CN101411780B - Pharmaceutical composition with function for resisting malignant tumor and preparation method thereof - Google Patents
Pharmaceutical composition with function for resisting malignant tumor and preparation method thereof Download PDFInfo
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- CN101411780B CN101411780B CN200710056165A CN200710056165A CN101411780B CN 101411780 B CN101411780 B CN 101411780B CN 200710056165 A CN200710056165 A CN 200710056165A CN 200710056165 A CN200710056165 A CN 200710056165A CN 101411780 B CN101411780 B CN 101411780B
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Abstract
The invention discloses a medicine composition with remarkable treatment effect against malignant tumor, small toxic side effect and safe use. The composition consists of an extract of traditional Chinese medicine Solanum nigrum and Sophora alopecuroide, seeds of herba sophorae alopecuroide as a leguminous plant or oxymatrine extracted from roots of kuhseng as the leguminous plant. In the medicine composition, the content of total alkaloids from solanum nigrum of the extract of the Solanum nigrum is more than 50 percent. In the medicine composition, the content of the total alkaloids from solanum nigrum is 1 to 4 weight portions more than 50 percent of the extract of the Solanum nigrum and 1 to 3 weight portions of the oxymatrine, wherein the preferred proportion is that the content of the total alkaloids from solanum nigrum is 3 weight portions more than 50 percent of the extract of the Solanum nigrum and 2 weight portions of the oxymatrine. The invention also discloses a method for preparing the medicine composition.
Description
Technical field
The present invention relates to a kind of drug regimen of treating malignant tumor; Said composition contains the kurarinone that extracts in the root by seed Herba Sophorae alopecuroidis of Herba Solani Nigri total alkaloids that extracts in the Chinese medicine Herba Solani Nigri and leguminous plant Sophora Alopecuroides L. or leguminous plant Radix Sophorae Flavescentis; This pharmaceutical composition has obvious effect to the treatment of malignant tumor, and the present invention also provides this preparation of drug combination method.
Background technology
Modern society's cancer (malignant tumor) has become one of subject matter that threatens human life's health; The World Health Organization's report shows; Incidence trend according to present cancer; The year two thousand twenty whole world cancer morbidity will be than present increase by 50%, and the annual newly-increased cancer patient's number in the whole world will reach 1,500 ten thousand people.The medical profession urgent needs is cancer treatment drugs safely and effectively.
Herba Solani Nigri total alkaloids of the present invention derives from single medical material---Herba Solani Nigri.Herba Solani Nigri is the Solanaceae nightshade, one to several years this plant of SHENGCAO, cold in nature, bitter in the mouth, little sweet, have mild toxicity, return lung, stomach, urinary bladder channel, the effect of heat-clearing and toxic substances removing, promoting blood circulation to remove blood stasis, inducing diuresis to remove edema, eliminating phlegm and stopping cough is arranged.But Herba Solani Nigri all herbal medicine, oral administration and external.Obtained the extensive concern of Chinese scholars in recent years as the Herba Solani Nigri of Chinese medicine; Pharmacy man has carried out further purification analysis to the chemical constituent of its single medicinal material on the basis of original Chinese medical theory at home and abroad; Carried out a large amount of research; No matter obtained comparatively objectively information, in the research of anti-tumor aspect, be that single medicinal material or its compound preparation are being done a large amount of work aspect basis and the clinical medicine especially.Herb of Herba Solani Nigri contains glycoside steroid alkaloid, Herba Solani Nigri polysaccharide, mineral, vitamin, pigment, aminoacid etc.; Also contain ester, carboxyl compound, sterol, phenoloid (its main component is yellow beta-unsaturated esters) in the extract in the Herba Solani Nigri berry, contain saponin in addition.And the chemical constituent that oncotherapy plays a crucial role is mainly Herba Solani Nigri total alkaloids (comprising solasonine, solamargine etc.), be polysaccharide secondly.
Kurarinone of the present invention; It is a kind of alkaloid that from the root of the seed Herba Sophorae alopecuroidis of leguminous plant Sophora Alopecuroides L. (Sophoro alopecuroides L.) or leguminous plant Radix Sophorae Flavescentis (Sophoro flavescens Ait.), extracts; Wherein oxymatrine concentration＞98% is the main component in the kurarinone.In the pharmacology and clinical research a large amount of, find that it has multiple pharmacological effect such as antiinflammatory, antiviral, anti-hepatic fibrosis and the liver protecting and ALT lowering, anticancer, leukocyte increasing, anti-arrhythmia, and untoward reaction is less to kurarinone.
We combine documents and materials; The utilization modern scientific method is studied at aspects such as preparation technology, quality standard, drug effect, toxicity and stability, is that raw material is processed pharmaceutical preparation with Herba Solani Nigri total alkaloids and kurarinone; Be used for treatment of cancer, have the effect of efficacy enhancing and toxicity reducing.At present; Relevant Herba Solani Nigri total alkaloids of Shang Weijian and folk prescription thereof, compound preparation are applied to the report aspect antitumor drug; Domestic still do not have the preparation of relevant Herba Solani Nigri total alkaloids to register at SFDA, and the patent protection content close with the present invention all do not appear in patent (Chinese patent, Japan Patent, Korean Patent, European patent, United States Patent (USP) etc.) both at home and abroad.
Summary of the invention
The purpose of this invention is to provide drug regimen that a kind of anti-malignant tumor is evident in efficacy, toxic and side effects is little, safe in utilization and preparation method thereof.This drug regimen is raw material with Herba Solani Nigri total alkaloids content greater than 50% Herba Solani Nigri extract and kurarinone.
The present invention realizes through following technical scheme:
1. in the Herba Solani Nigri extract of the present invention, Herba Solani Nigri total alkaloids content is more than 50.0%.
The extraction step of Herba Solani Nigri total alkaloids is following:
Get herb of Herba Solani Nigri and fruit, add 50%～90% alcoholic solution and extract each 6～8 times of amounts 2～3 times; Reclaim ethanol, be concentrated into relative density 1.25, add the 0.1mol/l acid solution of 2～4 times of amounts in the concentrated solution; Fully stir, cold preservation is filtered; Filtering residue is with hydrochloric acid solution washing 1～3 time, and merging filtrate and cleaning mixture are with low pole or middle polarity resin absorption.First water flushing resin column/bed to effluent is closely neutral behind the resin absorption; Closely colourless with 0.1mol/l alkaline solution flushing resin column/bed to effluent again, closely colourless to contain alcohol amount 10%～40% ethanol liquid flushing resin column/bed to effluent again.Discard.Carry out eluting with 50～90% ethanol again, show colourless, collect eluent, reclaim ethanol, transfer pH value to 8～10, leave standstill cold preservation, collecting precipitation with the alkaline solution of 0.5～1.5mol/l to there not being the alcohol flavor to eluent.Naturally dry, get final product Herba Solani Nigri total alkaloids content greater than 50% Herba Solani Nigri extract.
