JPS6136201A - Slow-releasing preparation for active substance - Google Patents

Abstract

PURPOSE:To obtain the titled slow-releasing preparation capable of keeping the releasing rate of the active substance in windy environment to the level samd as that of the windless state, and keeping the effect of the active substance for a long period, by protecting the releasing surface of the preparation containing the active substance in a manner to be inert to the influence of wind. CONSTITUTION:The releasing surface of the sheet or tape preparation 1 for the release of an active substance and containing an active substance such as Z-7- eicosen-11-one which is an insect pheromone, is formed to a structure 2 protecting the surface from the influence of wind. For example, the releasing surface 1a and the active substance-containing film 1b of the sheet preparation are attached to a proper supporting substrate 3, and the substrate is formed in the form of a cylinder, cone, or square pillar facing the releasing surface inward and the supporting substrate outward. The controlled release of the active substance can be maintained stably by the structure 2 protecting the releasing surface from the influence of wind. EFFECT:A stable slow-releasing property can be exhibited especially in an open field independent of the wind.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application This invention relates to a sustained release preparation for an active substance, particularly in the form of a sheet that has stable sustained release properties without being affected by wind when used outdoors. It also relates to tape-like preparations.

Conventional technology As a method of controlling insects without causing environmental pollution, in recent years, preparations containing insect sex pheromones have been sprayed outdoors, and by dispersing the pheromone into the atmosphere, insects are attracted to traps and killed. The so-called trout trapping method that does this, as well as the so-called disturbance method that disrupts the male's ability to sense the female and engage in mating behavior, is attracting attention.

Conventionally, various structures have been known for use for the above purpose, but in all of them, the pheromone emitting surface is exposed and is directly affected by the wind.

Problems to be Solved by the Invention As mentioned above, when the pheromone-releasing surface of the preparation is exposed to the outside, the release rate of the active substance becomes faster due to the influence of the wind.
The problem is that it can only be effective for a short period of time.

This invention was made in order to solve the above-mentioned problems, and an object of the present invention is to provide a sustained release preparation for an active substance whose release rate is not affected by wind and whose effective period can be extended. With the goal.

A means to solve a problem.

In order to solve the above-mentioned problems, the present invention protects the active substance release surface of a preparation containing an active substance with a structure that is not easily affected by wind, and improves the release speed of the active substance in a non-pressure state. It was done in the same way.

The active substance release surface of the sheet or tape-like preparation containing the active substance is protected from the wind, and since the wind does not directly impinge on said release surface, the active substance is released at the same rate as in windless conditions.

Embodiments Hereinafter, embodiments of the present invention will be described based on the accompanying drawings.

The present invention comprises a sheet-like or tape-like preparation 1 containing an active substance such as a pheromone, and a structure 2 that protects the active substance-releasing surface of this preparation from being affected by wind.

The above-mentioned sheet-like or tape-like preparation (hereinafter simply referred to as sheet-like preparation) is not particularly limited in its structure; for example, a porous polymer base material having continuous pores is impregnated with a liquid active substance. It is also possible to use formulations that are adsorbed to form a storage layer, wrapped in a polymeric membrane capable of controlling the release of the active substance, and heat-sealed around the periphery; A sheet-like preparation is used, which is a membrane body in which a liquid active substance having limited solubility in the polymer at room temperature is encapsulated as droplets in the micropores of the combined membrane.

A sheet-like formulation as described above may, for example, preferably contain a polymer and an active substance which is liquid at room temperature and which has limited solubility for the polymer at room temperature, in which both the active substance and the polymer are dissolved. The active substance is dissolved in an organic solvent that is more easily volatile than the active substance, and this solution is applied to the surface of a suitable support, and the solvent is evaporated to form the liquid active substance within the layer of the polymer. It is manufactured by dispersing and containing it in the form of minute droplets.

In the above, the liquid active substance is dispersed as a liquid in the polymer layer during preparation of the formulation, and is added to the polymer so that it is released from the polymer layer at a substantially constant rate after formulation. It is blended in an amount that exceeds the solubility.

