CN100431538C - An anticancer pharmaceutical composition and preparation method thereof - Google Patents
An anticancer pharmaceutical composition and preparation method thereof Download PDFInfo
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- CN100431538C CN100431538C CNB2006100278898A CN200610027889A CN100431538C CN 100431538 C CN100431538 C CN 100431538C CN B2006100278898 A CNB2006100278898 A CN B2006100278898A CN 200610027889 A CN200610027889 A CN 200610027889A CN 100431538 C CN100431538 C CN 100431538C
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- sophocarpine
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Abstract
The present invention relates to an anticancer medicine composition, particularly to an anticancer medicine composition containing sophocarpine and diazepam and a preparing method thereof.
Description
[technical field]
The present invention relates to a kind of anticancer pharmaceutical composition and preparation method thereof, particularly a kind of antitumor drug that contains sophocarpine and diazepam and preparation method thereof.
[background technology]
Sophocarpine is a kind of alkaloid that extracts from Herba Sophorae alopecuroidis (Sophora A1opecuroides L.), multiple animal solid tumor there is cancer suppressing action, clinical have significant curative effect to trophoblastic tumor, malignant lymphoma etc., Jiangxi Province health care of women institute uses the sophocarpine treatment and dislikes Portugal's 112 routine clinical cure 97 examples (86.6%), main organs is not had influence, bone marrow is not suppressed.
In therapeutic process since the treatment disease or character, the order of severity, patient's age, body weight, the general health state of pathological state, and patient is to the factors such as sensitivity, toleration and administering mode of used medicine, in order to reach therapeutic effect, the dosage individual variation is very big.Yet, along with nervous system reaction in various degree can appear in the increasing of dosage, as excited, clonospasm in various degree, even neurotoxicity such as death, symptom is relevant with dosage.
The objective of the invention is problem, invented a kind of anticancer pharmaceutical composition, neither influence the sophocarpine antitumaous effect, can obviously alleviate its neurotoxicity again at above-mentioned existence.
[summary of the invention]
Diazepam is usually used in the inhibition of nervus centralis as a kind of conventional medicine, and known clinical practice and effect are: anxiety, tranquilizing soporific, epilepsy and anticonvulsant action, central myorelaxant effects.Be characterized in that toxicity is low, safety range is big.
The invention provides a kind of anticancer pharmaceutical composition, neither influence the sophocarpine antitumaous effect, can alleviate its neurotoxicity again.Said composition comprises active component sophocarpine and diazepam.
The present invention tests and finds pleasantly surprisedly that diazepam is anticancer to sophocarpine, caused neurovirulent weakening has significant effect in the antitumor, not only can reduce the slight excitement, the uneasiness that cause under the sophocarpine low dosage, can under the neurovirulent situation that weakens under sophocarpine high dose, the overdose, improve the fatal dose (LD of mice greatly equally
100).Our experiment is found also pleasantly surprisedly, for independent use sophocarpine injection normal dose down can't the situation of kill cancer cell under, overdose uses the present composition not only can obviously reduce neurotoxicity, reduce the animal dead rate, can demonstrate effect anticancer significantly, that kill cancerous cell again.This is that those skilled in the art can't expect.
In an embodiment of the present invention, the weight ratio of sophocarpine and diazepam is 100 in the said pharmaceutical composition: 0.1-6.0.
In another preferred embodiment of the present invention, the weight ratio of sophocarpine and diazepam is 100 in the said pharmaceutical composition: 0.3-3.0.
In another preferred embodiment of the present invention, the weight ratio of sophocarpine and diazepam is 100 in the said pharmaceutical composition: 0.5-2.0.
Can use conventional method production known in the art or prepare pharmaceutical composition of the present invention.For example: the present composition can be made injection, comprising the following step: at first take by weighing the sophocarpine and the diazepam of scheduled volume, join in the The suitable solvent as dissolving in the water for injection, reconcile PH5.0-7.0, filter, embedding.Preferred injection, injectable sterile powder.
In order to make injection, can use the operable carrier of field of medicaments and excipient, solvent, for example: water for injection, propylene glycol, glycerol, Polyethylene Glycol, mannitol, xylitol, lecithin, vegetable oil, hydrochloric acid, phosphoric acid, citric acid, sodium hydroxide and bisulfite such as receive at antioxidant, chelating agent etc.
