CN110200960A - Genistein is preparing the purposes in the drug for preventing or treating African swine fever - Google Patents

Genistein is preparing the purposes in the drug for preventing or treating African swine fever Download PDF

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Publication number
CN110200960A
CN110200960A CN201910524468.3A CN201910524468A CN110200960A CN 110200960 A CN110200960 A CN 110200960A CN 201910524468 A CN201910524468 A CN 201910524468A CN 110200960 A CN110200960 A CN 110200960A
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CN
China
Prior art keywords
genistein
drug
purposes
swine fever
african swine
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Pending
Application number
CN201910524468.3A
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Chinese (zh)
Inventor
李荣立
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Individual
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Individual
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Priority to CN201910524468.3A priority Critical patent/CN110200960A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses

Abstract

The present invention provides Genistein and is preparing the purposes in the drug for preventing and treating African swine fever.Wherein, for Genistein when preparing the purposes in the drug for preventing African swine fever, dosage is the 1-2g/ previous day.For Genistein when preparing the purposes in the drug for treating African swine fever, dosage is the 2-20g/ previous day, and 7 days dosages of a dosage period are that preceding 2 days dosages are the 2-4g/ previous day, and latter 5 days are the 4-20g/ previous day.The present invention also provides Genisteins and other compositions use in conjunction to prepare the purposes in the pharmaceutical preparation for preventing and treating African swine fever jointly.

