TWI241160B - Novel formulation for counteracting an ethylene response in plants, preparation process thereof, and method using the same - Google Patents

Novel formulation for counteracting an ethylene response in plants, preparation process thereof, and method using the same Download PDF

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TWI241160B
TWI241160B TW89125778A TW89125778A TWI241160B TW I241160 B TWI241160 B TW I241160B TW 89125778 A TW89125778 A TW 89125778A TW 89125778 A TW89125778 A TW 89125778A TW I241160 B TWI241160 B TW I241160B
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acid
plant
lozenge
item
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Tian-Hung Jang
Ren-De Yang
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Lytone Enterprise Inc
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Abstract

Disclosed is a tablet dosage for inhibiting ethylene response in a plant containing a blocking agent, which has ethylene binding site inhibition activity to plants, and an effervescent ingredient in admixture with one or more acceptable excipients. A process of preparing the tablet dosage and a method for inhibiting ethylene response in plants are also disclosed therein.

Description

1241160 經濟部智慧財產局員工消費合作社印製 A7 五、發明說明(1 發明範f 本1月係關糸#新穎的錠劑調配物,其係用於調節植 物t理,特定石之阻礙乙缔反應,其中包含阻斷劑與發泡 成刀和種或夕種可接受的賦形劑混合,並有關製造此 調配物之方法及藉由施用本發明調配物來抑制各種乙烯反 應之方法。 發明背景 在植物生長反應中,植物荷爾蒙扮演著重要角色。乙烯 爲二種對植物生長,發育,衰老有很多重要影響之生長荷 爾蒙1乙烯最重要的影響包括和果實成熟,花朵衰退及葉 子脱落有關之過程。新鮮產品之商業價値往往因過量之乙 烯氣體而降低,因其會加速果實之成熟,花朵之衰退及葉 子之過早脱落。 由於乙烯謗發的問題,大量的研究集中於預防或減低其 對於植物影響的方法。減緩乙缔影響最有效方法之一爲利 用阻斷植物内接收乙烯訊號之受器之原理。針對此目的, 其中最爲人熟知的化合物之一爲硫代硫酸銀(” STS”)。STS 在植物細胞内乙烯結合位置提供一種不可逆之阻斷,因而 予員防或減低乙%對植物的有害影響。儘管s τ s非常有效, 但由於銀是一種對大部分活生物體有毒的重金屬,所以會 造成嚴重的廢棄物處理問題。 席斯勒(Sisler)等人之 Plant Growth Reg. 9,1587-164,1990 揭示環戊一晞爲一種有效之植物乙晞結合位置阻斷劑。美 國專利案弟5,1〇〇,4625虎也揭不一種有效之重氮基環戊- 烯。然而,環戊二烯與重氮基環戊二烯不穩定且帶有強烈 臭味。 -4- 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) ^ AW Μ--------^--------- (請先閱讀背面之注意事項再填寫本頁) 1241160 A7 -------_______ 五、發明說明(2 ) 美國專利案號第5,5 1 8,988揭示了以氣態環丙烯及其衍生 物,如··甲基環丙晞作爲乙烯結合位置阻斷劑的用途。甲 基環丙晞在十億分之幾範圍内的極低劑量下便可生效,因 而可如同使用在花舟上安全地用於水果和蔬菜。甲基環丙 晞很各易進行氧化反應及其他反應,所以非常不穩定。最 近的美國專利案第6,017,849號中,以載體將甲基環丙烯氣 體封裝。如^環糊精之載體可用來穩定環丙烯氣體之反^ 性及不穩足性,因而提供了一個貯存、運送、施用或輸送 (delivering)此氣體至植物之方便且安全的方法。 商業用甲基環丙烯粉末產品通常包含〇 43%甲基環丙烯 乳體成分。粉末與水或緩衝液混合後會釋出此氣體。封閉 空,中每立方公尺〇.5公克粉末之施用率可達到成9〇〇 之最終甲基環丙烯濃度。如果於此濃度下曝露至少4小時 作爲收穫後處理,將可顯著延長花卉,水果和蔬菜的耐儲 時間。 粉末產品在使用上遠較氣態產品來得方便,但對使用者 仍不利。其依然具有這個領域上使用粉末的缺點,例如: 極谷易過早受潮及測量失誤。此外,通常推薦以手工混合 大量粉末,如:燻蒸大空間時需要每批次使用1〇克以上的 里。在搶閉空間内,由於工作人員於混合過程中進出密閉 工門也斗會^成其中甲基環丙缔之量比原來預期的濃度 減少,因而降低了甲基環丙烯的有利效益。 本發明提供一種減緩混合粉末型時相關缺點之發泡式錠 劑調配物。 _5 - 本紙張尺度適用中國國家標準(CNS)A4規格(21〇 x 297公釐) (請先閱讀背面之注意事項再填寫本頁) 訂---------線‘ 經濟部智慧財產局員工消費合作社印製。 12411601241160 Printed A7 by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. 5. Description of the invention (1 Invention scope f this January is Guan 糸 #novel lozenge preparations, which are used to regulate plant management, and the specific stone hinders the association. A reaction comprising a blocking agent mixed with a foaming knife and an acceptable excipient, and a method for manufacturing the formulation and a method for inhibiting various ethylene reactions by applying the formulation of the present invention. Background Phytohormones play an important role in plant growth responses. Ethylene is two types of growth hormones that have many important effects on plant growth, development, and senescence. The most important effects of ethylene are related to fruit maturity, flower decline, and leaf shedding. Process. The commercial price of fresh products is often reduced by excessive ethylene gas, which accelerates fruit maturation, flower decline and premature shedding. Due to the problem of ethylene slurries, a large amount of research has focused on preventing or reducing its Methods for plant effects. One