CN107714732A - A kind of medicine containing American cockroach and capecitabine and its application - Google Patents

A kind of medicine containing American cockroach and capecitabine and its application Download PDF

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CN107714732A
CN107714732A CN201611174010.2A CN201611174010A CN107714732A CN 107714732 A CN107714732 A CN 107714732A CN 201611174010 A CN201611174010 A CN 201611174010A CN 107714732 A CN107714732 A CN 107714732A
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american
cockroach
capecitabine
extract
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耿福能
林庆华
沈咏梅
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SICHUAN GOOD DOCTOR PANXI PHARMACEUTICAL CO Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/56Materials from animals other than mammals
    • A61K35/63Arthropods

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Abstract

The invention provides a kind of medicine containing American cockroach and capecitabine and its application, the active component of described medicine includes American cockroach and capecitabine.Wherein, described American cockroach is American-cockroach-extract or American cockroach medicinal powder.Described medicine constituent can be 1000~2500 parts of American-cockroach-extract by weight, 200~300 parts of capecitabine;It can also be 500~800 parts of American cockroach medicinal powder, 200~300 parts of capecitabine.The pharmaceutical composition of the present invention has very strong Apoptosis to tumour, tumour can effectively be treated, positive effect is used alone better than American cockroach and capecitabine, illustrate that the two has a synergistic function after being used cooperatively under present invention proportioning, potential applicability in clinical practice is good.

Description

A kind of medicine containing American cockroach and capecitabine and its application
Technical field
The invention belongs to pharmaceutical formulation field, it is especially useful in a kind of medicine containing American cockroach and capecitabine and its should With.
Background technology
Capecitabine is a kind of new xeloda, can be sticked after oral in the form of prototype through stomach and intestine rapidly Film absorbs, and after liver metabolism, the selective tumour cell for acting on high expression thymidine phosphorylase (TP), plays anti- Tumor promotion, the characteristic of capecitabine three steps activation in vivo make the medicine with targeting, and radiotherapy can be with Increase the expression of class TNF A, so as to increase TP activity, normal tissue joins without influence, therefore with radiotherapy Its targeting can be strengthened by closing application.External clinical research shows that capecitabine is to the tumor in upper digestive tract such as cancer of the esophagus, nasopharynx Cancer, stomach cancer and cancer of pancreas etc. have sensitization.
American cockroach (Periplaneta american) belongs to Insecta, Blattidae, is commonly called as cockroach.American cockroach is as medicine With initially seeing《Sheng Nong's herbal classic》, for controlling bloody sputum disease, fever and chills, broken accumulation, laryngopharynx numbness, interior cold s.m.p.Sent out at present in research Existing American cockroach ethanol extract is white to chronic marrow-derived leukocythemia (K562), promyelocytic leukemia (HL60), mouse in vitro Blood disease (P388D1) cell line, nasopharyngeal carcinoma (CNE), lung cancer (A549), oral epithelium cancer (KB) cell line, oophoroma (HO8910), cervical carcinoma (Hela) and prostate cancer (PC3) cell line, the cancer of the esophagus (Ecal09), sdenocarcinoma of stomach (BGC823), colon Cancer (LS174T) cell line has growth inhibition effect.
Have not yet to see the report of American cockroach and its extract joint capecitabine in the radiosensitivity for improving tumour Road.
The content of the invention
The invention provides a kind of medicine containing American cockroach and capecitabine, described medicine is improving putting for tumour Significant effect in sensitiveness is penetrated, its action effect is substantially better than American cockroach and capecitabine independent medication effect.
The active component of medicine of the present invention includes American cockroach and capecitabine.
Wherein, described American cockroach is American-cockroach-extract or American cockroach medicinal powder.
Further, the active component of described medicine by weight, including:American-cockroach-extract 1000~2500 Part, 200~300 parts of capecitabine;Preferably, 2500 parts of American-cockroach-extract, 300 parts of capecitabine.
