CN113855668A - An antiviral and antibacterial cantharidin preparation, its preparation method, and its application in preventing and treating coronavirus infection - Google Patents

An antiviral and antibacterial cantharidin preparation, its preparation method, and its application in preventing and treating coronavirus infection Download PDF

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Publication number
CN113855668A
CN113855668A CN202110545158.7A CN202110545158A CN113855668A CN 113855668 A CN113855668 A CN 113855668A CN 202110545158 A CN202110545158 A CN 202110545158A CN 113855668 A CN113855668 A CN 113855668A
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cantharidin
oil
solution
water
following components
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王卫
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Gansu Yuanmei Pharmaceutical Co ltd
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Gansu Yuanmei Pharmaceutical Co ltd
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Priority to PCT/CN2021/095429 priority Critical patent/WO2021238836A1/en
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    • A61K35/644—Beeswax; Propolis; Royal jelly; Honey
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    • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/481—Astragalus (milkvetch)
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Abstract

An antiviral and antibacterial cantharidin preparation comprises cantharidin as effective component, which is dissolved in oil-water or oil-oil to obtain cantharidin solvent carrier, and can be mixed with pharmaceutically acceptable carrier or excipient to make into antiviral and antibacterial preparations. The medicine can be used for preventing and treating the infection of the novel coronavirus, and the cantharidin solvent carrier can also be used as a solution for preparing an ecological antibiotic inactivated vaccine for resisting the novel coronavirus.

Description

An antiviral and antibacterial cantharidin preparation, its preparation method, and its application in preventing and treating coronavirus infection
Technical Field
The invention relates to the field of biological pharmacy, and particularly provides a cantharidin antiviral and antibacterial preparation and a preparation method thereof. The preparation provided by the invention can be used as a medicine for preventing and treating antivirus and antibiosis. In particular, the compound also has important prevention and treatment effects on infection of novel coronavirus, influenza virus, Ebola virus, AIDS virus and other pathogens.
Background
Cantharidin is a defensive substance of animals, is a high-efficiency, low-toxicity and broad-spectrum antiviral and antibacterial bioactive raw material medicine, and is recorded in China for a long time in medicine.
Records of Shen nong Ben Cao Jing and Ben Cao gang mu: cantharis, turnip, elephantopus … …, relieve furunculosis; Canine Virus … … ".
Cantharidin is also a raw material medicine of modern western medicines. One hundred years ago, the western medicien has purified cantharidin and studied its physical properties and chemical structure, and clinically characterized this defensive substance of insects of the family of the lilac as "skin irritant, vesicant".
The ability to make defensive substances resistant to various microorganisms, not exclusively present in animals; i.e., the subgenus, and even bacteria (Pasteur and Joubert, 1877) can sometimes produce substances that inhibit or prevent the growth of other species of microorganisms. Such substances are collectively referred to as Antibiotics (Antibiotics).
Inspired by the ancient and modern medical achievements, the inventor establishes a medical research topic of cantharidin as an antibiotic in 1959. In 1963, animal antiviral experiments for cantharidin experimental study were started in rural areas. In 1971, cantharidin fat-soluble 'hospital preparations' were used in rural primary medical institutions to conduct research combining antiviral and antibacterial clinical practice with scientific research.
In 1974 of Shanghai, the pharmaceutical standards of the water-soluble agent, cantharidin tablet and cantharidin injection, were produced in batches. For the treatment of tumors, the daily dose is 4.0mg for a patient of 60kg body weight.
The inventor published cantharidin-antiviral antibiotic in the journal of nature 6 in 1980.
"four new drugs" antiviral drug "cantharidin cream" was produced in batches by Ministry of health in 1991, 12 and 5 months.
A large number of clinical verifications show that the cantharidin cream has obvious effects of defervescence, antiemetic and antidiarrheal when used for treating infantile autumn diarrhea. After treatment, the effective rate is 97% within 48 hours, the average improvement time is 23.4 hours, the antiemetic time is 19.7 hours, the antipyretic time is 18.75 hours, and the disease course is obviously shortened. The external treatment can also avoid the difficulty of taking medicine caused by the vomiting of children patients. No local adverse reaction and other toxic and side effects of the skin are found during the treatment period. The cantharidin cream for treating infantile diarrhea is a safe and effective medicine.
The inventor researches cantharidin antiviral and antibacterial series preparations prepared by using oil and essential oil in the work of researching cantharidin antiviral and antibacterial series preparations and searching a cantharidin solvent carrier, and obtains ZL90106365.7 and 01140066.8 patents. However, the research on cantharidin antiviral and antibacterial series preparations finds a cantharidin solvent carrier until essential oil is applied, and an ideal cantharidin solvent carrier is far from being obtained.
