Department of Pharmaceutics and Industrial Pharmacy, Al-Azhar University, Assiut, Egypt.
Al-Azhar Centre of Nanosciences and Applications, Al-Azhar University, Assiut, Egypt.
Drug Dev Ind Pharm. 2019 Dec;45(12):1973-1981. doi: 10.1080/03639045.2019.1689993. Epub 2019 Nov 13.
The main objective of this study is to increase the dissolution rate of gliquidone using its solid dispersions with pluronic F-68 by solvent evaporation method. The solid dispersion of the drug with pluronic at ratio 1:3 showed the highest dissolution efficiency (50.7%) after 10 min, so it was incorporated in fast dissolving tablets. Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) were used to study the interaction between gliquidone and pluronic in the solid state. The FTIR spectroscopic studies revealed no chemical interaction between the drug and pluronic, while the DSC results indicated the amorphous state of gliquidone in the solid dispersion. A 3 full factorial design was used to study the effect of varying concentrations of croscarmellose and sodium starch glycolate as superdisintegrants on the disintegration time and the percentage released after 10 min. The optimized formula showed a disintegration time of 39.1 ± 1.2 s and 85.43% ± 5.16% released after 10 min and was selected for the studies in rabbits. The selected formula showed significant enhancement of gliquidone bioavailability, about 1.8 times compared with the commercial Glurenor tablets.
本研究的主要目的是通过溶剂蒸发法提高格列喹酮与聚氧乙烯醚 F-68 的固体分散体的溶出速率。药物与聚氧乙烯醚以 1:3 的比例形成的固体分散体在 10 分钟后显示出最高的溶解效率(50.7%),因此将其纳入速溶片中。傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)用于研究药物与聚氧乙烯醚在固态下的相互作用。FTIR 光谱研究表明药物与聚氧乙烯醚之间没有化学相互作用,而 DSC 结果表明格列喹酮在固体分散体中处于无定形状态。采用 3 因素完全析因设计研究了不同浓度的交联羧甲基纤维素钠和交联聚维酮作为超分散剂对崩解时间和 10 分钟后释放百分比的影响。优化的配方显示崩解时间为 39.1±1.2s,10 分钟后释放 85.43%±5.16%,并选择用于兔体内研究。所选配方显著提高了格列喹酮的生物利用度,与 Glurenor 市售片剂相比约提高 1.8 倍。