JPS58113103A - Method for slowing release of drug - Google Patents

Abstract

PURPOSE:To control the release of a drug, without causing the loss and blooming of the drug, by mixing a drug with a resin, curing and granulating the mixture, mixing further with a resin, and curing the mixture. CONSTITUTION:A drug (e.g. insecticide, synergist, repellent, etc.) is mixed with a resin (e.g. nitrocellulose, polyvinyl chloride resin, polyester resin, etc.), cured, granulated, mixed again with a resin and cured to achieve the control of the drug release. The dissipation of the drug can be arbitrarily and extremely effectively controlled according to the purpose. The slow-releasing composition obtained by the above process, i.e. mixing of a drug with a resin, curing and granulation of the mixture, mixing of the granules to a resin, and curing of the product, is used in combination with a supporting substrate (e.g. polyethylene, nylon, etc.)

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a method for sustained drug release, a composition thereof, and a sustained release material.

Is it conventionally known to mix drugs into resins to achieve sustained release of drugs (4)?The rate of release of the crosslinking material depends on the resin used, and it is difficult to achieve sustained release of highly volatile drugs. or control the sustained release of drugs as desired.
There were many things I couldn't do.

In addition, during or after curing, the bleaming phenomenon in which the drug is pushed out to the outer surface is likely to occur, resulting in loss of the drug, wetting, and
Furthermore, it had fatal drawbacks in terms of safety during use and impact on the texture of the ground material.

In view of the current situation, as a result of extensive research into a sustained release method that can prevent drug loss and moderately control drug volatilization, the present invention has been developed. 1. Sustained release of a drug, which is characterized by controlling the release of the drug by mixing the drug and resin A, curing, and then mixing the mixture into powder or granules with resin B and curing. Method. 2. The drug is an insecticide,
2. The method according to item 1, which is one or more of synergists, repellents, insect repellents, insecticides, fragrances, and deodorants. 3. 1. A sustained release composition for a drug, characterized in that a drug and resin A are mixed, the resulting powder/granules are mixed with resin B, and the mixture is cured. 4.
Sustained release of a drug, characterized in that the drug and resin A are mixed, the resulting powder/granules are mixed with resin B, and the cured sustained release composition is held on a base material. Related to materials.

In the present invention, as described above, the drug and resin A are mixed, hardened (or dried), made into powder or granules, and further mixed with resin B and cured, thereby unexpectedly reducing the amount of drug and the drug. It has the characteristics of preventing pluming and controlling the volatilization of chemicals arbitrarily and extremely effectively depending on the purpose.

In the present invention, the mixing ratio when mixing the drug and resin A to form powder or granules can be arbitrarily determined depending on the properties of the drug and resin B and the purpose. On the other hand, 1 to 100 parts by weight of the resin A is suitable, and powdering and granulation can be carried out by any commonly used method.

Also, the mixing ratio with resin B can be arbitrarily determined according to the purpose as described above, but it is preferable that the resin
1 to 50 parts by weight of IIIV B O is suitable.

The tree lI used by the present invention Yuuko! To specifically list examples of the class, cellulone derivatives include nitrose V-lose,
Acetyl cellulose, acetyl lebutyrylse M loose,
Methi I cellulose, Ethi M cellulose, acetylprobionylse! Reulose, benzyl cellulose, hydroxypropyl cellulose, 8- and phosphorylated cellulose, etc. Vinyl resins include polyvinyl alcohol, polyvinyl acetate, polyvinyl chloride, vinyl acetate/vinyl chloride copolymer, polyvinyl acetal, polyvinyl butyral, polystyrene. , polymethyl acrylate resin, etc. Alkyto resins include condensed resins made by modifying the condensate of polyhydric alcohols such as glycerin and pentaerythritol and polybasic acids such as phthalic acid with oil or fatty acids to make them soluble.

