Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China; Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China; Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
Fitoterapia. 2018 Sep;129:85-93. doi: 10.1016/j.fitote.2018.06.018. Epub 2018 Jun 21.
Baicalein (BE) is a flavonoid compound derived from the roots of Scutellaria baicalensis. It has widely been used as anti-oxidant, anti-virus, anti-bacteria, anti-inflammatory and anti-allergic therapies. Due to its poor water solubility (16.82 μg/ml), the therapeutic effectiveness and oral bioavailability of Baicalein are highly limited. The purpose of this study was to investigate the possibility of baicalein-theophylline (BE-TH) cocrystals to achieve the simultaneous enhancement in dissolution and oral bioavailability of BE. The cocrystal had the new characteristic of scanning electron microscopy, differential scanning calorimetry thermograms and X-ray powder diffraction. Compared with coarse powder of BE, BE-TH cocrystals had significantly improved the solubility of BE. The dissolution test showed that the BE-TH cocrystals demonstrated 2.2-fold and 7.1-fold higher rate of dissolution than that of BE coarse powder in HCl (pH = 1.2) and phosphate buffer (PBS, pH = 6.8), respectively. Moreover, the cocrystals exhibited a 5.86-fold higher area under the curve in rats after the oral administration. This investigation enriched the present understanding of cocrystals on their behavior in vitro and in vivo, and built the groundwork for future development of BE as a promising compound into efficacious drug products.
黄芩素 (BE) 是一种黄酮类化合物，来源于黄芩的根。它被广泛用作抗氧化剂、抗病毒、抗菌、抗炎和抗过敏治疗。由于其水溶性差（16.82μg/ml），黄芩素的治疗效果和口服生物利用度受到极大限制。本研究旨在探讨黄芩素-茶碱（BE-TH）共晶提高 BE 溶解和口服生物利用度的可能性。该共晶具有扫描电子显微镜、差示扫描量热法图谱和 X 射线粉末衍射的新特征。与 BE 粗粉相比，BE-TH 共晶显著提高了 BE 的溶解度。溶出度试验表明，BE-TH 共晶在盐酸（pH=1.2）和磷酸盐缓冲液（pH=6.8）中的溶解速度分别比 BE 粗粉高 2.2 倍和 7.1 倍。此外，共晶在大鼠体内的曲线下面积提高了 5.86 倍。该研究丰富了共晶在体外和体内行为的现有认识，为未来将 BE 开发成一种有前途的化合物作为有效药物奠定了基础。