American-cockroach-extract preparation method is as follows:
American cockroach, which crushes to be placed in ethanol, to be soaked, and refluxing extraction 2~3 times, is concentrated into no alcohol taste, obtains extract solution, past Water is added in extract solution, after being well mixed, stands, cools down, filtering, be concentrated under reduced pressure, be drying to obtain;
Further, American-cockroach-extract of the present invention can be Kangfuxin Liquid, meet WS3-B-3674-2000 (Z) to the limit standard of " Kangfuxin Liquid " in, 0.72mg must not be less than containing total amino acid per 1ml, such as commercially available Kangfuxin Liquid.
It is also possible that the active component of described medicine is by weight, including:500~800 parts of American cockroach medicinal powder, 200~300 parts of capecitabine;Preferably, 800 parts of American cockroach medicinal powder, 300 parts of capecitabine.
American cockroach medicinal powder preparation method is:
A. adult bombay canary is placed in vacuum desiccator, it is 2~5% to be dried at 20~55 DEG C to water content, is obtained Dry adult bombay canary;
B. it is -200 DEG C~-50 DEG C ultralow the adult bombay canary of the drying obtained in step a to be placed in into temperature setting 60~300 mesh are crushed in warm pulverizer, produce American cockroach medicinal powder.
Although selected in the specific embodiment of the invention through intestines and stomach absorbable preparation to embody the treatment of pharmaceutical composition effect Fruit, however, this form of medication that can not be used to limit pharmaceutical composition of the present invention.With reference to modern separating and purifying technology or/and Preparation means, those skilled in the art can also be prepared into transdermal absorption formulation, outer by American cockroach or its extract after purification With other form of medication such as lotion, et al. Ke preparation, injections, so as to strengthen target-oriented drug, improve drug effect or avoid not Necessary toxicity.
Present invention also offers a kind of compound formulation to cancer with Apoptosis, and it is extracted by American cockroach Thing or American cockroach medicinal powder and capecitabine are as active component, plus pharmaceutically acceptable auxiliary material or auxiliary element preparation Into preparation.
Described cancer includes:The cancer of the esophagus, nasopharyngeal carcinoma, breast cancer, oophoroma, stomach cancer, colorectal cancer.
Pharmaceutically acceptable auxiliary material of the present invention, refer to the material being included in addition to the active ingredient (s in formulation, bag Include but be not limited only to filler (diluent), lubricant (glidant or antitack agent), dispersant, wetting agent, adhesive, regulation Agent, solubilizer, antioxidant, bacteriostatic agent, emulsifying agent, disintegrant etc..Adhesive include syrup, Arabic gum, gelatin, sorbierite, Tragacanth, cellulose and its derivates (such as microcrystalline cellulose, sodium carboxymethylcellulose, ethyl cellulose or hydroxypropyl methylcellulose Element etc.), gelatine size, syrup, starch slurry or polyvinylpyrrolidone etc.;Filler include lactose, Icing Sugar, dextrin, starch and its Derivative, cellulose and its derivates, inorganic calcium salt (such as calcium sulfate, calcium phosphate, calcium monohydrogen phosphate, precipitated calcium carbonate), sorb Alcohol or glycine etc.;Lubricant includes superfine silica gel powder, magnesium stearate, talcum powder, aluminium hydroxide, boric acid, hydrogenated vegetable oil, poly- second Glycol etc.;Disintegrant includes starch and its derivative (such as sodium carboxymethyl starch, Explotab, pregelatinized starch, improvement shallow lake Powder, hydroxypropul starch, cornstarch etc.), polyvinylpyrrolidone or microcrystalline cellulose etc.;Wetting agent includes dodecyl sulphate Sodium, water or alcohol etc.;Antioxidant packages are containing sodium sulfite, sodium hydrogensulfite, sodium pyrosulfite, dibutyl benzoic acid etc.;Bacteriostatic agent includes 0.5% phenol, 0.3% cresols, 0.5% anesin etc.;Conditioning agent includes hydrochloric acid, citric acid, potassium hydroxide (sodium), citron Sour sodium and buffer (including sodium dihydrogen phosphate and disodium hydrogen phosphate) etc.;Emulsifying agent includes Tween-80, aliphatic acid sorb Smooth, pluronic gram F-68, lecithin, Fabaceous Lecithin etc.;Solubilizer includes Tween-80, bile, glycerine etc..
