JPH02189162A - Sublimation drug discharge system - Google Patents

Abstract

PURPOSE:To provide a system which discharges a sublimation drug suitable for absorption of a sublimation physiological activated material through a nosee emucous membrane by a method wherein a sublimation physical activated material and a chemical exothermic agent are combined together. CONSTITUTION:A sublimation physical activated material, e.g. peonol, and chemical exothermic agent consisting mainly of iron powder and utilizing oxidization reaction are placed in a breathable cloth bag or a Japanese paper bag. The bag is further contained in an airtight bag or an airtight bag filled with nitrogen, and the bag is broken where occasion demands, the middle bag is taken out, and is shaked and mixed so that contents are sufficiently mixed together. This shaking causes iron powder to easily change for ferrous oxide through iron hydroxide resulting from oxidization of oxygen in air and to be oxidized to ferric oxide, and during the oxidization, quantities of reaction heats are generated. By means of the heat, the peonol being a sublimation physical activated material is sublimated and is sucked through a naris to provide a tranquility effect.

Description

DETAILED DESCRIPTION OF THE INVENTION (a) Field of Industrial Application This invention relates to a sublimation drug release system suitable for absorbing physiologically active substances through the nasal mucosa.

(b) Prior Art Nasal drops have been known as drugs that are administered to the mucous membranes of the nasal cavity for anti-inflammatory, astringent, sterilizing, and treatment of nasal obstruction. This nasal solution is in liquid form and is used by applying it. Aerosol preparations are a special form of nasal administration, but these preparations are made by suspending the main drug, which is normally insoluble in liquefied gas, into a fine powder. Fine particles of the main drug are obtained as an aerosol. On the other hand, caffeine is a physiologically active substance that is solid at room temperature but has sublimation properties, and has been administered as an oral preparation or an injection.

(c) Problems to be solved by the invention By using the above-mentioned caffeine or other physiologically active substances, by utilizing their sublimation properties, the sublimated substances are absorbed mainly through the nasal mucosa through natural breathing. However, there was no known administration form that could be expected to alleviate sedative or stimulant effects.

(d) Means for Solving the Problems According to the present invention, a sublimable physiologically active substance, such as paeonol, which has a sedative effect, and caffeine, which has an stimulant effect, can be sublimated, and the system does not scatter and release them into the air. The present invention provides a method of using a sublimable physiologically active substance that is completely different from the known method of using it.

This invention relates to a sublimable drug release system comprising a combination of a sublimable physiologically active substance and a chemical exothermic agent.

The sublimable physiologically active substance of this invention is about 50°C to 220°C.
It is a substance that can sublime at ℃ and has physiological activity. A typical example is paeonol (a substance present in the root of Peonpi: molecular formula: CJIloOa).

Sublimation point: 50°C), caffeine (csn+oN4oy, sublimation point: 118°C), abscisic acid (C01itoOa, sublimation point: 120°C), camphor (C+.+t+SO, sublimation point: room temperature), borneol (C+.!1..0. Sublimation point: 208°C), cinchonine (C, gII□N!0. Sublimation point: 220°C), bergabten (C+zll+s04. Sublimation point: 188°C), benzoic acid (C?I!60!).

sublimation point 100℃), salidyl alcohol (CvllsO
t.

Noboru! 100°C), Zarydylic acid (C?I1.08. Sublimation point 76°C), Angelic acid (C-11,O*, Sublimation point 45°C), Cantharidin (C1, +1□04. Sublimation point 110°C) , chrysophonic acid (C1slltaOa, sublimation point 196°C), and aspidosvermine (C**t13°N, sublimation point 180°C).

The chemical exothermic agent of this invention is preferably one whose main component is an inorganic compound that generates heat through oxidation reaction or hydration reaction.Specifically, the chemical exothermic agent that utilizes oxidation reaction includes:
Examples include those whose main component is iron powder. The iron powder may be reduced iron powder, electrolytic iron powder, cast iron powder, or the like. These iron powders produce triiron tetroxide through air oxidation, and at this time generate heat of formation. Iron powder usually contains water-retaining agents (e.g. activated carbon, wood flour, perlite, zeolite, vermiculite, silica gel, water-retaining substances such as water-absorbing polymers) and reaction aids (e.g. potassium chloride, sodium chloride, calcium chloride, ferrous chloride, etc.) are combined. The addition m of water retention agent and reaction aid is usually for iron powder,
about 10-50 parts and about 5-15 parts, respectively. In order to sustain heat generation for a long time, volcanic rock that can generate infrared rays may be added to the iron powder, or the iron powder may be subjected to ion treatment in order to increase the temperature at the start of heat generation. On the other hand, an example of a chemical exothermic agent that uses a hydration reaction is quicklime.When used, quicklime causes a hydration reaction when mixed with liquid water and generates heat.The amount of water used is: For example, quicklime 1
00 parts, it is 15 to 40 parts. Instead of using liquid water, combine hydrated salts (e.g., sodium sulfate decahydrate, sodium phosphate decahydrate, sodium silicate decahydrate, etc.) and use the water in the hydrated salt. You can also do that.

