CN103860561A - Medicament composition for preventing and treating breast cancer and application thereof - Google Patents
Medicament composition for preventing and treating breast cancer and application thereof Download PDFInfo
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- CN103860561A CN103860561A CN201410135416.4A CN201410135416A CN103860561A CN 103860561 A CN103860561 A CN 103860561A CN 201410135416 A CN201410135416 A CN 201410135416A CN 103860561 A CN103860561 A CN 103860561A
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- cetirizine hydrochloride
- ftorafur
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- breast carcinoma
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Abstract
The invention discloses a medicament composition for preventing and treating breast cancer and application thereof. The active ingredient of the medicament composition comprises cetirizine hydrochloride and tegafur, wherein the weight ratio of the cetirizine hydrochloride to the tegafur in the active ingredient is preferably 1:(1-5). The medicament composition for preventing and treating breast cancer is remarkable in cancer suppression activity and low in toxic and side effect.
Description
Technical field
The invention belongs to medical technical field, in particular to a kind of cancer therapy drug, relate in particular to a kind of pharmaceutical composition and application thereof that prevents and treats breast carcinoma.
Background technology
Breast carcinoma is that one has a strong impact on one of even life-threatening modal malignant tumor of women's physical and mental health, is the modal nauseating tumor of global women, and its therapeutic modality is that auxiliary surgical is with chemotherapy, radiotherapy.Chemotherapy is one of conventional non-operative treatment for the treatment of breast carcinoma, but it has serious side effects.Therefore, improve sensitivity and the specificity of tumor cell to chemotherapeutic is research focus always.
Ftorafur (Tegafur, FT, FT-207) is one of miazines anticarcinogen, and it is the prodrug of 5-fluorouracil (5-FU), and most solid tumors are had to inhibitory action.Competent biosynthesis of disturbing blocking dna, RHA and protein in vivo, thus its antitumaous effect produced.Prove by medical basic research and clinical observation, ftorafur toxic and side effects is less, and chemotherapeutic index is higher, on immunosuppressive action and also less on the impact about immune internal organs, be can be clinically the safe drugs of use continuously.This medicine belongs to one of oral anti-cancer medicine few in number, oral after through gastrointestinal absorption, within 1-3 hour, blood level reaches summit.Last longer than intravenously administrable, therefore can bring into play its good therapeutic effect.Be mainly used in gastric cancer, colon and rectum carcinoma, etc. digestive tract cancer, also can be used for breast carcinoma, primary hepatocarcinoma, cancer of pancreas and pulmonary carcinoma.In addition, to preventing that recurrence after operation, transfer from having certain curative effect.The topmost untoward reaction of ftorafur is symptom of digestive tract and bone marrow depression, and gastral untoward reaction can badly influence cancer patient's compliance as nausea,vomiting,diarrhea etc.
Cetirizine (Cetirizine Hydrochloride) is a kind of potent H1 receptor antagonist, pharmaceutically active is stronger, there are good antiallergic and antiinflammatory action, and there is higher bioavailability, after administration, urticaria can not only be suppressed on a large scale and skin is general red, can also suppress inflammatory cell and divide a word with a hyphen at the end of a line to anaphylaxis position, thereby suppress later stage anaphylaxis, be a medicine with dual anti-allergic effects simultaneously.Cetirizine hydrochloride oral formulations (tablet, capsule etc.) is applicable to respiratory system, skin and eye anaphylactic disease, comprise perennially allergic disease, as anaphylaxis dermatosis, urticaria, allergic rhinitis, eye pruritus, eye conjunctivitis and asthma etc.Cetirizine hydrochloride oral formulations is also used for the treatment of all kinds department of dermatologry anaphylactic disease, as the treatment of chronic, artificial property, cold, tardy pressure, day photosensitiveness urticaria and atopic dermatitis etc.
At present, also do not have bibliographical information cetirizine hydrochloride to can be used to anti-breast cancer, there is no bibliographical information by cetirizine hydrochloride and ftorafur use in conjunction treatment breast carcinoma yet.
Summary of the invention
The inventor is surprised to find that while applying clinically cetirizine hydrochloride treatment patient with breast cancer's anaphylactic disease, and cetirizine hydrochloride coordinates ftorafur to have comparatively significant therapeutical effect to patient with breast cancer.Confirm that by internal and external test heavy dose of cetirizine hydrochloride has certain antitumor activity really subsequently, also confirmed that cetirizine hydrochloride associating ftorafur has collaborative anti-breast cancer effect more significantly simultaneously.Therefore, the object of the present invention is to provide a kind of pharmaceutical composition and pharmaceutical applications of preventing and treating breast carcinoma.
The inventor studies by lot of experiments, has finally obtained following technical scheme:
Prevent and treat a pharmaceutical composition for breast carcinoma, active component comprises cetirizine hydrochloride and ftorafur.
Preferably, prevent and treat as mentioned above the pharmaceutical composition of breast carcinoma, in active component, the weight ratio of cetirizine hydrochloride and ftorafur is 1: 1-5.