Description

Genistein is preparing the purposes in the drug for preventing or treating African swine fever
Technical field
The present invention relates to a kind of medicinal usage more particularly to Genistein in preparation for preventing or treating African swine fever Drug in purposes, belong to pharmaceutical technology field.
Background technique
Genistein is dissolved in DMSO and ethyl alcohol, is practically insoluble in water, and structure is as follows:
Genistein is derived from the isoflavone compound of bean and dentation plant, chemistry entitled 4 ', 5,7- Trihydroxy-isoflavone.Genistein have prevent early atherosclerosis and chronic vascular disease, antitumor, women's climacteric The multiple pharmacological effects such as phase syndrome and bioactivity.Genistein is strength tyrosine protein kinase and topoisomerase Inhibitor, by the regulation to oncogene, to realize that multipath inhibits the growth and transfer of tumour.In vitroandin vivotrial and Epidemiology shows that Genistein has inhibiting effect to kinds of tumors, such as breast cancer, prostate cancer, kidney, gastric cancer, knot The carcinoma of the rectum, bladder cancer, lung cancer, uterine cancer, cutaneum carcinoma, leukaemia, lymthoma, neuroblastoma and head and neck cancer etc..
Genistein is practically insoluble in water, poor water solubility, the system being prepared by traditional formulation method Agent, it is difficult to reach the bioavilability for the treatment of diseases demands after oral administration, while also greatly limit the type that preparation is made, such as The dosage forms such as soluble powder or intravenous administration formulation.In addition, the content of Genistein in the formulation is lower, and controlled to reach Drug concentration is treated, curative effect can only be improved by increasing the dosage of preparation, but increase hair again to a certain extent in this way The risk of raw adverse reaction, but also will increase drug cost.
African swine fever (African Swine fever, East African Swine fever, ASF), is a kind of urgency Property, generate heat the very high filterable virus of infectiousness caused by swine disease, it is characterized in that pathogenic process is short, but the death rate is up to 100%, clinical manifestation is fever, skin cyanosis, lymph node, kidney, the obvious bleeding of gastrointestinal mucosa.
In recent years, though have part treatment African swine fever medicament research and development come out, its therapeutic effect is slow, the state of an illness easily repeatedly, Treatment is not thorough, and African swine fever rapid onset, infectiousness are strong, and mortality in acute phase is high, and the animal of virus infection can treated mostly It is dead in the process, though part infection pig remission, but the probability of disease relapse is larger, and some drugs contain a large amount of resist Raw element, after medication, causes to leave a large amount of antibiotic in vivo.On the other hand, the Chinese materia medica preparation mouth currently used for treatment African swine fever It is poor to take therapeutic effect, and most Antibacterial Constituents can be digested system fast decoupled and metabolism, lose therapeutic effect.Mesh Before, there are no the oral drug for developing quick, thorough, efficient and safe treatment African swine fever, infect after African swine fever only Slaughter at once, the anti-spread path of isolation can be taken.
Summary of the invention
The present invention provides efficient one kind, quick, cure rate height and safety to solve above-mentioned problems of the prior art Treatment African swine fever method.
The present invention provides Genistein and is preparing the purposes in the drug for preventing and treating African swine fever.
Wherein, the Genistein is preparing the purposes in the drug for preventing African swine fever, dosage 1- The 2g/ previous day.
Wherein, the Genistein is preparing the purposes in the drug for treating African swine fever, dosage 2- The 20g/ previous day.
Above-mentioned Genistein is 7 days preparing the purposes in the drug for treating African swine fever, a dosage period, It can be according to state of an illness interruption or continual administration multiple periods.
Wherein, the Genistein is preparing the purposes in the drug for treating African swine fever, a dosage period 7 It dosage is that preceding 2 days dosages are the 2-4g/ previous day, and latter 5 days are the 4-20g/ previous day.
Above-mentioned Genistein is preparing the purposes in the drug for preventing or treating African swine fever, and the drug is straight Connect and take or taken as additive, form be tablet, capsule, suspension, solution, emulsion, injection, ointment, Gelling agent, film, pill, granule or powder.
