CN101822770A - Medicinal composition with anti-tumor effect and application thereof - Google Patents
Medicinal composition with anti-tumor effect and application thereof Download PDFInfo
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Abstract
The invention discloses a medicinal composition with anti-tumor effect and application thereof. The medicinal composition uses kuh-seng alkaloid and rhizoma hterosmilacis as raw materials, and effective ingredients of the raw materials comprise matrine, oxidized matrine, sophocarpine, oxidized sophocarpine and rhizoma hterosmilacis glycoside and the like. Pharmacodynamical experiments show that the medicinal composition can be used for resisting tumor and relieving cancer swelling pain, has synergy and detoxification effects on tumor chemotherapy medicaments and effects of improving the immunity and improving the quality of life for cancer patients, and can be used for treatment of hepatitis resistance and liver fibrosis.
Description
Invention field
The present invention relates to a kind of medical composition and its use, particularly a kind of medical composition and its use with antitumor action.
Technical background
Tumor (Tumor) be body under various carcinogenic factor effects, some cells of local organization lose the normal regulation to its growth on gene level, cause its clonal abnormality hypertrophy and the neoplasm that forms.It is generally acknowledged that tumor cell is a monoclonicity, promptly all oncocytes in tumor all are offsprings of the cell of a sudden change.Generally tumor is divided into optimum and pernicious two big classes.All malignant tumor are generically and collectively referred to as cancer (cancer).Nowadays tumor has become several serious diseases therefore that threaten human life's health, and environment, heredity all become tumorigenic principal element.Benign tumor is less to the influence of body, mainly shows as local compression and obstructive symptom, and its influence mainly changes relevant with happening part and secondary.Also can produce serious consequence if occur in vitals.Malignant tumor is soaked into the 26S Proteasome Structure and Function that destroys organ, and can be shifted because differentiation is immature, growth is very fast, thereby serious to the body influence.Malignant tumor also can have heating, intractable pain except that can causing local compression and obstructive symptom similar to above-mentioned benign tumor, can occur late period seriously becoming thin, the state of weak, anemia and whole body depletion.In a word, tumor has caused through human life quality and life and health and has had a strong impact on.
The treatment means of malignant tumor mainly is operation, chemotherapy and radiation.Long-term a large amount of clinical proof, though western medicine and medical practitioners treatment tumor effect is better, side effect is bigger.Surgical operation is applicable to the treatment of some locality tumor early and middle portion, but the treatment of most patient's armrest art is to prevent the recurrence of tumor and metastasis.Though put, chemotherapy has quite high cure rate, often causes as toxicities such as bone marrow depression, immunocompromised, gastricisms, makes the patient be difficult to adhere to treatment.The drug resistance that chemotherapeutics occurs in therapeutic process has become one of difficult problem in the present clinical treatment.The method of overcoming if can be searched out, the cure rate of many tumors can be further improved undoubtedly.And thereby the quality of life that the decline problem of patient's life quality that various Therapeutic Method brought makes the function that how to keep body and respectively get involved organ improve patient becomes the current extensively problem of attention that is subjected to.
Just because of above-mentioned a variety of causes, make in the world the scientists of many countries progressively the research center of gravity be shifted to the Chinese medicine aspect.The Chinese medicine of tumor has long history in China, and the utilization Chinese medicine is very general on China's clinical tumor.Clinical practice for many years also shows, prevention and treatment in Chinese and western malignant tumor curative effect certainly, Chinese medicine in ameliorate tumor patient symptom, improve immunologic function and body condition, improve operation and put, the effect of chemotherapy, alleviate the toxic and side effects of its generation, aspect effects such as raising patient life quality are remarkable.
Present antitumor Chinese medicine majority is made of big compound recipe, and preparation method is generally also fairly simple, is difficult to satisfy modern Chinese medicine safety, effective, quality controllable requirement.The monomer extract of part Chinese medicine has certain curative effect, but lose that Chinese medicine is integrally-regulated, the advantage of multipath, many target treatments, effect is difficult as people's will.
Summary of the invention
The object of the invention is to disclose a kind of pharmaceutical composition with antitumor action, the present invention also aims to disclose the purposes of this pharmaceutical composition.
The present invention seeks to be achieved by the following scheme.
The raw material of pharmaceutical composition of the present invention consists of:
Radix Sophorae Flavescentis biology total alkali 5-30 weight portion Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 1-10 weight portion
Wherein, the Radix Sophorae Flavescentis biology total alkali is prepared from by following method:
Get the Radix Sophorae Flavescentis medical material, it is standby to be crushed to coarse powder; With concentration is that the hydrochloric acid solution of 0.1%-0.3% carries out percolation, to percolate inanimate object alkali reaction, collects percolate; Regulate percolate pH to 5-9 with ammonia, leave standstill, the filtering precipitate is collected filtrate; With the 110 type cation exchange resin columns of filtrate,, collect eluent with the ammonia eluting exchanger resin of 4～6 times of amount column volume 3%-7% by 0.5-2 times of medical material amount volume; Reclaim ammonia, eluent is concentrated into dried, the Radix Sophorae Flavescentis biology total alkali;
Wherein, Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract is to be prepared from by following method:
Get the Smilax lanceaefolia Roxb. Var.opaca A.DC. decoction pieces, be crushed to coarse powder, add water supersound extraction 1-3 time, each 20-40 minute, amount of water was 2-8 times, gets extracting solution; Centrifugal behind the extracting liquid filtering, get clear liquor; Through the HPD-100 type macroporous adsorptive resins of 3-7 times of medical material amount volume, flow velocity is 0.5-2 times of column volume per hour, discards effluent; Get macroporous adsorptive resins express developed with 0.5-2 times of column volume purified water, 4～6 times of column volume amounts of reuse purified water eluting, flow velocity is 1-3 times of column volume per hour; Collect eluent, concentrating under reduced pressure, drying gets Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract.