The present composition can be made transdermal absorption formulation such as patch, liniment, gel, ointment, ointment.
Pharmaceutical composition of the present invention can be mixed with the solution that is suitable for oral administration, powder, tablet, granule, pill, Emulsion, suspending agent, capsule, gel etc.Among the present invention, preferred oral liquid.
In another preferred embodiment of the present invention, wherein said pharmaceutical composition is according to preparation characteristic, and sophocarpine exists with salt form in preparation, preferred salt hydrochlorate, phosphate, acetate, citrate, maleate.
In general, the dosage of pharmaceutical composition of the present invention was generally 1-100mg/kg/ days, certainly, definite dosage should be according to character, the order of severity, patient's age, body weight, the general health state of disease to be treated or pathological state, and patient is determined by the clinician according to the principle of individuation the factors such as sensitivity, toleration and administering mode of used medicine.
[specific embodiment]
Further specify the present invention by embodiment, therefore do not limit the invention among the scope of embodiment.
[experimental example 1] sophocarpine is to the neural influence of mice
Select at random 4 age in week 90 of mices, 10 every group, reference substance sophocarpine aqueous solution of lumbar injection (ip) various dose (50,120,200mg/kg) and corresponding present composition aqueous solution were observed result's (seeing Table 1) respectively 30 minutes respectively.
The result as seen, compare with matched group, injected the present composition that comprises diazepam and compare with the caused neurotoxicity of the experiment mice of independent use sophocarpine, no matter its mice excitement degree such as Folium Pini occur, shake, muscle spasm etc., still death toll all demonstrates significant reduction.The present composition is better than matched group significantly.
Table 1 sophocarpine is to the neural influence of mice
Experimental example 2 present compositions are to the inhibitory action of mouse cervical cancer
Carry out routinely with anticancer experiment of cervical cancer 14 (U14) and method for estimating curative effect, 24h behind the inoculation oncocyte, difference lumbar injection (ip) normal saline (blank group), sophocarpine 60mg/kg (matched group 1), sophocarpine 120mg/kg (matched group 2), the present composition (sophocarpine and diazepam weight ratio 100: 2) experimental group, once a day, injection is 8-10 days.The results are shown in Table 2
Table 2 present composition is to the inhibitory action of mouse cervical cancer
Annotate: dosage is the sophocarpine amount in this experimental group,
*P＜0.05,
* *P＜0.01
Above experimental result shows that when the sophocarpine low dosage used, the present composition was compared matched group, and cancer suppressing ratio is basic identical, but weakening aspect the neurotoxicityes such as uneasiness that sophocarpine causes, Folium Pini, spasm, has significant inhibitory effect.Experimental result makes that we are beyond thought to be, under high dose, the present composition has reduced the mortality rate of animal significantly, compares low dose group simultaneously, and its cancer suppressing ratio obviously increases.
[experimental example 3] present composition is to the inhibitory action of mouse tumor
With murine sarcoma 37 (S37), sarcoma 180 (S180), No. 1, lymphosarcoma (Lio1).Anticancer experiment and method for estimating curative effect carry out routinely.
24h behind the inoculation oncocyte, lumbar injection (ip) normal saline (blank group), sophocarpine (matched group) and the present composition (being equivalent to sophocarpine amount 200mg/kg), once a day, injected 8 days, the result is to solid tumor, S180, S37, the cancer suppressing ratio of Lio1 are 32-55.5% (p＜0.01) (tables 3).
Table 3 anticancer pharmaceutical composition is to the influence of solid tumor.
**p＜0.05
***p＜0.01
Above-mentioned evidence pharmaceutical composition of the present invention both can reduce the neurotoxicity of sophocarpine significantly under high dose, can improve anticancer therapeutic significantly again simultaneously.
[formulation example 1]
Prescription: sophocarpine 25g diazepam 0.25g
Method for making: take by weighing ormal weight sophocarpine, diazepam respectively, add the injection water and dissolve in right amount, add water to 1000ml, drip an amount of dilute hydrochloric acid and transfer PH5.0-7.0, filtration, fill, sterilization.
[formulation example 2]
Prescription: sophocarpine 25g diazepam 0.125g
Method for making: take by weighing ormal weight sophocarpine, diazepam respectively, add the injection water and dissolve in right amount, add water to 1000ml.Filtration, fill, lyophilizing.
