Jiang Yan-Rong, Zhang Zhen-Hai, Huang Sai-Yan, Lu Yan, Ma Tian-Tian, Jia Xiao-Bin
Chinese Herb Preparation Room, Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China ; College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China.
Chinese Herb Preparation Room, Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China.
Pharmacogn Mag. 2014 Jul;10(39):332-7. doi: 10.4103/0973-1296.137375.
Tanshinone IIA (TSIIA) exhibits a variety of cardiovascular effects; however, it has low solubility in water. The preparation of poorly soluble drugs for oral delivery is one of the greatest challenges in the field of formulation research. Among the approaches available, solid dispersion (SD) technique has proven to be one of the most commonly used these methods for improving dissolution and bioavailability of drugs, because of its relative simplicity and economy in terms of both preparation and evaluation.
This study was aimed at investigating the dissolution behavior and physical stability of SDs of TSIIA by employing nano-hydroxyapatite (n-HAp).
The TSIIA SDs was prepared to use a spray-drying method. First, an in vitro dissolution test was performed to assess dissolution characteristics. Next, a set of complementary techniques (differential scanning calorimetry, scanning electron microscopy, X-ray powder diffraction, and Fourier transform infrared spectroscopy) was used to monitor the physicochemical properties of the SDs. The SDs was stored at 40°C/75% relative humidity for 6 months, after which their stability was assessed.
TSIIA dissolution remarkably improved because of the formulation of the SDs with n-HAp particles. Comparisons with the corresponding physical mixtures revealed changes in the SDs and explained the formation of the amorphous phase. In the stability test, virtually no time-dependent decrease was observed in either in vitro drug dissolution or drug content.
SD formulation with n-HAp may be a promising approach for enhancing the dissolution and stability of TSIIA.
丹参酮IIA（TSIIA）具有多种心血管效应；然而，其在水中的溶解度较低。制备用于口服给药的难溶性药物是制剂研究领域最大的挑战之一。在现有的方法中，固体分散体（SD）技术已被证明是提高药物溶出度和生物利用度最常用的方法之一，因为其在制备和评价方面相对简单且经济。
本研究旨在研究采用纳米羟基磷灰石（n-HAp）制备的TSIIA固体分散体的溶出行为和物理稳定性。
采用喷雾干燥法制备TSIIA固体分散体。首先，进行体外溶出试验以评估溶出特性。接下来，使用一组互补技术（差示扫描量热法、扫描电子显微镜、X射线粉末衍射和傅里叶变换红外光谱）监测固体分散体的物理化学性质。将固体分散体在40°C/75%相对湿度下储存6个月，之后评估其稳定性。
由于与n-HAp颗粒形成固体分散体，TSIIA的溶出度显著提高。与相应物理混合物的比较揭示了固体分散体的变化，并解释了无定形相的形成。在稳定性试验中，体外药物溶出度或药物含量几乎没有随时间下降。
用n-HAp制备固体分散体可能是提高TSIIA溶出度和稳定性的一种有前途的方法。
