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基于聚乙烯吡咯烷酮(PVP)纳米分散体的药物传递系统对黄烷酮苷元、柚皮素和橙皮苷的溶出速率和稳定性研究。

Dissolution rate and stability study of flavanone aglycones, naringenin and hesperetin, by drug delivery systems based on polyvinylpyrrolidone (PVP) nanodispersions.

机构信息

Department of Pharmaceutics and Drug Control, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, Greece.

出版信息

Drug Dev Ind Pharm. 2010 Mar;36(3):292-301. doi: 10.1080/03639040903140589.

DOI:10.1080/03639040903140589
PMID:19663560
Abstract

OBJECTIVE

To study the dissolution behavior, the release mechanism and the stability of nanodispersion system of aglycones with PVP.

METHODS

The nanodispersion system of polyvinylpyrrolidone (PVP)/naringenin-hesperetin was prepared using the solvent evaporation method. The chemical stability (compatibility) of naringenin and hesperetin in the prepared dispersions was studied under accelerated conditions for 3 months. The evaluation of physical stability was performed by X-ray diffraction analysis (XRD) and by comparing the dissolution profile before and after storage at high temperature and moisture (40 masculineC, RH 75%).

RESULTS

The dissolution rate of naringenin and hesperetin released was dramatically increased in the nanodispersion system of PVP/naringenin-hesperetin (80/20, w/w). The release mechanism of both flavanone aglycones was better described by the diffusion model (Higuchi model). Also it was found that the rate-limiting step that controlled the release of naringenin and hesperetin in the nanodispersion system was dissolution of the carrier (PVP).

CONCLUSIONS

During accelerated degradation analysis, for 3 months at high temperature and moisture, PVP nanodispersion system showed enhanced chemical compatibility and physical stability. The physical evaluation (obtained from XRD analysis) of PVP/naringenin-hesperetin (80/20, w/w) in the selected storage conditions did not show any crystallization of flavanone aglycones in the PVP nanodispersion system or any change in their release profile.

摘要

目的

研究与 PVP 形成的苷元纳米分散体的溶出行为、释放机制和稳定性。

方法

采用溶剂蒸发法制备聚维酮(PVP)/柚皮素-橙皮素纳米分散体。在加速条件下研究 3 个月,研究制备分散体中柚皮素和橙皮素的化学稳定性(相容性)。通过 X 射线衍射分析(XRD)和比较高温高湿(40°C,RH75%)储存前后的溶出曲线来评估物理稳定性。

结果

PVP/柚皮素-橙皮素(80/20,w/w)纳米分散体显著提高了柚皮素和橙皮素的溶出速率。两种黄烷酮苷元的释放机制均较好地用扩散模型(Higuchi 模型)描述。还发现,控制纳米分散体中柚皮素和橙皮素释放的速度限制步骤是载体(PVP)的溶解。

结论

在高温高湿加速降解分析中,3 个月后,PVP 纳米分散体显示出增强的化学相容性和物理稳定性。在所选储存条件下,对 PVP/柚皮素-橙皮素(80/20,w/w)的物理评价(XRD 分析获得)并未显示出 PVP 纳米分散体中黄烷酮苷元结晶或其释放曲线有任何变化。

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