The Preparation And Study Of Oral Premicelle Albendazole

Objective:The purpose of research is to prepare a new premicelle albendazole formulation for the improvement of bioavalibility and delivery targets,and to lay a foundation of the researching methods and application of premicelle albendazole formulation.Methods:(1) Special dissolution,dissolubility in some kinds of solvent,oil/water distribution coefficient,ionization constants of albendazole were obtained through experiments to provide the basis of prescription and process design.(2) Entrapment rate and particle sizes were chose as index and orthogonal design was used to process prescription screening that include two factors:①the ratio of drug and solvent②the ratio of drug and surfactant.(3) Established of determining HPLC method for measuring content of premicelle albendazole formulation.(4)Investigated the physics and chemical character of premicelle albendazole that before and after hydration.(5) Factors experiment,Accelerated testing,and Long-term tests processed.(6) Albendazole tablets powder were chose as control and we investigated the pharmacokinetics in vivo of premicelle albendazole through animal experiments.Results:(1) Special dissolution,dissolubility in 18 kinds of solvent,oil/water distribution coefficient,ionization constants of albendazole were obtained through experiments.(2) Established the prescription of premicelle albendazole(abendazole: lactic acid:tween 80=1:3:1 mass ratio) through orthogonal design and considering entrapped percentage,particle sizes and the drug loading.(3) HPLC method was used to determine the concentration of premicelle albendazole formulation,and there was a good linearity within the range of 4-40μg/ml.(4) The entrapped percentage of premicelle albendazole was 81.22%,particle sizes is less than 1μm.(5) Stability experiment showed that high temperature,high humidity and light will take an effect on premicelle albendazole formulation,especially high humidity.Thus this formulation should be preserved in the place that protected high temperature,high humidity and light,and in this circumstance the formulation could be stabilized.(6) Animal experiment showed that the bioavalibility of premicelle albendazole was higher than that of abendazole tablets(relative bioavalibility F=230.45%).Conclusion:(1) The composition of formulation is reasonable because of its high entrapped percentage and easier preparing procession.As research of a new formulation, the objective was accomplished although its stability is not perfect.(2) The premicelle albendazole formulation showed higher bioavalibility after oral administration.