Note that the chemical exothermic agent is not limited to those mentioned above, and any chemical exothermic agent may be used as long as it achieves the purpose of the present invention.

The above-mentioned chemical exothermic agents are selected and used in consideration of the sublimation temperature and location of the sublimable active substance.

In the case of iron powder, it has a low exothermic temperature and is preferably combined with a sublimation point of about 70° C. or lower like camphorberionol. In the case of quicklime, it is usually 60 to 90
Although it is possible to generate heat to a temperature of .degree. C., a high temperature heating type of about 250.degree. C. is also possible. Therefore, it can be combined with substances having a high sublimation point, such as caffeine, abscisic acid, cantharidin, cinchonine, and asvidospermine.

The physiologically active substances of this invention are solid at room temperature, but they can be used as is or in pharmaceutically less toxic organic solvents (
For example, it is dissolved in water, alcohol, acetone, ethyl acetate, hexanoate, etc.) and impregnated or mixed with a suitable carrier. In this case, the above-mentioned chemical exothermic agents such as iron powder, water retention agent, and quicklime are suitable as materials to be impregnated or mixed. The amount of impregnation or mixing is not particularly limited. However, it is necessary that the drug be released into the air and absorbed through the nasal mucosa to provide enough nails to be bioactive. For example, the amount of Paeonol that does not have physiological effects on the human body is 55K
200B-1500mg per g, and caffeine is 30mg to 100mg.

A chemical exothermic agent that utilizes an oxidation reaction is placed in a breathable inner bag, which is sealed with a non-breathable outer bag, and when used, the outer bag is torn.
Heat generation occurs due to ventilation. Thereby,
Physiologically active substances are sublimated. Further, chemical exothermic agents that utilize a hydration reaction include, for example, a form in which quicklime is stored in an outer bag and water or an inorganic hydrated salt is stored in an inner bag, and both can be mixed at the time of use. When water is used, it is preferable that the physiologically active substance is impregnated or mixed into a suitable carrier, and a breathable bag containing the physiologically active substance is placed adjacent to the above-mentioned outer bag. When using inorganic hydrated salt, the physiologically active substance is impregnated or mixed with quicklime,
An example of this is storing it in a breathable bag.

Note that the sublimation drug release system of the present invention may utilize a disposable body warmer or a container that can be used for instant heating of foods and beverages.

(E) Examples Example 1 1. 40 g of metal iron powder made from 5 g of Paeonol as fine powder
In addition to a mixture of 6 g of water, 69 g of activated carbon, 59 g of salt, and 5 g of leech powder, 1. Or put it in a Japanese paper bag,
This bag is further placed in an airtight bag or an airtight bag filled with nitrogen, and when necessary, the outer bag is torn open, the inner bag is taken out, and the contents are shaken well to mix thoroughly. As a result, the iron powder is oxidized by oxygen in the air, changes into iron hydroxide, easily changes to ferrous oxide, and is further oxidized to ferric oxide. During this process, a large amount of reaction heat is generated, and 20 After a minute the temperature is up to 75
℃ and kept at 58℃ or higher for more than 1 hour. By this heating, paeonol, a sublimable physiologically active substance, rises by 1°C.
It exerts a sedative effect when inhaled through the nasal cavity.

Example 2 5g of paeonol was dissolved in 15xQ ethanol and 5a
A paeonol-impregnated woven fabric is prepared by adsorbing it onto a non-combustible woven fabric of 500 mm and drying it.

Place this on top of a container filled with quicklime pieces 2002, and add 30yz (l) of water to the quicklime.
It generates heat up to 0°C, and the heat generation lasts about 30 minutes.

During this period, in about 7 minutes, paeonol completely sublimates and is inhaled through the nasal cavity, producing a sedative effect.

(f) Effects of the Invention Based on the above, the drug release system according to the present invention sublimates and scatters caffeine into the air when you need to wake up, such as when driving a car, and when you are drowsy. When you feel irritated by traffic jams, etc., you can sublimate and scatter Paeonol into the interior of the car to calm the mounds. It has a wide range of applications, and it is thought that the present invention will open up a new field of usefulness for Matirahui, which is completely different from the conventional use of aromatic properties of essential oils and the like at room temperature.

Claims (1)

[Claims] 1. A sublimable drug release system comprising a combination of a sublimable physiologically active substance and a chemical exothermic agent. 2. The system according to claim 1, wherein the chemical exothermic agent comprises iron powder, a water retention agent, and a reaction aid. 3. The system of claim 1, wherein the chemical exothermic agent comprises quicklime and an inorganic hydrated salt. 4. The system of claim 1, wherein the chemical exothermic agent comprises quicklime and water. 5. The system according to any one of claims 1 to 3, wherein the sublimable physiologically active substance is impregnated, adsorbed or mixed with a chemical exothermic agent (excluding water). 6. The system according to claim 1 or 2, comprising a breathable inner bag and a non-breathable outer bag, the inner bag containing a sublimable physiologically active substance and a chemical heating agent.