【発明の詳細な説明】本発明は、揮発性物質の蒸気を長期間にわたり安定的に
均一に放出する揮発性物質徐放性製剤に関するものであ
る。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a volatile substance sustained release preparation that stably and uniformly releases volatile substance vapor over a long period of time.
近年、香料、フェロモン、医薬品、農薬等の揮発性物質
を、目的の場所で、長期間安定して継続的に徐々（二揮
散せしめることが、実用的に重要な課題となっている。In recent years, it has become an important practical issue to gradually and steadily dissipate volatile substances such as fragrances, pheromones, pharmaceuticals, and agricultural chemicals at a target location over a long period of time.
上記課題を実現させるための一つの方法が米国特許第３
，５３９，４６５号、同第３，５７７，５１５号に示さ
れており、これらはいずれもマイクロカプセルに揮発性
物質を収納する方法である。しかしこのような方法はマ
イクロカプセル化において収納されるべき揮発性物質を
損失することが多く、また１力月以−ヒにわたる長期間
において均一な徐放性を発揮する製剤を装造することが
困難であるなどの欠点を有する。他方、米国特許第４，
０１７゜０３０号には、中空繊維に揮発性物質を収納す
る方法が揚案されているが、この方法も揮発性の速さが
大きく、また多くの揮発性物質を収納する目的ζ二は不
同きであるという欠点を有する。One way to achieve the above-mentioned problems is as described in U.S. Patent No. 3.
, No. 539,465 and No. 3,577,515, both of which are methods of storing volatile substances in microcapsules. However, such methods often result in the loss of volatile substances that should be contained in microencapsulation, and it is difficult to package preparations that exhibit uniform sustained release over a period of one month or more. It has disadvantages such as being difficult. On the other hand, U.S. Patent No. 4,
No. 017゜030 proposes a method of storing volatile substances in hollow fibers, but this method also has a high rate of volatility, and the purpose of storing a large amount of volatile substances ζ2 is different. It has the disadvantage of being
本発明者らはかかる課題に対し鋭意研究を重ねた結果、
プラスチックス製の中空チューブに１性物質を充填し、
両端をシールすることＣ：より、ある条件下では比較的
多量の揮発性物質を長期に安定的に徐放することか可能
であることを見出し、本発明を完成した。As a result of intensive research into this problem, the present inventors found that
A hollow plastic tube is filled with a monovalent substance,
By sealing both ends (C), the present invention was completed based on the discovery that under certain conditions, it is possible to stably and sustainably release a relatively large amount of volatile substances over a long period of time.
すなわち、本発明は管の内径に基づく断面積Ｓｍ♂と外
周Ａｍとの比Ａ／８が２〜２Ｑｍｍ−’である高分子材
料製の細管に、揮発性物質を封入してなる揮発性物質徐
放性製剤に関するものである。That is, the present invention provides a volatile substance which is obtained by sealing a volatile substance in a thin tube made of a polymeric material in which the ratio A/8 of the cross-sectional area Sm♂ and the outer circumference Am based on the inner diameter of the tube is 2 to 2Qmm-'. This invention relates to sustained release preparations.
本発明の目的に特シー望ましい細管は、平均内径０、５
％ ４ ｙｎｘ、平均外周２〜２０ ｗｒ、ｍ、長さ
５０〜１０００ｍを有し、かつ前記Ａ／８の比が４〜８
ｍｘ−’である細管であり、このような条件を満足する
細管を使用することにより極めてすぐれた均一な徐放性
を有する製剤を得ることができる。Particularly desirable capillary tubes for the purposes of this invention have an average inner diameter of 0.5
% 4 ynx, average circumference 2-20 wr, m, length 50-1000 m, and the ratio of A/8 is 4-8
mx-', and by using a capillary that satisfies such conditions, it is possible to obtain a preparation with extremely excellent uniform sustained release properties.