Further, Genistein is preparing the purposes in the drug for preventing or treating African swine fever, the medicine Contain Genistein inclusion compound in object, which is made of Genistein and inclusion agents, the use of the two Amount is in parts by weight are as follows: 1-100 parts of Genistein, 5-800 parts of inclusion agents;Wherein, the inclusion agents are selected from cyclodextrin or ring Dextrin derivative is selected from alpha-cyclodextrin, gamma-cyclodextrin, hydroxyethyl-β-cyclodextrin, hydroxypropyl-β-cyclodextrin, dihydroxypropyl β- Cyclodextrin, methyl-B-cyclodextrin, glucose ring dextrin, maltose cyclodextrin, maltotriose cyclodextrin, carboxymethyl cyclodextrin, sulphur The combination of one or more of alkyl cyclodextrins;Inclusion agents are more preferably hydroxypropyl-β-cyclodextrin, dihydroxypropyl β-ring The combination of dextrin or hydroxypropyl-β-cyclodextrin and glucose ring dextrin by weight 1:2.
Further, Genistein is preparing the purposes in the drug for preventing or treating African swine fever, the medicine In object contain Genistein solid dispersions, the Genistein solid dispersions by Genistein and matrix preparation and At the two weight ratio is 1:2-6, and the matrix is selected from Macrogol 6000, Macrogol 4000, polyethylene glycol 2000, gathers In ethylene glycol 1500, cetomacrogol 1000, odium stearate, glycerin gelatine, poloxamer, stearic acid and glycerol monostearate acid It is one or more of;It is preferred that Macrogol 4000.
The present invention also provides Genisteins and the Genistein and other compositions use in conjunction to prepare for preventing With the purposes in the pharmaceutical preparation for the treatment of African swine fever, the other compositions are selected from lauric monoglyceride, gallic acid laurel One or more of alcohol ester, apiolin, L- carragheen, L- Polaprezinc, resveratrol, phenylbutyrate sodium or Enrofloxacin.
Present invention firstly discovers that Genistein has good prevention or therapeutic effect for African swine fever, there is treatment Effect is fast, control the state of an illness be not easy repeatedly, thorough treatment, it is highly-safe the advantages that, solve at present treatment African swine fever technology The problems such as existing therapeutic effect is poor.
Specific embodiment
Following embodiments of the invention be only to clearly illustrate example of the present invention, and not be to the present invention Embodiment restriction.For those of ordinary skill in the art, it can also make on the basis of the following description Other various forms of variations or variation.There is no necessity and possibility to exhaust all the enbodiments.And these belong to this The obvious changes or variations that the spirit of invention is extended out are still in the protection scope of this invention.
Embodiment 1: the preparation of Genistein dry suspensoid agent
Prescription information
Preparation method:
Genistein is added in 300ml ethyl alcohol, stirring and dissolving, it is rear that beta-cyclodextrin and magnetic agitation is added, then It is concentrated, dry, pulverize, cross 120 meshes;Filler, disintegrating agent, suspending agent sieve with 100 mesh sieve respectively, spare.By the title of recipe quantity Genistein inclusion compound, lactose and mannitol, carboxyrnethyl starch sodium, xanthan gum mixing are taken, stirring 30 minutes or more, mixing was equal It is even.The saccharin sodium of recipe quantity, flavoring pineapple essence are set in remaining ethyl alcohol and dissolved, is adhesive, softwood processed.The granulation of 20 meshes, 55-60 DEG C drying;18 mesh sieves.Fill compound membrane bag or bottle.
Embodiment 2: the preparation of Genistein dry suspensoid agent
Prescription information
Preparation method:
Genistein is added in 720ml ethyl alcohol, stirring and dissolving, simultaneously magnetic force stirs rear addition hydroxypropyl-β-cyclodextrin It mixes, is then concentrated, dry, pulverize, cross 120 meshes;Filler, disintegrating agent, suspending agent sieve with 100 mesh sieve respectively, spare.By prescription Amount weighs Genistein inclusion compound, sucrose and mannitol, hydroxypropul starch, xanthan gum mixing, stirring 30 minutes or more, mixes It closes uniform.The stirring of 10% polyvinylpyrrolidone ethanol solution is added in the above-mentioned main and supplementary materials mixed, softwood processed.20 meshes Granulation, 55-60 DEG C of drying;18 mesh sieves.Fill compound membrane bag or bottle.
Embodiment 3: the preparation of genistein dripping pills
100g Macrogol 4000 is taken by prescription, sets heating melting in 80 DEG C of water-baths, the goldspink that 50g is added under stiring is different Flavine, stirring makes it be uniformly dispersed under 80 DEG C of heat preservations, and medical fluid is transferred in pill dripping machine constant temperature preserving jar, drips fast 60 drops/minute, Coolant is atoleine, under the conditions of coolant temperature is 15 DEG C, adjusts dripping pill ball weight 60mg, dripping pill is made, removes dripping pill table Face coolant, packing to get.