Claims (6)
1, a kind of anticancer pharmaceutical composition is characterized in that the weight ratio of said active ingredient in pharmaceutical is as follows:
Sophocarpine 100 diazepam 0.1-6.0.
2,, it is characterized in that the weight ratio of sophocarpine and diazepam is: 100: 0.3-3.0 as the said pharmaceutical composition of claim 1.
3,, it is characterized in that the weight ratio of sophocarpine and diazepam is: 100: 0.5-2.0 as the said pharmaceutical composition of claim 1.
4, pharmaceutical composition as claimed in claim 1 is characterized in that: wherein add one or more pharmaceutically acceptable carrier or excipient.
5, as any said pharmaceutical composition of claim 1-4, it is characterized in that: it is injection, oral formulations or transdermal absorption formulation.
6, as the said pharmaceutical composition of claim 5, it is characterized in that: the preparation method of this injection comprises the steps:
A gets sophocarpine and diazepam solubilizer stirring and dissolving,
B regulates pH5.0-7.0,
C filtration, fill, seal.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100278898A CN100431538C (en) | 2006-06-20 | 2006-06-20 | An anticancer pharmaceutical composition and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100278898A CN100431538C (en) | 2006-06-20 | 2006-06-20 | An anticancer pharmaceutical composition and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN1864678A CN1864678A (en) | 2006-11-22 |
| CN100431538C true CN100431538C (en) | 2008-11-12 |
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| Application Number | Title | Priority Date | Filing Date |
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| CNB2006100278898A Expired - Fee Related CN100431538C (en) | 2006-06-20 | 2006-06-20 | An anticancer pharmaceutical composition and preparation method thereof |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN113995753A (en) * | 2021-12-20 | 2022-02-01 | 杭州师范大学 | Application of Chinese medicinal molecular sophocarpine in preparing medicament for treating glioblastoma |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1135979C (en) * | 1999-10-26 | 2004-01-28 | 上海第二医科大学附属仁济医院 | Application of sophocarpine in preparation of medicine for curing coxsackievirus B myocarditis and its preparation method |
| CN1600308A (en) * | 2003-09-28 | 2005-03-30 | 上海第二医科大学附属仁济医院 | Application of l-sophocarpine on preparing medication for curing disease caused by coronavirus |
| CN1785184A (en) * | 2004-12-10 | 2006-06-14 | 上海第二医科大学附属仁济医院 | Application of sophocarpine in use of making medicines |
-
2006
- 2006-06-20 CN CNB2006100278898A patent/CN100431538C/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1135979C (en) * | 1999-10-26 | 2004-01-28 | 上海第二医科大学附属仁济医院 | Application of sophocarpine in preparation of medicine for curing coxsackievirus B myocarditis and its preparation method |
| CN1600308A (en) * | 2003-09-28 | 2005-03-30 | 上海第二医科大学附属仁济医院 | Application of l-sophocarpine on preparing medication for curing disease caused by coronavirus |
| CN1785184A (en) * | 2004-12-10 | 2006-06-14 | 上海第二医科大学附属仁济医院 | Application of sophocarpine in use of making medicines |
Non-Patent Citations (4)
| Title |
|---|
| 苦参及其生物碱抗肿瘤活性研究进展. 许相儒等.中国中西医结合杂志，第18卷第5期. 1998 |
| 苦参及其生物碱抗肿瘤活性研究进展. 许相儒等.中国中西医结合杂志，第18卷第5期. 1998 * |
| 苦参类生物碱抗肿瘤作用. 胡淑平等.特产研究，第3期. 2004 |
| 苦参类生物碱抗肿瘤作用. 胡淑平等.特产研究，第3期. 2004 * |
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| CN1864678A (en) | 2006-11-22 |
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Owner name: SHANGHAI FANGDA PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: JU HONGFU Effective date: 20110629 Owner name: JU HONGFU Free format text: FORMER OWNER: SHANGHAI FUJIA MEDICAL SCIENTIFIC RESEARCH CO., LTD. |
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Effective date of registration: 20110629 Address after: 201714 No. 363 Shen brick road, Qingpu District, Shanghai Co-patentee after: Ju Hongfu Patentee after: Shanghai Fangda Pharmaceutical Co., Ltd. Address before: 200331 No. 318 Chang He road, Shanghai, Putuo District Co-patentee before: Shanghai Fujia Medical Scientific Research Co., Ltd. Patentee before: Ju Hongfu |
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