Further preferably, prevent and treat as mentioned above the pharmaceutical composition of breast carcinoma, in active component, the weight ratio of cetirizine hydrochloride and ftorafur is 1: 2.5.
Again further preferably, prevent and treat as mentioned above the pharmaceutical composition of breast carcinoma, it can be made into oral formulations; Described oral formulations preferred tablet and capsule.
Again further preferably, the above-mentioned pharmaceutical composition of preventing and treating breast carcinoma, the effective dose that in wherein said tablet or capsule, per unit preparation contains cetirizine hydrochloride is 50mg, the effective dose that contains ftorafur is 100mg-250mg.
Test confirms: heavy dose of cetirizine hydrochloride has certain anti-breast cancer cancer activity, can significantly suppress the growth of human breast carcinoma MDA-MB-231 cell transplanted tumor in nude mice.Therefore, second object of the present invention is to provide a kind of pharmaceutical applications of compound, i.e. the purposes of cetirizine hydrochloride in the medicine of preparing anti-breast cancer.In addition, in test, also find, the tumor-inhibiting action highly significant of ftorafur+cetirizine hydrochloride high dose group, compare model control group and single medicine group and all there is utmost point significant difference (P < 0.01), this is indicating that the cetirizine hydrochloride of high dose can promote the active anticancer of ftorafur, and two kinds of drug combinations demonstrate obvious synergism.Therefore, the 3rd object of the present invention is to provide a kind of pharmaceutical applications of compositions, the purposes of the active component that comprises cetirizine hydrochloride and ftorafur in the medicine of preparing anti-breast cancer.
Compared with prior art, the pharmaceutical composition antitumor activity of preventing and treating breast carcinoma provided by the invention is remarkable, and toxic and side effects is little, has enriched prior art, for having increased clinically a kind of potential anti-breast cancer new drug, there is social meaning and the economic implications of highly significant.
The specific embodiment
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, within the apparent change that those of ordinary skills make according to the present invention simultaneously and modification are also contained in the scope of the invention.
Embodiment 1: the preparation of tablet
Preparation technology:
Ftorafur, cetirizine hydrochloride are crossed to 120 mesh sieves, be dissolved in 60-80 ℃ of hot water with beta-schardinger dextrin-, more than keeping 60min, cooling, beta-schardinger dextrin-is separated out rear filtration, dries, and sieves; Mannitol, low-substituted hydroxypropyl cellulose, aspartame are crossed 100 mesh sieves, take by recipe quantity, and mix homogeneously, adds distilled water appropriate, granulate, and dry, and granulate, adds recipe quantity Pulvis Talci, mix tabletting and get final product.
Embodiment 2: the preparation of tablet
Preparation technology:
Ftorafur, cetirizine hydrochloride are crossed to 120 mesh sieves, fully be ground with beta-schardinger dextrin-, lactose, carboxymethyl starch sodium, Fructus Citri Limoniae essence are crossed 100 mesh sieves, take by recipe quantity, mix homogeneously, add distilled water appropriate, granulate, dry, granulate, add recipe quantity magnesium stearate, mix, tabletting and get final product.
Embodiment 3: cetirizine hydrochloride and ftorafur coupling pair
40 of SPF level BALB/c-nu mices, 6 week age, body weight 18g-20g.Will be in exponential phase, in the MDA-MB-231 breast cancer cell bottle of degree of converging 80%～90%, culture medium is inhaled and is abandoned, and uses phosphate buffer wash cell 2-3 time, trypsin 0.25%) digestion, collecting cell, with phosphate buffer washing, piping and druming mixes, counts again; Adjust concentration with serum-free RPMI-1640 again, by every nude mice back subcutaneous vaccination cell number 1.0 × 10
7/ 0.2mL pallium cell injection is subcutaneous in nude mice back.After inoculation, 7d starts, the subcutaneous visible lesser tubercle of oncocyte inoculation position, about 5mm × 5mm size; To the 10th day, the about 7mm × 7mm of tumor size.
Get into 35 of tumor nude mices, adopt random and homeostatic principle to be divided into 7 groups, 5 every group.Each group gastric infusion, its tested material and dosage are: 1. matched group, pure water 0.6mL/ is only; 2. ftorafur group (100mg/kg); 3. cetirizine hydrochloride low dose group (5mg/kg); 4. cetirizine hydrochloride high dose group (20mg/kg); 5. ftorafur (100mg/kg)+cetirizine hydrochloride low dosage (5mg/kg) group; 6. ftorafur (50mg/kg)+cetirizine hydrochloride high dose (20mg/kg) group.The equal administration of each group 2 weeks, once a day.