Acid-curing urea resins include urea with a low degree of etherification or urea/melamine cocondensation resins, etc. Epoxy resins include halogenated bisphenol type, resorcinol type, hispheno-/I/F type, tetrahydrophenylethane type, novolac type, and polyester resin. Alcohol/polyglycol type, glycerin triether type, polyolefin type, epoxidized soybean oil or epoxy resin amine, etc. are available, and if necessary, diethylene triamine, 4-triethylenetetramine, m-phenylene diamine, diaminodiphenyll/nupropolyamide Amine-based curing agents such as phthalic anhydride, hexahydrophthalic anhydride, pyromellitic anhydride, maleic anhydride mixtures, and other organic acid anhydride-based curing agents can be used.

Examples of the polyester resin include unsaturated dibasic acids such as maleic anhydride and phthalic acid, saturated dibasic acids such as adipic acid, phthalic anhydride, isophthalic acid and tetrachlorophthalic anhydride, ethylene glycol, glopylene glycol, 1. l-
There are polyester resins that are made by condensing dihydric alcohols such as butylene glycol, diethylene glycol, diethylene glycol, and neopentyl glycol.Urethane resins are resins that have urethane bonds, and contain isocyanates and at least two hydroxyl groups at the end of the molecule. The isocyanates include hexamethylene diisocyanate, naphthalene-1,5-diisocyanate), 4,4'-diphenyVmethane diisocyanate, polymers of the above diisocyanates, and the above diisocyanates. Reaction products with trimethylo-propane etc., biliols include ethylene glycol-2, glopylene glycol, butylene glycol (
1゜3-butanedio-v) 1,2,6-hexane trio-I, polyhydric alcohols such as trimethylolpropane, glycerin, sorbitol, etc., polyethers which are polymers of the above polyhydric alcohols, polyethers which are polymers of the above polyhydric alcohols, Polyester polyol or acrylic direboliol, which is a reaction product of alcohols and their polymers with dibasic organic acids, or alkyd polyol-V, etc., which is obtained by modifying the above-mentioned polyether V polyol-7 with coconut oil or mustard oil. There is.

Examples of polysaccharides include vegetable gums such as gum arabic, chitin, xatone, pectin, starch, and inulin; examples of proteins include gelatin, casein, peptone, and a! There are Repmin etc.

Natural trees 11 include rosin, cashew, rosin or rosin methyv5 monoethylene glycol, diethylene glycol-I, esters such as greichlin, rosin derivatives such as hydrogenated rosin, dehydrogenated rosin, polymerized rosin, amber, Some examples include kohl, kaurigam, dammer mastic, sandarac, shellac, and 48i.

The drugs used for the invention are not particularly limited, but include the following:

Insecticides include pyrethrin, allethrin, phtarnurin, resmethrin, permethrin, fenvalerate, phenothrin, flamethrin, cypermethrin, cyphenothrin, 1-ethynyl-2k, 1 1[ -methy! 2-pentenyl 2,2-dimethyl rv -8
-! Birenuroid dry insecticides such as (2'-methifre-1'-propenyl)-ncropropoxylate (hereinafter referred to as MA), organophosphorus insecticides such as DDVP, diazinon, numithion, marathon, dibrome, etc. Carbamate parasiticides such as pyridafenthione, propoxal, and sevin are synergistic agents such as S-421, piperonyl butoxide, cinevirin 222, and cinepirin 500.
, Viperoner (dimethyl acetal, etc., or repellent)
i N, N-diethyl V-m-toyamide, butyridiacetanilide, ethylhexanediol, butylhydroxyaniso-〃, pt-butyl-m-cresol, etc., but for insect repellents naphthalene, camphor, paradichlor Bactericidal agents such as benzoic acids, sorbic acids, P
CMX, BCA, thiophanate, triazine, Iμgasan DP 800, hinokitiol, TBZ, Daconil, etc. are used as fragrances and deodorants such as Harinaol, geraniol,
These include cinnamic alcohol, 8-anethole, citler W, tronella V, cinnamaldehyde, lilyaz, limonene, vanillin, musk ketone, cineole, lauric acid methacrylate, and the like.

Depending on the purpose, one or more of these can be used in any combination.

The present invention also provides a lace material, which is made by holding the above-mentioned cotton lint 41 silk composition on a base material. Applicable '
The f,t-AU material can be used as a sheet cover material, furniture member, etc. that has pest repellent properties by taking advantage of the characteristics of the base material.