of the most effective ways to mitigate the effects of ethylene is to block the reception of ethylene signals in plants. For this purpose, one of the most well-known compounds is silver thiosulfate ("STS"). STS provides an irreversible blockade of ethylene binding sites in plant cells, thus preventing or reducing B % Harmful effects on plants. Although s τ s is very effective, silver is a heavy metal that is toxic to most living organisms, which can cause serious waste disposal problems. Plant Growth by Sisler et al. Reg. 9,1587-164,1990 revealed that cyclopentaamidine is an effective plant acetamidine binding site blocker. US Patent No. 5,10,4625 Tiger also did not disclose an effective diazocyclopentane -Ethylene. However, cyclopentadiene and diazocyclopentadiene are unstable and have a strong odor. -4- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ^ AW Μ -------- ^ --------- (Please read the notes on the back before filling this page) 1241160 A7 -------_______ V. Description of the invention (2) United States Patent No. 5,5 1 8,988 discloses the use of gaseous cyclopropene and its derivatives, such as methylcyclopropane It is an ethylene binding site blocker. Methylcyclopropane works at very low doses in the parts per billion range, so it can be safely used for fruits and vegetables as it is used on flower boats. Methyl Cyclopropane easily undergoes oxidation and other reactions, so it is very unstable. In the recent US Patent No. 6,017,849, methylcyclopropene gas is encapsulated by a carrier. A carrier such as cyclodextrin can be used to stabilize cyclopropene The reversibility and instability of gas provide a convenient and safe method for storing, transporting, applying or delivering this gas to plants. Commercial methylcyclopropene powder products typically contain 43% methylcyclopropene milk ingredients. This powder is released when the powder is mixed with water or buffer. In the closed space, the application rate of 0.5 g powder per cubic meter can reach a final methylcyclopropene concentration of 900. Exposure to this concentration for at least 4 hours as a post-harvest treatment will significantly extend the shelf life of flowers, fruits and vegetables. Powder products are far more convenient to use than gaseous products, but they are still disadvantageous to users. It still has the disadvantages of using powder in this field, for example: Jigu is susceptible to premature moisture and measurement errors. In addition, it is generally recommended to mix large amounts of powder by hand. For example, when fumigating a large space, more than 10 grams of mile per batch should be used. In the evacuation space, as the staff enters and exits the closed gate during the mixing process, the amount of methylcyclopropane is reduced compared to the original expected concentration, thereby reducing the beneficial benefits of methylcyclopropene. The present invention provides a foamed tablet formulation that alleviates the related disadvantages when mixing powder types. _5-This paper size is applicable to China National Standard (CNS) A4 specification (21 × 297 mm) (Please read the precautions on the back before filling this page) Order --------- Line 'Ministry of Economy Wisdom Printed by the Consumer Cooperative of the Property Bureau. 1241160

