CN108125936A - 一种辅酶q10纳米制剂的制备及应用 - Google Patents

一种辅酶q10纳米制剂的制备及应用 Download PDF

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CN108125936A
CN108125936A CN201810009640.7A CN201810009640A CN108125936A CN 108125936 A CN108125936 A CN 108125936A CN 201810009640 A CN201810009640 A CN 201810009640A CN 108125936 A CN108125936 A CN 108125936A
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ubiquinone
nanometer formulation
preparation
application
suspension
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罗猛
牟璠松
杨璇
阮鑫
邢文淼
陈民
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Northeast Forestry University
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Northeast Forestry University
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/12—Ketones
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
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    • A61K9/513—Organic macromolecular compounds; Dendrimers
    • A61K9/5161—Polysaccharides, e.g. alginate, chitosan, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51—Nanocapsules; Nanoparticles
    • A61K9/5192—Processes

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Abstract

本发明涉及药物制剂领域，具体涉及叶酸‑葡聚糖‑辅酶Q10纳米制剂的制备及应用。本发明所制备的纳米制剂具有良好的稳定性和生物利用度，且制备工艺简单，易于生产，有广阔的产业化前景。

Description

一种辅酶Q10纳米制剂的制备及应用
技术领域
本发明涉及一种辅酶Q10纳米制剂的制备及应用，具体涉及叶酸-葡聚糖-辅酶Q10纳米制剂的制备及应用，属于药物制剂领域。
背景技术
辅酶Q10又称泛醌，是脂溶性醌类化合物，广泛存在于生物界。它可以在人体细胞中自行合成，也可以从天然食物中获取。辅酶Q10具有促进氧化磷酸化反应以及保护生物膜结构完整性等功能。它在人体的呼吸链和电子传递过程中具有极其重要的作用，也是重要的抗氧化剂，具有广泛的药理活性。研究表明，辅酶Q10可治疗心脑血管疾病、糖尿病、动脉硬化等疾病。同时，其还广泛用于保健品和化妆品领域。不过辅酶Q10分子量大以及水溶性非常差，在肠道中的吸收很慢，造成其生物利用度较低，限制了其应用范围。因此，通过制剂手段有效地提高辅酶Q10生物利用度已成为近年来研究的热点。本文制备纳米制剂采用的方法是通过加入表面活性剂，并使用特殊设备将难溶性药物制备成纳米级粒子，可显著提高药物的口服生物利用度。
本文所制备的叶酸-葡聚糖-辅酶Q10纳米制剂，不仅能增强辅酶Q10的稳定性，而且能提高其生物利用度，该制备方法适合工业化生产。
发明内容
本发明的目的在于制备一种辅酶Q10纳米制剂。
为实现上述目的，本发明采用以下技术方案：本发明中将辅酶Q10与叶酸葡聚糖偶联物以1:1-1:9的质量比混合，再加入卵磷脂，其与辅酶Q10的的质量比为0.1:1-0.4:1，将混合物加入水中，固液比为1:4(g/mL)充分搅拌后，经过高速匀浆机匀浆(10000rpm，2min)形成初混悬剂。将制备好的初混悬剂在500-1000bar均质压力下循环3-10次，制备成辅酶Q10纳米混悬剂，冷冻干燥24h，得到辅酶Q10纳米制剂。
本发明的优点：
(1)本发明所制备的纳米制剂具有良好的稳定性和生物利用度。
(2)本发明制备工艺简单，易于生产，有广阔的产业化前景。
附图说明
附图1辅酶Q10原药和纳米制剂的红外图谱
附图2辅酶Q10原药和纳米制剂的XRD图谱
附图3辅酶Q10原药和纳米制剂的DSC图谱
附图4辅酶Q10原药和纳米制剂的平均血药浓度
具体实施方案
实施例1：
称取辅酶Q10 30mg，叶酸葡聚糖偶联物30mg，以及稳定剂5mg，将混合物加入到120mL 水中充分搅拌后，经过高速匀浆机匀浆(10000rpm，2min)形成初混悬剂。将制备好的初混悬剂在800bar均质压力下循环7次，制备成辅酶Q10纳米混悬剂，冷冻干燥24h，得到辅酶Q10纳米制剂。
经过0-6个月存储，平均粒径均小于200nm，稳定性良好。
取禁食的Wistar雄性大鼠随机12只分为一组，共两组。分别将原药和纳米制剂按CoQ10 60mg/kg的剂量给予大鼠灌胃处理，每个时间点12只大鼠，给药0.5，1，2，4，8，12，24h后分别取血，置于肝素抗凝管中，离心分离处理后测样。纳米制剂生物利用度是原药的2倍。

Claims (4)

1.一种辅酶Q10纳米制剂的制备及应用，其特征在于：将叶酸-葡聚糖-辅酶Q10和稳定剂溶于水中，固液比为1:4(g/mL)充分混合后，经过高速匀浆机匀浆(10000rpm，2min)后形成初混悬剂，将制备好的初混悬剂在一定的均质压力下循环数次，制备成辅酶Q10纳米混悬剂，冷冻干燥24h，得到辅酶Q10纳米制剂。
2.根据权利要求1所述的一种辅酶Q10纳米制剂的制备及应用，其特征在于：所述的辅酶Q10与叶酸葡聚糖偶联物的质量比为1:1-1:9。
3.根据权利要求1所述的一种辅酶Q10纳米制剂的制备及应用，其特征在于：所述的稳定剂为卵磷脂、α-环糊精、β-环糊精、γ-环糊精、羟丙甲纤维素的一种或几种的组合，稳定剂与辅酶Q10的质量比为0.1:1-0.4:1。
4.根据权利要求1所述的一种辅酶Q10纳米制剂的制备及应用，其特征在于：所述的均质压力为500-1000bar，循环次数为3-10次。
CN201810009640.7A 2018-01-05 2018-01-05 一种辅酶q10纳米制剂的制备及应用 Pending CN108125936A (zh)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109674749A (zh) * 2019-01-07 2019-04-26 东北林业大学 一种高含量辅酶q10口服纳米混悬剂及其制备工艺

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102293753A (zh) * 2010-06-25 2011-12-28 沈阳药科大学 辅酶q10纳米混悬剂冻干组合物及其制备方法和应用

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102293753A (zh) * 2010-06-25 2011-12-28 沈阳药科大学 辅酶q10纳米混悬剂冻干组合物及其制备方法和应用

Non-Patent Citations (1)

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王建萍: "主动靶向叶酸葡聚糖纳米给药系统的研究", 《临床医学工程》 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109674749A (zh) * 2019-01-07 2019-04-26 东北林业大学 一种高含量辅酶q10口服纳米混悬剂及其制备工艺

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