Zhou MiaoMiao, Wang YouJie, Wu Fei, Shen Lan, Lin Xiao, Feng Yi
College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine Shanghai 201203 PR China
Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine Shanghai 201203 PR China +86 21 51322429 +86 21 51322429.
RSC Adv. 2018 Jul 4;8(43):24250-24260. doi: 10.1039/c8ra04125c. eCollection 2018 Jul 2.
Herein, we report a study on the influence of particles having different porosities on tablet performance. The ethanol extract of Radix (EPL) was chosen as the model drug. A series of porous EPL particles were prepared by co-spray drying EPL with different amounts of ammonium bicarbonate (NHHCO), and their powder properties (particle morphology, particle size, porosity, flowability, bulk density, and tap density) and tablet properties (tensile strength, , yield pressure, dissolution, ) were comparatively investigated. The results showed that there were significant differences in the fundamental and functional properties of the spray-dried and parent EPLs. First, the irregular and dense primary EPL particles were transformed into loose, hollow, and spheroidal particles co-spray drying with NHHCO. Second, compared to parent EPL, porous EPLs showed a significant improvement (1.80-7.03 times) in compactibility. Third, the dissolution rates of porous EPLs were similar, and all were more than twice as fast as that of parent EPL. The increased porosity, on the one hand, led to the increase in interparticle and intraparticle bonding forces during tableting and, on the other hand, facilitated water intrusion into tablets for disintegration and dissolution. Porous particle design is therefore promising, especially for drugs with both poor compactibility and dissolution.
在此，我们报告一项关于具有不同孔隙率的颗粒对片剂性能影响的研究。选取了黄芪乙醇提取物（EPL）作为模型药物。通过将EPL与不同量的碳酸氢铵（NH₄HCO₃）共喷雾干燥制备了一系列多孔EPL颗粒，并对其粉末性质（颗粒形态、粒径、孔隙率、流动性、堆密度和振实密度）和片剂性质（拉伸强度、 、屈服压力、溶出度）进行了比较研究。结果表明，喷雾干燥的EPL与母体EPL在基本性质和功能性质方面存在显著差异。首先，通过与NH₄HCO₃共喷雾干燥，不规则且致密的初级EPL颗粒转变为松散、中空的球形颗粒。其次，与母体EPL相比，多孔EPL在可压性方面有显著提高（1.80 - 7.03倍）。第三，多孔EPL的溶出速率相似，且均比母体EPL快两倍以上。孔隙率的增加一方面导致压片过程中颗粒间和颗粒内结合力增加，另一方面促进水侵入片剂以实现崩解和溶解。因此，多孔颗粒设计具有前景，特别是对于可压性和溶出度均较差的药物。
