Summary of the invention:
The object of the present invention is to provide the application of a kind of Rhizoma Fagopyri Dibotryis in the preparation antiviral drugs.
Technical solution of the present invention is:
The application of Rhizoma Fagopyri Dibotryis in the preparation antiviral drugs.
Described antiviral drugs is the medicine of treatment respiratory viral disease.
Described antiviral drugs is the medicine of treatment influenza virus property disease.
Described antiviral drugs is the medicine of treatment respiratory syncytial virus disease.
The present invention is used to prepare antiviral drugs with Rhizoma Fagopyri Dibotryis, treats the medicine of the respiratory tract disease of infection such as influenza virus, respiratory syncytial virus especially for preparation, and the disease that causes for the above-mentioned virus of treatment has tangible pharmacological action.
The specific embodiment:
Embodiment 1:
Depletion Semen Fagopyri Esculenti medical material is selected, and removes impurity, cleans, and dries, and (major diameter 2~20mm, minor axis 1~10mm) add 1-10 and doubly measure the 20-90% alcohol reflux three times, each 0.5-3.0 hour to be broken into coarse granule.Extracting solution concentrates (steam pressure: 0.005~0.06MP with No. seven sievings, filtrate decompression
aTemperature: 45~85 ℃; Vacuum: 0.03~0.08MP
a) become the concentrated solution of relative density 1.05~1.25 (40~60 ℃), add antioxidant and intercalating agent, mixing.Concentrated solution spray drying (100~180 ℃ of intake air temperatures, 55~100 ℃ of air outlet temperature) is made extract powder, adds excipient, and mixing is granulated, and adds magnesium stearate, mixing, filled capsules.
Antioxidant can be vitamin C, sodium sulfite, sodium thiosulfate, cysteine etc., and its consumption is 0.001%~0.004% of a Rhizoma Fagopyri Dibotryis weight; Intercalating agent can be tartaric acid, two mercapto ethyl glycines, edetate, citric acid etc., and its consumption is 0.001%~0.006% of a Rhizoma Fagopyri Dibotryis weight; Excipient is conventional excipients (can be ethyl cellulose, pregelatinized Starch, microcrystalline Cellulose, carboxymethyl starch sodium or low-substituted hydroxypropyl cellulose).
The capsule that obtains is used for the treatment of influenza virus property disease and treatment respiratory syncytial virus disease.
Embodiment 2:
Commercially available Rhizoma Fagopyri Dibotryis preparation (Nantong Jinghua Pharmacy Co. Ltd's production) is used for the treatment of influenza virus property disease and treatment respiratory syncytial virus disease.
Rhizoma Fagopyri Dibotryis preparation with embodiment 1 is the checking medicine; With the positive control drug of ribavirin injection (Suzhou No.6 Pharmaceutical Factory produces, lot number 000223), following determination test result is arranged:
Table 1 Rhizoma Fagopyri Dibotryis is to the toxicity test result of mdck cell and VERO cell
Medicine | Test method | Mdck cell | The VERO cell |
?TD
0μg/ml
| TD
50μg/ml
| TD
0μg/ml
| ?TD
50μg/ml
|
Rhizoma Fagopyri Dibotryis | The CPE method | ?625±0 | 1250±0 | 625±0 | ?1212±66 |
Mtt assay | ?979.6±35.2 | 1502±66.5 | 662±64 | ?1250±0 |
Ribavirin | The CPE method | ?>1000±0 | >1000±0 | >1000±0 | ?>1000±0 |
Mtt assay | ?>1000±0 | >1000±0 | >1000±0 | ?>1000±0 |
Table 2 Rhizoma Fagopyri Dibotryis influenza first 3 type viruses, anti-RSV virus result of the test
Medicine | Test method | Influenza first 3 type viruses | Anti-RSV virus |
IC
50g/ml
| MICμg/ml | TI | IC
50μg/ml
| MICμg/ml | TI |
Rhizoma Fagopyri Dibotryis | The CPE method | 10±0.5 | 18.3±2.0 | 34.4 | 13±5.6 | 39±0 | 16 |
Mtt assay | 10±0.4 | 18.3±2.0 | 34.4 | 16.3±5.6 | 39±0 | 16 |
Ribavirin | The CPE method | <7.8±0 | <7.8±0 | 128 | <7.8±0 | <7.8±0 | 128 |
Mtt assay | <7.8±0 | <7.8±0 | 128 | <7.8±0 | <7.8±0 | 128 |
The resisiting influenza virus test of pesticide effectiveness is the result of the test of indication with mouse death rate, protective rate in the table 3 Rhizoma Fagopyri Dibotryis body
Medicine name | Drug dose (g/Kg) | Number of mice (only) | The survival number | Death toll | Mortality rate % | Protective rate % | Statistical procedures | Interpretation of result |
?????X
2 | ??????P | Obvious resisiting influenza virus effect is arranged |
Rhizoma Fagopyri Dibotryis | ?????5 | ???30 | ????30 | ????0 | ????0 | ????100 | ????49.1 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
????2.5 | ???30 | ????23 | ????7 | ????23 | ????74 | ????27.2 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
????1.25 | ???30 | ????18 | ????12 | ????40 | ????56 | ????16.5 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
Ribavirin | ????0.1 | ???30 | ????30 | ????0 | ????0 | ????100 | ????49.1 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
????0.05 | ???30 | ????29 | ????1 | ????3 | ????97 | ????45.3 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
????0.025 | ???30 | ????29 | ????1 | ????3 | ????97 | ????45.3 | ??<D.01 | Obvious resisiting influenza virus effect is arranged |
Virus control | ??10?LD
50 | ???30 | ?????3 | ????27 | ????90 | | | | |
The resisiting influenza virus test of pesticide effectiveness is the result of the test of indication with the mouse lung pathological changes in the table 4 Rhizoma Fagopyri Dibotryis body
Medicine name | Drug dose (g/Kg) | Number of mice (only) | Pulmonary lesion | Pulmonary lesion rate % | Pulmonary lesion slip % | Statistical procedures | Interpretation of result |
Have | Do not have | ????X
2 | ????P | Obvious resisiting influenza virus effect is arranged |
Rhizoma Fagopyri Dibotryis | ?????5 | ???30 | ????2 | ????28 | ????7 | ????91 | ???30.2 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
?????2.5 | ???30 | ????5 | ????25 | ????17 | ????78 | ???21.7 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
?????1.25 | ???30 | ????11 | ????19 | ????37 | ????52 | ????9.8 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
Ribavirin | ?????0.1 | ???30 | ????0 | ????30 | ????0 | ????100 | ???37.3 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
?????0.05 | ???30 | ????3 | ????27 | ????10 | ????87 | ???27.2 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
?????0.025 | ???30 | ????4 | ????26 | ????13 | ????83 | ???24.3 | ??<0.01 | Obvious resisiting influenza virus effect is arranged |
Virus control | ??10?LD
50 | ???30 | ????23 | ????7 | ????77 | | | | |