ABSTRACT
Objective: To prepare Puerariae Radix Flavones Dropping Pills and to investigate the dissolution. Methods: Exterior quality, weight variation, and resolving time were used as comprehendsive evaluation indicators to select dropping conditions by orthogonal design. HPLC was used to determine the content of puerarin and rotating basket method was used to determine the dissolution rate in vitro of the dropping pills and tablets. Results: The optimal preparation conditions for the pills were as follows: proportion of drug and matrix was 1:3, drop rate was 20 d/min, the temperature of drug fluids was 80°C, the condensate tube outlet temperature was 50°C, dimethylsilicone was the refrigerant at the temperature of 10°C and 6 cm distance above liquid level. The content of peurarin in the dropping pills was 5.542 mg/g. The accumulated dissolution rate of puerarin in the dropping pills reached 98.81% in 20 min, while the accumulated dissolution rate of puerarin in tablets was only 10.70% in 20 min. Conclusion: The preparation process and HPLC determination method are simple, stable, and feasible. The dissolution rate of puerarin can be improved in the Dropping pills.
ABSTRACT
BACKGROUND: If erythromycin is micronized into microspheres with suitable particle size, it can improve pulmonary drug concentration to maximize its effectiveness and minimize the adverse side effects. AIM: In this study, erythromycin gelatin microspheres (EM-GMS) were prepared and some characteristics of EM-GMS were investigated. The drug-targeting index (DTI) of EM-GMS was evaluated to predict their potential as a targeted delivery system. METHOD: Erythromycin was microencapsulated with gelatin by a double emulsion solvent evaporation method. Some characteristics of EM-GMS, including morphology, particle size, in vitro release, and safety were researched. RESULTS: EM-GMS had a spherical shape and smooth surface morphology. The drug loading and encapsulation efficiency of EM-GMS were 13.56 +/- 0.25% and 55.82 +/- 2.23%, respectively. The release of erythromycin from EM-GMS showed an initial burst and following a sustained release, with an accumulate release of 80% at 4 hours. The EM-GMS was safe since there was no vein irritation and no hemolysis on the erythrocyte of rabbit at 3.5 mg/mL and a LD50 of 173.07 mg/kg. After administering EM-GMS to rabbits, the concentration of erythromycin in lung was 15.92 times higher than that in plasma and the DTI of EM-GMS in lung was 6.65 as compared with erythromycin lactobionate. CONCLUSIONS: The preparation technology of EM-GMS for lung targeting was successful and the quality of microspheres was good.
