JPH02207002A - Gel type volatile drug - Google Patents

Abstract

PURPOSE:To obtain the subject drug capable of stably and sustainedly releasing a drug gel containing a drug volatile at ordinary temperature by filling the drug gel in an inner container provided with a nonwoven fabric in one side part thereof and housing the inner container in a state in which the surface of the nonwoven fabric is placed downward or tilted obliquely downward in an outer container having through- hole parts. CONSTITUTION:The subject drug obtained by filling a drug gel (G) containing a drug volatile at ordinary temperature in an inner container 1 so as to bring the above- mentioned gel (G) into contact with a nonwoven fabric 2 covering an opening of the inner container and housing the inner container 1 in an outer container 3 having through-hole parts 4 so that the surface of the nonwoven fabric 2 may be tilted downward or obliquely downward. Although the volume of the drug gel (G) is reduced with time by volatilization of the drug, the gel is always in a state of contact with the nonwoven fabric by own weight thereof. Thereby, the solvent in the gel and volatile drug are exuded and impregnated into the nonwoven fabric to volatilize the drug using the surface of the nonwoven fabric as a volatile surface having a wide volatilizing surface with high efficiency. Since the volatile drug is stably and sustainedly volatilized for a prescribed period without forming any residue, the drug has advantages in that the end point can be definitely discriminated.

Description

[Detailed Description of the Invention] [Field of Industrial Application] The present invention relates to a gel-type volatile agent, and more specifically, a gel-type volatile agent that can stably and slowly volatilize a room-temperature volatile agent for a certain period of time. Regarding drugs.

[Conventional technology]

The method of gelatinizing and solidifying volatile drugs is used, for example, in the field of deodorant fragrances, and gelling agents for such solid deodorant fragrances generally include agar, carrageenan, locust bean gum, and xanthan gum. (For example, see JP-A-49-1204 (I) and JP-A-53-50340.) In general, in the case of gel-like products of such conventional deodorant air fresheners, water Since it is a base and active ingredients such as fragrances are relatively easy to volatilize, no measures such as accelerating volatilization or regulating volatilization are taken, and they are volatilized directly from the surface of the gel.

On the other hand, sublimable solid agents such as paradichlorobenzene, naphthalene, and camphor have conventionally been used as insect repellents for clothing. Since these substances gradually sublimate themselves at room temperature and pressure, the remaining state of drug efficacy and its end point can be determined by the size and disappearance state of the drug in the form of granules, tablets, and balls. However, these solid insect repellents
Paradichlorobenzene and naphthalene have problems in terms of off-odor and safety (toxicity), while camphor has a problem in that it has low insecticidal efficacy. In recent years, liquid insecticides that are volatile at room temperature,
Insect repellents, especially emventrin, a pyrethroid insecticide, are attracting attention, and many products using this are now available. For example, a patent application published in 1982-159 proposed a method of packaging an insect repellent mat in which paper or plastic is impregnated with emventrin, which has no odor and is highly safe, in a plastic case or laminated paper or non-woven interior paper.
It is disclosed in No. 40.

[Problem to be solved by the invention]

In the case of the conventional gel-type deodorant air fresheners, active ingredients such as fragrances are volatilized directly from the surface of the gel, so active ingredients such as fragrances are relatively easy to volatilize at the beginning of use, but over time the surface of the gel becomes hard. There is a drawback that the amount of volatilization gradually decreases, and even though a considerable amount of the active ingredient still remains in the drug gel, the amount of volatilization is small, and a desirable constant amount of volatilization cannot be obtained throughout the period of use.

