Studies On Arbidol Hydrochloride Freeze-dried Powder Injection

Arbidol(ARB) is an antiviral compound that was originally proven effective for treatment of influenza and several other respiratory viral infections. Its oral bioavailability was very low. Because it is a poorly soluble water drug, there is no injectable preparation to be launched until now. The present work is to study the solubilization of ARB/HP-β-CD as a compound and prepare ARB/HP-β-CD injectable freeze-dried power. The following research work was done:ARB/HP-β-CD as a compound was prepared, and the solubility of the complex was also investigated. The surfactant, which were used commonly in intravenous administration, such as Tween-80, Poloxamer188 and Cremophoe EL were used to determine the effect of solubilization. The influences of temperature and pH values on the formulation of the complex were also evaluated. The results showed that HP-β-CD could significantly improve the solubility of ARB, and poloxamer188 could also significantly improve the solubility of ARB, and if it was used as an aided solubilizing agent before the process of complex, the amount was about 1.0%(w/v). The solubility of the complex was increased with increasing the temperature, and the more suitable temperature for the complex was about 50°C. Under the different pH values, the solubility of ARB was linear increased with the increasing the consistency of the HP-β-CD. It was assessed that the corresponding inclusion complex of HP-β-CD at the molar ratio of 1:1 was obtained, and its solubility was significantly improved under the pH values from 4.0 to 5.0. ARB/HP-β-CD as a compound could significantly improve the solubility of ARB, and satisfy the requirements of the injectable freeze-dried power.ARB freeze-dried power injection was prepared. The freeze-dried preparation of the complex was also assessed by detecting the eutectic point using electric resistance method. The formation of ARB/HP-β-CD complex was evaluated using Thermo Gravimetric Analysis (TGA) and Infrared Analysis (IR) method. The results indicated that the eutectic point of the freeze-dried product was -21°C, and white freeze-dried power with rarefaction was achieved without adding other aided freeze drying agent. The results of TGA and IR showed that no other characteristic absorption peak was detected, ARB/HP-β-CD complex was perfect. Arbidol hydrochloride; HP-β-CD; Complex; Freeze-dried injection; Stability...