Preparation and  Pharmacokinetics in Rats of Nimodipine Nanostructured Lipid Carries

WANG Hong-yuan; LIU Qiang; ZHANG Yun-jie; WANG Ying; ZHOU Min jing; YANG Chun-rong

doi:10.11653/syfj2013160178

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Preparation and Pharmacokinetics in Rats of Nimodipine Nanostructured Lipid Carries

更新时间：2024-01-04

- Preparation and Pharmacokinetics in Rats of Nimodipine Nanostructured Lipid Carries
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 19, Issue 16, Pages: 178-182(2013)
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- DOI：10.11653/syfj2013160178
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- Published：2013
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WANG Hong-yuan, LIU Qiang, ZHANG Yun-jie, et al. Preparation and Pharmacokinetics in Rats of Nimodipine Nanostructured Lipid Carries[J]. Chinese journal of experimental traditional medical formulae, 2013, 19(16): 178-182.
DOI：

WANG Hong-yuan, LIU Qiang, ZHANG Yun-jie, et al. Preparation and Pharmacokinetics in Rats of Nimodipine Nanostructured Lipid Carries[J]. Chinese journal of experimental traditional medical formulae, 2013, 19(16): 178-182. DOI： 10.11653/syfj2013160178.

摘要

目的: 制备尼莫地平纳米结构脂质载体

考察其性质及大鼠体内药代动力学。方法: 采用熔融-超声法制备经甲氧基聚乙二醇磷脂酰乙醇胺修饰的尼莫地平纳米结构脂质载体(mPEG2000-DSPE-NMD-NLC)

通过透射电镜观察形态

测定粒径、包封率、载药量和Zeta电位

考察体外释药特性。采用HPLC测定不同时间点大鼠血浆中尼莫地平质量浓度

以尼莫地平注射液为对照

计算mPEG2000-DSPE-NMD-NLC在大鼠体内的药代动力学参数。结果: 制备的mPEG2000-DSPE-NMD-NLC形态呈类球形

大小均匀

表面圆整;粒径约85 nm

Zeta电位(-12.77±0.15) mV

包封率和载药量分别为(97.66±0.45)%

(1.46±0.05)%;在0~6 h累计释放率20.03%

24 h则为43.06%;药代动力学参数为t1/2=21.65 h

MRT=21.09 h

CL=557.30 mL·h-1·kg-1

AUC(0-t)=6 411.96 μg·h2·L-1。结论: mPEG2000-DSPE-NMD-NLC的粒径分布均匀

体内外缓释效果明显

体内循环时间明显延长

为改善尼莫地平的临床疗效提供参考。

Abstract

Objective: To prepare nanostructured lipid carriers modified with mPEG2000-DSPE(mPEG2000-DSPE-NMD-NLC) and investigate its properties and in vivo pharmacokinetics in rats. Method: mPEG2000-DSPE-NMD-NLC were prepared by melt ultrasonication method

morphology was observed by TEM

particle size

entrapment efficiency

drug loading and Zeta potential were determined

in vitro release was examined.Plasma concentrations of nimodipine at different time point in rats were determined by HPLC

with nimodipine injection as control

pharmacokinetics parameters of mPEG2000-DSPE-NMD-NLC in rats were calculated. Result: Prepared mPEG2000-DSPE-NMD-NLC showed spherical with uniform size and rounded surface;Particle size was about 85 nm

Zeta potential was (-12.77±0.15) mV

entrapment efficiency and drug loading were (97.66±0.45)% and (3.36±1.53)%

respectively;Cumulative release of mPEG2000-DSPE-NMD-NLC was 20.03% within 0-6 h

and 43.06% at 24 h.Pharmacokinetic parameters were as follows:t1/2=21.65 h

MRT=21.09 h

CL=557.30 mL·h-1·kg-1

AUC(0-t)=6 411.96 μg·h2·L-1. Conclusion: Particle size distribution of mPEG2000-DSPE-NMD-NLC was uniform

its showed obvious in vitro and in vivo sustained-release characteristic.This study could lay foundation for improving clinical efficacy of nimodipine.

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Related Institution

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