CN104398490A - 一种纳米化水飞蓟宾磷酸钙复合微胶囊的制备方法 - Google Patents
一种纳米化水飞蓟宾磷酸钙复合微胶囊的制备方法 Download PDFInfo
- Publication number
- CN104398490A CN104398490A CN201410614641.6A CN201410614641A CN104398490A CN 104398490 A CN104398490 A CN 104398490A CN 201410614641 A CN201410614641 A CN 201410614641A CN 104398490 A CN104398490 A CN 104398490A
- Authority
- CN
- China
- Prior art keywords
- calcium phosphate
- silybin
- silibinin
- preparation
- nanocrystalized
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 229910000389 calcium phosphate Inorganic materials 0.000 title claims abstract description 22
- 239000001506 calcium phosphate Substances 0.000 title claims abstract description 22
- 238000002360 preparation method Methods 0.000 title claims abstract description 14
- 239000003094 microcapsule Substances 0.000 title claims abstract description 13
- 239000002131 composite material Substances 0.000 title claims abstract description 11
- SEBFKMXJBCUCAI-HKTJVKLFSA-N silibinin Chemical compound C1=C(O)C(OC)=CC([C@@H]2[C@H](OC3=CC=C(C=C3O2)[C@@H]2[C@H](C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 SEBFKMXJBCUCAI-HKTJVKLFSA-N 0.000 claims abstract description 44
- SEBFKMXJBCUCAI-UHFFFAOYSA-N NSC 227190 Natural products C1=C(O)C(OC)=CC(C2C(OC3=CC=C(C=C3O2)C2C(C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 SEBFKMXJBCUCAI-UHFFFAOYSA-N 0.000 claims abstract description 39
- 235000014899 silybin Nutrition 0.000 claims abstract description 36
- 235000011010 calcium phosphates Nutrition 0.000 claims abstract description 14
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims abstract description 14
- 230000003993 interaction Effects 0.000 claims abstract description 3
- 239000000463 material Substances 0.000 claims abstract description 3
- 229950000628 silibinin Drugs 0.000 claims description 31
- 230000000975 bioactive effect Effects 0.000 claims description 5
- 150000001875 compounds Chemical class 0.000 claims description 5
- 150000002500 ions Chemical class 0.000 claims description 2
- FDQAOULAVFHKBX-UHFFFAOYSA-N Isosilybin A Natural products C1=C(O)C(OC)=CC(C2C(OC3=CC(=CC=C3O2)C2C(C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 FDQAOULAVFHKBX-UHFFFAOYSA-N 0.000 abstract description 7
- VLGROHBNWZUINI-UHFFFAOYSA-N Silybin Natural products COc1cc(ccc1O)C2OC3C=C(C=CC3OC2CO)C4Oc5cc(O)cc(O)c5C(=O)C4O VLGROHBNWZUINI-UHFFFAOYSA-N 0.000 abstract 5
- 229940043175 silybin Drugs 0.000 abstract 5
- CYGIJEJDYJOUAN-UHFFFAOYSA-N Isosilychristin Natural products C1=C(O)C(OC)=CC(C2C3C=C(C4C(C3=O)(O)OCC42)C2C(C(=O)C3=C(O)C=C(O)C=C3O2)O)=C1 CYGIJEJDYJOUAN-UHFFFAOYSA-N 0.000 description 4
