JP2005198861A - Sustained-release gel form composition of volatile substance - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a sustained-release gel form composition of a volatile substance which is excellent in the persistence of volatile substance release and can keep the effect for a long period. <P>SOLUTION: This gel form composition contains the volatile substance, oil constituents, water soluble constituents, polyacrylic acid and/or polyacrylate, and a crosslinking agent. In the composition, the volatile substance and the oil constituents are contained by 1 to 40 mass% in total. In the gel form composition, with shrinking of the gel in the process of use, the volatile substance or the oil constituents containing a volatile constituent contained in the gel are gradually oozed out. In addition, by imparting an absorptive medium absorbing the oozed out volatile substance or the oil constituents containing the volatile constituent to the gel form composition, a volatilization area can be increased to suppress the reduction of the volatilization of the volatile substance in the latter half of the period of use to keep the effect of the volatile substance of the same degree as that at the primary stage of the use. <P>COPYRIGHT: (C)2005,JPO&NCIPI

Description

  The present invention contains a volatile substance, an oily component, a water-soluble component, polyacrylic acid and / or a polyacrylate, and a cross-linking agent, and is excellent in sustainability of volatile substance release and can maintain its effect for a long time. The present invention relates to a sustained-release gel-like composition of an active substance.

  Products such as solid-type fragrances and deodorants that use water-absorbent resins may cause contamination of the surroundings due to the fall of the container if separation of non-water-soluble components such as fragrances occurs during use. There's a problem. Therefore, various studies have been made in order not to cause separation of the fragrance.

  For example, a surfactant is added to uniformly disperse an oily component such as a fragrance in a water-soluble component, and a basic composition includes a water absorbent resin, a fragrance, a surfactant, and water (Patent Document 1). Moreover, from the viewpoint that the perfume is considered to prevent volatilization from the water system due to the presence of the surfactant even in a small amount, no oil-soluble substance is used, and water, perfume, water absorption There is one (Patent Document 2) based on a composition composed of a functional resin, and it is described that a water-absorbing resin having a fine particle diameter is used in order not to cause separation of a fragrance. All of these are provided as fragrances that do not allow the perfume to exude excessively.

  Products using these water-absorbing resins have a fresh and wide gel composition surface at the initial stage of use, so that the volatilization of volatile substances is fast and the drug effect is good. In the process, as the gel contracts, the surface solidifies, dries, and contracts, and the drug effect of the volatile substance is lowered, and there is a problem that the uniformity of the effect is inferior in the process of use.

Therefore, in order to solve these drawbacks, as a developed method, a method of increasing the surface area of the gel by chopping the gel during use or using a container having a partition piece inside (Patent Document 3), a drug There is a technique (Patent Document 4) composed of a first gel-like part containing an ingredient and a second gel-like part containing a higher concentration of the drug component than the first gel-like part. There wasn't.
JP-A-57-131450 JP-A-10-295794 JP-A-3-57456 JP 2000-70352 A

  An object of the present invention is to obtain a sustained release property that is the same as that in the initial stage even in a later stage of use in which a gel contraction has progressed in a sustained release gel composition of a volatile substance.

  In the process of using the gel composition according to the present invention, as the gel contracts, the volatile substance contained in the gel or the oily component containing the volatile substance is gradually leached from the gel. Volatile substances that maintain the sustainability of volatile substance release by actively utilizing `` exudation of volatile substances '' and can achieve the same pharmacological effects of volatile substances in the later stages of use A sustained-release gel composition is provided.

  More specifically, it is a gel-like composition containing a volatile substance, an oily component, a water-soluble component, polyacrylic acid and / or a polyacrylate, and a crosslinking agent, wherein the volatile substance and The said subject is achieved by containing an oil-soluble component in the ratio of 1-40 mass% in total amount.

  Furthermore, by applying an absorbing medium to the gel surface, the absorbing volatile substance or oil component containing the volatile substance is reabsorbed by the absorbing medium, so that the surface of the medium that matches the surface area of the contracted gel is used. By doing so, the area of the volatile surface can be made constant and the volatilization rate can be controlled without attenuation.

  In the gel composition of the present invention, as the gel contracts in the process of use, the volatile substance contained in the gel or the oily component containing the volatile substance gradually exudes from the gel. By absorbing the volatile substances that have exuded or the oily components containing the volatile substances into the absorbent medium with the ability to impregnate or absorb oil, the volatilization area is increased to suppress the reduction of volatilization of the volatile substances in the later stages of use. Can maintain the same effect as volatile substances. Furthermore, by changing the constituent components of the oily component to be used, the leaching rate can be arbitrarily adjusted, and the volatilization amount of the volatile substance can be controlled.

