CN100453071C - Oral resveratrol multi-phase liposome and preparation method thereof - Google Patents
Oral resveratrol multi-phase liposome and preparation method thereof Download PDFInfo
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- CN100453071C CN100453071C CNB2006100700220A CN200610070022A CN100453071C CN 100453071 C CN100453071 C CN 100453071C CN B2006100700220 A CNB2006100700220 A CN B2006100700220A CN 200610070022 A CN200610070022 A CN 200610070022A CN 100453071 C CN100453071 C CN 100453071C
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Abstract
The invention discloses an oral polyphase liposome of resveratrol, wherein the ingredients of the liposome include resveratrol, phosphatidy icholine, soybean lecithin, cholesterin, polyvinylpyrrolidone, hydroxypropylcellulose, Twain-80 or Twain-85, and phosphonate buffer solution. The oral preparation has the advantages of better adaptability for patients and simpler preparing process.
Description
Technical field
The present invention relates to a kind of anti-tumor drug, specifically, relate to a kind of oral resveratrol multi-phase liposome and preparation method thereof.
Background technology
Tumor is a kind of commonly encountered diseases and frequently-occurring disease, and is very big to the people's life and health threat, is the research topic that more and more comes into one's own in medical domain.In a plurality of at home big cities, malignant tumor has surpassed cardiovascular and cerebrovascular disease, come first of all disease death reasons, and at 35～59 years old age bracket, tumor is first killer always.Because the deadly infectious disease of many serious threat people's life health is under control in the past, the average life span prolongs gradually, and diagnostic techniques improves constantly, but the carcinogenic factor in the human environment day by day increases, therefore in a lot of countries, it is the first or per two that cancer occupies the cause of death at present.
Tumor treatment has operation, radiation and chemotherapy at present, to a great extent based on chemotherapy.Operation is relatively poor with the compliance of radiation therapy method, and chemotherapy can bring bigger toxic and side effects to the patient, when suppressing and poisoning the tumor cell of active proliferation, medullary cell, enterocyte, hair cell and sexual cell are produced inhibitory action too, lose therapeutical effect thereby be easy to generate drug resistance simultaneously.Along with improving constantly of The development in society and economy and people's lives, people are also improving constantly the requirement of life, quality of life, and the appearance of the antitumor drug of high-efficiency low-toxicity green environmental protection is also enjoyed popular confidence.
Resveratrol is the stronger non-flavonoid polyphenolic substance of a kind of activity that exists in many plants, resveratrol has the prevention of cardiovascular disease and tumor and health-care effect are caused in the world paid close attention to widely and furtherd investigate, and extensively sells in American-European market as health product and food additive.In recent years, active and concrete mechanism is furtherd investigate in a large number to the resveratrol antineoplastic both at home and abroad, thinks at present one of most promising anticancer composition that can match in excellence or beauty with paclitaxel.Studies have shown that at present resveratrol not only has the cardiovascular disease of control, antiinflammation, and the more important thing is that it has extensive anti-cancer, antitumaous effect.
Though resveratrol is a up-and-coming tumor prevention and a curative, because resveratrol is insoluble in water, and to photo-labile, the limitation of himself physicochemical properties, it is relatively poor to cause it to absorb in vivo, and bioavailability is not high, and clinical effectiveness is not satisfactory.
Summary of the invention
It is simple to the purpose of this invention is to provide a kind of preparation technology, oral resveratrol multi-phase liposome of nontoxic, non-immunogenicity, degradable, slow release and preparation method thereof.
For achieving the above object, technical scheme of the present invention is: oral resveratrol multi-phase liposome is characterized in that: described liposome is grouped into by following one-tenth:
Resveratrol, lecithin or soybean phospholipid, cholesterol, adjuvant.
Below be improvement of the technical scheme:
Described adjuvant is grouped into by following one-tenth:
Polyvinylpyrrolidone or hyprolose, tween 80 or tween 85, phosphate buffered solution.