2. above-mentioned Herba Solani Nigri extract and kurarinone is even with the regulation mixed, add suitable adjuvant, promptly get drug regimen according to the invention.
Above-described alkaline solution is selected from sodium hydroxide, calcium hydroxide, potassium hydroxide, magnesium hydroxide and ammonia spirit; Described acid solution is selected from acetic acid, hydrochloric acid, sulphuric acid and citric acid solution; Described eluting uses organic solvent one or two or three mixed phase that form with arbitrary proportion as methanol, ethanol, n-butyl alcohol, chloroform, benzene.
Contain Herba Solani Nigri total alkaloids content in the drug regimen of the present invention greater than 50% Herba Solani Nigri extract 1～4 weight portion, kurarinone 1～3 weight portion.Wherein preferred proportion is a Herba Solani Nigri total alkaloids content greater than 50% Herba Solani Nigri extract 3 weight portions, kurarinone 2 weight portions.
Pharmaceutical preparation of the present invention contains 1%～99% Herba Solani Nigri total alkaloids content greater than 50% the Herba Solani Nigri extract and the pharmaceutical excipient (comprising the medicine that other compatibility is used) of kurarinone mixture and 99%～1%; Preferably contain 45%～95% Herba Solani Nigri total alkaloids content greater than 50% the Herba Solani Nigri extract and the pharmaceutical excipient (comprising the medicine that other compatibility is used) of kurarinone mixture and 55%～5%, preferably contain 75%～90% Herba Solani Nigri total alkaloids content greater than 50% the Herba Solani Nigri extract and the pharmaceutical excipient (comprising the medicine that other compatibility is used) of kurarinone mixture and 25%～10%.
Press practice of pharmacy, can become the various clinical pharmaceutical dosage form as antitumor drug greater than 50% Herba Solani Nigri extract with the kurarinone preparation of compositions Herba Solani Nigri total alkaloids content of the present invention, comprise the dosage form of oral formulations or parenterai administration.Said oral formulations is tablet, capsule, granule, powder, pill, suspensoid, oral liquid etc.; Said parenterai administration dosage form is injection, infusion solution, freeze dried injection, injectable emulsion, aerosol, suppository etc.
Adjuvant in the antitumor drug combination preparation of the present invention is meant conventional excipient, as: solvent, disintegrating agent, correctives, binding agent, coloring agent, antiseptic etc.The medicine that other compatibility in the antitumor drug of the present invention is used, the Herba Solani Nigri extract and the kurarinone compositions that refer to effective dose are certain medicine material, again compatibility other allowed the Chinese medicine or the chemical drugs that share.
Herba Solani Nigri total alkaloids content of the present invention has antitumor action greater than 50% Herba Solani Nigri extract and kurarinone drug regimen and pharmaceutical preparation thereof, is to be confirmed greater than 50% Herba Solani Nigri extract 3 weight portions and the pharmacodynamic experiment of kurarinone 2 medicaments in part by weight combination through following Herba Solani Nigri total alkaloids content.
Experimental example 1The external inhibitory action of Herba Solani Nigri extract and kurarinone pharmaceutical composition to tumor
Herba Solani Nigri extract and kurarinone pharmaceutical composition (3: 2) are divided into five groups of dosage (0.5,2.5,12.5,50,150 μ gml
-1), interaction in vitro is in 10 kinds of tumor cells respectively.Can find out from whole experiment; Under 150 μ g/ml and 50 μ g/ml dosage; Drug regimen all shows very strong inhibitory action for 10 kinds of tumor cells, and along with the reduction of drug level, tumor control rate descends gradually; When drug regimen concentration was reduced to 0.4 μ g/ml, tumor cell was unaffected basically.This drug regimen is respectively 10.38 μ g/ml (SMMC-7721), 15.47 μ g/ml (BGC-803), 12.45 μ g/ml (A549), 12.93 μ g/ml (LOVO), 11.08 μ g/ml (B16), 5.81 μ g/ml (NCI-H460), 11.26 μ g/ml (KETR-3), 29.14 μ g/ml (PC-12), 5.10 μ g/ml (ECA-109), 120.17 μ g/ml (S180) to the half suppression ratio of various tumor cells through calculating.
See that from the tumor cell form under 150 μ g/ml and 50 μ g/ml dosage effects, the tumor cell structure is all destroyed, cell quantity is rare; Along with the reduction of drug regimen dosage, the tumor cell form is tending towards complete, but quantity is still less; At 0.5 μ gml
-1Under the dosage, drug regimen disappears to the inhibitory action of tumor, and cellular morphology is complete, and quantity is more.
In sum; Herba Solani Nigri total alkaloids content all has stronger inhibitory action for various tumor cells external greater than 50% Herba Solani Nigri extract 3 weight portions and the combination of kurarinone 2 medicaments in part by weight; Can obviously suppress tumor cell in external growth; Change the form of tumor cell, cause the death of tumor cell.
Experimental example 2Herba Solani Nigri extract and kurarinone pharmaceutical composition are to the influence of Hep hepatocarcinoma transplanted tumor
Experimental technique: aseptic condition extracts 8 days ascites cells suspension of growth in the ICR mouse peritoneal down; Cancerous cell suspension and sterile saline are got 70 of ICR mices, ♀ ♂ half and half by dilution in 1: 3; Body weight 18～22g, the cancerous cell suspension 0.2ml after the inoculation dilution is subcutaneous in armpit.Be divided into 7 groups behind the 24h at random; Be model group, 5-Fu group (25mg/kg), cinobufacin group (3g/kg) and injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose organizes (1.2mg/kg, 2.4mg/kg, 4.8mg/kg) and oral group (2.4mg/kg); Every group 10; Intravenous injection gives relative medicine Pu type group injection isometric(al) normal saline, oral group of gastric infusion respectively), the administration volume is 10ml/kg.Administration was put to death mice after 8 days, stripped tumor, weighed, and calculated tumour inhibiting rate by following formula.Experiment repetition 2 times.
Experimental result: after the mouse inoculation Hep hepatocarcinoma tumor; 4 days subcutaneous can contact tumor, dissects exemplary embodiment lock after 8 days all greater than 1g, and three dose groups mouse tumors of drug regimen soak into scope all less than model group; The tumor body is prone to peel off, and tumor weight obviously alleviates (P＜0.01).Drug regimen does not have obvious influence to weight of mice rate, thymus index, spleen index.The tumour inhibiting rate of three dose groups of drug regimen intravenous injection is all greater than oral group.The result sees table 1-5.
Table 1 injection Herba Solani Nigri extract and kurarinone drug regimen are to the influence (
n=10) of Hep hepatocarcinoma transplanted solid tumor tumour inhibiting rate
Annotate: compare with model group,
*P＜0.05,
*P＜0.01.
