suitable solubilizing agents, such as sodium acetate, sodium benzoate, sodium salicylate, sodium citrate, ethylenediamine, triethanolamine, etc., and as is commonly practiced. Stabilizers, preservatives, tonicity agents, etc. may also be added. As other non-drinking preparations, it may be used as a dry product for injection to be dissolved before use, or as a layer or ointment by mixing with a suitable base.

The content of uracil in the preparation must be determined so as to provide an appropriate dose, but may be changed as appropriate depending on the subject of administration, route of administration, desired therapeutic effect, etc. Generally, for adults, uracil is administered orally for 100-s, ooo■,
It is administered parenterally at 10-1.500 ml.

The solution can also be used in combination with other analgesics, sedatives, etc.

Below, examples of formulations according to the present invention are shown, whereby:
This invention is not limited.

(1) Injection Uracil Father ■ Solubilizing agent Appropriate amount Dry product for injection 2td After dissolving, filter as appropriate, fill in ampoules, fuse and seal, then sterilize.

(2) Capsules Uracil 100 ■ Lactose 300■ Barley Sea Starch 50 ■ The above ingredients are mixed uniformly and filled into hard capsules.

Agent: Patent Attorney Murayama Sababe

Claims (1)

[Claims] (1) Analgesics and sedatives containing uracil as an active ingredient