- 239000000047 product Substances 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 230000004071 biological effect Effects 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 235000013376 functional food Nutrition 0.000 description 3
- 210000004185 liver Anatomy 0.000 description 3
- 229960004245 silymarin Drugs 0.000 description 3
- 235000017700 silymarin Nutrition 0.000 description 3
- 239000006228 supernatant Substances 0.000 description 3
- FDQAOULAVFHKBX-KMRPREKFSA-N (+)-Isosilybin A Natural products C1=C(O)C(OC)=CC([C@@H]2[C@H](OC3=CC(=CC=C3O2)[C@@H]2[C@@H](C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 FDQAOULAVFHKBX-KMRPREKFSA-N 0.000 description 2
- FDQAOULAVFHKBX-HKTJVKLFSA-N (2r,3r)-3,5,7-trihydroxy-2-[(2r,3r)-2-(4-hydroxy-3-methoxyphenyl)-3-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-6-yl]-2,3-dihydrochromen-4-one Chemical compound C1=C(O)C(OC)=CC([C@@H]2[C@H](OC3=CC(=CC=C3O2)[C@@H]2[C@H](C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 FDQAOULAVFHKBX-HKTJVKLFSA-N 0.000 description 2
- KDMGQPNVTKUNHV-UHFFFAOYSA-N Isosilybin Natural products C1=C(O)C(OC)=CC=C1C1C(CO)OC2=CC=C(C3C(C(=O)C4=C(O)C=C(O)C=C4O3)O)C=C2O1 KDMGQPNVTKUNHV-UHFFFAOYSA-N 0.000 description 2
- RIAZZJBPJQWPIS-UHFFFAOYSA-N Silychristin Natural products COc1cc(ccc1O)C2OC3C(C=C(C=C3O)C4Oc5cc(O)cc(O)c5C(=O)C4O)C2CO RIAZZJBPJQWPIS-UHFFFAOYSA-N 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 230000003078 antioxidant effect Effects 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- BMLIIPOXVWESJG-LMBCONBSSA-N silychristin Chemical compound C1=C(O)C(OC)=CC([C@H]2[C@@H](C3=C(C(=CC(=C3)[C@@H]3[C@H](C(=O)C4=C(O)C=C(O)C=C4O3)O)O)O2)CO)=C1 BMLIIPOXVWESJG-LMBCONBSSA-N 0.000 description 2
- BMLIIPOXVWESJG-UHFFFAOYSA-N silychristin A Natural products C1=C(O)C(OC)=CC(C2C(C3=C(C(=CC(=C3)C3C(C(=O)C4=C(O)C=C(O)C=C4O3)O)O)O2)CO)=C1 BMLIIPOXVWESJG-UHFFFAOYSA-N 0.000 description 2
- CYGIJEJDYJOUAN-JSGXPVSSSA-N silydianin Chemical compound C1=C(O)C(OC)=CC([C@H]2[C@H]3C=C([C@@H]4[C@@](C3=O)(O)OC[C@@H]42)[C@@H]2[C@H](C(=O)C3=C(O)C=C(O)C=C3O2)O)=C1 CYGIJEJDYJOUAN-JSGXPVSSSA-N 0.000 description 2
- 238000001179 sorption measurement Methods 0.000 description 2
- 241000208838 Asteraceae Species 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- MZBGBHVFCYCYLX-UHFFFAOYSA-N Silydianin Natural products COc1cc(ccc1O)C2C3COC4(O)C3C=C(C5Oc6cc(O)cc(O)c6C(=O)C5O)C2C4=O MZBGBHVFCYCYLX-UHFFFAOYSA-N 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 230000003064 anti-oxidating effect Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 231100000481 chemical toxicant Toxicity 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 229960000935 dehydrated alcohol Drugs 0.000 description 1