五、發明說明(3 經濟部智慧財產局員工消費合作社印製 發明概i 所以本發明之目的爲提供一種抑制植物乙晞反應之發泡 卜其包含-種阻斷植物乙晞結合位置之藥劑、及—種 發泡成分與-種或多種可接受載體和/或賦形劑混合。 本發明另-目的爲提供製備本發明新穎錠劑之方法。 本發明更進一步之目的爲提供抑制植物乙烯反應之方 法。 乃 本發明詳纟 本發明提供-種新賴劑調配物,其包含—種阻斷植物 乙晞結合位置藥劑和-種發泡成分,肖—種或多種可接受 載體和/或賦形劑混合。 根據本發明,阻斷植物乙晞結合位置的藥劑包括所有慣 用於抑制植物乙晞反應的化合物如,不限於,環丙缔 1-甲基-環丙晞’ 3,3_二甲基環丙燒’亞甲基環丙燒,重氮 環己二埽,反-環辛晞,順-環辛烯,及2,5-原冰片二烯: 相關的先前技藝,如美國專利案第3,879,1 88, 5,1〇〇,462, 5,5 1 8,988,及 6,017,849 號,與席斯勒(Sisler)等人之 ρι_V. Description of the invention (3 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs, the invention is printed. Therefore, the purpose of the present invention is to provide a foam that inhibits the reaction of the plant ’s ethyl acetate. And a foaming ingredient is mixed with one or more acceptable carriers and / or excipients. Another object of the present invention is to provide a method for preparing the novel lozenges of the present invention. A further object of the present invention is to provide inhibition of ethylene reaction in plants. The method is a detailed description of the present invention. The present invention provides a novel lysine formulation comprising a plant blocking agent and a foaming ingredient, and one or more acceptable carriers and / or additives. According to the present invention, the agent that blocks the binding site of acetamidine in plants includes all compounds conventionally used to inhibit the response of acetamidine in plants such as, without limitation, cyclopropyl 1-methyl-cyclopropylamidine '3,3_ Methylcyclopropane, methylenecyclopropane, diazocyclohexane, trans-cyclooctane, cis-cyclooctene, and 2,5-orbornadiene: related prior art such as US patents Case No. 3,879,1 88, 5,10,462,5,5 1, 8,988, and 6,017,849, ρι_ with Sisler and others

Growth Reg. 9, 157-164, 199〇已以提及之方式完全併入本 Λ月曰中。阻|g斤植物乙晞結合位置之較佳藥劑爲1 _甲基環 丙晞。 根據本發明,”植物”一詞除了指木本植物外,還包含田 間作物,盆栽,切花,採收之水果,蔬菜及觀賞植物。 接文抑制乙晞反應之本發明錠劑處理之植物必需接受不 具植物毒性的量處理。此植物毒性量不僅隨植物,並且隨 -6- 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) ------*------裝--------訂---------線 111^· (請先閱讀背面之注音?事項再填寫本頁) A7Growth Reg. 9, 157-164, 199〇 has been fully incorporated by reference in this article. The preferred medicament for hindering the binding site of the plant's ethyl acetate is 1-methylcyclopropane. According to the present invention, the term "plant" includes, in addition to woody plants, field crops, pot plants, cut flowers, harvested fruits, vegetables, and ornamental plants. The plants treated with the lozenges of the present invention that inhibit the acetamidine response must be treated in amounts that are not phytotoxic. This phytotoxicity varies not only with plants, but also with -6- This paper size is applicable to Chinese National Standard (CNS) A4 specifications (210 X 297 mm) ------ * ------ packing ---- ---- Order --------- line 111 ^ · (Please read the note on the back? Matters before filling out this page) A7

1241160 五、發明說明(4 ) 培育植物品種而改變。 根據本毛日月,可如美國專利案第ms,㈣及3,8乃,⑻號 中所揭示,預防許多乙晞反應。乙缔反應可由外因性或内 因性乙烯源開始。乙埽反應包括,例如,花卉,水果及蔬 采之成熟和/或衰老;葉子,花朵和果實的脱落;觀賞植 物如皿栽’切;f匕’灌木,和休眠幼苗之成熟及/或壽命之 縮短;抑制-些植物㈣豆之生長;及刺激—些植物如稻 之生長。 、根據本發明,可接受處理以抑制衰老植物包括綠色葉菜 噙萵宦(e.g·5 Lactuea sativa),蔽菜(Spinaca oleracea)及 甘監采(Brassica oleracea);各種根莖類,如馬鈴薯 (Solammi tuberosum),胡蘿蔔(Daucus);球基類,如洋蔥 (Allium SP·) ’ 香料植物’如羅勒(Ocimum basilicum),牛至 (Origamim vulgare)及蒔蘿(Anethum grave〇lens);及大豆 (Glycine max),利馬豆(Phase〇lus nmensis),豌豆(Lathyrus sp.) ’ 玉蜀黍(Zea mays),球花甘藍(Brassica oleracea italica),花椰菜(Brassica oleracea botrytis)及石刁柏 (Asparagus officinalis)。 根據本發明,可接受處理以抑制其成熟的水果包括蕃茄 (Lycopersicon esculentum),蘋果(Malus domes tica),香蕉 (Musa sapientum),洋梨(Pyrus communis),木瓜(Carica papya),芒果(Mangifera indica),才兆子(Prunus persica),杏 子(Prunus armeniaca),油才兆(Prunus persica nectarina),柳 燈(Citrus sp.),擰檬(Citrus limonia),莱姆(Citrus 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) "--------------訂---------線 (請先閱讀背面之注意事項再填寫本頁) 經濟部智慧財產局員工消費合作社印製 1241160 經濟部智慧財產局員工消費合作社印製 A7 B7 五、發明說明(5 ) aurantifolia),葡萄柚(Citrus paradisi),橘子(chrus n〇biHs deliciosa),奇異果(Actinidia. Chinenus),甜瓜如羅馬甜瓜 (C· cantalupensis)及香瓜(C· mel〇),鳳梨(Αγ_〇 c ⑽ _s), 柿子((Di〇Spyros sp·),及木莓(如,Fragaria 或 Rubus ursinus),藍莓(Vacciniumsp·),青豆(phase〇lusvulgaris), 甜瓜屬之成員如黃瓜(C· sativus)及鱷梨(Persea Americana) 〇 根據本發明,可接受處理以抑制衰老和/或延長開花期 及外觀(如延期枯萎)之觀賞植物包含盆栽觀賞植物及切 花。