細管を作るための高分子材料としては、ポリエチレン、
ポリプロピレン、酢ビ−エチレンコポリマー、塩化ビニ
ル樹脂、セルローズアセテート、ビニロンなどが例示さ
れるが、たとえば揮発性物質がアルコール系化合物、カ
ルボン酸系化合物などの場合ｌ二はビニロンあるいはセ
ルローズアセテート製の細管を、また揮発性物質が芳香
族系化合物、エステル系化合物、ハイドロカーボン系化
合物などの場合にはポリエチレンあるいは酢ビーエチレ
ンコポリマー特細管を使用することが望ましい。Examples of polymer materials for making thin tubes include polyethylene,
Examples include polypropylene, vinyl acetate-ethylene copolymer, vinyl chloride resin, cellulose acetate, and vinylon. For example, when the volatile substance is an alcohol compound or a carboxylic acid compound, a thin tube made of vinylon or cellulose acetate is used. Furthermore, when the volatile substance is an aromatic compound, an ester compound, a hydrocarbon compound, etc., it is desirable to use a polyethylene or acetic acid-vinyl ethylene copolymer special capillary tube.
細管の断面形状は円形、正方形、星形等いかなる形状で
もよいが、工業的には円形、だ円形、波形、星形が使用
される。比較的大きい細管の場合には波形または星形等
の凸凹形状であることが好ましい。The cross-sectional shape of the capillary may be any shape such as circular, square, or star-shaped, but circular, oval, wavy, or star-shaped are used industrially. In the case of a relatively large capillary, it is preferable that the tube has an uneven shape such as a wave shape or a star shape.
他方、細管に金属線を添設することもよく、これによれ
ば細管の長手方向の形状をいろいろの形に保つことが可
能であり、ラセン状、カタツムリ状等任意の形状（二す
ることができる。On the other hand, it is also possible to attach a metal wire to the thin tube, and with this, it is possible to maintain the shape of the thin tube in the longitudinal direction in various shapes, such as spiral shape, snail shape, etc. can.
本発明においては、前記したとおり、細管の内径断面積
Ｓ ｍＪと外周Ａｍｍとの比Ａ／Ｓが２〜２〇１朋 （好ましくは４〜ｓＨ）であることが必須とされる
。このＡ／Ｓ比が２以下になると収納された揮発性物質
の放出速度が小さくなり丁ぎて好ましくなく、しかも収
納された川の約半晴が放出されたのちはこの放出速度が
一段と小さくなり、当初の目的を達成し得なくなる。−
万Ａ／Ｓ比が２０以上になると、該放出速度が速くなり
すぎ、しかもその放出速度は時間の経過にしたがって急
激に低下してしまう。すなわち、この場合は揮発性物質
と細管を作る原料である高分子材料とを混合、混練した
ものにおける揮発性物質の放出カーブと同じようになり
、目的とする均一な放出速度を与えられない。In the present invention, as described above, it is essential that the ratio A/S of the inner diameter cross-sectional area S mJ of the thin tube to the outer circumference A mm is 2 to 201 mm (preferably 4 to sH). When this A/S ratio becomes less than 2, the release rate of the stored volatile substances decreases, which is quite undesirable, and furthermore, after about half of the stored volatile substances are released, this release rate becomes even smaller. , it becomes impossible to achieve the original purpose. −
When the A/S ratio exceeds 20, the release rate becomes too high, and moreover, the release rate rapidly decreases over time. That is, in this case, the release curve of the volatile substance is the same as that in a mixture and kneading of the volatile substance and the polymeric material that is the raw material for making the capillary, and the desired uniform release rate cannot be achieved.
細管の平均内径は、前記したように、０．５〜４」特に
は０．８〜３ｍｍであることが望ましい。この内径が０
．５朋以下では容量が小さいばかりでなく、初期速昭が
大きく均一な放出は得られず、−万５朋以上では放出速
１更がおそいだけでなく、特に後半には著しく放出速度
が低下し本発明の目的を達することはできない。As mentioned above, the average inner diameter of the capillary tube is preferably 0.5 to 4 mm, particularly 0.8 to 3 mm. This inner diameter is 0
．． If it is less than 5,000, the capacity is not only small, but the initial rate is large and uniform release cannot be obtained, and if it is more than -5,000, not only is the discharge rate slow to increase, but the release rate decreases significantly, especially in the latter half. The purpose of the invention cannot be achieved.
