Preparation And Evaluation Of Aidi Lyophilized Powder For Injection

Objective: To prepare Aidi lyophilized powder for injection and evaluate its pharmaceutical properties, safety and pharmacokinetic characteristics.Methods: (1) An HPLC method was established for determination of ginsenoside Rg1, Re, Rb1, Syringin and Astragaloside-Ⅳ, a visible spectrophotometry was used for determination of Astrganoside and Ginsenoside. (2) The isolation and purification process of ATGs, Astrganoside and Ginsenoside by foramen magnu absorption rein were studied. (3) The formulation and preparing process of Aidi lyophilized powder for injection were optimized. (4) The safety of the Aidi lyophilized powder was assessed by the experiments of hypersensitiveness, haemolyticus and stimulation. (5) The concentration of ginsenoside Rg1, Re and Astragaloside-Ⅳin rat plasma was determined by LS-MS/MS with digoxin as an internal standard, and the preliminary pharmacokinetic study of Aidi lyophilized powder was carried out in rats after intravenous administration.Results: (1) The determination method of Rg1, Re, Rb1, Syringin, Astragaloside-Ⅳ, Astrganoside and Ginsenoside were stable and reliable. (2) Content of ATGs, Astrganoside and Ginsenoside in extracts were about 13%, 54% and 89% respectively. (3) The optimal formulation and preparing process of Aidi Aidi lyophilized powder for injection were as follows: injection solution treated with 0.2% activated carbon at 80oC for 30 min, sterilization at 115oC for 30min, and using 8%mannitol and NaCl (4:1) as cryoprotectant. (4) The results of safety assessment indicated that the hypersensitiveness, haemolyticus, muscle and blood vessel stimulation of rabbits were all negative. (5) After intravenous administration, the elimination half-life of ginsenoside Rg1, Re and Astragaloside-Ⅳwas 0.882, 0.787, 1.384 h and MRT was 1.273, 1.136, 2.011 h respectively, and Vapp was 0.224, 0.161, 0.257 L·kg^-1, respectively. Conclusion: The preparation method of Aidi lyophilized powder for injection is successfully established, and satisfied safety results are attaineded by preliminary approaches. The results pharmacokinetic test of Aidi lyophilized powder for injection in rats afterⅳadministration will provide potential bases for its further research and development.