可接受本發明方法處理之盆栽觀賞植物及切花包括杜 鵑花(Rhododendron spp.),繡球花屬植物(Macr〇phylla hydrangea) ’ 木槿(Hibiscus rosasanensis),金魚讓 (Antirrhinum sp_),聖誕紅(Euphorbia pulcherima),仙人掌 (e.g·,Cactaceae schlumbergera truncata),秋海棠(Begonia sp.) ’ 玫瑰(Rosa sp.),鬱金香(Tulipa sp·),黃水仙 (Narcissus sp.),牽牛花(Petunia hybrida),康乃馨(Dianthus caryophyllus),百合(如 Lilium sp.),劍蘭(Gladiolus sp.), 百合水仙(Alstroemaria brasiliensis),秋牡丹(如 Anemone bland),摟斗菜(Aquilegia sp.),惚木屬(如自木),紫莞屬植 物(如 Aster carolinianus),九重(Bougainvillea sp.),山茶 (Camellia sp·),風铃草(Campanula sp.),難冠花(Celosia sp·),扁柏(Chamaecyparis sp·),菊花(Chrysanthemum sp.), 鐵線蓮(Clematis sp·),櫻草(Cyclamen sp.),小蒼蘭(e g, Freesia refracta),及蘭科之蘭花。 -8- 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) --------------------訂---------線 (請先閱讀背面之注意事項再填寫本頁) 經濟部智慧財產局員工消費合作社印製 1241160 A7 五、發明說明(6 ) 根據本發明,可接受處理以抑制葉,花和果實脱除之植 物包括棉花(G〇SSyPium spp.),蘋果,洋梨,櫻桃(prunus aV1Um),大胡桃(Carva illinoensis),葡萄(Vitis vinifera), 橄欖(如,〇lea europaea),咖啡(c〇fffea arabica),菜豆 (Phase〇lus vulgaris)和垂枝無花果樹(爾咖叫fig)(Ficus benjamma)及如包括蘋果之許多果樹,觀賞植物,灌木和 樹幼苗之休眠幼苗。 此外’根據本發明,可接受處理以抑制葉脱落之灌木包 括水蠟樹(Ligustrum sp·),石楠(photina sp.),冬青(llex sp·) ’水龍骨科的蕨類,鵝掌柴(Schefflera sp ),萬年青 (Aglaonema sp ),枸子(c〇t〇neaster sp ),伏牛花(Berberris sp.) ’楊梅(Myrica sp.),六道木(Abelia sp ),阿拉伯樹膠 (Acacia sp·),及鳳梨科的鳳梨(Br〇meliades)。 根據本發明,發泡成分用於控制阻斷植物乙烯結合位置 樂劑在水溶液中分解的速度。任何可引起發泡效力之反應 混合物皆可在本發明中使用。本發明之發泡成分較佳之具 體實施例包括在常溫下爲固體之溫和鹼性化合物和溫和酸 性化合物。溫和鹼性化合物在溶劑中與溫和酸性化合物反 應產生二氧化碳氣體。 根據本發明,溫和鹼性化合物與溫和酸性化合物之比例 爲約9: 1至約1: 1。此比例以約4: 1爲佳。 溫和鹼性化合物之較佳具體實施例爲NaHC〇3,KHC〇3,1241160 V. Description of the invention (4) Changed by cultivating plant varieties. According to the present sun and the moon, many acetamidine reactions can be prevented as disclosed in US Patent Case Nos. Ms, ㈣ and 3,8, and 乃. The ethylene reaction can begin with an exogenous or endogenous ethylene source. Acetidine reactions include, for example, maturation and / or senescence of flowers, fruits, and vegetables; shedding of leaves, flowers, and fruits; ornamental plants such as 'cuts'; f. Shrubs; and maturity of seedlings and / or longevity Shortening; inhibiting the growth of some plants of cowpea; and stimulating the growth of some plants such as rice. According to the present invention, plants that can be treated to inhibit senescence include green leafy lettuce (eg · 5 Lactuea sativa), spinaca oleracea and Brassica oleracea; various rhizomes, such as potatoes (Solammi tuberosum), carrots (Daucus); ball bases, such as onions (Allium SP ·) 'spice plants' such as basil (Ocimum basilicum), oregami (vulgare) and dill (Anethum grave〇lens); and soybeans (Glycine max), Lima beans (Phase olis nmensis), peas (Lathyrus sp.) 'maize (Zea mays), broccoli (Brassica oleracea italica), broccoli (Brassica oleracea botrytis), and Asparagus officinalis. Fruits that can be treated to inhibit their maturity according to the present invention include tomatoes (Lycopersicon esculentum), apples (Malus domes tica), bananas (Musa sapientum), pears (Pyrus communis), papaya (Carica papya), and mangifera indica , Prunus persica, Apricot (Prunus armeniaca), Prunus persica nectarina, Citrus sp., Citrus limonia, Citrus (CNS) A4 specification (210 X 297 mm) " -------------- Order --------- line (Please read the precautions on the back before filling in this Page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 1241160 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Invention Description (5) aurantifolia), Citrus paradisi, Orange (chrus n〇biHs deliciosa) , Kiwi (Actinidia. Chinenus), Melons such as Roman Melon (C. cantalupensis) and Muskmelon (C. mel〇), Pineapple (Αγ_〇c ⑽ s), Persimmon ((Di〇Spyros sp.), And Raspberry (E.g. Fragaria or Rubus ursinu s), blueberry (Vacciniumsp ·), green beans (phase 0lusvulgaris), members of the genus Melon such as cucumber (C. sativus) and avocado (Persea Americana) 〇 according to the present invention, can be treated to inhibit senescence and / or prolong flowering The ornamental plants of the period and appearance (such as delayed wilting) include potted ornamental plants and cut flowers. Potted ornamental plants and cut flowers that can be treated by the method of the present invention include rhododendron spp., Macrophylla hydrangea ' Hibiscus rosasanensis, Antirrhinum sp_, Christmas Red (Euphorbia pulcherima), Cactus (eg ·, Cactaceae schlumbergera truncata), Begonia (Begonia sp.) 