Embodiment 4: the preparation of genistein dripping pills
150g Macrogol 6000 is taken by prescription, sets heating melting in 80 DEG C of water-baths, the goldspink that 50g is added under stiring is different Flavine, stirring makes it be uniformly dispersed under 80 DEG C of heat preservations, and medical fluid is transferred in pill dripping machine constant temperature preserving jar, drips fast 60 drops/minute, Coolant is atoleine, under the conditions of coolant temperature is 5 DEG C, adjusts dripping pill ball weight 50mg, dripping pill is made, removes dripping pill surface Coolant, packing to get.
Embodiment 5: the preparation of Genistein capsule
Prescription information
Preparation method:
Genistein is added in 350ml ethyl alcohol, stirring and dissolving, simultaneously magnetic force stirs rear addition dihydroxypropyl beta-cyclodextrin It mixes, is then concentrated, dry, pulverize, cross 120 meshes;Filler, disintegrating agent, suspending agent sieve with 100 mesh sieve respectively, spare.By prescription Amount weighs Genistein inclusion compound, lactose and mannitol, carboxyrnethyl starch sodium, tragacanth mixing, stir 30 minutes or more, It is uniformly mixed.The saccharin sodium of recipe quantity, flavoring pineapple essence are set in remaining 60% ethyl alcohol and dissolved, is adhesive, softwood processed.20 meshes Granulation, 55-60 DEG C of drying;18 mesh sieves.Fill No. 0 capsule.
Embodiment 6: the preparation of Genistein capsule
Prescription information
Preparation method:
Genistein is added in 700ml ethyl alcohol, stirring and dissolving, it is rear that glucose ring dextrin and magnetic agitation is added, Then it is concentrated, dry, pulverize, cross 120 meshes;Filler, disintegrating agent, suspending agent sieve with 100 mesh sieve respectively, spare.By recipe quantity Weigh Genistein inclusion compound, lactose, it is low replace light propyl cellulose, xanthan gum mixing, stirring 30 minutes or more, mixing Uniformly.The saccharin sodium of recipe quantity, flavoring pineapple essence are set in remaining 60% ethyl alcohol and dissolved, is adhesive, softwood processed.20 mesh Shai Zhi Grain, 55-60 DEG C of drying;18 mesh sieves.Fill No. 0 capsule.
7 pharmacodynamic test 1 of embodiment
28 6 ± 1 monthly ages of pig farm, 80 ± 5kg of weight, the boar for infecting disease stage African swine fever early period, this stage Symptom predominantly generate heat (up to 40~42 DEG C), be slow in action, appetite is low, expiratory dyspnea, part cough, eye, nose have serosity or Mucopus sexual secretion.
28 pigs are divided into 4 groups, every group 7, oral medication are carried out to every group of pig, administration mode is as follows:
1st group: the dry suspensoid agent of 2 days daily 1g containing Genistein of embodiment 1 before every pig, latter 5 days daily The dry suspensoid agent of the 3g containing Genistein of embodiment 1 is taken, it is accumulative continuously to take 7,
2nd group: the dry suspensoid agent of 2 days daily 2g containing Genistein of embodiment 2 before every pig, latter 5 days daily The dry suspensoid agent of the 3g containing Genistein of embodiment 2 is taken, it is accumulative continuously to take 7,
3rd group: the capsule of 2 days daily 1g containing Genistein of embodiment 3 before every pig, latter 5 days daily The capsule of the 4g containing Genistein of embodiment 3, it is accumulative continuously to take 7,
4th group: the capsule of 2 days daily 1.5g containing Genistein of embodiment 4 before every pig often takes daily for latter 5 days It is accumulative continuously to take 7 with the capsule of the 8g containing Genistein of embodiment 4.
Shown in 4 groups of therapeutic effect table 1.
Table 1
Note: the normal body temperature of Adult Pig is 38 DEG C~39.5 DEG C
8 pharmacodynamic test 2 of embodiment
28 pigs after the treatment of embodiment 7 have no that any pig has recurrence after observing January.
The pharmacodynamic test of 9 drug combination of embodiment
28 6 ± 1 monthly ages of pig farm, 80 ± 5kg of weight, the boar for infecting disease stage African swine fever early period are taken, is divided into 4 Group, carries out oral medication to every group of pig, administration mode is on the basis of the administration of embodiment 7, and every adds 300mg by every group 7 Enrofloxacin, after even served 7 days, all pigs show that feed improves and body temperature is normal.And compared with the data of table 1, more Pig realizes feed improvement for 3 days before the treatment and body temperature is normal.After observing January, have no that any pig has recurrence.