The maximum solubility of cantharidin in water is 33.33 ppm; after the research of more than 50 years, the preparation of cantharidin with human body external target drug effect is prepared by only using water as a cantharidin solvent carrier, and the highest drug concentration of the cantharidin can reach 33.33ppm after the water is volatilized, so that compared with the conclusion of a large amount of long-term cantharidin toxicological research on cantharidin, the data that the drug concentration of cantharidin at the human body target is less than or equal to 5.6ppm, the obvious drug concentration is too high. Therefore, the cantharidin preparation which is simply dissolved in water is changed into a vesicant with toxic and side effects when applied to a target point outside a human body, and the due treatment effect of the cantharidin cannot be generated.
At present, the novel coronavirus (COVID-19) has been abused worldwide, and although there is evidence that Reidsvir, chloroquine and some traditional Chinese medicines have certain curative effects on inhibiting the novel coronavirus, the large-scale spread of the virus cannot be prevented. The hope of controlling new coronaviruses is therefore held in the development of vaccines as soon as possible. In the preparation of vaccines, one is inactivated vaccine, which is the most traditional vaccine, and the pathogen loses activity, so the vaccine has good safety and simplicity in clinical application. One of the key steps in the development of vaccines against novel coronaviruses is the search for a carrier that inhibits or kills the infection of novel coronaviruses pathogens to the human body while sparing the normal physiological functions of the human body.
To date, there has been no report on the use of cantharidin as a drug for preventing and treating infection by pathogens such as novel coronavirus and the use of cantharidin as an ecological antibiotic solution for preparing vaccines against novel coronavirus.
Disclosure of Invention
In order to solve the problems of the cantharidin in pharmacy and toxicology, the inventor finds that the preparation prepared by selecting the oil-oil mutual dissolving body or the oil-water mutual dissolving body as the solvent carrier of the cantharidin overcomes the problems of the cantharidin in pharmacy and toxicology and can ensure that the high-efficiency antiviral and antibacterial efficacies of the cantharidin are safely and ideally exerted.
When the oil is selected, one oil is simply applied, the requirements of cantharidin pharmacy, pharmacology and toxicology can not be met, and the oil conforming to the physicochemical property of cantharidin must be selected from various oils to achieve the purpose of obviously improving the pharmacological action of cantharidin.
According to records of synthesized practical spice handbooks, at present, more than 1700 spices which are recognized to be safe to eat abroad are provided. The method comprises the following steps: hydrocarbons and their derivatives, alcohols, ethers, phenols and their derivatives, aldehydes, acetals, ketones, lactones, acids, esters, sulfur-and nitrogen-containing compounds … …. Through years of experimental research, the invention finds that only ketone and lactone essential oils are suitable to be used as solvent carriers of cantharidin and have certain practicability.
The invention selects oil-oil mutual solution and oil-water mutual solution as solvent carrier of cantharidin, and the oil and the essential oil applied in cantharidin pharmacy, toxicology and pharmacodynamics are obviously improved compared with those applied in patent ZL90106365.7 and 01140066.8 invention patents.
In order to provide a medicament for preventing and treating novel coronavirus and an ecological antibiotic solution for preparing a vaccine against the novel coronavirus, the first aspect of the invention is to provide a cantharidin antiviral and antibacterial preparation, which comprises cantharidin as an effective medicinal ingredient, wherein the cantharidin is dissolved in an oil-water mutual solution or an oil-oil mutual solution to obtain a cantharidin solvent carrier, and the cantharidin solvent carrier and a medicinal carrier or excipient are prepared into a plurality of dosage forms to be used as the medicament for preventing and treating the novel coronavirus.
Preferably, the oil-in-water solution or oil-in-oil solution contains essential oils of ketones and/or lactones.
In a second aspect of the present invention, there is provided a cantharidin skin absorption paint for preventing and treating a novel coronavirus, comprising cantharidin as an effective pharmaceutical ingredient, a cantharidin solvent carrier being an oil-water mutual solution, comprising:
cantharidin: 160-200mg
Vegetable oil: 8.0-12.0g
Animal oil: 8.0-12.0g
Ketone essential oil: 40.0-60.0g
Octadecanol: 20.0-40.0g
Stearic acid: 20.0-40.0g
Emulsifier (Tween-80) 40-60.0g
And (3) the rest of distilled water: total 1000.0g
Making into transdermal absorption liniment containing cantharidin 0.16-0.2mg per gram.