Wherein, the Radix Sophorae Flavescentis biology total alkali preferably is prepared from by following method:
Get the Radix Sophorae Flavescentis medical material, it is standby to be crushed to coarse powder; With concentration is that 0.2% hydrochloric acid solution carries out percolation, to percolate inanimate object alkali reaction, collects percolate; Regulate percolate pH to 7 with ammonia, leave standstill, the filtering precipitate is collected filtrate; With the 110 type cation exchange resin columns of filtrate,, collect eluent with the ammonia eluting exchanger resin of 5 times of amount column volumes 5% by 1 times of medical material amount volume; Reclaim ammonia, eluent is concentrated into dried, the Radix Sophorae Flavescentis biology total alkali.
Wherein, Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract preferably is prepared from by following method:
Get the Smilax lanceaefolia Roxb. Var.opaca A.DC. decoction pieces, be crushed to coarse powder, add the water supersound extraction 2 times, each 30 minutes, amount of water was respectively 6 times and 4 times, got extracting solution; Centrifugal behind the extracting liquid filtering, get clear liquor; Through the HPD-100 type macroporous adsorptive resins of 5 times of medical material amount volumes, flow velocity is 1 times of column volume per hour, discards effluent; Get macroporous adsorptive resins express developed with 1 times of column volume purified water, 5 times of column volume amounts of reuse purified water eluting, flow velocity is 2 times of column volumes per hour; Collect eluent, concentrating under reduced pressure, drying gets Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract.
The raw material composition of pharmaceutical composition of the present invention is preferably:
Radix Sophorae Flavescentis biology total alkali 20 weight portion Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 5 weight portions
The raw material composition of pharmaceutical composition of the present invention is preferably:
Radix Sophorae Flavescentis biology total alkali 25 weight portion Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 2.5 weight portions
The raw material composition of pharmaceutical composition of the present invention is preferably:
Radix Sophorae Flavescentis biology total alkali 15 weight portion Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 5 weight portions
The raw material composition of pharmaceutical composition of the present invention is preferably:
Radix Sophorae Flavescentis biology total alkali 8 weight portion Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 8 weight portions
The raw material of pharmaceutical composition of the present invention consists of:
Matrine 1-30 weight portion oxymatrine 1-30 weight portion
Sophocarpine 1-20 weight portion N-oxysophocarpine 1-20 weight portion
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 1-20 weight portion
The raw material composition of pharmaceutical composition of the present invention is preferably:
Matrine 20 weight portion oxymatrines 20 weight portions
Sophocarpine 5 weight portion N-oxysophocarpine 5 weight portions
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 15 weight portions
The raw material composition of pharmaceutical composition of the present invention is preferably:
Matrine 15 weight portion oxymatrines 25 weight portions
Sophocarpine 5 weight portion N-oxysophocarpine 15 weight portions
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 5 weight portions
The raw material composition of pharmaceutical composition of the present invention is preferably:
Matrine 25 weight portion oxymatrines 15 weight portions
Sophocarpine 15 weight portion N-oxysophocarpine 5 weight portions
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 10 weight portions
The raw material composition of pharmaceutical composition of the present invention can also add one or both in the following raw material:
Sophoridine 0.5-5 weight portion sophoramine 0.5-5 weight portion
The raw material of pharmaceutical composition of the present invention is formed one or both in the following raw material of all right preferred adding:
Sophoridine 2 weight portion sophoramines 2 weight portions
The raw material of pharmaceutical composition of the present invention is formed one or both in the following raw material of all right preferred adding:
Sophoridine 1 weight portion sophoramine 4 weight portions
The raw material of pharmaceutical composition of the present invention is formed one or both in the following raw material of all right preferred adding:
Sophoridine 4 weight portion sophoramines 1 weight portion
Get above-mentioned raw materials, add conventional adjuvant, make clinical acceptable forms: tablet, granule, oral liquid, pill, capsule, slow releasing preparation or injection according to common process.
Pharmaceutical composition of the present invention can be used for antitumor, alleviate cancerous protuberance pain, the cancer patient there is the effect that improves the immunity and the quality of making the life better, in addition, effect experiment shows that pharmaceutical composition of the present invention also can be used for the treatment of pain relieving, hemostasis, anti-hepatitis, hepatic fibrosis, and tumor chemotherapeutic drug is had the efficacy enhancing and toxicity reducing effect.The present invention makes with extra care and gets via Chinese medicine extraction, and constituent is simple, structure is clear and definite, be easy to control, through the verification experimental verification curative effect certainly.Satisfy the clinical application demand of modern Chinese medicine, adapted to the requirement of modern medicine technology and drug evaluation system again.