The influence of table 2 pair Hep hepatocarcinoma transplanted solid tumor weight of mice rate (experiment for the first time) (
n=10)
Annotate: compare with model group,
*P＜0.01.
The influence of table 3 pair Hep hepatocarcinoma transplanted solid tumor mouse thymus index, spleen index (experiment for the first time)
Annotate: compare with model group,
*P＜0.01.
The influence of table 4 pair Hep hepatocarcinoma transplanted solid tumor weight of mice rate (experiment for the second time) (
n=10)
Annotate: compare with model group,
*P＜0.01.
Table 5 pair Hep hepatocarcinoma transplanted solid tumor mouse thymus index, the influence of spleen index (experiment for the second time)
Annotate: compare with model group,
*P＜0.01.
Experimental example 3Herba Solani Nigri extract and kurarinone pharmaceutical composition are to S
180The influence of transplanted solid tumor tumour inhibiting rate
Experimental technique: aseptic condition extracts 8 days ascites cells suspension of growth in the ICR mouse peritoneal down; Cancerous cell suspension and sterile saline are got 70 of ICR mices, ♀ ♂ half and half by dilution in 1: 3; Body weight 18～22g, the cancerous cell suspension 0.2ml after the inoculation dilution is subcutaneous in armpit.Be divided into 7 groups behind the 24h at random; Be model group, 5-Fu group (25mg/kg), cinobufacin group (3g/kg) and injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose organizes (1.2mg/kg, 2.4mg/kg, 4.8mg/kg) and oral group (2.4mg/kg); Every group 10; Intravenous injection gives relative medicine (model group injection isometric(al) normal saline, oral group of gastric infusion) respectively, and the administration volume is 10ml/kg.Administration was put to death mice after 8 days, stripped tumor, weighed, and calculated tumour inhibiting rate by following formula.Experiment repetition 2 times.
Result of the test: behind the mouse inoculation S180 transplanted solid tumor; 3 days subcutaneous can contact tumor, dissects exemplary embodiment lock after 8 days all greater than 1g, and three dose groups mouse tumors of injectable drug combination soak into scopes all less than model group; The tumor body is prone to peel off, and tumor weight obviously alleviates (P＜0.01).The injectable drug combination does not have obvious influence to weight of mice rate, thymus index, spleen index.The tumour inhibiting rate of three dose groups of injectable drug combination intravenous injection is all greater than oral group.The result sees table 6～10.
Table 6 injection Herba Solani Nigri extract and kurarinone drug regimen are to the influence (
n=10) of S180 transplanted solid tumor tumour inhibiting rate
Annotate: compare with model group,
*P＜0.05,
*P＜0.01.
The influence of table 7 pair S180 transplanted solid tumor weight of mice rate (experiment for the first time) (
n=10)
Annotate: compare with model group,
*P＜0.01.
Table 8 couple S
180The influence of transplanted solid tumor mouse thymus index, spleen index (experiment for the first time)
Annotate: compare with model group,
*P＜0.01.
The influence of table 9 pair S180 transplanted solid tumor weight of mice rate (experiment for the second time) (
n=10)
Annotate: compare with model group,
*P＜0.01.
The influence of table 10 pair S180 transplanted solid tumor mouse thymus index, spleen index (experiment for the second time)
Annotate: compare with model group,
*P＜0.01.
Experimental example 4Herba Solani Nigri extract and kurarinone pharmaceutical composition are to the influence of Walker-256 transplantability Hepar Mus cancer
Experimental technique: rat model is divided into 5 groups at random, 10 every group.Be model group, cinobufacin group (25mg/kg) and injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose of group (1.2mg/kg, 2.4mg/kg, 4.8mg/kg).Each is organized rat and gives the corresponding reagent thing that receives respectively, and the administration volume is 10ml/kg, successive administration 10 days.After the administration 10 days, take off cervical vertebra and put to death rat, record weight size is calculated gross tumor volume according to following formula.Tumor tissues is used 10% formaldehyde fixed, pathological study to be done.
Experimental result: in injection Herba Solani Nigri extract and the kurarinone drug regimen, the gross tumor volume of heavy dose of group compares with model group, significantly dwindles, and has statistical significance (P＜0.05).Pathological examination scoring shows in injection Herba Solani Nigri extract and the kurarinone drug regimen, heavy dose of group can reduce gross tumor volume, inhibition tumor growth (P＜0.05).
Pathologic finding shows:
(1) after the Walker-256 cancer ascites is planted liver, in liver, form lump, in the lump oncocyte atypia obvious, size, form differ, nuclear is big, engrain, karyokinesis are prone to see mutually.Tumor cell is arranged closely, and the subregion has downright bad and hemorrhage.Tumor without capsule is infiltrative growth to the periphery hepatocyte.
(2) tumor-bearing rat decreased number behind application injection Herba Solani Nigri extract and the kurarinone drug regimen, the gross tumor volume of formation reduces, and is obviously downright bad.Part connective tissue peplos appears in the tumor periphery, and sees that mononuclearcell soaks into.The above results is explained in injection Herba Solani Nigri extract and the kurarinone drug regimen, heavy dose of medicine has inhibitory action to plantation property Walker-256 hepatocarcinoma.The result sees table 11～12.
The influence
of table 11 pair Walker-256 transplantability Hepar Mus tumor volume
Annotate: compare with model group,
*P＜0.01.
The influence
of table 12 pair Walker-256 transplantability Hepar Mus carninomatosis reason scoring
Annotate: compare with model group,
*P＜0.01.
Experimental example 5Herba Solani Nigri extract and kurarinone pharmaceutical composition are to lotus Hep liver cancer mouse leukocyte, hematoblastic influence
Experimental technique: aseptic condition extracts 8 days ascites cells suspension of growth in the ICR mouse peritoneal down, and cancerous cell suspension and sterile saline are got 70 of ICR mices by dilution in 1: 3, and the cancerous cell suspension 0.2ml after the inoculation dilution is subcutaneous in armpit.Be divided into 7 groups behind the 24h at random; Be model group, 5-Fu group (25mg/kg), cinobufacin group (3g/kg) and injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose organizes (1.2mg/kg, 2.4mg/kg, 4.8mg/kg) and oral group (2.4mg/kg); Every group 10; Intravenous injection gives relative medicine (model group injection isometric(al) normal saline, oral group of gastric infusion) respectively, and the administration volume is 10ml/kg.Administration was put to death mice after 8 days, stripped tumor, weighed, and calculated tumour inhibiting rate by following formula.