In order to eliminate these drawbacks, Japanese Patent Application Laid-open Sho (i3-1886
No. 57 discloses that a volatile drug solution is stored in a container having a lid made of a microporous film, and the container is periodically orientated automatically or manually with the lid upward, sideways, or downward. A method has been proposed for controlling the amount of volatilization of a chemical, which is characterized by leaving it for a while. However, this method of manually changing the orientation of the container periodically places the burden on the consumer, and the method of automatically changing the orientation requires special equipment, which reduces the product price. In any case, it would be difficult to commercialize the product. In addition, because the chemical vapor needs to pass through a microporous film, the effect is low unless the chemical itself is highly volatile; in the case of chemicals that are relatively difficult to volatilize, such as insecticides, There is a problem that the necessary amount of volatilization cannot be secured. Furthermore, there is a risk that the drug solution in the container may ooze out excessively and cause dripping, and if the container or film is damaged, there is a possibility that the surrounding area will be contaminated.

On the other hand, liquid insecticides that are volatile at room temperature, such as emventrin, have high efficacy and are sufficiently satisfactory compared to the sublimable insect repellents. However, on the other hand, unlike the sublimation insect repellent, which clearly indicates its end point by disappearing, liquid drugs such as emventrin are generally used in the form of an impregnated body. Therefore, even at the end of efficacy, the impregnated body such as paper or plastic remains in the same shape, and there is no change in appearance, so there is a problem that the end point of use cannot be clearly recognized.

Therefore, the object of the present invention is to eliminate the above-mentioned drawbacks and
Gel-type volatilization that can volatilize all room-temperature volatile chemicals in a stable and sustained manner for a certain period of time depending on the purpose of use, and leaves almost no residue after the volatilization of the chemicals is completed, so the end point can be clearly identified. The goal is to provide medicine.

[Means to solve the problem]

According to the present invention, in order to achieve the above object, a drug gel containing a room temperature volatile drug is filled into an inner container provided with a nonwoven fabric on at least one side so that the drug gel comes into contact with the nonwoven fabric, The inner container filled with the drug gel is tilted downward or diagonally downward so that the surface of the nonwoven fabric is entirely or partially at an angle of 0" to less than 90" with respect to the horizontal plane. A gel-type volatile chemical is provided which is housed in an outer container having a through hole.

[Operation and mode of the invention]

As described above, when a volatile drug is directly volatilized from the gel surface in a water-based drug gel, the surface of the gel becomes hard over time, the amount of volatilization gradually decreases, and the volatilization efficiency deteriorates. In addition, in the case of oil-based gels containing liquid insecticides, etc.
Since these insecticides and the like are difficult to volatilize compared to aromatic and deodorizing ingredients, the required amount of volatilization cannot be secured using the same conventional formulation, that is, the method of volatilizing directly from the gel surface.

On the other hand, as in the present invention, the inner container filled with the drug gel so as to be in contact with the nonwoven fabric is provided so that the surface of the nonwoven fabric is entirely or partially at an angle of 0'' to less than 90'' with respect to the horizontal plane. If the container is stored in an outer container having a through hole in a downward or diagonally downwardly inclined state, the volatile drug can be vaporized in a sustained manner for a certain period of time with high efficiency. In other words, the solvent and volatile agent in the gel ooze out and impregnate the nonwoven fabric, and the surface of the nonwoven fabric, which is microscopically uneven and has a large volatilization area, is used as the volatilization surface. The chemical is vaporized. At this time, if the gel and the nonwoven fabric are not in constant contact, the solvent and the volatile drug will not ooze out onto the surface of the nonwoven fabric, resulting in a decrease in volatilization efficiency. This can occur when the volume of the gel decreases as volatilization progresses, but in the present invention, the inner container is stored in the outer container with the surface of the nonwoven fabric facing downward or diagonally downward. Even when the volume of the gel decreases, the gel always comes into contact with the non-woven fabric surface, allowing the solvent and volatile chemicals to ooze out to the non-woven fabric surface and volatilize from the non-woven fabric surface efficiently, making up for the amount of volatilization. As a result, the solvent and the volatile drug ooze out onto the surface of the nonwoven fabric, and the volatile drug can be evaporated in a sustained manner over a certain period of time with high efficiency. Note that instead of using only the nonwoven fabric described above, it is possible to use a transparent film in which nonwoven fabric is attached to both sides of the transparent film, as described below, and it will have the same effect as the above and will also prevent liquid leakage when the gel liquefies. Can be effectively prevented.