Following experimental example and embodiment are used to further specify but are not limited to the present invention.
The experimental example 1 external tumor that presses down is tested (cellulotoxic experiment mtt assay)
With human hepatoma cell strain HEPG
2, BEL and stomach cancer cell line M803 be incubated in the RPMI1640 culture fluid that contains 5% hyclone and (include penicillin 100u/ml, streptomycin 100u/ml).Cell is containing 5%CO
2Incubator in cultivate, every 2d passes a generation.
Get people's gastric cancer MG803, the people's hepatocarcinoma HEPG of above-mentioned three kinds of 24h that increased
2, the BEL cell strain, after 0.25% trypsinization, adjust cell number with RPMI1640 (containing 10% new-born calf serum) and be: 1.5 * 10
5The slender cytosol of/ml, 150 μ l add 96 orifice plates with oncocyte liquid, and every hole adds the drug combination injection of the present invention 50 μ l of embodiment 1 preparation again, is equivalent to drug level 3.75,1.88,0.94,0.47,0.23,0.12,0.059mgmL respectively
-1, 6 every group multiple holes, totally 7 dosage groups, the positive matched group of amycin (Adr0.25 μ g/mL) with culture plate jolting gently, is put into 37 ℃, 5%CO after the dosing
2Cultivate 48h in the incubator, 4h added MTT20 μ l (5mg/ml) before experiment stopped, and continued to cultivate 4h, abandoned supernatant, added dimethyl sulfoxide (MDSO) 100 μ l/ holes, measured the OD value at microplate reader 490nm wavelength place.Every kind of oncocyte experiment all repeats 3 times.Obtain growth inhibition ratio (IR): IR (%)=(1-medication group OD value/matched group OD value) * 100% by following formula and the results are shown in Table 1.
Table 1 drug combination injection of the present invention is to the cytotoxicity of 3 kinds of human tumor cells
The result shows that after drug combination injection of the present invention was handled above-mentioned 3 kinds of tumor cells, the ability of the concentration group cellular metabolism MTT that medicament contg is high obviously descended, and cell-cytotoxic reaction is obvious, and growth inhibition ratio is strengthened with the increase of drug level.Experiment repeats 3 batches, as a result basically identical.
Press down the tumor experiment in experimental example 2 bodies
1, pharmaceutical composition of the present invention is to the tumor-inhibiting action of S180 sarcoma in the mice body
Get 64 of ICR mices, male and female half and half are pressed the strain of transplanted tumor research inocalation method aseptic inoculation S180 solid tumor tumor, claim behind the 24h that Mus is heavy, and be divided into 5 groups at random, be respectively the little (75mgkg of drug combination injection group of the present invention of model control group, positive drug cyclophosphamide group, embodiment 5 preparations
-1), in (150mgkg
-1), big (300mgkg
-1) each dosage group.Each dosage group of injection of the present invention adopts intraperitoneal injection, once a day, and continuous 10 days.The next day of positive control drug cyclophosphamide group intraperitoneal injection once, totally 5 times.The model control group lumbar injection gives isopyknic physiological saline solution.24h puts to death tumor-bearing mice and weighs after the last administration, cuts open to get the tumor body and weigh, and calculates tumour inhibiting rate (%) by following formula.
The gained data are carried out statistical procedures (t-check), the results are shown in Table 2.
Table 2 drug combination injection of the present invention is to mice S
180The tumor-inhibiting action research of transplanted tumor
Annotate: compare with model control group,
1)P＜0.05,
2)P＜0.01
2, pharmaceutical composition of the present invention is to the influence of rat liver cancer H22 solid tumor
The inoculation of mice, grouping, medication, result processing method etc. the results are shown in Table 3. all with above-mentioned experiment
Table 3 drug combination injection of the present invention is to rat liver cancer H
22The tumor-inhibiting action of transplanted tumor
Annotate: compare with model control group,
1)P＜0.05;
2)P＜0.01.
The result proves in the table, and each dosage group of drug combination injection of the present invention all can obviously suppress the growth of rat liver cancer H22 solid tumor, and strengthens with the increase tumor-inhibiting action of dosage.Body weight gain to mice does not have obvious influence simultaneously.
3, pharmaceutical composition of the present invention is to the influence of hepatic ascites cancer survival time of mice
The inoculation of mice, grouping, medication are with above-mentioned experiment, and self administration of medication begins promptly to note the death condition of observed and recorded mice, observe to the first administration 45 days (the longest observation to 45 day), and calculate and respectively be subjected to reagent thing group increase in life span (%).
Result's statistics: the test data of organizing of every batch of test represents with mean ± standard deviation that all each dosage group of injection of the present invention and positive control drug fluorouracil group compare with model group respectively, with t-check carrying out statistical analysis.Its computing formula of increase in life span is as follows:
Increase in life span (%)=(T-C)/C * 100%
T=administration treated animal survival natural law C=model control group animals survived natural law
Result: injection 75,150 of the present invention, 300mgkg
-1, continuously gastric infusion is 12 days, and the life span of hepatic ascites cancer mice is had tangible prolongation effect (with model group P＜0.01 relatively), and increase in life span is 60～93%.The result shows that drug combination injection of the present invention has the effect of obvious prolongation hepatic ascites cancer mice life span.The results are shown in Table 4.