The third aspect of the present invention provides an intravenous injection for treating novel coronavirus, which is an oil-water mutual-dissolving cantharidin solvent carrier, and contains cantharidin as an effective medicine component, and comprises the following components:
cantharidin: 15.0-30.0mg
2-butanone: 30.0-60.0g
3-heptanone: 0.3-0.6g
2-sec-butylcyclohexanone: 0.3-0.6g
The balance of physiological water for injection: the total amount was 16000.00 g.
In a fourth aspect of the present invention, there is provided a cantharidin tablet for treating a novel coronavirus in which an oil-oil mutual-dissolution body is a cantharidin solvent carrier, comprising cantharidin as an effective pharmaceutical ingredient, comprising:
cantharidin: 200.0-300.0mg
Cocoa butter: 80.0-120.0g
Olive oil: 60.0-90.0g
2-butanone: 60.0-90.0g
2-sec-butylcyclohexanone: 200.0-300.0g
Starch: 3200.0-4800.0g
Gluten powder: 320.0-480.0g
The total amount of the prepared materials is as follows: 10000 tablets; each tablet is 0.392-0.588g cantharidin tablet.
The fifth aspect of the present invention provides a cantharidin capsule as a cantharidin solvent carrier in oil-oil mutual solution for treating novel coronavirus, containing cantharidin as an effective pharmaceutical ingredient, comprising:
cantharidin: 200.0-300.0mg
Deodorizing beef tallow: 80.0-120.0g
Olive oil: 60.0-90.0g
2-butanone: 60.0-90.0g
6-hydroxy-3, 7-dimethyl octanoic acid lactone: 200.0-300.0g
Starch: 3200.0-4800.0g
Gluten powder: 320.0-480.0g
The total amount of the prepared materials is as follows: 10000 capsules, each capsule weighing 0.392-0.588g cantharidin.
The sixth aspect of the present invention provides a cantharidin nasal-ocular spray using an oil-water mutual-dissolving vehicle as a cantharidin solvent carrier for preventing novel coronavirus, containing cantharidin as an effective pharmaceutical ingredient, comprising:
cantharidin: 1.6-3.2mg
375.0-525.0g of 95% ethanol
2-butanone: 80.0-120.0g
Propylene glycol: 495.0-725.0g
Benzyl alcohol: 6.0-12.0g
2-phenethyl alcohol: 6.0-12.0g
Raspberry ketone: 3.0-6.0g
The balance of distilled water: the total amount of the cantharidin nasal and ocular spray is 10000.0 g.
The seventh aspect of the present invention provides a cantharidin nose-eye medicinal oil which is used for preventing novel coronavirus and takes cantharidin solvent carrier as oil-oil mutual dissolving body, containing cantharidin as effective medicinal ingredients, comprising:
cantharidin: 2.2-3.6mg
2-butanone: 80.0-120.0g
Raspberry ketone: 3.0 to 6.0g of a mineral,
the rest is olive oil: making into cantharidin nose eye medicinal oil 1000.0g in total amount.
The eighth aspect of the present invention provides a cantharidin solution disinfectant wipe as a cantharidin solvent carrier for oil-water mutual dissolution for preventing novel coronavirus, containing cantharidin as an effective pharmaceutical ingredient, comprising:
cantharidin: 1.0-2.6mg
500.0-600.0g of 95% ethanol
2-butanone: 40.0-60.0g
Propylene glycol: 425.0-525.0g
Benzyl alcohol: 8.0-10.0g
2-phenethyl alcohol: 8.0-10.0g
Raspberry ketone: 2.0-4.0g
The balance was distilled water to obtain 10000.0 g. Spraying the obtained solvent on the carrier to obtain cantharidin solution sterilized cloth towel.
The ninth aspect of the present invention provides a cantharidin traditional Chinese and western medicine combined oral pill for treating the novel coronavirus, which contains cantharidin as an effective medicine component, wherein a cantharidin solvent carrier is an oil-oil mutual solution and comprises the following components:
the cantharidin solution comprises the following components:
cantharidin: 330.0mg
Olive oil: 20.0g
Cocoa butter: 10.0g
Gamma-lactone: 6.0g
2-butanone: 30.0g
2-sec-butylcyclohexanone: 60.0g
The cantharidin traditional Chinese and western medicine combined oral pill comprises the following components:
cantharidin solution (containing cantharidin 330.0mg) 126.0g
Starch: 2000.0g
Gluten powder: 274.0g
Astragalus extract: 100.0g
Chinese bee honey: 2500.0g
Making into cantharidin Chinese and western medicinal oral pill 1000 pills, each pill containing cantharidin 0.33 mg.