The above-mentioned liquid substance refers to a substance that is liquid at room temperature and has chemical or physiological activities such as attractant activity, pesticide activity, repellent activity, and scent release activity, and is particularly used as a pest communication disruption agent as described above. When used, pheromones having attractant activity may be mentioned, such as the following:

Z-8-dodecenyl acetate E-9-dodecenyl acetate Z-9-dodecenyl acetate 11-dodecenyl acetate 10-methyldodecenyl acetate E-9-tetradecenyl acetate Z- 9-tetradecenyl acetate E-11-tetradecenyl acetate Z-11-tetradecenyl acetate Z-7-e]cen-11-one Specific examples of active substances include, for example: P! Pharmaceutical active substances include insecticides such as Naled, Diazinon, Sumithion, etc., insecticides such as β-propiolactone, triethylene glycol monohexyl ether, N5N-diethyl-m-
Repellents such as toluamide, limonene, benzyl alcohol, esters derived from hydrocarbons having 6 to 16 carbon atoms,
Examples include aroma active substances such as ethers and aldehydes.

The polymer for forming the above-mentioned porous polymer layer needs to have a limited solubility in the liquid active substance used as described above, and is usually in the range of 5 parts by weight or less of the liquid active substance. Polymers that only dissolve, especially 0.01 to 2
A polymer that can be dissolved in a range of parts by weight is preferably used. Such polymers are appropriately selected depending on the liquid active substance used, and specific examples include polysulfone,
Polycarbonate, polystyrene, poly(meth)acrylic esters including polymethyl methacrylate, polyamides, polyvinylidene chloride, polyvinylidene fluoride, cellulose esters, regenerated cellulose, polyurethane, polyvinyl alcohol, polyvinyl chloride, polyvinyl acetate, ethylene-vinyl acetate Examples include one or a mixture of two or more of copolymers, vinyl chloride-vinyl acetate copolymers, polystyrene-polybutadiene block copolymers, and the like.

In addition, the organic solvent used in manufacturing the preparation used in this defense must be able to dissolve both the active substance and the polymer, be more volatile than the active substance, and have a lower boiling point. They are appropriately selected depending on the substance and type of polymer, but specifically, lower aliphatic halogenated hydrocarbons such as methylene chloride, chloroform, and carbon tetrachloride, lower aliphatic alcohols such as methanol and ethanol, In addition to these acetic esters, one or a mixture of two or more of acetonitrile, acetone, ethyl ether, tetrahydrofuran, etc. can be used. In particular, lower aliphatic halogenated hydrocarbons such as methylene chloride are preferably used.

The concentration of the total amount of liquid active substance and polymer in a solution containing them is usually 10 to 40% by weight, preferably 15 to 30% by weight.

After this solution is applied onto a suitable support such as a resin film, metal foil or thin sheet, or a laminate thereof, the organic solvent is removed by evaporation.

The temperature when evaporating the organic solvent is usually 0 to 100°.
C1 is preferably in the range of 15 to 10°C and below the boiling point of the solvent. Normally, it may be at room temperature, but it may be heated if necessary. Alternatively, it may be evaporated under reduced pressure. In this way, as the organic solvent is evaporated, the liquid active substance has only a limited solubility in the polymer, and since the content exceeds the solubility in the polymer, the active substance and the polymer Phase separation occurs during coalescence, and the tiny droplets of active substance are uniformly dispersed in the polymer matrix, and thus the polymer forms a porous layer with a large number of independent micropores, within which The liquid active substance will be encapsulated in the liquid active substance. Usually, on the surface of the polymer, the concentration of the polymer increases as the solvent evaporates, and eventually a dense thin layer is formed on the surface of the porous layer, which is integrated therewith. In sheet-like preparations obtained by such methods, the micropores formed in the porous polymer layer usually have a thickness of 0.
．． These are independent pores partitioned by partition walls to 1 to 5 microns, and the pore diameter is approximately 0.5 to 10 microns. In addition, since the porous polymer layer has a porosity of about 30 to 80%, it can contain up to about 70% by weight of the liquid active substance, but in practical terms it can contain up to 50% by weight. The thickness of the porous polymer layer is not particularly limited, but is usually in the range of 10 to 500 microns.