The percentage by weight of described each composition of liposome is:
Resveratrol 5～10%
Lecithin or soybean phospholipid 2～15%
Cholesterol 2～15%
Polyvinylpyrrolidone or hyprolose 0.1～0.5%
Tween 80 or tween 85 0.5～1.5%
Phosphate buffered solution 60～80%.
The percentage by weight of described each composition of liposome is:
Resveratrol 6～8%
Lecithin or soybean phospholipid 5～10%
Cholesterol 5～10%
Polyvinylpyrrolidone or hyprolose 0.2～0.4%
Tween 80 or tween 85 0.7～1.3%
Phosphate buffered solution 65～75%.
The percentage by weight of described each composition of liposome is:
Resveratrol 7%
Lecithin or soybean phospholipid 8%
Cholesterol 8%
Polyvinylpyrrolidone or hyprolose 0.3%
Tween 80 or tween 85 1%
Phosphate buffered solution 70%.
The preparation method of oral resveratrol multi-phase liposome may further comprise the steps:
(1) proportionally take by weighing soybean phospholipid or lecithin, cholesterol and tween 80 or tween 85, and be dissolved in the ethanol, obtain alcoholic solution, standby;
(2) in proportion resveratrol, polyvinylpyrrolidone or hyprolose are dissolved in the phosphate buffered solution then, are incubated 50～70 ℃, under constant temperature, stir, and slowly add alcoholic solution, continue to stir 60～90min, ethanol is all volatilized to the greatest extent;
(3) continue to add phosphate buffer solution to full dose, handle 1 time, promptly get oral resveratrol multi-phase liposome by tissue mashing machine.
The structural formula of resveratrol is:
Resveratrol, English name are Resveratro|, Res, and chemistry is by name 3,4 ', 5-trihydroxy-anti--stilbene, molecular formula is C
14H
12O
3, molecular weight is 228.2.
Resveratrol is the non-flavonoid polyphenolic substance of a kind of activity that exists in many plants.The resveratrol acicular crystal that is white in color is insoluble in water, is insoluble to ether, can be dissolved in ethanol, and ethyl acetate is in the acetone equal solvent.Found first in 1940 to be subjected to the attention of the world of medicine since this composition always.Studies show that up to now: resveratrol has antitumor, antioxidation, anti-cardiovascular disease, antibacterium, antiinflammatory, and anticoagulant is regulated effects such as immunity.Resveratrol is called the another new green cancer therapy drug after paclitaxel, has become the active skull cap components that scientists is paid much attention to, has very big medical value and market prospect.
Resveratrol be plant under adverse circumstances or suffer pathogen when infringement, the excretory a kind of antitoxin of plant self can be resisted the infection of mycete.It is because of plant is subjected to fungal infection, produces under ultraviolet radiation or the pathological condition, and similar is in the estrogen diethylstilbestrol.
Resveratrol extensively is present in the various plants such as Vitaceae, Liliaceae, Polygonaceae, pulse family, Umbelliferae, the section that takes to the greenwood, Palmae, Gnetaceae, also contains this material in 70 kind of plant such as Semen arachidis hypogaeae, Fructus Mori, Fructus Vitis viniferae.In plants such as the Chinese medicine Rhizoma Polygoni Cuspidati of China, Radix Polygoni Multiflori, also found the existence of resveratrol.The most noticeable in every pharmacological action of resveratrol is antitumor action, but it is reported and the propagation of kinds of tumor cells in a plurality of systems such as the digestion of resveratrol antagonism, breathing, blood, reproduction source nasopharyngeal carcinoma, hepatocarcinoma, pulmonary carcinoma, gastric cancer, breast carcinoma, carcinoma of prostate, thyroid carcinoma, leukemia etc. are all had therapeutical effect.
Think that at present resveratrol mainly is by suppressing the cytochrome enzyme, inducing approach such as separating toxenzyme, inhibition Cycloxygenase, Profilin kinases, antagonism estrogen receptor, the differentiation of promotion tumor cell and apoptosis to reach antineoplastic action.