The tenth aspect of the invention provides a household and soldier stock cleaning agent capable of preventing trauma infection by mutual dissolution of oil and water, which is characterized in that the solution is cantharidin oil-water mutual solution and comprises the following components:
cantharidin: 1.6-3.2mg
375.0-525.0g of 95% ethanol
2-butanone: 80.0-120.0g
Propylene glycol: 495.0-725.0g
Benzyl alcohol: 6.0-12.0g
2-phenethyl alcohol: 6.0-12.0g
Raspberry ketone: 3.0-6.0g
The balance of distilled water. The preparation method comprises the following steps: the total amount of the cantharidin is 10000.0g, and the cantharidin is a conventional cleaning agent for families and soldiers who prevent trauma infection.
The eleventh aspect of the invention provides a cantharidin antiviral and antibacterial intangible condom for preventing HIV sexual behavior infection, which is characterized in that the solution is cantharidin oil-water mutual solution, and comprises the following components:
cantharidin: 16.0-36.0mg
100.0-300.0g of 95% ethanol
Propylene glycol: 495.0-725.0g
Glycerol: 495.0-725.0g
Lactic acid: 1000.0g
Sodium lactate: 2000.0g
Benzyl alcohol: 16.0-21.0g
2-phenethyl alcohol: 6.0-12.0g
Hyaluronic acid: 30.0-120.0 g
Guar gum: 10.0-40.0 g
The balance of distilled water, and the preparation method comprises the following steps: the total amount is 10000.0g, and the cantharidin intangible condom for preventing HIV sexual behavior infection.
The twelfth aspect of the invention provides a cantharidin antibiotic solution for preparing an anti-novel coronavirus inactivated vaccine, which contains cantharidin as an effective medicinal ingredient and contains the cantharidin of not more than 1.6ppm and not more than 3.6 ppm.
Preferably, the solution containing cantharidin of 1.6ppm or more and cantharidin of 3.6ppm or less is cantharidin oil-oil or cantharidin oil-oil.
Preferably, the oil-oil miscible body is a cantharidin solvent carrier, comprising: 2-butanone and olive oil, wherein the cantharidin content is 1.6-3.6ppm, the 2-butanone content is 8-12 wt%, and the balance is the olive oil.
Preferably, the oil-water miscible body is a cantharidin solvent carrier, comprising: cantharidin with content of 1.6-3.6 ppm; 3.75 to 5.2 percent of ethanol by weight; 2-butanone in the content: 0.8-1.2 wt%; propylene glycol, the content is: 4.95-7.25 wt%; benzyl alcohol, content: 0.06-0.12 wt%; 2-phenethyl alcohol, the content is: 0.06-0.12 wt%; raspberry ketone, the content is: 0.03.-0.06 wt%; the balance of distilled water.
The thirteenth aspect of the present invention provides a process for preparing a cantharidin antibiotic solution for inactivated vaccine against novel coronavirus, which comprises dissolving a certain amount of cantharidin and 2-butanone in olive oil, adding olive oil until the cantharidin content is 1.6-3.6ppm, the 2-butanone content is 8-12 wt%, and the rest is the cantharidin antibiotic solution of olive oil.
The fourteenth aspect of the present invention provides a preparation method of cantharidin antibiotic solution for preparing inactivated vaccine against new coronavirus, which is prepared by dissolving a certain amount of cantharidin in 1.6-3.6 ppm; 3.75 to 5.25 percent of ethanol by weight; 2-butanone in the content: 0.8-1.2 wt%; propylene glycol, the content is: 4.95-7.25 wt%; benzyl alcohol, content: 0.06-0.12 wt%; 2-phenethyl alcohol, the content is: 0.06-0.12 wt%; raspberry ketone, the content is: 0.03.-0.06 wt%; dissolving in distilled water, and adding distilled water to obtain cantharidin antibiotic solution.
The cantharidin solvent with the concentration less than or equal to 5.6ppm is used as a solution and can be used for preparing antibiotic 'ecological' inactivated vaccines. The solution is used for inactivating pathogens to prepare virus or bacteria inactivated vaccines by using the ecological biological activity of the cantharidin solution without using a physical method or a chemical method. In ecological theory, compared with the inactivated vaccine by high temperature or chemical method, the antigenicity of the invention is more ideal, and the invention is a new technical route for manufacturing the inactivated vaccine which is highly worthy of test.
The technical solution of the present invention will be further described below by way of examples.
Detailed Description
The exemplary embodiments will be described herein in detail, and the embodiments described in the following exemplary embodiments do not represent all embodiments consistent with the present invention. They are merely examples that further illustrate the cantharidin antibiotic solutions and methods of formulating the same in accordance with aspects of the present invention in detail.
