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采用纳米混悬技术制备化学稳定性良好的槲皮素制剂。

Preparation of a chemically stable quercetin formulation using nanosuspension technology.

机构信息

Department of Pharmacy, The First Affiliated Hospital of General Hospital of PLA, No 51 Fucheng Road, Beijing 100048, China. business

出版信息

Int J Pharm. 2011 Feb 14;404(1-2):231-7. doi: 10.1016/j.ijpharm.2010.11.009. Epub 2010 Nov 17.

Abstract

In the present study the evaporative precipitation into aqueous solution (EPAS) process and the high homogenization press (HPH) process were compared to evaluate their feasibility to form a chemically stable quercetin nanosuspension. The particle size and Zeta potential of the EPAS nanosuspension were similar to those of the HPH nanosuspension. Differences in results of differential scanning calorimetery and X-ray measures were observed between the two processes. The crystalline-to-amorphous phase transition was shown in the profile of EPAS dried powder. On the contrary the initial crystalline state of drug was maintained throughout the HPH process. Dissolution test results indicated that the EPAS process showed a higher improvement in the drug solubility and dissolution rate than the HPH process. At last the high performance liquid chromatography (HPLC) analysis proved the superiority of both nanosuspensions over QCT solution formulation for the chemical and photo-stability. As a result, it can be concluded that the EPAS and HPH techniques were feasible to prepare a chemically stable QCT nanosuspension with significantly enhanced dissolution rate.

摘要

在本研究中,比较了蒸发沉淀成水溶液(EPAS)工艺和高均化压力(HPH)工艺,以评估它们形成化学稳定槲皮素纳米混悬液的可行性。EPAS 纳米混悬液的粒径和 Zeta 电位与 HPH 纳米混悬液相似。两种工艺的差示扫描量热法和 X 射线测量结果存在差异。EPAS 干燥粉末的图谱显示出结晶-无定形相转变。相反,在 HPH 过程中,药物保持初始结晶状态。溶出试验结果表明,EPAS 工艺在提高药物溶解度和溶出速率方面优于 HPH 工艺。最后,高效液相色谱(HPLC)分析证明,两种纳米混悬剂在化学和光稳定性方面均优于 QCT 溶液制剂。因此,可以得出结论,EPAS 和 HPH 技术可用于制备化学稳定的 QCT 纳米混悬液,显著提高溶出速率。

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