Experimental result: after the mouse inoculation Hep hepatocarcinoma tumor; 4 days subcutaneous can contact tumor; Dissect exemplary embodiment lock after 8 days all greater than 1g; Three dose groups mouse tumors of injection Herba Solani Nigri extract and kurarinone drug regimen soak into scope all less than model group, and the tumor body is prone to peel off, and tumor weight obviously alleviates (P＜0.01).Injection Herba Solani Nigri extract and kurarinone drug regimen do not have obvious influence to murine interleukin, platelet, body weight gain rate, thymus index, spleen index.The tumour inhibiting rate of injection Herba Solani Nigri extract and three dose groups of kurarinone drug regimen intravenous injection is all greater than oral group.The result sees table 13～16.
Table 13 injection Herba Solani Nigri extract and kurarinone drug regimen are to the influence (
n=10) of Hep hepatocarcinoma transplanted solid tumor tumour inhibiting rate
Annotate: compare with model group,
*P＜0.05,
*P＜0.01.
The influence of table 14 pair Hep hepatocarcinoma transplanted solid tumor weight of mice rate (experiment for the first time) (
n=10)
Annotate: compare with model group,
*P＜0.01.
The influence of table 15 pair Hep hepatocarcinoma transplanted solid tumor mouse thymus index, spleen index (experiment for the first time)
Annotate: compare with model group,
*P＜0.01.
The influence
of table 16 pair Hep hepatocarcinoma transplanted solid tumor murine interleukin, platelet count
Annotate: compare with model group,
*P＜0.01.
Experimental example 6Herba Solani Nigri extract and kurarinone pharmaceutical composition subtract mould effect to the potentiation of lotus tumor (Hep) mice 60Co radiotherapy
Experimental technique: aseptic condition extracts 8 days ascites cells suspension of growth in the ICR mouse peritoneal down; Cancerous cell suspension and sterile saline are got 70 of ICR mices, ♀ ♂ half and half by dilution in 1: 3; Body weight 18～22g, the cancerous cell suspension 0.2ml after the inoculation dilution is subcutaneous in armpit.Be divided into 7 groups behind the 24h at random, i.e. model group, combination radiotherapy group, radiotherapy adds cinobufacin group (3g/kg) and radiotherapy adds the injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose of group (1.2mg/kg, 2.4mg/kg, 4.8mg/kg) and oral group (2.4mg/kg), 10 every group; Except that model group; Other all shine once with 60Co after respectively organizing mouse inoculation 24h, and exposure dose is 500Cgy, penetrate back 2h; Radiotherapy adds the cinobufacin group; Radiotherapy adds the injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose organizes respectively that intravenous injection gives relative medicine, model group injection isometric(al) normal saline, oral group of gastric infusion.Posterior orbit was got blood in 8 days, measured routine blood test.Put to death mice after getting blood, strip tumor, weigh, calculate tumour inhibiting rate by following formula; Get thymus, spleen, weigh, calculate thymus index and spleen index according to following formula.
Experimental result: behind the mouse inoculation Hep hepatocarcinoma transplanted solid tumor; Model group 4 days is subcutaneous can to contact tumor; Dissect exemplary embodiment lock after 8 days greater than 1g; Radiotherapy and radiotherapy add the injection Herba Solani Nigri extract and three dose groups mouse tumors of kurarinone drug regimen soak into scope all less than model group, and the tumor body is prone to peel off, and tumor weight obviously alleviates (P＜0.01).Radiotherapy adds injection Herba Solani Nigri extract and three dose groups tumors of kurarinone drug regimen weight average and strives less than combination radiotherapy group (P＜0.05, P＜0.01) and show that injection Herba Solani Nigri extract and kurarinone drug regimen are right
60Co radiotherapy has certain potentiation.Radiotherapy adds leukocyte and the platelet count of injection Herba Solani Nigri extract and three dose groups of kurarinone drug regimen all greater than combination radiotherapy group, but not statistically significant.Radiotherapy adds the injection Herba Solani Nigri extract and three dose groups weight of mice of kurarinone drug regimen rate all is higher than combination radiotherapy group (P＜0.01); Radiotherapy adds the injection Herba Solani Nigri extract and the heavy dose of thymus index of kurarinone drug regimen is higher than combination radiotherapy group (P＜0.05), has statistical significance.The result sees table 17～20.
The influence
of table 17 pair lotus tumor (Hep) mice tumour inhibiting rate
Annotate: compare with model group
△ △P＜0.01; Compare with combination radiotherapy group,
*P＜0.05,
*P＜0.01.
The influence
of table 18 pair lotus tumor (Hep) murine interleukin, platelet count
Annotate: compare with model group,
△ △P＜0.01; Combination radiotherapy group is compared,
*P＜05,
The influence (
n=10) of table 19 pair lotus tumor (Hep) weight of mice rate
Annotate: with model group mutually, comparison,
△ △P＜0.01; Compare with combination radiotherapy group,
*P＜0.05,
*P＜0.01.
The influence
of table 20 pair lotus tumor (Hep) mouse thymus index, spleen index
Annotate: compare with model group,
△ △P＜0.01; Compare with combination radiotherapy group
*P＜0.05.
Experimental example 7Herba Solani Nigri extract and kurarinone pharmaceutical composition are to lotus tumor (S
180) the efficacy enhancing and toxicity reducing effect of mice CTX chemotherapy
Experimental technique: aseptic condition extracts 8 days ascites cells suspension of growth in the ICR mouse peritoneal down; Cancerous cell suspension and sterile saline are got 70 of ICR mices, ♀ ♂ half and half by dilution in 1: 3; Body weight 18～22g, the cancerous cell suspension 0.2ml after the inoculation dilution is subcutaneous in armpit.Be divided into 7 groups behind the 24h at random; Be model group, CTX group (10mg/kg), CTX (10mg/kg) adds cinobufacin group (3g/kg) and CTX (10mg/kg) adds the injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose organizes (1.2mg/kg, 2.4mg/kg, 4.8mg/kg) and oral group (2.4mg/kg); Every group 10, intravenous injection gives relative medicine (model group injection isometric(al) normal saline, oral group of gastric infusion) respectively; Posterior orbit was got blood in 8 days, measured routine blood test.Put to death mice after getting blood, strip tumor, weigh, calculate tumour inhibiting rate by following formula; Get thymus, spleen, weigh, calculate thymus index and spleen index according to following formula.