In the above-mentioned sheet-like preparation, the liquid active substance encapsulated within the pores of the polymer layer has limited solubility in the polymer, so diffusion into the polymer is suppressed. In this way, emissions into the environment are reduced,
The liquid active substance is released at a controlled rate.

The active substance release surface 1a of the sheet-like preparation 1 is protected by a structure 2 that protects it from being easily affected by wind.

It is designed to maintain a stable and controlled release rate.

The structure 2 that is not susceptible to the effects mentioned here means, for example, as shown in FIG. The base material 3 is on the outside; examples include those formed into a cylindrical shape, a conical shape, or a prismatic shape.

In addition, as shown in FIG.
The active substance-containing film body 1b may be provided via the active substance-containing film body 1b, and this may be wound up into a cylindrical coil shape.

Further, the sheet-like preparation 1 may be stored in a container 6 having an opening 5 in a cylindrical, conical or prismatic shape as shown in FIG. 3, or in a bag having an opening 5 at one end as shown in FIG. It may be housed within the body 7 or may be formed by being housed within a bag body 9 provided with a plurality of holes 8 as shown in FIG.

In addition, a wind cover having an opening may be attached to the active substance release surface of the sheet-like preparation.

The base material of the container 6, the bag body 7.9, and the windshield cover may be plastic, paper, metal, or a laminate of these materials.

In either case, the area of the opening 5 or hole 80 is the area of the active substance release surface, the sum of the area of the active substance release surface and the effective area inside the container, or the area of the active substance release surface and the inside of the windshield cover. It may be 0.1 to 25% of the sum of effective areas, preferably 1 to 12.5%.

Example Insect pheromone, 7-7-ni]sen-11-
3 parts of polysulfone and 15 parts of polysulfone were dissolved in 100 parts of methylene chloride, and this solution was placed between 150 μm thick paper and 30 μm thick paper.
The above-mentioned Z A sheet-like preparation was obtained in which a film with a thickness of about 80 μm containing about 15% by weight of -7-nycosen-11-one was formed.

This sheet-like preparation 1010 x 25 pieces with a diameter of 1.6 cm,
It was fixed in a cylindrical polyethylene container with a height of 8 cm and one bottom open.

Next, this container was placed at a temperature of 25° C. and a wind speed of 2 m/w, and the release rate of Z-7-eicosen-11-one was measured.

At the same time, the release rate of Z-7-■ icosen-11-one was measured by placing the sheet-like preparation 1010X2S piece at the same location.

The release rate was calculated by quantitatively analyzing the amount of 7-fuA]sen-11-one remaining in the formulation.

The release rate of 7-eicosen-11-one from a sheet-like formulation in a plastic container was 6.0μ2dday.
This was the same as the set release rate at 25°C and no wind.

On the other hand, the release rate from the sheet-like preparation left uncontained was as high as 16.5μ2 days.

Effects As described above, according to the present invention, the active substance release surface of a preparation containing an active substance is protected by a structure that is less susceptible to the effects of wind. The effect of the active substance can be maintained over a long period of time.

[Brief explanation of drawings]

Each of FIGS. 1 to 5 is an explanatory diagram showing a typical example of the sustained release preparation according to the present invention. 1... Sheet-like preparation 2... Protective structure 3...
・Support base material 4... Spacer 5... Opening 6
... Container 7.9 ... Bag 18 ... Hole Patent applicant Nitto Electric Industry Co., Ltd. Agent Patent attorney Kazu 1) Showa-1
2-. Figure 1 Figure 2 1 bow 11, ・□・ni] Figure 8 Figure 5 '1a91

Claims (2)

[Claims] (1) An active substance sustained release preparation in which the active substance release surface of the preparation containing the active substance is protected by a structure that is less susceptible to wind effects. (2) Claim 1 in which the active substance is a pheromone
Active substance sustained release formulations as described in Section 1.