Ibrahim Mohamed A, Zayed Gamal M, Alsharif Fahd M, Abdelhafez Wael A
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt.
Saudi Pharm J. 2019 Feb;27(2):182-190. doi: 10.1016/j.jsps.2018.10.002. Epub 2018 Oct 19.
In this study, we aimed to optimize theophylline pellet formulations using a two-factor three-level full-factorial design (3) by monitoring the concentration of two pellet excipients, polyvinyl pyrrolidone K30 (PVP) binder solution (X1) and the hydrophilic excipient mannitol (X2). Their impact on pellet characteristics (responses) were evaluated. Increasing PVP concentration in the binder solution resulted in an increase in the wet mass torque value. The effect of mannitol, however, was antagonistic. Moreover, the pellet particle size was significantly influenced by the level of mannitol, PVP solution, and quadratic effect of mannitol. Mannitol significantly antagonized the pellet particle size. Furthermore, increased mannitol concentrations significantly enhanced drug dissolution rate from the pellets, whereas PVP concentration in the binder solution significantly reduced the drug dissolution rate. In conclusion, wet granulations can be controlled by monitoring the composition of the binder solution and pellet composition.
在本研究中，我们旨在通过监测两种微丸辅料（聚乙烯吡咯烷酮K30（PVP）粘合剂溶液（X1）和亲水性辅料甘露醇（X2））的浓度，采用二因素三水平全因子设计（3）来优化茶碱微丸制剂。评估了它们对微丸特性（响应）的影响。粘合剂溶液中PVP浓度的增加导致湿质量扭矩值增加。然而，甘露醇的影响是拮抗的。此外，微丸粒径受甘露醇水平、PVP溶液以及甘露醇的二次效应显著影响。甘露醇显著拮抗微丸粒径。此外，甘露醇浓度的增加显著提高了微丸的药物溶出速率，而粘合剂溶液中PVP浓度则显著降低了药物溶出速率。总之，通过监测粘合剂溶液的组成和微丸组成可以控制湿法制粒。