Table 4 drug combination injection of the present invention is to the influence of hepatic ascites cancer survival time of mice
Annotate: compare with model control group,
2)P＜0.01
4, pharmaceutical composition of the present invention is to the influence of people's hepatocarcinoma Nude Mice
Experimental technique: mouse back scapula position subcutaneous aseptic inoculation hepatocarcinoma tumor tissue piece, 24h begins the administration of dividing into groups in the inoculation back, and experiment is established: model control group, positive control drug cyclophosphamide group 15mgkg
-1, embodiment 5 preparation drug combination injection of the present invention establish 75,150,300mgkg
-1Three dosage groups, totally 5 groups.Each dosage group intraperitoneal injection every day of injection of the present invention 1 time, successive administration 26 days, the next day of the positive drug cyclophosphamide intraperitoneal injection once, totally 13 times.Each is organized mice 24h after the last administration and weighs, puts to death mice and peel off the tumor body and weigh, and calculates tumour inhibiting rate (%).
Result's statistics: each is organized test data and represents with mean ± standard deviation that all each dosage group of injection of the present invention and positive control drug cyclophosphamide group compare with model group respectively, carries out statistical analysis with the t-check, the results are shown in Table 5.
Table 5 drug combination injection of the present invention is to tumor-inhibiting action research in the body of nude mice hepatocarcinoma (BAL7402)
Annotate: compare with model control group,
1)P＜0.05,
2)P＜0.01
Table 4 is the result show, drug combination injection 150 of the present invention, 300mgkg
-1To the mouse peritoneal injection, every day 1 time, successive administration 26 days, the tumor that can obviously suppress nude mice hepatocarcinoma (BAL7402) transplanted tumor weighs (comparing P＜0.05 or P＜0.01 with model group), and experiment repeats two batches, as a result basically identical.
Brief summary: drug combination injection 75,150 of the present invention, 300mgkg
-1Transplanted tumor in the nude mouse all there is the obvious suppression effect, can obviously prolongs the survival period of liver abdomen cancer mice, and demonstrate tangible dose-effect relationship.Illustrate that drug combination injection of the present invention has stronger antitumor action.
The experiment of experimental example 3 analgesic activities
1, drug combination injection of the present invention is to the influence (hot plate method) of the inductive pain of thermostimulation
Test method: get 70 of ICR female mices, before the test mice is carried out the pain threshold screening.Hot plate temperature is adjusted to 55 ± 0.1 ℃, with the single hot plate analyzer of only putting into of mice, with put into behind the mice to the time that licking between the metapedes action appears in mice be pain threshold.Pain threshold is lower than 6 seconds persons and surpasses 30 seconds or the leaper is eliminated.The mice of screening after qualified evenly is divided into 5 groups by pain threshold, 12 every group.Experiment is established: the drug combination injection of the present invention of matched group, positive drug tramadol hydrochloride group, embodiment 8 preparations is little, in, big three each dosage groups.The disposable vein drug administration by injection is adopted in experiment.The isopyknic normal saline of matched group intravenous injection.Respectively at behind the medicine 30,60,120min measures each treated animal pain threshold 3 times.Surpass 60 seconds mice for pain threshold after the medication, promptly take out for preventing to scald only to observe after 60 seconds, the result calculated with 60 seconds.
Result's statistical disposition: each is organized experimental data and represents with mean ± standard deviation that all compared with matched group by the reagent thing, the result checks with t-and carries out statistical analysis.The results are shown in Table 6.
Table 6 drug combination injection of the present invention is to the influence (n=12) of mice hot plate pain threshold (s)
Annotate: compare with matched group
1)P＜0.05
2)P＜0.01
The result: the result proves in the table, each dosage group disposable vein drug administration by injection of drug combination injection of the present invention, the pain that 30,60,120 minutes three time points bring out thermostimulation behind medicine all demonstrates significant analgesia role, and demonstrates tangible dose-effect relationship.
2, drug combination injection of the present invention stimulates the influence (writhing method) of inductive pain to chemical substance
Experimental technique: get 60 of ICR female mices, evenly be divided into 5 groups by body weight, the grouping situation is with above-mentioned experiment.All disposable vein injection in preceding 1 hour gives injection to each group causing bitterly, and matched group gives isopyknic normal saline.1h respectively organizes the glacial acetic acid 0.2ml of the equal lumbar injection 0.6% of mice behind medicine, with being about to the single mice string cage of only putting into of mice, record observe every mice in injection glacial acetic acid to mice begins to occur turning round time (incubation period) and 15 minutes of body mice turn round the body number of times.
Statistical disposition as a result: each is organized test data and represents with mean ± standard deviation that all administration group and positive control drug group compare with model group respectively.The result carries out statistical analysis with the t-check, the results are shown in Table 7.