The pharmaceutically acceptable complementary composition, it has certain physiologically active, but the addition of the composition will not change Become the leading position of above-mentioned health products or pharmaceutical composition in treatment of diseases, and only play auxiliary effect, these are auxiliary Assist effect is only the utilization to the composition known activity, is the usual adjuvant treatment modality of field of medicaments.
In above-mentioned compound formulation, the weight proportion of American-cockroach-extract and capecitabine is (1000~2500):(200 ~300);Preferably, the weight proportion of American-cockroach-extract and capecitabine is 2500:300.
Above-mentioned preparation can also be that the weight proportion of American cockroach medicinal powder and capecitabine is (500~800):(200~ 300);Preferably, the weight proportion of American cockroach medicinal powder and capecitabine is 800:300.
Further, in the preparation, the content of the every big Lian extracts in daily unit formulation Central America and capecitabine is total Count 18.7g;The content of the every big Lian medicinal powder in daily unit formulation Central America and capecitabine amounts to 7.3g." every daily unit Dosage " refers to the preparation total amount taken daily.
Embodiment
The preparation of the American-cockroach-extract of embodiment 1
American-cockroach-extract:500g American cockroaches, which crush to be placed in 90% ethanol, soaks 12h, refluxing extraction 2 at 85 DEG C ~3 times, no alcohol taste is concentrated into, obtains extract solution, 1500g water is added into extract solution, after being well mixed, is stood, cooling, mistake Filter, it is concentrated under reduced pressure, dries, crushing and produce.
The preparation of the American cockroach medicinal powder of embodiment 2
American cockroach medicinal powder:Adult bombay canary is placed in vacuum desiccator, dried at 20~55 DEG C to water content For 2%, dry adult bombay canary is obtained, it is -100 DEG C super that the adult bombay canary of obtained drying is placed in into temperature setting 60~300 mesh are crushed in Lowtemperaturepulverizer, produce American cockroach medicinal powder.
Embodiment 3
The medicine is American-cockroach-extract 2500mg and capecitabine 300mg combination medicines in embodiment 1.
Embodiment 4
The medicine is American-cockroach-extract 1000mg and capecitabine 200mg combination medicines in embodiment 1.
Embodiment 5
The medicine is American-cockroach-extract 2500mg and capecitabine 200mg combination medicines in embodiment 1.
Embodiment 6
The medicine is American-cockroach-extract 1000mg and capecitabine 300mg combination medicines in embodiment 1.
Embodiment 7
The medicine is American cockroach medicinal powder 800mg and capecitabine 300mg combination medicines in embodiment 2.
Embodiment 8
The medicine is American cockroach medicinal powder 500mg and capecitabine 200mg combination medicines in embodiment 2.
Embodiment 9
The medicine is American cockroach medicinal powder 800mg and capecitabine 200mg combination medicines in embodiment 2.
Embodiment 10
The medicine is American cockroach medicinal powder 500mg and capecitabine 300mg combination medicines in embodiment 2.
The combination medicine of American cockroach and capecitabine described in any one of 3~embodiment of above example 10 can be with Plus pharmaceutically conventional auxiliary material or complementary composition, capsule, tablet, sustained release is made according to technological means commonly used in the art The oral formulations such as preparation, liquid preparation.
Beneficial effects of the present invention are proved below by way of specific pharmacodynamic experiment.Wherein, used in test example 1 and test example 2 American-cockroach-extract+capecitabine composition be the medicine described in embodiment 3;U.S. used in test example 1 and test example 2 The big Lian medicinal powder+capecitabine composition in continent is the medicine described in embodiment 7.
Test example 1
First, research of the medicine of the present invention to esophageal carcinoma cell line EC9706 radiosensitizing effects
1. experiment material
1.1 experimental cell
Human esophagus cancer cell strain EC9706 (is provided) by Chengdu University of Traditional Chinese Medicine's Basic Experimental Teaching Center.With containing 10% tire ox blood Clear RPMI 1640 culture mediums are placed in 37 DEG C, 5%CO2Constant temperature training case in cultivate, with 0.25%EDTA pancreatin had digestive transfer cultures, Exponential phase of growth cell is taken to be tested.
1.2 experimental drugs and configuration
Capecitabine (Xeloda) (Shanghai Co., Ltd of Roche Group):Specification:500mg/ pieces.