The gel type volatile agent of the present invention includes agar, carrageenan, locust bean gum, xanthan gum, water gelling agent (for example, Sumikagel N-100 manufactured by Sumitomo Chemical ■), gelatin,
Isoeugenol, benzaldehyde, octylaldehyde, jasmine, g-carvone, benzyl acetate, methyl benzoate are produced using alginate, casein, polyvinyl alcohol, polyethylene oxide, polyacrylate, etc., and various conventionally known gelling agents based on these. Not only can it be applied to water-based deodorant fragrance gels made by gelatinizing various fragrances and blended fragrances such as , methylbenzyl carbinol, acetaldehyde, and pineapple oil, but also to oil-based gels. From the viewpoint of efficient volatilization, it can be suitably applied to topical gels such as insecticides and fungicides that are volatile at room temperature, and can be used to sustainably release insecticides and fungicides over a long period of time. It can be suitably used as an insect repellent for clothing, a mold repellent, etc., which is volatilized.

According to the research conducted by the present inventors, liquid insecticides and volatile fungicides that are volatile at room temperature are conventionally used to solidify oils, such as N-acylamino acid amides and N-acylamino acid amine salts. , N-acyl amino acid derivative gelling agent such as N-acyl amino acid ester (Japanese Patent Publication No. 51-4207
9), 12-hydroxystearic acid, benzyl sorbitol derivatives (for example, product name GELOL T1 manufactured by Shin Nippon Rika), hydrogenated castor fatty acids, etc., and when a hydrocarbon solvent is used, gelation is achieved well. It has been found that the volatilization of the above-mentioned drug is carried out stably over a long period of time.

Examples of such insecticides that are volatile at room temperature include (R,5)-1-ethynyl-2-methylbent-2-
enyl (IR)-cis, transchrysanthemate (hereinafter referred to as emventrin), 1-ethynyl-2-methyl-2=pentenyl-2,2-dimethyl-3-(2'2
'-dichlorovinyl)-cyclopropane-1carboxylate, 1-ethynyl-2-methyl-2-pentenyl-
2,2,3,3-tetramethylcyclopropanecarboxylate, 3-allyl-2-methylcyclobent-2-
en-4-one-1-yl-2,2,3,3-tetramethylcyclopropanecarboxylate (hereinafter referred to as terrarethrin), 5-(2-propargyl)-3-furylmethylchrysanthemate (-generic name flamethrin),
pyrethroid insecticides such as dichlorvos, room temperature volatile insecticides such as dichlorvos, dimethyl phthalate, diethyl phthalate, dibutyl phthalate, diethyl fumarate, N,N-diethyl-
Insect repellents and repellents such as m-toluamide, six insect repellents such as ethyl benzoate, safrole, isopropyl, eugenol, citronellol, anethole, and g-carvone, insect repellents and fungicides such as cinnamic aldehyde and benzaldehyde, and other sublimation agents. The above insecticidal agents can be used alone or in combination of two or more. Further, examples of the volatile fungicide include α-bromucinnamaldehyde (BCA), 2-isopropyl-5-methylphenol (thymol), and the like.

The three types of N used as gelling agents for the various drugs mentioned above.
- Among the acylamino acid derivatives, N-acylamino acid esters and N-acylamino acid amides can be prepared, for example, by heating reaction of N-acylamino acids with alcohols or amines in the presence of an acid catalyst or without a catalyst, or Alternatively, it can be obtained by N-acylating an amino acid amide with an acylating agent such as a fatty acid halide. Further, N-acylamino acid amine salts can be easily obtained by neutralizing N-acylamino acids with amines.

The amino acids of the above N-acylamino acid derivatives include α
-Various amino acids such as β-ω-amino acids are used, especially glycine, α-alanine, β-alanine, valine, serine, methionine, phenylalanine, 3,4-dioxyphenylalanine, aspartic acid, glutamic acid, lysine, ornithine. , arginine, histidine, ε
-Aminocaproic acid etc. are used. In addition, mixtures of amino acids may be used, such as hydrolysates of proteins from soybeans, fish meat, yeast, algae, or residual amino acids in waste liquid from amino acid production.

