CN1210021C - Novel formulation for counteracting ethylene response in plants, preparation process thereof and method using the same - Google Patents

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

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Publication number
CN1210021C
CN1210021C CN00818661.8A CN00818661A CN1210021C CN 1210021 C CN1210021 C CN 1210021C CN 00818661 A CN00818661 A CN 00818661A CN 1210021 C CN1210021 C CN 1210021C
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tablet
plants
acid
blocking
ethylene
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CN1433301A (en
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W·T·H·张
杨仁德
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LYSTONE ENTERPRISE Inc
Lytone Enterprise Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007—Effervescent
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N27/00—Biocides, pest repellants or attractants, or plant growth regulators containing hydrocarbons
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23B—PRESERVING, e.g. BY CANNING, MEAT, FISH, EGGS, FRUIT, VEGETABLES, EDIBLE SEEDS; CHEMICAL RIPENING OF FRUIT OR VEGETABLES; THE PRESERVED, RIPENED, OR CANNED PRODUCTS
    • A23B7/00—Preservation or chemical ripening of fruit or vegetables
    • A23B7/14—Preserving or ripening with chemicals not covered by groups A23B7/08 or A23B7/10
    • A23B7/153—Preserving or ripening with chemicals not covered by groups A23B7/08 or A23B7/10 in the form of liquids or solids
    • A23B7/154—Organic compounds; Microorganisms; Enzymes

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
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  • General Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Microbiology (AREA)
  • Polymers & Plastics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Food Science & Technology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Dentistry (AREA)
  • Environmental Sciences (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

The present invention discloses a tablet for inhibiting an ethylene reaction of plants, which is prepared by mixing a blocking agent, a foaming component and one or a plurality of acceptable excipients, wherein the blocking agent can be used for inhibiting the activity of ethylene combining positions of the plants. The present invention also discloses a method for preparing the tablet, and a method for inhibiting the ethylene reaction of the plants.

Description

New prescription, its preparation method and the using method thereof of counteracting ethylene response in plants
Invention field
The invention relates to a kind of tablet formulation of novelty, it is used to regulate plant physiology, hinder ethylene reaction specifically, wherein comprise blocker and foaming ingredient, with one or more acceptable mixed with excipients, and the relevant method of making this prescription reaches by using the method that prescription of the present invention suppresses various ethylene reactions.
Background technology
In the plant growing reaction, the plant hormone is being played the part of important role.Ethylene is a kind of to plant growing, grows, and aging has the HGH of a lot of material impacts.The most important influence of ethylene comprises and fruit maturation, flower decline and the relevant process of leaves.The commercial value of fresh products often reduces because of excessive ethylene gas, because of it can quicken the maturation of fruit, and the coming off too early of the decline of flower and leaf.
Because the ethylene problem of bringing out, a large amount of research concentrate on and prevent or lower its method for the plant influence.Slow down ethylene and influence one of most effectual way for utilizing the principle that receives the receiver of ethylene signal in the blocking-up plant.At this purpose, one of chemical compound of knowing of wherein behaving most is Argylene (" STS ").STS ethylene binding site in plant cell provides a kind of irreversible blocking-up, thereby prevention or lower the adverse effect of ethylene to plant.Although STS is very effective, because silver is a kind of to the deleterious heavy metal of most of live organism, so can cause serious offal treatment problem.
Xi Sile people's such as (Sisler) Plant Growth Reg.9,1587-164,1990 announcement cyclopentadiene are a kind of effective ethylene binding site in plants blocker.United States Patent (USP) the 5th, 100 also discloses a kind of effective diazo cyclopentadiene No. 462.Yet cyclopentadiene and diazo cyclopentadiene are unstable and have a strong odor.