'Rose (Rosa sp.), Tulip (Tulipa sp ·) , Narcissus sp., Petunia hybrida, Dianthus caryophyllus, Lily (such as Lilium sp.), Gladiolus sp., Lily narcissus (Alstroemaria brasiliensis), Autumn peony (such as Anemone bland ), Aquilegia sp., Alnus (such as Zimu), purple genus (such as Aster carolinianus) Bougainvillea sp., Camellia sp., Campanula sp., Celosia sp., Chamaecyparis sp., Chrysanthemum sp., Clematis Clematis sp.), Primrose (Cyclamen sp.), Freesia (eg, Freesia refracta), and orchids of the orchid family. -8- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) -------------------- Order ------- --- line (please read the notes on the back before filling this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1241160 A7 V. Description of the invention (6) According to the present invention, it is acceptable to treat the leaves, flowers and fruits Except plants include cotton (GOSSyPium spp.), Apples, pears, cherries (prunus aV1Um), giant walnut (Carva illinoensis), grapes (Vitis vinifera), olives (e.g., olea europaea), coffee (cofffea) arabica), Phaseolus vulgaris, and fig tree (Ficus benjamma) and dormant seedlings of many fruit trees including apples, ornamentals, shrubs and tree seedlings. In addition, according to the present invention, shrubs that can be treated to inhibit leaf fall include Ligustrum sp., Photina sp., Holly (llex sp.). Ferns of the Orthodoxaceae, Schefflera (Schefflera sp), evergreen (Aglaonema sp), cotoneaster (cotonase sp), barberry (Myrica sp.), barberry (Abelia sp), Acacia sp. ), And Bromeliad (Bromeliades). According to the present invention, the foaming component is used to control the rate at which the plant ethylene-blocking site blocking agent decomposes in an aqueous solution. Any reaction mixture that causes foaming effectiveness can be used in the present invention. Preferred specific examples of the foaming component of the present invention include mild basic compounds and mild acidic compounds which are solid at ordinary temperatures. Mild basic compounds react with mildly acidic compounds in solvents to produce carbon dioxide gas. According to the present invention, the ratio of the mild basic compound to the mild acidic compound is from about 9: 1 to about 1: 1. This ratio is preferably about 4: 1. Preferred specific examples of mild basic compounds are NaHC03, KHC03,

CaC03,Na2C03,K2C03,NaKC03 及甘胺酸碳酸鈉,以 NaHC03 更佳。 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) 裝--------tr---------線 (請先閱讀背面之注音?事項再填寫本頁) 1241160 A7 B7 五、發明說明( 溫和酸性化合物之較佳具體實施例 反丁缔二酸,水楊酸,草酸,琥珀酸,:丨二’榉檬酸, 酸,乙醇酸,鳥尿酸和葡萄糖酸 項^布二酸,頻果 根據本發明,用於阻斷植物乙更佳。 0.01%至約0.5%。此數量約〇 〇5%至約二〈劑!由約 發明。載體與賦形劑之較佳具體== 形劑皆適用於本 甘油基/?是乙乙二醇山荼酸酯。 G舌’但不限於, 户:王要優點是其提供一種適合非技術性客 發泡_少了和粉末型式相關::::=劑型。此 叫本發明進:步提供製備本發明鍵劑之方法。熟諳製備竣 了ΐ者可採用所有慣用方法來製備本發明鍵劑广 ,、……夕'專利榷(錠劑之慣用方法包括 成…混合後粉末送入印模,然後在約5至約8公斤 千万么分4壓力下壓縮印模成劑型。 本ft明鍵劑可製成容易使用的適合劑型。爲了在辟存及 ^日、的艮好保護,本發明鍵劑可在如:低於3〇%的低相 度下,以塑膠發S包包裝,或可肋封裝。 、本發明另一項具體實施例爲-種抑制植物乙烯反應的方 法。,方法包括由本發明之發泡㈣與溶劑接觸。阻斷植 物乙烯、'、。口位置之樂劑從錠劑中透過發泡作用釋放至空氣 中’然後與植物接觸。 本1月之务/包作用促進鍵劑在水溶液中迸裂,因而促使 -1 0 - 丨X 297公釐) (請先閱讀背面之注音?