Further, the N-acyl group in the N-acyl amino acid derivative is a linear or branched saturated or unsaturated aliphatic or aromatic acyl group or alicyclic acyl group having 1 to 30 carbon atoms, preferably 2 to 18 carbon atoms. In particular, it may be a caproyl group, a capryloyl group, a lauroyl group, a myristoyl group, a stearoyl group, or a mixture thereof.

The alcohol used for esterification is a linear or branched saturated or unsaturated aliphatic or aromatic alcohol or alicyclic alcohol having 1 to 30 carbon atoms, preferably 8 to 18 carbon atoms, such as octyl alcohol, lauryl alcohol, hexasol alcohol, isostearyl alcohol,
Examples include stearyl alcohol, benzyl alcohol, and cyclohexanol.

In addition, the amines used for amidation and amine salts include ammonia, linear and branched saturated and unsaturated primary and secondary amines having 2 to 60 carbon atoms, preferably 2 to 18 carbon atoms, mono- and dialcohol amines ( For example, mono- and jetanolamines), aromatic amines, cycloaliphatic amines and tertiary amines, trialolamines (eg triethanolamine) are used in amine salts.

Various types of gelling agents are commercially available, such as oil gelling agent GP-IJ manufactured by Ajinomoto Co., Ltd. and Gel All D manufactured by Shin Nippon Chemical Co., Ltd. The above rGP-IJ is preferable in that it gels at a certain concentration. Also, regarding 12-hydroxystearic acid, an oil-based gelling agent manufactured by Nippon Oil & Fats Co., Ltd. is commercially available.

Further, a hydrocarbon solvent is used as the solvent, and for example, aliphatic or aromatic hydrocarbons such as kerosene, liquid paraffin, benzene, and toluene can be used. In the case of paraffinic hydrocarbons, it is preferable to use a paraffinic hydrocarbon having 13 to 18 carbon atoms, since the smaller the number of carbon atoms, the faster the paraffinic hydrocarbons volatilize, making stable volatilization difficult over a long period of time.

By using a paraffinic hydrocarbon having a carbon number in this range as a solvent, continuous volatilization for about 4 to 7 months is possible. Furthermore, if a kerosene-based solvent is used, continuous volatilization for about 6 months is possible.

The blending ratio of each component of such an oil-based drug gel is 2 to 15 ffi of gelling agent to 100 parts by weight of carbon hydrogen solvent.
A suitable amount is 0.65 to 10 parts by weight of the room temperature volatile agent, and after adding a predetermined amount of the gelling agent to the hydrocarbon solvent and dissolving it by heating above the dissolution temperature (about 70-150°C), the above-mentioned A gel-like product can be easily produced by adding a predetermined amount of a liquid insecticidal agent or other volatile agent at room temperature and allowing it to cool.

Generally, when the temperature rises, gel begins to synergate and liquefy. For example, when 12-hydroxystearic acid is used as a gelling agent, the formed gel gradually begins to liquefy at temperatures above 60°C. Therefore, in order to prevent liquid leakage during liquefaction, it is preferable to laminate a permeable film, such as a polyolefin film, on the inner surface of the nonwoven fabric of the inner container. In this case, during use, the active ingredient and solvent from the gel gradually pass through the permeable film as a liquid and are once impregnated into the nonwoven fabric, and volatilization occurs through the nonwoven fabric with a large surface area, so the volatilization rate is constantly maintained. It is very preferable to do so. The thickness of the transparent film is 15-70μm
is preferred. If it is thinner than 15 μm, pinholes will easily occur and it will be difficult to prevent liquid leakage at high temperatures, which is undesirable. On the other hand, if it is thicker than 70 μm, it will be difficult to heat-fuse during processing or the active ingredients in the gel will be This is not preferable because it makes it difficult for the solvent to penetrate, resulting in a decrease in the volatilization rate.

