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 PDFInfo
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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
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。
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Cited By (1)
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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)
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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 |
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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)
Title |
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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)
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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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