1.3 experiment packet
It is divided into 6 groups:Control group, American cockroach medicinal powder group, American-cockroach-extract group, capecitabine group, American cockroach Extract+capecitabine group, American cockroach medicinal powder+capecitabine group.
1.4 radiosensitizations are tested
1.4.1 illuminating method
Irradiated using 6MeV x-rays linear accelerator, irradiation distance 100cm, irradiation field is 10cm × 10cm, at room temperature Single fraction irradiation.Exposure dose 2Gy, ensure that each group cell is illuminated.
1.4.2 the measure of cell inhibitory rate
Take the logarithm growth period EC9706 cell, by 1 × 104/ ml, 100 μ l/ holes are inoculated with 96 orifice plates, are divided into 6 described in 1.3 Individual group, every group sets 6 multiple holes.After cell is completely adherent, each group adds corresponding pastille culture medium, and control group is culture completely Base, it is placed in 37 DEG C, 5%CO2After incubator is incubated culture 24h, wavelength 450nm optical density is determined on ELIASA using MTS It is worth (OD values), calculates inhibition rate of tumor cell (%), calculation formula is as follows.
Inhibiting rate (%)=(1- administration groups OD values/control group OD values) × 100%
1.4.3 colony-forming test determines Radiosensitizing
EC9706 after the illuminating method irradiation as described in 1.4.1 is placed into 4h in incubator, obtains sublethal damage To repair, homogeneous cell suspension then is mixed into through the digestion of 0.25% tryptic digestive juice, 6 orifice plates are inoculated in per hole 2ml In, ensure per hole cell number to be 1000 or so.It is divided into 6 groups described in 1.3,3 multiple holes of every group of setting, each group adds corresponding Pastille culture medium, control group are complete medium.Continue to cultivate 14d, daily Microscopic observation, when each thin in constant incubator When growing up to the colony more than 50 cells around born of the same parents, add methanol and fix, the dyeing of Ji's nurse Sa, count under mirror each Drug level group Colony number.Colony-forming efficiency represents that cell survival fraction is represented with SF with PE.Model is clicked using more targets of SPSS statistical softwares Analyzed, draw each group parameter (N, D0、Dq、SF2、SERDq)。
Colony-forming efficiency (PE)=colony number/inoculating cell number × 100%
Cells survival fraction (SF)=each exposure dose PE/ does not irradiate PE × 100%
Enhance-ment ratio (SERDq)=the Dq values irradiated merely/compare the Dq values of dosing
1.4.4 flow cytometry
Take the logarithm growth period EC9706 cell, by 1 × 104/ ml, 100 μ l/ holes are inoculated with 96 orifice plates, are divided into 6 described in 1.3 Individual group, every group sets 6 multiple holes, separately sets one group of blank control as negative control group.Each group adds corresponding pastille culture medium, blank Group and control group are complete medium, are placed in 37 DEG C, 5%CO2 incubators incubation culture 24h.After abandoning medicine, in addition to blank group, often Group cell illuminating method as described in 1.4.1 is irradiated, and 24h is then incubated in culture, and then pancreatin digests, 1000r/min centrifugations 5min, supernatant is abandoned, D-hanks is cleaned 2 times, and overnight, centrifugation discards ethanol, and D-hanks is washed 2 times again for 80% 4 DEG C of ethanol fixation, uses Rnase (whole mass concentration 0.02mg/ml), PI (whole mass concentration is 0.1mg/ml) lucifuge dyeing 30min, flow cytometer point Analyse cell cycle distribution situation.
1.5 statistical method
Analyzed using SPSS17.0 statistical softwares, data information represents that multigroup is compared from single factor test variance with x ± s Analyze, compare two-by-two using independent samples t test in group, with P<0.05 is that difference is statistically significant, P<0.01 is that difference has There is significant statistical significance.