U.S. Patent number the 5th, 518,988 have disclosed with gaseous cyclopropene and derivant thereof, as: methyl cyclopropene is as the purposes of ethylene binding site blocker.Just can come into force under the very low dose of methyl cyclopropene in the parts per billion scope, thereby can on flowers, be used for fruits and vegetables safely as using.Methyl cyclopropene is easy to carry out oxidation reaction and other reaction, so very unstable.In No. the 6th, 017,849, the nearest United States Patent (USP) case, methylcyclopropene gas is encapsulated with carrier.Can be used to the reactivity and the unstability of stabilizing ring propylene gas as the carrier of alpha-cyclodextrin, thereby provide one to store, transport, use or carry (delivering) this gas to the convenience of plant and the method for safety.
Commerce comprises 0.43% methylcyclopropene gas composition usually with the methyl cyclopropene powder-product.Powder with can disengage this gas after water or buffer mix.The rate of application of 0.5 g of powder of every stere can reach into the final methyl cyclopropene concentration of 900ppb in the enclosed space.If under this concentration, expose at least 4 hours to the open air as the results post processing, but with the significant prolongation flowers, the anti-storage time of fruits and vegetables.
Powder-product comes conveniently far beyond gaseous product in the use, but still unfavorable to user.It still has on this field the shortcoming of using powder, for example: as easy as rolling off a logly make moist too early and measure error.In addition, recommend usually with a large amount of powder of manual mixing, as: need every batch to use the above amount of 10 grams when fumigating large space.In confined space,, perhaps can cause the concentration of the wherein original expection of amount ratio of methyl cyclopropene to reduce, thereby reduce the favourable benefit of methyl cyclopropene because the staff passes in and out confined space in mixed process.
The invention provides a kind of foaming type tablet formulation of disadvantages associated when slowing down the mixed-powder type.
Brief summary of the invention
So purpose of the present invention is for providing a kind of foaming tablet that suppresses ethylene response in plants, its comprise a kind of medicament of blocking ethylene binding site in plants, and a kind of foaming ingredient and one or more can accept carrier and/or mixed with excipients.
The method for preparing novel tablet of the present invention that provides is provided.
Further object of the present invention is for providing the method that suppresses ethylene response in plants.
Detailed description of the invention
The invention provides a kind of novel tablet prescription, it comprises a kind of blocking-up ethylene binding site in plants medicament and a kind of foaming ingredient, can accept carrier and/or mixed with excipients with one or more.
According to the present invention, the medicament of blocking-up ethylene binding site in plants comprise all be customarily used in chemical compounds of suppressing ethylene response in plants as, but be not limited to, cyclopropylene, 1-methyl-cyclopropylene, 3, the 3-dimethylcyclopropane, the methylene cyclopropane, the diazonium cyclohexadiene, anti--cyclo-octene, suitable-cyclo-octene, and 2, the 5-norbornadiene.Relevant Prior Art, as United States Patent (USP) the 3rd, 879,188,5,100,462,5,518,988, and 6,017, No. 849, with Xi Sile people's such as (Sisler) Plant Growth Reg.9,157-164,1990 have incorporated in this description fully in the mode of mentioning.The preferable medicament of blocking-up ethylene binding site in plants is the 1-methyl cyclopropene.
According to the present invention, " plant " speech also comprises field crops except referring to xylophyta, potted plant, cut-flower, the fruit of gathering, vegetable and ornamental plant.
Accept the plant of the tablet processing of the present invention of ethene suppressing reaction and must accept the not phytotoxic amount processing of tool.This phytotoxicity amount is not only with plant, and changes with the kind that cultivates plants.
According to the present invention, can be as United States Patent (USP) the 5th, 518,988 and 3,879, disclosed in No. 188, prevent many ethylene reactions.Ethylene reaction can be begun by exogen or endogenous sources of ethylene.Ethylene reaction comprises, for example, and flowers, fruit and vegetable ripe and/or old and feeble; Leaf, the coming off of flower and fruit; Ornamental plant such as potted plant, cut-flower, the maturation of shrub and dormancy seedling and/or the shortening in life-span; Suppress the growth of some plants such as Semen Pisi sativi; And the growth that stimulates some plants such as rice.
