CN101632391A - Development of novel indoor acaricide - Google Patents

Abstract

The invention discloses a method for developing a novel indoor acaricide. The novel acaricide uses clove and other Chinese medicinal materials as raw materials, the main active component thereof is eugenic acid, and the novel acaricide is a pure natural chemical substance, has no notable harms to human bodies and other organic bodies, has no potential hazards to the environment too, and can be widely applied to killing, preventing and controlling various dust mites of dermatophagoides pteronyssinus, dermatophagoides farinae and the like in various regions and various indoor environments. The novel acaricide can effectively control the number of the dust mites in the living environments of people, greatly reduce the density of dust mite allergens in the indoor environments, and significantly reduce the disease incidence of dust mite anaphylactic diseases. Besides, the novel acaricide has outstanding effects of preventing and performing adjuvant therapy on various anaphylactic diseases taking the dust mites as the allergens, such as allelgic asthma, rhinitis and the like.

Description

A kind of development of novel indoor acaricide

Technical field

The invention belongs to the hygienic insecticide technical field, specifically, relate to a kind of research and development and technology of preparing thereof of novel indoor acaricide.

Background technology

Along with improving constantly of industrialization degree in the world wide, the incidence of disease of anaphylactia is the trend that increases year by year in the world.In August, 2005 world's allergy tissue (WAO) is in first world anaphylactia day, announced that 30 countries carry out anaphylactia epidemiology survey result: in 1,200,000,000 total populations of these countries, 22% (2.5 hundred million people) suffers from the anaphylactia of immunoglobulin E (IgE) mediation, as allergic rhinitis, asthma, conjunctivitis, eczema, food hypersenstivity, drug allergy and severe allergic reaction etc.The U.S. has more than 5,000 ten thousand people to suffer from anaphylactia, and the adult of 10%-30% and 40% children suffer from allergic rhinitis; In addition, there are every year 1800000 person-times to go to a doctor, receive treatment in hospital because of asthma for 46.5 ten thousand person-times because of allergic asthma goes to emergency department.Estimate that according to the World Health Organization whole world has 1.5 hundred million people to suffer from asthma approximately, wherein the adult 50% or more reaches at least 80% child patient and brings out by irritated factor, and has every year people more than 180,000 to die from asthma.

Anaphylactogen is the arch-criminal who causes anaphylactia, and in numerous anaphylactogens that oneself determines, the dirt mite is most important inhalant allergens, also is most important indoor anaphylactogen, is subjected to the extensive concern of global medical treatment and researcher.The topmost dirt mite of global distribution has two kinds, and promptly the dermatophagoides pteronyssinus of dirt mite subfamily and dust mite account for the 80%-90% of all mite quantity, and is worldwide main indoor anaphylactogen.The dirt mite investigation of carrying out in room, 15 cities and towns of China shows: all more than 40%, Shanghai reaches 66.67% to the recall rate of dirt mite in the room, city.

At present, specific active immunotherapy is considered to unique etiological treatment method of anaphylactia.But standardization anaphylactogen vaccine and standard items that China does not also ratify by SFDA.Because the difference of region, also may there be certain difference in anaphylactogen of the same race.In addition, import anaphylactogen vaccine price costliness has increased the cost of patient.The immunization therapy route of administration is confined to hypodermic injection at present more, and its course of treatment is long, and long-term treatment patient's tolerance is relatively poor.

Discover, reduce the dust mite allergen quantity in the environment, can reduce the danger that children and teenager suffer from anaphylactic disease, and in the process of immunization therapy anaphylactia, reduce the dirt mite quantity in the environment of patient place simultaneously, can obtain better result of treatment.Therefore, this prophylactico-therapeutic measures has effect to alleviating and treating children's anaphylactia.The dirt mite quantity that reduces in the indoor environment has three kinds of approach usually: the one, and clean, as sweep environment, cleaning clothes; The 2nd, the rising temperature reduces humidity; Three are to use effective miticide.In removing the whole bag of tricks of mite, miticide has conveniently, efficient, special advantage and being subject to people's attention day by day.

Present miticide mainly is to be main active ingredient with syntheticses such as γ-BHC, DEET, Ergols, is mainly used in dissipation and the control of agricultural evil mite.Although these chemicalses can better be controlled the dirt mite, need long-term the use just to produce effect, and strong toxicity, residual of a specified duration, side effect is big, and environment is had bigger influence, is not suitable for indoor use.Therefore, the novel miticide of quick, efficient, the low toxicity of research, environmentally safe becomes one of emphasis of current anaphylactia study on prevention work.