2 results
The measure of 2.1 cell inhibitory rates
The American cockroach medicinal powder of table 1, American-cockroach-extract and the two combine card respectively and accompany his shore to EC9706 Carbazole alkaloids Rate influence (n=6,)
Group Dosage (μ g/ml) OD values Inhibiting rate (%)
Control group - 4.37±0.43△ -
Capecitabine group 6 1.89±0.13* 56.75
American-cockroach-extract group 50 3.26±0.10*△ 25.40
American cockroach medicinal powder group 16 2.99±0.09*△ 31.58
American-cockroach-extract+capecitabine group 50+6 1.46±0.07*△ 66.59
American cockroach medicinal powder+capecitabine group 16+6 1.31±0.07*△ 70.02
Note:Compared with control group, * P < 0.05;Compared with capecitabine group, △ P < 0.05.
After capecitabine it can be seen from the result of table 1 and American-cockroach-extract drug combination, to human esophagus cancer cell strain The inhibitory action of EC9706 cell propagation has statistics apparently higher than capecitabine and American-cockroach-extract is used alone Meaning;Capecitabine and the suppression after American cockroach medicinal powder drug combination, bred to human esophagus cancer cell strain EC9706 cell Effect has statistical significance apparently higher than capecitabine and American-cockroach-extract is used alone;
2.2 pairs of EC9706 radiotherapy sensitizations
Compared with capecitabine group, American-cockroach-extract+capecitabine group and American cockroach medicinal powder+capecitabine group pair EC9706 radiotherapy effect of enhanced sensitivity is notable.
The American cockroach medicinal powder of table 2, American-cockroach-extract and the two combine card respectively and accompany his shore to EC9706 radiotherapies Enhanced sensitivity ratio (SER)
Note:Compared with capecitabine group, △ P < 0.05.
After capecitabine it can be seen from the result of table 2 and American-cockroach-extract drug combination, to human esophagus cancer cell strain EC9706 radiosensitizing effect has statistical significance apparently higher than capecitabine is used alone;Capecitabine is big with America After Lian medicinal powder drug combinations, to human esophagus cancer cell strain EC9706 radiosensitizing effect apparently higher than Ka Peita is used alone Shore, there is statistical significance.
The influence of 2.3 cell cycles
The American cockroach medicinal powder of table 3, American-cockroach-extract and the two combine the influence that card accompanies his shore cell cycle respectively (n=6,)
Note:Compared with control group, * P < 0.05;Compared with capecitabine group, △ P < 0.05.
As can be seen from Table 3:Capecitabine group G0/G1 phase cell proportions are significantly raised, illustrate that it suppresses tumour cell The mechanism of action of propagation is probably to block the G0/G1 phases;The S phase ratios of American-cockroach-extract group increase, and illustrate that it suppresses tumour The mechanism of action of propagation is probably to block the S phases.And capecitabine and American-cockroach-extract drug combination group act on EC9706 After cell line 24h, G0/G1 phase cell quantities increase, and ratio substantially increases, but S phases and G2/M phases ratio decline, and illustrate both connection Cell cycle has retardation after sharing medicine, make tumour cell it is more rest on the G0/G1 phases, both hinder after being used in combination The stagnant more alone medicine group of effect is high, generates the effect of Synergistic;Similarly analysis can obtain, and American cockroach medicinal powder joins with capecitabine With the rear inhibitory action to tumor cell proliferation apparently higher than independent medication group, both have the function that Synergistic at combination.
Test example 2
2nd, research of the medication combined radiotherapy of the present invention to tumor-bearing mice
1. experiment material
1.1 experimental animal
BALB/C-nu/nu nude mices, SPF levels, 4~5 week old, 15~17g of body weight, nude mice are raised under Clean Facility, permanent Warm (24~26 DEG C), cage tool, bedding and padding, drinking water and feed are sterile-processed, and experimenter strictly carries out sterile working.
1.2 experimental cell
Human esophagus cancer cell strain EC9706 (is provided) by Chengdu University of Traditional Chinese Medicine's Basic Experimental Teaching Center.
1.3 experimental drugs and configuration
Capecitabine (Xeloda) (Shanghai Co., Ltd of Roche Group):Specification:500mg/ pieces.
Illuminating method:Using Beijing company of Daheng KB1800 type medical computerized linear accelerators, 6MV-X lines are irradiated, SSD is 100cm, dosage 2Gy/min.