Beneficial effect:
The present invention adopts above technical scheme, will have the RES of antitumor action to wrap in the liposome, thereby has increased the concentration of medicine at target organ, simultaneously the release time of medicine because the specificity of liposome structure can slow down again, can play a role for more time.The RES multiphasic liposomes is an oral formulations, and is better to patient's compliance, and RES multiphasic liposomes preparation technology is simple, has characteristics such as nontoxic, non-immunogenicity, degradable, slow release in human body.
Tumor disease can effectively be prevented and treat to characteristics such as that the present invention has is nontoxic, non-immunogenicity, degradable, slow release, so have than higher economic value and social value.
Specific embodiment
Embodiment 1: oral resveratrol multi-phase liposome, and described liposome is grouped into by following one-tenth: resveratrol, lecithin, cholesterol, polyvinylpyrrolidone, tween 80, phosphate buffered solution;
The percentage by weight of described each composition of liposome is:
Resveratrol 6%
Lecithin 10%
Cholesterol 10%
Polyvinylpyrrolidone 0.2%
Tween 80 0.6%
Phosphate buffered solution 73.2%;
The preparation method of oral resveratrol multi-phase liposome may further comprise the steps:
(1) proportionally take by weighing lecithin, cholesterol and tween 80, and be dissolved in the ethanol, obtain alcoholic solution, standby;
(2) in proportion resveratrol, polyvinylpyrrolidone are dissolved in the phosphate buffered solution then, are incubated 50 ℃, under constant temperature, stir, and slowly add alcoholic solution, continue to stir 60min, ethanol is all volatilized to the greatest extent;
(3) continue to add phosphate buffer solution to full dose, handle 1 time, promptly get oral resveratrol multi-phase liposome by tissue mashing machine.
Embodiment 2: oral resveratrol multi-phase liposome, and described liposome is grouped into by following one-tenth: resveratrol, soybean phospholipid, cholesterol, hyprolose, tween 85, phosphate buffered solution;
The percentage by weight of described each composition of liposome is:
Resveratrol 7%
Soybean phospholipid 8%
Cholesterol 8%
Hyprolose 0.3%
Tween 85 1%
Phosphate buffered solution 70%;
The preparation method of oral resveratrol multi-phase liposome may further comprise the steps:
(1) proportionally take by weighing soybean phospholipid, cholesterol and tween 85, and be dissolved in the ethanol, obtain alcoholic solution, standby;
(2) in proportion resveratrol, hyprolose are dissolved in the phosphate buffered solution then, are incubated 60 ℃, under constant temperature, stir, and slowly add alcoholic solution, continue to stir 75min, ethanol is all volatilized to the greatest extent;
(3) continue to add phosphate buffer solution to full dose, handle 1 time, promptly get oral resveratrol multi-phase liposome by tissue mashing machine.
Embodiment 3: oral resveratrol multi-phase liposome, described liposome is grouped into by following one-tenth: resveratrol, lecithin, cholesterol, hyprolose, tween 80, phosphate buffered solution.
The percentage by weight of described each composition of liposome is:
Resveratrol 9%
Lecithin 14%
Cholesterol 14%
Hyprolose 0.5%
Tween 80 1.5%
Phosphate buffered solution 61%.
The preparation method of oral resveratrol multi-phase liposome may further comprise the steps:
(1) proportionally take by weighing lecithin, cholesterol and tween 80, and be dissolved in the ethanol, obtain alcoholic solution, standby;
(2) in proportion resveratrol, hyprolose are dissolved in the phosphate buffered solution then, are incubated 70 ℃, under constant temperature, stir, and slowly add alcoholic solution, continue to stir 90min, ethanol is all volatilized to the greatest extent;
(3) continue to add phosphate buffer solution to full dose, handle 1 time, promptly get oral resveratrol multi-phase liposome by tissue mashing machine.