The starting materials used in the following examples:
1. the cantharidin is refined cantharidin obtained by the prior art (ZL patent No. 90106365.7 or 01140066.8).
2. Other raw materials are refined industrial products.
Example 1
The cantharidin skin absorption coating agent of oil-oil mutual dissolving body is prepared by the following components:
cantharidin: 160.0-200.0mg
Vegetable oil: 8.0-12.0g
Animal oil: 8.0-12.0g
Ketone essential oil: 40.0-60.0g
Octadecanol: 20.0-40.0g
Stearic acid: 20.0-40.0g
Emulsifier (Tween-80) 40-60.0g
And (3) the rest of distilled water: total 1000.0g
Making into skin absorption liniment containing cantharidin 0.16-0.2mg per gram.
The skin absorption liniment is applied to chest, back and limbs of 60kg adult by applying for three times per day, 2.0g for each time, and the skin absorption liniment contains cantharidin 0.32-0.4 mg. The preparation enters blood circulation through lymphatic system, exerts drug effect on cantharidin human viscera target spot, and can be used for treating respiratory system infection such as influenza, etc., with remarkable curative effect. Can be preferably used for treating infection of virus and germ such as novel coronavirus and influenza virus.
Example 2
The intravenous injection with oil-water mutual solution as cantharidin solvent carrier is prepared from the following components:
cantharidin: 15.0-30.0mg
2-butanone: 30.0-60.0g
3-heptanone: 0.3-0.6g
2-sec-butylcyclohexanone: 0.3-0.6g
The balance of physiological water for injection, the total amount is 16000.00 ml.
For patients infected by virus and germ in lung, the cantharidin anti-infective preparation is suitable for alternate application or combination with other cantharidin anti-infective preparations in rescue. Intravenous injection is 100.0-160.0ml per day (0.1-0.3 mg per day based on cantharidin). Can be used for treating infection of virus and bacteria such as novel coronavirus and influenza virus.
Example 3
The cantharidin tablet with oil-oil mutual dissolving body as cantharidin solvent carrier is prepared with the following components:
cantharidin: 200.0-300.0mg
Olive oil: 60.0-90.0g
2-butanone: 60.0-90.0g
2-sec-butylcyclohexanone: 200.0-300.0g
Starch: 3200.0-4800.0g
Gluten powder: 320.0-480.0g
The total amount of the prepared materials is as follows: 10000 tablets; each tablet weighs 0.384-0.58 g.
The adult of 60kg is used for treating respiratory system viral and bacterial infection 2-3 times a day, and 8-16 tablets are taken once, which is equivalent to 0.32-1.44mg of pure cantharidin. Can be used for treating infection of virus and bacteria such as novel coronavirus and influenza virus.
Example 4
Preparing cantharidin capsules with an oil-oil mutual-dissolving body as a cantharidin solvent carrier, which comprises the following components:
cantharidin: 200.0-300.0mg
Deodorizing beef tallow: 80.0-120.0g
Olive oil: 60.0-90.0g
2-butanone: 60.0-90.0g
6-hydroxy-3, 7-dimethyl octanoic acid lactone: 200.0-300.0g
Starch: 3200.0-4800.0g
Gluten powder: 320.0-480.0g
The total amount of the prepared materials is as follows: 10000 granules, each granule weight is 0.392-0.588 g.
The adult of 60kg is used for treating respiratory system virus and bacterial infection 2-3 times a day, and 8-16 granules are taken once, which is equivalent to 0.32-1.44mg of pure cantharidin. Can be used for treating infection of virus and bacteria such as novel coronavirus and influenza virus.
Example 5
The preparation method of the oil-water-soluble trauma cleaning agent which is prepared for families and soldiers and is used for eradicating infection comprises the following components:
cantharidin: 1.6-3.2mg
375.0-525.0g of 95% ethanol
2-butanone: 80.0-120.0g
Propylene glycol: 495.0-725.0g
Benzyl alcohol: 6.0-12.0g
2-phenethyl alcohol: 6.0-12.0g
Raspberry ketone: 3.0-6.0g
The balance of distilled water, and the preparation method comprises the following steps: 10000.0g cantharidin in total is a conventional trauma cleaning agent for families and soldiers to avoid infection.
The preparation can be used for cleaning wounds and preventing trauma infection, and is proved to be very effective by long-term clinical practice. Can also be sprayed to nose and eyes for preventing and treating infection of virus and bacteria such as novel coronavirus and influenza virus. Is a sanitary cleaning product for families and soldiers.