  The sustained-release gel-like composition of the volatile substance of the present invention is a gel-like composition containing a volatile substance, an oily component, a water-soluble component, polyacrylic acid and / or polyacrylate, and a crosslinking agent. The composition contains volatile substances and oil-soluble components in a total amount of 1 to 40% by mass, and in the process of using the gel-like composition, the volatilization contained in the gel accompanying the gel shrinkage. The oily component containing volatile substances or volatile substances gradually exudes from the gel, and this exudate is absorbed into the absorbent medium, increasing the volatilized area, thereby suppressing the reduction of volatilization of volatile substances in the later stages of use, and the initial use It is characterized by maintaining the effect of volatile substances at the same level as time.

  The polyacrylic acid and polyacrylic acid salt used in the present invention are not particularly limited in their molecular weight and linear, branched, etc. shapes, and two or more types can be used in combination. Examples of the polyacrylic acid salt include monovalent metal salts of polyacrylic acid such as sodium salt and potassium salt of polyacrylic acid. When polyacrylic acid and polyacrylic acid salt are used in combination, the compounding ratio (mass ratio) is preferably 1:10 to 10: 1. The polyacrylic acid salt may be 100% neutralized or partially neutralized polyacrylic acid. When using partially neutralized polyacrylate alone or in combination with polyacrylic acid, the ratio of neutralized carboxyl groups to carboxyl groups in polyacrylate and polyacrylic acid should be the above ratio Is preferred. The total content of polyacrylic acid and polyacrylate can be appropriately selected in order to obtain the intended gel strength, and is preferably 0.1 to 20% by mass, more preferably based on the total amount of the gel composition. Is blended in an amount of 0.5 to 10% by mass.

  As the medium constituting the gel composition, water is used. In addition to water, antifreezing and as a low temperature stabilizer, ethanol, isopropyl alcohol, ethylene glycol, propylene glycol, 1,3-butanediol, Polyhydric alcohols such as xylene glycol and glycerin, glycols and the like can be appropriately added.

  The crosslinking agent used in the present invention is not particularly limited as long as it acts on the carboxyl group of polyacrylic acid to form a crosslinked structure and is a compound having at least two reactive sites in the molecule. For example, a compound having an epoxy group, a polyvalent metal salt, and the like can be mentioned, and a polyvalent metal salt is particularly preferable, and examples thereof include magnesium hydroxide, calcium hydroxide, aluminum hydroxide, and aluminum sulfate. The blending amount of these crosslinking agents can be appropriately selected in order to obtain the intended gel strength, and is 0.001 to 20% by mass, more preferably 0.01 to 5%, based on the total amount of the gel composition. It is blended by mass%.

  In order to adjust the curing by the crosslinking agent, an acid can be added as necessary. The acid may be an inorganic acid or an organic acid, and examples thereof include citric acid, lactic acid, malic acid, acetic acid, tartaric acid, phosphoric acid, adipic acid, and the like. Can be used in appropriate combination. These acids can be added according to a known method to adjust the gel strength. The preferable addition amount of these acids is 0.001-5 mass%, More preferably, it is about 0.005-2 mass%.

  The volatile substance used in the present invention is transpiration under room temperature conditions such as a fragrance, a deodorant, a deodorant, an insecticide, an insecticide, a repellent, an attractant, etc., depending on the intended use of the resulting gel composition. It is a substance having a property, and is a mixture of one or more of them. The blending amount of these volatile substances can be appropriately selected in order to obtain the intended release control or according to the difference in the type, application, form, etc. of the volatile substances. Generally, it is 1-40 mass% with respect to the gel composition whole quantity, More preferably, 3-30 mass% is mix | blended. If it is less than 1% by mass, the volatilization amount of the volatile substance is small, so that the intended function of the volatile substance-containing composition cannot be exhibited. On the other hand, if it exceeds 40% by mass, the gel state is deteriorated.

  The oily component used in the present invention is used as a carrier solvent for volatile substances, and any oily component can be blended. Examples of the oil component include hydrocarbons such as liquid paraffin, polar oils such as isopropyl myristate, and the blending amount of these oil components is 0 to 0 based on the total amount of the gel composition. It is 39% by mass and is appropriately blended depending on the volatilization state of the volatile substance. In order to maintain the stability of the gel, the total amount of the volatile substance and the oil component is preferably 40% by mass or less with respect to the entire gel composition.

