Evaluation of molecular pharmaceutical and in-vivo properties of spray-dried isolated andrographolide-PVP
Evaluation of molecular pharmaceutical and in-vivo properties of spray-dried isolated andrographolide-PVP
复制标题
DOI：
10.1211/jpp/61.11.0005
复制
发表时间：
2009-11-01
影响因子：
3.3
通讯作者：
Pawar, Atmaram P.
中科院分区：
文献类型：
--
作者：
Bothiraja, C.;Shinde, Mukesh B.;Pawar, Atmaram P.
目的穿心莲内酯是一种天然的亲脂性分子，具有广泛的药理作用。然而，由于水溶性低，其口服生物利用度低。本研究的目的是增加的溶解度和溶解速率的分离穿心莲通过制定其固体dispersions.Method固体分散体，通过喷雾干燥技术，使用不同比例的药物聚乙烯吡咯烷酮（PVP K-30）获得。固体分散体的压缩与分离的药物和相应的物理混合物的特点是各种分子药物的性质和稳定性研究长达3 months.Key发现五倍增加饱和溶解度的穿心莲内酯具有较高的Q值（5分钟）在不同的溶出介质中，观察到固体分散体的t（5 min内的累积释放百分比）和较低的t值（75%）（75%w/w药物释放所需的时间）。这归因于药物与PVP K-30之间形成无定形性质和分子间氢键。稳定性研究表明，在3个月的时间内，分子药物特性和溶出曲线没有显著变化。此外，在Wistar白化病大鼠的体内研究也证明了提高穿心莲内酯的治疗效果后，固体dispersion.Conclusions本研究表明，利用固体分散体，以提高初级和二级药物性能的穿心莲内酯使用PVP K-30作为载体。
Objectives Andrographolide, a natural lipophilic molecule, has a wide range of pharmacological actions. However, due to low aqueous solubility, it has low oral bioavailability. The purpose of the study was to increase the solubility and dissolution rate of isolated andrographolide by formulating its solid dispersion.Method Solid dispersions were obtained by a spray-drying technique using different ratios of drug to polyvinylpyrrolidine (PVP K-30). Solid dispersions in compression with isolated drug and corresponding physical mixtures were characterized for various molecular pharmaceutical properties and subjected to stability study for up to 3 months.Key findings A five-fold increase in saturation solubility of andrographolide with higher values of Q(5min) (cumulative percentage release in 5 min) and lower values of t(75%) (time required for 75% w/w drug release) for solid dispersion was observed in different dissolution mediums. This was attributed to the formation of amorphous nature and intermolecular hydrogen bonding between drug and PVP K-30. The stability study showed there to be no significant change in molecular pharmaceutical properties and dissolution profile over the period of 3 months. Moreover, the in-vivo study in Wistar albino rats also justified improvement in the therapeutic efficacy of andrographolide after solid dispersion.Conclusions This study demonstrates the utility of solid dispersion to improve primary and secondary pharmaceutical properties of andrographolide using PVP K-30 as a carrier.