According to the present invention, can accept processing and comprise green leaf vegetables to suppress old and feeble plant, as Caulis et Folium Lactucae sativae (e.g., Lactuea sativa), Herba Spinaciae (Spinaca oleracea) and Brassica oleracea L.var.capitata (Brassica oleracea); Various tuberses are as Rhizoma Solani tuber osi (Solanum tuberosum), Radix Dauci Sativae (Daucus); The ball base class is as Bulbus Allii Cepae (Allium sp.); Spice berry, as Herba Ocimi (Herba Ocimi Pilosi) (Ocimum basilicum), Adeps Bovis seu Bubali (Origanum vulgare) and Fructus anethi (Anethumgraveolens); And Semen sojae atricolor (Glycine max), Phaseolus lunatus L. (Phaseolus limensis), Semen Pisi sativi (Lathyrus sp.), corn (Zea mays), globe daisy Caulis et Folium Brassicae capitatae (Brassica oleraceaitalica), Brassica oleracea L. var. botrytis L. (Brassica oleracea botrytis) and asparagus (Asparagusofficinalis).
According to the present invention, can accept to handle and comprise Fructus Lycopersici esculenti (Lycopersicon esculentum) to suppress its ripened fruit, Fructus Mali pumilae (Malus domes tica), Fructus Musae (Musasapientum), bartlett pear (Pyrus communis), Fructus Chaenomelis (Carica papya), Fructus Mangifera Indicae (Mangifera indica), Fructus Persicae (Prunus persica), Fructus Pruni (Prunusarmeniaca), Prunus persicanucipersica Schneider (Prunus persica nectarina), orange (Citrus sp.), Fructus Citri Limoniae (Citrus limonia), Lyme (Citrus aurantifolia), grapefruit (Citrusparadisi), Fructus Citri tangerinae (Citrus nobilis deliciosa), kiwi fruit (Actinidia.Chinenus), Fructus Melo such as cantaloupe (C.cantalupensis) and Fructus Melo (C.melo), Fructus Ananadis comosi (Aranae comosus), Fructus Kaki ((Diospyros sp.), and rasp berry (as, Fragaria or Rubus ursinus), blue berry (Vaccinium sp.), Semen phaseoli radiati (Phaseolus vulgaris), the member of Cucumis such as Fructus Cucumidis sativi (C.sativus) and American Avocado Tree (Persea Americana).
According to the present invention, the ornamental plant that can accept to handle to suppress aging and/or prolongation florescence and outward appearance (withering as delaying) comprises potted ornamental plant and cut-flower.Potted ornamental plant and the cut-flower that can accept the inventive method processing comprise Folium Rhododendri Simsii (Rhododendron spp.); hydrangea plant (Macrophylla hydrangea); Hibiscus syriacus L. (Hibiscus rosasanensis); hornwort (Antirrhinum sp.); poinsettia (Euphorbia pulcherima); Radix et Caulis Opuntiae Dillenii (e.g.; Cactaceae schlumbergera truncata); Flos Begoniae Evansianae (Begonia sp.); Flos Rosae Rugosae (Rosa sp.); Flos Tulipae Gesnerianae (Tulipa sp.); daffodil (Narcissus sp.); morning glory (Petunia hybrida); Dianthus carryophyllus (Dianthus caryophyllus); Bulbus Lilii (as Lilium sp.); gladiolus (Gladiolus sp.); herb lily (Alstroemariabrasiliensis); Herba anemones vitifoliae (as Anemone bland); garden columbine (Aquilegia sp.); Hu wood belongs to (as chimney wood), Aster tataricus platymiscium (as Aster carolinianus), nine weights (Bougainvillea sp.); Flos Camelliae Japonicae (Camellia sp.); Canterburybells (Campanula sp.), Flos Celosiae Cristatae (Celosia sp.), Cupressus funebris (Chamaecyparis sp.); Flos Chrysanthemi (Chrysanthemum sp.); Radix clematidis floridae (Clematis sp.), primrose (Cyclamen sp.), freesia (e.g.; Freesia refracta), reach the Cymbidium ensifolium (L.) Sw. of the orchid family.
