Valsartan has been used for the treatment of hypertension disease. However, the oral bioavailability of valsartan has been reported to be only ∼23%, accompanied with high permeability and poor aqueous solubility. The object of this research was to prepare solid dispersions of valsartan with an inorganic (CaCO₃) and organic base (N-methyl-d-glucamine) in an effort to increase the aqueous solubility and dissolution rate of the drug. The as-prepared solid dispersions of valsartan were prepared in an environmentally friendly manner using CaCO₃ and MG and a roll mill. The physicochemical properties were studied in the solid state using DSC, PXRD and IR. Furthermore, the solubility of valsartan increased 46-fold in solid dispersion with CaCO₃ and 9-fold in solid dispersion with MG. More than 95% of valsartan in solid dispersions was found to be released in simulated intestinal fluid, whereas only 35% was found to be released using pure valsartan within the same time interval. Storage tests showed that the as-prepared solid dispersions were equally stable compared to pure valsartan at 40 °C. Potentially, the synthesized solid dispersions of valsartan with enhanced solubility and dissolution rates may represent promising formulations for improving the overall oral bioavailability of the drug in clinical applications.

缬沙坦已用于治疗高血压疾病。然而，据报道缬沙坦的口服生物利用度仅为23％左右，同时具有高渗透性和较差的水溶性。这项研究的目的是用无机碳酸钙（CaCO制备缬沙坦的固体分散体₃）和有机碱（Ñ甲基d，努力提高药物的水溶解度和溶出速率-glucamine）。使用CaCO ₃以环保的方式制备制得的缬沙坦固体分散体还有MG和轧机。使用DSC，PXRD和IR在固态下研究了理化性质。此外，缬沙坦的溶解度在使用CaCO _3的固体分散体中增加了46倍，在使用MG的固体分散体中增加了9倍。固体分散体中超过95％的缬沙坦被发现在模拟肠液中释放，而在同一时间间隔内使用纯缬沙坦仅释放了35％。储存测试表明，与纯缬沙坦相比，所制备的固体分散体在40°C下同样稳定。潜在地，具有增强的溶解度和溶解速率的合成的缬沙坦固体分散体可以代表在临床应用中用于改善药物的总体口服生物利用度的有前途的制剂。