- 239000008367 deionised water Substances 0.000 description 1
- 229910021641 deionized water Inorganic materials 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 230000002443 hepatoprotective effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 230000008929 regeneration Effects 0.000 description 1
- 238000011069 regeneration method Methods 0.000 description 1
- 229950004304 silidianin Drugs 0.000 description 1
- 239000012086 standard solution Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
本发明提供一种纳米化水飞蓟宾磷酸钙复合微胶囊的制备方法，选择具有良好生物相容性、生物活性的纳米级无定型磷酸钙(ACP)为主体材料，通过离子、电荷相互作用对水飞蓟宾进行复合。具体的为：配制浓度为5600ug/mL的水飞蓟宾，取配制好的水飞蓟宾溶液5mL，并加入5mg纳米级无定型磷酸钙(ACP)，超声20分钟，于摇床中在160r/min的转速、37℃的温度下摇匀，在加入纳米磷酸钙后10min，水飞蓟宾的装载量达到最大值，纳米化水飞蓟宾磷酸钙复合微胶囊制备成功。本发明的优点在于：可以较理想的稳定水飞蓟宾结构、发挥其生物活性，实现功能分子的高效利用，对功能性食品、保健品及生物医学应用均具有极其重要的研究和现实意义。
Description
技术领域
本发明涉及微胶囊的制备方法，尤其涉及一种水飞蓟宾磷酸钙复合微胶囊的制备方法。
背景技术
水飞蓟素(Silymarin)是指从菊科药用植物水飞蓟种子的种皮中提取所得的一种黄酮木脂素类化合物，呈黄色粉末，味苦。其分子式如下：
主要的活性成分有水飞蓟宾(Silybin)、异水飞蓟宾(Isosilybin)、水飞蓟亭(Silychristin)和水飞蓟宁(Silydianin)等四种同分异构体，其中水飞蓟宾含量为50％-70％。水飞蓟素用来治疗肝胆疾病已有2000多年的历史，水飞蓟宾作为其主要的活性成分可以防止化学毒素、食物毒素和药物等对肝脏造成的损伤，促进肝细胞的再生和修复，被称为“天然的保肝药”；作为强抗氧化剂，能够清除人体内的自由基，延缓衰老。近年来，由于水飞蓟宾显示出保肝和抗氧化以外的活性而备受关注，其中水飞蓟宾表现出的抗癌和肿瘤预防作用已经显示出很好的开发潜力。它被广泛应用于医药、保健品、食品和化妆品等产品中。
水飞蓟宾是具有抗肿瘤、抗氧化活性的天然活性分子，但是具有稳定性差、易降解、生物利用率低的缺点，使其在功能食品、生物医学等领域的应用受到极大限制。
如何能够较理想的稳定水飞蓟宾的结构、发挥其生物活性，实现功能分子的高效利用，对功能性食品、保健品及生物医学应用均具有极其重要的研究和现实意义。
发明内容
本发明的所要解决的技术问题在于提供一种纳米化水飞蓟宾磷酸钙复合微胶囊的制备方法，能够较理想的稳定水飞蓟宾结构、发挥其生物活性，实现功能分子的高效利用。
本发明采用以下技术方案解决上述技术问题的：一种纳米化水飞蓟宾磷酸钙复合微胶囊的制备方法，选择具有良好生物相容性、生物活性的纳米级无定型磷酸钙(ACP)为主体材料，通过离子、电荷相互作用对水飞蓟宾进行复合。
具体的制备方法为：配制浓度为5800ug/mL的水飞蓟宾，取配制好的水飞蓟宾溶液5mL，并加入5mg纳米级无定型磷酸钙(ACP)，超声20分钟，于摇床中在160r/min的转速、37℃的温度下摇匀，在加入纳米磷酸钙后10min，水飞蓟宾的装载量达到最大值，纳米化水飞蓟宾磷酸钙复合微胶囊制备成功。
本发明的优点在于：可以较理想的稳定水飞蓟宾结构、发挥其生物活性，实现功能分子的高效利用，对功能性食品、保健品及生物医学应用均具有极其重要的研究和现实意义。
附图说明
图1是水飞蓟宾的标准曲线。
图2是不同浓度下水飞蓟宾的装载量曲线。
图3是不同吸附时间下水飞蓟宾的装载量曲线。
具体实施方式
以下结合附图对本发明进行详细的描述。
1标准曲线的制作
分别取0.1mL、0.2mL、0.4mL、0.8mL、1.0mL水飞蓟宾，放入50mL容量瓶中，再分别加入19.9mL、19.8mL、19.6mL、19.2mL、19.0mL 75％无水乙醇。分别配置成5ug/L、10ug/L、20ug/L、40ug/L、50ug/L的标准溶液。标准曲线的相关系数r2＝0.9902，说明相关性较好。
2、不同浓度下水飞蓟宾分子同纳米磷酸钙的吸附
分别配置50ug/mL、100ug/mL、200ug/mL、500ug/mL、1000ug/mL、1200ug/mL、1400ug/mL、1600ug/mL、1800ug/mL、2000ug/mL、2200ug/mL、2400ug/mL2600ug/mL、2800ug/mL、3000ug/mL、3200ug/mL、3400ug/mL、3600ug/mL、3800ug/mL、4000ug/mL、4200ug/mL、4400ug/mL、4600ug/mL、5000ug/mL、5200ug/mL、5400ug/mL、5600ug/mL、5800ug/mL、6000ug/mL的水飞蓟宾分子溶液，从中取出8mL于离心管中，分别加入5mgACP，超声20分钟，于摇床中在160r/min，37℃摇匀6h，并每隔2h离心管取出摇匀一次。吸附完成后将样品置于冰箱中静置12h(或者离心)，取上清液进行紫外表征，下层放在冰箱待用。由标准曲线，计算装载量，并作相关曲线。
(1)装载量L(％)＝(m1/W1)×100％
M1:微胶囊中所包埋的活性分子的质量
W1:复合物的总重量(理论上是说干态样品)
装载量(mg/g):(活性分子的加入量-上清液中的活性分子的量)/复合物重量。
(2)由曲线可知，在水飞蓟宾的浓度为5800ug/mL时，装载量最合适为902.61mg/g。