Example 6
Preparing cantharidin nose-eye medicinal oil with oil-oil mutual solubility, which comprises the following components:
cantharidin: 2.2-3.6mg
2-butanone: 80.0-120.0g
Raspberry ketone: 3.0 to 6.0g of a mineral,
and the balance of olive oil, and the preparation method comprises the following steps: the total amount is 1000.0g cantharidin nose eye medicinal oil.
The preparation can be used for wrapping up trauma, is applied to surgical treatment rooms in hospitals and rural primary medical institutions, is applied to the preparations in medical institutions for a long time, has tens of thousands of cases of clinical practices, does not show a case of wound infection treated by the preparation, and shows that the preparation can be used for trauma and can completely kill viruses and bacteria capable of infecting people. It is preferably used for preventing infection of virus and bacteria such as novel coronavirus and influenza virus.
Example 7
The cantharidin solution disinfectant cloth towel is prepared, wherein the cantharidin is 1.0-2.6ppm, and the preparation method of the oil-water miscible solution comprises the following steps:
cantharidin: 1.0-2.6mg
500.0-600.0g of 95% ethanol
2-butanone: 40.0-60.0g
Propylene glycol: 425.0-525.0g
Benzyl alcohol: 8.0-10.0g
2-phenethyl alcohol: 8.0-10.0g
Raspberry ketone: 2.0-4.0g
The balance of distilled water, and the preparation method comprises the following steps: 10000.0g total, and cantharidin 1.0-2.6ppm solution.
Soaking cotton fabric in the above solution to obtain cantharidin solution sterilized cloth towel. The cloth can be used as inner lining of mask for preventing infection of new coronavirus and influenza virus.
Example 8
Preparation of cantharidin Chinese and western medicine combined oral pill
Preparation of oil-oil miscible cantharidin solution:
cantharidin: 330.0mg
Olive oil: 20.0g
Cocoa butter: 10.0g
Gamma-lactone: 6.0g
2-butanone: 30.0g
2-sec-butylcyclohexanone: 60.0g
The preparation of the cantharidin traditional Chinese and western medicine combined oral pill comprises the following steps:
adding 330.0mg cantharidin into the combined oil, heating to 60-70 deg.C, maintaining for about 30 min until cantharidin is completely dissolved, and naturally cooling at room temperature to obtain oily mixed solution of cantharidin as main effective component of the pill.
Cantharidin solution (containing cantharidin 330.0mg) 126.0g
Starch: 2000.0g
Gluten powder: 274.0g
Astragalus extract: 100.0g
Chinese bee honey: 2500.0g
Making into cantharidin Chinese and western medicinal oral pill 1000 pills. Each pill contains cantharidin 0.33 mg. The dosage of the cantharidin is 0.66-1.0mg per day, and the dosage is 1 pill once for 60kg adult 2-3 times per day. It is preferably used for preventing infection of virus and bacteria such as novel coronavirus and influenza virus.
Example 9
The preparation of the cantharidin antibiotic solution for the ecological antibiotic inactivated vaccine comprises the following steps:
dissolving cantharidin 1.6-3.6mg and 2-butanone 80.0-120.0g, adding into olive oil 200g, stirring to dissolve, adding olive oil, and making into cantharidin solution with total amount of 1000.0g oil-oil miscible solution.
Example 10
The preparation of the cantharidin antibiotic solution for the ecological antibiotic inactivated vaccine comprises the following steps:
adding cantharidin 16.0-36.0mg, 95% ethanol 375.0-525.0g, 2-butanone 80.0-120.0g, propylene glycol 495.0-725.0g, benzyl alcohol 6.0-12.0g, 2-phenethyl alcohol 6.0-12.0g and raspberry ketone 3.0-6.0g into distilled water 1000g, stirring for dissolving, and adding distilled water to obtain cantharidin solution with total amount of 10000.0g oil-water miscible.
The cantharidin solution obtained in examples 9 and 10 was used as a parent for vaccine preparation, and pathogens were put into the solution separately and in groups according to conventional techniques, protected from light, kept at a constant temperature of 34-36 deg.C, and used for research experiments of various ways of cantharidin antibiotic "ecological" inactivated vaccines.
Examples of clinical applications
Since 1-5 months in 2020, the subject group has obvious effect on clinical application of 10 suspected people with the novel coronavirus by using the cantharidin preparation prepared by the invention.