According to the present invention, can accept to handle to suppress leaf, the plant that flower and fruit remove comprises Cotton Gossypii (Gossypium spp.), Fructus Mali pumilae, bartlett pear, Fructus Pruni pseudocerasi (Prunus avium), pecan (Carvaillinoensis), Fructus Vitis viniferae (Vitis vinifera), Fructus Canarii albi (as, Olea europaea), coffee (Cofffea arabica), Kidney bean (Phaseolus vulgaris) and weeping branch Ficus carica L. (weeping fig) (Ficus benjamina) reach as comprise many fruit trees of Fructus Mali pumilae, ornamental plant, the dormancy seedling of shrub and tree seedling.
In addition; according to the present invention; can accept to handle the shrub that comes off with the inhibition leaf and comprise regel's privet (Ligustrum sp.); Chinese photinia (photina sp.); Ilicis Purpureae (Ilex sp.); the fern of Polypodiaceae; schefflera (Schefflera sp.); Rohdea japonica Roth (Aglaonema sp.), Xun (Cotoneaster sp.), Flos Damnacanthi indici (Berberris sp.); Fructus Myricae rubrae (Myrica sp.); Fructus Abeliae biflorae (Abelia sp.), Radix Acaciae senegalis (Acacia sp.), and the Fructus Ananadis comosi (Bromeliades) of Fructus Ananadis comosi section.
According to the present invention, foaming ingredient is used for controlling the speed that blocking-up ethylene binding site in plants medicament decomposes at aqueous solution.Any reactant mixture that causes that foaming is renderd a service all can use in the present invention.The preferable specific embodiment of foaming ingredient of the present invention comprises being solid gentle alkali compounds and gentle acid compound at normal temperatures.Gentle alkali compounds produces carbon dioxide with gentle acid compound reaction in solvent.
According to the present invention, the ratio of gentle alkali compounds and gentle acid compound is about 9: 1 to about 1: 1.This ratio was good with about 4: 1.
The preferred embodiment of gentle alkali compounds is NaHCO 3, KHCO 3, CaCO 3, Na 2CO 3, K 2CO 3, NaKCO 3And the glycine sodium carbonate, with NaHCO 3Better.
The preferred embodiment of gentle acid compound is a tartaric acid, citric acid, and fumaric acid, salicylic acid, oxalic acid, succinic acid, maleic acid, malic acid, glycolic, ornithuric acid and gluconic acid, and better with malic acid.
According to the present invention, be used to block the dosage of ethylene binding site in plants by about 0.01% to about 0.5%.This quantity about 0.05% to about 0.24% is preferable.
Known all carriers and excipient all are applicable to the present invention on the preparation tablet formulation.The preferred embodiment of carrier and excipient includes, but not limited to glyceryl/polyethylene glycol behenate.
The major advantage of dosage form of the present invention is that it provides a kind of suitable inartful client, florist and whole seller effectively and to the real favourable dosage form of user.This foaming tablet has reduced the shortcoming of the mixed process relevant with the powder pattern.
The present invention further provides the method for preparing tablet of the present invention.This area prepares the tablet formulation technical staff and can adopt all conventional processes to prepare tablet of the present invention.
According to the present invention, the conventional process of preparation the application Patent right tablet comprises blending constituent, will mix afterwards powder and send into die, becomes dosage form about 5 to about 8 kilograms/square centimeter pressure lower compression die then.
Tablet of the present invention can be made into easy-to-use suitable dosage form.For the good protection when storing and transporting, tablet of the present invention can as: be lower than under 30% the low relative humidity, with plastic foamed collation package, or the encapsulation of available aluminium foil.