1.4 experimental method
1.4.1 Nude Mouse Model is established
Human esophagus cancer EC9706 cell lines are subjected in vitro culture to exponential phase, with 0.25% trypsase and 0.04%EDTA vitellophags, blow and beat repeatedly to be collected into after single cell suspension in centrifuge tube.1000rpm/min centrifuges 5min, Abandoning supernatant, PBS are resuspended after washing 2 times with PBS, and light Microscopic observation number of alive cell > after blue dyeing is expected at 0.4% 95%, count, be configured to 1 × 107Concentration, aseptically fix nude mice.After armpit skin routine disinfection on the right side of nude mice Hold 1ml asepsis injectors forelimb armpit on the right side of nude mice and 0.2ml cell suspensions are subcutaneously injected, form locality tumor model.Note The local obvious skin mound of appearance is penetrated, occurs the big lesser tubercle of grain grain after 5 days, Transplanted tumor model is established, tumor formation rate 100%.
1.4.2 packet and administration
BALB/C-nu/nu SPF levels nude mice 48 use in experiment, inoculation human esophagus cancer EC9706 cell suspensions, visible after 11d The subcutaneous tumour for having about 0.5cm × 0.5cm sizes is generated, and 48 nude mices are randomly divided into 6 groups, every group 8:(1) control group is not Carry out perfusion;(2) capecitabine group, by 300mg/kg gavage capecitabines;(3) American cockroach medicinal powder group, is filled by 800mg/kg Stomach American cockroach medicinal powder;(4) American-cockroach-extract group, by 2500mg/kg gavage American-cockroach-extracts;(5) American cockroach Extract+capecitabine group, by 2500mg/kg+300mg/kg gavages American-cockroach-extract and capecitabine;(6) America is big Lian medicinal powder+capecitabine group, by 800mg/kg+300mg/kg gavage American cockroach medicinal powder and capecitabine.In addition to control group, often The daily gavage of group mouse 1 time, continuous 28 days, meanwhile, every group of mouse x-ray bombardment tumor by local 4Gy/ times × 4 times, the next day enter Row 1 time.
After last therapeutic 72h, nude mice tumorous size is measured, nude mice is put to death with spinal cord dislocation method, nude mice dorsal position is fixed, To right upper extremity skin routine disinfection, knurl body at armpit is peeled off, scales/electronic balance weighing knurl body tumour is used after being blotted with filter paper, is calculated swollen Knurl tumour inhibiting rate.
Tumour inhibiting rate (%)=(the average knurl weight of the average knurl weight-treatment group of control group) average knurl weight × 100% of/control group
1.5 statistical method
Analyzed using SPSS17.0 statistical softwares, data information represents that multigroup is compared from single factor test variance with x ± s Analyze, compare two-by-two using independent samples t test in group, with P<0.05 is that difference is statistically significant, P<0.01 is that difference has There is significant statistical significance.
2. experimental result
As can be seen from Table 4:Compared with control group, each experimental group can reduce tumour inhibiting rate, and tumour inhibiting rate is 37.1%~ 72.17%, wherein American-cockroach-extract+capecitabine group and American cockroach medicinal powder+capecitabine group tumor killing effect is notable.Card The tumour inhibiting rate after his shore and American-cockroach-extract combined radiotherapy is trained apparently higher than American cockroach and capecitabine independent medication simultaneously Tumour inhibiting rate after combined radiotherapy;Tumour inhibiting rate after capecitabine and American cockroach medicinal powder combined radiotherapy apparently higher than American cockroach and Tumour inhibiting rate after capecitabine independent medication and combined radiotherapy.By can be seen that capecitabine and the present invention in the data in upper table Treating cancer is used in combination in described American cockroach, substantially increases the therapeutic action to tumour.
The American cockroach medicinal powder of table 4, American-cockroach-extract and the two combine card respectively and accompany his influence (n of the shore to tumour inhibiting rate =8,)
Group Dosage (μ g/ml) Knurl weight (g) Tumour inhibiting rate (%)
Control group - 4.42±0.13△ -
Capecitabine group 300mg/kg 1.89±0.09* 57.24
American-cockroach-extract group 2500mg/kg 2.78±0.10*△ 37.10
American cockroach medicinal powder group 800mg/kg 2.65±0.13*△ 40.05
American-cockroach-extract+capecitabine group 2500mg/kg+300mg/kg 1.39±0.11*△ 68.55
American cockroach medicinal powder+capecitabine group 800mg/kg+300mg/kg 1.23±0.10*△ 72.17
Note:Compared with control group, * P < 0.05;Compared with capecitabine group, △ P < 0.05.