Claims (10)

1. Genistein is preparing the purposes in the drug for preventing or treating African swine fever.
2. Genistein as described in claim 1 is preparing the purposes in the drug for preventing African swine fever, feature It is, dosage is the 1-2g/ previous day.
3. Genistein as described in claim 1 is preparing the purposes in the drug for treating African swine fever, feature It is, dosage is the 2-20g/ previous day.
4. Genistein as claimed in claim 3 is preparing the purposes in the drug for treating African swine fever, feature It is, a dosage period is 7 days.
5. Genistein as claimed in claim 4 is preparing the purposes in the drug for treating African swine fever, feature It is, 7 days dosages of a dosage period are that preceding 2 days dosages are the 2-4g/ previous day, and latter 5 days are 4-20g/ head It.
6. Genistein as described in claim 1 is preparing the purposes in the drug for preventing or treating African swine fever, It is characterized in that, the drug is directly to take or take as additive, form is tablet, capsule, suspension, solution Agent, emulsion, injection, ointment, gelling agent, film, pill, granule or powder.
7. Genistein as claimed in claim 6 is preparing the purposes in the drug for preventing or treating African swine fever, It is characterized in that, containing Genistein inclusion compound in the drug, the Genistein inclusion compound is by Genistein and packet Mixture composition, the dosage of the two is in parts by weight are as follows: 1-100 parts of Genistein, 5-800 parts of inclusion agents.
8. Genistein as claimed in claim 7 is preparing the purposes in the drug for preventing or treating African swine fever, It is characterized in that, the inclusion agents are selected from cyclodextrin or cyclodextrine derivatives, it is selected from alpha-cyclodextrin, gamma-cyclodextrin, ethoxy- Beta-cyclodextrin, hydroxypropyl-β-cyclodextrin, dihydroxypropyl beta-cyclodextrin, methyl-B-cyclodextrin, glucose ring dextrin, malt saccharide ring The combination of one or more of dextrin, maltotriose cyclodextrin, carboxymethyl cyclodextrin, sulfoalkyl cyclodextrin.
9. Genistein as claimed in claim 6 is preparing the purposes in the drug for preventing or treating African swine fever, It is characterized in that, containing Genistein solid dispersions in the drug, the Genistein solid dispersions are different by goldspink Flavine and matrix are prepared, the two weight ratio be 1:2-6, the matrix be selected from Macrogol 6000, Macrogol 4000, Polyethylene glycol 2000, polyethylene glycol 1500, cetomacrogol 1000, odium stearate, glycerin gelatine, poloxamer, stearic acid and list One or more of glycerol stearate acid.
10. Genistein as described in claim 1 is preparing the purposes in the drug for preventing or treating African swine fever, It is characterized in that, the Genistein and other compositions use in conjunction;The other compositions are selected from lauric monoglyceride, do not have One in gallate-based laurel alcohol ester, apiolin, L- carragheen, L- Polaprezinc, resveratrol, phenylbutyrate sodium or Enrofloxacin Kind is several.
CN201910524468.3A 2019-06-18 2019-06-18 Genistein is preparing the purposes in the drug for preventing or treating African swine fever Pending CN110200960A (en)

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CN201910524468.3A CN110200960A (en) 2019-06-18 2019-06-18 Genistein is preparing the purposes in the drug for preventing or treating African swine fever

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112089726A (en) * 2020-08-18 2020-12-18 河南佰景生物科技有限公司 Application of special amino acid derivative in preparation of preparation for preventing and controlling African swine fever
US20220273573A1 (en) * 2020-10-16 2022-09-01 Humanetics Corporation Solid dispersion genistein compositions and methods of making and using the same

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
JOÃO COELHO等: "Functional characterization and inhibition of the type II DNA topoisomerase coded by African swine fever virus", 《VIROLOGY》 *
新乡大北农: "你必须知道丨这些疫苗和药物或能有效控制非洲猪瘟!", 《HTTPS://WWW.SOHU.COM/A/291070614_769261》 *
杨有福: "防治非洲猪瘟疫苗和药物还有多远?", 《微信公众号:PSY应用研究院》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112089726A (en) * 2020-08-18 2020-12-18 河南佰景生物科技有限公司 Application of special amino acid derivative in preparation of preparation for preventing and controlling African swine fever
US20220273573A1 (en) * 2020-10-16 2022-09-01 Humanetics Corporation Solid dispersion genistein compositions and methods of making and using the same

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Application publication date: 20190906