Table 7 pharmaceutical composition of the present invention is to the influence (n=12) of the inductive mouse writhing reaction of glacial acetic acid
Annotate: compare with model group
1)P＜0.05,
2)P＜0.01,
The result proves in the table, and the injection of mice disposable vein gives injection 20,40,80mgkg
-11h, each dosage group all can obviously prolong mice occur the incubation period of writhing response, obviously reduce mice turn round the body number of times.
Drug combination injection 20,40 of the present invention, 80mgkg
-1The disposable vein drug administration by injection all demonstrates significant analgesia role to above-mentioned two kinds of mice pain models, and obviously strengthens with dosage increasing analgesic activity, illustrates that drug combination injection of the present invention has stronger analgesic activity.
The experiment of experimental example 4 anastalsises
Experimental technique: get 50 of healthy ICR male mices, by body weight mice evenly is divided into 5 groups, 10 every group, test is established: normal control group, positive control drug ZHIXUEBAO (0.4g crude drug kg
-1), the drug combination injection of the present invention of embodiment 9 preparation is little, in, big (37.5,75,150mgkg
-1) three dosage groups.Injection adopts intraperitoneal injection, and the positive control drug ZHIXUEBAO adopts gastric infusion, once a day, and totally 3 times.0.5h after the last administration, get the hematometry clotting time with capillary tube method from the eye socket venous plexus, cut apart from tail point 0.5cm place with profit afterwards and cut off the Mus tail, naturally flow out from blood and to pick up counting, adsorbed Mus tail section gently once with filter paper in per 30 seconds, observe till do not have bloodstain and ooze out, this section period is counted the hemorrhage time of mice.
The statistical disposition of data: the data of each group represent with mean ± standard deviation that all each dosage group of injection and positive drug ZHIXUEBAO group compare with model group respectively, and the result checks with t-and carries out statistical analysis.The results are shown in Table 8.
Table 8 drug combination injection of the present invention is to the influence (n=10) of normal mouse bleeding time and clotting time
Annotate: compare with model group:
1)P＜0.05,
2)P＜0.01
The result proves, in the drug combination injection of the present invention, heavy dose of group successive administration 3 days, all can obviously shorten the clotting time of mice and bleeding time (with model group relatively P＜0.05 or P＜0.01).The result shows that drug combination injection of the present invention has tangible anastalsis.
Following embodiment all can realize the described effect of above-mentioned experimental example
The specific embodiment
Embodiment 1: medicine composition injection of the present invention
Radix Sophorae Flavescentis biology total alkali 2000g Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 500g
Wherein, the Radix Sophorae Flavescentis biology total alkali is prepared from by following method:
Get the Radix Sophorae Flavescentis medical material, it is standby to be crushed to coarse powder; With concentration is that 0.2% hydrochloric acid solution carries out percolation, to percolate inanimate object alkali reaction, collects percolate; Regulate percolate pH to 7 with ammonia, leave standstill, the filtering precipitate is collected filtrate; With the 110 type cation exchange resin columns of filtrate,, collect eluent with the ammonia eluting exchanger resin of 5 times of amount column volumes 5% by 1 times of medical material amount volume; Reclaim ammonia, eluent is concentrated into dried, the Radix Sophorae Flavescentis biology total alkali;
Wherein, Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract is prepared from by following method:
Get the Smilax lanceaefolia Roxb. Var.opaca A.DC. decoction pieces, be crushed to coarse powder, add the water supersound extraction 2 times, each 30 minutes, amount of water was respectively 6 times and 4 times, got extracting solution; Centrifugal behind the extracting liquid filtering, get clear liquor; Through the HPD-100 type macroporous adsorptive resins of 5 times of medical material amount volumes, flow velocity is 1 times of column volume per hour, discards effluent; Get macroporous adsorptive resins express developed with 1 times of column volume purified water, 5 times of column volume amounts of reuse purified water eluting, flow velocity is 2 times of column volumes per hour; Collect eluent, concentrating under reduced pressure, drying gets Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract.
Get above-mentioned raw materials, add conventional adjuvant, make injection, be used for the treatment of pain relieving, hemostasis, anti-hepatitis, hepatic fibrosis according to common process.
Embodiment 2: pharmaceutical composition tablet of the present invention
Radix Sophorae Flavescentis biology total alkali 2500g Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 2500g
Wherein, the Radix Sophorae Flavescentis biology total alkali is prepared from by following method:
Get the Radix Sophorae Flavescentis medical material, it is standby to be crushed to coarse powder; With concentration is that 0.2% hydrochloric acid solution carries out percolation, to percolate inanimate object alkali reaction, collects percolate; Regulate percolate pH to 7 with ammonia, leave standstill, the filtering precipitate is collected filtrate; With the 110 type cation exchange resin columns of filtrate,, collect eluent with the ammonia eluting exchanger resin of 5 times of amount column volumes 5% by 1 times of medical material amount volume; Reclaim ammonia, eluent is concentrated into dried, the Radix Sophorae Flavescentis biology total alkali;
Wherein, Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract is prepared from by following method:
Get the Smilax lanceaefolia Roxb. Var.opaca A.DC. decoction pieces, be crushed to coarse powder, add the water supersound extraction 2 times, each 30 minutes, amount of water was respectively 6 times and 4 times, got extracting solution; Centrifugal behind the extracting liquid filtering, get clear liquor; Through the HPD-100 type macroporous adsorptive resins of 5 times of medical material amount volumes, flow velocity is 1 times of column volume per hour, discards effluent; Get macroporous adsorptive resins express developed with 1 times of column volume purified water, 5 times of column volume amounts of reuse purified water eluting, flow velocity is 2 times of column volumes per hour; Collect eluent, concentrating under reduced pressure, drying gets Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract.