Note that the drug gel used in the present invention may contain colorants, fragrances, antioxidants, ultraviolet absorbers, and the like as appropriate.

〔Example〕

The present invention will be specifically described below with reference to Examples.

Example 1 A gel consisting of 6 parts by weight of fragrance, 0.6 parts by weight of emulsifier, 3 parts by weight of carrageenan, 0.5 parts by weight of potassium chloride, and 100 parts by weight of water was prepared.

As shown in FIG. 1(A), this gel G is filled into the inner container 1 so that it comes into contact with the rayon nonwoven fabric 2 covered at the opening of the inner container. The inner container 1 filled with the gel G was housed in the outer container 3 having a through hole 4 so that the surface of the nonwoven fabric 2 faced diagonally downward.

Figure 1 (B) shows how the gel changes over time as the drug evaporates.
and (C), the volume of the gel gradually decreased as the drug volatilized, but it was always in contact with the nonwoven fabric due to its own weight.

Comparative Example 1 Gel G prepared according to Example 1 above was filled into the inner container 1 as shown in FIG. 8, and directly volatilized from the gel surface in that state.

Changes in the fragrance of the gel products of Example 1 and Comparative Example 1 over time were evaluated by olfaction. The results are shown in Table-1.

Table-1 Meaning of the symbols in the above table (O: smells good, Δ: smells, ×
When the gel products were compared after 8 weeks, more gel remained in Comparative Example 1.

Examples 2 to 13 Gels were prepared according to the various formulations shown in Table 2.
The container was filled as shown in Figure (A). Note that the amount of solvent used was 100 parts by weight.

The gelation state and volatilization period of each example are also shown in Table 2.

Example 14 100 parts by weight of No. 0 solvent (Japan Petrochemical side! 2),
A gel consisting of 5 parts by weight of 12-hydroxystearic acid and 5 parts by weight of empenthrin was prepared, and this was shown in Figure 1 (A
20g was filled into the container as shown in ).

However, the nonwoven fabric 2 covering the opening of the inner container 1 is made by laminating a 20 μm thick polyethylene film on the inner surface of a rayon nonwoven fabric.

Example 15 20 g of the gel prepared according to Example 14 was placed in a container as shown in FIG. 2(A).

That is, the inner container 1 filled with gel G is
The rayon nonwoven fabric 2 laminated with m-thick polyethylene film was housed in the outer container 3 so that the surface thereof faced downward and was spaced a certain distance from one side of the outer container 3 via the legs 5. The state of the product changing over time as the chemical volatilizes is shown in FIGS. 2(B) and 2(C), and the gel G is always in contact with the nonwoven fabric.

Example 16 As shown in FIG. 3, the gel prepared according to Example 14 was placed in a bag-shaped inner container 1a made of a non-woven fabric 2 whose inner side was laminated with a polyethylene film having a thickness of 20 μm.
0 g was filled and stored in the outer container 3a in an upright state.

Example 17 As shown in FIG. 4, 20 g of gel was stored in a container in the same manner as in Example 16, except that the nonwoven fabric 2 was placed with its surface facing downward.

Comparative Example 2 Same as Example 14 above, except that the inner container 1 filled with gel G was placed so that the surface of the nonwoven fabric 2 faced diagonally upward so as not to come into contact with the nonwoven fabric 2, as shown in FIG. The gel was stored in a container.

Comparative Example 3 As shown in FIG. 6, gel G was placed in contact with nonwoven fabric 2.
The gel was stored in the container in the same manner as in Example 14, except that the inner container 1 filled with gel was placed so that the surface of the nonwoven fabric 2 faced diagonally upward.

The changes over time of the products of Comparative Examples 2 and 3 as the chemicals volatilize are shown in FIG.

Comparative Example 4 As shown in FIG. 8, 20 g of gel G prepared according to Example 14 was filled into the inner container 1, and directly volatilized from the gel surface without covering with a nonwoven fabric.

