ABSTRACT
OBJECTIVE: To prepare starch microspheres of diclofenac sodium by inverse crosslink emulsification method. METHODS: Mean particle size and encapsulation efficiency of starch microspheres were used as indicators, single factor and orthogonal design methods were performed for optimizing preparation process and formulations of starch microspheres. The appearance and structure of the microspheres were researched by optical microscope, transmission electron microscope, infrared spectroscopy and differential thermal analyzer. In vitro drug release behavior was investigated by dialysis method. RESULTS The preparation conditions optimized by orthogonal design; the concentration of starch 10%, crosslinking temperature 55℃, dosage of cross-linking agent 0.2 g, the volume ratio of oil phase and water 5:1, amount of emulsifier 5 mL, cross-linking time 60 min. Starch microsphere obtained by above condition has an average particle size of 9 μm, appearance is irregular spherical shape, and encapsulation efficiency was 67.52%. Results of IR spectra and DTA curves showed that starch cross-links have happened. CONCLUSION In vitro releasing curve showed that the diclofenac sodium starch microspheres have good sustain release effect, drug release complies with the Weibull equation.
ABSTRACT
OBJECTIVE: To prepare coenzyme Q10-γ-cyclodextrin nano-crystal suspension using high pressure homogeneous combining freeze-drying method, optimize the preparation technology, and evaluate the quality of the product. METHODS: Encapsulation efficiency and mean particle size of inclusion complex were used as indicators, and response surface method was performed for optimizing preparation process and formulations. The stability and transdermal performance in vitro of the inclusion complexes were investigated. RESULTS: The optimal technical parameters were as follows; the mass ratio of γ-cyclodextrin and drug, 7.76:1; ultrasonic temperature, 40℃; ultrasonic time, 28.33 min; homogeneous pressure, 40 MPa. Under such conditons, an average encapsulation efficiency of 48.39% and average particle size of 324 nm were obtained for the nano-crystal suspension. The transdermal experiment in vitro showed that the infiltration rate of inclusion was 5.68 μg·cm-2·h-1. CONCLUSION: The preparation method is simple and feasible. The product quality is stable. Moreover, it is easy to manufacture.
ABSTRACT
OBJECTIVE: To investigate the O/W submicron emulsion injection formulation, and investigate its pharmacokinetics in the rat. METHODS: Pseudo-ternary phase diagrams were established using the water titration method. The effects of different surfactants, cosurfactants and Km values on the phase diagram were investigated, and the prescription of submicron emulsion formulation was optimized. Stability of coenzyme Q10 submicron emulsion was evaluated, and the pharmacokinetics in the rat after intravenous injection was study. RESULTS: Coenzyme Q10 submicron emulsion consisting of Poloxamer188/Lipoid S100/ethanol/PEG400/water has the lower viscosity, the smaller size and the higher encapsulation efficiency. An obvious sustained-release effect of coenzyme Q10 submicron emulsion was observed after iv injection in the pharmacokinetics experiment, and mean residence time is 6. 55 h. CONCLUSION: The optimized coenzyme Q10 submicron emulsion consumes smaller quantities of auxiliary materials and shows good stability. Moreover, it is easy to manufacture and convenient for clinical use. Copyright 2012 by the Chinese Pharmaceutical Association.