Here, examples of the base material include polyethylene, polypropylene, nylon, polyvinyl chloride, polyvinylidene chloride, polyester, etc. 61) II? Sheets, sheets made of animal or plant matter or inorganic materials (paper, cloth, non-woven fabric, leather, etc.), mixed sheets or blended fabrics of synthetic fibers and inorganic fibers or powder, combinations of the above synthetic resins and animal and plant a fibers, etc. Examples include blended fabrics or nonwoven fabrics, foils or foils of metals such as aluminum, stainless steel, and zinc, and laminated sheets of the above-mentioned various sheets. Further, as the above-mentioned base material, it is also possible to effectively utilize natural wood such as awl, pencil lumber, oak, etc., and molded products of plastics such as vinyl chloride resin, chlorinated polyethylene, polyethylene, polypropylene, etc., which are used as furniture members.

The method of holding the composition is not particularly limited, for example, by coating, impregnating, dripping, kneading, etc., and retaining it in the form in which it is held on the base material. It can be placed or pasted on the desired location and used from a pot.

The amount retained is also not particularly limited, and may be determined as appropriate, or may be determined by saturation impregnation of the base material, etc.

By changing the mixing ratio of drugs treated in this way with Class 1!8 A, the desired sustained release properties can be obtained, and the drug can be used as a product that matches the purpose and period of use of the drug. It will be of practical use.

The following is a detailed explanation of ``Unexploded 1υ'' as an example.

Example 1゜The chemicals shown in the table number above are mixed with 1 mol fat A, placed on a plate, and then cured or dried 1'! ! ! and crush it with an atomizer. Passed 200 mesos! 5) Add the end to the sugar for remixing! After mixing with the old 72 Q/Wl upper 'α paper (20x2
After applying 60 g/g of the material to a 0 cm), it was dried and cured for 100 minutes and used as a sheet cover.

Test Example 1 Using the treated sheet of Example 1 and a sheet prepared by mixing only the drug and remixing resin (comparison sheet), the sustained release effect was compared by analyzing the number of remaining drugs over time. did.

N-
Added 0.25 parts by weight of die 4-rue m-treamide.
Mix, cool and solidify, then crush to form a powder. To 1 part by weight of this powder, 4 parts by weight of SDR drying backing agent (manufactured by Numata Chemical Products Co., Ltd.) was added and mixed, and hand-woven (8 parts by weight)
Apply yellow equivalent to 1.4λg/d to 0X80/71+),
Test Example 2 The efficacy of the insect repellent carpet shown in Example 2 was tested over time to compare the sustainability of the efficacy and confirm the sustained release effect.

That is, 60
Transplant Kenagako 1' Naguni saturated medium 109 onto the back side of a 60t7R tatami overlay, apply adhesive around the overlay, then seal the back side of the tatami with a 60x60 vinyl V sheet.
It was set so that it could only move to the surface of the overlay through the eyes of the overlay.

When the movement of woolly mites was observed on the surface of the overlay, an insect-proof carpet was installed on the overlay, and the temperature was 28℃ and the humidity was 90%.
I placed it indoors. The results were determined by counting the number of woolly mites on nine sheets of black high-quality paper (5 x 5 CM) placed on the carpet at 48:00 + J1a.

A carpet treated with only N,N-diethyl m-1-lamide by the method of Example 2 was used as a comparison.

Table 2 (In Table 2, 100 or more animals are a#) Example 3゜For 1 part by weight of molten hydrogen-processed rosin ester / I / (manufactured by Arakawa Chemical Industries Co., Ltd., trade name Ester Gum H), D
25 parts by weight of DVPo is added and mixed, cooled and assimilated, and then ground to form a powder. A uniform mixture of the most part of this powder and 4 parts by weight of urethane tree-shin emulsion (solid content 20%, manufactured by Nippon Soflan Kako Co., Ltd.) was prepared into 1209
/d high-quality paper after applying 100 g/d equivalent @, 100 g/d
℃, 5 minutes drying test example 3 An efficacy test of the insecticidal sheet shown in Example 3 was carried out to compare the durability of the efficacy and confirm the sustained release effect.