2、不同时间下水飞蓟宾分子同纳米磷酸钙的吸附
配制水飞蓟宾浓度为5800ug/mL，取溶液5mL，并加入5mgACP，超声20分钟，于摇床中在160r/min，37℃摇匀，分别在加入ACP后0、10、20、40、60、90、120min，离心后取上层清液50μL于2mL管中，并加入450μL去离子水稀释以做紫外表征，由标准曲线，计算装载量，作相关曲线，下层放在冰箱待用。平行测量三组实验。
可以看出，对于ACP，在25min左右，水飞蓟宾的装载量达到最大值，然后随着吸附时间的增加，装载量逐渐递减。
以上所述仅为本发明创造的较佳实施例而已，并不用以限制本发明创造，凡在本发明创造的精神和原则之内所作的任何修改、等同替换和改进等，均应包含在本发明创造的保护范围之内。
Claims (2)
1.一种纳米化水飞蓟宾磷酸钙复合微胶囊的制备方法，其特征在于：选择具有良好生物相容性、生物活性的纳米磷酸钙为主体材料，通过离子、电荷相互作用对水飞蓟宾进行复合。
2.如权利要求1所述的一种纳米化水飞蓟宾磷酸钙复合微胶囊的制备方法，其特征在于：具体的制备方法为：配制浓度为5600ug/mL的水飞蓟宾，取配制好的水飞蓟宾溶液5mL，并加入5mg纳米级无定型磷酸钙(ACP)，超声20分钟，于摇床中在160r/min的转速、37℃的温度下摇匀，在加入纳米磷酸钙后10min，水飞蓟宾的装载量达到最大值，纳米化水飞蓟宾磷酸钙复合微胶囊制备成功。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410614641.6A CN104398490A (zh) | 2014-11-04 | 2014-11-04 | 一种纳米化水飞蓟宾磷酸钙复合微胶囊的制备方法 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410614641.6A CN104398490A (zh) | 2014-11-04 | 2014-11-04 | 一种纳米化水飞蓟宾磷酸钙复合微胶囊的制备方法 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104398490A true CN104398490A (zh) | 2015-03-11 |
Family
ID=52636202
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410614641.6A Pending CN104398490A (zh) | 2014-11-04 | 2014-11-04 | 一种纳米化水飞蓟宾磷酸钙复合微胶囊的制备方法 |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN104398490A (zh) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101557720A (zh) * | 2006-12-12 | 2009-10-14 | 弗门尼舍有限公司 | 具有无定形金属盐作为载体的活性成分递送系统 |
| CN102657598A (zh) * | 2012-05-09 | 2012-09-12 | 上海交通大学 | 一种基于多孔无机材料二次分散难溶性药物的口服制剂及其制备方法 |
| AU2014100743A4 (en) * | 2014-02-25 | 2014-07-24 | Macau University Of Science And Technology | A Pickering Emulsion Comprising Nano Crystals of Silybin and A Method of Preparation Thereof |
-
2014
- 2014-11-04 CN CN201410614641.6A patent/CN104398490A/zh active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101557720A (zh) * | 2006-12-12 | 2009-10-14 | 弗门尼舍有限公司 | 具有无定形金属盐作为载体的活性成分递送系统 |
| CN102657598A (zh) * | 2012-05-09 | 2012-09-12 | 上海交通大学 | 一种基于多孔无机材料二次分散难溶性药物的口服制剂及其制备方法 |
| AU2014100743A4 (en) * | 2014-02-25 | 2014-07-24 | Macau University Of Science And Technology | A Pickering Emulsion Comprising Nano Crystals of Silybin and A Method of Preparation Thereof |
Non-Patent Citations (1)
| Title |
|---|
| 柯玲玲，等: "水飞蓟宾生物粘附微球的制备", 《光谱实验室》 * |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Chan et al. | Encapsulation of herbal aqueous extract through absorption with ca-alginate hydrogel beads | |
| Jayachandran et al. | Green synthesized silver nanoparticle-loaded liposome-based nanoarchitectonics for cancer management: in vitro drug release analysis | |
| Luo et al. | Particle-stabilizing effects of flavonoids at the oil− water interface | |