本発明の他の利点は透明性にすぐれたポリエチレン製チ
ューブ等を使用することにより内容物の放出速度および
残量を容易に確認できることである。特に内容物をあら
かじめ青色しておけば該放出速度および残量の確認が一
段と容易となる。Another advantage of the present invention is that by using a polyethylene tube with excellent transparency, the release rate and remaining amount of the contents can be easily confirmed. In particular, if the contents are colored blue in advance, it will be easier to confirm the release rate and remaining amount.
なお、揮発性物質が紫外線により分解され易いものであ
る場合には、細管を作る原料である高分子材料中に紫外
線防止剤、染料または顔料を漏入するとか、あるいは揮
発性物質にも酸化防止剤、安定剤等を含有させることが
よい。In addition, if the volatile substance is easily decomposed by ultraviolet rays, UV inhibitors, dyes, or pigments may be leaked into the polymeric material that is the raw material for making the tubes, or the volatile substance may also be treated with oxidation inhibitors. It is preferable to contain agents, stabilizers, etc.
揮発性物質としては、ダイアジノン、ジメチルジクロル
ビニルホスフェート等の揮発性農薬、香料、医薬品、各
種生理活性揮発性物質を使用することが可能である。As the volatile substance, volatile agricultural chemicals such as diazinon and dimethyldichlorovinyl phosphate, fragrances, pharmaceuticals, and various physiologically active volatile substances can be used.
つぎに、発明の内容を実施例で説明する。Next, the content of the invention will be explained with examples.
実施例１゜内径０．９朋、外径の異なる長さ４０確の高密度ポリエ
チレンチューブＡ、ＢおよびＣを作り（下記参照）、こ
れらにンスヘキセニルチグレート（揮発性物質）１８０
■を封入し、４０℃の条件下で該揮発性物質の放出速度
を測定した。Example 1 High-density polyethylene tubes A, B, and C of 40 lengths with an inner diameter of 0.9 mm and different outer diameters were made (see below), and sthexenyl tiglate (volatile substance) 180 mm was added to these tubes.
(2) was sealed, and the release rate of the volatile substance was measured under conditions of 40°C.
結果は第１図に示すとおりであった。これから判るよう
にチューブＢおよびＣは艮好な放出速度を示したが、チ
ューブＡは放出速度が急激であり、本発明の目的には適
さない。The results were as shown in Figure 1. As can be seen, tubes B and C exhibited excellent release rates, whereas tube A had a rapid release rate and was not suitable for the purposes of the present invention.
実施例２゜断面積（Ｓ）約７−１長さ２ｏＣＩｒＬ、断面形状が第
２図（イ）、ｔｏ＋、（ハ）およびに）に示す形状を有
するチューブ（イ）、（ロ）、（／樽、に）断面形状チューブ（イ）・・・・・・・・・・・・・・・・・・
・・・第２図イ）〃 呻）―・…用６■……用
〃（Ｃ１チューブ（ハ）叩・・・・・明・・曲・・・・
・第２図（ハ）〃 に）、、、１．１．１．、、、、
．０１８．．９０．１．〃 に）を酸ピーエチレンコ
ポリマーより製造し、これらにＺ−１１−トリデセニル
アセテート１゜１ｇを封入し、２０℃の条件下で放出速
度を測定した。Example 2 Tubes (A), (B), (B) having a cross-sectional area (S) of about 7-1, a length of 2oCIrL, and a cross-sectional shape as shown in FIGS. /barrel, ni) Cross-sectional tube (a)・・・・・・・・・・・・・・・・・・
...Fig. 2 A) 〃 Groan) --- for... 6 ■... for...