Test Example 1 The gel products of Examples 14 to 16 and Comparative Examples 2 to 4 above were volatilized, and the remaining amount of gel and emventrin were determined 4-1 at regular intervals, and the volatilization rate of each product was compared. . The results are shown in Table-3.

Table 3 Table 4: Relationship between thickness and volatilization rate of laminate film Test example 2 No. 0 solvent (Japan Petrochemical Co., Ltd. An insect repellent gel for clothing consisting of 100 parts by weight (manufactured by Co., Ltd.), 5 parts by weight of 12-hydroxystearic acid, and 5 parts by weight of empenthrin was filled, and the remaining amount of the gel was compared at regular intervals. The results are shown in Table 4.

As is clear from the results shown in Section 3 above, in the case of the gel-type volatile chemical according to the storage mode of the present invention, the chemical can be volatilized with high volatilization efficiency over a long period of about 6 months. In addition, from the results shown in Table 4, it can be seen that when laminating a transparent film on a nonwoven fabric, the appropriate thickness of the film is 15-70 μm.

〔Effect of the invention〕

As described above, the gel-type volatile drug of the present invention is arranged so that the inner container filled with the drug gel is in contact with the non-woven fabric so that the surface of the non-woven fabric is entirely or partially 0" to 90@ Because the gel is stored in an outer container with perforations that is tilted downward or diagonally downward at an angle of less than The non-woven fabric surface, which is microscopically very uneven and has a wide volatilization area, is used as the volatilization surface, so volatile chemicals are volatilized with high efficiency, and when the gel volume becomes small, Since the gel is always in contact with the non-woven fabric surface, the solvent and volatile drug can be efficiently exuded to the non-woven fabric surface and volatilized from the non-woven fabric surface, and the solvent and volatile drug can be removed from the non-woven fabric surface in a way that compensates for the amount of volatilization. The leaching progresses and the volatile agent can be evaporated with high efficiency in a sustained manner for a certain period of time.As a result, the surface of the gel becomes hard over time, unlike traditional water-based deodorant air freshener gels. There is no problem that the amount of volatilization gradually decreases, and even oil-based gels containing liquid insecticides and the like that have a relatively slow volatilization rate can be efficiently volatilized.

Furthermore, because of its gel-like dosage form, it is easy to use, and the end point of use can be clearly determined because most of the active ingredient evaporates at the end point of efficacy, leaving almost no residue.

[Brief explanation of the drawing]

FIG. 1 is a vertical cross-sectional view showing an embodiment of the gel-type volatile chemical of the present invention, in which FIG.
and (C) show the state after a certain period of time has elapsed, and FIG. 2 is a longitudinal cross-sectional view showing another embodiment of the present invention.
A) shows the state when the gel is filled, FIGS. 2B and 2C show the state after a certain period of time, FIGS. 3 and 4 are longitudinal sectional views of other embodiments, and FIGS. FIG. 8 is a longitudinal cross-sectional view of a comparative example. 1.1a is an inner container, 2 is a nonwoven fabric, 3, 3a is an outer container, 4
is the transparent pore, and G is the gel. Figure +41 1B+ (C1 Figure / Figure Figure

Claims (3)

[Claims] (1) A drug gel containing a drug that is volatile at room temperature is filled into an inner container provided with a nonwoven fabric on at least one side so that the drug gel comes into contact with the nonwoven fabric, and the drug gel is filled in this way. The container is tilted downward or diagonally downward so that the surface of the nonwoven fabric is entirely or partially at an angle of 0° to less than 90° with respect to the horizontal plane,
A gel-type volatile chemical stored in an outer container with a through hole. (2) The gel-type volatile drug according to claim 1, wherein a permeable film is laminated on the inner surface of the nonwoven fabric, and the drug gel is in contact with the nonwoven fabric via the permeable film. (3) The gel-type volatile chemical according to claim 1, wherein the nonwoven fabric is a nonwoven fabric adhered to both sides of a transparent film.