Benjasirimongkol Pontip, Piriyaprasarth Suchada, Sriamornsak Pornsak
Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, 73000, Thailand.
Pharmaceutical Biopolymer Group (PBiG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, 73000, Thailand.
Heliyon. 2019 Mar 27;5(3):e01399. doi: 10.1016/j.heliyon.2019.e01399. eCollection 2019 Mar.
In this study, resveratrol (RVT) was loaded onto porous calcium silicate (PCS) powders to improve its dissolution and photostability properties. The effects of RVT/PCS powders that included varying amounts of low-methoxyl pectin (LMP), ethyl acetate (EA) and PCS on drug loading capacity, encapsulation efficiency and drug dissolution at 5-min intervals (Q) were investigated using a Box-Behnken design. The experimental results demonstrated that the EA and PCS amounts significantly influenced drug loading capacity. Encapsulation efficiency was affected by EA amount, whereas the amount of PCS had a significant effect on Q. Empirical experiments demonstrated the reliability of mathematical models. A design space was established based on the criteria set for maximizing each response of the RVT/PCS powders. An optimized formulation containing 2.6% w/w LMP, 19% w/w EA and 13% w/w PCS prepared within the design space satisfied all criteria. The dissolution and photostability of RVT in the RVT/PCS powders were significantly improved. Further, the bulk density of the PCS powders in RVT/PCS was increased by LMP. The Box-Behnken design used in this study provided an improved understanding of the effects of formulation factors on RVT/PCS powder characteristics as well as the optimization of RVT/PCS powder formulations with the desired properties
在本研究中，白藜芦醇（RVT）被负载到多孔硅酸钙（PCS）粉末上，以改善其溶解性能和光稳定性。采用Box-Behnken设计研究了不同含量的低甲氧基果胶（LMP）、乙酸乙酯（EA）和PCS的RVT/PCS粉末对载药量、包封率以及每隔5分钟的药物溶出度（Q）的影响。实验结果表明，EA和PCS的用量对载药量有显著影响。包封率受EA用量的影响，而PCS的用量对Q有显著影响。经验实验证明了数学模型的可靠性。根据为使RVT/PCS粉末的各响应最大化而设定的标准建立了设计空间。在设计空间内制备的含有2.6% w/w LMP、19% w/w EA和13% w/w PCS的优化配方满足所有标准。RVT在RVT/PCS粉末中的溶解性能和光稳定性得到显著改善。此外，LMP提高了RVT/PCS中PCS粉末的堆密度。本研究中使用的Box-Behnken设计有助于更好地理解配方因素对RVT/PCS粉末特性的影响，以及对具有所需性能的RVT/PCS粉末配方进行优化。