事項再填寫本頁} 訂· --線- 經濟部智慧財產局員工消費合作社印製 1241160CaC03, Na2C03, K2C03, NaKC03 and sodium glycine carbonate, NaHC03 is preferred. This paper size applies to China National Standard (CNS) A4 specifications (210 X 297 mm). Packing -------- tr --------- line (please read the note on the back first? Matters before filling in This page) 1241160 A7 B7 V. Description of the invention (Preferred embodiments of mild acidic compounds: fumaric acid, salicylic acid, oxalic acid, succinic acid, di-zelic acid, acid, glycolic acid, orniuric acid And gluconic acid ^ adipic acid, according to the present invention, it is better for blocking plant B. 0.01% to about 0.5%. This amount is about 0.05% to about two agents! Invented by about. The carrier and The preferred specifics of the excipients == the excipients are suitable for the present glyceryl group /? Is ethylene glycol mandelate. G tongue 'but not limited to the household: the main advantage is that it provides a suitable for non-technical customers The lack of foaming is related to the powder type :::: = dosage form. This is called the present invention. It further provides a method for preparing the bonding agent of the present invention. Those who are familiar with the preparation can use all conventional methods to prepare the bonding agent of the present invention. ..., Xi 'patent discussion (the usual method of tablets includes mixing the powder into a stamp, and then weighing about 5 to about 8 kilograms) The compression impression is compressed into a dosage form under 4 pressures. The ft bonding agent can be made into a suitable dosage form that is easy to use. In order to save and protect the bonding agent, the bonding agent of the present invention can be used at a concentration of less than 30%. In low phase, it is packaged with plastic S bag, or ribbed package. Another specific embodiment of the present invention is a method for inhibiting the ethylene reaction in plants. The method includes contacting the foamed concrete of the present invention with a solvent. Broken plant ethylene, '.. The mouth-feeling agent is released from the lozenge into the air through the foaming action' and then contacted with the plant. This month's task / package action promotes the cracking of the bonding agent in the aqueous solution, thus promoting -1 0-丨 X 297 mm) (Please read the phonetic on the back? Matters before filling out this page} Order ·-Line-Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 1241160

發明說明(8 丨且tot劑釋放至所處理之環境中。 梟._ +斟、太v切 卜’水落液中發泡作用 虱〜對"1L力楗供均勻溶解所需曰人 放至環境中。 札口政果並將阻斷劑釋 根據本發明,本文使用之溶 _ , a括但不限於,水及稀 釋的驗性溶液。 h 在未進一步闡述下,熟諳此藝者 丄、 上逑杨不内容及下 逑實例將本發明利用至其最大程度。 二、,nn % & 丁述貫例僅可供舉例 呪月晃、褚此蟄者如何操作本申請專利權之方法但未以任 方式限制其餘揭示内容。 貫例1 何 經濟部智慧財產局員工消費合作社印製 錠齊 下述一般製程可用來製備錠劑。一般來説,這些步驟 低相對澄度,如低於30%與25T之溫度下之控制環境^ 什所有成分均句混合。接著使用一種裝備有特定大小 形狀之模子的錠劑壓製器,以約8kg/cm2之壓力壓縮粉 混合物。然後檢查錠劑後,貯存在低相對溼度下接著以 膠發泡形包或鋁箔包裝。 實例2 比幸父!式,驗 式甲基環丙烯錠劑 取1 〇克1 -甲基線丙)布粉末(A n s i P ◦’來自同企業有限公司 北,台灣,中華民國)(AnsiP⑧ from Lytone Enterprise, 1 aiPei,Taiwan,ROC)依上述實例之方法配製成錠劑。每一 片鍵劑包含0.5至1克之1 -甲基環丙烯粉末。需要少量潤滑 -11- 本紙張尺度適用中國國家標準(CNS)A4規格mo X 297公釐) 在 進 與 束 塑 台 Inc. ' 3H- sa ϋ D— βι ϋ s IB f n ϋ ϋ ϋ I H I I 一=0、I I I ϋ H I ϋ ί I ϋ ϋ I ϋ L- I— I (請先閱讀背面之注咅?事項再填寫本頁) 1241160Description of the invention (8 丨 and the tot agent is released into the environment being treated. 枭 ._ + 、, 太 v 切卜 'foaming effect in the water drop lice ~ to 1L force 楗 for uniform dissolution required In the environment, spit mouth and release the blocking agent according to the present invention, the solvents used herein include, but are not limited to, water and dilute test solutions. H Without further elaboration, familiar with this artist, The contents of the upper case and the lower case make use of the present invention to its fullest extent. Second, nn% & Ding Shuguan only provides examples to illustrate how Yue Yuehuang and Chu Yu can use the method of the patent right of this application but not to Any method restricts the rest of the disclosure. Example 1 The following general process can be used to prepare tablets by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. Generally speaking, these steps have low relative clarity, such as less than 30% and Controlled environment at a temperature of 25T ^ All ingredients are mixed