1. For 2 suspected persons with obvious symptoms of the novel coronavirus, the cantharidin skin absorption liniment prepared in example 1 is applied to the skins of the chest, the back and the limbs of a 60kg adult three times a day, 2.0g of the cantharidin skin absorption liniment is applied to the skins of the chest, the back and the limbs of the adult each time, the temperature is reduced to 37.6 ℃ after 12 hours of application, and the temperature is reduced to normal after 24 hours. After taking the medicine for 2 days, the symptoms of chest distress and anorexia are obviously relieved. After continuous medication for 4 days, suspected persons have no self-induced symptoms and return to normal.
2. For 8 suspected persons who feel slight chest distress and have dry cough symptoms, the cantharidin skin absorption liniment prepared in example 1 is applied to chest, back and limbs of a 60kg adult three times a day, 2.0g is applied every time, after 1 day of application, the symptoms of hypodynamia and dry cough are relieved, and after 3 days of application, the suspected persons feel the symptoms completely disappeared and return to normal.
3. To 20 workers of the applicant company, sterilized a cloth towel using the cantharidin solution prepared in example 7, or coated a mask with the cantharidin solution. These people remain healthy.
The clinical application results of the subject group suggest that the invention has important prevention and treatment effects on the infection of viruses and germs such as novel coronavirus, influenza virus and the like.
Other embodiments of the present invention will readily suggest themselves to such skilled persons having the benefit of this disclosure. This application is intended to cover any variations, uses, or adaptations of the invention following, in general, the principles of the invention and including such departures from the present disclosure as come within known or customary practice within the art to which the invention pertains.

Claims (12)

1. An antiviral and antibacterial cantharidin preparation contains cantharidin as effective component, and is characterized by that the cantharidin is dissolved in oil-water or oil-oil to obtain cantharidin solvent carrier, and the cantharidin solvent carrier and medicinal carrier or excipient are made into various dosage forms for preventing and curing new type coronavirus.
2. The cantharidin antiviral, antibacterial agent according to claim 1, wherein said oil-in-water or oil-in-oil mutual solution comprises an essential oil of a ketone and/or a lactone.
3. A cantharidin skin absorption coating agent contains cantharidin as an effective medicinal component, and is characterized in that a cantharidin solvent carrier is an oil-oil mutual dissolving body and comprises the following components:
cantharidin: 160.0-200.0mg
Vegetable oil: 8.0-12.0g
Animal oil: 8.0-12.0g
Ketone essential oil: 40.0-60.0g
Octadecanol: 20.0-40.0g
Stearic acid: 20.0-40.0g
Emulsifier (Tween-80) 40-60.0g
And (3) the rest of distilled water: total 1000.0g
Making into skin absorption liniment containing cantharidin 0.16-0.2mg per gram.
4. An intravenous injection of cantharidin contains cantharidin as effective component, and features that the cantharidin solvent carrier is oil-water mutual solution comprising the following components:
cantharidin: 15.0-30.0mg
2-butanone: 30.0-60.0g
3-heptanone: 0.3-0.6g
2-sec-butylcyclohexanone: 0.3-0.6g
The balance of physiological water for injection: 16000.00g in total, and making into cantharidin intravenous injection.
5. A cantharidin tablet contains cantharidin as an effective medicinal component, and is characterized in that a cantharidin solvent carrier is an oil-water mutual solution and comprises the following components:
cantharidin: 200.0-300.0mg
Cocoa butter: 80.0-120.0g
Olive oil: 60.0-90.0g
2-butanone: 60.0-90.0g
2-sec-butylcyclohexanone: 200.0-300.0g
Starch: 3200.0-4800.0g
Gluten powder: 320.0-480.0g
The total amount of the prepared materials is as follows: 10000 tablets; each tablet is 0.392-0.588g cantharidin tablet.
6. A cantharidin capsule contains cantharidin as effective component, and features that the cantharidin solvent carrier is oil-water mutual solution comprising the following components:
cantharidin: 200.0-300.0mg
Deodorizing beef tallow: 80.0-120.0g
Olive oil: 60.0-90.0g
2-butanone: 60.0-90.0g
6-hydroxy-3, 7-dimethyl octanoic acid lactone: 200.0-300.0g
Starch: 3200.0-4800.0g
Gluten powder: 320.0-480.0g
The total amount of the prepared materials is as follows: 10000 capsules, each capsule weighing 0.392-0.588g cantharidin.
7. A cantharidin nose eye medicinal oil, contain cantharidin as active pharmaceutical ingredient, characterized by, cantharidin solvent carrier is oil-oil mutual solution, according to the following ingredients:
cantharidin: 2.2-3.6mg
2-butanone: 80.0-120.0g
Raspberry ketone: 3.0-6.0g
The rest is olive oil: the total amount of cantharidin nose-eye medicinal oil is 1000.0 g.
