CN105147695A - Anti-breast cancer powder containing metformin hydrochloride and gdc 0941 - Google Patents
Anti-breast cancer powder containing metformin hydrochloride and gdc 0941 Download PDFInfo
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- CN105147695A CN105147695A CN201510394747.4A CN201510394747A CN105147695A CN 105147695 A CN105147695 A CN 105147695A CN 201510394747 A CN201510394747 A CN 201510394747A CN 105147695 A CN105147695 A CN 105147695A
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- metformin hydrochloride
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Abstract
The invention discloses anti-breast cancer powder containing metformin hydrochloride and gdc0941. Active components of the anti-breast cancer powder are the metformin hydrochloride and gdc 0941. The anti-breast cancer powder further comprises pharmaceutically acceptable auxiliary materials. The anti-breast cancer powder is simple to prepare, easy to operate, lower in cost and economical and practical; the anti-breast cancer powder disperses easily and takes effect fast, and dosage of the powder is easily controllable; in-vitro antitumor tests show that the combination of the metformin hydrochloride and gdc 0941 provides higher anti-cancer activity and the powder is worthy of clinical popularization.
Description
Technical field
The invention belongs to medical art, be specifically related to a kind of solid orally ingestible being active component with metformin hydrochloride and gdc0941.
Background technology
The discovery of the novelty teabag of known drug is an important directions of new drug development; as the metformin (Metformin) of type 2 diabetes mellitus patient initial therapy choice drug; there is low price, cross patent protection period, safety and the advantage be widely used.And its potentiality on oncotherapy, also become a focus recently.A lot of observational study report discloses, and accept the diabetics of Or Metformin In Treating, Tumor incidence and mortality rate all have reduction.In the report of Evans, the diabetics accepting Or Metformin In Treating compares the patient not accepting Or Metformin In Treating, and the former amounts to 8170 objects of observation than the latter's cancered risk reduction 4.3%(two groups).ZODIAC(hereby Waller Diabetes Clinic patient integrate existing nursing care plan) in research, author reports that the standard cancer case fatality rate of all patients is 1.47 and the danger ratio of metformin group drops to 0.43.And show that the consumption often increasing by 1 gram of metformin just can reduce the conclusion of the danger ratio of the cancer case fatality rate of 42%.Meanwhile, a large amount of preclinical models also demonstrate that metformin has obvious growth inhibited effect to multiple cancerous cell and mouse tumor model.Nearest research confirms, metformin also has effect to breast carcinoma stem cell, and overcomes the drug resistance to Trastuzumab because breast carcinoma stem cell causes.
Breast carcinoma is the common cancer that women ranks the first.The recent statistics data display of U.S. CA:ACancerJournalforClinicians magazine announcement in 2012, the U.S. estimates there will be 226870 routine women's suffers from breast in 2012, account for 29% of women's de novo malignancy, rank female malignant sickness rate first.In China Beijing, Shanghai, Tianjin etc., metropolitan statistics display breast carcinoma is the modal malignant tumor of China women equally, and sickness rate is in ascendant trend year by year.Therefore study the effect of metformin anti-breast cancer and there is certain realistic meaning.But find in process metformin being developed as a kind of cancer therapy drug, metformin, under physiological dose, is difficult to as a kind of independent cancer therapy drug.Therefore being necessary that selection is a kind of can have synergistic medicine to carry out administering drug combinations to reduce the dosage of metformin with metformin.
The anticancer mechanism of the metformin disclosed mainly can be divided into direct effect (non-insulin dependence) and indirect action (insulin dependency) two kinds.In indirect action, metformin suppresses transcribing of the crucial glyconeogenesis gene of liver by AMPK mediation, and stimulated muscle to the picked-up of glucose, thus reduces fasting glucose and insulin.Because insulin has mitogenesis effect, the normal high level expression Insulin receptor INSR of tumor cell, therefore the effect of metformin reduction insulin level plays pivotal role in its active anticancer.In direct effect, metformin reduces mTOR signal level by activating AMPK thus inhibits the synthesis of cell protein.MTOR is main " the synthesis person " of somatomedin and nutrient signal, is the critical mediator of PI3K/Akt/mTOR signal path, and this signal path is one of the most common molecular network out of control of human tumor.The AMPK activation of metformin mediation result in the suppression of mTOR signal path, the crucial effector molecule phosphorylation in its downstream reduces, eukaryotic initiation factor 4E associated proteins (4E-BPs), Ribosomal protein (S6Ks) and the suppression to total protein synthesis and a large amount of different carcinoma cell line proliferation.