〃(C1 tube (c) hit...light...song...
・Figure 2 (c)〃), 1.1.1. ,,,,
．． 018. ．． 90.1. (2) were prepared from acid pyethylene copolymer, 1.1 g of Z-11-tridecenyl acetate was encapsulated therein, and the release rate was measured at 20°C.
結果は第３図に示すとおりであり、特にチューブ（／場
およびに）は艮好な放出速度を示した。The results are as shown in FIG. 3, and in particular the tube (/ba and ni) showed an excellent release rate.
実施例３゜内径０．９ ｍｍ、外径１．５ｗＲ，長さ２２ｃｒｎの
低密度ポリエチｖンチューブ（Ａ／Ｓ＝７．４＋ｕ−’
）にダイアジノン９８■を封入し、３５℃の条件下で放
出速度を測定した。結果は弔４図に示すとおりであり、
良好であった。Example 3 Low-density polyethylene tube (A/S=7.4+u-') with inner diameter of 0.9 mm, outer diameter of 1.5 wR, and length of 22 crn.
) was encapsulated with 98 µm of diazinon, and the release rate was measured at 35°C. The results are shown in Figure 4.
It was good.
第１図、第３図および第４図はそれぞれ実施例１、実施
例２および実施例３の結果を示したものである。第２図
（イ）〜に）は実施例２におけるチューブ（イ）、吋１
、（ハ）およびに）のそれぞれ断面形状を示したもので
ある。特許出願人 信越化学工業株式会社□口数□日 数第２図（ロ）Ｃ＝＝フ第４図一′ＥＪ 数特許庁長官 若 杉 和 夫 殿１、事件の表示昭和５８年特許願第８８９７３号２、発明の名称揮発性物質徐放性製剤３、補正をする者事件との関係 特許出願人名称 （２０６） 信越化学工業株式会社４、代理人５、補正の対象図 面６、補正の内容第１図□ヨ救第３回□日 数FIG. 1, FIG. 3, and FIG. 4 show the results of Example 1, Example 2, and Example 3, respectively. Figure 2 (a) to 2) show the tube (a) in Example 2,
, (C) and (B) respectively. Patent Applicant: Shin-Etsu Chemical Co., Ltd. □ Number of Parts □ Number of Days Figure 2 (B) C==F Figure 4 1' EJ Commissioner of the Patent Office Kazuo Wakasugi 1, Indication of Case 1988 Patent Application No. 88973 No. 2, Name of the invention Volatile substance sustained release preparation 3, Relationship with the case of the person making the amendment Name of the patent applicant (206) Shin-Etsu Chemical Co., Ltd. 4, Agent 5, Drawings to be amended 6, Amendment Contents Figure 1 □ Yo Salvation 3rd □ Number of days
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP58088973AJPS59216802A (en) | 1983-05-20 | 1983-05-20 | Slow-releasing preparation of volatile substance |
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP58088973AJPS59216802A (en) | 1983-05-20 | 1983-05-20 | Slow-releasing preparation of volatile substance |
| Publication Number | Publication Date |
|---|---|
| JPS59216802Atrue JPS59216802A (en) | 1984-12-06 |
| JPS629561B2 JPS629561B2 (en) | 1987-02-28 |
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP58088973AGrantedJPS59216802A (en) | 1983-05-20 | 1983-05-20 | Slow-releasing preparation of volatile substance |
| Country | Link |
|---|---|
| JP (1) | JPS59216802A (en) |
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62223101A (en)* | 1986-03-25 | 1987-10-01 | Shin Etsu Chem Co Ltd | Slowly-releasing pheromone dispenser |
| JPS62258301A (en)* | 1986-04-23 | 1987-11-10 | Shin Etsu Chem Co Ltd | Sustained release pheromone dispenser |
| US6663913B2 (en) | 1996-12-20 | 2003-12-16 | Scientec Research Pty. Ltd. | Method of coating a bioactive substance |
| WO2013084983A1 (en)* | 2011-12-09 | 2013-06-13 | 信越化学工業株式会社 | Slow-release formulation containing gel composition for use on pests |
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102596097B (en) | 2009-06-03 | 2015-05-20 | 弗赛特实验室有限责任公司 | an eye insert |
