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羟丙甲纤维素稳定的萘普生纳米混悬剂的处方前研究及工艺优化。

Formulation and process optimization of naproxen nanosuspensions stabilized by hydroxy propyl methyl cellulose.

机构信息

Gayatri College of Pharmacy, Sambalpur, Odisha 768200, India.

Shri Ram Murti Smarak College of Engg. and Technology (Pharmacy), Bareilly, U.P. 243202, India.

出版信息

Carbohydr Polym. 2015 Aug 20;127:300-8. doi: 10.1016/j.carbpol.2015.03.077. Epub 2015 Apr 1.

DOI:10.1016/j.carbpol.2015.03.077
PMID:25965487
Abstract

In present study precipitation-ultrasonication was used to obtain nanosuspensions of poorly water-soluble drug, naproxen (NPX). We investigated the effects of HPMC concentration (X1) and time of ultrasonication (X2) on imperative attributes like mean particle size (Y1), % drug content (Y2), and time required to 90% drug release (Y3) via 3(2) factorial design. The morphology of nanosuspensions was found almost spherical by SEM observation. DSC and XRD studies suggested slight crystalline change in drug. FT-IR revealed lack of significant interactions between NPX and HPMC. Nanosuspensions of mean particle size 530.55 nm was achieved. Dissolution rate obtained from all nanosuspensions were markedly higher than pure NPX. Response surface methodology and optimized polynomial equations were used to select optimal formulation i.e. 1.36%W/V of X1 and 13.9 min of X2 to get desired response Y1; 727.97 nm, Y2; 95.59% and Y3; 8.67 min that were in reasonable agreement with observed value.

摘要

在本研究中,采用沉淀-超声法制备难溶性药物萘普生(NPX)的纳米混悬剂。通过 3(2) 因子设计,考察了 HPMC 浓度(X1)和超声时间(X2)对重要属性的影响,如平均粒径(Y1)、药物含量(Y2)和 90%药物释放所需时间(Y3)。通过 SEM 观察发现,纳米混悬剂的形态几乎呈球形。DSC 和 XRD 研究表明,药物的结晶性略有变化。FT-IR 表明 NPX 和 HPMC 之间没有明显的相互作用。获得了平均粒径为 530.55nm 的纳米混悬剂。所有纳米混悬剂的溶出速率均明显高于纯 NPX。响应面法和优化多项式方程用于选择最佳配方,即 X1 为 1.36%W/V 和 X2 为 13.9min,以获得所需的响应 Y1:727.97nm、Y2:95.59%和 Y3:8.67min,与观察值吻合良好。

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