China's tradition Chinese herbal medicine has draw materials extensive, numerous advantages such as cost of material is low, effect is remarkable, no serious toxic and side effect, and application is widely all being arranged aspect medicine, agricultural, beauty treatment, the health care etc. a lot.Chinese medicine has all been obtained the achievement that attracts people's attention in the treatment of the research and development of new drug, clinical multiple difficult and complicated cases.Therefore the novel indoor acaricide of efficient, the low toxicity of research and development, environmentally safe is one of breach of current miticide research and development from China's tradition Chinese herbal medicine.

Plants essential oil contains multiple natural constituent, has been widely used in the production of perfume, spices, in the attention that application facet has also caused the researcher that prevents and treats of dirt mite, and is expected to develop the novel miticide of substituted chemistry synthetic acaricide.For example caryophyllus oil all has good killing effect to dust mite and dermatophagoides pteronyssinus, as miticide good application prospects is arranged, and it could be introduced to the market but also will carry out a series of study on the industrialization.

Summary of the invention

The present invention is intended to overcome deficiencies such as chemosynthesis miticide toxic and side effect is big, need use for a long time, environmental pollution is serious and researches and develops the novel miticide of dirt mites such as the indoor dermatophagoides pteronyssinus of a kind of effective dissipation, dust mite, characteristics such as that this novel miticide has is convenient, fast, efficient, low toxicity, environmentally safe, be with China's tradition Chinese herbal medicine be raw material in conjunction with the modern times extract, preparation technology is refining forms.

Second purpose of the present invention is to determine the novel acaricidal raw material of drawing materials, comprise cloves, tealeaves, caraway, fennel seeds, peppermint, rose, geranium, kuh-seng, Chinese prickly ash, the tuber of stemona, betel nut, frutus cnidii, chaulmoogra, Fructus meliae toosendan, black false hellebore, hairyvein agrimony, the coptis, geranium, lemon grass (Cymbopogon citratus), rosemary,, the traditional Chinese herbal medicines of China such as eucalyptus leaves, coffee bean, thyme, wrinkled giant hyssop, dried orange peel, golden cypress, the root of Chinese wild ginger, the fruit of Rangoon creeper, Chinese cassia tree.

Novel acaricidal main active ingredient is all eugenol compounds and various derivative thereof among the present invention.

Eugenol

Another object of the present invention provides novel acaricidal preparation method, may further comprise the steps:

(1) extracts solvent and comprise that benzinum (I), benzinum (II), n-hexane, cyclohexane are equal to the isopolarity solvent;

(2) method of Ti Quing comprises similar extracting method such as leaching method, cable-styled extraction method, supercritical extraction;

(3) method of HPLC and MS combination is mainly adopted in the analysis of active ingredient, and the HPLC fingerprint pattern technology is mainly adopted in the control of quality;

(4) with CH ₃(CH ₂) _nOH is secondary solvent (n=0-5), C _nH _N+2Be high pressure vapor (n=2-10) that the sealing tinning makes finished product.

Compare with existing chemosynthesis miticide, miticide among the present invention has efficiently, low toxicity, environmentally safe, advantage such as easy to use, adopt low polarity, easy volatile solvent effective component extracting such as benzinum to greatly reduce the pollution of production cost and production process to environment, quality with the more effective control product of HPLC fingerprint pattern technology energy, with small molecule alcohol and alkanes is that auxiliary raw material also greatly reduces the cost of product and the difficulty of production, and ultimogenitary aerosol products is very convenient in the use, and numerous indoor environments all are suitable for.

