Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune, Maharashtra, India.
J Pharm Pharmacol. 2009 Nov;61(11):1465-72. doi: 10.1211/jpp/61.11.0005.
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.
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.
A five-fold increase in saturation solubility of andrographolide with higher values of Q(5 min) (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.
This study demonstrates the utility of solid dispersion to improve primary and secondary pharmaceutical properties of andrographolide using PVP K-30 as a carrier.
穿心莲内酯是一种天然亲脂性分子，具有广泛的药理作用。然而，由于其水溶性低，口服生物利用度低。本研究旨在通过制备其固体分散体来提高分离穿心莲内酯的溶解度和溶解速率。
采用喷雾干燥技术，以不同比例的药物与聚乙烯吡咯烷酮（PVP K-30）制备固体分散体。对含有分离药物的固体分散体和相应的物理混合物进行各种分子药物特性的表征，并进行长达 3 个月的稳定性研究。
在不同的溶解介质中，穿心莲内酯的饱和溶解度增加了五倍，Q（5 分钟）（5 分钟内累积释放的百分比）更高，t（75%）（释放 75%w/w 药物所需的时间）更低，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，分子药物特性和溶解曲线没有明显变化。此外，在 Wistar 白化大鼠体内研究中，也证明了固体分散体改善穿心莲内酯治疗效果的作用。
本研究表明，使用 PVP K-30 作为载体，固体分散体可提高穿心莲内酯的主要和次要药物特性。