PI3K/Akt/mTOR signal path is the drug development target spot of very attractive, there is this path targeted drug a series of just under development, comprise PI3K/mTOR double inhibitors, the mono-inhibitor of PI3K, the mono-inhibitor of mTOR and Akt inhibitor etc., and existing medicine to enter the I/II phase clinical.The medicine GDC0941 that this project intends adopting is the PI3K inhibitor having very much application prospect developed by U.S.'s technique for gene engineering (Genetech) company.One of main anticancer mechanism of metformin is exactly suppress mTOR by activating AMPK, and communicate with the effect of PI3K/Akt/mTOR signal pathway inhibitor part, is therefore necessary to combine the effect whether having collaborative increase anticancer both checking.
Summary of the invention
Technical problem to be solved by this invention is for above-mentioned deficiency of the prior art, a kind of the anti-breast cancer powder and the preparation method that contain metformin hydrochloride and gdc0941 are provided, it is simple that this oral formulations has composition, the feature of convenient drug administration, persistent, stable curative effect.
Realizing main technical schemes of the present invention is:
Contain an anti-breast cancer powder of metformin hydrochloride and gdc0941, its active component is metformin hydrochloride and gdc0941.
Described a kind of anti-breast cancer powder containing metformin hydrochloride and gdc0941, preferred scheme is, described metformin hydrochloride and gdc0941 weight ratio are that 1:0.5-3(is preferred, and metformin hydrochloride and gdc0941 weight ratio are 1:1).
Described a kind of anti-breast cancer powder containing metformin hydrochloride and gdc0941, preferred scheme is, also comprises pharmaceutically acceptable adjuvant.
Described a kind of anti-breast cancer powder containing metformin hydrochloride and gdc0941, described adjuvant is diluent (preferred lactose, Icing Sugar, dextrin etc., usage ratio is metformin hydrochloride: diluent=1:2-6).
Described a kind of anti-breast cancer powder containing metformin hydrochloride and gdc0941, the weight ratio of metformin hydrochloride and diluent is 1:4.
Present invention also offers a kind of preparation method containing the anti-breast cancer powder of metformin hydrochloride and gdc0941, step is as follows:
(1) metformin hydrochloride, gdc0941, diluent were pulverized respectively 100-150 mesh sieve (preferred, to pulverize 120 mesh sieves);
(2) diluent of pulverizing is put into mortar to grind, pour out after mortar is saturated, in mortar, add metformin hydrochloride and the gdc0941 of pulverizing, grind well, then the mode of equal increments adds diluent, grinds well, subpackage.
Compared with prior art, the solid orally ingestible antitumor activity preventing and treating breast carcinoma provided by the invention is remarkable, and toxic and side effects is little, has enriched prior art, for adding a kind of potential anti-breast cancer new drug clinically, there is social meaning and the economic implications of highly significant.Specifically, be embodied in:
1, the present invention is prepared simply, and operate easy, cost is lower, economical and practical;
2, the present invention verifies through antitumor activity in vitro, and the active anticancer of metformin hydrochloride and gdc0941 has summation action, and both couplings have higher active anticancer, and clinic is promoted;
3, the made powder of the present invention easily disperses, and instant effect, dosage is easy to control.
Detailed description of the invention
Now further describe implementation process of the present invention and effect test by following examples, embodiment is only for the object of illustration, do not limit the scope of the invention, the simultaneously apparent change made according to the present invention of those of ordinary skill in the art and modification are also contained within the scope of the invention.
embodiment 1contain an anti-breast cancer powder of metformin hydrochloride and gdc0941, be prepared from primarily of following bulk drugs: metformin hydrochloride 20g, gdc094120g, Icing Sugar 80g.