Experimental result: mouse inoculation S
180Behind the midship transplanted solid tumor; 3 days subcutaneous can contact tumor; Dissect exemplary embodiment lock after 8 days all greater than 1g; CTX and CTX add the injection Herba Solani Nigri extract and three dose groups mouse tumors of kurarinone drug regimen soak into scope all less than model group, and the tumor body is prone to peel off, and tumor weight obviously alleviates (P＜0.01).CTX adds the injection Herba Solani Nigri extract and three dose groups tumors of kurarinone drug regimen weight average is organized less than CTX, and wherein CTX adds in the injection Herba Solani Nigri total alkaloids, heavy dose is organized compares with the CTX group, and statistical significance (P＜0.05, P＜0.01) is arranged.Show that injection Herba Solani Nigri extract and kurarinone drug regimen have certain antitumor potentiation to CTX.CTX adds the leukocyte of three dose groups of injection Herba Solani Nigri extract and kurarinone drug regimen and compares no significant difference with platelet with the CTX group.The thymus index that CTX adds injection Herba Solani Nigri extract and the heavy dose of group of kurarinone drug regimen mice is significantly higher than CTX group (P＜0.05); The body weight gain rate that CTX adds injection Herba Solani Nigri extract and three dose groups mices of kurarinone drug regimen all is significantly higher than CTX group (P＜0.05, P＜0.01).The result sees table 21～24.
Table 21 couple lotus tumor (S
180) influence of mice tumour inhibiting rate
Annotate: compare with model group
△ △P＜0.01; Compare with the CTX group,
*P＜0.05,
*P＜0.01.
Table 22 pair influence
to lotus tumor (S180) murine interleukin, platelet count
Annotate: compare with model group,
△ △P＜0.01.
Table 23 is pair to lotus tumor (S
180) the weight of mice rate influence (
N=10)
Annotate: compare with model group,
△ △P＜0.01; Compare with the CTX group,
*P＜0.05,
*P＜0.01.
Table 24 is pair to lotus tumor (S
180) influence of mouse thymus index, spleen index
Annotate: compare with model group,
△ △P＜0.01; Compare with the CTX group
*P＜0.05.
Experimental example 8Herba Solani Nigri extract and kurarinone pharmaceutical composition are to the efficacy enhancing and toxicity reducing effect of lotus tumor (Hep) mice MMC chemotherapy
Experimental technique: aseptic condition extracts 8 days ascites cells suspension of growth in the ICR mouse peritoneal down; Cancerous cell suspension and sterile saline are got 70 of ICR mices, ♀ ♂ half and half by dilution in 1: 3; Body weight 18～22g, the cancerous cell suspension 0.2ml after the inoculation dilution is subcutaneous in armpit.Be divided into 7 groups behind the 24h at random; Be model group, MMC group (1mg/kg), MMC (1mg/kg) adds cinobufacin group (3g/kg) and MMC (1mg/kg) adds the injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose organizes (1.2mg/kg, 2.4mg/kg, 4.8mg/kg) and oral group (2.4mg/kg); Every group 10, intravenous injection gives relative medicine (model group injection isometric(al) normal saline, oral group of gastric infusion) respectively; Put to death mice after 8 days; Strip tumor, weigh, calculate tumour inhibiting rate by following formula.Get thymus, spleen, weigh, calculate thymus index and spleen index according to following formula.
Experimental result: behind the mouse inoculation Hep hepatocarcinoma transplanted solid tumor; 4 days subcutaneous can contact tumor; Dissect exemplary embodiment lock after 8 days all greater than 1g; MMC and MMC add the injection Herba Solani Nigri extract and three dose groups mouse tumors of kurarinone drug regimen soak into scope all less than model group, and the tumor body is prone to peel off, and tumor weight obviously alleviates (P＜0.01).MMC adds the injection Herba Solani Nigri extract and three dose groups tumors of kurarinone drug regimen weight average is organized less than MMC, and wherein MMC adds in injection Herba Solani Nigri extract and the kurarinone drug regimen, heavy dose of group compares with the MMC group, and statistical significance (P＜0.01) is arranged.Show that injection Herba Solani Nigri extract and kurarinone drug regimen have certain antitumor potentiation to MMC.MMC adds the injection Herba Solani Nigri extract and compares no significant difference with leukocyte, platelet, thymus index and the spleen index of three dose groups of kurarinone drug regimen with the MMC group.The body weight gain rate that MMC adds injection Herba Solani Nigri extract and three dose groups mices of kurarinone drug regimen all is significantly higher than MMC group (P＜0.01).The result sees table 25～28.
The influence
of table 25 pair lotus tumor (Hep) mice mice tumour inhibiting rate
Annotate: compare with model group
△ △P＜0.01; Compare with the MMC group,
*P＜0.05,
*P＜0.01.
The influence
of table 26 pair lotus tumor (Hep) murine interleukin, platelet count
Annotate: compare with model group,
△ △P＜0.01; Compare with the MMC group
*P＜0.05.
The influence (
n=10) of table 27 pair lotus tumor (Hep) weight of mice rate
Annotate: compare with model group,
△ △P＜0.01; Compare with the MMC group,
*P＜0.05,
*P＜0.01.
The influence (
n=10) of table 28 pair lotus tumor (Hep) mouse thymus index, spleen index
Annotate: compare with model group,
△ △P＜0.01; Compare with the MMC group
*P＜0.05.
Experimental example 9Herba Solani Nigri extract and kurarinone pharmaceutical composition subtract mould effect to the potentiation of lotus tumor (Hep) mice 5-Fu chemotherapy
Experimental technique: aseptic condition extracts 8 days ascites cells suspension of growth in the ICR mouse peritoneal down; Cancerous cell suspension and sterile saline are got 70 of ICR mices, ♀ ♂ half and half by dilution in 1: 3; Body weight 18～22g, the cancerous cell suspension 0.2ml after the inoculation dilution is subcutaneous in armpit.Be divided into 7 groups behind the 24h at random; Be model group, 5-Fu group (15mg/kg), 5-Fu (15mg/kg) adds cinobufacin group (3g/kg) and 5-Fu (15mg/kg) adds the injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose organizes (1.2mg/kg, 2.4mg/kg, 4.8mg/kgg) and oral group (2.4mg/kg); Every group 10, intravenous injection gives relative medicine (model group injection isometric(al) normal saline, injection once next day of the 5-Fu group) respectively; Put to death mice after 8 days; Strip tumor, weigh, calculate tumour inhibiting rate by following formula.
Experimental result: behind the mouse inoculation Hep hepatocarcinoma transplanted solid tumor; 4 days subcutaneous can contact tumor; Dissect exemplary embodiment lock after 8 days all greater than 1g; 5-Fu and 5-Fu add the injection Herba Solani Nigri extract and three dose groups mouse tumors of kurarinone drug regimen soak into scope all less than model group, and the tumor body is prone to peel off, and tumor weight obviously alleviates (P＜0.01).5-Fu adds three dose groups tumors of injection Herba Solani Nigri total alkaloids weight average and organizes less than 5-Fu, and wherein 5-Fu adds the heavy dose of group of injection Herba Solani Nigri extract and kurarinone drug regimen and organizes with 5-Fu and compare, and statistical significance (P＜0.01) is arranged.Show that injection Herba Solani Nigri extract and kurarinone drug regimen have certain antitumor potentiation to 5-Fu.5-Fu adds the injection Herba Solani Nigri extract and compares no significant difference with leukocyte, platelet, spleen index and the 5-Fu group of three dose groups of kurarinone drug regimen.The thymus index that 5-Fu adds injection Herba Solani Nigri extract and the heavy dose of group of kurarinone drug regimen mice is significantly higher than 5-Fu group (P＜0.05), and the body weight gain rate that 5-Fu adds injection Herba Solani Nigri extract and three dose groups mices of kurarinone drug regimen all is significantly higher than 5-Fu group (P＜0.05).The result sees table 29～32.