In addition to the above components, the gel composition of the present invention can be blended with components that are usually used in gel compositions. Examples of these components include anionic surfactants such as fatty acid soaps and alkyl sulfates, nonionic surfactants such as polyoxyethylene alkyl ethers, polyoxyalkylphenols, and polyoxyethylene sorbitan alkylates, and quaternary ammonium. Surfactants such as cationic surfactants such as salts; Gel-based reinforcing agents such as natural polymers such as xanthan gum and roast bean gum; synthetic polymer materials such as cellulose and polyvinyl alcohol; aqueous dyes, fluorescent dyes, natural pigments And pigments such as inorganic pigments; parabens such as methylparaben; antiseptics such as benzoates; and UV absorbers.

  The method for producing the gel composition of the present invention is not particularly limited. For example, a volatile substance, an oil component, polyacrylic acid and / or polyacrylate, and a crosslinking agent are mixed at room temperature. The mixture is adjusted by adding a water-soluble component thereto and mixing at room temperature.

  In the present invention, as a medium for absorbing a volatile substance that exudes from the gel surface in the course of use or an oil component containing a volatile substance, any medium that has the ability to impregnate or absorb oil can be arbitrarily selected and is particularly limited. Although it is not a thing, For example, paper, cloth, mat, a piece of wood, powder particles, etc. are mentioned, and there is no limitation in particular also about a shape. The exudate absorbing medium is applied in contact with the gel composition, for example, on the surface of the gel composition or on the bottom of the container of the gel composition.

  EXAMPLES The present invention will be specifically described below with reference to examples, but the present invention is not limited to these examples.

(Examples 1 and 2)
According to Table 1, a predetermined amount of polyacrylic acid partially neutralized product (Acpana: manufactured by Sumitomo Seika Co., Ltd.), dry aluminum hydroxide gel (aluminum gel: manufactured by Chugai Pharmaceutical Co., Ltd.), apple flavor (made by Kamata Fragrance Co., Ltd.), Triethyl citrate and propylene glycol were mixed at room temperature (mixture A), and predetermined amounts of water and tartaric acid were mixed at room temperature (mixture B). Next, the mixture B was added to the mixture A and mixed at room temperature to obtain 50 g of a gel composition. A non-woven fabric (thickness: 1 mm, Φ: 5 cm circular shape) is laid on the bottom of the container, and the gel-like composition 50 g obtained thereon is placed thereon, and a sustained-release gel-like composition of the volatile substance (product of the present invention) ) Was produced.

(Comparative Examples 1 and 2)
According to Table 1, predetermined amounts of carrageenan, propylene glycol, water, and potassium chloride were weighed and dissolved uniformly at about 70 ° C. with heating and stirring. There, a mixed solution of a predetermined amount of a fragrance and a surfactant (Tween 80) was added and stirred, filled into a container, and cooled to room temperature to prepare 50 g of a gel composition.

  Each gel composition (gel fragrance) produced as described above was left in the room, and the state of the gel in the volatilization process was visually observed to examine the presence or absence of liquid exudation. Furthermore, the gel fragrance | flavor (Comparison of Example 1 and Comparative Example 1, the comparison of Example 2 and Comparative Example 2) with the same compounding amount of a fragrance | flavor was sniffed and compared by the special panel, and fragrance intensity was compared.

(Evaluation criteria for fragrance intensity)
○: Example (invention product) is stronger than comparative example Δ: Example (invention product) and comparative example are as much as ×: Example (invention product) is weaker than comparison example

  Thus, Examples 1 and 2 in which volatile substances or oily components containing volatile substances exude from the gel composition in the course of use have a stronger scent intensity over a longer period than the comparative examples in which no exudation occurs. I understand.

  The present invention is excellent in release control of substances having transpiration under room temperature conditions such as a fragrance, a deodorant, a deodorant, an insect repellent, an insecticide, a repellent, an attractant, and the composition ratio of volatile components in particular. Is particularly useful for those that affect the effect.

Claims (3)

A gel composition containing a volatile substance, an oily component, a water-soluble component, polyacrylic acid and / or a polyacrylate, and a crosslinking agent, and the total amount of the volatile material and the oil-soluble component in the composition The gel-like composition characterized by containing in the ratio of 1-40 mass%. 2. The gel composition according to claim 1, wherein the release of the volatile substance is controlled by leaching out the volatile substance or the oily component containing the volatile substance as the gel contracts. A volatile substance sustained-release molded article, wherein an exudate absorbing medium is applied to the surface of the gel-like composition according to claim 1 or the container bottom of the gel-like composition.