| CN103917202B (en) | 2011-09-14 | 2016-06-29 | 弗赛特影像5股份有限公司 | Eye insert devices and methods |
| AU2013334169B2 (en) | 2012-10-26 | 2018-03-29 | Forsight Vision5, Inc. | Ophthalmic system for sustained release of drug to eye |
| EP3283004A4 (en) | 2015-04-13 | 2018-12-05 | Forsight Vision5, Inc. | Ocular insert composition of semi-crystalline or crystalline pharmaceutically active agent |
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62223101A (en)* | 1986-03-25 | 1987-10-01 | Shin Etsu Chem Co Ltd | Slowly-releasing pheromone dispenser |
| JPS62258301A (en)* | 1986-04-23 | 1987-11-10 | Shin Etsu Chem Co Ltd | Sustained release pheromone dispenser |
| US6663913B2 (en) | 1996-12-20 | 2003-12-16 | Scientec Research Pty. Ltd. | Method of coating a bioactive substance |
| WO2013084983A1 (en)* | 2011-12-09 | 2013-06-13 | 信越化学工業株式会社 | Slow-release formulation containing gel composition for use on pests |
| WO2013084984A1 (en)* | 2011-12-09 | 2013-06-13 | 信越化学工業株式会社 | Slow-release formulation containing gel composition for use on pests |
| US9549546B2 (en) | 2011-12-09 | 2017-01-24 | Shin-Etsu Chemical Co., Ltd. | Sustained release preparation comprising insect pest-targeting gel composition |
| Publication number | Publication date |
|---|---|
| JPS629561B2 (en) | 1987-02-28 |
| Publication | Publication Date | Title |
|---|---|---|
| ES2299792T3 (en) | BIODEGRADABLE SUSTAINED RELEASE PEST CONTROL AGENT. | |
| US5614217A (en) | Capsule shell formulation to produce brittle capsules | |
| FI83389C (en) | BAERARSYSTEM FOER SAMTIDIG FRIGOERING AV TVAO ELLER FLERA AKTIVA AEMNEN. | |
| DE2908794A1 (en) | PROCESS FOR PRODUCING A POLYMER PREPARATION CONTAINING A PHYSIOLOGICALLY ACTIVE SUBSTANCE | |
| JPS59216802A (en) | Slow-releasing preparation of volatile substance | |
| JPS58194969A (en) | Composite body for releasing effective substance long time | |
| KR850008094A (en) | Sustained release drug delivery device | |
| EP0464023A4 (en) | Realease assist microcapsules | |
| JPH0741402A (en) | Drug sustained-release resin molding and method for producing the same | |
| JP2915284B2 (en) | Sustained release formulation | |
| JPH0257044B2 (en) | ||
| JPH04295418A (en) | Synthesized product controlled in release of component | |
| JPH0263017B2 (en) | ||
| JPH0361402B2 (en) | ||
| JPS6351121B2 (en) | ||
| AU2004267046B2 (en) | Chlorine dioxide releasing composite article | |
| JPS62258301A (en) | Sustained release pheromone dispenser | |
| JP2957788B2 (en) | Sustained release pheromone preparation | |
| JP3243866B2 (en) | Granules of volatile substances | |
| JPH0246374B2 (en) | ||
| WO2001031999A1 (en) | Improving the long-term diffusion rate of controlled release herbicides in thin-walled drip irrigation lines | |
| JPS6113521Y2 (en) | ||
| JPH1017407A (en) | Biodegradable pheromone dispenser | |
| JPH02174628A (en) | Solution absorbing core and insecticide | |
| JPS58163724A (en) | Hollow fiber filled with latent heat-storing agent |