in a sentence. Then use a tablet press equipped with a mold of a specific size and shape to compress the powder mixture at a pressure of about 8kg / cm2. Then check the tablet and store it in At low relative humidity It is packed in a plastic foam bag or aluminum foil. Example 2 Than Xingfu! Type, test type methylcyclopropene lozenges take 10 grams of 1-methylline C) cloth powder (A nsi P ◦ 'from the same company limited Company North, Taiwan, Republic of China (AnsiP⑧ from Lytone Enterprise, 1 aiPei, Taiwan, ROC) was formulated into tablets according to the method described above. Each bonding agent contains 0.5 to 1 g of 1-methylcyclopropene powder. Requires a small amount of lubrication -11- This paper size is in accordance with Chinese National Standard (CNS) A4 size mo X 297 mm 0, III ϋ HI ϋ ί I ϋ ϋ I ϋ L- I— I (Please read the note on the back? Matters before filling out this page) 1241160

五、發明說明(9 劑以防鍵劑黏附在模子上。 匈甘p ^ 此減馭製造了兩種形式的鍵 y。其一另包含膨脹劑,另— 。 7lC Φ ^ ^ ^ ΛΑ ^ J 口 如此元成之錠劑投入 ,:“生落液中’以測試其溶解度。觀察到錠劑 炊进衣作用及溶解非常缓慢’即使是含有膨脹劑的錠劑亦 ’ ' —日、後,匕們仍未冗全分散或溶解。所以,在不使 用發泡劑下,由"基環丙烯粉末製成之錠劑形式並不令 人滿意。 互·無/包式1 -甲基環丙晞鍵劑 耳1甲基環丙晞粉末调配成發泡i定劑,其包含40重量% NaHC〇3,1〇%蘋果酸及5〇%依上述製法製造之卜甲基環丙 烯粉末。每個錠劑重量由0·5至2克,依使用模子的大小而 定。當此發泡式錠劑投入水中時,立即發出嘶嘶聲,並且 在60分鐘内完全溶於水中。 實例3 ----— 疑劑 本發明錠劑可依下述調配:V. Description of the invention (9 agents are bonded to the mold with an anti-bonding agent. Hungarian p ^ This reduction produces two forms of bond y. One contains an expansion agent, and the other-. 7lC Φ ^ ^ ^ ΛΑ ^ J I put such a Yuancheng tablet in the mouth, "In the liquid to test its solubility. Observed the slow cooking and the dissolution of the tablet." Even the tablets containing the bulking agent are also '" The daggers have not been completely dispersed or dissolved. Therefore, the form of a tablet made of " base cyclopropene powder is not satisfactory without the use of a foaming agent. Propylene bond agent ear 1 methylcyclopropane powder is formulated into a foaming agent, which contains 40% by weight of NaHC03, 10% malic acid and 50% of the methylcyclopropene powder manufactured according to the above-mentioned production method. Each The weight of the lozenge varies from 0.5 to 2 grams, depending on the size of the mold used. When this foamed lozenge is put into water, it immediately hissed and was completely dissolved in water within 60 minutes. Example 3- --- Doubts The tablets of the present invention can be formulated as follows:

調配物A (請先閱讀背面之注意事項再填寫本頁) 經濟部智慧財產局員工消費合作社印製 成分 每錠含量 1 -甲基環丙缔粉末 500毫克 (包含〇·1 to 0.5% 1-甲基環丙烯, 其餘爲惰性載體) NaHC03 400毫克 蘋果酸 1 〇〇毫克 甘油基/聚乙烯乙二醇山茶酸酯 50毫克 -12- 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐)Formulation A (please read the precautions on the back before filling this page) Printed by the Intellectual Property Bureau of the Ministry of Economic Affairs, the Consumer Cooperatives, the content of each tablet is 1-methylcyclopropyl powder 500 mg (including 0.1 to 0.5% 1- Methylcyclopropene, the rest are inert carriers) NaHC03 400 mg malate 100 mg glyceryl / polyethylene glycol camelliate 50 mg -12- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm)

Claims (1)

1241 m_8號專利申請案 中文申請專利範圍替換本(92年10月) A8 B8 V.1241 m_8 patent application Chinese patent application scope replacement (October 1992) A8 B8 V. 煩請委員明示,本案修正後是否變更原實質i'··f 其中阻斷植物乙晞結合 其中阻斷植物乙婦結合 其中溫和驗性化合物與 1· 一種發泡錠劑,其包含阻斷植物乙烯結合位w、 直 < 藥劑 及發泡成分,與一種或多種可接受載體和/或職形劑混 合,其中該阻斷植物乙烯反應之藥劑係選自由環丙 烯、1-甲基環丙婦、3,3-二τ基環丙婦、亞甲基環丙 燒、重氮基環戊二締、反式-環辛婦、順式-環辛缔及 2,5-原冰片二晞,及其衍生物,及其混合物所組成之群, 且該發泡成分包含在常溫下為固態之溫和鹼性化合物 與溫和酸性化合物。 2.如申請專利範圍第1項之錠劑,其中阻斷植物乙缔結合 位置之藥劑為1 -甲基環丙烯。 3·如申請專利範圍第1項之錠劑,其溫和鹼性化合物係選 自:NaHC03,KHC03,CaC03,Na2C03,K2C〇3, NaKC〇3及甘胺酸碳酸鈉,及其混合物。 4.如申請專利範圍第1項之錠劑,其中溫和酸性化合物選 自··酒石酸,擰檬酸,反丁缔二酸,水楊酸,草酸, 琥拍酸’蘋果酸,順丁烯二酸,乙醇酸,鳥尿酸,葡 荀糖酸及其混合物。 5·如申請專利範圍第1項之錠劑, 位置之藥劑量為0.01 %至0.5%。 6·如申請專利範圍第5項之錠劑, 位置之藥劑量為0.05%至0.24% 7 ·如申請專利範圍第1項之錠劑, 溫和酸性化合物之比例為9: 1至1: 1。 