After last administration, 48h puts to death nude mice, gets transplanted tumor and measures tumor size, and method is: respectively with vernier cursor measure subcutaneous transplantation tumor bottom Y-axis (L) and × axle (W) length, by formula [V=0.52 × L × W] calculating gross tumor volume.The heavy suppression ratio of tumor (%)=[1-(the average tumor weight of the average tumor weight/matched group of experimental group)] × 100%.Strip transplanted tumor, each tumor tissue cuts part and carries out routine pathology section, HE dyeing.Under mirror, visible cancerous tissue is separated into the cancer nests differing in size by interfibrillar substance, visible lumen of gland, glandular tube spline structure; Cancerous cell differs in size, rounded or oval; Core is large, and kernel is obvious, visible pathologic mitosis picture, and the micro-basophilic of endochylema is translucent.Each group nude mice by subcutaneous growth of xenografted situation is in table 1.
The heavy suppression ratio comparison of the each group of table 1 mice-transplanted tumor tumor
With matched group comparison,
*p < 0.05,
*p < 0.01;
With the comparison of ftorafur group,
$p < 0.05,
$$p < 0.01;
With the comparison of cetirizine hydrochloride high dose,
$p < 0.05,
$ $p < 0.01.
Result of the test by table 1 can be found out, outside demineralizing acid cetirizine low dose group, other each experimental group tumor volumes and tumor are heavily starkly lower than matched group (P < 0.05 or P < 0.01), cetirizine hydrochloride low dose group does not show antitumor activity, but cetirizine hydrochloride high dose group has shown certain tumor-inhibiting action, especially the tumor-inhibiting action highly significant of ftorafur+cetirizine hydrochloride high dose group, compare matched group and single medicine group and all there is utmost point significant difference (P < 0.01), this is indicating that the cetirizine hydrochloride of high dose can promote the active anticancer of ftorafur, two kinds of drug combinations demonstrate obvious synergism.
In addition, observe and find at experimental session, ftorafur high dose group mice engenders movable minimizing, lethargy, diarrhoea, leukocyte and centriole Leukopenia, the performances such as appetite and weight loss, but all the other each group nude mices have no obvious adverse reaction.This explanation, the ftorafur of high dose has comparatively significantly toxic reaction to nude mice, and while reducing ftorafur consumption, the toxic and side effects that this chemotherapy is brought has obtained effective control.
Claims (8)
1. prevent and treat a pharmaceutical composition for breast carcinoma, be prepared from by active component and pharmaceutically acceptable auxiliaries, it is characterized in that: described active component comprises cetirizine hydrochloride and ftorafur.
2. the pharmaceutical composition of preventing and treating breast carcinoma according to claim 1, is characterized in that: in described active component, the weight ratio of cetirizine hydrochloride and ftorafur is 1: 1-5.
3. the pharmaceutical composition of preventing and treating breast carcinoma according to claim 1, is characterized in that: in described active component, the weight ratio of cetirizine hydrochloride and ftorafur is 1: 2.5.
4. according to the pharmaceutical composition of preventing and treating breast carcinoma described in claim 1-3 any one, it is characterized in that: described pharmaceutical composition is oral formulations.
5. according to the pharmaceutical composition of preventing and treating breast carcinoma described in claim 1-3 any one, it is characterized in that: described pharmaceutical composition is tablet, capsule.
6. the pharmaceutical composition of preventing and treating breast carcinoma according to claim 5, is characterized in that: the effective dose that in described tablet or capsule, per unit preparation contains cetirizine hydrochloride is 50mg, the effective dose that contains ftorafur is 100mg-250mg.
7. the purposes of cetirizine hydrochloride in the medicine of preparing anti-breast cancer.
8. the purposes of the active component that comprises cetirizine hydrochloride and ftorafur in the medicine of preparing anti-breast cancer.
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| CN201410135416.4A CN103860561B (en) | 2014-04-08 | 2014-04-08 | A kind of pharmaceutical composition and application thereof preventing and treating breast carcinoma |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101193622A (en) * | 2005-06-09 | 2008-06-04 | 比奥里波克斯公司 | Method and composition for treating inflammatory disorders |
| WO2009124755A1 (en) * | 2008-04-08 | 2009-10-15 | European Molecular Biology Laboratory (Embl) | Compounds with novel medical uses and method of identifying such compounds |
| CA2828877A1 (en) * | 2011-03-03 | 2012-09-07 | Vanderbilt University | 6-alkyl-n-(pyridin-2-yl)-4-aryloxypicolinamide analogs as mglur5 negative allosteric modulators and methods of making and using the same |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101193622A (en) * | 2005-06-09 | 2008-06-04 | 比奥里波克斯公司 | Method and composition for treating inflammatory disorders |
| WO2009124755A1 (en) * | 2008-04-08 | 2009-10-15 | European Molecular Biology Laboratory (Embl) | Compounds with novel medical uses and method of identifying such compounds |
| CA2828877A1 (en) * | 2011-03-03 | 2012-09-07 | Vanderbilt University | 6-alkyl-n-(pyridin-2-yl)-4-aryloxypicolinamide analogs as mglur5 negative allosteric modulators and methods of making and using the same |
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