The influence
of table 29 pair lotus tumor (Hep) mice tumour inhibiting rate
Annotate: compare with model group
△ △P＜0.01; Compare with the CTX group,
*P＜0.05,
*P＜0.01.
The influence
of table 30 pair lotus tumor (Hep) murine interleukin, platelet count
Annotate: compare with model group,
△ △P＜0.01.
The influence (
n=10) of table 31 pair lotus tumor (Hep) weight of mice rate
Annotate: compare with model group,
△ △P＜0.01; Compare with the 5-Fu group,
*P＜0.05,
*P＜0.01.
The influence (
n=10) of table 32 pair lotus tumor (Hep) mouse thymus index, spleen index
Annotate: compare with model group,
△ △P＜0.01; Compare with the 5-Fu group
*P＜0.05.
Experimental example 10Herba Solani Nigri extract and kurarinone pharmaceutical composition are to tumor-bearing mice TNF-α, the influence of IL-2
Experimental technique: aseptic condition extracts 8 days ascites cells suspension of growth in the ICR mouse peritoneal down; Cancerous cell suspension and sterile saline are got 70 of ICR mices, ♀ ♂ half and half by dilution in 1: 3; Body weight 18～22g, the cancerous cell suspension 0.2ml after the inoculation dilution is subcutaneous in armpit.Be divided into 7 groups behind the 24h at random; Be model group, 5-Fu group (25mg/kg), cinobufacin group (3g/kg) and injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose organizes (1.2mg/kg, 2.4mg/kg, 4.8mg/kg) and oral group (2.4mg/kg); Every group 10, other gets 10 mices as the normal control group.Intravenous injection gives relative medicine (normal control group and model group injection isometric(al) normal saline, oral group gastric infusion ') respectively.The administration volume is 10ml/kg.After the administration 8 days, eye socket is got blood, conventional separation of serum ,-20 ℃ of preservations, TNF-α to be measured and IL-2; Take off cervical vertebra and put to death mice, strip tumor, weigh, calculate tumour inhibiting rate according to following formula; Get thymus, spleen, weigh, calculate thymus index and spleen index by following formula.
Experimental result: behind the mouse inoculation S180 transplanted solid tumor; 3 days subcutaneous can contact tumor; Dissect exemplary embodiment lock after 8 days all greater than 1g; Three dose groups mouse tumors of injection Herba Solani Nigri extract and kurarinone drug regimen soak into scope all less than model group, and the tumor body is prone to peel off, and tumor weight obviously alleviates (P＜0.01).Model group mice serum TNF-α, IL-2 content all are lower than the normal control group; Each organizes all can raise serum TNF-α, IL-2 content injection Herba Solani Nigri extract and kurarinone drug regimen; Wherein in injection Herba Solani Nigri extract and the kurarinone drug regimen, heavy dose of group is compared with model group; Has statistical significance (P＜0.05, P＜0.01).The result sees table 33～35.
Table 33 injection Herba Solani Nigri extract and kurarinone drug regimen are to the influence
of S180 transplanted solid tumor tumour inhibiting rate
Annotate: compare with model group,
*P＜0.05,
*P＜0.01.
Table 34 injection Herba Solani Nigri catches gets the influence
to S180 transplanted solid tumor mouse thymus index, spleen index of thing and kurarinone drug regimen
Annotate: compare with normal control group group,
*P＜0.05,
*P＜0.01.
The influence
of table 35 couple S180 transplanted solid tumor mice serum TNF-α and IL-2 content
Annotate: compare with the normal control group,
△ △P＜0.01; Compare with model group
*P＜005,
*P＜0.01.
Experimental example 11Herba Solani Nigri extract and kurarinone pharmaceutical composition are to the influence of mice serum hemolysin amount
Experimental technique: 70 of ICR mices, body weight 20～24g, male and female half and half.Be divided into 7 groups then at random; Every group 10, promptly normal control group, model group, Radix Astragali injection group (6.7g/kg) and injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose of group (1.2mg/kg, 204mg/kg, 4.8mg/kg) and oral group (2.4mg/kg).Each is organized mouse mainline and gives the corresponding reagent thing (normal control group and model group intravenous injection give the isometric(al) normal saline, oral group of gastric infusion) that receives, and the administration volume is 10ml/kg, gives 7 continuously.After the administration the 4th, 6 day, remove all the other each groups of normal control group lumbar injection 30mg/kg cyclophosphamide respectively, normal control group injection isometric(al) normal saline.Each organize mice since the 3rd day respectively lumbar injection 5% sheep red blood cell (SRBC) normal saline suspension 0.2ml carry out immunity, totally 4 days.
30min behind the last gastric infusion, mouse orbit is got blood, and separation of serum 50 μ l are with 500 times of normal saline dilutions.Get dilute serum 1ml; Add 5% sheep red blood cell (SRBC) 0.5ml and 10% complement (fresh Cavia porcellus pooled serum through SRBC＜10: 1＞in 4 ℃ absorb 30min be placed on 20 ℃ subsequent use) 1ml; Mixing is placed on 30min in 37 ℃ of waters bath with thermostatic control, moves to cessation reaction in the ice bath then.The centrifugal 5min of 1500rpm gets supernatant 1ml, adds Dou Shi reagent (sodium bicarbonate 1.0g, high-potassium ferricyanide 0.2g, potassium cyanide 0.05g add distilled water 1000ml) 3ml, behind the placement 10min, surveys the trap value in the 540nm place.
Trap value during the SRBC HD50: get 5%SRBC0.25ml and add Dou Shi liquid to 4ml, behind the placement 10min, colorimetric reads the absorbance value.Calculate the half hemolysis value (HC50) of every mice sample by following formula.
Experimental result: mice serum hemolysin amount descends after the modeling, and model group and normal control group relatively have significant difference (p＜0.05), shows that mice obviously descends through the modeling bleeding from anus lysin level that purifies the blood; Three dose groups of injection Herba Solani Nigri extract and kurarinone drug regimen mice serum blood lysin water gaging that all can obviously raise is flat, with model group significant difference (p＜0.05) is arranged relatively.The result sees table 36.
The influence of table 36 pair mice serum hemolysin
Annotate: compare with the normal control group,
△ △P＜0.01; Compare with model group,
*P＜0.05,
*P＜0.01.