Get above-mentioned raw materials, add conventional adjuvant, make tablet, be used for antitumor, alleviate cancerous protuberance pain, improve cancer patient's immunity, improve its quality of life according to common process.
Embodiment 3: medicament composition granule agent of the present invention
Radix Sophorae Flavescentis biology total alkali 1500g Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 500g
Wherein, the Radix Sophorae Flavescentis biology total alkali is prepared from by following method:
Get the Radix Sophorae Flavescentis medical material, it is standby to be crushed to coarse powder; With concentration is that 0.2% hydrochloric acid solution carries out percolation, to percolate inanimate object alkali reaction, collects percolate; Regulate percolate pH to 7 with ammonia, leave standstill, the filtering precipitate is collected filtrate; With the 110 type cation exchange resin columns of filtrate,, collect eluent with the ammonia eluting exchanger resin of 5 times of amount column volumes 5% by 1 times of medical material amount volume; Reclaim ammonia, eluent is concentrated into dried, the Radix Sophorae Flavescentis biology total alkali;
Wherein, Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract is prepared from by following method:
Get the Smilax lanceaefolia Roxb. Var.opaca A.DC. decoction pieces, be crushed to coarse powder, add the water supersound extraction 2 times, each 30 minutes, amount of water was respectively 6 times and 4 times, got extracting solution; Centrifugal behind the extracting liquid filtering, get clear liquor; Through the HPD-100 type macroporous adsorptive resins of 5 times of medical material amount volumes, flow velocity is 1 times of column volume per hour, discards effluent; Get macroporous adsorptive resins express developed with 1 times of column volume purified water, 5 times of column volume amounts of reuse purified water eluting, flow velocity is 2 times of column volumes per hour; Collect eluent, concentrating under reduced pressure, drying gets Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract.
Get above-mentioned raw materials, add conventional adjuvant, make granule, as the drug use that tumor chemotherapeutic drug is had the efficacy enhancing and toxicity reducing effect according to common process.
Embodiment 4: drug composition oral liquid of the present invention
Radix Sophorae Flavescentis biology total alkali 800g Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 800g
Wherein, the Radix Sophorae Flavescentis biology total alkali is prepared from by following method:
Get the Radix Sophorae Flavescentis medical material, it is standby to be crushed to coarse powder; With concentration is that 0.2% hydrochloric acid solution carries out percolation, to percolate inanimate object alkali reaction, collects percolate; Regulate percolate pH to 7 with ammonia, leave standstill, the filtering precipitate is collected filtrate; With the 110 type cation exchange resin columns of filtrate,, collect eluent with the ammonia eluting exchanger resin of 5 times of amount column volumes 5% by 1 times of medical material amount volume; Reclaim ammonia, eluent is concentrated into dried, the Radix Sophorae Flavescentis biology total alkali;
Wherein, Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract is prepared from by following method:
Get the Smilax lanceaefolia Roxb. Var.opaca A.DC. decoction pieces, be crushed to coarse powder, add the water supersound extraction 2 times, each 30 minutes, amount of water was respectively 6 times and 4 times, got extracting solution; Centrifugal behind the extracting liquid filtering, get clear liquor; Through the HPD-100 type macroporous adsorptive resins of 5 times of medical material amount volumes, flow velocity is 1 times of column volume per hour, discards effluent; Get macroporous adsorptive resins express developed with 1 times of column volume purified water, 5 times of column volume amounts of reuse purified water eluting, flow velocity is 2 times of column volumes per hour; Collect eluent, concentrating under reduced pressure, drying gets Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract.
Get above-mentioned raw materials, add conventional adjuvant, make oral liquid, be used for the treatment of pain relieving, hemostasis, anti-hepatitis, hepatic fibrosis according to common process.
Embodiment 5: medicine composition injection of the present invention
Matrine 2000g oxymatrine 2000g
Sophocarpine 500g N-oxysophocarpine 500g
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 1500g
Get above-mentioned raw materials, add conventional adjuvant, make injection, be used for antitumor, alleviate cancerous protuberance pain, improve cancer patient's immunity, improve its quality of life according to common process.
Embodiment 6: medicament composition capsule agent of the present invention
Matrine 1500g oxymatrine 2500g
Sophocarpine 500g N-oxysophocarpine 1500g
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 500g
Get above-mentioned raw materials, add conventional adjuvant, make capsule, as the drug use that tumor chemotherapeutic drug is had the efficacy enhancing and toxicity reducing effect according to common process.
Embodiment 7: pharmaceutical composition slow releasing agent of the present invention
Matrine 2500g oxymatrine 1500g
Sophocarpine 1500g N-oxysophocarpine 500g
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 1000g
Get above-mentioned raw materials, add conventional adjuvant, make slow releasing preparation, be used for the treatment of pain relieving, hemostasis, anti-hepatitis, hepatic fibrosis according to common process.