A kind of preparation method containing the anti-breast cancer powder of metformin hydrochloride and gdc0941 is:
(1) metformin hydrochloride, gdc0941, Icing Sugar were pulverized 100 mesh sieves respectively;
(2) Icing Sugar of pulverizing is put into mortar to grind, pour out after mortar is saturated, add metformin hydrochloride and the gdc0941 of pulverizing in mortar, grind well, then the mode of equal increments adds sucrose, grinds well, subpackage.
embodiment 2contain an anti-breast cancer powder of metformin hydrochloride and gdc0941, be prepared from primarily of following bulk drugs: metformin hydrochloride 20g, gdc094120g, dextrin 80g.
A kind of preparation method containing the anti-breast cancer powder of metformin hydrochloride and gdc0941 is:
(1) metformin hydrochloride, gdc0941, dextrin were pulverized 150 mesh sieves respectively;
(2) dextrin of pulverizing is put into mortar to grind, pour out after mortar is saturated, add metformin hydrochloride and the gdc0941 of pulverizing in mortar, grind well, then the mode of equal increments adds glucose, grinds well, subpackage.
embodiment 3contain an anti-breast cancer powder of metformin hydrochloride and gdc0941, be prepared from primarily of following bulk drugs: metformin hydrochloride 20g, gdc094120g, lactose 40g.
A kind of preparation method containing the anti-breast cancer powder of metformin hydrochloride and gdc0941 is:
(1) metformin hydrochloride, gdc0941, lactose were pulverized 120 mesh sieves respectively;
(2) lactose of pulverizing is put into mortar to grind, pour out after mortar is saturated, add metformin hydrochloride and the gdc0941 of pulverizing in mortar, grind well, then the mode of equal increments adds lactose, grinds well, subpackage.
embodiment 4contain an anti-breast cancer powder of metformin hydrochloride and gdc0941, be prepared from primarily of following bulk drugs: metformin hydrochloride 20g, gdc094120g, lactose 80g.
A kind of preparation method containing the anti-breast cancer powder of metformin hydrochloride and gdc0941 is:
(1) metformin hydrochloride, gdc0941, lactose were pulverized 120 mesh sieves respectively;
(2) lactose of pulverizing is put into mortar to grind, pour out after mortar is saturated, add metformin hydrochloride and the gdc0941 of pulverizing in mortar, grind well, then the mode of equal increments adds lactose, grinds well, subpackage.
experimental example:the mensuration of different pharmaceutical anti tumor activity in vitro
Material: cell strain: MCF-7 cell strainHJ2mm (Shanghai Inst. of Cytobiology, Chinese Academy of Sciences provides), cultivate in the RPMI-1640 culture medium of 10% hyclone, be placed in 37 DEG C, cultivate in the incubator of carbonated 5%, within every 2 days, change liquid once, after cultivating, select exponential phase cell to test.
Test method: adopt MTT analytic process to analyze MCF-7 cell strainHJ2mm, target cell is all with 7 × 10
4the concentration of individual/mL is inoculated on 96 well culture plates, 100 μ l/ holes, overnight incubation, add medicine, metformin hydrochloride and gdc0941 establish 6 Concentraton gradient, are respectively 12.5,25,50,75,100,125 μm of ol/L, uniting array concentration combination of interactions is (12.5+12.5), (25+25), (50+50), (75+75), (100+100), (125+125) μm ol/L, often kind of drug level has 3 multiple holes, test repetition 3 times, and establishes not drug containing matched group.After cultivating 24h and 48h, process, and measure the light absorption value of each group for the treatment of fluid under microplate reader 490nm wavelength.Calculate drug level (IC needed for 50% cell growth inhibition
50) value.Result sees table 1.
IC after table 1 different pharmaceutical process 24h and 48h
50value
As shown in Table 1, the made powder of the present invention significantly can suppress the growth of MCF-7 Breast Cancer Cell, good to the more single medicine metformin hydrochloride of the inhibit activities of human breast carcinoma and gdc0941, has significant difference (P < 0.05).Illustrate metformin hydrochloride and gdc0941 composite after, tumor killing effect achieves synergistic function.