Experimental example 12The influence that Herba Solani Nigri extract and kurarinone pharmaceutical composition are cleaned up the mice carbon granule
Experimental technique: 90 of ICR mices, body weight 18～22g, male and female half and half.Be divided into 6 groups then at random, 15 every group, promptly normal control group, Radix Astragali injection group (6.7g/kg) and injection Herba Solani Nigri extract and the kurarinone drug regimen is little, in, heavy dose of group (1.2mg/kg, 2.4mg/kg, 4.8mg/kg) and oral group (2mg/kg).Intravenous injection gives the corresponding reagent thing (normal control group and model group intravenous injection give the isometric(al) normal saline, oral group of gastric infusion) that receives, and the administration volume is 10ml/kg, gives 5 continuously.30min after the last administration; The india ink 0.1ml/10g of tail vein injection 25%; In 2min and 10min respectively eye socket get blood 20 μ l, add and fill in sodium carbonate liquor (concentration 1mg/ml) test tube of 2ml, go out to survey absorbance OD2min and OD10min at 680nm; The mice of having adopted blood is put to death, get liver, spleen is weighed.Clean up index k and phagocytic index a by following formula calculating.The result organizes a t check.
Experimental result: compare with the normal control group; In injection Herba Solani Nigri extract and the kurarinone drug regimen, heavy dose of group all can increase carbon clearance index and the phagocytic index of mice; Has statistical significance (P＜0.05; P＜0.01), shows that injection Herba Solani Nigri extract and kurarinone drug regimen can strengthen the phagocytic function of mouse monokaryon macrophage.The result sees table 37.
The influence of table 37 pair mice carbon clearance rate (
n=15)
△ △Compare with the blank group p＜0.01;
*P＜0.05,
*Compare with model group p＜0.01.
The specific embodiment
Embodiment 1
The preparation of Herba Solani Nigri extract and kurarinone drug regimen
(1) get herb of Herba Solani Nigri and fruit and add 80% alcoholic solution extraction 3 times, each 8 times of amounts reclaim ethanol; Be concentrated into relative density 1.25, add the 0.1mol/l hydrochloric acid solution of 3 times of amounts in the concentrated solution, fully stir; Cold preservation is filtered, and filtering residue is with hydrochloric acid solution washing 2 times; Merging filtrate and cleaning mixture are with low pole or middle polarity resin absorption.First water flushing resin column/bed to effluent is closely neutral behind the resin absorption; Closely colourless with 0.1mol/l ammonia spirit flushing resin column/bed to effluent again, closely colourless to contain alcohol amount 20% ethanol liquid flushing resin column/bed to effluent again.Discard.Carry out eluting with 70% ethanol again, show colourless, collect eluent, reclaim ethanol, transfer pH value to 9, leave standstill cold preservation, collecting precipitation with the sodium hydroxide solution of 1.0mol/l to there not being the alcohol flavor to eluent.Naturally dry, get final product Herba Solani Nigri total alkaloids content greater than 50% Herba Solani Nigri extract extract.
1. above-mentioned Herba Solani Nigri extract 3 weight portions and kurarinone 2 weight portions with mix homogeneously, promptly got drug regimen according to the invention.
Above-described alkaline solution is selected from sodium hydroxide, calcium hydroxide, potassium hydroxide, magnesium hydroxide and ammonia spirit; Described acid solution is selected from acetic acid, hydrochloric acid, sulphuric acid and citric acid solution; Described eluting uses organic solvent one or two or three mixed phase that form with arbitrary proportion as methanol, ethanol, n-butyl alcohol, chloroform, benzene.
(2) get herb of Herba Solani Nigri and fruit and add 70% alcoholic solution extraction 3 times, each 7 times of amounts reclaim ethanol; Be concentrated into relative density 1.15, add the 0.1mol/l hydrochloric acid solution of 2.5 times of amounts in the concentrated solution, fully stir; Cold preservation is filtered, and filtering residue is with hydrochloric acid solution washing 3 times; Merging filtrate and cleaning mixture are with low pole or middle polarity resin absorption.First water flushing resin column/bed to effluent is closely neutral behind the resin absorption; Closely colourless with 0.1mol/l sodium hydroxide solution flushing resin column/bed to effluent again, closely colourless to contain alcohol amount 30% ethanol liquid flushing resin column/bed to effluent again.Discard.Carry out eluting with 75% ethanol again, show colourless, collect eluent, reclaim ethanol, transfer pH value to 9, leave standstill cold preservation, collecting precipitation with the sodium hydroxide solution of 1.0mol/l to there not being the alcohol flavor to eluent.Naturally dry, get final product Herba Solani Nigri total alkaloids content greater than 50% Herba Solani Nigri extract extract.
2. above-mentioned Herba Solani Nigri extract 2 weight portions and kurarinone 1 weight portion with mix homogeneously, promptly got drug regimen according to the invention.
Above-described alkaline solution is selected from sodium hydroxide, calcium hydroxide, potassium hydroxide, magnesium hydroxide and ammonia spirit; Described acid solution is selected from acetic acid, hydrochloric acid, sulphuric acid and citric acid solution; Described eluting uses organic solvent one or two or three mixed phase that form with arbitrary proportion as methanol, ethanol, n-butyl alcohol, chloroform, benzene.
(3) get herb of Herba Solani Nigri and fruit and add 75% alcoholic solution extraction 2 times, each 8 times of amounts reclaim ethanol; Be concentrated into relative density 1.10, add the 0.15mol/l hydrochloric acid solution of 3 times of amounts in the concentrated solution, fully stir; Cold preservation is filtered, and filtering residue is with hydrochloric acid solution washing 3 times; Merging filtrate and cleaning mixture are with low pole or middle polarity resin absorption.First water flushing resin column/bed to effluent is closely neutral behind the resin absorption; Closely colourless with 0.1mol/l ammonia spirit flushing resin column/bed to effluent again, closely colourless to contain alcohol amount 20% ethanol liquid flushing resin column/bed to effluent again.Discard.Carry out eluting with 70% ethanol again, show colourless, collect eluent, reclaim ethanol, transfer pH value to 10, leave standstill cold preservation, collecting precipitation with the magnesium hydroxide solution of 1.0mol/l to there not being the alcohol flavor to eluent.Naturally dry, get final product Herba Solani Nigri total alkaloids content greater than 50% Herba Solani Nigri extract extract.
3. above-mentioned Herba Solani Nigri extract 1 weight portion and kurarinone 1 weight portion with mix homogeneously, promptly got drug regimen according to the invention.
Above-described alkaline solution is selected from sodium hydroxide, calcium hydroxide, potassium hydroxide, magnesium hydroxide and ammonia spirit; Described acid solution is selected from acetic acid, hydrochloric acid, sulphuric acid and citric acid solution; Described eluting uses organic solvent one or two or three mixed phase that form with arbitrary proportion as methanol, ethanol, n-butyl alcohol, chloroform, benzene.