Claims (1)
1, oral resveratrol multi-phase liposome, it is characterized in that: the percentage by weight of described each composition of liposome is: resveratrol 6%, lecithin 10%, cholesterol 10%, polyvinylpyrrolidone 0.2%, tween 80 0.6%, phosphate buffered solution 73.2%, and its preparation method may further comprise the steps:
(1) proportionally take by weighing lecithin, cholesterol and tween 80, and be dissolved in the ethanol, obtain alcoholic solution, standby;
(2) in proportion resveratrol, polyvinylpyrrolidone are dissolved in the phosphate buffered solution then, are incubated 50 ℃, under constant temperature, stir, and slowly add alcoholic solution, continue to stir 60min, ethanol is all volatilized to the greatest extent;
(3) continue to add phosphate buffer solution to full dose, handle 1 time, promptly get oral resveratrol multi-phase liposome by tissue mashing machine.
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| CN100453071C true CN100453071C (en) | 2009-01-21 |
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Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101874763A (en) * | 2009-04-29 | 2010-11-03 | 上海家化联合股份有限公司 | Resveratrol flexible liposome and preparation method thereof |
| CN104587140B (en) * | 2014-12-30 | 2018-11-30 | 中国中医科学院中药研究所 | Black false hellebore estrogen receptor antagon sample new role |
| CN108283624B (en) * | 2017-01-10 | 2021-01-12 | 北京化工大学 | Sorafenib nano liposome preparation and preparation method thereof |
| CA3058782A1 (en) * | 2017-04-03 | 2018-10-11 | The Regents Of The University Of California | Deformable nano-scale vehicles (dnvs) for trans-blood brain barrier, trans-mucosal, and transdermal drug delivery |
| CN109125302A (en) * | 2018-10-09 | 2019-01-04 | 上海市杨浦区中心医院(同济大学附属杨浦医院) | Application of resveratrol in medicine for treating bacterial pneumonia |
| CN113521005A (en) * | 2021-06-25 | 2021-10-22 | 卫士药业有限公司 | Nanometer lipid particle carrier for delivering resveratrol drug and preparation method and application thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1377262A (en) * | 1999-07-30 | 2002-10-30 | 宝洁公司 | Method and composition for prophylaxis and treatment of symptoms associated with cold and influenza-like illnesses |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1377262A (en) * | 1999-07-30 | 2002-10-30 | 宝洁公司 | Method and composition for prophylaxis and treatment of symptoms associated with cold and influenza-like illnesses |
Non-Patent Citations (6)
| Title |
|---|
| 具有肝脏靶向性的白藜芦醇脂质体. 王莉，张三奇，顾宜.解放军药学学报，第22卷第4期. 2006 |
| 具有肝脏靶向性的白藜芦醇脂质体. 王莉，张三奇，顾宜.解放军药学学报，第22卷第4期. 2006 * |
| 大豆磷脂组成与特性. 刘元法，王兴国.粮食与油脂，第3期. 2000 |
| 大豆磷脂组成与特性. 刘元法，王兴国.粮食与油脂，第3期. 2000 * |
| 白黎芦醇脂质体的制备工艺改进. 王莉，周红，张三奇等.第四军医大学学报，第26卷第20期. 2005 |
| 白黎芦醇脂质体的制备工艺改进. 王莉，周红，张三奇等.第四军医大学学报，第26卷第20期. 2005 * |
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Effective date of registration: 20090206 Address after: Mailbox 105, Department of pharmacy, Weifang Medical University, 288 Shengli East Street, Kuiwei District, Shandong Province, 261042, Weifang Co-patentee after: Wang Luyun Patentee after: Li Wan Zhong Co-patentee after: Li Aifeng Address before: Mailbox 105, Department of pharmacy, Weifang Medical University, 288 Shengli East Street, Kuiwei District, Shandong Province, 261042, Weifang Patentee before: Li Wanzhong |
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Granted publication date: 20090121 Termination date: 20101103 |