Embodiment 8: medicine composition injection of the present invention
Matrine 2000g oxymatrine 2000g
Sophocarpine 500g N-oxysophocarpine 500g
Sophoridine 200g sophoramine 200g
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 1500g
Get above-mentioned raw materials, add conventional adjuvant, make injection, be used for antitumor, alleviate cancerous protuberance pain, improve cancer patient's immunity, improve its quality of life according to common process.
Embodiment 9: medicine composition injection of the present invention
Matrine 1500g oxymatrine 2500g
Sophocarpine 500g N-oxysophocarpine 1500g
Sophoridine 400g
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 500g
Get above-mentioned raw materials, add conventional adjuvant, make injection, as the drug use that tumor chemotherapeutic drug is had the efficacy enhancing and toxicity reducing effect according to common process.
Embodiment 10: medicine composition injection of the present invention
Matrine 2500g oxymatrine 1500g
Sophocarpine 1500g N-oxysophocarpine 500g
Sophoridine 100g sophoramine 400g
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 1000g
Get above-mentioned raw materials, add conventional adjuvant, make injection, be used for the treatment of pain relieving, hemostasis, anti-hepatitis, hepatic fibrosis according to common process.
Claims (13)
1. pharmaceutical composition with antitumor action is characterized in that the raw material of this pharmaceutical composition consists of:
Radix Sophorae Flavescentis biology total alkali 5-30 weight portion Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 1-10 weight portion
Wherein, the Radix Sophorae Flavescentis biology total alkali is prepared from by following method:
Get the Radix Sophorae Flavescentis medical material, it is standby to be crushed to coarse powder; With concentration is that the hydrochloric acid solution of 0.1%-0.3% carries out percolation, to percolate inanimate object alkali reaction, collects percolate; Regulate percolate pH to 5-9 with ammonia, leave standstill, the filtering precipitate is collected filtrate; With the 110 type cation exchange resin columns of filtrate,, collect eluent with the ammonia eluting exchanger resin of 4～6 times of amount column volume 3%-7% by 0.5-2 times of medical material amount volume; Reclaim ammonia, eluent is concentrated into dried, the Radix Sophorae Flavescentis biology total alkali;
Wherein, Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract is to be prepared from by following method:
Get the Smilax lanceaefolia Roxb. Var.opaca A.DC. decoction pieces, be crushed to coarse powder, add water supersound extraction 1-3 time, each 20-40 minute, amount of water was 2-8 times, gets extracting solution; Centrifugal behind the extracting liquid filtering, get clear liquor; Through the HPD-100 type macroporous adsorptive resins of 3-7 times of medical material amount volume, flow velocity is 0.5-2 times of column volume per hour, discards effluent; Get macroporous adsorptive resins express developed with 0.5-2 times of column volume purified water, 4～6 times of column volume amounts of reuse purified water eluting, flow velocity is 1-3 times of column volume per hour; Collect eluent, concentrating under reduced pressure, drying gets Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract.
2. pharmaceutical composition as claimed in claim 1 is characterized in that the raw material of this pharmaceutical composition consists of:
Radix Sophorae Flavescentis biology total alkali 20 weight portion Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 5 weight portions
Or
Radix Sophorae Flavescentis biology total alkali 25 weight portion Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 2.5 weight portions
Or
Radix Sophorae Flavescentis biology total alkali 15 weight portion Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 5 weight portions
Or
Radix Sophorae Flavescentis biology total alkali 8 weight portion Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract 8 weight portions.
3. pharmaceutical composition as claimed in claim 1 or 2 is characterized in that wherein the Radix Sophorae Flavescentis biology total alkali is prepared from by following method:
Get the Radix Sophorae Flavescentis medical material, it is standby to be crushed to coarse powder; With concentration is that 0.2% hydrochloric acid solution carries out percolation, to percolate inanimate object alkali reaction, collects percolate; Regulate percolate pH to 7 with ammonia, leave standstill, the filtering precipitate is collected filtrate; With the 110 type cation exchange resin columns of filtrate,, collect eluent with the ammonia eluting exchanger resin of 5 times of amount column volumes 5% by 1 times of medical material amount volume; Reclaim ammonia, eluent is concentrated into dried, the Radix Sophorae Flavescentis biology total alkali.
4. as the arbitrary described pharmaceutical composition of claim 1-3, it is characterized in that Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract is prepared from by following method:
Get the Smilax lanceaefolia Roxb. Var.opaca A.DC. decoction pieces, be crushed to coarse powder, add the water supersound extraction 2 times, each 30 minutes, amount of water was respectively 6 times and 4 times, got extracting solution; Centrifugal behind the extracting liquid filtering, get clear liquor; Through the HPD-100 type macroporous adsorptive resins of 5 times of medical material amount volumes, flow velocity is 1 times of column volume per hour, discards effluent; Get macroporous adsorptive resins express developed with 1 times of column volume purified water, 5 times of column volume amounts of reuse purified water eluting, flow velocity is 2 times of column volumes per hour; Collect eluent, concentrating under reduced pressure, drying gets Smilax lanceaefolia Roxb. Var.opaca A.DC. Extract.