Another specific embodiment of the present invention is a kind of method that suppresses ethylene response in plants.The method comprises by foaming tablet of the present invention and contacting with solvent.The medicament of blocking-up ethylene binding site in plants sees through foaming effect and is released in the air from tablet, then with plant contact.
Foaming effect of the present invention promotes that tablet advances to split in aqueous solution, thereby impels blocker to be released in the handled environment.In addition, the convection current power of foaming effect gas provides the required mixed effect of uniform dissolution and blocker is released in the environment in the aqueous solution.
According to the present invention, solvent used herein includes, but not limited to the alkaline solution of water and dilution.
Under further not setting forth, those skilled in the art can utilize the present invention to it at utmost according to the above-mentioned following example that openly reaches.How following example only can be implemented this claim method but not limit all the other disclosures by any way for illustrating those skilled in the art.
Example 1
Preparation tablets
Following general processing procedure can be used to prepare tablet.In general, these steps are in low relative humidity, as are lower than in the controling environment under 30% and 25 ℃ the temperature and carry out.The all the components uniform mixing.Then use a kind of tablet press device that is equipped with the mould of specific size and shape, with about 8kg/cm 2Pressure compressing powder mixture.After checking tablet then, be stored under the low relative humidity then with plastic foamed shape bag or In Aluminium Foil Packing.
Example 2
Comparative test
A. non-foaming type methyl cyclopropene tablet
Get 10 gram 1-methyl cyclopropene powder (Ansip , the sharp business corporation that unites, the Taibei, Taiwan, the Republic of China) and (AnsiP From Lytone Enterprise, Inc.Taipei, Taiwan, ROC) method according to above-mentioned example is mixed with tablet.Each sheet tablet comprises the 1-methyl cyclopropene powder of 0.5 to 1 gram.Need minor amounts of lubricants in case tablet sticks on the mould.The tablet of two kinds of forms has been made in this test.One also comprises extender, and another does not then have.With in this tablet of finishing input water or in the alkaline solution of dilution, to test its dissolubility.Observe tablet advance to split the effect and the dissolving very slow, also be like this even contain the tablet of extender.After 4 hours, they do not disperse or dissolve yet fully.So, do not using under the foaming agent, also unsatisfactory by the tablet form that 1-methyl cyclopropene powder is made.
B. foaming type 1-methyl cyclopropene tablet
Get 1-methyl cyclopropene powder and be deployed into the foaming tablet, it comprises 40 weight %NaHCO 3, 10% malic acid and 50% 1-methyl cyclopropene powder according to above-mentioned method for making manufacturing.Each tablet weight is decided according to the size of using mould by 0.5 to 2 gram.When this foaming type tablet drops in the water, hiss immediately, and soluble in water fully in 60 minutes.
Example 3
The allotment of tablet
Tablet of the present invention can be complied with following allotment:
Prescription A
CompositionEvery content
500 milligrams in 1-methyl cyclopropene powder
(comprise 0.1 to 0.5%1-methyl cyclopropene,
All the other are inert carrier)
NaHCO 3400 milligrams
100 milligrams of malic acids
50 milligrams of glyceryls/polyethylene glycol behenate

Claims (13)

  1. One kind the foaming tablet, it comprises a kind of medicament and foaming ingredient of blocking ethylene binding site in plants, can accept carrier and/or mixed with excipients with one or more, it is solid-state gentle alkali compounds and gentle acid compound at normal temperatures that wherein said foaming ingredient comprises.
  2. 2. tablet as claimed in claim 1, the medicament of wherein said blocking ethylene response in plants is selected from: cyclopropylene, 1-methyl cyclopropene, 3,3-dimethyl cyclopropylene, methylene cyclopropane, diazo cyclopentadiene, trans-cyclo-octene, cis-cyclo-octene and 2,5-norbornadiene and derivant thereof, and composition thereof.