That is, using a pillow containing approximately 1.7 kq of buckwheat moths, eight insecticidal sheets were placed inside the buckwheat moths, and then 60 mesh nylon gusset bags containing 25 adult moths and fishmeal were placed inside the buckwheat moths over time. After sealing the pillow in a polyethylene (80μ) bag, it was placed in a dark place at 25°C for 77 days. The number of deaths was counted 7 days after the installation of adult Kokumemodo, and the mortality rate was determined.

For comparison, a sheet treated with only the same amount of DDVP was used.

Table 3 19-Example 4. PC
Add and mix 0.8 parts by weight of MX, cool and solidify, and then crush to obtain a powder. This powder product 1 division and vinyl acetate 1000 resin Emma V! Red lauan (10 g
0x100x 0.7 IN) on both sides of the board.
Test Example 4 An amount equivalent to 0.091 vol was tested for the efficacy of the mold-proof plywood shown in Example 4 in accordance with the mold resistance test method (JIS z2911), and the durability of the efficacy was compared. The sustained release effect was confirmed.

That is, a potato decoction was attached to the defense plywood, and after air-drying, a mixed suspension of the test 100 spores was sprayed every 1 kg. Af
The culture was carried out for 14 days and the degree of occurrence was investigated. 14 strains are Penicillium ciLrnum
Al'CC9849Rh1zopus nigrica
nsS, N, 82 Chae also omium gl
ol)osum A'rCC6205, Aspergi
llusoryzae IFO4075ノ4 Fi!
'4t child K Lt ta.

In addition, as a comparison, plywood heated to the same amount of PCIN4X was used.

Table 4 Degree of mold generation - No growth of the tree is observed at all.

+ Ura growth is observed within approximately z of the plywood.

The growth of J is approximately h-%1 of plywood.

More than 1 plywood can be seen growing on the plywood.

Example 5° Melted tape-phenol co-car underbody crocodile shield (manufactured by Yasushi Yuki Kogyo Co., Ltd., trade name YS Polyster T+130) 5
After adding and mixing t and max and jt parts, the mixture is cooled, solidified, and crushed to form a dressing.

3 parts by weight of this powder and a linear polyethylene V oxide homopolymer (manufactured by Union Carby F, trade name: Po1y)
ox WSRN-1011 overlap part and water wheel 9; Tobe?
Mixed Y 70 g/#/ and 75 g
////Ta.

501 with clothes? After placing 8 insect repellent sheets manufactured in Example 5 in the middle of the clothes using a storage drawer,
During 1 hour, a 60-mesh nylon bag containing 20 35-day-old burr larvae and two double layers of muslin cloth (approximately 50 bags) was placed, and the number of fatal larvae of larva installation 2 @f71Iiil was counted. The mortality rate was calculated.

(Chest storage condition = 25C dark Ffr).

For comparison, only the same amount of the drug used in Example 5I was applied to high-quality paper, and the same amount was added to the same amount.
A sheet coated with the same amount of i11B yw was used.

As a blank, a drawer containing no drug was used, and larvae were placed between clothes.

The results are shown in Shimoda Table 5.

lively 11□1 the law of nature Table 5 Shows the average value of two series (that's all) Patent applicant: Earth Pharmaceutical Co., Ltd.

Claims (1)

[Scope of Claims] 1. What is the product of mixing the drug and fat replenishing substance A and curing it into a powder/granular material? - A method for sustained release of a drug, which comprises controlling the release of the drug by mixing it with resin B and curing it. 2. The drug is an insecticide, synergist, repellent, insect repellent, j-bicide,
The method according to item 1, wherein the method is one or more of fragrances and deodorants. 3. A sustained release composition for a drug, characterized in that a drug and a resin Ay are mixed, and after hardening, a powder/granular material L/) is mixed with a resin B and then cured. 4. Resin B++: a mixture of a drug and resin A, which is made into a powder or granule after curing; a drug characterized in that the above-mentioned sustained release composition that has been mixed and cured is held on a base material. Sustained release material.