To sum up, the medicine of the present invention containing capecitabine and American-cockroach-extract, radiated for cancer cell Property sensitization, tumour inhibiting rate it is stronger than the effect that capecitabine and American cockroach are used alone, illustrate American cockroach and Ka Peita There is obvious synergistic function after the combination of shore.Its drug combination ratio is:The weight of American-cockroach-extract and capecitabine Amount proportioning is (1000~2500):(200~300);The weight proportion of American cockroach medicinal powder and capecitabine is (500~800): (200~300) have good effect.Preferably, American-cockroach-extract 2500mg, capecitabine 300mg, if conversion adult With dosage (assuming that the body weight of people is 60kg), every daily dosage of optimum proportioning of the present invention should be 18.7g;Another optimal proportion For American cockroach medicinal powder 800mg, capecitabine 60mg, if converting adult's dosage, every daily dosage of optimum proportioning of the present invention Should be 7.3g.

Claims (10)

1. a kind of medicine containing American cockroach and capecitabine, it is characterised in that the active component of described medicine includes U.S. The big Lian in continent and capecitabine;Wherein, described American cockroach is American-cockroach-extract or American cockroach medicinal powder.
2. medicine according to claim 1, it is characterised in that the active component of described medicine by weight, including: 1000~2500 parts of American-cockroach-extract, 200~300 parts of capecitabine;Preferably, 2500 parts of American-cockroach-extract, card Train his 300 parts of shore.
3. medicine according to claim 2, it is characterised in that the preparation method of described American-cockroach-extract is:It is beautiful The big Lian in continent, which crushes to be placed in ethanol, to be soaked, and refluxing extraction 2~3 times, is concentrated into no alcohol taste, is obtained extract solution, adds into extract solution Enter water, after being well mixed, stand, cool down, filtering, be concentrated under reduced pressure, be drying to obtain.
4. medicine according to claims 1 to 2, it is characterised in that the American-cockroach-extract is Kangfuxin Liquid.
5. medicine according to claim 1, it is characterised in that the active component of described medicine by weight, including: 500~800 parts of American cockroach medicinal powder, 200~300 parts of capecitabine;Preferably, 800 parts of American cockroach medicinal powder, capecitabine 300 parts.
6. medicine according to claim 5, it is characterised in that the preparation method of described American cockroach medicinal powder is:
A. adult bombay canary is placed in vacuum desiccator, it is 2~5% to be dried at 20~55 DEG C to water content, obtains drying Adult bombay canary;
B. the adult bombay canary of the drying obtained in step a is placed in the ultralow temperature powder that temperature setting is -200 DEG C~-50 DEG C 60~300 mesh are crushed in broken machine, produce American cockroach medicinal powder.
7. a kind of compound formulation to cancer with Apoptosis, it is characterised in that it is by American cockroach and Ka Peita Shore is as active component, the preparation being prepared plus pharmaceutically acceptable auxiliary material or auxiliary element, wherein, described America Big Lian is American-cockroach-extract or American cockroach medicinal powder.
8. compound formulation according to claim 7, it is characterised in that described American-cockroach-extract and capecitabine Weight proportion is (1000~2500):(200~300);Preferably, the weight proportion of American-cockroach-extract and capecitabine is 2500:300.
9. compound formulation according to claim 7, it is characterised in that described American cockroach medicinal powder and the weight of capecitabine Amount proportioning is (500~800):(200~300);Preferably, the weight proportion of American cockroach medicinal powder and capecitabine is 800: 300。
10. compound formulation according to claim 7, it is characterised in that:Described cancer includes the cancer of the esophagus, nasopharyngeal carcinoma, stomach Cancer.
CN201611174010.2A 2016-12-16 2016-12-16 A kind of medicine containing American cockroach and capecitabine and its application Pending CN107714732A (en)

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Application publication date: 20180223