Embodiment

The preparation of embodiment 1 caryophyllus oil

The traditional Chinese medicine cloves, 45 ℃ of oven dry are pulverized, and apparatus,Soxhlet's is installed, and with the water-bath heating, benzinum (II) is a solvent, extracts cloves active ingredient.Extract is removed impurity by vacuum filtration, adds anhydrous Na ₂SO ₄Drying is removed solvent with rotary evaporator and is got extract.Embodiment 2 contact methods test caryophyllus oil acaricidal activity

Set a certain maximum concentration of caryophyllus oil, the two-fold dilution is 8 concentration successively, drawing 300 μ l respectively evenly is adsorbed onto on the filter paper of diameter 5.6cm, treat that solvent evaporates is complete, filter paper is put into the culture dish that the adult mite of some (60 ± 10) is housed, put into constant incubator, observe the mite situation of killing behind the 24h.Number goes out the dead number (under anatomical lens, gently stab the mite body 3 times with pin, the acarid four limbs are motionless, can judge acarid death) of mite, calculates lethality, repeats 3 times, calculates LD ₅₀

The acaricidal activity of embodiment 3 fumigating systems test caryophyllus oil

The filter paper of diameter 7cm is put in the culture dish lid of diameter 6cm, the extract 300 μ l that draw variable concentrations evenly are adsorbed onto on the filter paper, after treating that solvent evaporates fully, filter paper is placed on the culture dish that is placed with the adult mite of some (60 ± 10), put into constant incubator.Observe the mite situation of killing behind the 24h, calculate LD ₅₀

The 4 test caryophyllus oil acaricidal action times of embodiment

Draw the caryophyllus oil of 300 μ l variable concentrations, evenly be adsorbed onto on the filter paper of diameter 5.6cm, treat that solvent evaporates is complete, filter paper is put into the culture dish that is placed with the adult mite of some (60 ± 10), put into constant incubator, observe the death condition of mite when 0.5h, 1h, 1.5h, 2h, 2.5h respectively, calculate lethality, repeated test 3 times.

Embodiment 5 tests contain the acaricidal activity of the spray of caryophyllus oil

Caryophyllus oil is dissolved in be made into 2,3,4 in the ethanol, the spray of 5mg/ml, the adult acarid of some (60 ± 10) places paper, glass, pottery, silk fabric surface respectively, the spray of variable concentrations is sprayed once above about distance acarid 30cm, observes the death condition of acarid behind the 2.5h.

Effectively kill the separation of acaricidal composition in embodiment 6 caryophyllus oils

At first use silica gel-adsorption chromatography initial gross separation caryophyllus oil, TLC detects and finds that composition mainly concentrates on two sections, after the ratio of adjustment eluent benzinum and ethyl acetate two sections is separated.Do the acaricidal activity test respectively, the composition of acarid lethal dose 100% is further separated with HPLC, pillar is a μ Bio-sil post, and with n-hexane/ethyl acetate (8: 2, v/v, 2 mL/min) wash-out, 286nm detects.The composition of the acaricidal activity that is separated to carries out structure again to be identified.

Claims (4)

1. the novel miticide of dirt mites such as the indoor dermatophagoides pteronyssinus of effective dissipation, dust mite, it is characterized in that with China's tradition Chinese herbal medicine be raw material in conjunction with the modern times extract, preparation technology is refining forms.

2. miticide according to claim 1, it is characterized in that drawing materials into cloves, tealeaves, caraway, fennel seeds, peppermint, rose, geranium, kuh-seng, Chinese prickly ash, the tuber of stemona, betel nut, frutus cnidii, chaulmoogra, Fructus meliae toosendan, black false hellebore, hairyvein agrimony, the coptis, geranium, lemon grass (Cymbopogon citratus), rosemary,, the traditional Chinese herbal medicine of China such as eucalyptus leaves, coffee bean, thyme, wrinkled giant hyssop, dried orange peel, golden cypress, the root of Chinese wild ginger, the fruit of Rangoon creeper, Chinese cassia tree.

3. miticide according to claim 1 is characterized in that it mainly kills acaricidal composition is all eugenol compounds and various derivative thereof.

Eugenol

4. according to the described acaricidal preparation method of claim 1, it is characterized in that may further comprise the steps:

(1) extracts solvent and comprise that benzinum (I), benzinum (II), n-hexane, cyclohexane are equal to the isopolarity solvent;

(2) method of Ti Quing comprises similar extracting method such as leaching method, cable-styled extraction method, supercritical extraction;

(3) method of HPLC and MS combination is mainly adopted in the analysis of active ingredient, and the HPLC fingerprint pattern technology is mainly adopted in the control of quality;

(4) with CH ₃(CH ₂) _nOH is secondary solvent (n=0-5), C _nH _N+2Be high pressure vapor (n=2-10) that the sealing tinning makes finished product.