| Xiao et al. | Synthesis, characterization, and evaluation of genistein-loaded zein/carboxymethyl chitosan nanoparticles with improved water dispersibility, enhanced antioxidant activity, and controlled release property | |
| Shen et al. | Cyclodextrin-metal-organic frameworks (CD-MOFs): main aspects and perspectives in food applications | |
| RU2017101992A (ru) | Очищенные терапевтические наночастицы и способы их получения | |
| Lukova et al. | Application of starch, cellulose, and their derivatives in the development of microparticle drug-delivery systems | |
| Zhao et al. | Effects of different drying methods on the characterization, dissolution rate and antioxidant activity of ursolic acid-loaded chitosan nanoparticles | |
| AbouAitah et al. | Nanomedicine as an emerging technology to foster application of essential oils to fight cancer | |
| Ferreira et al. | Flavonoids-based delivery systems towards cancer therapies | |
| Arriagada et al. | Nanoantioxidant–based silica particles as flavonoid carrier for drug delivery applications | |
| Prabhakar et al. | Macromolecular microencapsulation using pine pollen: Loading optimization and controlled release with natural materials | |
| Petchsomrit et al. | Alginate-based composite sponges as gastroretentive carriers for curcumin-loaded self-microemulsifying drug delivery systems | |
| EP2942061A3 (en) | Ige ch3 peptide vaccine | |
| Zhou et al. | The commonly used stabilizers for phytochemical-based nanoparticles: stabilization effects, mechanisms, and applications | |
| Coiai et al. | Rosmarinic acid and Ulvan from terrestrial and marine sources in anti-microbial bionanosystems and biomaterials | |
| Sanghi et al. | Herbal drugs an emerging tool for novel drug delivery systems | |
| CN107041874A (zh) | 一种岩藻黄素微胶囊及其制备工艺 | |
| Li et al. | The application of natural carotenoids in multiple fields and their encapsulation technology: A review | |
| Tong et al. | Extraction and nano-sized delivery systems for phlorotannins to improve its bioavailability and bioactivity | |
| Almukainzi et al. | Chitosan/hesperidin nanoparticles for sufficient, compatible, antioxidant, and antitumor drug delivery systems | |
| Saif et al. | Potential of CME@ ZIF-8 MOF nanoformulation: smart delivery of silymarin for enhanced performance and mechanism in albino rats | |
| Tornese et al. | Antiangiogenic potential of pomegranate extracts | |
| Kim et al. | Plant-derived nanoscale-encapsulated antioxidants for oral and topical uses: A brief review | |
| Ozsoysal et al. | Non-Traditional Natural Stabilizers in Drug Nanosuspensions |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20150311 |
|
| RJ01 | Rejection of invention patent application after publication |