It should be pointed out that detailed description of the invention is the more representational example of the present invention, obvious technical scheme of the present invention is not limited to above-described embodiment, can also have a lot of distortion.Those of ordinary skill in the art, with the present invention clear and definite disclosed or according to undoubted the obtaining of the written description of file, the claimed scope of this patent all should be thought.
Claims (6)
1. contain an anti-breast cancer powder of metformin hydrochloride and gdc0941, it is characterized in that, active component is metformin hydrochloride and gdc0941.
2. a kind of anti-breast cancer powder containing metformin hydrochloride and gdc0941 according to claim 1, it is characterized in that, described metformin hydrochloride and gdc0941 weight ratio are that 1:0.5-3(is preferred, and metformin hydrochloride and gdc0941 weight ratio are 1:1).
3. a kind of anti-breast cancer powder containing metformin hydrochloride and gdc0941 according to claim 1 and 2, is characterized in that, also comprise pharmaceutically acceptable adjuvant.
4. a kind of anti-breast cancer powder containing metformin hydrochloride and gdc0941 according to claim 3, it is characterized in that, described adjuvant is diluent (preferred lactose, Icing Sugar, dextrin etc., usage ratio is metformin hydrochloride: diluent=1:2-6).
5. a kind of anti-breast cancer powder containing metformin hydrochloride and gdc0941 according to claim 4, it is characterized in that, the weight ratio of metformin hydrochloride and diluent is 1:4.
6. a kind of preparation method containing the anti-breast cancer powder of metformin hydrochloride and gdc0941 according to claim 1 and 2, it is characterized in that, step is as follows:
(1) metformin hydrochloride, gdc0941, diluent were pulverized respectively 100-150 mesh sieve (preferred, to pulverize 120 mesh sieves);
(2) diluent of pulverizing is put into mortar to grind, pour out after mortar is saturated, add metformin hydrochloride and the gdc0941 of pulverizing in mortar, grind well, then the mode of equal increments adds diluent, grinds well, subpackage.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108553446A (en) * | 2018-05-16 | 2018-09-21 | 上海交通大学 | A kind of double nanoparticulate carriers and nano particle preparations for carrying medicine of sensitive |
| WO2020076432A1 (en) * | 2018-10-08 | 2020-04-16 | Genentech, Inc. | Methods of treating cancer with pi3k alpha inhibitors and metformin |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN104644649A (en) * | 2013-11-21 | 2015-05-27 | 广东泰禾医药科技有限公司 | Medicinal composition for inhibiting IGF-1 signal transduction pathway |
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2015
- 2015-07-08 CN CN201510394747.4A patent/CN105147695A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104644649A (en) * | 2013-11-21 | 2015-05-27 | 广东泰禾医药科技有限公司 | Medicinal composition for inhibiting IGF-1 signal transduction pathway |
Non-Patent Citations (3)
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| C GRIMALDI 等: "AMP-dependent kinase/mammalian target of rapamycin complex 1 signaling in T-cell acute lymphoblastic leukemia: therapeutic implications", 《LEUKEMIA》 * |
| 戴炜辰 等: ""磷脂酰肌醇3-激酶抑制剂抗肿瘤临床研究进展"，戴炜辰 等，海峡药学，2014年12月31日，第26卷第6期，第6-13页", 《海峡药学》 * |
| 穆兰 等: ""二甲双胍与乳腺癌关系的研究进展"，穆兰 等，中国肿瘤临床，2014年12月31日，第41卷，第21期，第1413-1415页", 《中国肿瘤临床》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108553446A (en) * | 2018-05-16 | 2018-09-21 | 上海交通大学 | A kind of double nanoparticulate carriers and nano particle preparations for carrying medicine of sensitive |
| WO2020076432A1 (en) * | 2018-10-08 | 2020-04-16 | Genentech, Inc. | Methods of treating cancer with pi3k alpha inhibitors and metformin |
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Address after: 744300, Gansu Province, Dingxi District, Liberty Street, No. 54 Wen Yuan District, building 2, 1-202 Applicant after: Li Rongqin Address before: Kang Hong Lu 250000 Shandong province Ji'nan city high tech Development Zone No. 758 Applicant before: Li Rongqin |
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Application publication date: 20151216 |