5. pharmaceutical composition with antitumor action is characterized in that the raw material of this pharmaceutical composition consists of:
Matrine 1-30 weight portion oxymatrine 1-30 weight portion
Sophocarpine 1-20 weight portion N-oxysophocarpine 1-20 weight portion
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 1-20 weight portion.
6. pharmaceutical composition as claimed in claim 5 is characterized in that the raw material of this pharmaceutical composition consists of:
Matrine 20 weight portion oxymatrines 20 weight portions
Sophocarpine 5 weight portion N-oxysophocarpine 5 weight portions
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 15 weight portions;
Or
Matrine 15 weight portion oxymatrines 25 weight portions
Sophocarpine 5 weight portion N-oxysophocarpine 15 weight portions
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 5 weight portions;
Or
Matrine 25 weight portion oxymatrines 15 weight portions
Sophocarpine 15 weight portion N-oxysophocarpine 5 weight portions
Smilax lanceaefolia Roxb. Var.opaca A.DC. glycosides 10 weight portions.
7. as claim 5 or 6 described pharmaceutical compositions, the raw material that it is characterized in that this pharmaceutical composition is formed and is added in the following raw material one or both again:
Sophoridine 0.5-5 weight portion sophoramine 0.5-5 weight portion.
8. as claim 5 or 6 described pharmaceutical compositions, the raw material that it is characterized in that this pharmaceutical composition is formed and is added in the following raw material one or both again:
Sophoridine 2 weight portion sophoramines 2 weight portions
Or
Sophoridine 1 weight portion sophoramine 4 weight portions;
Or
Sophoridine 4 weight portion sophoramines 1 weight portion.
9. as the arbitrary described pharmaceutical composition of claim 1-8, it is characterized in that getting raw material, add conventional adjuvant, make the dosage form of clinical acceptance according to common process: tablet, granule, oral liquid, pill, capsule, slow releasing preparation or injection.
10. has application in the medicine of antitumor action as the arbitrary described pharmaceutical composition of claim 1-8 in preparation.
11. have in preparation as the arbitrary described pharmaceutical composition of claim 1-8 and to alleviate cancerous protuberance pain, improve cancer patient's immunity, and improve the application in the medicine of effect of its quality of life.
12. have pain relieving, hemostasis, antihepatitic activity as the arbitrary described pharmaceutical composition of claim 1-8 in preparation, the application in the medicine of treatment hepatic fibrosis.
13. as the application of the arbitrary described pharmaceutical composition of claim 1-8 in preparing the medicine that tumor chemotherapeutic drug is had the efficacy enhancing and toxicity reducing effect.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201010164339A CN101822770A (en) | 2010-04-29 | 2010-04-29 | Medicinal composition with anti-tumor effect and application thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201010164339A CN101822770A (en) | 2010-04-29 | 2010-04-29 | Medicinal composition with anti-tumor effect and application thereof |
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| Publication Number | Publication Date |
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| CN101822770A true CN101822770A (en) | 2010-09-08 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201010164339A Pending CN101822770A (en) | 2010-04-29 | 2010-04-29 | Medicinal composition with anti-tumor effect and application thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114558059A (en) * | 2022-02-25 | 2022-05-31 | 南京中医药大学 | Radix sophorae flavescentis-coptis chinensis extract with anti-tumor activity and quality detection method and application thereof |
| CN114617894A (en) * | 2022-02-17 | 2022-06-14 | 暨南大学附属第一医院（广州华侨医院） | Pharmaceutical composition and application thereof in preparation of medicine for treating colon cancer |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1171960A (en) * | 1997-07-16 | 1998-02-04 | 山西金晶药业有限公司 | Compound sophora flavescens injection |
| CN1679883A (en) * | 2005-02-04 | 2005-10-12 | 张海峰 | Compound light-yellow sophora root freeze-drying injection and preparation thereof |
| CN1876016A (en) * | 2005-06-07 | 2006-12-13 | 北京振东光明药物研究院 | Preparation method of compound kuhseng preparation for injection and medical use thereof |
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2010
- 2010-04-29 CN CN201010164339A patent/CN101822770A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1171960A (en) * | 1997-07-16 | 1998-02-04 | 山西金晶药业有限公司 | Compound sophora flavescens injection |
| CN1679883A (en) * | 2005-02-04 | 2005-10-12 | 张海峰 | Compound light-yellow sophora root freeze-drying injection and preparation thereof |
| CN1876016A (en) * | 2005-06-07 | 2006-12-13 | 北京振东光明药物研究院 | Preparation method of compound kuhseng preparation for injection and medical use thereof |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114617894A (en) * | 2022-02-17 | 2022-06-14 | 暨南大学附属第一医院（广州华侨医院） | Pharmaceutical composition and application thereof in preparation of medicine for treating colon cancer |
| CN114558059A (en) * | 2022-02-25 | 2022-05-31 | 南京中医药大学 | Radix sophorae flavescentis-coptis chinensis extract with anti-tumor activity and quality detection method and application thereof |
| CN114558059B (en) * | 2022-02-25 | 2023-09-29 | 南京中医药大学 | Radix Sophorae Flavescentis-Coptidis rhizoma extract with antitumor activity, and quality detection method and application thereof |
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Application publication date: 20100908 |