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Preparation extracted from stephania tetrandra S. Moor and the use thereof

A technology for powdered fangji and its use is applied in the field of preparations extracted from fangchi from powdered fangji, which can solve the problems of increasing various infections of patients, treatment failure, and lowering of white blood cell levels.

Inactive Publication Date: 2006-11-01
INST OF CHINESE MATERIA MEDICA CHINA ACADEMY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the current antineoplastic drugs, especially cytotoxic drugs, are immunosuppressants. Patients are likely to develop multidrug resistance after long-term use, which will lead to treatment failure. Therefore, it is necessary to find chemotherapy sensitizing drugs, which can eliminate the Drug resistance to chemotherapeutic drugs can restore the sensitivity of tumor tissue to chemotherapeutic drugs, or make it easy for chemotherapeutic drugs to enter the cell interior and increase the cumulative concentration of chemotherapeutic drugs in cells, or it has anti-tumor effects. Chemotherapy drugs work synergistically to sensitize chemotherapy; in radiation therapy, a large dose of radiation is usually required to achieve the therapeutic purpose, which makes it difficult for patients to bear due to the suppression of the immune system. Sexual drugs, so that low-dose radiation therapy can also achieve the therapeutic purpose
In addition, chemotherapy and radiotherapy usually lead to serious side effects, mainly manifested as decreased leukocyte level, nausea, vomiting, hair loss, etc. The decreased leukocyte level will increase the probability of various infections in patients. Therefore, it is necessary to find ways to reduce chemotherapy and radiation therapy Toxic side effects of radiation therapy, especially drugs that raise white blood cell levels

Method used

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  • Preparation extracted from stephania tetrandra S. Moor and the use thereof
  • Preparation extracted from stephania tetrandra S. Moor and the use thereof
  • Preparation extracted from stephania tetrandra S. Moor and the use thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0017] The preparation of the present invention is obtained by the following method:

[0018] (1) Extract the Fangji powder or decoction pieces with dilute acid for at least 24 hours, collect the acid extract; then soak in water to collect the water liquid; combine the acid liquid and water liquid, add alkali to adjust the pH to 10-12, and let it stand overnight;

[0019] (2) filtering the liquid in step (1), drying and pulverizing the solid to obtain powder 1;

[0020] (3) Extract the powder 1 by heating to reflux with alcohol for 30 minutes;

[0021] (4) concentrating, placing, and filtering the alcohol solution in step (3) to obtain solid 2;

[0022] (5) Solid 2 was dissolved in hot ammonia ethanol and left to obtain a precipitate.

[0023] The preparation mainly contains tetrandrine of molecular formula (I) and tetrandrine of molecular formula (II), the molar ratio of the two is 9.8:0.2-8:2, preferably 9.8:0.2-6:4, The total content of the two is greater than 50%, and t...

Embodiment 1

[0037] Preparation, preparation of tetrandrine and tetrandrine

[0038] A. Preparations

[0039] Add 20 liters of 1% dilute sulfuric acid to 10 kilograms of Fangji coarse powder or about 1-2 mm thick decoction pieces to extract for 24 hours, collect the acid cold dipping solution, soak the remainder in 10 liters of water for 30 minutes, and collect the water liquid; Acid-cold immersion-water-washing treatment cycle is carried out 3 times, the acid-cooled immersion liquid and water liquid of each time are combined, calcium oxide or calcium hydroxide is added to it to adjust to pH10-12, stand overnight, supernatant is poured and discarded, Filter the turbid liquid in the lower part with a filter cloth to obtain about 2 kg of precipitate, dry, crush (10-40 mesh sieve), heat and reflux with 95% ethanol, pour out the alcohol, concentrate, place, filter, and dissolve the obtained solid in ammonia In neutral ethanol, let it stand for precipitation, dissolve the obtained crystal in e...

Embodiment 2

[0043] The preparation and the effect of tetrandrine on leukopenia induced by cyclophosphamide in mice

[0044] Give mice a one-time intraperitoneal injection of antitumor drug cyclophosphamide 75mg / kg, three days later, the number of peripheral blood leukocytes significantly decreases, and start oral or intramuscular injection of the preparation obtained in A in Example 1 on the same day when mice are injected with cyclophosphamide , once a day, for 3 consecutive days, the results are listed in Table 1, Table 2 and Table 3, it can be seen that the Tetrandrine and its preparation can significantly inhibit the leukopenia caused by cyclophosphamide, indicating that the leukocytes caused by cyclophosphamide The toxic and side effects of low white blood cells have a certain attenuation effect.

[0045] group

[0046] group

[0047] group

[0048] Note: Compared with the model group * P** P<0.01

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Abstract

The present invention relates to a preparation extracted from Stephania tetrandra S. Moor and its use for manufacture of medecine for enhancing the sensitivity or effect of chemotherapy, enhancing the sensitivity of radiotherapy, improving the level of leukocytes in body, and having antineoplastic and antianaphylaxis effects. Said preparation is mainly composed of tetrandrine and fangchinoline with the ratio of 9:1 to 8:2 (moles), which is obtained by the following process: (1) the powder or piece of Stephania tetrandra S. Moor is extracted with dilute acid with the cool acid extract being collected; and washed with water with the aqueous extract being collected; then the cool acid extract and aqueous extract are combined, adjusted with base pH 10 to 12, kept overnight; (2) the fluid of Step (1) is filtered, the solid dried, pulverized to give Powder 1; (3) Powder 1 is heated under reflux in alcohol for 30 min.; (4) the alcohol extract from Step (3) is concentrated, kept, filtered to give Solid 2; (5) Solid 2 is dissolved in warm ammoniac ethanol, kept for crystallization. The present invention also relates to the use of tetrandrine and the pharmaceutically acceptable salt thereof for manufacture of medecine for improving the level of leukocytes in body.

Description

technical field [0001] The present invention relates to a preparation extracted from fang fang and its application. In addition, the present invention also relates to the use of tetrandrine, one of the main components of the preparation, in the preparation of medicines for increasing leukocyte levels. Background technique [0002] Tumor is one of the diseases with high mortality rate, and its incidence rate is increasing year by year. Chemotherapy and radiotherapy are the main means of clinical treatment of tumors. Most of the current antineoplastic drugs, especially cytotoxic drugs, are immunosuppressants. Patients are likely to develop multidrug resistance after long-term use, which will lead to treatment failure. Therefore, it is necessary to find chemotherapy sensitizing drugs, which can eliminate the Drug resistance to chemotherapeutic drugs can restore the sensitivity of tumor tissue to chemotherapeutic drugs, or make it easy for chemotherapeutic drugs to enter the c...

Claims

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Application Information

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IPC IPC(8): A61K36/59A61K31/47A61P35/02A61K36/00
CPCA61K31/47A61K36/59A61P35/02A61K2300/00
Inventor 王智民叶祖光梁爱华
Owner INST OF CHINESE MATERIA MEDICA CHINA ACADEMY OF TRADITIONAL CHINESE MEDICINE
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