8·如申請專利範圍第7項之錠劑,其中溫和驗性化合物與 本紙張尺度適用中國國家標準(CNS) A4規格(210 x 297公釐) 1241160 A8 B8 C8 D8 六、申請專利範圍 溫和酸性化合物之比例為4: 1。 9. 如申請專利範圍第1至8項中任一項之錠劑,其中阻斷 植物乙晞結合位置之藥劑係呈氣態釋出。 10. —種製備如申請專利範圍第1項錠劑之方法,其包括混 合阻斷植物乙烯結合位置之藥劑、發泡成分和一種或 多種可接受載體和/或賦形劑,且將該混合物於5至8公 斤/平方公分壓力下壓縮成錠劑。 11 · 一種抑制植物乙婦反應之方法,其包括由如申請專利 範圍第1項之發泡錠劑與溶劑接觸,藉此透過發泡作 用,使錠劑釋出阻斷植物乙缔結合位置之藥劑。 12. 如申請專利範圍第11項之方法,其中溶劑選自水和稀 釋鹼性溶液。 13. 如申請專利範圍第12項之方法,其中溶劑為水。 -2- 本紙張尺度適用中國國家標準(CNS) A4規格(210X 297公釐)Members are kindly requested to state clearly whether the original substance i '·· f will be changed after the amendment of this case. Among them, blocking plant acetamidine binding, among them, blocking plant acetamidine binding, among which are mildly test compounds and 1. a foaming lozenge, which contains blocking plant ethylene The binding site w, straight < medicament and foaming ingredients are mixed with one or more acceptable carriers and / or formulations, wherein the medicament for blocking the plant ethylene reaction is selected from the group consisting of cyclopropene and 1-methylcyclopropene , 3,3-Di-Tau-Cycloprofen, Methylene-Cyclopropane, Diazo-Cyclopentadiene, Trans-Cyclopropyl, Cis-Cyclopropyl, and 2,5-Original Borneol, And its derivatives, and mixtures thereof, and the foaming component includes a mild basic compound and a mild acidic compound which are solid at normal temperature. 2. The lozenge according to item 1 of the scope of patent application, wherein the agent that blocks the site of plant ethylene binding is 1-methylcyclopropene. 3. As for the lozenge of item 1 of the patent application scope, the mild alkaline compounds are selected from: NaHC03, KHC03, CaC03, Na2C03, K2C03, NaKC03 and sodium glycine carbonate, and mixtures thereof. 4. The tablet according to item 1 of the scope of patent application, wherein the mildly acidic compound is selected from the group consisting of tartaric acid, citric acid, fumaric acid, salicylic acid, oxalic acid, succinic acid, malic acid, and maleic acid. Acid, glycolic acid, guanuric acid, gluconic acid and mixtures thereof. 5. If the lozenge of item 1 of the patent application scope, the dosage of the medicine is 0.01% to 0.5%. 6. If the lozenge of item 5 of the patent application is applied, the dosage of the position is 0.05% to 0.24%. 7. If the lozenge of item 1 of the patent application is applied, the ratio of the mild acidic compound is 9: 1 to 1: 1. 8. If the tablet of item 7 in the scope of the patent application, the mildly test compound and the paper size apply the Chinese National Standard (CNS) A4 specification (210 x 297 mm) 1241160 A8 B8 C8 D8 6. The scope of the patent application is mildly acidic The compound ratio is 4: 1. 9. The tablet according to any one of claims 1 to 8 of the scope of application for a patent, wherein the agent that blocks the binding site of the plant's acetamidine is released in a gaseous state. 10. A method for preparing a lozenge such as item 1 of the scope of patent application, which comprises mixing an agent that blocks the ethylene binding site of a plant, a foaming ingredient, and one or more acceptable carriers and / or excipients, and mixing the mixture It is compressed into tablets at a pressure of 5 to 8 kg / cm². 11 · A method for inhibiting the response of a plant, which comprises contacting a foaming lozenge such as the item 1 in the patent application with a solvent, thereby releasing the lozenge through blocking the site of blocking the binding of the plant ’s ethylene through the foaming effect Pharmacy. 12. The method of claim 11 in which the solvent is selected from the group consisting of water and a dilute alkaline solution. 13. The method of claim 12 in which the solvent is water. -2- This paper size applies to China National Standard (CNS) A4 (210X 297 mm)
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