Embodiment 2The preparation of injection
(1) Herba Solani Nigri total alkaloids content greater than the method for preparing of 50% Herba Solani Nigri extract and kurarinone drug regimen with embodiment 1.
(2) preparation of aqueous injection: take by weighing Herba Solani Nigri total alkaloids content at Herba Solani Nigri extract more than 50% and kurarinone pharmaceutical composition 10g, with the water for injection dissolving, accent pH value to 7 filters, sterilization, and check, packing gets 1000 of aqueous injection.
(3) preparation of infusion solution: take by weighing Herba Solani Nigri total alkaloids content at Herba Solani Nigri extract more than 50% and kurarinone pharmaceutical composition 10g, after an amount of water for injection dissolving, regulate pH value to 6～7 with the hydrochloric acid of 0.1mol/l; Stirred 30 minutes, and added certain active carbon, continue to stir half an hour; Filter, behind the 0.22 μ m filter membrane, add an amount of water for injection excessively; Stir fill, promptly get infusion solution.
(4) preparation of lyophilized injectable powder: take by weighing Herba Solani Nigri total alkaloids content at Herba Solani Nigri extract more than 50% and kurarinone pharmaceutical composition 10g; Add 1000ml water for injection, 80 ℃～90 ℃ insulated and stirred are fully after the dissolving; The mannitol that adds 100g stirs and makes dissolving; Regulate pH value to 6～7, aseptic fine straining quantitatively is sub-packed in the pipe-produced glass bottle, and lyophilization promptly gets.
Embodiment 3The preparation of solid preparation
(1) Herba Solani Nigri total alkaloids content greater than the method for preparing of 50% Herba Solani Nigri extract and kurarinone drug regimen with
Embodiment 1.
(2) preparation of tablet: Herba Solani Nigri total alkaloids content restrains greater than 50% Herba Solani Nigri extract and kurarinone drug regimen 10, pharmaceutic adjuvant starch, magnesium stearate 100 grams.Mix homogeneously is pulverized, and sieves, granulate, and drying, tabletting, check, packing gets 10000 in tablet.
(3) preparation of capsule: take by weighing Herba Solani Nigri total alkaloids content at Herba Solani Nigri extract more than 50% and kurarinone pharmaceutical composition 100g, medical starch 1000g, mix homogeneously, the capsule of packing into No. 2, every drug compositions 100mg.
(4) preparation of powder: take by weighing Herba Solani Nigri total alkaloids content at Herba Solani Nigri extract more than 50% and kurarinone pharmaceutical composition 1000g, starch 1000g, mix homogeneously, packing promptly gets every bag of drug compositions 100mg.
Claims (7)
1. pharmaceutical composition with anticarcinogenesis is characterized in that by Herba Solani Nigri total alkaloids content adding appropriate amount of auxiliary materials and processing greater than 50% Herba Solani Nigri extract 1～4 weight portion and kurarinone 1～3 weight portion;
Get herb of Herba Solani Nigri and fruit, add 50%～90% alcoholic solution and extract each 6～8 times of amounts 2～3 times; Reclaim ethanol, be concentrated into relative density 1.25, add the 0.1mol/l acid solution of 2～4 times of amounts in the concentrated solution; Fully stir, cold preservation is filtered; Filtering residue is with hydrochloric acid solution washing 1～3 time, and merging filtrate and cleaning mixture are with low pole or middle polarity resin absorption; First water flushing resin column/bed to effluent is closely neutral behind the resin absorption; Closely colourless with 0.1mol/l alkaline solution flushing resin column/bed to effluent again, closely colourless to contain alcohol amount 10%～40% ethanol liquid flushing resin column/bed to effluent again, discard, carry out eluting with 50～90% ethanol again; Show colourless to eluent, collect eluent, reclaim ethanol to there not being the alcohol flavor; Alkaline solution with 0.5～1.5mol/l is transferred pH value to 8～10, leaves standstill cold preservation; Collecting precipitation dries naturally, Herba Solani Nigri total flavones content greater than 50% Herba Solani Nigri extract;
With above-mentioned Herba Solani Nigri extract and kurarinone mix homogeneously according to the above ratio, add suitable adjuvant, promptly get said pharmaceutical composition;
Above-described alkaline solution is selected from sodium hydroxide, calcium hydroxide, potassium hydroxide, magnesium hydroxide and ammonia spirit; Described acid solution is selected from acetic acid, hydrochloric acid, sulphuric acid and citric acid solution.
2. pharmaceutical composition according to claim 1 is characterized in that preferred proportion is a Herba Solani Nigri total flavones content greater than 50% Herba Solani Nigri extract 3 weight portions, kurarinone 2 weight portions.
3. pharmaceutical composition according to claim 1 is characterized in that this pharmaceutical composition and one or more pharmaceutical excipients are prepared into antineoplastic oral drug preparation or non-intestinal pharmaceutical preparation.
4. pharmaceutical composition according to claim 3 is characterized in that described oral drug preparation or non-intestinal pharmaceutical preparation contain 1%～99% Herba Solani Nigri total alkaloids content greater than 50% the Herba Solani Nigri extract and the pharmaceutical excipient of kurarinone mixture and 99%～1%.
5. pharmaceutical composition according to claim 4 is characterized in that described oral drug preparation or non-intestinal pharmaceutical preparation contain 45%～95% Herba Solani Nigri total alkaloids content greater than 50% the Herba Solani Nigri extract and the pharmaceutical excipient of kurarinone mixture and 55%～5%.
6. pharmaceutical composition according to claim 5 is characterized in that described oral drug preparation or non-intestinal pharmaceutical preparation contain 75%～90% Herba Solani Nigri total alkaloids content greater than 50% the Herba Solani Nigri extract and the pharmaceutical excipient of kurarinone mixture and 25%～10%.
7. pharmaceutical composition according to claim 3 is characterized in that said oral drug preparation is tablet, capsule, granule, powder, pill, suspensoid, oral liquid; Said non-intestinal pharmaceutical preparation is injection, infusion solution, freeze dried injection, injectable emulsion, aerosol, suppository; Said pharmaceutical excipient is solvent, disintegrating agent, correctives, binding agent, coloring agent, antiseptic.
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| Title |
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| 季宇彬 |
| 季宇彬;高世勇;王宏亮;邹翔.龙葵总碱对肿瘤细胞膜钠泵及钙泵活性影响的研究.《世界科学技术-中医药现代化》.2006,第8卷(第4期), * |
| 王宏亮 |
| 邹翔.龙葵总碱对肿瘤细胞膜钠泵及钙泵活性影响的研究.《世界科学技术-中医药现代化》.2006,第8卷(第4期), |
| 高世勇 |
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