8. A cantharidin solution disinfectant cloth towel contains cantharidin as an effective medicinal component, and is characterized in that a cantharidin solvent carrier is an oil-water mutual solution and comprises the following components:
cantharidin: 1.0-2.6mg
500.0-600.0g of 95% ethanol
2-butanone: 40.0-60.0g
Propylene glycol: 425.0-525.0g
Benzyl alcohol: 8.0-10.0g
2-phenethyl alcohol: 8.0-10.0g
Raspberry ketone: 2.0-4.0g
The balance of distilled water: the total amount was 10000.0 g. Spraying the obtained solvent on the carrier to obtain cantharidin solution sterilized cloth towel.
9. A cantharidin Chinese and western medicine combined oral pill contains cantharidin as an effective medicine component, and is characterized in that a cantharidin solvent carrier is an oil-oil mutual solution and comprises the following components:
the cantharidin solution comprises the following components:
cantharidin: 330.0mg
Olive oil: 20.0g
Cocoa butter: 10.0g
Gamma-lactone: 6.0g
2-butanone: 30.0g
2-sec-butylcyclohexanone: 60.0g
The cantharidin traditional Chinese and western medicine combined oral pill comprises the following components:
cantharidin solution (containing cantharidin 330.0mg) 126.0g
Starch: 2000.0g
Gluten powder: 274.0g
Astragalus extract: 100.0g
Chinese bee honey: 2500.0g
Making into cantharidin Chinese and western medicinal oral pill 1000 pills, each pill containing cantharidin 0.33 mg.
10. The household and soldier cleaning agent capable of preventing trauma infection by mutual dissolution of oil and water is characterized in that the solution is a cantharidin oil-water mutual solution, and comprises the following components:
cantharidin: 1.6-3.2mg
375.0-525.0g of 95% ethanol
2-butanone: 80.0-120.0g
Propylene glycol: 495.0-725.0g
Benzyl alcohol: 6.0-12.0g
2-phenethyl alcohol: 6.0-12.0g
Raspberry ketone: 3.0-6.0g
The balance of distilled water. The preparation method comprises the following steps: the total amount of the cantharidin is 10000.0g, and the cantharidin is a conventional cleaning agent for families and soldiers who prevent trauma infection.
11. An antiviral, antibacterial invisible cantharidin condom for preventing HIV sexual behavior infection, which is characterized in that the solution is an oil-water mutual solution of cantharidin and comprises the following components:
cantharidin: 16.0-36.0mg
100.0-300.0g of 95% ethanol
Propylene glycol: 495.0-725.0g
Glycerol: 495.0-725.0g
Lactic acid: 1000.0g
Sodium lactate: 2000.0g
Benzyl alcohol: 16.0-21.0g
2-phenethyl alcohol: 6.0-12.0g
Hyaluronic acid: 30.0-120.0 g
Guar gum: 10.0-40.0 g
The balance of distilled water, and the preparation method comprises the following steps: the total amount is 10000.0g, and the cantharidin intangible condom for preventing HIV sexual behavior infection.
12. A cantharidin antibiotic solution for preparing an inactivated vaccine of ecological antibiotics for resisting novel coronavirus is characterized in that the solution is a cantharidin oil-oil solution or a cantharidin oil-oil solution, and the content of cantharidin is less than or equal to 1.6ppm and less than or equal to 3.6 ppm.
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CN115322089A (en) * 2022-07-18 2022-11-11 中国农业科学院烟草研究所(中国烟草总公司青州烟草研究所) Raspberry ketone hapten, artificial antigen, preparation method of raspberry ketone hapten, antibody and application of raspberry ketone hapten and artificial antigen

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CN111568897A (en) * 2020-05-25 2020-08-25 甘肃芫美药业有限公司 An antiviral and antibacterial cantharidin preparation, its preparation method, and its application in preventing and treating new coronavirus infection
WO2021238836A1 (en) * 2020-05-25 2021-12-02 甘肃芫美药业有限公司 Cantharidin antiviral and antibacterial preparation, preparation method therefor, and use thereof for preventing and treating novel coronavirus infection

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CN111568897A (en) * 2020-05-25 2020-08-25 甘肃芫美药业有限公司 An antiviral and antibacterial cantharidin preparation, its preparation method, and its application in preventing and treating new coronavirus infection

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CN114642658A (en) * 2022-01-24 2022-06-21 甘肃芫美药业有限公司 Oil-soluble micromolecule natural biological acid antiviral and antibacterial preparation, and preparation method and application thereof
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