  3. 3. tablet as claimed in claim 2, the medicament of wherein said blocking-up ethylene binding site in plants are the 1-methyl cyclopropene.
  4. 4. tablet as claimed in claim 1, wherein said gentle alkali compounds is selected from: NaHCO 3, KHCO 3, CaCO 3, Na 2CO 3, K 2CO 3, NaKCO 3And the glycine sodium carbonate, and composition thereof.
  5. 5. tablet as claimed in claim 1, wherein said gentle acid compound is selected from: tartaric acid, citric acid, fumaric acid, salicylic acid, oxalic acid, succinic acid, malic acid, maleic acid, glycolic, ornithuric acid, gluconic acid and composition thereof.
  6. 6. tablet as claimed in claim 1, the pharmaceutical quantities of wherein said blocking-up ethylene binding site in plants are 0.01% to 0.5%.
  7. 7. tablet as claimed in claim 6, the pharmaceutical quantities of wherein said blocking-up ethylene binding site in plants are 0.05% to 0.24%.
  8. 8. tablet as claimed in claim 1, the ratio of wherein said gentle alkali compounds and gentle acid compound are 9: 1 to 1: 1.
  9. 9. tablet as claimed in claim 8, the ratio of wherein said gentle alkali compounds and gentle acid compound are 4: 1.
  10. 10. one kind prepares the method for tablet according to claim 1, and it comprises that the medicament that mixes the blocking-up ethylene binding site in plants, foaming ingredient and one or more can accept carrier and/or excipient.
  11. 11. a method that suppresses ethylene response in plants, it comprises by foaming tablet as claimed in claim 1 and contacting with solvent, sees through foaming effect then, makes tablet disengage the medicament of blocking-up ethylene binding site in plants.
  12. 12. method as claimed in claim 11, wherein said solvent are selected from water and dilution alkaline solution.
  13. 13. method as claimed in claim 12, wherein said solvent are water.
CN00818661.8A 2000-09-22 2000-09-22 Novel formulation for counteracting ethylene response in plants, preparation process thereof and method using the same Expired - Lifetime CN1210021C (en)

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Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6762153B2 (en) 2001-10-18 2004-07-13 Rohm And Haas Company Delivery system for cyclopropenes
US6770600B1 (en) * 2003-02-28 2004-08-03 Rohm And Haas Company Delivery systems for cyclopropene compounds
TW200538037A (en) * 2004-05-19 2005-12-01 Rohm & Haas Compositions with cyclopropenes and adjuvants
TW200603731A (en) * 2004-05-19 2006-02-01 Rohm & Haas Compositions with cyclopropenes and metal-complexing agents
US8691728B2 (en) * 2006-11-09 2014-04-08 Rohm And Haas Company Cyclopropene compositions
WO2008071714A1 (en) * 2006-12-15 2008-06-19 Rohm And Haas Company Mixtures comprising 1-methylcyclopropene
WO2008089140A1 (en) 2007-01-17 2008-07-24 Dow Agrosciences Llc Delivery of ethylene blocking and/or promoting agents
CN105437676B (en) 2014-08-14 2020-03-24 上海利统生化制品有限公司 Laminate for blocking ethylene reaction of plant and preparation method thereof
CN104872126B (en) * 2015-04-13 2020-09-01 禾金正生物科技(北京)股份有限公司 Plant growth regulator 1-methylcyclopropene effervescent granule/effervescent tablet and preparation method thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5100462A (en) * 1991-04-01 1992-03-31 North Carolina State University Method of counteracting ethylene response by treating plants with diazocyclopentadiene and derivatives thereof
US5518988A (en) * 1994-06-03 1996-05-21 North Carolina State University Method of counteracting an ethylene response in plants
US6017849A (en) * 1998-08-20 2000-01-25 Biotechnologies For Horticulture, Inc. Synthesis methods, complexes and delivery methods for the safe and convenient storage, transport and application of compounds for inhibiting the ethylene response in plants

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